Nigerian Journal of Pharmaceutical Research
The Nigerian Journal of Pharmaceutical Research publishes scientific work in all areas of Pharmaceutical and life sciences, including (but not restricted to): medicinal plant research; herbal medicines and cosmetics; development of drugs and pharmaceuticals; quality assurance of drugs; safety and efficacy of drugs; pharmacy practice; veterinary pharmacy. The Nigerian Journal of Pharmaceutical Research is published twice yearly by the Nigeria Association of Pharmacists in Academia
Nigeria Association of Pharmacists in Academia
ANALYSIS OF ANTIBIOTIC AND HEAVY METAL RESIDUES IN CLARIAS GARIEPINUS (AFRICAN CATFISH)
Background: Pharmaceuticals, including antibiotics and heavy metals, are emerging contaminants in many African countries affecting all facets of life as a result of indiscriminate disposal. Objectives: This study evaluates the presence and potential health risks of pharmaceuticals in catfish from western Nigeria. Material and Methods: Ten Fish samples were collected from local markets and aquaculture farms. Antibiotic and heavy metal residues were analysed using solid-phase extraction (SPE) and high-performance liquid chromatography (HPLC) and Inductively Coupled Plasma Optical Emission Spectroscopy (ICP-OES) respectively. Results: Seven antibiotics were tested: Trimethoprim (TM), Tetracycline (TC), Ciprofloxacin (CP), Sulfamethoxazole (SZ), Enrofloxacin (EN), Metronidazole (MT), and Ampicillin (AP). TM, TC, CP, SZ, EN, and AP were detected. TC was found at 0.2 µg/g, exceeding the maximum residue limits (MRLs). CP, SZ, EN, and AP averaged 0.1 µg/g, also above MRLs. TM was below MRLs at 0.05 µg/g, and MT was absent in all samples. On the other hand, the levels of Iron, Zinc, and Chromium present in all samples ranged from 6.0196 to 846.8667 mg/kg, 0.3985 to 579.4926 mg/kg and 0.2336 to 18.8947 mg/kg respectively, well above the EU’s maximum safe level of 5 mg/kg. Arsenic, Manganese Copper, Cobalt, Arsenic have concentrations below the maximum safe level. All samples were Lead (Pb)-free which conforms to the EU specification. Conclusion: The findings confirm that antibiotics and heavy metals are significant contaminants in catfish. This highlights the urgent need for legislation to control pharmaceutical waste, regulate antibiotic use in aquaculture, and implement stringent screening and monitoring measures to safeguard public and aquatic life.
(c) Copyright Nigerian Journal of Pharmaceutical Research 2025 https://creativecommons.org/licenses/by-nc-nd/4.0
EVALUATION OF FORMULATED HERBAL LOZENGES OF PAVETTA CRASSIPES AND ANOGEISSUS LEIOCARPUS LEAF EXTRACTS FOR TREATMENT OF COUGH
Background: Medicinal plants are a vital healthcare component, particularly in regions where access to conventional medicine is limited. The study aims is to formulate lozenges containing dried hydro-alcohol extracts of leaves of Pavetta crassipes and Anogeissus leiocarpus and evaluate their physico-mechanical properties, antimicrobial efficacy and cough-suppressing ability in laboratory mice. Methods: Hydro-alcoholic extracts of the plants were evaluated for their pharmacological efficacy using ammonia-induced cough model in albino mice, antimicrobial susceptibility testing against selected microorganism and acute toxicity. Four batches of hard lozenges containing 0 % extract, 10 % of either extract and combination of both extracts at 5 % each were prepared and labelled L1, L2, L3, L4 respectively. The lozenges were evaluated for physico-mechanical properties. Pharmacological efficacy of the lozenges in cough suppression was determined in albino mice. Antimicrobial susceptibility of the lozenges was also evaluated against selected micro-organisms. Results: The lozenges had characteristic odor, sticky texture, and moderately sweet to moderately bitter taste. All the batches had uniform weights ranging between 1.43 and 1.68 g, hardness was between 15.98 and 25.24 kgF and friability was < 1 %. Moisture content was low (0.79 and 1.10 %) and dissolution time was between 9- and 11-min. Antimicrobial susceptibility was more significant with formulations L2 and L4 while cough suppression effect was most significant with L4 (88.61 %). Conclusion: This study presents a promising natural alternative for management of cough, potentially reducing the heavy reliance on synthetic drugs and offering a sustainable, culturally integrated approach to healthcare.
LOCAL PRODUCTION OF ACTIVE PHARMACEUTICAL INGREDIENTS (APIS) IN WEST AFRICA: A SURVEY OF STAKEHOLDERS’ PERCEPTION AND VIEWS
Background: The pharmaceutical sector in West Africa is faced by challenges due to limited domestic capacity for production of medicines and heavy reliance on imports. Local pharmaceutical manufacturers face challenges such as high cost of doing business, poor infrastructure, and lack of standardized equipment. This study aims to assess the perception towards local manufacturing of Active Pharmaceutical Ingredients (APIs) in West Africa and explore strategies to improve access to medicines and achieve self-reliance in the region. Methods: A cross-sectional survey was conducted amongst stakeholders that attended a conference targeted at improving local manufacturing of APIs in West Africa. Online and physical data were collected through the use of a validated questionnaire. Retrieved data were analyzed using Statistical Package for Social Sciences version 25. Data were presented in form of tables, frequencies, percentages and chi square analysis was used for inferential statistics. Results: A total of 191 valid responses were received. Close to half (48.2%) of the stakeholders were female, majority of the study participants were between the ages of 18 and 40 years and were educated up to bachelor’s degree level (62.8% and 58.1% respectively). The majority of participants (85.5%) acknowledged significant gaps in access to medicines and essential pharmaceutical commodities in West Africa. Over two-thirds of the respondents (83.3%) believed that West Africa is suitable for cost-effective production of quality medicines and majority of them (83.0%) were willing to patronize locally manufactured APIs. Conclusion: Findings from this study identifies significant gaps with access to medicines and essential pharmaceutical commodities in the region and suggests the need for more strategic investments and policy action towards the promotion of local API production in the region.
BIOCHEMICAL AND HISTOPATHOLOGICAL EVIDENCE OF METRONIDAZOLE-INDUCED NEUROTOXICITY IN RATS
Background: Metronidazole-induced neurotoxicity is a recurring challenge in pharmacotherapy of susceptible infections, however pathological evidence and biomolecular involvement needs unravelling. Objectives: this study aims to gather neuropathologic evidence and determine biomolecular involvement in metronidazole-induced neurotoxicity. Methods: Twenty rats were assigned to 2 groups (n=10). Group 1 was given 5 mL/kg 0.5% Tween-80®, group 2 received 50 mg/kg metronidazole. The treatments were administered via oral gavage on a daily basis. On the fifteenth day, 5 rats from each group were sacrificed under halothane anesthesia, blood and the brains were excised for toxicological analysis. The remaining animals were treated for 28 days and euthanized on the 29th day and the same parameters assessed. Results: Histological distortions and hemorrhage occurred in the granular layer, loss of Purkinje fibres and congestion were seen in the Purkinje layer and over expression of neuron specific enolase occurred in the cerebellum of metronidazole treated rats. Reduced superoxide dismutase activity, increased malondialdehyde (brain homogenate) and reduced serum brain derived neurotrophic factor concentrations were recorded in metronidazole treated rats. Conclusion: Histological distortions in the granular and Purkinje layers of the cerebellar cortex, increased oxidative stress and reduced BDNF concentrations in treated rats are manifestations of metronidazole-induced neurotoxicity.
Sub-Acute Toxicity Studies of Methanol Root Bark Extract of Azanza Garckeana (F Hoffm.) Exell And Hillc. in Rats
Background: Plants are widely used for various medicinal purposes without careful consideration of potential adverse effects on the system. The fruit of Azanza garckeana is eaten as food, while the other parts are shown to have different medicinal uses and serve as treatments in managing several diseases and ailments throughout its geographical coverage. The study is a necessary/relevant addition in the ongoing efforts to increase awareness about the potential dangers of Azanza garckeana that is presently in use for multiple purposes without prior toxicity studies. Objectives: This study aimed to determine the sub-acute toxicity of the methanol root bark extract of A. garckeana (MEAG). Methods: The Organization for Economic Co-operation and Development (OECD) test guidelines (TG) 425 and 407 were followed for conducting acute oral toxicity and sub-acute toxicity study of MEAG, respectively. Results: In the overall acute toxicity test carried out on MEAG, there were no observed signs and symptoms of toxicity, morbidity or mortality and the LD50 was estimated to be greater than 5000 mg/kg in the oral route of administration. Sub-acute toxicity study, revealed a significant increase (p<0.05) in direct (conjugated) bilirubin at 400 and 800 mg/kg as well as in serum urea at 200 and 400 mg/kg in the MEAG treated groups respectively when compared to the control group. Also, histology of the rats’ organs such as liver, kidney, brain and the heart revealed some level of tissue damage such as, moderate hepatic and slight periportal necrosis, slight glomerular necrosis, as well as slight neuronal necrosis and slight myocardial necrosis, respectively. Conclusion: Prolonged administration of methanol root bark extract of Azanza garckeana appears to be toxic to Wistar rats.
Xylopia parviflora (A. Rich.) Benth. Ameliorates Ketamine-Induced Positive, Negative, and Cognitive Symptoms of Psychosis through Down-regulation of Neuro-oxidative Damage in Mice
Background: Ethno-botanical investigations on Xylopia parviflora (A. Rich.) Benth. revealed its application in the management of neurological disorders, including psychotic conditions. Objective: To evaluate the neuroprotective effects of the hydroethanol leaf extract of Xylopia parviflora (XPE) on the positive, negative, and cognitive manifestations of psychosis in mouse models. . Methods: Thirty mice were allocated into six groups (n=5). Treatments for each group are as follows: distilled water only (10 mL/kg; Grp A), distilled water + ketamine (50 mg/kg; Grp B), the extract (50, 100, and 200 mg/kg; Grps C-E), and haloperidol (5 mg/kg; Grp F). One hour subsequent to the administration of the extract and haloperidol, all groups were administered ketamine (50 mg/kg, i.p.) to induce psychosis. These treatment regimens were repeated over a period of 21 consecutive days. Twenty-four hours following the final treatment, the mice underwent forced swim (FST), open field (OFT), and object recognition tests (ORT), during which relevant parameters were monitored for a duration of five minutes. Thereafter, the animals were euthanized via cervical dislocation, and their brain tissues were harvested for antioxidant analyses. Results: XPE (50-200 mg/kg) diminished the duration of immobility in the FST; enhanced the duration spent with the novel object and reduced the duration spent with the familiar object in the ORT; and diminished the frequency of section crossings in the OFT when compared with the distilled water + ketamine treated group. Furthermore, XPE increased antioxidant biomarkers in the brain. Conclusion: XPE ameliorates ketamine-induced symptoms of psychosis through the attenuation of oxidative stress.
Development of the Cream Formulation of Morinda lucida (Benth) Extracts and Evaluation of its Wound Healing Properties in an Animal Model
Background: Morinda lucida Benth (Rubiaceae) commonly known as brimstone has been used in ethnomedicine for wound healing. However, the presentation of this plant in a conventional dosage form for standard dosing and patient acceptance has not been done. Objectives: This study was designed to formulate the extracts into pharmaceutical cream and investigate its wound healing activity in animal model. Methods: Leaf ethanol (LE), Leaf aqueous (LAQ), stem-bark ethanol (SE) and stem-bark aqueous (SAQ) extracts of M. Lucida were prepared by maceration. Pharmaceutical creams were prepared by standard procedures using 10%w/w extract and assessed by pH, viscosity, extrudability and spreadability. Extracts and creams were evaluated in Wistar rats using incision and excision wound models. For incision, animals were euthanized after 14 days and wound site tissues collected for histology. Excision model was based on wound contraction, closure and epithelialization for 20 days. Results: The creams had acceptable pH, viscosity, extrudability and spreading times. Histology photomicrographs showed that LE, LAQ and 10% LE cream showed dense, well-arranged and well-positioned collagen, with moderate diffuse cellular dermis infiltration compared to controls. All extracts and cream formulations enhanced wound healing compared to their negative controls while leaf ethanol cream showed optimal activity in significantly (<0.05) reducing wound diameter compared to gentamycin as positive control. Conclusion: Morinda lucida extracts and cream formulations demonstrated significant (<0.05) wound-healing activity in-vivo, in comparison with negative controls and can be improved for translational outcomes.
Assessment of Nephroprotective Potentials of Citrus aurantifolia (Christm) Swingle Peels Extract in Gentamicin-Induced Kidney Toxicity in Mice
Background: Peels from Citrus aurantifolia are used in ethnomedicine to cure a variety of illnesses. These extracts have been used traditionally as cold treatments, anti-inflammatory, and antibacterial agents, suggesting that they could be used in contemporary nephroprotective drugs. Objective: The objective of this investigation was to assess the nephroprotective properties of Citrus aurantifolia peels extract (CAPE) in gentamicin-induced kidney toxicity. Method: Dried Citrus aurantifolia peels were extracted with 80% methanol. Thirty mice were randomly assigned to six groups (Groups 1-6, n = 5). Group I received normal saline only (10 mL/kg; baseline), while Groups II, III, IV, V, and VI received gentamicin (100 mg/kg) intraperitoneally to induce kidney toxicity, with concomitant administration of normal saline (10 mL/kg), different doses of CAPE (100, 200, and 400 mg/kg), and ascorbic acid (200 mg/kg), respectively. Treatments were administered orally for 8 days. Twenty-four hours after the final dose, blood samples were collected, allowed to clot, and centrifuged to separate the serum for measuring urea, creatinine, and blood urea nitrogen (BUN). Furthermore, the levels of malondialdehyde (MDA) and glutathione (GSH) in kidney tissue were assessed. Results: The data indicated a decrease in tissue MDA, serum creatinine, urea, and BUN in the CAPE-treated groups. Moreover, the CAPE-treated groups exhibited elevated tissue CAT activity and higher GSH concentrations. Conclusion: The study concluded that CAPE displayed nephroprotective effects, which were possibly mediated via inhibition of oxidative stress.
Assessment of Heavy Metal Content in Erythrina senegalensis and their Human Health Risk Index
Background: The general use of herbal drugs is gaining wide popularity. Part of the quality attributes of a drug is its safety and efficacy, as these are important components of quality assurance in the production and use of drugs. The presence of heavy metals in herbal drugs can have severe health consequences. Therefore, there is need to evaluate the quality of plant materials used for therapeutic and drug development purposes. Objectives: The aim of this study is to determine the level of cadmium, lead, zinc, calcium, magnesium and nickel, and evaluate their health risk index in herbal plant, Erythrina senegalensis. Materials and Methods: The leaves of the plant were obtained from traditional medicine suppliers at the local market of Mushin, Lagos. The plant extract was digested using a mixture of hydrochloric acid and nitric acid in the ratio of 3:1. cadmium, lead, zinc, calcium, magnesium and nickel were determined using Atomic Absorption Spectrophotometer and health risk index was determined. Results: The results obtained showed that cadmium concentration (3.21 mg/kg) was above the permissive limit set by FAO/WHO. The health risk index (HRI) showed that cadmium (8504, 15765) and zinc (62.6617, 167.0977) values in adults and children were respectively greater than 1 which implies that users are considered to be at risk of various health complications that arise from the consumption of heavy metals beyond the required daily intake. Conclusion: This study highlights the concerning levels of cadmium and lead in the herbal plant, which pose potential health risks despite the presence of beneficial minerals like calcium and magnesium; and the presence of nickel and zinc at concentrations below the expected limits. The findings underscore the urgent need for stringent monitoring and regulation of heavy metal content in herbal products to ensure consumer safety.
The Combination Effect of the Active Fractions of Ficus mucuso Welw. Ex Ficalho and Standard Antibiotics against Selected Uropathogens
Background: Urinary tract infections (UTIs) are a global health challenge, causing high mortality rates annually. With rising antimicrobial resistance, the search for effective alternatives has intensified. Medicinal plants serve as substitutes. Ficus mucuso Welw. Ex Fichalo has been purportedly used in ethnomedicine for the treatment of UTIs. Objective: To evaluate the antibacterial effects of Ficus mucuso extract and fractions on UTI isolates and assess synergy with first-line antibiotics. Methods: Pulverized leaves of Ficus mucuso were extracted with methanol by cold maceration. The crude extract was partitioned into n- hexane, ethyl acetate and methanol. Qualitative and quantitative phytochemical screening was carried out. Antioxidant activity of the plant was assessed. Antibiogram of clinical uropathogenic isolates and standard strains was determined using disc-diffusion method. The antimicrobial efficacy of plant extract was tested using agar-well diffusion. Bioassay-guided fractionation of the active fractions was by vacuum liquid chromatography. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values were determined via microbroth dilution assay. Combination antimicrobial testing with ciprofloxacin and amoxicillin-clavulanate was performed using checkerboard assay. Brine-shrimp assay was used to assess cytotoxicity of the plant. Results: The secondary metabolites detected; flavonoids (98.41mg/g), phenols (79.17mg/g) and tannins (27.26mg/g) were more abundant in the ethyl acetate fraction. The plant had appreciable antioxidant activity. Plant extracts and fractions had appreciable inhibitory activities against MDR bacteria with MIC and MBC ranges of 1.5625 to 12.5mg/mL 3.125 and 25mg/mL respectively. Combination testing indicated a synergistic effect with ciprofloxacin. Cytotoxicity assay yielded LC50 value of 31.30 µg/mL. Conclusion: Leaf extracts of Ficus mucuso have antimicrobial potentials which demonstrated enhanced synergistic activity against UTI organisms when combined with standard chemotherapeutics
Cobalt Modulates Healing of Gastric Ulceration in Male Wistar Rats: iNOS/COX-2 Crosstalk
Background: Information on the interplay between gastric iNOS and COX-2 expression by Cobalt (CoCl2) during gastro-protection is unclear. Objective: Cobalt activities on iNOS and COX-2 interplay was investigated using Reserpine (RGU), and Pyloric-ligation (PLGU) gastric ulcer models. Materials and Methods: In RGU, 50 Wistar rats grouped; 1-control, 2-ulcerated untreated (RUU), 3, 4, and 5 were ulcerated pre-treated with 62mg/kg, 25mg/kg CoCl2 and 3.6mg/kg omeprazole for 5 days and sacrificed 3 and 8 hours after reserpine administration. In PLGU, 25 Wistar rats grouped; A-25mg/kg Cocl2, B-62mg/kg Cocl2, C-Cimetidine (36.88mg/kg), D-ulcerated untreated (UU), and E–control, were pretreated for 8 days prior 18 hours pyloric-ligation. Thereafter, macroscopic gastric ulceration (GU), biochemical analysis with histology, and immunohistochemistry were evaluated on excised stomach. Data were expressed as Mean+SEM, and p<0.05 was significant. Results: In RGU model, significant increase in GU score, nitric oxide, lipid peroxidation, and degranulated mast cells but a decrease in sulfhydryl, hydrogen peroxide levels in RUU by 3H and 8H were ameliorated by CoCl2. Histology revealed increased degranulated mast cells in the RUU compared with CoCl2-treated groups. CoCl2 treatment significantly decreased gastric acid secretion, ulcer index, parietal cell count, H+/K+ATPase and Na+/K+ATPase activities compared with UU. Gastric sulfhydryl, mucin, pepsin, with mucous cell count significantly increased in CoCl2-treated groups compared with UU. Gastric iNOS positive reactivity was upregulated while COX-2 positive reactivity was downregulated in CoCl2-treated groups compared with UU . Conclusion: Cobalt chloride exerted gastrointestinal cytoprotective action via mast cell stabilization, mucus production, with modulated expressions of gastric iNOS and COX-2 reactivity at the ulcerated site.
Formulation and Characterization of Stimuli-Responsive In Situ Gel For Treatment of Bacterial Keratitis
Background: The aim of this study is to develop an in-situ gelling system for the effective delivery and sustained-release of levofloxacin in the treatment of anterior corneal infections. Material and Methods: Sodium alginate (SA) and hydroxypropyl methylcellulose (HPMC) were used to formulate in-situ gels (ISGs) with formulation codes F1-F12 and 0.5% levofloxacin solution was used as a control. The formulations were evaluated for clarity, pH, gelling capacity, drug content and antimicrobial activity against Escherichia coli, Pseudomonas aeruginosa, Streptococcus pneumoniae and Staphylococcus aureus using the Kirby-Bauer disk diffusion test. The irritability and toxicity of select formulations were assessed using the Hen’s Egg Test, Chorioallantoic Membrane (HETCAM) assay. Results: The formulated ISGs were within pH range of 5.86 and 7.60. Formulation F7 (0.5% SA + 1.5% HPMC) had the highest gelling capacity and all ISGs had comparable activity against the tested organisms. Formulation F6 (1% HPMC + 1% SA) had the slowest release with approximately 60% release after 4 h, formulation F11 (1.5% HPMC + 2% SA) had the fastest release of 72% after 4 h while LVF solution (control) released 70% in 1 h. There was no significant (p = 0.101) change in the concentration of levofloxacin ISGs after storage at 25o C for 60 days and the HETCAM test confirmed the non-toxicity and non-irritability of the formulations. Conclusions: Levofloxacin in-situ gels formulated with SA and HPMC E5 LV are able to sustain the release of levofloxacin for 8 h and retain their effectiveness against relevant ocular bacterial infections.
Effect of Semi-Synthetic Bases and Hydrophile-Lipophile Balance (HLB) Of Mixed Surfactants on In-Vitro Release Profile of Ibuprofen Suppositories
Background: The emphasis on the use of surfactants in enhancing drug release from fatty suppository bases has always been on the concentration and type of surfactants. However, the Hydrophile-Lipophile Balance (HLB) of the surfactants added, the concentrations and the type of suppository base used have significant effects. Objective: The study aimed to evaluate the effect of HLB of incorporated mixed surfactants, the concentration, and the type of base used on the physical and release properties of Ibuprofen suppository formulations. Methodology: Ibuprofen suppositories (200mg) were prepared using Witepsol® H15, Suppocire® CM, Witepsol® W35, Witepsol® E85 semi-synthetic bases. Mixed surfactants (Span® 80 and Tween® 80) were added at 4 %w/w in varied ratios to give HLB values of 4.3 to 15.0, and at 2 and 6% w/w at optimum HLB. The suppositories' physical properties and release profiles were evaluated using established procedures. Results: The release followed Witepsol® W35>Witepsol® H15>Suppocire® CM>Witepsol® E85. Release from Suppocire® CM and Witepsol® E85 was favored at lipophilic HLB while release from Witepsol® W35 and Witepsol® H15 was favored at hydrophilic HLB. There was a general increase in the release of Ibuprofen with the increase in the concentration of mixed surfactants at the optimum HLBs. The release kinetics were majorly fitted for Higuchi’s kinetic model and followed Fickian and Non-Fickian (anomalous) drug transport mechanisms depending on the HLB of the mixed surfactants. Conclusions: The HLB, concentration of mixed surfactants, and the type of base greatly influenced the variation in the release profile of the Ibuprofen suppository.
Biofilm Inhibitory Activity of Nauclea latifolia, Ocimum gratissimum and Garcinia kola Extracts Against Enteroaggregative Escherichia coli
Background: Enteroaggregative Escherichia coli (EAEC), a biofilm-forming E. coli pathotype, is recognized as one of foremost causes of diarrhea in children under five years old, traveller’s diarrhea and persistent diarrhea. Biofilm complicates treatment as it enhances the pathogen’s ability to undermine host immune responses, often resulting in emergence of resistant mutant. Objectives: In search for potential therapeutic leads against EAEC with less selection pressure, the study was designed to investigate selected medicinal plants for biofilm inhibitory activity against EAEC. Material and Methods: Pulverised dry plant materials of Nauclea latifolia (leaf), Ocimum gratissimum (leaf) and Garcinia kola (seed) were macerated in acetone for 24 hrs. The supernatants were concentrated at reduced pressure and dried in vacuo. Thereafter, varying concentrations (0.31-5.0 mg/mL) of the extracts were evaluated for growth and biofilm inhibitory activities against EAEC 042 strain using the crystal violet-based biofilm assay method. Biofilm inhibitory data were analysed using 2-way ANOVA, while the most bioactive of the extracts was profiled by phytochemical analysis. Results: Nauclea latifolia reproducibly inhibited biofilm formation by greater than 30% (defined biofilm inhibition cut-off) while inhibiting growth by under 10% (defined growth inhibition cut-off). The other two plants showed relatively weak biofilm inhibitory activities. Phytochemical evaluation revealed the presence of alkaloids, tannins, steroids, saponins, flavonoids, and cardiac glycosides. Conclusions: Nauclea latifolia exhibited good biofilm inhibitory activity against EAEC 042 strain with less selection pressure. The plant represents a potential source of novel antibiofilm compounds against enteroaggregative E. coli.
Impact Of Learning Management System In Pharmacy Education In Selected Universities In Southern Nigeria And Contributing Factors
Introduction: Information and communication technologies (ICT) continue to impact the learning landscape all over the world, particularly the use of learning management system (LMS.). The study assessed the impact of Learning Management System (LMS) in pharmacy education and explored factors influencing its adoption for learning in selected Universities in Southern Nigeria. Method: The study samples consist of 66 pharmacy lecturers and 779 undergraduate pharmacy students, drawn from four universities, by employing a multistage sampling method and primary data sources. The instruments employed were two sets of questionnaires, one for each of the lecturers and students. Collected data were summarised using descriptive statistics including frequencies, percentages, weighted averages (WA) and medians while inferential statistics namely independent samples t-tests and analysis of variance (ANOVA) were employed in answering research questions about variables at 5% level of significance. Results: The results show that the impacts of LMS in pharmacy education include improving educational outcome, for lecturers (80.8%; WA 2.7) and for students (55.5%; WA 2.2); promoting collaborative learning, for lecturers (76.9%; WA = 2.7), and among students (59.2%, WA 2.4) and promoting students’ independent learning, for lecturers (92.3%; WA 3.0) and for students (68.3%; WA 2.6)). Factors reported as important in adoption of LMS technology are institutional support for technology tools (84.9%, WA = 3.7), electricity availability (93.9%, WA = 3.8), price of technology (62.1%; WA = 3.4) and internet access (87.9%, WA=3.7). Conclusion: The study concludes that the impact of LMS technology in pharmacy education include promoting student’s independent learning, improving educational outcomes and promotion of collaborative learning among students; while the most important factors facilitating the adoption of technology for learning were electricity, availability of internet connectivity and institutional support for technology use.
Physicochemical and Lipid Peroxidation Evaluation of Fabricated Extract from Securidica longipedunculata Root Bark
Background: Modification of some crude extracts have improved the stability, functional properties and process ability of their bioactive. Objective: To fabricate bioactive from Securidica longipedunculata root bark and compare its activities with the crude extract. Methods: Modified extract was fabricated from Securidica longipedunculata root bark using microencapsulation and freeze drying technique, and evaluated. Results: Fourier Transform Infrared Spectroscopy evaluation showed similar leading peaks in the crude and fabricated extracts, indicating absence of chemical alteration from modification. Energy-Dispersive X-ray (EDX) of the fabricated extract revealed no new detectable element from the EDX of the crude extract, indicating chemical similarities in the crude and fabricated extracts. Scanning Electron Microscopy (SEM) of crude extract revealed flatbed surface with no observed particles, while SEM of fabricated extract revealed distinct, larger and sharp edged particles, indicating structural changes from modification. In comparison to crude extract, fabricated extract showed controlled dissolution, starting with lower dissolution over 30 min, on to higher dissolution after 45 min. At 20 – 100 mcg / ml actives, Vitamin E showed 60 – 80 % lipid peroxidation, while crude and fabricated extracts both showed 12 – 20 % lipid peroxidation, indicating that modification did not significantly alter the antioxidant efficacy of Securidaca longipedunculata crude extract material. Conclusion: The physicochemical and biological properties of fabricated Securidaca longipedunculata root bark extract showed promise in fast delivery of bioactive. There is need for further in vivo studies to ascertain the therapeutic potential of this fabricated form.
FORMULATION AND EVALUATION OF NATURAL BASED COSMECEUTICAL OINTMENTS: AN APPROACH TO MANAGE DRY SCALP DANDRUFF
Background and objectives: Pityriasis capitis, commonly known as dandruff, is a prevalent, chronic scalp ailment that affects over half of the world's population. Dry scalp dandruff is a type of dandruff. Ointments are a good example of a pharmacological formulation that have emollient effects on the scalp and hair. Thus, this study aimed at formulating cosmeceutical herbal ointment as an approach to managing dry scalp dandruff disorder. Methods: Phytochemical screening of Amla (Phyllanthus emblica Linn.) powder and Avocado (Persea americana Mill.) oil was carried out. The ointments were formulated using shea butter as base. Physicochemical, cosmeceutical (conditioning) evaluations, draize skin irritancy test, and stability studies were also carried out. Results: The natural-based ointment formulations, had good organoleptic properties and a pH range of 4.8-7.4. Viscosity was in the range of 20433 to 28007 cp. Spreadability was in the range of 28.49 to 85.24 g.cm/sec. Loss on drying was in the range of 1.77 to 6.73 %. Globule size was in the range of 0.2 – 2.0 µm. The cosmeceutical or conditioning evaluation showed the average score for shine /oiliness, softness and washability to be 2.6 to 4.6, 2.6 to 3.6 and 3.0 respectively. Skin irritancy showed that there was no inflammation, oedema and erythema observed. The formulations exhibited stability in terms of colour, smell, texture and there was no syneresis observed, but there was a difference in the pH of all the formulations. Conclusion: This study has shown that natural based cosmeceutical herbal ointment can be used in managing dry scalp dandruff disorder through its conditioning activities.
A CROSS SECTIONAL SURVEY OF THE PREVALENCE OF INSOMNIA AND ASSOCIATED SOCIODEMOGRAPHICS AMONG AMBULATORY ADULT PATIENTS IN A NIGERIAN TEACHING HOSPITAL
Background: Insomnia is a mental health condition that affects an estimated one-third of the global population. The disorder can impact the social and economic activities of the sufferers. In sub-Saharan Africa including Nigeria, the magnitude of, and the socio-demographics associated with insomnia is rarely known. Objective: This study aimed to determine the prevalence of insomnia and the associated socio-demographics among ambulatory patients in Nigeria. Methods: This was a quantitative cross-sectional survey among consecutively sampled ambulatory adult patients aged 18 years and above at the General Outpatient clinics of the Olabisi Onabanjo University Teaching Hospital, Sagamu, Southwest Nigeria between January and June 2023. A 35-item structured questionnaire sectioned into three segments was used to evaluate the sociodemographic (section A), the medical and family history, and the living conditions of the respondents (Section B). Section C used the Athens Insomnia Scale (AIS) to evaluate insomnia. A Pearson Chi-square test was used to explore the association between insomnia and the socio-demographics of the respondents. A p-value <0.05 was considered statistically significant. Results: Of the 469 respondents, 127 (27.1%) were aged >65 years (mean age= 44.3±13.21 years), 299 (63.8%) were females and 198 (42.2%) had insomnia. Slightly above half of the respondents (52.6%) who had a family history of sleep disorder had insomnia in this study. Marital status (p=0.012), living arrangements (p=0.001), educational qualification (p=0.003) and the number of children in the family (p=0.007) were significantly associated with insomnia in this study. Conclusion: Insomnia is common among ambulatory adult patients in OOUTH, Sagamu Nigeria. Certain sociodemographic factors including living arrangements, educational qualification, number of children in the family and marital status are associated with insomnia in this population.
Physico-Mechanical and Tableting Properties of Metronidazole Obtained by Crystallo Co-Agglomeration Technique
Background: Due to its simplicity and cost-effectiveness, direct compression has become the approach most frequently used to create tablet. Nonetheless, the active pharmaceutical ingredient should have acceptable flow and good compaction qualities in order to use direct compression in tablet manufacture. Crystallo co-agglomeration (CCA) technique has shown to be efficient in improving the earliest stages of tablet manufacture. By combining crystallization (primary particles design) and agglomeration (secondary particles design), it increases the product’s added value. Objectives: This study exploits the CCA approach to boost the physico-mechanical and tableting properties of metronidazole tablet. Methods: Metronidazole co-agglomerates was formulated with hydrophilic polymers using CCA technique. The dilution potential of the produced agglomerates was assessed to obtain suitable concentration that was used to prepare metronidazole tablet by direct compression method after which the tablet properties were evaluated. Results: Metronidazole agglomerate powder had a very good flow rate and angle of repose, low bulk and tapped densities as well as improved Carr’s compressibility index, 15.00±0.14% and Hausner’s ratio 1.18±0.03 compared to pure metronidazole (27.54±0.14% and 1.38±0.04 respectively). The CSFR/Dt ratio for batches F3 and F4 showed higher compactability and functionality. The dissolution profiles of batches F3 and F4 of metronidazole exhibited improved dissolution behaviour than pure drug containing batches (batches F1 and F2). Conclusion: The CCA technique yielded metronidazole with increased particle size and compactability resulting in excellent flowability and packability due to reduced inter-particulate friction, which exhibited improved compressibility, dilution potential, disintegration and dissolution rate.
(c) Copyright Nigerian Journal of Pharmaceutical Research 2024 https://creativecommons.org/licenses/by-nc-nd/4.0
Antibacterial, Antibiofilm Activities and Toxicity of Uvaria chamae P. Beauv (Annonaceae)
Background: Bacteria biofilms are a serious global health concern. The rapid increase of antimicrobial resistance in diarrheagenic bacteria due to biofilm formation has limited the clinical usefulness of some antibiotics in circulation. Objectives: Uvaria chamae has shown broad spectrum antibacterial activity, hence the need to study its antibiofilm activity against enteroaggregative Escherichia coli (EAEC) strains implicated in paediatric diarrhoea. Methods: Samples of authenticated U. chamae root, stem and leaf were collected, air-dried, ground and extracted by cold maceration in dichloromethane and methanol separately. The EAEC strains tested were; O42, DH5α, MN5DE, D25D and D28I. The plant extracts were subjected to quantitative and qualitative phytochemical screening and the 50% lethality (LC50) brine shrimp assay carried out. Extracts were screened for antibacterial activity using agar diffusion method, while agar dilution and broth dilution methods were used to determine minimum inhibitory and bactericidal concentrations, respectively. Biofilm inhibition of the active extracts was investigated by crystal violet method. Results: All the EAEC strains were multi-drug resistant, but susceptible to gentamicin and azithromycin. Dichloromethane leaf extract (DLE) and methanol leaf extract (MLE) inhibited the growth of the tested EAEC strains with the MIC of MLE D28I being MIC 3.75 mg/mL. The percentage biofilm inhibition by MLE against EAEC strains O42, MND5E and D25D were 72%, 74.5%, and 63%, respectively. Alkaloids were the most abundant in the methanol leaf extract of U. chamae (MLE). The extracts had LC50 >1000 μg/mL. Conclusion: Uvaria chamae is non-toxic and possesses antibiofilm potential that could be further developed as a natural remedy for diarrhoea.
Antifungal Activity of Alchornea cordifolia and Ficus exasperata Leaves Against Trichophyton mentagrophyte and Trichophyton verrucosum
Background: The use of plant based natural products as alternative remedy for mycosis has gained global prominence, hence the need to explore the antifungal potentials of readily available herbs. Aim: To compare the antifungal activity of the ethanol leaf extracts of Alchornea cordifolia and Ficus exasperata against Trichophyton mentagrophyte and Trichophyton verrucosum with that of conventional griseofulvin. Method: Plant samples were extracted with ethanol via maceration. Phytochemical screening was carried out using standard techniques. The ethanol extract of the fresh and dried leaves of Ficus exasperata and Alchornea cordifolia were compared with griseofulvin (0.03mg/ml) for activity against Trichophyton mentagrophyte and Trichophyton verrucosum using agar well diffusion method at varying concentrations. Results: Both crude drugs contains flavonoids, saponins, tannins, and cardiac glycosides. Ficus exasperata extracts also contains phlobatannin and terpene. The extracts exhibited a dose dependent fungal inhibition. The highest concentration (150mg/ml) of A. cordifolia and F. exasperata extracts exerted the highest zones of inhibition (16.7mm, 19.3mm, and 19.00mm, 19.7mm, respectively) against T. mentagrophyte. The zones of inhibition of the test drugs against T. verrucosum were 20mm, 19.3mm, and 21.3mm, 24.7mm, respectively. The least mean zone of inhibition was observed at 25mg/ml. Minimum inhibitory concentration (MIC) of 50mg/ml was obtained for Alchornea cordifolia fresh and dried leaves and Ficus exasperata dried leaves while minimum inhibitory concentration of 25mg/ml was obtained for the Ficus exasperata (fresh) leaves. Conclusion: These results clearly elucidates the potentials of fresh and dry extracts of A. cordifolia and F. exasperata as a good source of antifungal compounds.
Effect of Hibiscus Sabdariffa (Linn) Water Extract on the Pharmacokinetics of Lisinopril in Healthy Human Volunteers
Background: The concurrent use of Hibiscus sabdariffa and drugs for the treatment of various ailments is a common practice amongst patients; a practice that could result in drug-herb interaction. Objective: To evaluate the effects of Hibiscus sabdariffa water extract on the pharmacokinetics of lisinopril. Methodology: The study involved 24 apparently healthy humans randomly selected and divided into two groups of 12 each. Study was carried out in four phases as crossover study with a washout period of two weeks between the phases; Group 1 (received lisinopril 10 mg alone), group 2 (received lisinopril 10 mg with 200 mL Hibiscus sabdariffa calyxes water extract (25 mg/mL) concurrently), group 2 (received lisinopril 30 min after administration of Hibiscus sabdariffa water extract) and group 1 (received Hibiscus sabdariffa water extract 30 minutes after administration of lisinopril). Saliva samples collected at 0.5 to 36.0 hr in each phase were analysed for lisinopril content using a developed and validated RP-HPLC method. Results were analysed using one-way Anova followed by Tukey’s post Hoc. Results: Lisinopril administered alone (group 1) achieved Cmax of 95.36 ng/mL at 7 hr (Tmax). Slight increases in Cmax of lisinopril were observed when the drug was interacted with Hibiscus sabdariffa in groups 2 (97.50 ng/mL), 3 (97.37 ng/mL) and 4 (99.24 ng/mL) respectively. The of lisinopril alone was 736805.83 ng.hr/mL. The corresponding for group 2, 3 and 4 are 800409.29, 816866.47, and 10450.03 ng.hr/mL respectively. However, these increases in Cmax and seen were not statistically significant (p < 0.05). Pharmacokinetic parameters were computed using Kinetica software. Conclusion: Hibiscus sabdariffa calyxes water extract (200 mL of 25 mg/mL) does not significantly affect the pharmacokinetics of lisinopril in healthy humans.
In Silico Identification of Canthin-6-one as a Pancreatic Lipase Inhibitory Anti-Obesity Drug Lead from Hibiscus Sabdariffa
Background: The therapeutic use of the only Pancreatic Lipase (PL) - inhibiting anti-obesity drug available in clinical practice, orlistat, is bedevilled with unbearable side effects, necessitating the discovery of new and better-tolerated ones. Hibiscus sabdariffa, a folkloric anti-obesity plant is a plausible repertoire from which such agents could be sought. Objective: The main objective of this work was to evaluate in silico the phytochemicals of Hibiscus sabdariffa for a possible identification of potential leads for PL inhibitory anti-obesity drug discovery.. Methods: Phytoligands from H. sabdariffa were subjected to a series of in silico evaluations including site directed docking, MM/GBSA calculations, SwissADME drug-likeness screening, Protox II-based toxicity evaluations and a 20 ns molecular dynamics (MD) simulation. Results: MM/GBSA ranking of docked phytoligands and SwissADME evaluations produced three PL inhibitor hits. One of them, canthin-6-one, demonstrated minimal end-organ toxicity with a 1200 mg/kg LD50; its PL complex generated stability-implying root mean square deviation (RMSD), root mean square fluctuation (RMSF), radius of gyration (Rg) and solvent accessible surface area (SASA) plots, after the 20 ns MD simulation. Conclusion: Hibiscus sabdariffa-based canthin-6-one has demonstrated, in silico, high human PL binding affinity, impressive drug-likeness/toxicity profiles and stability-implying MD simulation parameters. It is therefore, herein, recommended as lead for further in vitro, in vivo and molecular modification studies for possible development into a clinical PL inhibitory anti-obesity drug.
Phytochemical and Anticonvulsant Activity of the Ethanol Root Bark Extract of Mimosa pigra L. (Fabaceae) in Laboratory Animals
Background and objectives: Various parts of Mimosa pigra (MPG) are used in traditional medicines to treat convulsive disorders. The objective of this study was to investigate the anticonvulsant properties of Mimosa pigra ethanol root extract (EREM). Methods: The acute toxicity of the extract was investigated using OECD 423 protocol of 2002. The anticonvulsant properties of EREM at 200,400 and 800 mg/kg were evaluated using Maximal Electroshock Test (MEST) in chicks; strychnine (SCN-) and pentylenetetrazole (PTZ)-induced seizures in mice. Results: The extract at 400 and 800 mg/kg significantly (p<0.05) prolonged the mean onset of clonic and tonic convulsions in mouse model of SCN-induced seizure. In PTZ-induced seizure, the extract at 400 mg/kg significantly (p<0.05) increased the mean onset of clonic seizure, while at 800 mg/kg, there was significant (p<0.05) prolongation in the mean onset of clonic and tonic seizure compared to control. The extract did not protect the chick against MEST but significantly (p < 0.05) reduced the mean recovery time at the of 200, 400 and 800 mg/kg. The extract offered 60 and 100% protection at 400 and 800 mg/kg respectively in SCN-induced seizure. Similarly, EREM offered 20 and 40% protection at 400 and 800 mg/kg respectively in PTZ-induced seizure. Diazepam (10 mg/kg), a reference drug significantly (p<0.05) prolonged the onset of clonic-tonic seizure and protected against SCN-, and PTZ-induced convulsion in mice. Conclusion: These findings indicated that EREM may possess anticonvulsant activity in SCN-, and PTZ-induced seizure in mice. Thus, lend scientific credence to the anticonvulsant claim of EREM in ethnomedicine.
MAMA Decoction, Nigerian Herbal Antimalarial Preparation, Alters the Disposition of Amodiaquine in Healthy Humans
Background: MAMA Decoction (MD) is prepared from the leaves of Mangifera indica, Alstonia boonei, Morinda lucida and Azadirachta indica. A co-administration of MD with amodiaquine led to synergism in the clearance of malaria parasites in a previous report. The pharmacokinetic basis for this observation was the subject of another study in mice which found significant MD-induced increase in the exposure and half-life of desethylamodiaquine, the major metabolite of amodiaquine. Objective: This study aimed at evaluating previously identified murine herb-drug interactions in healthy human volunteers. Materials and Methods: Single oral doses of amodiaquine (10 mg/kg) with/without MD (120 mg/kg) were co-administered to 16 healthy subjects in a three-period crossover design. Five millilitres of blood samples were collected employing sparse sampling from 0.25, 0.5, 1, 2, 4, 8, 12, 24 and 48 h postdose, for each study period and analysed for amodiaquine and desethylamodiaquine contents. The effect of MD on amodiaquine disposition across study periods was investigated using a non-linear mixed-effect pharmacokinetic model which estimated population parameters with the stochastic approximation expectation maximization algorithm implemented in Monolix 2020R1. Results: The disposition of amodiaquine and desethylamodiaquine was each described, adequately, by two- and one-compartment structural models respectively, and a first-order oral absorption rate. The co-administration of amodiaquine with MD resulted in about 41% decrease in the apparent volume of distribution of amodiaquine (VAQ/F). Pre-administration of MD prior to amodiaquine led to a 22% decrease in VAQ/F. Conclusion: MAMA decoction appeared to decrease the tissue partitioning of amodiaquine in man. The consequence of this on effective parasite clearance in man is, not yet understood.
Effect of Garcinia kola on Atorvastatin Dissolution Profile: An Indication for Possible Drug-Drug Interactions After Oral Administration
Background: Herb-drug interactions are of growing concern due to the widespread use of herbal supplements alongside medications. These interactions can affect therapeutic outcomes. Understanding and identifying specific interactions is crucial for ensuring safe and effective medication use. Objective: This study investigated the impact of Garcinia kola, a common food supplement, on the dissolution of atorvastatin tablets. Methods: The dissolution profiles of atorvastatin tablets were investigated alone and in the presence of varying concentrations of G. Kola by mixing 1, 2, or 4g of G. Kola powder respectively with the dissolution medium. Samplings were performed at predetermined time points (10, 20, 30, 45 and 60 minutes) and the amount of atorvastatin dissolved was measured using a validated HPLC method. Statistical analyses were conducted to assess the significance of the observed differences. Results: The percentages of atorvastatin released in dissolution medium without G. kola were 31.38±11.81, 46.02±8.73, 72.23±33.30, 63.55±27.10, 82.54±31.12% across the sampling time points. Whereas the percentage of drug released were 17.01±7.33, 27.02±8.42, 34.70±13.90, 39.74±13.53, 28.47±11.78% in the presence of 1g G. kola; 12.44±5.89, 11.87±1.51, 23.33±5.18, 27.33±8.50, 52.49±11.66% in the presence of 2g G. kola and 2.28±3.53, 4.94±7.21, 7.26±9.01, 4.68±7.37, 6.86±8.70% in the presence of 4g G. kola. There was a statistically significant difference in the amount of drug dissolved in conditions studied. Conclusion: There was a significant change in the dissolution profile of atorvastatin with increasing concentrations of G. kola. This suggests a need to establish the impact of G. kola on the disposition of atorvastatin in vivo.
Development and Evaluation of Encapsulated Self-Emulsifying Drug Delivery System of Hydrochlorothiazide
Background: Formulation of solid self-emulsifying drug delivery system (Solid SEDDS) provides a dual benefit of improved drug stability and enhanced delivery system. Objective: This study was aimed at developing and evaluating a solid self-emulsifying drug delivery system of hydrochlorothiazide. Methods: Solubility of hydrochlorothiazide in some oils was determined and pseudo-ternary system of the most effective oil, water and surfactant system was constructed. Four Liquid SEDDSs were formulated to contain Tween 80/oleic acid or PEG 400/oleic acid (surfactant systems) and castor oil combined in ratio 2:8 or 3:7 based on the pseudo-ternary plot. Each preparation was made by adding the drug to the oil/surfactant system and heating up to 60 0C under continuous stirring followed by cooling to room temperature. Viscosity of each Liquid SEDDS was determined; Solid SEDDS was prepared by mixing the Liquid SEDDS with microcrystalline cellulose in 1:2 proportion and then encapsulated. Drug release profile of the Solid SEDDSs in comparison with a marketed product was studied. Results: Castor oil was found to be the best solvent for hydrochlorothiazide and the viscosity of the Liquid SEDDSs was in the range of 79.41 and 187.32 mPa.s. The in vitro release studies showed 85.46 – 87.17 % drug release from the formulated SEDDSs with ratio 3:7 of surfactant mix being superior; and percentage drug release for each formulation was twice that of the marketed product. Conclusion: The prepared Solid SEDDS of hydrochlorothiazide exhibited improved drug release characteristics, hence superior to the conventional commercial product.
Assessment of Knowledge, Attitude and Practices of Pharmacy Clients about Antibiotic Use and Misuse in Ogun State, Nigeria
Background: The rise of antimicrobial resistance poses a global health challenge, driven by the widespread misuse of antibiotics. This misuse includes self-medication, sharing of antibiotics and failing to complete prescribed courses. This fosters an environment conducive for antibiotic resistance making future treatment less effective. Objectives: This study aims to evaluate the knowledge, attitudes, and practices (KAP) of antibiotic use/misuse and their influencing factors among pharmacy clients in Ogun State, Nigeria. Methods: A descriptive cross-sectional study was carried out in ten (10) community pharmacies obtained from the list provided by the Association of Community Pharmacists of Nigeria, Ogun State branch, across its five zones in Ogun State, Nigeria. Pre-tested questionnaires adapted from previous studies were used to collect data which was entered into Microsoft Excel 2016 and analyzed using the Statistical Package for Social Sciences (SPSS) version 23.0. Descriptive and inferential statistical analyses were carried out with significance level set at ≤0.05. Results: Good knowledge and practice (KP) scores of pharmacy clients about antibiotic use of 54.5% and 56.2% but poor attitude to antibiotics (60.5%) was documented along with notable misconceptions. Several demographic factors influenced the KP levels including gender (p=0.00027), marital status (p=0.013), religion (p=0.005), and education (p=0.001) for knowledge; and religion (p=0.027) and education (p=0.006) for practices. Conclusion: The study showed that though moderate levels of KP were obtained, there is a need for targeted interventions to improve public awareness about antibiotics and promote responsible use.
Design and Preliminary Characterization of Sweet Potato Starch – Urea-Borate Polymer
Background – Sweet potato (Ipomoea batatas) starch has been reported for its potential as a directly compressible and sustained-release polymer in its native and modified forms. Chemical modification by crosslinking with urea and borax to form starch urea-borate will enhance its drug release-retarding properties. Objective – To design starch-urea-borate (SUB) polymer using sweet potato starch to produce a new, affordable biodegradable polymer, and carry out preliminary characterization of the polymer. Method – Native starch was extracted from sweet potato tubers and crosslinked with urea and borax to form starch-urea borate (SUB) polymer. The native and modified starches were characterized for morphology (SEM), FT-IR, DSC, pH, densities, swelling, flow properties and viscosity. Results – Modification yielded 96.66% w/w of SUB and disrupted the granular structure of the native starch, producing significantly larger (p<0.01) granules with irregular shapes. FTIR spectrum revealed a peak at 3369.05 cm-1 due to –NH2 confirming the presence of a secondary amide resulting from the polymerization reaction between urea and starch in the presence of borate. A shift in the peak of DSC endotherm was observed for SUB. Modification yielded lower particle density but higher bulk and tapped densities. The swelling index increased significantly (p<0.01). Hausner’s ratio (1.06± 0.00), Carr’s index (6.33± 0.01%) and angle of repose (26.14±1.15º) showed good flow but reduction in compressibility of SUB. Viscosity revealed shear thickening or dilatant behaviour. Conclusion- The material and physicochemical properties of SUB polymer showed its potential for application in drug delivery systems, possibly as a release retarding polymer.
Comparative Evaluation of Some Moxifloxacin Hydrochloride Tablet Brands Marketed in Nigeria Using Five Different Validated Analytical Methods
Background: Assay of pharmaceuticals is an important aspect of quality control. It is necessary to compare the bioequivalence of generic brands of the any drug to an innovator/comparator brand as this forms the basis for comparing their therapeutic equivalence. Objective: This study aimed to determine the most accurate method for the assay of moxifloxacin hydrochloride (MOX-HCl) tablet brands in Nigerian markets by using five different validated analytical methods and also verify their interchangeability. Material & Methods: This study involved three brands of MOX-HCl including the comparator brand, Moxiget®. The study involves both quality control tests including: weight uniformity, diameter, thickness, friability, hardness, disintegration, dissolution and content of active ingredient (assay) methods including: phosphate buffered UV-Vis spectrophotometric, UV spectrophotometric, kinetic spectrophotometric, colorimetry and utilization of oxidation-reduction reaction methods. Results: All the samples used for this study passed the quality control tests and thus were of standard quality and therefore pharmaceutically equivalent. Conclusion: This study therefore conclude that phosphate buffered UV-Vis spectrophotometry provide the most accurate method to assay Moxifloxacin tablet, colorimetry assay method can serve as a substitute to the preferred method for the moxifloxacin assay and the three samples assayed in this work are interchangeable with the comparator brand (Moxiget®).