Nigerian Journal of Pharmaceutical Sciences
The Nigerian Journal of Pharmaceutical Sciences publishes original articles and reviews on pharmaceutical and related clinical and basic sciences. It will also serve as a medium for publicizing and communicating the ever growing and changing development in the field of pharmacy practice. The journal will further serve as a medium for continuing Education in Pharmacy. The language of the journal is English. This journal will only consider original articles which have not been published previously or not considered in part or whole for publication elsewhere in the same or any other language. Authors should prepare their manuscripts submitted to the journal exactly according to instruction provided. As a policy the opinion of reviewers with cognate expertise in the subject will be sought before decision is made as to whether the paper should be accepted, rejected or returned to the authors for revision. The journal reserves the exclusive right to make any further changes and language corrections necessary in a manuscript accepted for publication so that it conforms to the requirement of the journal.
Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nigeria
RISK FACTORS ASSOCIATED WITH MULTIDRUG-RESISTANT ESCHERICHIACOLI O157:H7 ISOLATED FROM STOOL SAMPLES OF PATIENTS PRESENTINGWITH GASTROENTERITIS
Enterohaemorrhagic Escherichia coli (EHEC) O157:H7 is a significant aetiological agent of diarrhoeal diseases, causing illnesses ranging from mild diarrhoea to severe conditions such as haemorrhagic colitis and haemolytic uremic syndrome (HUS), which has not been widely documented in Nigeria. This study investigated the prevalence and antibiotic susceptibility patterns of Escherichia coli and E. coli O157:H7, isolated from stool samples of patients attending the Ahmadu Bello University Medical Center in Zaria, Nigeria. A total of 100 stool samples were collected from consenting patients and analyzed using standard microbiological techniques. Identification of isolates was based on cultural, microscopic, and biochemical characteristics. Antibiotic susceptibility testing was performed using the Kirby-Bauer disc diffusion method. Out of the 100 samples, 25% were positive for E. coli. Of these, three were confirmed as E. coli O157:H7, resulting in a prevalence rate of 3% for this strain. Socio-demographic analysis showed a higher infection among patients aged 10–25 years. Although, there was no statistically significant association between the prevalence of the infection and the risk factors assessed in the study (p >0.05), there was increased risk of the infection in patients who kept pets (26.8%;19/71), exposed to livestock and their wastes (26.7%:8/30) and eating of raw vegetables (26.8%;19/71). Antibiotic susceptibility results revealed a high level of resistance to Amoxicillin-Clavulanic acid (95%). These findings emphasize the urgent need for ongoing surveillance of E. coli infections and their resistance profiles to guide effective treatment and public health strategies in the region.
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PHYSICOCHEMICAL CHARACTERIZATION OF HIBISCUS SABDARIFFA L.CALYX MUCILAGE FOR PHARMACEUTICAL APPLICATION
The pharmaceutical formulation industry is increasingly turning to excipients sourced from edible natural products, as these have proven effective in stabilizing, enhancing the solubility, absorption, and bioavailability of Active Pharmaceutical Ingredients (APIs). This study aimed to evaluate the physicochemical properties of mucilage extracted from red and white calyces of Hibiscus sabdariffa Linn for potential pharmaceutical use. The mucilage was extracted from red and white calyces of Hibiscus sabdariffa, and the yield (%) was determined. Subsequent evaluations included the determination of various physicochemical properties, such as particle density, flow properties, swelling capacity, moisture content, moisture sorption capacity, and pH. Other analyses such as FTIR, SEM, and XRD were carried out on both samples. Yields of 10.87% (red) and 9.66% (white) mucilage were obtained. Both samples exhibited acceptable flow properties. The swelling capacity reached 280% and 260% after 24 h and moisture contents were 0.29% and 0.19% for the red and white samples, respectively. The pH measurements were 4.01 (red) and 3.81 (white). FTIR spectroscopy identified functional groups characteristic of polysaccharides. Differences in the 1700–1500 cm⁻¹ range suggested variations in protein or secondary metabolite interactions. SEM analysis revealed that the red sample had a more porous, fibrous texture, while the white sample appeared denser and more compact. XRD analysis confirmed the amorphous nature of both samples. The physicochemical properties of both mucilage especially high swelling capacity of both samples highlight their potential as suitable disintegrants for pharmaceutical applications. Further studies are recommended to evaluate the functional applications of the mucilage because of their good hydration and moisture sorption properties.
COMPUTATIONAL EXPLORATION OF ANNONA SENEGALENSISPHYTOCHEMICALS AS PROMISING ANTIVENIN AGENTS TARGETING SNAKEVENOM ENZYMES
Snakebite envenomation poses a significant public health challenge, particularly in rural developing regions with limited access to effective antivenoms. Annona senegalensis, a plant revered in traditional medicine, is recognized for its potential antivenin properties. This study employs computational chemistry, utilizing tools such as AutoDock Vina, to investigate the phytochemicals of A. senegalensis for their ability to inhibit venom enzymes from Naja species. Twelve phytochemicals were screened using SwissADME for drug-likeness and Protox 3.0 for toxicity profiles. Molecular docking simulations identified three promising candidates; kaempferol (Lig4), caffeic acid (Lig6), and ellagic acid (Lig8) with superior binding affinities to key venom enzymes: Phospholipase A2 (Lig4: - 7.1, Lig6: -7.1, Lig8: -7.4 kcal/mol), Metalloprotease (Lig4: -8.2, Lig6: -7.5, Lig8: -8.6 kcal/mol), and Serine Protease (Lig4: -8.5, Lig6: -6.9, Lig8: -6.9 kcal/mol), which drive venom-induced cytotoxicity and hemorrhage. These findings substantiate the traditional use of A. senegalensis in folk medicine and suggest its phytochemicals could serve as effective, accessible alternatives or complements to conventional antivenin therapies. Further in-vivo studies are recommended to validate these results and explore the therapeutic potential of A. senegalensis phytochemicals in snakebite management.
DETERMINANTS OF HEALTH-RELATED QUALITY OF LIFE (HRQOL) IN ADULTPATIENTS UNDERGOING ANTI-MALARIAL TREATMENT AT A SECONDARYHEALTHCARE FACILITY IN ILORIN, NIGERIA
This study aimed to evaluate the health-related quality of life (HRQoL) and related factors among patients receiving antimalarial treatment at a General hospital Ilorin (GHI). Participants were drawn after a sample size of 291 participants were calculated. An EQ-5D-5L, EQ-VAS instrument was used to collect the data (from July to September 2023). Informed consent was obtained from all participants, and Ethical approval was obtained from Ministry of Health Ethical Research Committee (ERC) and Ethical Review and Research Committee of General Hospital Ilorin (GHI) with assigned number: ERC/MOH/2023/07/130 and GHI/ADM/134/VOL.I/081 respectively. Of the 291 participants included, 182 (62.5%) were female, and 109 (37.5%) were male. Most of the participants were aged 18–24 years (93; 32%), had tertiary education (195; 67%), and had low incomes, earning less than ₦3,000 (126; 43.3%). Also, a significant majority lacked health insurance (211; 72.5%). The most commonly used treatment was Artemether/Lumefantrine (281; 96.6%). The mean EQ-5D utility scores and EQ-VAS scores were 0.74 ±0.152 and 67.17±19.48 respectively. The EQ-5D descriptive system had 11111 as the health state of majority of participants 89(30.6%) followed by 11121 (19)6.5%, both states having utilities of 0.9 and 0.646 respectively. Sixty-three-point six percent of participants had problem in the pain and discomfort domain. The results of multivariate regression analysis showed marital status (p=0.005) and family history (p= 0.004) of any disease correlated with EQ-5D-5L index score (Health state). These variables contributed approximately 58.93% and 41.07% respectively to the EQ-5D index score of patients. The findings indicate that malaria patients in this study generally reported a good health-related quality of life. Most participants experienced minimal problems across domains except for pain/discomfort Socio-demographic factors such as marital status and family history of disease had significant influence on HRQoL, suggesting that social support and underlying health vulnerabilities play crucial roles in patients’ well-being. Overall, malaria’s impact on HRQoL extends beyond clinical symptoms, underscoring the need for patient-centered care that addresses both physical and psychosocial factors.
PHARMACOGNOSTIC PROPERTIES OF CANNABIS SATIVA L. (CANNABACEAE)SAMPLES COLLECTED FROM VARIOUS REGIONS OF NIGERIA
Cannabis sativa (C. sativa) belonging to the family Cannabaceae and commonly referred to as ‘marijuana’, is one of the most used illicit drugs in Nigeria. There is significant level of C. sativa cultivation and trafficking in Nigeria. To date, pharmacognostic properties of C. sativa material confiscated and cultivated in various regions of Nigeria have not been reported. This study aimed to determine the pharmacognostic properties of C. sativa grown in various regions of Nigeria. This study used C. sativa sample of unknown origin confiscated from traffickers in Kaduna State (A) and five samples seized from farms (cultivated) in Kaduna (B), Adamawa (C), Edo (D), Enugu (E) and Ondo (F) States of Nigeria. Standard, validated techniques were used to evaluate pharmacognostic parameters including morphological, organoleptic, microscopic, physical and phytochemical properties of six matured C. sativa samples, comprising leaves and flowering parts. All the six samples conformed to the general characteristics of C. sativa and showed no significant morphological and organoleptic differences. Quantitative microscopy and other physicochemical analyses produced similar results. Phytochemical screening yielded carbohydrate, cardiac glycoside and phenols in all samples. Anthraquinones, flavonoids, tannins and tritepenoids were present in most samples. Saponin was absent in all samples. Colour tests and TLC confirmed the presence of cannabinoids in all samples. Phytochemical profile and TLC fingerprints of the sample confiscated in Kaduna State (A) and that cultivated in Ondo State (F) were very similar, suggesting a common chemical identity of both. This study showed that cannabis grown in various regions of Nigeria shared many important features. The result forms important baseline records for further studies of cannabis confiscated and cultivated in various regions of Nigeria with possible applications in medicine, forensics and law enforcement.
SEIZURE CONTROL STATUS AND ITS PREDICTORS AMONG CHILDREN WITHEPILEPSY IN SOKOTO
Epilepsy comprises a diverse group of neurological disorders affecting approximately 10.5 million children globally and 671,000 in Nigeria. Appropriately selected antiseizure medication (ASM) remains the first-line treatment for its management. This study, therefore, assessed the predictors of good seizure control status among children with epilepsy receiving care at tertiary health facilities in a Northwestern Nigerian state. This study presents a seven-year retrospective review of epilepsy management among patients under 15 years of age who received care at the Paediatric Neurology Clinics of Usmanu Danfodiyo University Teaching Hospital, Sokoto and Federal Neuropsychiatric Hospital, Kware, Sokoto. A total of 2,250 children with epilepsy (CWE) were included in the study. The median (IQR; range) age, age at seizure onset, and epilepsy duration were 9 (5–12; 0.33–14) years, 2 (1– 5; 0.003–13) years, and 5 (2.42–6.58; 0–14) years, respectively. Most participants were males (65.3%), in school (50.7%), without comorbidities (76.9%), triggers (94.2%), or ASM adverse effects (88.0%). ASM monotherapy (91.1%) and adherence (71.1%) were common. Good seizure control occurred in 51.1% of CWE and was predicted by low socioeconomic status (P=0.000, OR=2.166, 95% CI=1.683–2.788), absence of comorbidity (P=0.000, OR=2.428, 95% CI=1.819–3.242), no epilepsy-induced injury (P=0.000, OR=3.324, 95% CI=1.849–5.976), history of status epilepticus (P=0.000, OR=2.345, 95% CI=1.805–3.047), herbal remedy use (P=0.000, OR=3.735, 95% CI=2.841–4.909), and carbamazepine monotherapy (P=0.000, OR=3.816, 95% CI=2.822–5.161). Good seizure control in the study cohort was predicted by carbamazepine monotherapy, low socioeconomic status, history of status epilepticus or herbal remedy use, and absence of comorbidity or epilepsy-induced injury.
MODULATION OF DOLUTEGRAVIR-INDUCED GEOTACTIC DEFICITS INDROSOPHILA MELANOGASTER BY HEXANE EXTRACT OF BRASSICA OLERACEA
This study investigated the protective role of Brassica oleracea against dolutegravir-induced effects on geotactic behavior in Drosophila melanogaster. Conducted at the Africa Center of Excellence in Phytomedicine Research and Development, University of Jos, flies were exposed to varying concentrations of dolutegravir (0.5–4 mg/5 g diet) and B. oleracea extract (7.5–1000 mg/5 g diet) for toxicity (LC50 determination) and behavioral assessments. A fiveday exposure to specific extract doses (50–400 mg/5 g diet) was followed by geotaxis assays and acetylcholinesterase (AChE) activity analysis. B. oleracea extract was non-toxic and improved AChE activity, negative geotaxis and climbing ability in flies exposed to dolutegravir. These results suggest that the hexane extract of B. oleracea has modulatory activity against dolutegravir-induced geotactic deficits in Drosophila melanogaster.
TABLETING POTENTIAL OF CO-PROCESSED STARCH, ALGINIC ACID ANDPOLYVINYL PYRROLIDONE AS DIRECTLY COMPRESSIBLE EXCIPIENT
The goal of the study was to evaluate the functionality of co-processed material containing starch, alginic acid and polyvinyl pyrrolidone in tableting. This was achieved by co-processing maize starch with alginic acid and polyvinyl pyrrolidone in an optimized ratio to develop a robust excipient with multifunctional properties. A systematic approach was applied to optimize the composition of the co-processed excipient by determining the proportion by percentage weight of each of the materials used in the co-processing. The optimized formula for preparing the coprocessed excipient with multifunctional properties was found to be maize starch (82%), alginic acid (8%) and polyvinyl pyrrolidone (10%) respectively. Solid state characterization of the co-processed excipient revealed an increase in size of the particles, with spherical shape and rough surfaces. The flowability and compression properties of the co-processed excipient were found to be superior to that of maize starch, alginic acid and polyvinyl pyrrolidone, and the excipients were found to be compatible with one another when co-processed together and also compatible with the drug of choice for the study. The tablets produced using the co-processed excipient by direct compression conformed to the official specification for desirable immediate release tablets and compared well with the commercially available co-processed excipient, Ludipress®.
SUBACUTE TOXICITY, HORMONAL EFFECTS AND HPLC PHYTOCHEMICALANALYSIS OF SPONDIAS MOMBIN LEAF EXTRACT IN FEMALE WISTAR RATS
Uterine fibroids are benign growths in the uterus that commonly develop during a woman’s reproductive years. Since estrogen and progesterone play a key role in fibroid development, researchers have explored herbal treatments that may help regulate these hormones. This study investigated the safety profile and effects of ethanol extract of Spondias mombin Linn (Anacardiaceae) leaves on serum estradiol and progesterone levels in female Wistar rats. Wistar rats were administered the plant extract in graded doses (100 and 200 mg/kg) for 28 days after which blood samples and organs were collected for toxicity studies and hormonal assay. Additionally, High-Performance Liquid Chromatography (HPLC) was employed to identify bioactive compounds in the extract. The extract did not significantly alter adversely, any of the tested biochemical and hematological parameters. It induced minimal toxic damage to the selected tissues of the rats. The biochemical assay showed that Spondias mombin extract did not significantly (P>0.05) reduce serum estradiol levels. The doses of 100 and 200 mg/kg decreased serum progesterone by 39.52 % and 39.26 % respectively. HPLC analysis identified several bioactive compounds such as caryophyllene, quercetin, kaempferol, gallic acid, and β-sitosterol. This result shows that Spondias mombin leaves are relatively safe and suggests that they have potential antiprogestogenic activity that warrants further study.
ANXIOLYTIC PROPERTIES OF ETHANOL LEAF EXTRACT AND RESIDUALAQUEOUS FRACTION OF ROTHMANNIA LONGIFLORA FOLLOWING CHRONICCONSTRICTION INJURY-INDUCED NEUROPATHIC PAIN IN RATS
Rothmannia longiflora leaf is used in the management of pain and inflammation in African traditional medicine. Previous studies demonstrated its analgesic and anti-inflammatory properties but there are no documented reports on the anxiolytic properties of Rothmannia longiflora. The aim of this study is to investigate the anxiolytic properties of the ethanol leaf extract of Rothmannia longiflora and its aqueous fraction following chronic constriction injuryinduced neuropathic pain in rats. The anxiolytic potentials of ethanol leaf extract of Rothmannia longiflora and its residual aqueous fraction at 500 and 1000 mg/kg (p.o) were investigated using anxiety open field model (OF) and elevated plus maze (EPM) test. The negative control received Distilled water 1 mL/kg while the positive control received Minocycline 30 mg/kg. The ethanol extract of Rothmannia longiflora (EERL) significantly (p <0.05) increased the time spent by the rats in central square and decreased the number of stretch attend posture significantly (p <0.05) compared to the negative control. Similarly, the rats that received residual aqueous fraction and the minocycline showed reduced number of stretch attend posture significantly (p <0.05) compared to the negative control in OF model. The EERL significantly (p <0.05) increased the number of entries of the rats into the open arm, the time spent in open arm, and the time spent in central square compared to the negative control in EPM model. EERL and residual aqueous fraction were found to exhibit anxiolytic properties following chronic constriction injury-induced neuropathic pain in rats.
DETERMINATION OF SYNTHETIC PHARMACEUTICAL ADULTERANTS ANDPHYSICOCHEMICAL ANALYSIS OF SOME ANTIHYPERTENSIVE HERBALPRODUCTS
The use of herbal medicines and phytonutrients is expanding rapidly across the world with many people now resorting to these products for treatment of various health challenges. This is as a result of its cultural acceptability, affordability, and lack of access to modern medicine. The safety of these herbal remedies is however poorly understood. This study was aimed at determining the presence of synthetic pharmaceutical (bendroflumethiazide and furosemide) adulterants and evaluating the physicochemical parameters of some selected antihypertensive herbal products marketed within three Northwestern states (Kastina, Kebbi and Jigawa) of Nigeria. A total of twenty-three samples were collected for this study. Screening of the samples for the presence of bendroflumethiazide and furosemide as undeclared adulterants was carried out using thin layer chromatographic (TLC) and Fourier transform infra-red (FTIR) analyses. Physicochemical analyses of the antihypertensive herbal samples were conducted according to the standard methods. Four of the analysed samples (M7, M10, M11 and M14) were found to have spot corresponding to that of bendroflumethiazide standard powder. However, the spots were discovered not to be bendroflumethiazide by the FTIR analysis. Furosemide was not detected in any of the analysed samples. The physicochemical analyses of the antihypertensive herbal samples showed that 53 % of the sample failed the weight uniformity test as it was found to be above the permissible limit. Furthermore, 27 % of the samples had moisture content above recommended 8 % NAFDAC limit while all the samples were found to have extractives values of below the minimum recommended limits. The total ash values in 17 % of the samples were higher than the 14 % maximum acceptable limit recommended by European Pharmacopoeia. The analysed antihypertensive herbal products did not contain bendroflumethiazde and furosemide as undeclared adulterants; however, their quality may be considered substandard, since none complied with all quality tests conducted.
HEALTH-RELATED QUALITY OF LIFE, WORK PRODUCTIVITY, ANDASSOCIATED FACTORS AMONG PATIENTS WITH TYPE 2 DIABETES MELLITUSON ANTI-DIABETIC MEDICATIONS: A CROSS-SECTIONAL STUDY IN NORTHCENTRAL NIGERIA
Diabetes mellitus poses a major public health challenge in Africa, particularly in Nigeria, due to its high morbidity, mortality, and economic impact, which are worsened by its chronic nature and related complications. The aim of this study was to assess the health-related quality of life (HRQoL), work productivity, and associated factors among patients with Type 2 Diabetes Mellitus (T2DM) receiving anti-diabetic medications at a secondary health facility in Ilorin, Kwara State, North Central Nigeria. A cross-sectional study through convenient sampling was conducted in patients registered in the last ten years (10) from (May 2013 to August 2023). Participants were drawn after a sample size of 304 participants was calculated. Informed consent was obtained from all participants, and ethical approval was granted by Ethics and Research Committee of the Institution (Approval ID: ERC /MOH/2023/04/102). Data on health-related quality of life were collected using the EQ-5D-5L and EQ-VAS instruments, while the Work Productivity and Activity Impairment (WPAI) questionnaire was used to assess changes in work productivity. Statistical analysis involved both descriptive and inferential methods, with results presented in tables. Of the 304 participants included, 108(35.5%) were female, 196(64.4%) were male. Majority fell within the age group of 55-65 years old (39.5%). Majority140 (46%) were in the lower middle income ($39-130) category. Biguanide plus sulphonyl urea combination therapy recorded the highest usage (71.1%). Overall loss of productivity and activity impairment as outcomes of work productivity was found to be 24.8% and 33.6%. The mean EQ-5D utility scores and EQ-VAS scores were 0.7033±0.1525 and 63.57±17.16 Factors such as older age, presence of complications and comorbidities, and higher overall productivity loss are significantly associated with lower HRQoL scores. Conversely, being employed and having a good monthly income are significantly associated with better. Healthrelated quality of life of individuals with type 2 diabetes, as measured by EQ-5D utility and EQ-VAS scores. Results highlight the importance of socioeconomic and clinical factors in influencing the quality of life of patients with type 2 diabetes.
PREPARATION AND EVALUATION OF DISINTEGRANT PROPERTIES OFCROSS-LINKED SORGHUM (SORGHUM ARUNDINACEUM) STARCH INMETRONIDAZOLE TABLET FORMULATIONS
Starch is one of the most versatile excipients used in this process due to its multifunctional properties. In its native form, it is commonly employed as a disintegrant in tablet formulations. However, several limitations that affect its stability on storage, compressibility, and flowability have led to its modification to obtain starch derivatives with better physicochemical and physicochemical properties. In the present study, native sorghum starch (NSS) and its cross-linked derivative were tested as a disintegrant in metronidazole tablets. NSS was cross-linked with phosphorus oxychloride (POCl3), 0.3 %v/v, to obtain cross-linked sorghum starch (CSS). Both starches were evaluated for their physicochemical and micrometric properties and evidence of crosslinking and compatibility with the model drug was determined using Fourier Transform Infrared (FTIR) spectroscopy. Metronidazole tablets were formulated using both the wet granulation and direct compression methods, and the tablets were evaluated using standard pharmacopeia methods. FTIR revealed the presence of phosphorus-bound symmetry in CSS at 1273.06 cm-1 and 995.30 cm-1 . An improvement in the flow properties of CSS over NSS was achieved. Generally, the tablets had friability values of less than 1%, irrespective of the method of preparation. Also, tablets made by direct compression showed higher crushing strengths and DER but lower disintegration times for both NSS and CSS. All the tablets disintegrated and released 75 % of their drug content in less than 15 min, with slower release rates seen with CSS. The two starches perform well in both wet granulation and direct compression; however, the CSS formulation had longer disintegration time compared to those formulations of NSS and MSBP when used in both wet granulation and direct compression.
EFFICACY OF A PERSONALIZED FOOD AVOIDANCE DIETARY APPROACH FORTHE CONTROL OF ESSENTIAL HYPERTENSION
Essential Hypertension (EH) is the leading cause of global morbidity and mortality. Ongoing clinical trials of a Personalized Food Avoidance Dietary Approach to Stop Hypertension (PFADASH) implicate some dietary constituents in the phenotypic expression of EH. The aim of this study was to evaluate the adjunctive efficacy of a PFADASH on the control of EH. This was part of an open controlled clinical trial of a PFADASH approved by the University of Nigeria Teaching Hospital (UNTH) Ethics Committee. Study was carried out at Medical Outpatient Clinics UNTH and Chiolive International Medical Research Organization, Tran-Ekulu Enugu from 2015 to 2019. Seven Study Participants (SPs) met the inclusion/exclusion criteria of being on at least two antihypertensive drugs, adult and literate. Dietary Compliance (DC) to a PFADASH which excludes food additives and hydrogenated fats, Blood Pressure (BP), antihypertensive drug requirements and echocardiography assessments was done for SPs by collaborating dieticians, pharmacists and physicians. Study adopted a longitudinal prospective study design. Analysis of variance (ANOVA), Spearman correlation coefficient and Pearson test were used for inferential statistics. Drug treatment parameters: prescribed treatment (Rx), actual adherence (Adh), adherence score (AdhRx), Antihypertensive Drug Treatment Requirement score (ADTR), blood pressure and echocardiographic parameters did not show positive association with DC (P>0.05) although ADTR and average BP scores was lower in SPs with good DC without significant impact from potential confounders like sleep and exercise habits. Study participants with good DC to a PFADASH had lower BP scores with slight improvements in the echocardiographic parameter: Left Ventricular Ejection Fraction (LVEF). These observations should be pivotal in demonstrating the role of some dietary constituents in the aetiopathogenesis of EH.
ANTIDEPRESSANT ACTIVITY OF METHANOL LEAF EXTRACT OF ZIZIPHUSMAURITIANA LAM IN SWISS ALBINO MICE
The leaves of Ziziphus mauritiana have been reported to be used in the management of depressive illnesses in traditional medicine. The present study aimed at investigating the antidepressant activity of the methanol leaf extract of Ziziphus mauritiana (25, 50,100 and 200 mg/kg) using tail suspension (TST) and forced swim tests (FST) while the effect of the extract on recognition memory, motor coordination, and exploration activity was also evaluated using novel object recognition (NORT), beam walking assay (BWAT) and open field tests (OFT) respectively in mice. The LD50 of the extract was found to be above 5000 and phytochemical constituents such as flavonoids, cardiac glycoside, and alkaloids were present. The extract significantly decreased the duration of immobility in the TST and FST and produced insignificant change in exploratory activity and motor coordination in OFT and BWAT when compared with the control group. The methanol leaf extract of Ziziphus mauritiana possesses antidepressant property.
FORMULATION AND EVALUATION OF ASCORBIC ACID AND METRONIDAZOLETABLETS CONTAINING MICROCRYSTALLINE CELLULOSE DERIVED FROMORYZA SATIVA
The research aims to formulate and evaluate the tableting properties of microcrystalline cellulose derived from Oryza sativa chaff, which was used as a direct compression excipient in the formulation of ascorbic acid and metronidazole tablets. Portion of the samples of Oryza sativa chaff after cleaning and drying (300 g) was soaked in 500 mL of 17.5 % sodium hydroxide solution. The slurry obtained was maintained under constant stir for 1 h at room temperature. The pre-treated chaff was filtered at room temperature and then washed with 500 mL 95 % ethanol to remove the base; the sample was then dried in an oven at 60 for 24 h. Each of the sample was further mixed with 300 mL distilled water, 50 mL glacial acetic acid and 200 mL of sodium hypochloride. The mixtures were stirred on a water-bath at 75 for 2 h and the residue washed with 95 % ethanol and distilled water. Each of the extracted cellulose samples A and C (72.1 and 84.2 g) was added to a 1 L beaker containing 500 mL of 2.5 M hydrochloric acid and heated to a temperature of about 100 on a hot plate for 15 mins. The resulting crystalline cellulose was collected and filtered, then washed with aqueous ammonia solution and distilled water. This was dried at room temperature to constant weight. Physicochemical characteristics was done on the extracted materials to determine the suitability of varieties of MCC used as direct compression agent in formulation of ascorbic acid and metronidazole tablet in relation to the standard Avicel®PH-102. The chaff derived microcrystalline cellulose (CDMCC) obtained was light-yellow, tasteless powder with characteristic odour. FTIR spectral study showed that there was no chemical interaction and introduction of new peak across all the samples just like the Avicel®PH-102. The dilution potential CDMCC with respect to ascorbic acid was 60:40 with a tensile strength of 0.97 MN/m2 and metronidazole to be 50:50. The tablet properties of the respective formulation met the requirements in the British Pharmacopoeia. The dissolution studies showed that the Avicel®PH-102 gave better results than the CDMCC. The standard Avicel®PH-102 performed better than the microcrystalline cellulose extracted (CDMCC) as a direct compression agent in the formulation of ascorbic acid and metronidazole tablet. CDMCC from a good variety can serve as alternative to costly available direct compressible excipients such Avicel®PH-102 for immediate release tablets.
SAFETY PROFILE, HPLC ANALYSIS, AND EFFECT OF VERNONIA AMYGDALINADELILE (ASTERACEAE) LEAVES ON STEROIDAL HORMONES ASSOCIATEDWITH UTERINE FIBROID
Uterine fibroids are non-cancerous growths in the uterus that commonly develop during the reproductive years in women. The role of estrogen and progesterone in fibroid development has been well established, prompting research into potential herbal interventions to regulate these steroidal hormones. This study aimed to evaluate the safety profile and effects of ethanol extract of Vernonia amygdalina Delile (Asteraceae) leaves on serum estradiol and progesterone levels in female Wistar rats, as well as identify the bioactive compounds present in the extract. The leaves of V. amygdalina were extracted with ethanol using a Soxhlet apparatus. Wistar rats were administered the plant extract in graded doses (100 and 200 mg/kg) for 28 days after which blood samples and organs were collected for toxicity studies and hormonal assay. Additionally, High-Performance Liquid Chromatography (HPLC) was employed to identify bioactive compounds in the extract. The extract did not adversely alter any of the tested safety biochemical and hematological parameters. It boosted the immune system, induced bronchiolar dilation and improved blood flow within the vessels of the heart. The hormonal assay revealed that the extract at 100 and 200 mg/kg did not decrease serum estradiol levels. However, a significant lowering of serum progesterone was observed (p<0.05). HPLC analysis identified several bioactive compounds including benzophenone, garcinoic acid, vernodalin, luteolin, and andrographoside. These findings suggest that V. amygdalina is safe, and possesses significant potential in reducing progesterone levels, possibly due to its diverse bioactive constituents, which may contribute to its hormone-modulatory activity.
EXTRACTION AND PURIFICATION OF STEM BARK GUM OF GREWIA MOLLISJUSS. FOR USE AS A DISINTEGRANT IN TABLET FORMULATION
Gums are polysaccharides of natural origin that have been used traditionally as binders in the formulation of tablets by wet granulation. This research aimed at extraction of Grewia mollis gum (GG) by dispersing 600 g of the dried and pulverized inner stem bark of the Grewia mollis shrub in about 20 litres of demineralized water using an impeller, which was further purified by treatment with 0.1 M hydrochloric acid for about 5 minutes followed by extraction with 25 ml of 95 % Acetone and evaluating the use of bleached acetylated stem bark gum of Grewia mollis Juss (BAGG) as a disintegrant in tablet formulations using Ibuprofen as a model drug. The yields of the gums were found to be 58.5, 80.3, and 60.0 % for GG (Grewia Gum), AGM (Acetylated Grewia Gum), and BAGG (Bleached Acetylated Grewia Gum) respectively. The pH values for the gums were 4.83, 4.95, and 4.01 for GG, AGM, and BAGG respectively. The swelling capacities were 1.59 ± 0.00, 2.90 ± 0.01, and 2.80 ± 0.00 respectively for GG, AGM, and BAGG. Moisture contents were 0.54 ± 0.01, 0.13 ± 0.01, and 0.12 ± 0.01 for GG, AGM and BAGG respectively. The LD 50 values of both the native and derivatized gums were both greater than 5000 mg. Tablets weighing 500 mg were prepared by compressing ibuprofen granules containing BAGG as disintegrant at concentrations ranging from 1.25 to 10 % in comparison to maize starch B.P. at the same concentrations. The tablets formulated were kept for about 24 hours and subsequently evaluated for tablet properties. The outcome of the study showed that tablets formulated with BAGG - A as disintegrant with a concentration of 1.25 % had an enhanced disintegration time and dissolution profile comparable to other formulations. Formulation of ibuprofen tablets containing BAGG - A with 1.25 %, as disintegrant was obtained with the following properties; Crushing strength (6.9 ± 1.24 kgf), disintegration time (9.47 ± 3.06 min) and friability (0.78 %). The results of this study had been able to establish that bleached acetylated Gewia mollis stem bark gum, concentration 1.25 %, could be used effectively to formulate Ibuprofen tablets that disintegrated within 15 mins.
QUALITY ASSESSMENT OF SELECTED ANTIMALARIAL HERBAL DRUGS
The use of herbal medicinal products for the treatment and prevention of diseases has a long tradition worldwide and it has played an important role in the health care of numerous divergent societies, ranging from developing countries in Asia and Africa to western developed nations Herbal medicinal products are readily available and are not regulated and as such, serious safety concerns might be associated with these herbal medicines. This study was aimed at evaluating the physico-chemical and phytochemicals of some selected antimalarial herbal products marketed within Zaria metropolis. The physico-chemical analysis was carried out using standard analytical method reported by Trease and Evans. The result of physicochemical analysis shows that only 25 % of the samples passed the uniformity test. Phytochemical screening was conducted according to the standard procedures and the result revealed the presence of alkaloids, flavonoids, cardiac glycosides, saponins, terpenoids and tannins in 75, 100, 92, 96, 80 and 100 % respectively in the samples. Some (25 %) of the samples passed the weight uniformity test as none of these samples deviated from the mean weight by more than 7.5%. This indicates that good manufacturing practice was not adhered to during the packaging of these antimalarial herbal products. Also, all the samples were found to have phytochemicals required for antimalarial activity however, only few (25 %) of them is safe for consumption as per their weight variation studies. Thus, implying that there will be no consistency in dosing with these products and therefore, the therapeutic effect needed may not be achieved.