Distribution of Methicillin-Resistant Staphylococcus aureus (MRSA) in Apparently Healthy Population and its Susceptibility to Saponins from Dialium guineense.

Aims: The ethanolic extracts of stem bark and fruit pulp as well as saponins from Dialium guineense were assayed for antibacterial activity against Gram positive and negative strains and clinical strains of methicilin resistant Staphylococcus aureus (MRSA) isolated from different locations on human body aged 20-30 years within the University of Nigeria community. Methodology: Agar diffusion technique was adopted. Results: The results showed that MRSA is predominant in apparently healthy population of the University community with 100% in males and 92.3% females showing positive case in nasal swab, 87.5% and 96.6 % positive from ear swabs of male and female volunteers respectively; and 77.7% positive from the high vaginal swabs of females. MRSA and other clinical isolates showed higher susceptibility to saponins compared to crude extracts; however, Bacillus cereus (NRRL 14724 and 14725) were not susceptible to the saponins from D. guineense. The MICs of the saponins were 31.25 mg/mL (B. subtilis ATCC 6051, P. aeruginosa, S. typhi, S. knitambo, P. mirabilis and S. aureus), 62.50 mg/mL (E. coli) and 125 mg/mL (P. aeruginosa ATCC 10145). Comparable MICs of higher values were obtained with the crude ethanolic extracts of stem bark and fruit pulp against MRSA and clinical isolates. Conclusion: The present findings revealed wide distribution of MRSA in an apparently healthy population in Nigeria and the susceptibility patterns showed the presence of a broad spectrum antibacterial agent in D. guineense.

Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS).

Aims: To formulate sustained release diclofenac potassium tablets based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties of the tablets. Study Design: Formulation, in vitro and in vivo evaluation of sustained release diclofenac potassium. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka and Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria. Methodology: SRMS, consisting of mixtures of phospholipid and triglyceride were prepared in the ratios of 1:1, 2:1 and 1:2 (Phospholipon® 90H: Softisan® 154) respectively. SRMS-based tablets containing 100 mg of diclofenac potassium each were prepared using validated plastic mould. The physicochemical properties of the tablet formulations were studied and compared with the market brands of the drug for sustained release properties. In vitro release was carried out in simulated intestinal fluid (SIF, pH 7.5) using the USP paddle method. Anti-inflammatory, analgesic/anti-nociceptive and ulcerogenic properties of the formulated tablets were studied using adult Wistar rats. Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix (LM) used (p < 0.05). The hardness of the tablets ranged from 4.55 ± 0.50 to 5.10 ± 0.39 kgf for tablets formulated with LM 1:2 and 1:1 (M3 and M1) respectively. Friability results indicated that all the SRMs tablets exhibited friability values less than 1 %. The erosion time ranged from 35.8 ± 1.10 to 120.3 ± 0.32 min. The release profile of the tablets showed maximum release between 8 – 11 h for all the batches. Diclofenac potassium tablets based on SRMS had good anti-inflammatory and analgesic properties and also inhibited the ulcerogenicity of the NSAID by up to 85 %. Conclusion: Diclofenac potassium tablets based on SRMS could be used for once daily administration.

Pharmacological justification for the ethnomedical use of Clausena anisata root-bark extract in the management of epilepsy.

Various morphological parts of the tropical plant, Clausena anisata (Wild) Hook [family: Rutaceae], have ethnomedical claim for use in the management of epilepsy. This study examined the antiepileptic activity of Clausena anisata root bark, stem bark and leaf ethanolic extracts (i.e. CARE, CASE and CALE respectively) against pentylenetetrazole (PTZ) induced seizures in mice. Phytochemical and acute toxicity tests were performed on the extracts followed by oral administration of graded doses of CASE (500, 750 and 1000 mg/kg), CARE and CALE (400, 600 and 800 mg/kg) to the mice, thirty minutes before the administration of PTZ (90 mg/kg i.p.). The anticonvulsant effect of the extracts and diazepam (4 mg/kg) were compared. CALE was found to possess large amount of saponins, CARE large amounts of tannins and saponins, CASE large amounts of flavonoids, alkaloids and tannins. While CARE at the dose level of 800 mg/kg significantly (p<0.05) delayed the onset of convulsions and afforded 33.33 % protection, neither CALE nor CASE could exert any significant protective effect on PTZ induced convulsions, whereas diazepam totally abolished the episodes of convulsions. This study suggests that the ethanolic root bark extract of Clausena anisata contains bioactive constituents that may be beneficial in petit mal epilepsy and lend pharmacological credence to the ethnomedical claim for the use of the plant in the management of epilepsy. Abbreviations: NMDA= N-methyl-D-aspartate, SCMC= sodium carboxy methyl cellulose, CARE= Clausena anisata root bark ethanolic extract, CASE= Clausena anisata stem bark ethanolic extract, CALE= Clausena anisata leaf ethanolic extract, PTZ= pentylenetetrazole.