RESUMO
This study deals with the formulation of antihyperglycemic leaf extracts of Zizyphus spina-christi (L.) Willd. A bioactivity guided fractionation of different leaf extracts [defatted ethanol 70% (a), butanol (b), ethanol 70% (c), ethyl acetate (d) and petroleum ether (e) extracts] revealed that extract (c) possessed the highest antihyperglycemic activity followed by (b) and (a). HPLC was adopted for standardization of the extract (c) based on evaluation of the major saponin christinin-A which was used as marker. The detection limit was 9.45 mg/ml for Christinin-A. Extracts (a), (b) and (c) were separately formulated in soft (S) and hard (H) gelatin capsules. Two different formulations (F1 and F2) were tried using different excipients suitable for oral drug delivery. Formula 1, used for soft gelatin capsules [(F1) Sa, Sb, Sc] Formula 2, used for hard gelatin capsules [(F2) - Ha, Hb, Hc]. The recovery rates of the samples of saponin were in the range 99.43-101.86% at 200, 800 microg/ml and 1200 microg/ml. Saponin release rates from different formulae were carried out using dissolution tester USP XXIV. The highest release was obtained from formulation Sc. The release of the extracts followed diffusion mechanism. The selected formula Sc exhibited highest anti-diabetic activity (P < 0.01) on acute and long-term administration and highest saponin release. This formula (Sc) contained poly-oxyethylene (20) cetyl ether (BC-20TX), PEG 400, PEG 6000, purified water, meglyol 810, ascorbic acid and 200 mg of extract (c).
Assuntos
Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/farmacologia , Ziziphus/química , Administração Oral , Animais , Glicemia/metabolismo , Calibragem , Cápsulas , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Hipoglicemiantes/toxicidade , Metabolismo dos Lipídeos/efeitos dos fármacos , Testes de Função Hepática , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Folhas de Planta/química , Ratos , Ratos Sprague-Dawley , Padrões de Referência , Reprodutibilidade dos Testes , Espectrofotometria UltravioletaAssuntos
Anti-Infecciosos/síntese química , Nitrofuranos/síntese química , Antibacterianos , Anti-Infecciosos/farmacologia , Antibiose , Bacillus subtilis/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Micrococcus/efeitos dos fármacos , Nitrofuranos/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Salmonella paratyphi A/efeitos dos fármacos , Sarcina/efeitos dos fármacos , Staphylococcus/efeitos dos fármacosRESUMO
The antimicrobial activity of the volatile oil of Nigella sativa Linneaus seeds was studied. The antimicrobial principle has been isolated, identified as thymohydroquinone, and found to be active against gram-positive bacteria and yeasts.
