ABSTRACT
Aims: Solanum trilobatum Linn., (Solanaceae) is one of the most widely used plants as food supplement in southern part of India and some parts of Southeast Asia. This plant is traditionally used for the treatment of respiratory illness. In animal studies, the extract of S. trilobatum showed significant antimicrobial, hepatoprotective and anticancer activities. The complete phytochemical profile, antimicrobial and mast cell stabilizing activities of S. trilobatum remains unclear. This study tests the antimicrobial, antihistaminic and mast cell stabilizing activities of ethanolic extract of leaves of S. trilobatum (EEST). Methodology and results: The phytochemical test was carried out using chemical and instrumental [Gas Chromatography Mass Spectrometry (GC-MS)] analytical methods. Antimicrobial effect of EEST was tested against Streptococcus pneumonia, Escherichia coli and Staphylococcus aureus. Intestinal mesentery of Sprague Dawley (SD) rats was used to study the peritoneal mast cell stabilization activity of EEST. The rat intestinal mesentery was exposed to 50, 100, 200, 300, 400 and 600 μg/mL of EEST and the peritoneal mast cell stabilization activity was compared with that of standards (pheniramine 20 μg/mL and ketotifen 20 μg/mL). The phytochemical test showed the presence of carbohydrates, saponins, flavonoids, alkaloids, tannins and phenolic compounds. GC-MS analysis indicated the presence of 45 fragmented compounds which included epoxylinalol, himachalol, illudol, epibuphanamine, baimuxinal and edulan IV. EEST exhibited antimicrobial activity at 10 mg/mL against S. aureus, S. pneumonia. Significant mast cell stabilizing activity was observed from the dose of 100 μg/mL to 600 μg/mL. Conclusion: Ethanolic extract of leaves of S. trilobatum possess significant antimicrobial and antihistaminic activity.
ABSTRACT
The objective of the present work is to study the dissolution behavior of olanzapine from its solid dispersions with mannitol. Solid dispersions were prepared by melt dispersion method and characterized by phase solubility studies, drug content and in vitro dissolution studies. The best releasing dispersions were selected from release data, dissolution parameters and their release profiles. Solid state characterization techniques like Fourier transform infrared (FT-IR) spectroscopy, X-ray diffractometry, differential scanning calorimetry, near-infrared and Raman spectroscopy were used to characterize the drug in selected dispersions. The dispersions were also evaluated by wettability studies and permeation studies. The results of phase solubility studies and the thermodynamic parameters indicated the spontaneity and solubilization effect of the carrier. The release study results showed greater improvement of drug release from solid dispersions compared to pure drug, and the release was found to increase with an increase in carrier content. The possible mechanism for increased release rate from dispersions may be attributed to solubilization effect of the carrier, change in crystal quality, phase transition from crystalline to amorphous state, prevention of agglomeration or aggregation of drug particles, change in surface hydrophobicity of the drug, and increased wettability and dispersability of the drug in dissolution medium. The suggested reasons for increased release rate from dispersions were found to be well supported by results of solid state characterization, wettability and permeation studies. The absence of any interaction between the drug and the carrier was also proved by FT-IR analysis.
O objetivo do presente trabalho é estudar o comportamento de dissolução da olanzapina a partir de suas dispersões sólidas de manitol. As dispersões sólidas foram preparadas por dispersão por fusão e caracterizadas por estudos de solubilidade de fase, conteúdo de fármaco e dissolução in vitro. As melhores dispersões quanto à liberação foram selecionadas a partir dos dados de liberação, parâmetros de dissolução e perfis de liberação. Técnicas de caracterização de estado sólido como espectroscopia no infravermelho pela transformada de Fourier (FTIR), difratometria de raios X, calorimetria de varredura diferencial, infravermelho próximo e espectroscopia Raman foram utilizadas para caracterizar os fármacos a partir das dispersões selecionadas. As dispersões foram, também, avaliadas pelos estudos de capacidade de umedecimento e permeação. Os resultados dos estudos de solubilidade de fase e os parâmetros termodinâmicos indicaram a espontaneidade e o efeito de solubilização do transportador. Os resultados dos estudos de liberação mostraram maior aperfeiçoamento da liberação do fármaco das dispersões sólidas, comparativamente à do fármaco puro, e descobriu-se que a liberação aumenta com o aumento do conteúdo de transportador. O mecanismo possível para o aumento da taxa de liberação das dispersões pode ser atribuído ao efeito de solubilização do transportador, mudança da qualidade do cristal, transição de fase cristalina para estado amorfo, prevenção da aglomeração ou agregação das partículas do fármaco, mudança na superfície de hidrofobicidade do fármaco e aumento da capacidade de umedecimento e dispersividade do fármaco no meio de dissolução. As razões sugeridas para o aumento da taxa de liberação a partir das dispersões foram apoiadas pelos resultados da caracterização do estado sólido, capacidade de umedecimento e pelos estudos de permeação. A ausência de qualquer interação entre o fármaco e o transportador foi, também, comprovada pela análise no FTIR.