Résumé
OBJECTIVE:To prepare m-nisoldipine solid dispersion from poorly-soluble m-nisoldipine so as to improve its solubility and dissolution rate in vitro. METHODS: Solid dispersions of m-nisoldipine were prepared by coprecipitation method with poloxamer as carrier; Differential scanning calorimetry (DSC) was used to determine the status of nimodipine in carrier. The solubility and the dissolution rate of the solid dispersion in vitro were studied. RESULTS: DSC analysis indicated that eutectic mixture was formed from m-nisoldipine and poloxamer. The solubility of m-nisoldipine and the its solid dispersions prepared from m-nisoldipine and poloxamer at different ratio (1∶3, 1∶5, 1∶7) were 0.89, 4.50, 15.35, and 23.03 mg?L-1, respectively, and their 120 min dissolution rates were 26.80%, 38.57%, 41.38%, and 45.92%, respectively. In the same ratio, the dissolution rates of the solid dispersions were higher than those of their physics mixtures. CONCLUSIONS: The solid dispersion of m-nisoldipine prepared with poloxamer as carrier can increase the solubility and dissolution rate in vitro.
Résumé
Objective: To explorate the drug releasing rule in vitro of Maxingshigan Dropping pill and Suppository. Methods: Their dissolution rates in vitro were determined by the rotary basket method, the contents of total alkaloid in ephedra alkaloid in the two preparations were determined by acidic dye colorimetry, and they were used as markers of dissolution.Results:The dissolution quantity in 45 min of Dropping pill reached 100%, whereas that of suppository reached 92.58%. Conclusion: T 50 , T d of the two preparations showed significant difference ( P
Résumé
AIM:To study the prepartion of Ruanganxiaoshui Cataplasma and it's percutaneous absorption in vitro as well as dissolvability in vitro. METHODS: In the experiment,orthogonal test was used to optimize the preparation.Meanwhile,with the help of azole and propylene alcohol the percutaneous absorption of ginsenoside Rg_1 from the cataplasma carriers in vitro was determined by Franz's diffusion cell and HPLC,as well as dissolution rate in vitro. RESULTS: The percutaneous absorption rate of ginsenoside Rg_1 through rat skin in vitro was 0.394 ?g/cm~2/h.And the dissolution process fitted to first order model. CONCLUSION: The Cataplasma carriers possess a good drug dissolution property.To add compound penetration enhancers is one of the effective methods for raising percutaneous absorption.