目的 篩選鹽酸決奈達(dá)隆片的處方組成,并評(píng)價(jià)其溶出度.方法 以鹽酸決奈達(dá)隆的溶出度為指標(biāo),采用L₉(3⁴)正交試驗(yàn)優(yōu)化鹽酸決奈達(dá)隆片處方主要因素填充劑乳糖-淀粉比例、黏合劑聚維酮K30的乙醇體積分?jǐn)?shù)、增溶劑波洛沙姆用量、崩解劑交聯(lián)聚維酮用量.以賽諾菲-安萬(wàn)特公司原研制劑邁達(dá)龍為參比制劑,采用f₂相似因子法進(jìn)行鹽酸決奈達(dá)隆溶出曲線的相似度評(píng)價(jià).結(jié)果 鹽酸決奈達(dá)隆片的最佳處方為填充劑比例2:1,選用5% PVP K30 40%乙醇溶液為黏合劑,泊洛沙姆188用量為2%,交聯(lián)聚維酮用量為3%.在不同pH值的溶出介質(zhì)中,自制制劑和參比制劑的溶出曲線f₂相似因子均大于50.結(jié)論 自制制劑與參比制劑在不同pH值的溶出介質(zhì)中得體外溶出行為相似.

Objective To optimize the prescription of Dronedarone Hydrochloride Tablets, and to evaluate its dissolubility. Methods The main factors, such as the filler proportion of lactose and starch, concentration of 5% adhesive povidone K30 ethanol solution, content of solubilizing agent Poloxamer 188, and content of disintegrant polyvinylpolypyrrolidone were optimized by L₉(3⁴) orthogonal test with dissolubility of dronedarone hydrochloride as index. Dronedarone Hydrochloride Tablets (Multaq) from Sanofi-Aventis were selected as reference preparation, and the similarity of dissolubility curves were evaluated by the similarity factor (f₂) method. Results The optimized prescription of Dronedarone Hydrochloride Tablets was as follows: filler proportion of lactose and starch was 2:1, ethanol concentration of 5% adhesive povidone K30 was 40%, content of solubilizing agent Poloxamer was 2%, and content of disintegrant polyvinylpolypyrrolidone was 3%. In various dissolution media with different pH values, the dissolubility curves of Dronedarone Hydrochloride Tablets between self-prepared preparations and reference Multaq were compared, and similar factors f₂ were above 50. Conclusion The dissolution behaviors of self-prepared preparations and reference Multaq in various dissolution media with different pH values are similar.