卡维地洛固体分散体的制备及其性质研究
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摘要
为提高卡维地洛溶解度和溶出速率,采用固体分散技术,通过溶剂法,以PVP K30为载体,以药辅质量比(CAR∶PVP K30)、溶剂用量、溶剂蒸发的温度为考察因素,采用正交试验法,得出卡维地洛固体分散体制备的最佳工艺:药物与载体材料质量比1∶9,加入10 m L无水乙醇,蒸发溶剂的温度50℃。与卡维地洛原料药相比,按最佳工艺制备的卡维地洛固体分散体,60min溶出百分率从16.25%提高到98.04%。
In order to improve the solubility and dissolution rate of carvedilol,the solid dispersion technology is used,through the solvent method,and PVP K30 is used as the carrier,the drug assisted mass ratio(CAR∶ PVP K30),the amount of solvent and the temperature of solvent evaporation are selected as tested factors,orthogonal test method is used to obtain the optimum process for the preparation of carvedilol solid dispersion system: The mass ratio of drug and carrier material is 1∶ 9,adding 10 m L anhydrous ethanol,and the temperature of evaporation solvent is 50 ℃. Compared with the carvedilol API,the solid dispersion of carvedilol prepared by the best process has a 29-fold increase in solubility,and the percentage of dissolution after 60 min increases from below 16. 25% to 98. 04%.
In order to improve the solubility and dissolution rate of carvedilol,the solid dispersion technology is used,through the solvent method,and PVP K30 is used as the carrier,the drug assisted mass ratio(CAR∶ PVP K30),the amount of solvent and the temperature of solvent evaporation are selected as tested factors,orthogonal test method is used to obtain the optimum process for the preparation of carvedilol solid dispersion system: The mass ratio of drug and carrier material is 1∶ 9,adding 10 m L anhydrous ethanol,and the temperature of evaporation solvent is 50 ℃. Compared with the carvedilol API,the solid dispersion of carvedilol prepared by the best process has a 29-fold increase in solubility,and the percentage of dissolution after 60 min increases from below 16. 25% to 98. 04%.
引文
[1]DULIN B,ABRAHAM W T.Pharmacology of carvedilol[J].Am J Cardiol,2004,93(9A):3B-6B.
[2]张生潭,兰新宇,杨达宇,等.国产与进口降压药物治疗高血压患者临床疗效的荟萃分析[J].河北医科大学学报,2015,36(6):632-637.
[3]刘敏华.用卡维地洛治疗顽固性心力衰竭的效果研究[J].当代医药论丛,2015(16):287-288.
[4]MCTAVISH D,CAMPOLI-RICHARDS D,SORKIN E M.Carvedilol.A review of its pharmacodynamic and pharmacokinetic properties,and therapeutic efficacy[J].Drugs,1993,45(2):232-258.
[5]KASIM N A,WHITEHOUSE M,RAMACHANDRAN C,et al.Molecular properties of WHO essential drugs and provisional biopharmaceutical classification[J].Mol Pharm,2004,1(1):85-96.
[6]王丽亮.提高难溶性药物生物利用度方法研究进展[J].继续医学教育,2016,30(10):143-144.
[7]SHEWALE B D,SAPKAL N P,RAUT N A,et al.Effect of hydroxylpropyl-β-cyclodextrin on Solubility of Carvedilol[J].Indian J Pharm Sci,2008,70(2):255-257.
[8]刘文利,魏振平.新型固体分散体技术改善水难溶药物溶解度的研究进展[J].中国药学杂志,2016,51(22):1 901-1 906.
[9]POTLURI R H,BANDARI S,JUKANTI R,et al.Solubility enhancement and physicochemical characterization of carvedilol solid dispersion with Gelucire 50/13[J].Arch Pharm Res,2011,34(1):51-57.
[10]LOFTSSON T,VOGENSEN S B,DESBOS C,et al.Carvedilol:solubilization and cyclodextrin complexation:atechnical note[J].AAPS Pharm Sci Tech,2008,9(2):425-430.
[11]PRADHAN R,TRAN T H,KIM S Y,et al.Preparation and characterization of fast dissolving flurbiprofen and esomeprazole solid dispersion using spray drying technique[J].Int J Pharm,2016,502(1/2):38-46.
[12]刘娱姗,高署,柯学,等.难溶性药物固体分散体研究新进展[J].药学进展,2013,37(4):166-173.
[13]乔井会,郭建鹏,马艳,等.阿托伐他汀钙泊洛沙姆188固体分散体的制备及表征[J].中国药房,2015,26(1):103-106.
[2]张生潭,兰新宇,杨达宇,等.国产与进口降压药物治疗高血压患者临床疗效的荟萃分析[J].河北医科大学学报,2015,36(6):632-637.
[3]刘敏华.用卡维地洛治疗顽固性心力衰竭的效果研究[J].当代医药论丛,2015(16):287-288.
[4]MCTAVISH D,CAMPOLI-RICHARDS D,SORKIN E M.Carvedilol.A review of its pharmacodynamic and pharmacokinetic properties,and therapeutic efficacy[J].Drugs,1993,45(2):232-258.
[5]KASIM N A,WHITEHOUSE M,RAMACHANDRAN C,et al.Molecular properties of WHO essential drugs and provisional biopharmaceutical classification[J].Mol Pharm,2004,1(1):85-96.
[6]王丽亮.提高难溶性药物生物利用度方法研究进展[J].继续医学教育,2016,30(10):143-144.
[7]SHEWALE B D,SAPKAL N P,RAUT N A,et al.Effect of hydroxylpropyl-β-cyclodextrin on Solubility of Carvedilol[J].Indian J Pharm Sci,2008,70(2):255-257.
[8]刘文利,魏振平.新型固体分散体技术改善水难溶药物溶解度的研究进展[J].中国药学杂志,2016,51(22):1 901-1 906.
[9]POTLURI R H,BANDARI S,JUKANTI R,et al.Solubility enhancement and physicochemical characterization of carvedilol solid dispersion with Gelucire 50/13[J].Arch Pharm Res,2011,34(1):51-57.
[10]LOFTSSON T,VOGENSEN S B,DESBOS C,et al.Carvedilol:solubilization and cyclodextrin complexation:atechnical note[J].AAPS Pharm Sci Tech,2008,9(2):425-430.
[11]PRADHAN R,TRAN T H,KIM S Y,et al.Preparation and characterization of fast dissolving flurbiprofen and esomeprazole solid dispersion using spray drying technique[J].Int J Pharm,2016,502(1/2):38-46.
[12]刘娱姗,高署,柯学,等.难溶性药物固体分散体研究新进展[J].药学进展,2013,37(4):166-173.
[13]乔井会,郭建鹏,马艳,等.阿托伐他汀钙泊洛沙姆188固体分散体的制备及表征[J].中国药房,2015,26(1):103-106.