非洛地平固体分散体缓释片的研制与优化
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摘要
为探讨非洛地平固体分散体缓释片的研制与优化,在单因素试验的基础上,采用正交试验设计的方法,对处方因素进行详细的考察,进一步优化处方工艺,并对按最优处方制备的样品进行验证.结果显示:优选的非洛地平固体分散体缓释片处方工艺合理,由其制备的缓释片体外释药2h释放度为20%~25%,4h释放度为44%~46%,8h释放度为78%~84%,12h释放度为96%~100%.
To improve the release of Felodipine,solid dispersion techniques were used,and a 12 hsustainedrelease drug was prepared with the solid dispersions.Solid dispersions(SD)were prepared by melting method with PEG6000 as a carrier.On the basis of the single factor test,the orthogonal test was conduct to get optimized formulation,which took two kinds of HPMC as sustained-release material,and sustainedrelease tablet was prepared by powder direct-compression method.Results show that the release of Felodipine was improved markedly with the solid dispersion techniques.Also,the drug release of self-made sustained-release tablet and the reference drug were consistent highly in vitro.the whole key quality of sustained-release tablet meet the requirements.It is concluded that the way that sustained-release drug were prepared with solid dispersions,which were made first to improve the dissolution of drug is a simple and feasible thought.
To improve the release of Felodipine,solid dispersion techniques were used,and a 12 hsustainedrelease drug was prepared with the solid dispersions.Solid dispersions(SD)were prepared by melting method with PEG6000 as a carrier.On the basis of the single factor test,the orthogonal test was conduct to get optimized formulation,which took two kinds of HPMC as sustained-release material,and sustainedrelease tablet was prepared by powder direct-compression method.Results show that the release of Felodipine was improved markedly with the solid dispersion techniques.Also,the drug release of self-made sustained-release tablet and the reference drug were consistent highly in vitro.the whole key quality of sustained-release tablet meet the requirements.It is concluded that the way that sustained-release drug were prepared with solid dispersions,which were made first to improve the dissolution of drug is a simple and feasible thought.
引文
[1]杨莹.高血压治疗的药物经济学分析[J].今日药学,2012,22(2):80-84.
[2]白树华,陈玉彬.二氢吡啶类钙拮抗剂研究的新进展[J].药学进展,1999,23(1):13-19.
[3]LEUNER C,DRESSMAN J.Improving Drug Solubility for Oral Delivery Using Solid Dispersions[J].Eur J30Pharm Biopharm,2000,50:47-60.
[4]SETHIA S,SQUILLANTE E.Solid Dispersion of Carbamazepine in PVP K30by Conventional Solvent Evaporation and Supercritical Methods[J].International Journal of Pharmaceutics,2004,272:1-10.
[5]ANANT P,AMBIKE AA,JADHAV B K,et al.Characterization of Curcumin-PVP Solid Dispersion Obtained by Spray Drying[J].International Journal of Pharmaceutics,2004,271:281-286.
[6]FORD J L,RUBINSTEIN M H.Aging of Indomethacin-Poly(Ethylene Glycol)6000Solid Dispersion[J].PharmActaHelv,1979,54(5):353-358.
[7]阮氏越秋,赵浩如.齐墩果酸固体分散体的制备及体外溶出度测定[J].中国药科大学学报,2003,34(3):236-239.
[8]NAKAMURA K,NARA E,AKIYAMA Y.Development of an Oral Sustained Release Drug Delivery System Utilizing pH-Dependent Swelling of Carboxyvinyl Polymer[J].J Control Release 2006,111(3):309-315.
[9]靖博宇,郑霞,何仲贵.非洛地平缓释片体外释药因素分析及释放度比较[J].海峡药学,2011(6):33-36.
[10]BACHRACH G,FRIEDMAN M,GILINSKI G,et al.Soluble Sustained Release Gene Delivery System[J].Jourmal of Biomedical Materials Research Part A,2006,77(4):811.
[11]廖娟,谭群友,熊华蓉.溴新斯的明1日2次缓释片的工艺优化及体外释放特性[J].重庆医科大学学报,2011,36(6):711-713.
[12]LONGER M A,CHNG H S,ROBINSON H S.Bioadhesive Polymers as Platforms for Oral Controlled Drug Delivery iii:Oral Delivery of Chlorotmazide Using a Bioadhesive Polymer[J].J Pharm Sci,1985,74(4):406-411.
[13]龚风阁.缓控释片剂的研究进展[J].天津药学,2010,22(5):57-59.
[14]ZHU S S,YUAN X J,LI Y X.Study on the Water-Soluble Composition Release of Compound Danshen Sustained-Release Tablet[J].Zhongguo Zhong Yao Za Zhi,2006,31(1):37-40.
[15]ZHANG S Q.Development and Evaluation of a ph-Dependent Sustained Release Tablet for iHitable Bowel Syndrome[J].Drug Development and Industrial Phannacy,2009,35:57-64.
[16]蒲道俊,徐洁,罗娟,等.熔融法制备盐酸二甲双胍缓释片及其稳定性考察[J].西南师范大学学报(自然科学版),2012,37(7):65-69.
[2]白树华,陈玉彬.二氢吡啶类钙拮抗剂研究的新进展[J].药学进展,1999,23(1):13-19.
[3]LEUNER C,DRESSMAN J.Improving Drug Solubility for Oral Delivery Using Solid Dispersions[J].Eur J30Pharm Biopharm,2000,50:47-60.
[4]SETHIA S,SQUILLANTE E.Solid Dispersion of Carbamazepine in PVP K30by Conventional Solvent Evaporation and Supercritical Methods[J].International Journal of Pharmaceutics,2004,272:1-10.
[5]ANANT P,AMBIKE AA,JADHAV B K,et al.Characterization of Curcumin-PVP Solid Dispersion Obtained by Spray Drying[J].International Journal of Pharmaceutics,2004,271:281-286.
[6]FORD J L,RUBINSTEIN M H.Aging of Indomethacin-Poly(Ethylene Glycol)6000Solid Dispersion[J].PharmActaHelv,1979,54(5):353-358.
[7]阮氏越秋,赵浩如.齐墩果酸固体分散体的制备及体外溶出度测定[J].中国药科大学学报,2003,34(3):236-239.
[8]NAKAMURA K,NARA E,AKIYAMA Y.Development of an Oral Sustained Release Drug Delivery System Utilizing pH-Dependent Swelling of Carboxyvinyl Polymer[J].J Control Release 2006,111(3):309-315.
[9]靖博宇,郑霞,何仲贵.非洛地平缓释片体外释药因素分析及释放度比较[J].海峡药学,2011(6):33-36.
[10]BACHRACH G,FRIEDMAN M,GILINSKI G,et al.Soluble Sustained Release Gene Delivery System[J].Jourmal of Biomedical Materials Research Part A,2006,77(4):811.
[11]廖娟,谭群友,熊华蓉.溴新斯的明1日2次缓释片的工艺优化及体外释放特性[J].重庆医科大学学报,2011,36(6):711-713.
[12]LONGER M A,CHNG H S,ROBINSON H S.Bioadhesive Polymers as Platforms for Oral Controlled Drug Delivery iii:Oral Delivery of Chlorotmazide Using a Bioadhesive Polymer[J].J Pharm Sci,1985,74(4):406-411.
[13]龚风阁.缓控释片剂的研究进展[J].天津药学,2010,22(5):57-59.
[14]ZHU S S,YUAN X J,LI Y X.Study on the Water-Soluble Composition Release of Compound Danshen Sustained-Release Tablet[J].Zhongguo Zhong Yao Za Zhi,2006,31(1):37-40.
[15]ZHANG S Q.Development and Evaluation of a ph-Dependent Sustained Release Tablet for iHitable Bowel Syndrome[J].Drug Development and Industrial Phannacy,2009,35:57-64.
[16]蒲道俊,徐洁,罗娟,等.熔融法制备盐酸二甲双胍缓释片及其稳定性考察[J].西南师范大学学报(自然科学版),2012,37(7):65-69.