陈秀莹1 黄健2 刘振华1 (1.武警总医院药局 北京100039; 2.军事医学科学院毒物药物研究所)
摘 要 目的：制备卡托普利缓释微丸，并对其处方工艺因素进行考察。方法：选用尤特奇RS 30 D与尤特奇RL 30 D的混合物作为包衣缓释材料，采用溶液层积法、流化床底喷方式，进行空白丸芯的上药和缓释包衣；并考察缓释聚合物尤特奇 RS 30D与尤特奇 RL 30D的不同比例、包衣增重，以及增塑剂用量对药物释放的影响。结果：当尤特奇 RS 30D与尤特奇 RL 30D的比例为4:1，包衣增重为10%，增塑剂用量为20%时，所制得的缓释微丸具有较好的缓释效果，在1、4和8 h的累积释放率分别为标示量的20%～35%，40%～65%和75%以上。结论：通过调整尤特奇RS 30D与尤特奇RL 30D之间的比例，或提高聚合物包衣增重等手段，能使卡托普利载药微丸具备较理想的缓释效果。
关键词 卡托普利；尤特奇RS 30D；尤特奇 RL 30D；缓释微丸
中图分类号：R944.9
文献标识码：A
文章编号：1008-049X(2007)08-0764-04
Preparation of Captopril Sustainedrelease Pellets and Study of the Formulation
Chen Xiuying1,Huang Jian2,Liu Zhenhua1（1.Department of Pharmacy, General Hospital of the Armed Police Force，Beijing 100039,China; 2.Institute of Pharmacology and Toxicology, Army Medical Academy）
ABSTRACT Objective: To prepare captopril sustained release pellets, and study the relevant process and formulation.Method: Mixed Eudragit RS 30D and Eudragit RL 30D was chosen as the sustained release coating material. Solution-layered method was employed to prepare both the drug loaded pellets and the sustained coating with fluid bed bottom spray (wutster insert); meanwhile, studied various influencing factors in coating formulation, including ratios of Eudragit RS 30D and Eudragit RL 30D, polymer weight gain and levels of plasticizer,etc, on the drug sustained-release behavior.Result: When ratio of Eudragit RS 30D and Eudragit RL 30D, polymer weight gain and level of plasticizer were 4∶1,10% and 20%, respectively, a ideal in vitro release behavior was reached, with the accumulated release percentage at 1,4 and 8h time intervals being 20%～35%，40%～65% and above 75% respectively.Conclusion: A ideal release behavior could be obtained by adjustment of the ratio between Eudragit RS 30D and Eudragit RL 30D, as well as altering polymer weight gain, etc.
KEY WORDS Couptopril; Eudragit RS 30D; Eudragit RL 30D; Sustained release pellets
参 考 文 献
1 Quarterman CP,Kendall MJ,Welling PG. Plasma levels and negative chronotropic effect of Atenolol following single doses of a conventional and sustainedrelease formulation［J］.Europ J Clin Pharmacol,1979,15(11):97-103
2 Schultz P,Kleinebudde P.A new mutiparticulate delayed release system.Part I:Dissolution properties and release mechanism ［J］.J Control Release 1997,47(9):181-189
3 Kramar A,Turk S, Vrecer F.Statistical optimization of diclofenac sustained release pellets coated with polymethacrylic films ［J］.Int J Pharm,2003,256(10):43-52
4 Maria A,Lippold BC,Schmitz A,et al.Aquesou ethylcellulose dispersion containing plasticeczers of different water solubility and hydroxypropyl methyl cellulose as coating material for diffusion pellets: I.Drug release rates from coated pellets ［J］.Int J Pharm,1999,177(1):69-82
5 Alkhatib HS,Sakr A.Optimization of methacrylic acid ester copolymers blends as controlled release coatings using response surface methodology ［J］.Pharm Dev Tech,2003,8(1):87-96
6 Hamed E,Sakr A.Effect of curing conditions and plasticizer level on the release of highly lipophilic drug from coated multiparticulate drug delivery system ［J］.Pharm Deve Tech,2003,8 (4):397-407
7 Shah VP, Sathe P,Tsong Y,et al.In Vitro Dissolution Profile ComparisonStatistics and Analysis of the Similarity Factor, f2 ［J］.Pharmaceutical Research,1998,15(6):889-896 资料来自:中国药师-专业站 |