The preparation of self-microemulsifying dropping pills of paclitaxel and its drug release in vitro
-
摘要: 目的 研究紫杉醇自微乳滴丸的最佳制备工艺,考察其体外累积释药量。 方法 以自微乳与基质的比例、滴距、滴制温度、滴速为考察因素,采用正交试验法,以丸重差异、硬度、圆整度为指标,优选紫杉醇自微乳滴丸的最佳制备工艺,并进行体外累积释药的测定。 结果 优选的紫杉醇自微乳滴丸的最佳制备工艺:自微乳与基质配比为1:3,滴距15 cm,滴制温度80℃,滴速30滴/min。 结论 优选的工艺稳定、可行,制备的紫杉醇自微乳滴丸溶出度高。Abstract: Objective The research is about optimization of preparation procedure of self-microemulsifying dropping pills of paclitaxel (PTX-SM-DP). The drug release in vitro of PTX-SM-DP was investigated. Methods The ratio of SMEDDS and bases, dropping distance, temperature and speed of dripping were investigated by using the orthogonal test. The weight difference of dropping pill, hardness and roundness were evaluated to optimize the preparation conditions of PTX-SM-DP. Dissolution of vitro was determined. Results The optimal preparation conditions were as follows:the ratio of SMEDDS and bases was 1:3, dropping distance was 15 cm, temperature of dripping preparation was 80℃ and dripping speed was 30 drops/min. Conclusion The optimized technical condition is stable and feasible. PTX-SM-DP can improve paclitaxel dissolution.
-
Key words:
- paclitaxel /
- self-microemulsifying /
- dropping pills /
- orthogonal test /
- cumulative release
-
[1] 郭倩倩.紫杉醇纳米脂质体的研究进展[J]. 中国药科大学学报, 2014, 45(5):599-606. [2] El-Kareh AW, Labes RE, Secomb TW. Cell cycle checkpoint models for cellular pharmacology of paclitaxel and platinum drugs[J]. AAPS J, 2008, 10(1):15-34. [3] 马雪莲, 查晓, 张国楠. 卵巢癌紫杉醇耐药机制的研究进展[J]. 肿瘤预防与治疗, 2008, 21(4):436-439. [4] 周丽娟, 陈曦, 刘清飞, 等. 紫杉醇自微乳释药体系的处方工艺及稳定性研究[J]. 医药导报, 2014, 33(8):1063-1067. [5] Malingré MM, Beijnen JH, Schellens JH. Oral delivery of taxanes[J]. Invest New Drugs, 2001, 19(2):155-162. [6] Gursoy RN, Benita S. Self-emulsifying drug delivery systems(SEDDS)for improved oral delivery of lipophilic drugs[J].Biomed Pharmacother, 2004, 58(3):173-182. [7] Dosio F, Stella B, Arpicco S,et al. Macromolecules as taxane delivery systems[J]. Expert Opin Drug Deliv, 2011, 8(1):33-55. [8] 赵佳丽, 温许, 张晶, 等. 口服固体自微乳化给药系统的研究进展[J]. 药学实践杂志, 2014, 32(4):257-260. [9] 姚依婧, 郭秉玉, 韩静, 等.星点设计-效应面法优化紫杉醇自微乳给药系统[J]. 中南药学, 2014, 12(5):1069-1072. [10] 宋凤兰, 潘育方, 侯冬枝, 等. 葛根总黄酮滴丸的制备与溶出度研究[J]. 中草药, 2014, 45(9):1252-1256. [11] Wang B. Orthogonal test design for optimisation of extraction of trans-resveratrol from Pinot Noir-grape pomace[J]. Nat Prod Res, 2012, 26(9):821-829. [12] 周丽娟,曹巍,刘敏, 等. 正交试验法优化蒺藜防白缓释滴丸的制备工艺[J]. 中成药, 2015, 37(8):1704-1708. [13] 夏海建, 张振海, 徐凤娟, 等. 正交试验法优化黄芩苷缓释滴丸的制备工艺[J]. 中华中医药杂志, 2013, 28(10):2937-2941. [14] 国家药典委员会.中华人民共和国药典2010年版二部[S].北京:中国医药科技出版社,2010:1007-1008,附录,85-87.
计量
- 文章访问数: 3550
- HTML全文浏览量: 288
- PDF下载量: 653
- 被引次数: 0