盐酸二甲双胍缓释微囊的制备

盐酸二甲双胍缓释微囊的制备

刘宏飞, 苏显英, 李想, 赵欣, 臧蕾, 潘卫三^*

1.沈阳药科大学药学院, 辽宁沈阳 110016;
2.东北制药集团沈阳市第一制药厂, 辽宁沈阳 110023

收稿日期:2006-02-12 修回日期:2006-08-10 出版日期:2006-09-15 发布日期:2006-09-15
通讯作者: 潘卫三*

Development of Prolonged Release Microspheres of Metformin Hydrochloride Using Ion Exchange Resins

LIU Hong-fei, SU Xian-ying, LI Xiang, ZHAO Xin, ZANG Lei, PAN Wei-san^*

1.Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China;
2.Institute of Material Medica, Shenyang No.1 Pharmaceutical Factory, Shenyang 110023, China

Received:2006-02-12 Revised:2006-08-10 Online:2006-09-15 Published:2006-09-15
Contact: PAN Wei-san*

摘要/Abstract

摘要： 目的制备盐酸二甲双胍缓释微囊。方法以自制的离子交换树脂-药物复合物作为核心材料, 乙基纤维素(EC)做为包衣材料, 用乳化溶剂扩散法制备了盐酸二甲双胍的缓释微囊。以药物的释放百分率作为单因素考察指标, 用正交实验优化包衣处方。结果处方组成为EC(20cps)∶EC(45cps) = 50∶50, 增塑剂∶包衣材料 = 1∶5, 药物树脂复合物∶包衣材料 = 5∶1。结论成功制备了具有明显缓释特性的盐酸二甲双胍药物树脂微囊。,

关键词: 盐酸二甲双胍, 盐酸二甲双胍, 盐酸二甲双胍, 离子交换树脂, 离子交换树脂, 离子交换树脂, 乳化溶剂扩散法, 乳化溶剂扩散法, 乳化溶剂扩散法, 缓释微囊, 缓释微囊, 缓释微囊

Abstract: Aim To prepare the prolonged-released microspheres of metformin hydrochloride. Methods Ion-exchange resin-drug metformin hydrochloride complexes were prepared as core materials, and followed by coating using ethylcellulose (EC) by the emulsion solvent diffusion technique. The release rate of metformin from the microcapsules was highly dependent on the encapsulating formulation, thus being used as an index for formulation screening. Orthogonal experiments were performed to optimize the coating formulation. Results The final chosen formulation for coating of metformin microcapsules were as follows: (1) the ratio of EC (20cps) to EC (45cps) was 50:50; (2) the ratio of plasticizer to coating materials was 20%; and (3) the ratio of resin-metformin complexes to coating materials was 5:1. Conclusion The prolonged release microspheres of metformin hydrochloride were successfully prepared.

Key words: metformin hydrochloride, metformin hydrochloride, ion exchange resin, ion exchange resin, emulsion solvent diffusion technique, emulsion solvent diffusion technique, sustained-release microcapsule, sustained-release microcapsule

中图分类号:

R943.41

Supporting: ^*Corresponding author. Tel.: 86-24-23953241

刘宏飞, 苏显英, 李想, 赵欣, 臧蕾, 潘卫三^*. 盐酸二甲双胍缓释微囊的制备[J]. .

LIU Hong-fei, SU Xian-ying, LI Xiang, ZHAO Xin, ZANG Lei, PAN Wei-san^*. Development of Prolonged Release Microspheres of Metformin Hydrochloride Using Ion Exchange Resins[J]. .

参考文献

[1] Geetha RCG, Motiwale AV, Yanarayana DS, et al. Formulation of taste masked oral suspension of quinine sulphate by complexation [J]. Indian J Pharm Sci, 2004, (3-4) : 329–331.
[2] Perumal D. Microencap sulation of ibup rofen and Eudragit RS 100 by the emulsion solvent diffusion technique [J]. Int J Pharm , 2001, 218 (1-2) : 1–11.
[3] Atyabi F, Sharma HL, Mohammad HAH, et al. Controlled drug release from floating ion exchange resin beads [J]. J Controlled Release, 1996, 42 (1) : 25–28.
[4] Hideki, Ichikawa, Kazuhiro, et al. Use of ion-exchange resins to p repare 100 μm-sized microcapsules with prolonged drug-release by the Wurster process [J]. Int J Pharm , 2001, 216 (1-2) : 67–76.
[5] Plaizier-Vercammen JA. Investigation of the bioavailability of codeine from a cation ion-exchange sulfonic acid 1. Effect of parameters [J]. Int J Pharm , 1992, 85 (1-3) : 45–50.
[6] Klepser TB, Kelly MW. Metformin hydrochloride: an antihyperglycemic [J]. Am J Health Syst Pharm , 1997, 54 (10) : 893–896.
[7] Vuorio M, Murtomakl L, Hirvonen J, et al. Ion-exchange fibers and drugs: a novel device for the screening of iontophoretic systems [J]. J Controlled Release, 2004, 97 (3) : 485–492.
[8] Mongokol, Sriwongjanya, Roland, et al. Effect of ion exchange resins on the drug release from matrix tablets [J]. Eur J Pharm Biopharm , 1998, 46 (3) : 321–327.
[9] Akkaramongkolporn P, Ngawhirunpat T. Dual ambroxol and chlorpheniramine resinates as an alternative carrier in concurrent resinate administration [J]. Phamazie, 2003, 58 (3) : 195–199.
[10] Sambol NC, Chiang JO, ConnerM. Pharmacokinetics and pharmacodynamics of metformin in healthy subjects and patients with noninsulin-dependent diabetesmellitus [J]. J Clin Pharmacol, 1996, 36 (11) : 1012–1021.
[11] Skaikh NA, Abidi SE, Block LH. Evaluation of ethylcellulose as a matrix for prolonged release formulation. Sparingly water-soluble drugs: ibuprofen and indomethacin [J]. Drug Dev Ind Pharm , 1987, 13 (14) : 2495–2499.
[12] Torres D, Garcia-Encina G, Seijo B. Biopharmaceutical evaluation of microencap sulated ion-exchange resins containing theophylline [J]. J Pharm Biopharm , 1995, 21 (1) : 127–132.
[13] Irwin WJ , Machale R, Watts PJ. Drug-delivery by ion-exchange, part Ⅶ: release of acidic drugs from anionic exchange resinate comp lexes [J]. Drug Dev Ind Pharm, 1990, 16 (6) : 883–898.
[14] Yahya, Farag J, Graham, N. Rate of release of organic carboxylic acids from ion-exchange resins [J]. J Pharm Sci, 1988, 77 (10) : 872–875.