Preparation and in vitro Release Behavior of Methylphenidate Hydrochlori Desustained-release Capsules_West China Medical Journal

Authors：

1. Department of Pharmacy, General Hospital of Chengdu Military Region, Chengdu, Sichuan 610083, P. R. China; 2. Department of Pharmacy, Chinese People’s Liberation Army of 96630 Troops, Beijing 102206, P. R. China; 3. Department of Orthopedics, General Hospital of Chengdu Military Region, Chengdu, Sichuan 610083, P. R. China; 4. Department of Pharmacy, Changhai Hospital, the Second Military Medical University, Shanghai 200433, P. R. China;

Corresponding author：

Keywords：

盐酸哌甲酯; 缓释微丸; 双层择时缓释微丸; 体外释放

DOI：

10.7507/1002-0179.20130542

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目的　制备一种盐酸哌甲酯（MPH）缓释微丸胶囊剂，并与进口控释片专注达?体外释放情况进行比较研究。方法　利用流化床包衣技术制备一种含有3种不同释药速率微丸的MPH缓释微丸胶囊剂：将部分载药微丸包保护层后制成速释微丸；以乙基纤维素（Surelease?）为缓释材料制备单层缓释微丸；通过内包溶胀层（欧巴代-7006，主成分为低黏度羟丙基甲基纤维素（HPMC），外加控释层制备具有时滞的双层择时缓释微丸。在模拟胃肠道pH值介质中比较自制胶囊剂与控释片的体外释药情况。结果　载药微丸实际载药量6.85%。单层缓释微丸包衣增重14%；双层择时缓释微丸溶胀层包衣增重16%，控释层包衣增重22%，时滞约3.5 h。3种微丸按以下比例混合后装胶囊：速释微丸含MPH 22%，单层缓释微丸含MPH 39%，双层择时缓释微丸含MPH 39%。该胶囊剂1 h释放可达25%，4 h释放约50%，12 h释放＞95%。两制剂在模拟胃肠道介质中的释放曲线相似。结论　制备出一种由3种微丸组成的，能连续12 h释药的MPH缓释微丸胶囊剂，其工艺简单，与进口控释片专注达?有相同的体外释放效果。

Citation： WU Juan,ZHANG Min,ZHENG Wei,GAO Shen.. Preparation and in vitro Release Behavior of Methylphenidate Hydrochlori Desustained-release Capsules. West China Medical Journal, 2013, 28(11): 1719-1725. doi: 10.7507/1002-0179.20130542 Copy

1.	陈光福, 崔艳丽, 陈美清.盐酸哌甲酯控释剂治疗儿童注意缺陷多动障碍的疗效[J]. 实用儿科临床杂志, 2011, 26(6): 452-459.
2.	Coghill D, Banaschewski T, Zuddas A, et al. Long-acting methylphenidate formulations in the treatment of attention-deficit/hyperactivity disorder: a systematic review of head-to-head studies[J]. BMC Psychiatry, 2013, 13(1): 237.
3.	Gormez V, Avery B, Mann H. Switching from immediate release to sustained release methylphenidate in the treatment of children and adolescents with attention deficit/hyperactivity disorder[J]. Eur Rev Med Pharmacol Sci, 2013, 17(17): 2345-2349.
4.	陈挺, 靳松, 陈庆华.乙基纤维素水分散体包衣微丸的体外释药特性研究[J].中国药科大学, 2000, 31(1): 25-28.
5.	杜璇, 屠锡德, 周建平. 硝苯地平延迟起释型缓释片的制备及体外释放[J] 中国药科大学学报, 2008, 39(5): 412-416.
6.	Ueda S, Hata T, Asakura S, et al. Development of a novel drug release system, time-controlled explosion system(TES).Ⅰ. Concept and design[J]. J Drug Target. 1994, 2(1): 35-44.
7.	郭涛, 郑春丽, 宋洪涛, 等.双氯芬酸钠脉冲控释微丸的研究[J]. 药学学报, 2003, 38(9): 707-710.
8.	陈志鹏,肖衍宇,陈洪轩, 等.盐酸维拉帕米择时缓释微丸的研制及犬体内药代动力学[J]. 药学学报, 2006, 41(8): 765-771.
9.	Maffione G, Iamartino P, Guglielmini G. et al. High-viscosity HPMC as a film-coating agent[J]. Drug Dev Ind Pharm, 1993, 19(16): 2043-2053.
10.	谢齐昂, 胡富强, 袁弘. 酒石酸唑吡坦双脉冲控释微丸的研制[J].中国药学杂志, 2009, 44(17): 1312-1320.
11.	陈燕忠, 张纪兴, 吕竹芬. 硫酸特布他林脉冲控释微丸的制备[J]. 中国药科大学学报, 2004, 35(4): 307-310.
12.	Cole G, Hogan J, Aulton M. 片剂包衣的工艺和原理[M].郑俊民, 译. 北京: 中国医药科技出版社, 2000: 8.
13.	Meunier JP, Cardot JM, Gauthier P, et al. Use of rotary fluidized-bed technology for development of sustained-release plant extracts pellets: potential application for feed additive delivery[J]. J Anim Sci, 2006, 84(7): 1850-1859.
14.	陈挺. 聚合物水性包衣技术在缓释制剂上的应用研究[D]. 上海: 上海医药工业研究院, 1998.
15.	WagneR K, Bodmeier R. Improvement of the low-temperature stability of an aqueous colloidal ethylcellulose dispersion, Aquacoat ECD, and preparation/characterization of a redispersible Aquacoat ECD powder[J]. Drug Dev Ind Pharm, 2003, 29(3): 267-275.
16.	Sadeghi F, Ford JL, Rajabi-Siahboomi A. The influence of drug type on the release profiles from Surelease-coated pellets[J]. Int J Pharm, 2003, 254(2): 123-135.
17.	陈挺, 陈庆华.乙基纤维素水性包衣技术Ⅱ. 热处理对衣膜性质的影响[J].中国医药工业杂志, 2000, 31(7): 298-301.

1. 　陈光福, 崔艳丽, 陈美清.盐酸哌甲酯控释剂治疗儿童注意缺陷多动障碍的疗效[J]. 实用儿科临床杂志, 2011, 26(6): 452-459.
2. 　Coghill D, Banaschewski T, Zuddas A, et al. Long-acting methylphenidate formulations in the treatment of attention-deficit/hyperactivity disorder: a systematic review of head-to-head studies[J]. BMC Psychiatry, 2013, 13(1): 237.
3. 　Gormez V, Avery B, Mann H. Switching from immediate release to sustained release methylphenidate in the treatment of children and adolescents with attention deficit/hyperactivity disorder[J]. Eur Rev Med Pharmacol Sci, 2013, 17(17): 2345-2349.
4. 　陈挺, 靳松, 陈庆华.乙基纤维素水分散体包衣微丸的体外释药特性研究[J].中国药科大学, 2000, 31(1): 25-28.
5. 　杜璇, 屠锡德, 周建平. 硝苯地平延迟起释型缓释片的制备及体外释放[J] 中国药科大学学报, 2008, 39(5): 412-416.
6. 　Ueda S, Hata T, Asakura S, et al. Development of a novel drug release system, time-controlled explosion system(TES).Ⅰ. Concept and design[J]. J Drug Target. 1994, 2(1): 35-44.
7. 　郭涛, 郑春丽, 宋洪涛, 等.双氯芬酸钠脉冲控释微丸的研究[J]. 药学学报, 2003, 38(9): 707-710.
8. 　陈志鹏,肖衍宇,陈洪轩, 等.盐酸维拉帕米择时缓释微丸的研制及犬体内药代动力学[J]. 药学学报, 2006, 41(8): 765-771.
9. 　Maffione G, Iamartino P, Guglielmini G. et al. High-viscosity HPMC as a film-coating agent[J]. Drug Dev Ind Pharm, 1993, 19(16): 2043-2053.
10. 　谢齐昂, 胡富强, 袁弘. 酒石酸唑吡坦双脉冲控释微丸的研制[J].中国药学杂志, 2009, 44(17): 1312-1320.
11. 　陈燕忠, 张纪兴, 吕竹芬. 硫酸特布他林脉冲控释微丸的制备[J]. 中国药科大学学报, 2004, 35(4): 307-310.
12. 　Cole G, Hogan J, Aulton M. 片剂包衣的工艺和原理[M].郑俊民, 译. 北京: 中国医药科技出版社, 2000: 8.
13. 　Meunier JP, Cardot JM, Gauthier P, et al. Use of rotary fluidized-bed technology for development of sustained-release plant extracts pellets: potential application for feed additive delivery[J]. J Anim Sci, 2006, 84(7): 1850-1859.
14. 　陈挺. 聚合物水性包衣技术在缓释制剂上的应用研究[D]. 上海: 上海医药工业研究院, 1998.
15. 　WagneR K, Bodmeier R. Improvement of the low-temperature stability of an aqueous colloidal ethylcellulose dispersion, Aquacoat ECD, and preparation/characterization of a redispersible Aquacoat ECD powder[J]. Drug Dev Ind Pharm, 2003, 29(3): 267-275.
16. 　Sadeghi F, Ford JL, Rajabi-Siahboomi A. The influence of drug type on the release profiles from Surelease-coated pellets[J]. Int J Pharm, 2003, 254(2): 123-135.
17. 　陈挺, 陈庆华.乙基纤维素水性包衣技术Ⅱ. 热处理对衣膜性质的影响[J].中国医药工业杂志, 2000, 31(7): 298-301.

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West China Medical Journal

Preparation and in vitro Release Behavior of Methylphenidate Hydrochlori Desustained-release Capsules

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