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：

鹽酸哌甲酯; 緩釋微丸; 雙層擇時緩釋微丸; 體外釋放

DOI：

10.7507/1002-0179.20130542

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目的　制備一種鹽酸哌甲酯（MPH）緩釋微丸膠囊劑，并與進口控釋片專注達?體外釋放情況進行比較研究。方法　利用流化床包衣技術制備一種含有3種不同釋藥速率微丸的MPH緩釋微丸膠囊劑：將部分載藥微丸包保護層后制成速釋微丸；以乙基纖維素（Surelease?）為緩釋材料制備單層緩釋微丸；通過內包溶脹層（歐巴代-7006，主成分為低黏度羥丙基甲基纖維素（HPMC），外加控釋層制備具有時滯的雙層擇時緩釋微丸。在模擬胃腸道pH值介質中比較自制膠囊劑與控釋片的體外釋藥情況。結果　載藥微丸實際載藥量6.85%。單層緩釋微丸包衣增重14%；雙層擇時緩釋微丸溶脹層包衣增重16%，控釋層包衣增重22%，時滯約3.5 h。3種微丸按以下比例混合后裝膠囊：速釋微丸含MPH 22%，單層緩釋微丸含MPH 39%，雙層擇時緩釋微丸含MPH 39%。該膠囊劑1 h釋放可達25%，4 h釋放約50%，12 h釋放＞95%。兩制劑在模擬胃腸道介質中的釋放曲線相似。結論　制備出一種由3種微丸組成的，能連續12 h釋藥的MPH緩釋微丸膠囊劑，其工藝簡單，與進口控釋片專注達?有相同的體外釋放效果。

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.	陳光福, 崔艷麗, 陳美清.鹽酸哌甲酯控釋劑治療兒童注意缺陷多動障礙的療效[J]. 實用兒科臨床雜志, 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.	陳挺, 靳松, 陳慶華.乙基纖維素水分散體包衣微丸的體外釋藥特性研究[J].中國藥科大學, 2000, 31(1): 25-28.
5.	杜璇, 屠錫德, 周建平. 硝苯地平延遲起釋型緩釋片的制備及體外釋放[J] 中國藥科大學學報, 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.	郭濤, 鄭春麗, 宋洪濤, 等.雙氯芬酸鈉脈沖控釋微丸的研究[J]. 藥學學報, 2003, 38(9): 707-710.
8.	陳志鵬,肖衍宇,陳洪軒, 等.鹽酸維拉帕米擇時緩釋微丸的研制及犬體內藥代動力學[J]. 藥學學報, 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.	謝齊昂, 胡富強, 袁弘. 酒石酸唑吡坦雙脈沖控釋微丸的研制[J].中國藥學雜志, 2009, 44(17): 1312-1320.
11.	陳燕忠, 張紀興, 呂竹芬. 硫酸特布他林脈沖控釋微丸的制備[J]. 中國藥科大學學報, 2004, 35(4): 307-310.
12.	Cole G, Hogan J, Aulton M. 片劑包衣的工藝和原理[M].鄭俊民, 譯. 北京: 中國醫藥科技出版社, 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.	陳挺. 聚合物水性包衣技術在緩釋制劑上的應用研究[D]. 上海: 上海醫藥工業研究院, 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.	陳挺, 陳慶華.乙基纖維素水性包衣技術Ⅱ. 熱處理對衣膜性質的影響[J].中國醫藥工業雜志, 2000, 31(7): 298-301.

1. 　陳光福, 崔艷麗, 陳美清.鹽酸哌甲酯控釋劑治療兒童注意缺陷多動障礙的療效[J]. 實用兒科臨床雜志, 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. 　陳挺, 靳松, 陳慶華.乙基纖維素水分散體包衣微丸的體外釋藥特性研究[J].中國藥科大學, 2000, 31(1): 25-28.
5. 　杜璇, 屠錫德, 周建平. 硝苯地平延遲起釋型緩釋片的制備及體外釋放[J] 中國藥科大學學報, 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. 　郭濤, 鄭春麗, 宋洪濤, 等.雙氯芬酸鈉脈沖控釋微丸的研究[J]. 藥學學報, 2003, 38(9): 707-710.
8. 　陳志鵬,肖衍宇,陳洪軒, 等.鹽酸維拉帕米擇時緩釋微丸的研制及犬體內藥代動力學[J]. 藥學學報, 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. 　謝齊昂, 胡富強, 袁弘. 酒石酸唑吡坦雙脈沖控釋微丸的研制[J].中國藥學雜志, 2009, 44(17): 1312-1320.
11. 　陳燕忠, 張紀興, 呂竹芬. 硫酸特布他林脈沖控釋微丸的制備[J]. 中國藥科大學學報, 2004, 35(4): 307-310.
12. 　Cole G, Hogan J, Aulton M. 片劑包衣的工藝和原理[M].鄭俊民, 譯. 北京: 中國醫藥科技出版社, 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. 　陳挺. 聚合物水性包衣技術在緩釋制劑上的應用研究[D]. 上海: 上海醫藥工業研究院, 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. 　陳挺, 陳慶華.乙基纖維素水性包衣技術Ⅱ. 熱處理對衣膜性質的影響[J].中國醫藥工業雜志, 2000, 31(7): 298-301.

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

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