盐酸地匹福林眼用凝胶剂的研究
王丽茹1，张强2
(1 浙江医药股份有限公司新昌制药厂，新昌 312500；2 北京大学药学院药剂研究室，北京 100083)
[摘要] 目的:研制盐酸地匹福林眼用凝胶剂。 方法:建立高效液相色谱法测定制剂的含量及体外释药量，采用透析膜扩散法进行处方的体外释药实验，应用离体角膜进行体外渗透实验。 结果:亲水凝胶材料含量越小，盐酸地匹福林从凝胶基质中释放越快，凝胶体外释药符合一级释放动力学方程，离体角膜渗透行为符合一级释放规律。 结论:盐酸地匹福林眼用凝胶达到了延迟释放的目的。
[关键词] 盐酸地匹福林；凝胶剂；高效液相色谱法；体外释放；离体角膜渗透
[中图分类号] R944.9；R927.2 [文献标识码] B [文章编号] 1003-3734(2001)
, 百拇医药
The study of dipivefrin hydrochloride ophthalmic gel-forming solution
WANG Li-ru 1, ZHANG Qiang2
(1 Xinchang Pharmaceutical factory,Zhejiang Medical Co., Ltd, Xinchang 312500, China; 2 Department of Pharmaceutics ,Schoool of Pharmaceutical Sciences, Peking University , Beijing 100083，China)
[Abstract] Objective: To study dipivefrin hydrochloride ophthalmic gel-forming solution. Methods: The release test of formation was conducteded by using permeable membrane. The content and the release amount of dipivefrin hydrochloride from the gel base were determined by high performance liquid chromatography. The cornea permeation test of formulation was studied by using rabbit corneas. Results: The formulation release behavior in vitro followed the first-order kinetic equation. The permeabilities of dipivefrin hydrochloride were raised significantly with the less amount of polymer in the formulation. The formulation permeation behavior in vitro followed the first-order kinetic equation. Conclusion: Dipivefrin ophthalmic gel-forming has longer release time than that of eyedrops.
, 百拇医药
[Key words] dipivefrin hydrochloride； Gel-forming solution； HPLC； Release in vitro；Corneal perfusion in vitro
[作者简介] 王丽茹(1973- )，女，硕士，主要从事药物制剂研究。联系电话(0575)6024773。
[参考文献]
[1] 武志坚,李美玉. 抗青光眼新药物的合理应用[J]. 中华眼科杂志,1998,34(3)：235-240.
[2] Pheyer U, Milani SK, Dukes A, et al. Effect of topically applied anti-CD4 nomoclonal antibodies on orthotopic corneal allografts in rat model[J]. Invest Ophthalmol Vis Sci, 1995,36(1):52-61.
, 百拇医药
[3] Pekka J, Krisriina J, Arto U, et al. The use of cyclodextrins in ophthalmic formulation of dipivefrin[J]. Inter J Pharm，1997,153(2):225-233.
[4] Durrani AM, Farr SJ, Kellaway IW. Influence of molecular weight and formulation pH on the precorneal clearance rate of hyaluronic acid in rabbit eye[J]. Inter J Pharm, 1995,118(16):243-250.
[5] Marchal-Heussler L, Maincent P, Hoffman M, et al. Antiglaucomatous activity of betaxolos chlorhydrate sorbed onto different isobutyl-cyanoacrylate nanoparticles preparations[J]. Inter J Pharm,1996,58(29):115-122.
, 百拇医药
[6] Durrani AM, Farr SJ, Kellauay IW. Precorneal clearance of mucoadhesive microsphere from the rabbit eye[J]. J Pharm Pharmacol,1995,47(7):581-584.
[7] Joseph BR, Diane DS， Tang-liu. A corneal perfusion device for estimating ocular bioavailability in vitro[J]. J Pharm Sci，1990,79(2):153-157.
[8] 魏树礼. 生物药剂学和药物动力学[M]. 北京：北京医科大学/北京协和医科大学联合出版社.1997,184-185.
[9] Foroutan SM, Watson DG. The in vitro evaluation of polyethylene glycol esters of hydrocortisone 21-succinate as ocular prodrugs[J]. Int J Pharm,1999,182(2):79-92.
[10] Forrester JV, Dick AD, Mcmenamin P, et al. The eye basic sciences in practice[M]. W.B.Saumders; London ,1996,137-198.
[11] Ahmed I, Patton TF. Disposition of timolol and insulin in the rabbit non-corneal absorption[J]. Inter J Pharm, 1987,38(1):9-21., http://www.100md.com
(1 浙江医药股份有限公司新昌制药厂，新昌 312500；2 北京大学药学院药剂研究室，北京 100083)
[摘要] 目的:研制盐酸地匹福林眼用凝胶剂。 方法:建立高效液相色谱法测定制剂的含量及体外释药量，采用透析膜扩散法进行处方的体外释药实验，应用离体角膜进行体外渗透实验。 结果:亲水凝胶材料含量越小，盐酸地匹福林从凝胶基质中释放越快，凝胶体外释药符合一级释放动力学方程，离体角膜渗透行为符合一级释放规律。 结论:盐酸地匹福林眼用凝胶达到了延迟释放的目的。
[关键词] 盐酸地匹福林；凝胶剂；高效液相色谱法；体外释放；离体角膜渗透
[中图分类号] R944.9；R927.2 [文献标识码] B [文章编号] 1003-3734(2001)
, 百拇医药
The study of dipivefrin hydrochloride ophthalmic gel-forming solution
WANG Li-ru 1, ZHANG Qiang2
(1 Xinchang Pharmaceutical factory,Zhejiang Medical Co., Ltd, Xinchang 312500, China; 2 Department of Pharmaceutics ,Schoool of Pharmaceutical Sciences, Peking University , Beijing 100083，China)
[Abstract] Objective: To study dipivefrin hydrochloride ophthalmic gel-forming solution. Methods: The release test of formation was conducteded by using permeable membrane. The content and the release amount of dipivefrin hydrochloride from the gel base were determined by high performance liquid chromatography. The cornea permeation test of formulation was studied by using rabbit corneas. Results: The formulation release behavior in vitro followed the first-order kinetic equation. The permeabilities of dipivefrin hydrochloride were raised significantly with the less amount of polymer in the formulation. The formulation permeation behavior in vitro followed the first-order kinetic equation. Conclusion: Dipivefrin ophthalmic gel-forming has longer release time than that of eyedrops.
, 百拇医药
[Key words] dipivefrin hydrochloride； Gel-forming solution； HPLC； Release in vitro；Corneal perfusion in vitro
[作者简介] 王丽茹(1973- )，女，硕士，主要从事药物制剂研究。联系电话(0575)6024773。
[参考文献]
[1] 武志坚,李美玉. 抗青光眼新药物的合理应用[J]. 中华眼科杂志,1998,34(3)：235-240.
[2] Pheyer U, Milani SK, Dukes A, et al. Effect of topically applied anti-CD4 nomoclonal antibodies on orthotopic corneal allografts in rat model[J]. Invest Ophthalmol Vis Sci, 1995,36(1):52-61.
, 百拇医药
[3] Pekka J, Krisriina J, Arto U, et al. The use of cyclodextrins in ophthalmic formulation of dipivefrin[J]. Inter J Pharm，1997,153(2):225-233.
[4] Durrani AM, Farr SJ, Kellaway IW. Influence of molecular weight and formulation pH on the precorneal clearance rate of hyaluronic acid in rabbit eye[J]. Inter J Pharm, 1995,118(16):243-250.
[5] Marchal-Heussler L, Maincent P, Hoffman M, et al. Antiglaucomatous activity of betaxolos chlorhydrate sorbed onto different isobutyl-cyanoacrylate nanoparticles preparations[J]. Inter J Pharm,1996,58(29):115-122.
, 百拇医药
[6] Durrani AM, Farr SJ, Kellauay IW. Precorneal clearance of mucoadhesive microsphere from the rabbit eye[J]. J Pharm Pharmacol,1995,47(7):581-584.
[7] Joseph BR, Diane DS， Tang-liu. A corneal perfusion device for estimating ocular bioavailability in vitro[J]. J Pharm Sci，1990,79(2):153-157.
[8] 魏树礼. 生物药剂学和药物动力学[M]. 北京：北京医科大学/北京协和医科大学联合出版社.1997,184-185.
[9] Foroutan SM, Watson DG. The in vitro evaluation of polyethylene glycol esters of hydrocortisone 21-succinate as ocular prodrugs[J]. Int J Pharm,1999,182(2):79-92.
[10] Forrester JV, Dick AD, Mcmenamin P, et al. The eye basic sciences in practice[M]. W.B.Saumders; London ,1996,137-198.
[11] Ahmed I, Patton TF. Disposition of timolol and insulin in the rabbit non-corneal absorption[J]. Inter J Pharm, 1987,38(1):9-21., http://www.100md.com