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一种用于每日一次给药的新型缓释茶碱微丸制剂的药剂学开发。

Galenical development of a new sustained-release theophylline pellet formulation for once-daily administration.

作者信息

Benedikt G, Steinijans V W, Dietrich R

机构信息

Department of Galenical Development, Byk Gulden Research Center, Konstanz, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1988 Aug;38(8A):1203-9.

PMID:3190808
Abstract

Euphylong is a sustained-release product consisting of encapsulated pellets covered with a porous membrane. Since the mechanism of release is osmotic, this new formulation has been termed a "micro-osmotic system". The course of theophylline release is linear over a wide range and is independent of pH value, surface tension and buffer concentration of the dissolution medium. Furthermore, the in-vitro release remains largely uninfluenced by the dissolution model used and by agitation of the dissolution medium. Variations in the in-vitro release profiles produce variations in the in-vivo absorption profiles determined by deconvolution. It is therefore possible, irrespective of the dissolution model and medium used, to produce in-vitro release profiles that enable in-vivo absorption to be predicted by varying the thickness or porosity of the membrane.

摘要

优菲龙是一种缓释产品,由包裹着多孔膜的包衣小丸组成。由于释放机制是渗透作用,这种新剂型被称为“微渗透系统”。茶碱的释放过程在很宽的范围内呈线性,且与溶出介质的pH值、表面张力和缓冲液浓度无关。此外,体外释放很大程度上不受所用溶出模型和溶出介质搅拌的影响。体外释放曲线的变化会导致通过反卷积确定的体内吸收曲线发生变化。因此,无论使用何种溶出模型和介质,都可以通过改变膜的厚度或孔隙率来产生能够预测体内吸收的体外释放曲线。

相似文献

1
Galenical development of a new sustained-release theophylline pellet formulation for once-daily administration.一种用于每日一次给药的新型缓释茶碱微丸制剂的药剂学开发。
Arzneimittelforschung. 1988 Aug;38(8A):1203-9.
2
Validation of the in-vitro dissolution method used for a new sustained-release theophylline pellet formulation.用于新型缓释茶碱微丸制剂的体外溶出方法的验证
Arzneimittelforschung. 1988 Aug;38(8A):1220-8.
3
Pharmacokinetic profile of a new sustained-release theophylline pellet formulation for once-daily evening administration.一种用于每日一次晚间给药的新型缓释茶碱微丸制剂的药代动力学特征。
Arzneimittelforschung. 1988 Aug;38(8A):1241-50.
4
In-vitro and in-vivo evaluation of enteric-coated starch-based pellets prepared via extrusion/spheronisation.通过挤出/滚圆法制备的肠溶包衣淀粉基微丸的体外和体内评价
Eur J Pharm Biopharm. 2008 Sep;70(1):302-12. doi: 10.1016/j.ejpb.2008.04.019. Epub 2008 Apr 29.
5
Feasibility of in-vitro/in-vivo correlation in the case of a new sustained-release theophylline pellet formulation.一种新型缓释茶碱微丸制剂的体外/体内相关性研究的可行性
Arzneimittelforschung. 1988 Aug;38(8A):1229-37.
6
[Comparison of the bioavailability and pharmacokinetic profile of a theophylline pellet formulation designed for once-daily dosage with a pellet preparation designed for twice-daily dosage].[设计用于每日一次给药的茶碱微丸制剂与设计用于每日两次给药的微丸制剂的生物利用度和药代动力学特征比较]
Arzneimittelforschung. 1989 Nov;39(11):1460-4.
7
Euphylong. A new sustained-release theophylline pellet formulation for once-daily evening administration.优菲龙。一种用于每晚一次给药的新型茶碱缓释微丸制剂。
Arzneimittelforschung. 1988 Aug;38(8A):1199-256.
8
Theophylline therapeutic drug monitoring in the case of a new sustained-release pellet formulation for once-daily evening administration.对于一种用于每日一次晚间给药的新型缓释微丸制剂的茶碱治疗药物监测。
Arzneimittelforschung. 1988 Aug;38(8A):1251-3.
9
In vitro and in vivo sustained-release characteristics of theophylline matrix tablets and novel cluster tablets.茶碱基质片和新型簇片的体外及体内缓释特性
Int J Pharm. 2007 Aug 16;341(1-2):105-13. doi: 10.1016/j.ijpharm.2007.03.048. Epub 2007 Apr 5.
10
Absorption of theophylline from a sustained-release theophylline tablet formulation, Theo-Dur.来自缓释茶碱片剂制剂Theo-Dur的茶碱吸收情况。
Int J Clin Pharmacol Ther Toxicol. 1987 Oct;25(10):530-5.

引用本文的文献

1
In vivo/in vitro correlation of experimental sustained-release theophylline formulations.
Pharm Res. 1993 Apr;10(4):588-92. doi: 10.1023/a:1018910421840.
2
Novel oral drug formulations. Their potential in modulating adverse effects.新型口服药物制剂。它们在调节不良反应方面的潜力。
Drug Saf. 1994 Mar;10(3):233-66. doi: 10.2165/00002018-199410030-00005.
3
Controversies in bioequivalence studies.生物等效性研究中的争议
Clin Pharmacokinet. 1992 Apr;22(4):247-53. doi: 10.2165/00003088-199222040-00001.