纤维素聚合物对醋酸氢化可的松过饱和度及体外膜转运的影响。

Effect of cellulose polymers on supersaturation and in vitro membrane transport of hydrocortisone acetate.

作者信息

Raghavan S L, Trividic A, Davis A F, Hadgraft J

机构信息

The Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff, UK.

出版信息

Int J Pharm. 2000 Jan 5;193(2):231-7. doi: 10.1016/s0378-5173(99)00345-2.

DOI:10.1016/s0378-5173(99)00345-2

PMID:10606787

Abstract

A systematic investigation on the influence of two cellulose polymers, methyl cellulose (MC) and hydroxypropyl cellulose (HPMC) on supersaturation and permeation of hydrocortisone acetate (HA) is reported. Diffusion of HA from a 0.5% Carbopol gel across a model silicone membrane was investigated using the Franz-cell technique. At constant polymer concentration, the flux increases proportionally with the degree of saturation up to 4.8x but decreases thereafter. For a particular degree of supersaturation (4.8x), the flux increases with the concentration of polymer up to 1% and decreases at higher concentrations. The behaviour is found to be consistent with crystallisation experiments. The results suggest that optimisation of supersaturation and polymer content is necessary to achieve both high permeation rates and inherent stability.

摘要

本文报道了对两种纤维素聚合物，即甲基纤维素（MC）和羟丙基纤维素（HPMC）对醋酸氢化可的松（HA）的过饱和度和渗透性影响的系统研究。采用Franz扩散池技术研究了HA从0.5%卡波姆凝胶中透过模型硅橡胶膜的扩散情况。在聚合物浓度恒定的情况下，通量随过饱和度增加成正比增加，直至4.8倍过饱和度，此后通量下降。对于特定的过饱和度（4.8倍），通量随聚合物浓度增加而增加，直至1%，在更高浓度下通量下降。该行为与结晶实验结果一致。结果表明，优化过饱和度和聚合物含量对于实现高渗透率和内在稳定性都是必要的。