국소제제의 약물방출에 미치는 polyethlylene glycol 400의 영향

Abstract

수용성 基劑인 PEG 400을 사용하여 p-aminobenzoic acid esters의 확산거동을 분명히 하기위한 in vitro系의 실험으로써, cellulose膜을 사용한 투과속도와 용액의 점도 및 약물농도와의 관계를 비교 검토하였다. 그 결과는 다음과 같다. 1. PEG를 첨가하였을 때, 용액에서는 점도의 증가로 인해 투과속도는 감소되었지만, 현탁액에서는 용해도의 증가가 점도에 의한 투과속도 감소를 上回하므로 투과속도가 증대되었다. 2. 주어진 약물농도가 일정한 때 용액에서 현탄액으로 이행하는 순간에서 투과속도가 극대가 되었다. 3. 최대 투과속도는 butamben에 비하여 p-aminobenzoic acid는 7.0배, benzocaine은 3.5배 빨랐다.;This is a report of investigation made to clarify the diffusional behaviors of esters of p-aminobenzoic acid in the presence of polyethylene glycol 400. Cellulose membrane permeation rate, solubility and viscosity of p-aminobenzoic acid methyl ester, benzocaine and butamben were determined with PEG solutions of various concentrations. The results were as follows: 1) With an increase in PEG concentrations, permeation rates from solutions decreased due to an increase in viscosity of the solution. From suspensions, however, permeation rates increased due to an increase in solubility. 2) When the initial drug concentration was constant, permeation rates was found to be greatest from the PEG-water system with the PEG concentration which transported from the solution to the suspension. 3) Permeation rate of 4.0mg/ml p-aminobenzoic acid methyl ester was 26.51ug/ml.hr from 5g/100ml PEG solution, and that of 4.0mg/ml benzocaine was 13.17ug/ml.hr from 15g/100ml PEG solution, and that of 2.0mg/ml butamben was 3.81ug/ml.hr from 10g/100ml PEG solution. Permeation rate was 7.0 fold in p-aminobenzoic acid methyl ester and 3.5 fold in benzocaine compared to butamben.