T Hayashi1, T Ogura, Y Takagishi. 1. Developmental Research Laboratories, Shionogi & Co., Ltd., Hyogo, Japan.
Abstract
PURPOSE: To establish the evaluating method for drug dissolution profiles in the gastrointestinal (GI) tract based on in vitro data for the enteric-coated multiple unit. METHODS: Dissolution profile in the GI tract was calculated by the convolution procedure using an in vitro dissolution profile as a weighting function, and the gastric-emptying (GE) process as an input function (GE-convolution method). A computer program, GECONV, was developed for numerical execution of the convolution integral. RESULTS: The in vivo dissolution profile of enteric-coated aspirin granules estimated by GE-convolution was in good agreement with the in vivo cumulative absorption profile calculated by the Wagner-Nelson method using the plasma concentration data after oral administration to healthy subjects. The in vitro/in vivo correlation improved markedly by taking the GE process into consideration. CONCLUSIONS: These findings indicated that this convolution method is useful for estimating the in vivo dissolution profile of drugs, when they are administered in an enteric-coated multiple unit type dosage form, because the gastric emptying process is a determinant process for the in vivo drug dissolution.
PURPOSE: To establish the evaluating method for drug dissolution profiles in the gastrointestinal (GI) tract based on in vitro data for the enteric-coated multiple unit. METHODS: Dissolution profile in the GI tract was calculated by the convolution procedure using an in vitro dissolution profile as a weighting function, and the gastric-emptying (GE) process as an input function (GE-convolution method). A computer program, GECONV, was developed for numerical execution of the convolution integral. RESULTS: The in vivo dissolution profile of enteric-coated aspirin granules estimated by GE-convolution was in good agreement with the in vivo cumulative absorption profile calculated by the Wagner-Nelson method using the plasma concentration data after oral administration to healthy subjects. The in vitro/in vivo correlation improved markedly by taking the GE process into consideration. CONCLUSIONS: These findings indicated that this convolution method is useful for estimating the in vivo dissolution profile of drugs, when they are administered in an enteric-coated multiple unit type dosage form, because the gastric emptying process is a determinant process for the in vivo drug dissolution.
Authors: N Aoyagi; H Ogata; N Kaniwa; M Koibuchi; T Shibazaki; A Ejima; M Mizobe; K Kohno; M Samejima Journal: Chem Pharm Bull (Tokyo) Date: 1986-01 Impact factor: 1.645