New evaluation method for in vitro/in vivo correlation of enteric-coated multiple unit dosage forms
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T Hayashi1, T Ogura, Y Takagishi
1Developmental Research Laboratories, Shionogi & Co., Ltd., Hyogo, Japan.
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.