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New evaluation method for in vitro/in vivo correlation of enteric-coated multiple unit dosage forms
T Hayashi1, T Ogura, Y Takagishi
1Developmental Research Laboratories, Shionogi & Co., Ltd., Hyogo, Japan.
Pharmaceutical Research
|September 1, 1995
Summary
This study introduces a novel GE-convolution method to predict in vivo drug dissolution for enteric-coated multiple units. The method accurately estimates dissolution profiles by integrating in vitro data with gastric emptying, improving in vitro-in vivo correlations.
Area of Science:
- Pharmacokinetics
- Drug Delivery Systems
- Computational Modeling
Background:
- Accurate prediction of in vivo drug dissolution is crucial for developing effective enteric-coated multiple unit dosage forms.
- Existing methods often lack precision in accounting for physiological processes like gastric emptying.
- Enteric coatings are designed to release drugs in specific gastrointestinal segments, making dissolution profile prediction complex.
Purpose of the Study:
- To develop and validate a novel method for evaluating drug dissolution profiles in the gastrointestinal tract using in vitro data.
- To establish a predictive model for in vivo drug release from enteric-coated multiple unit dosage forms.
- To assess the impact of gastric emptying on in vitro-in vivo correlations for drug dissolution.
Main Methods:
- A GE-convolution method was developed, utilizing in vitro dissolution profiles as weighting functions and gastric emptying (GE) as the input function.
- A dedicated computer program, GECONV, was created for the numerical execution of the convolution integral.
- In vivo dissolution profiles were estimated and compared against established methods like Wagner-Nelson using plasma concentration data.
Main Results:
- The GE-convolution method accurately estimated the in vivo dissolution profile of enteric-coated aspirin granules.
- The estimated in vivo dissolution showed good agreement with the in vivo cumulative absorption profile derived from plasma concentration data.
- Incorporating the gastric emptying process significantly enhanced the in vitro/in vivo correlation for drug dissolution.
Conclusions:
- The developed convolution method is a valuable tool for estimating in vivo drug dissolution profiles of enteric-coated multiple unit dosage forms.
- Gastric emptying is a critical determinant factor influencing in vivo drug dissolution from these dosage forms.
- This approach offers improved prediction accuracy compared to methods that do not account for gastric emptying.