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Correlations between in vitro dissolution rate and bioavailability of alaproclate tablets
Journal of Pharmacokinetics and Biopharmaceutics
|August 1, 1984
Summary
This study demonstrates quantitative correlations between in vitro dissolution rates and in vivo bioavailability for alaproclate hydrochloride tablets. Mean dissolution time effectively predicts drug bioavailability across different tablet formulations.
Area of Science:
- Pharmacokinetics and Drug Delivery
Background:
- Establishing reliable in vitro-in vivo correlations (IVIVC) is crucial for predicting drug bioavailability from various dosage forms.
- Alaproclate hydrochloride's absorption characteristics and the influence of tablet formulation on its bioavailability require detailed investigation.
Purpose of the Study:
- To quantitatively correlate in vitro dissolution rates with in vivo bioavailability of alaproclate hydrochloride.
- To evaluate the utility of statistical moment analysis and empirical single-value parameters for establishing IVIVC.
- To compare bioavailability across conventional and controlled-release matrix tablets.
Main Methods:
- Two absorption studies involving single oral administration of various alaproclate hydrochloride tablet compositions to healthy subjects.
- Analysis of in vitro dissolution rates and in vivo pharmacokinetic parameters, including mean dissolution time (MDT), mean residence time (MRT), and maximum plasma concentration (Cmax).
- Application of statistical moment analysis and empirical single-value parameter methods for correlation.
Main Results:
- Linear relationships were established between in vitro MDT and in vivo parameters for both conventional and controlled-release tablets.
- An IVIVC was successfully established for controlled-release tablets using Cmax as the in vivo parameter.
- Bioavailability of alaproclate hydrochloride remained above 80% of the aqueous solution value until in vitro MDT exceeded approximately 3 hours.
Conclusions:
- Quantitative in vitro-in vivo correlations for alaproclate hydrochloride bioavailability can be established using dissolution rate data.
- Statistical moment analysis demonstrates broader applicability for IVIVC compared to empirical point estimates, applicable to both conventional and controlled-release formulations.
- Mean dissolution time is a valuable predictor of alaproclate hydrochloride bioavailability, guiding formulation development for desired drug release profiles.