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Tablets of paliperidone using compression-coated technology for controlled ascending release
Yingying Tang1, Huan Teng1, Yanan Shi1
1School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Asian Journal of Pharmaceutical Sciences
|February 28, 2020
Summary
This study developed novel compression-coated paliperidone tablets for controlled 24-hour oral release. The formulation utilizes hydroxypropyl cellulose and methylcellulose for a unique ascending drug release mechanism.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
Background:
- Paliperidone (PAL) is an antipsychotic medication requiring controlled release for effective oral administration.
- Developing simple and efficient manufacturing techniques for sustained-release dosage forms is crucial.
Purpose of the Study:
- To prepare and characterize ascending release compression-coated (CC) tablets of paliperidone (PAL).
- To investigate the *in vitro* drug release behavior and mechanisms of the developed CC tablets.
Main Methods:
- Formulation of CC tablets using high viscosity hydroxypropyl cellulose (HPC-H) core and hydroxypropyl methylcellulose (HPMC-K100M) coating.
- Evaluation of formulation factors and drug release kinetics using gravimetric analysis.
- Analysis of release mechanism fitting to the Peppas model.
Main Results:
- Optimal ascending drug release achieved with a 5:1 weight ratio of paliperidone (core:layer).
- Key formulation components included 33% HPC/HPMC and 10% Eudragit RL-PO.
- Ascending release resulted from solvent penetration, matrix dissolution, and erosion.
Conclusions:
- Compression-coated tablets successfully demonstrated controlled ascending release of paliperidone over 24 hours.
- The release mechanism involves a combination of diffusion and erosion.
- This technology offers a promising system for oral drug delivery.
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