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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Response surface methodology to obtain naproxen controlled release tablets from its microspheres with Eudragit
A A Zaghloul1, S R Vaithiyalingam, J Faltinek
1Texas Technical University Health Sciences Center, School of Pharmacy, Amarillo 79106, USA.
Journal of Microencapsulation
|August 18, 2001
Summary
Naproxen controlled-release tablets were developed using Eudragit L100-55 microspheres. Formulation factors like deaggregating agent concentration and compression pressure significantly influenced naproxen release over 12 hours.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Naproxen is a widely used nonsteroidal anti-inflammatory drug (NSAID).
- Developing controlled-release (CR) oral dosage forms is crucial for improving patient compliance and therapeutic efficacy.
- Microsphere technology offers a promising approach for achieving sustained drug release.
Purpose of the Study:
- To evaluate the impact of deaggregating agent concentration (X1), compression pressure (X2), and precipitating water amount (X3) on naproxen release from Eudragit L100-55 microspheres.
- To optimize naproxen CR tablets for predictable 12-hour drug release.
Main Methods:
- Naproxen microspheres were prepared via coprecipitation using Eudragit L100-55 and calcium chloride.
- Tablets were formulated by compressing the naproxen-loaded microspheres.
- A 3-factor, 3-level Box-Behnken design was utilized to study the effects of independent variables on drug release.
- Dissolution studies were conducted according to USP specifications, adhering to Higuchi's square root of time kinetics for 12-hour release.
Main Results:
- A mathematical model (Y5 = 92.39 - 1.13X1 - 4.84X2 - 2.12X3 - 2.26X1X2 - 0.5X1X3 - 0.4X2X3 + 2.4X(1)(2) - 0.4X(2)(2), R² = 0.9) was established correlating formulation variables with 12-hour naproxen release.
- Deaggregating agent concentration (X1), compression pressure (X2), and precipitating water amount (X3) all inversely affected naproxen release.
- The interaction between deaggregating agent concentration (X1) and compression pressure (X2) was the most significant factor influencing drug release.
Conclusions:
- Optimized naproxen controlled-release tablets were successfully developed.
- The formulation achieved predictable naproxen release characteristics over a 12-hour period.
- Eudragit L100-55 microspheres are effective for creating sustained-release naproxen dosage forms.
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