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Multiple unit gastroretentive drug delivery systems: a new preparation method for low density microparticles
A Streubel1, J Siepmann, R Bodmeier
1College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.
Journal of Microencapsulation
|July 26, 2003
Summary
A novel method creates floating microparticles with high drug loading and tunable release. This technique avoids heat and toxic solvents, offering an efficient way to produce oral drug delivery systems.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Developing effective oral drug delivery systems is crucial for patient compliance and therapeutic outcomes.
- Floating microparticle systems offer prolonged drug release and improved bioavailability.
- Existing methods for microparticle preparation often involve harsh conditions or toxic solvents.
Purpose of the Study:
- To develop a novel, efficient preparation method for low-density, foam-based, floating microparticles.
- To evaluate the in vitro performance of these microparticles for oral drug delivery.
- To investigate the influence of formulation and processing parameters on microparticle characteristics and drug release.
Main Methods:
- Microparticles were prepared by soaking polypropylene foam powder with drug/polymer solutions, followed by drying.
- Various model drugs (chlorpheniramine maleate, diltiazem HCl, theophylline, verapamil HCl) and polymers (Eudragit RS, PMMA) were used.
- In vitro floating behavior, drug loading, release kinetics, and particle morphology were assessed.
- The effect of converting verapamil HCl salt to its free base on drug release from PMMA microparticles was studied.
Main Results:
- The novel preparation method demonstrated short processing times, no high temperatures, and avoidance of toxic solvents, achieving near 100% encapsulation efficiency.
- Most microparticle formulations exhibited good in vitro floating behavior.
- A wide range of drug release profiles were achieved by adjusting drug loading and polymer type.
- PMMA microparticles showed incomplete verapamil HCl release, which was resolved by using the drug's free base, acting as a plasticizer.
Conclusions:
- A new, advantageous method for preparing floating microparticles was successfully developed.
- The microparticles can be formulated into rapidly disintegrating tablets for oral administration.
- The preparation method offers flexibility in controlling drug release characteristics for various therapeutic applications.