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Dissolution rate enhancement of gliclazide by ordered mixing
Vikas A Saharan1, Pratim K Choudhury
1Institute of Pharmaceutical Sciences and Drug Research, Seth G.L. Bihani S.D. College of Technical Education, Sri Ganganagar, Rajasthan, India. vikas.pharmaceutics@gmail.com
Acta Pharmaceutica (Zagreb, Croatia)
|September 28, 2011
Summary
Mannitol and lactose significantly enhanced the dissolution rate of poorly soluble gliclazide (a diabetes drug). Optimal particle size and excipient selection are key for improving drug dissolution in ordered mixtures.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Gliclazide is a poorly water-soluble antidiabetic medication.
- Enhancing the dissolution rate of poorly soluble drugs is crucial for improving bioavailability.
- Ordered mixtures are a common formulation strategy.
Purpose of the Study:
- To investigate the impact of various excipients on the dissolution rate enhancement of gliclazide.
- To evaluate the influence of particle size and drug concentration on dissolution.
- To determine the optimal formulation parameters for improved gliclazide dissolution.
Main Methods:
- Preparation of ordered mixtures of micronized gliclazide with water-soluble excipients (lactose, mannitol, sorbitol, maltitol, sodium chloride).
- Dissolution rate studies were conducted on the prepared ordered mixtures.
- Kinetic modeling using the Hixson-Crowell model was applied to drug release data.
Main Results:
- All water-soluble excipients increased gliclazide dissolution rate, with mannitol showing the greatest improvement.
- Composite granules (355-710 μm) demonstrated superior dissolution enhancement.
- Reducing carrier particle size and increasing drug concentration decreased dissolution rate.
- Drug release data best fitted the Hixson-Crowell model, indicating cube root law adherence.
Conclusions:
- Mannitol and lactose are effective excipients for enhancing gliclazide dissolution.
- Optimizing carrier particle size and formulation composition is vital for improving drug dissolution.
- Ordered mixtures can be effectively formulated to improve the dissolution of poorly soluble drugs like gliclazide.
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