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Formulation development and dissolution rate enhancement of efavirenz by solid dispersion systems
P T Koh1, J N Chuah, Meghna Talekar
1School of Pharmacy and Health Sciences, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia.
Indian Journal of Pharmaceutical Sciences
|October 2, 2013
Summary
This study improved efavirenz dissolution using solid dispersion systems. Polyvinylpyrrolidone K30 formulations at a 1:10 ratio showed the best dissolution profile.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Efavirenz dissolution rate is a critical factor for its bioavailability.
- Solid dispersion technology offers a promising approach to enhance drug solubility and dissolution.
Purpose of the Study:
- To enhance the dissolution rate of efavirenz using binary and ternary solid dispersion systems.
- To compare the efficacy of solvent and fusion methods for preparing efavirenz solid dispersions.
- To investigate the impact of different polymers and surfactants on efavirenz dissolution.
Main Methods:
- Preparation of efavirenz solid dispersions using polyethylene glycol 8000 and polyvinylpyrrolidone K30.
- Formulation of ternary systems incorporating Tween 80.
- Evaluation of dissolution profiles and physicochemical properties (DSC, XRD, FTIR, SEM).
Main Results:
- Solid dispersions significantly improved efavirenz dissolution compared to the pure drug (P<0.05).
- An optimal drug:polymer ratio of 1:10 was identified.
- Polyvinylpyrrolidone K30 formulations exhibited the best dissolution.
- Amorphous form of efavirenz in solid dispersions was confirmed by physicochemical characterization.
Conclusions:
- Both binary and ternary solid dispersion systems effectively enhance efavirenz dissolution.
- Polyvinylpyrrolidone K30 is a suitable carrier for efavirenz solid dispersions.
- The amorphous state of efavirenz in solid dispersions is key to improved dissolution.
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