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Development and evaluation of solid dispersion of spironolactone using fusion method
Shamsuddin1, Mohammad Fazil2, Shahid Husain Ansari3
1Department of Pharmacy, OPJS University, Rajasthan, India.
International Journal of Pharmaceutical Investigation
|March 26, 2016
Summary
Solid dispersion (SD) technology significantly enhanced the solubility and dissolution of spironolactone (SPL), a poorly water-soluble drug. This approach improves drug bioavailability and therapeutic efficacy by overcoming formulation challenges.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Poor water-solubility of drugs presents a major challenge in formulation development, limiting therapeutic efficacy and potentially causing toxicity.
- Solid dispersion (SD) technology offers a promising strategy to enhance drug solubility and dissolution rates.
- Many potent drugs fail to achieve therapeutic effects due to poor solubility.
Purpose of the Study:
- To develop and characterize a solid dispersion (SD) of spironolactone (SPL) using polyethylene glycol 4000 (PEG 4000).
- To evaluate the impact of SD on the solubility and dissolution profile of spironolactone.
- To assess the potential of SD technology for improving the bioavailability of poorly soluble drugs.
Main Methods:
- Spironolactone (SPL) solid dispersion (SD) was prepared using polyethylene glycol 4000 (PEG 4000) via the conventional fusion method.
- Characterization of the developed SD was performed using various analytical techniques.
- Solubility and dissolution studies were conducted for pure SPL, physical mixture, and SPL SD.
Main Results:
- The solubility of spironolactone in water was significantly increased in the solid dispersion (61.73 ± 1.26 μg/mL) compared to the pure drug (23.54 ± 1.75 μg/mL).
- The maximum cumulative percentage release of SPL from the solid dispersion at 60 minutes in 0.1 N HCl was 74.24 ± 3.25%, substantially higher than the pure drug (27.25 ± 1.83%) and physical mixture (47.72 ± 2.45%).
- The developed SD formulation showed a statistically significant improvement in solubility (P < 0.05).
Conclusions:
- Solid dispersion (SD) of spironolactone (SPL) was successfully developed using PEG 4000.
- The SD formulation significantly enhanced the solubility and dissolution rate of spironolactone compared to the active pharmaceutical ingredient (API) and physical mixture.
- SD technology is an effective strategy for improving the solubility of poorly soluble therapeutic agents like spironolactone.
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