Title : The development of ternary and quaternary solid dispersion-based hydrotropic blends of atorvastatin calcium
Abstract:
Objective: The major goal of this current experimental study was to use various hydrotropic agents in the formation of solid dispersion-based hydrotropic blends to improve the solubility properties of poor aqueous soluble drug atorvastatin calcium (ATV). Since, atorvastatin calcium has a solubility in aqueous solutions of greater than 0.1 mg/ml, which is very slightly soluble. When developing dosage forms for these medications, formulation scientists still face challenges.
Methods: In this study, twenty-two distinct binary, ternary, and quaternary formulations of ATV were prepared by employing five different hydrotropic agents (sodium benzoate, sodium salicylate, resorcinol, d-mannitol, and PEG 6000), and combining at least two hydrotropic agents in concentrations of 10% and 20% (w/v). Moreover, four different solid dispersions by the solvent evaporation method and physical mixture-based hydrotropic blends in the ratio of (1:2) have been formulated. The produced formulations were characterized using an FTIR analysis.
Results and discussion: According to the findings, binary formulations containing 20% (w/v) concentrations of sodium benzoate (SB), sodium salicylate (SS), and resorcinol (R) boosted the solubility ratio of ATV by 439.31, 689.57, and 106.21 folds, respectively. Furthermore, ternary formulations (FT14) and quaternary formulations (FQ18) resulted in the enhancement of ATV solubility by 938.45 and 995.12 folds, respectively. Ternary solid dispersion demonstrated the highest enhancement in solubility ratio by 87.68 folds and resulted in a higher dissolution rate of ATV than pure samples of the drug. Finally, FTIR analyses ruled out any interactions between medications and excipients by showing no noticeable shift in the peaks.
Conclusion: Solid dispersion-based hydrotropic blends can provide the production of the dosage forms of practically insoluble drugs with a favorable enhancement ratio in solubility.
Keywords: Atorvastatin calcium, Solid dispersion, Hydrotropic blends, Dissolution rate, Physical mixture.
Audience Take Away Notes:
- The audience, which primarily consists of formulation scientists and researchers in the field of pharmaceutical drug development and manufacturing, can use the findings of this study to enhance the solubility properties of atorvastatin calcium (ATV). They can apply the knowledge gained from the study to develop dosage forms and formulations that improve the solubility and dissolution rate of ATV, thereby addressing the challenges faced in formulating medications with poor aqueous solubility
- The study provides valuable insights into the use of hydrotropic agents and solid dispersion-based hydrotropic blends for enhancing the solubility of drugs. Formulation scientists can utilize this information to develop more effective dosage forms of drugs with poor aqueous solubility, such as ATV. By employing the hydrotropic agents and formulation techniques discussed in the study, they can overcome solubility-related challenges and improve the efficiency and effectiveness of drug formulations
- This research can serve as a valuable resource for other faculty members in the field of pharmaceutical research and teaching. The study introduces the application of hydrotropic agents and solid dispersion-based hydrotropic blends, providing a basis for further research and exploration in the area of enhancing solubility and dissolution rate of poorly soluble drugs. Other faculty members can build upon this research to expand their own investigations, develop new formulations, and contribute to the advancement of pharmaceutical science and technology
- This research provides a practical solution to the problem of poor aqueous solubility of atorvastatin calcium. By developing ternary and quaternary solid dispersion-based hydrotropic blends, the solubility ratio of ATV was significantly enhanced. This solution simplifies the formulation process and makes the job of formulation scientists more efficient by offering a viable approach to improve the solubility properties of poorly soluble drugs. The findings of this study can guide designers in developing more effective and efficient drug formulations
- This research study provides new information that can assist in the design of drug formulations for poorly soluble drugs. The use of hydrotropic agents and solid dispersion-based hydrotropic blends is a novel approach to enhance solubility. The study demonstrates the impact of different hydrotropic agents and their concentrations on the solubility of ATV, offering valuable insights into the design parameters for improving solubility. By incorporating this new information, designers can develop more accurate and effective drug formulations
Other benefits:
- Increased knowledge of hydrotropic agents and their impact on solubility enhancement
- Enhanced understanding of the formulation techniques involving solid dispersion-based hydrotropic blends
- Potential for developing more patient-friendly dosage forms of poorly soluble drugs
- Possibility of improving bioavailability and therapeutic efficacy of atorvastatin calcium
- Contribution to the scientific literature and advancement of pharmaceutical research
- Potential for commercial applications and development of marketable formulations
