“Formulation Development and Solubility Enhancement of Rosuvastatin Calcium by Using Hydrophilic Polymers and Solid Dispersion Method”

Abstract

Objective: Preparation of Rosuvastatin Calcium by Using Hydrophilic Polymers and Solid Dispersion Method, Rosuvastatin calcium is a Dyslipidaemic agent, which act as a selective competitive inhibitor of HMG CoA educates enzyme and is used in the treatment of hyperlipidemia.
 Methods: In the present work, Solid Dispersion was prepared by kneading method to increase the solubility of Rosuvastatin Calcium.
 Results: Solid dispersions were evaluated by determining percentage yield, drug content, solubility, Scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), DSC and in vitro dissolution profile. The prepared solid dispersion are formulated into capsule dosage form and characterized by various parameters i.e. weight variation, content uniformity, disintegration and dissolution. The evaluated parameters of capsule dosage form increase in solubility and dissolution rate of the pure drug.
 Conclusion: These are various techniques to enhance the solubility of the drug, such as particle size reduction, use of surfactants, solid dispersion etc. Carriers are the major players in these formulations, e. g. Hydroxypropylmethylcellulose, ethylcellulose, Carbopol, Acacia Gum etc. Carbopol and Acacia Gum is one of the most efficient polymers work as a carrier for these drugs to enhance solubility.

Enhanced Aqueous Solubility and in Vitro Dissolution of the Anti-Hyperlipidemic Agent Using Synthesized Solid Dispersion Carrier

“…The pentaerythritol-eudragit ® RS100 co-processed excipients (CE) carrier was created using a slightly modified method from one literature published in Elsevier [13,18]. Briefly, 50 ml of ethanol was used to dissolve ~ 100 mg of pentaerythritol and ~100 mg of eudragit ® RS100 (ERS).…”

Improvement in solubility of BCS class II drug: Telmisartan

“…Improved bioavailability is the outcome of dissolving weakly water-soluble drugs in solid solutions in a carrier with comparatively excellent aqueous solubility [13]. By adjusting the characteristics of the carrier and solid dispersion particles, the suitable drug release profile is achieved using solid dispersions [14]. Telmisartan solid dispersions were prepared by using different carriers such as PEG 4000 and PEG 6000 in 1:3 molar ratio (drug: carrier).…”

Improvement of solubility and dissolution rate of Biopharmaceutical Class II drug atorvastatin calcium by using an essential amino acid L-leucine

“…The dissolution medium was 900 mL of phosphate buffer (pH 6.8). 22 5 ml samples were withdrawn from the dissolution vessels at specific time intervals (5,10,20,30, and 45 min) which were immediately replaced with the same volume of fresh dissolution medium. 23 ATC quantity was estimated at 245 nm with a UV spectrophotometer, and the percentage of drug release for each formulation was determined through the calibration curve.…”

“…This superiority of the SE method over KM is due to more reduction in particle size of ATC and greater enhancement in drug wettability, and finally, improvement in dissolution rate. 27,30 Among the prepared formulations, SE2 was selected as the best formula in terms of dissolution profile because it has a faster and more complete drug release after 5 minutes compared with SE1, KM1, KM2, and KM3. Also, it contains a half quantity of LUC compared to the SE3 formula.…”