Enhancement of Rosuvastatin Calcium Bioavailability Applying Nanocrystal Technology and in-vitro, in-vivo evaluations.
Journal Title: Asian Journal of Pharamceutical and Clinical Research - Year 2015, Vol 8, Issue 2
Abstract
Objective: The objective of this study is to prepare efficient dosage form using nanocrystal technology and to compare with micro and marketedformulations for its in-vitro and the in-vivo behavior. The nanocrystal technology has good potential to enhance the dissolution profile of poorlysoluble drugs by reducing particle size, increasing surface area, and also by raising the saturation solubility of the drug.Methods: In this study, solubility of rosuvastatin calcium is increased by adopting nanocrystal technology. Rosuvastatin calcium nanocrystals wasformulated using various stabilizers like sodium lauryl sulfate, hydroxyl propyl cellulose, hydroxyl propyl methyl cellulose, poloxamer 188, tween 80,poly vinyl pyrrolidine, by adopting two different methods top down and bottom up techniques. Formulations were compressed and physical parametersof tablets evaluated dissolution studies were performed to evaluate release and pharmacokinetic studies were done to evaluate in-vivo behavior.Results: Particle size obtained by employing top down method was found to be <749.04 nm (F-1 to F-7) whereas particle size obtained by followingbottom up method was higher than 2000 nm. The micronized particles possessed a size range of 61.51 μm, whereas nanoparticle formulations showedparticle size of 0.509 μm, 0.399 μm respectively. Differential scanning calorimetry studies showed good compatibility between drug and excipients.Friability values ranging from 0.15±0.0565% to 0.59±0.0283% and disintegration time lies between 29±1.414 and 44±1.414 seconds for the preparedformulations. The hardness of prepared tablets was between 3.0 and 4.5±0.707 kg/cm2 which are sufficient for maintaining the integrity of tablets.Friability, disintegration time and hardness for the micronized formulation (M-1) were 0.875±0.0919%, 50±2.828 seconds, 3.5±0.707 kg/cm2,which are higher than the values obtained for lyophilized nanocrystals in formulation. In-vitro studies have shown a 36% increase in dissolution ofnanocrystal formulation while in-vivo studies exhibited 1.87-fold increases in the bioavailability of rosuvastatin when compared to the micronizeddosage form.Conclusion: Formulations containing different constituents were prepared by following bottom up and top down techniques and evaluated in-vitro,in-vivo, observed significant differences between the formulations. The results proved that the bioavailability of rosuvastatin calcium has beenimproved considerably by applying nanocrystal technology. In-vitro and in-vivo evaluations showed that solubility and bioavailability have beenenhanced considerably.Keywords: Rosuvastatin calcium, Nanocrystal technology, Solubility, Bioavailability, Pharmacokinetics.
Authors and Affiliations
Kartick Palani, G. v. peter Christoper, Sathesh Kumar Kesavan
Keywords
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