STUDY THE SUSTAIN RELEASE EFFECT OF DIFFERENT POLYMERS USED IN THE FORMULATION OF ASPIRIN-ROSUVASTATIN TABLETS
Keywords:Rosuvastatin calcium, Hyperlipidemia, Aspirin, Sustain release tablet, Polymers
Objective: Low permeability of rosuvastatin calcium faces a problem of low bioavailability (absolute bioavailability 20%) as its permeation is the rate limiting factor. Rosuvastatin calcium is a selective competitive inhibitor of HMG-CoA reductase and it lowers plasma cholesterol level. Aspirin is an anti-platelet agent with half-life of 6-7 h. Frequency of dosing of both drugs is high to maintain the desired plasma drug concentration so it is selected to formulate a sustained release tablet of aspirin and rosuvastatin calcium, which release the drug in a sustained manner over a period of time by using various polymers and study the effect of polymers on the release pattern of both drugs. This approach will also enhance the residence time of rosuvastatin calcium at the absorption site and enhance permeation by the effect of the polymers used and this in turn will enhance bioavailability.
Methods: Tablets contain aspirin plus rosuvastatin calcium were prepared by direct compression method. The sustained release of the tablets was obtained by using different polymers (xanthan gum, microcrystalline cellulose, HPMC K4M and chitosan) incorporated in the tablet and responsible for the release of both drugs from each tablet. Tablets were evaluated for weight variation, drug content, friability, hardness and thickness for all batches (F1 to F12). In-vitro dissolution was studied for all batches (F1 to F12) according to the type and ratio of each polymer used within these formulas i.e. (10 mg, 20 mg and 30 mg) respectively.
Results: The release of aspirin and rosuvastatin calcium from sustained release tablets varied according to the type and amount (ratio) of each polymer used. After the 7 h release study; (F1, F2, F3) that uses xanthan gum as the sustain release polymer showed the most sustained formulations than other polymers. The sustained release of drugs from tablet enhanced by increasing the amount of polymer, so F3 for example, which contain 30 mg xanthan gum had most sustained release than F1 and F2 which contain (10 mg and 20 mg) of the polymer respectively, this due to polymer related viscosity, swelling and binding mechanisms.
Conclusion: Using suitable polymer for sustained release will enhance the pharmacokinetics and efficacy of drugs and increase patient complains about combination therapy.
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