Formulation and Development of Solid Dispersion System for Enhancement of Solubility and Dissolution Rate of Lovastatin

Ashutosh Kumar Upadhyay, Naveen Gupta, Neeraj Sharma, Dharmendra S. Rajput, Ankita Shukla
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Abstract

The solubility and dissolution rate of Lovastatin, a drug used for the treatment of hyperlipidaemia. Lovastatin is a selective competitive inhibitor of HMG Co-A reductase. However, its absolute bioavailability is 5%. To increase the solubility of drug solid dispersion was prepared. Solid dispersion prepared with polymer in 1:5 ratios shows the presence of amorphous form confirmed by the characterization study. Solid dispersion preliminary solubility analysis was carried out for the selection of the carrier and solid dispersion was prepared with Hydroxy Propyl Methyl Cellulose (HPMC) and Methyl Cellulose (MC). These solid dispersions were analyzed for the solubility and in-vitro dissolution profile solid dispersion of drug with polymer has shown enhanced solubility with improved dissolution rate. Further FTIR, X-Ray studies were carried out. The present investigations showed that solubility of Lovastatin Sodium was markedly increased by its solid dispersion using PVP K30 as carrier. The formulation SDF8 containing (1:8) shows highest dissolution rate. Hence the solid dispersion a way is useful technique in providing fastest onset of action of Lovastatin Sodium as well as enhanced dissolution rate. The study also shows that dissolution rate of Lovastatin can be enhanced to considerable extent by solid dispersion technique with Polymer.
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提高洛伐他汀溶解度和溶出率的固体分散体系的研制
洛伐他汀的溶解度和溶解率,一种用于治疗高脂血症的药物洛伐他汀是HMG Co-A还原酶的选择性竞争性抑制剂。但其绝对生物利用度为5%。为提高药物的溶解度,制备了固体分散体。用聚合物按1:5的比例制备的固体分散体显示出非晶态的存在,表征研究证实了这一点。对固体分散体进行初步溶解度分析,选择载体,并以羟丙基甲基纤维素(HPMC)和甲基纤维素(MC)制备固体分散体。对这些固体分散体的溶解度和体外溶出谱进行了分析,表明药物与聚合物的固体分散体溶解度增强,溶出率提高。进一步进行了FTIR和x射线研究。本研究表明,以PVP K30为载体,洛伐他汀钠的固体分散能显著提高其溶解度。含(1:8)的配方SDF8溶出率最高。因此,固体分散法是洛伐他汀钠最快起效和提高溶出速度的有效技术。研究还表明,聚合物固体分散技术可以在很大程度上提高洛伐他汀的溶出速度。
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