Slow-release tablet of simvastatin and nicotinic acid and preparation method thereof

Abstract

The invention provides a compound slow-release tablet of simvastatin and nicotinic acid and a preparation method thereof. The method prepares the slow-release nicotinic acid and the simvastatin into a compound tablet for the first time. In the compound tablet, each tablet contains 250-2000mg of nicotinic acid and 5-50mg of simvastatin. The compound tablet is prepared by the following steps: preparing a simvastatin quick-release tablet and preparing the compound slow-release tablet of the simvastatin and the nicotinic acid. The compound nicotinic acid slow-release tablet prepared by the method is suitable for the treatment of primary hypercholesteremia and mixed type blood lipid abnormality, takes the nicotinic acid as a slow-release part and the simvastatin as a quick-release part according to the respective properties, prepares a compound preparation, enables each component to exert a synergistic action in vivo, exerts the medicine effect furthest, can lower the side effect of the medicine, reduces the fluctuation of the blood concentration in vivo, reduces the administration frequency of a patient and has more obvious curative effect for relieving the hypercholesteremia in comparison with that of a method which only takes any one single-prescription preparation.

Description

technical field [0001] The invention relates to a compound simvastatin nicotinic acid sustained-release tablet and a preparation method thereof, belonging to the field of pharmaceutical preparations. technical background [0002] Primary hypercholesterolemia and mixed dyslipidemia is a common and frequently-occurring disease in clinic. Currently, the drugs for treating hyperlipidemia mainly include statins, fibrates and others. Statins can only raise high-density lipoprotein cholesterol (HDL-C) to a limited extent and lower triglycerides (TG) to a limited extent. Statins alone cannot achieve this goal for many patients with dyslipidemia, especially those with mixed dyslipidemia. Adequate lipid therapy targets. Niacin can significantly improve all major blood lipid components and restore them to normal. It is the only approved drug for lowering lipoprotein (a) Lp(a) and the most effective drug for raising HDL-C. However, due to the side effects of flushing and hepatotoxicit...

AI Technical Summary

Problems solved by technology

[0009] From the point of view of the mechanism of action, niacin affects the synthesis of cholesterol by inhibiting the synthesis of low-density lipoprotein. In large doses, it can increase HDL and lower TG, which has a significant effect, and at the same time has a slight effect of lowering LDL; Too high, often hepatotoxic

Simvastatin is an HMG-CoA reductase inhibitor, which competitively inhibits endogenous cholesterol synthesis rate-limiting enzyme HMG-CoA reductant, blocks intracellular mevalonate metabolic pathway, reduces intracellular cholesterol synthesis, and thus feeds back Sexual stimulation increases the number and activity of LDL receptors on the surface of cell membranes (mainly liver cells), which increases serum cholesterol clearance and significantly reduces LDL, but the effect of increasing HDL-C is weak

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