Quickly-dissolved atorvastatin calcium tablet and preparation method thereof

Abstract

The invention provides a quickly-dissolved atorvastatin calcium tablet and a preparation method thereof. The atorvastatin calcium tablet provided by the invention does not contain surface active agents and alkaline materials, is simple in process, and can be quickly dissolved in the stomach, thereby enhancing the compliance and treatment effect of the administration of patients.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a fast-dissolving atorvastatin calcium tablet and a preparation method thereof. Background technique [0002] Atorvastatin is a new type of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, which has the effect of lowering serum cholesterol and triacylglycerol at the same time, and its lipid-lowering effect is higher than that of other HMGs - CoA reductase inhibitors. Atorvastatin reduces plasma cholesterol and serum lipoprotein concentrations by inhibiting HMG-CoA reductase and cholesterol biosynthesis in the liver, and enhances the uptake and metabolism of LDL-C by increasing liver LDL receptors on the cell surface , reduce the synthesis of LDL-C and the number of particles, thereby reducing LDL-C and TC, and have the effect of reducing TG, HDL-C is also slightly increased. [0003] The structural formula of atorvastatin calc...

AI Technical Summary

Problems solved by technology

[0005] The clinical curative effect of atorvastatin calcium is definite and remarkable. However, the drug is very slightly soluble in water and has poor stability. It is highly sensitive to humidity, heat, light and acidic environment, especially in acidic environment, it will degrade into Lactone reduces pharmacological activity. After testing, the dissolution rate of commercially available products (Lipitor, batch number 031610K, Pfizer Pharmaceuticals) in pH 1.2 hydrochloric acid medium is about 36% in 10 minutes. How to improve the dissolution rate of drugs in acidic medium has always been bothering pharmacists

[0006] CN1630510A discloses a kind of technology, adopts wet granulation technology, adds calcium carbonate as stabilizer in prescription, to guarantee that medicine is in alkaline environment, avoids medicine degradation, but a large amount of calcium carbonate can react with stomach acid, causes constipation, gastric Intestinal flatulence, indigestion and other adverse reactions

However, the problem caused by a large amount of disintegrants is that it is easy to absorb moisture, which leads to the degradation of atorvastatin calcium

[0008] CN102309462A provides an atorvastatin calcium tablet, which adopts dry secondary granulation technology, and the process is relatively complicated

[0009] CN1911209A uses high-efficiency disintegrants and a certain amount of sodium lauryl sulfate to make fast disintegrating tablets, which improves the dissolution rate in vitro, but the addition of surfactants will cause gastrointestinal irritation

[0010] CN101791297B discloses a preparation technology to prepare atorvastatin calcium tasteless microcapsules, but the process is complicated and the dissolution is not fast

However, only 60% of it was dissolved in acid for 30 minutes, and it could not be completely dissolved quickly.

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