Stable pitavastatin calcium pharmaceutical composition and preparation method thereof

Abstract

The invention discloses a stable pitavastatin calcium pharmaceutical composition, at least one of zinc oxide, aluminium oxide and ferric oxide is taken as a stabilizing agent, and the obtained pitavastatin calcium pharmaceutical composition and a further-prepared preparation product both have good stability, and the dissolving-out property of the preparation accords with the medicinal standard.

Description

technical field [0001] The invention relates to a stable pharmaceutical composition and a preparation method thereof, in particular, the invention relates to a stable pitavastatin calcium pharmaceutical composition and a preparation method thereof. Background technique [0002] The chemical name of Pitavastatin Calcium (CAS147526-32-7) is (+)-bis{(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)3 -quinolyl]-3,5-dihydroxy-6-heptenoic acid} monocalcium salt, molecular formula C50H46CaF2N2O8, molecular weight 880.98, its structural formula is as follows: [0003] [0004] Pitavastatin Calcium is a new type of statin blood lipid-lowering drug jointly developed by Nissan Chemical Co., Ltd. and Kowa Co., Ltd., which belongs to the third generation of statin drugs. Its preparation product was approved for marketing in Japan for the first time in July 2003. "Liqingzhi" (LIVALO) is mostly used clinically for the treatment of hypercholesterolemia and familial hypercholesterolemia. C...

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Problems solved by technology

[0006] Chinese patent CN96192065.3 discloses a stable pitavastatin calcium composition. The stabilization effect is achieved by adding an alkaline stabilizer. The pH value of its aqueous solution or suspension is greater than 7 and less than 8, but the inventor found through repeated experiments that Only controlling the pH value cannot make the product stable, and the stability of the pitavastatin calcium composition also depends on the specific stabilizer

[0007] In the pitavastatin calcium solid preparation disclosed in Chinese patent CN201010237658.6, magnesium oxide is used as an alkaline stabilizer, but due to the uncontrollable color change of magnesium oxide during the preparation process, the color of the prepared tablet is extremely uneven , thus affecting the product quality

[0008] Chinese patent CN200610036573.5 discloses that calcium bicarbonate or sodium bicarbonate is used as an alkaline stabilizer in the pitavastatin calcium solid preparation, but the inventor found through repeated experiments that the pitavastatin calcium preparation prepared according to the method disclosed in the patent Insufficient stability for long-term storage

[0009] In addition, the dissolution properties are also an important indicator for evaluating the quality of preparation products. The pitavastatin calcium preparations disclosed in the prior art cannot have good dissolution properties while ensuring stability. For example, when arginine is used as a stabilizer, Drugs degrade rapidly under acidic conditions (pH=1.2), which affects drug bioavailability

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