Composition containing levamlodipine besylate hydrate and preparation method thereof

Abstract

The present invention relates to a composition containing levamlodipine besylate hydrate and its preparation, formulation and application, especially (S)-2-[(2-aminoethoxy)methyl]-4-(2- Chlorophenyl)-6-methyl-1, 4-dihydro-3, 5-pyridinedicarboxylic acid-3-ethyl ester, composition of 5-methyl ester benzenesulfonic acid hydrate and its preparation method and application. The composition of levamlodipine besylate hydrate crystallized in pure water and dried is easy for industrial production, has no organic solvent residue, good thermal stability and good dissolution rate of solid preparation.

Description

technical field [0001] The invention relates to the technical field of levamlodipine besylate, in particular to a composition containing levamlodipine besylate hydrate, its preparation method, preparation and use. Background technique [0002] Amlodipine was developed by Pfizer in the United States and entered the Chinese market under the trade name "Norhuoxie" in 1994 as a drug for the treatment of hypertension and angina pectoris. Amlodipine is a racemate composed of levamlodipine and dextroamlodipine, and the pharmacological functions of the levorotatory and dextroforms are different. Dexamlodipine lacks calcium channel blocker activity and is a potent inhibitor of smooth muscle cell migration; levamlodipine is a long-acting calcium channel antagonist and has the effect of treating hypertension and angina pectoris. Therefore, in the prior art, there is a technique of splitting amlodipine to obtain levamlodipine and treating hypertension and angina pectoris based on its l...

AI Technical Summary

Problems solved by technology

It can be seen that there is still a lack of pure water preparation method of levamlodipine t-besylate hydrate composition in the prior art, and research on the related performance effects of preparations made with this hydrate composition, and there is no research on these research results. Based on the proposed composition product of levamlodipine besylate hydrate with more beneficial preparation effect

[0006] In addition, it is known in the prior art that amlodipine besylate has poor solubility and low dissolution rate in pharmaceutical preparations, which is not conducive to rapid onset of action, and it is often necessary to adopt special preparation processes, such as micronization, and amlodipine besylate Clodipine and lactose solution are sprayed and granulated preparation technology (for example, CN103006600A) on double-nozzle spray drier respectively, or add disintegrating agent, but such preparation technology often reduces medicine because of disintegrant, micronization and other processes. Formulation Stability

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