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Levoamlodipine besylate composition containing antioxidant, preparation method and application thereof

A technology of levamlodipine and besylate, which is applied in the direction of medical preparations containing active ingredients, drug combinations, and medical preparations without active ingredients, etc., can solve the unavoidable exposure of levamlodipine besylate Oxidation, substance increase and other problems, to achieve good practical application value, ensure quality consistency, and improve stability

Active Publication Date: 2019-11-15
JIANGXI SHIMEI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, literature reports that levamlodipine besylate is unstable to high humidity and high temperature environment, and it is easy to change color and be oxidized when the temperature exceeds 40°C, mainly due to oxidative degradation of impurity I
The inventors have found that the existing levamlodipine besylate tablets are prepared by the main drug and auxiliary materials dry tableting process, spray drying process or inclusion process to increase the stability of the preparation, but the raw material drug is difficult to be completely wrapped by the auxiliary materials , the contact between the raw material drug and the air is relatively sufficient, and the exposure of levamlodipine besylate in the air cannot be avoided. The quality of the preparation is unstable during the preparation process or storage process, and the related substances increase significantly.

Method used

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  • Levoamlodipine besylate composition containing antioxidant, preparation method and application thereof
  • Levoamlodipine besylate composition containing antioxidant, preparation method and application thereof
  • Levoamlodipine besylate composition containing antioxidant, preparation method and application thereof

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preparation example Construction

[0024] In yet another specific embodiment of the present invention, the preparation method of the above-mentioned levamlodipine besylate composition containing an antioxidant is provided, the preparation method comprising: taking levamlodipine besylate and the antioxidant and mixing uniformly , and then prepared by mixing with other pharmaceutically acceptable pharmaceutical excipients.

[0025] In yet another specific embodiment of the present invention, an application of the above-mentioned levamlodipine besylate composition containing an antioxidant in the preparation of levamlodipine besylate tablets is provided.

[0026] In yet another specific embodiment of the present invention, a levamlodipine besylate tablet is provided, and the levamlodipine besylate tablet comprises the above-mentioned levamlodipine besylate composition containing an antioxidant.

[0027] In yet another specific embodiment of the present invention, the preparation method of the above-mentioned levam...

Embodiment 1

[0031] Levoamlodipine besylate tablet prescription: specification 2.5mg (in terms of levamlodipine), prescription quantity is 1000 tablets, antioxidant is anhydrous sodium sulfite, the weight ratio of levamlodipine besylate and antioxidant It is 1:0.2.

[0032] name g / 1000 tablets levamlodipine besylate 3.662 microcrystalline cellulose 53.007 pregelatinized starch 41.001 Sodium carboxymethyl starch 18.005 Anhydrous sodium sulfite 0.745 colloidal silica 2.441 Magnesium stearate 1.223

[0033] Preparation:

[0034] (1) Get levamlodipine besylate, microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch, and anhydrous sodium sulfite respectively and pass through an 80-mesh sieve for subsequent use;

[0035] (2) Take levamlodipine besylate and anhydrous sodium sulfite according to the prescription ratio and mix them by hand, add them into the three-dimensional mixer, and then add microcrystalline cellu...

Embodiment 2

[0038] Levoamlodipine besylate tablet prescription: specification 2.5mg (in terms of levamlodipine), the prescription quantity is 1000 tablets, antioxidant is vitamin C, and the weight ratio of levamlodipine besylate and antioxidant is 1:0.5.

[0039]

[0040]

[0041] Preparation:

[0042] (1) Take levamlodipine besylate, microcrystalline cellulose, anhydrous calcium hydrogen phosphate, sodium carboxymethyl starch, and vitamin C respectively and pass through an 80-mesh sieve for subsequent use;

[0043] (2) Take levamlodipine besylate and vitamin C according to the prescription ratio and mix them evenly, add them into the high-speed mixing granulator, and then add microcrystalline cellulose, anhydrous calcium hydrogen phosphate, and carboxymethyl starch in the prescription ratio Sodium, mix evenly and then perform dry granulation and granulation;

[0044] (3) The obtained granules are uniformly mixed with the magnesium stearate of the prescription ratio, and the mixed...

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Abstract

The invention provides a levoamlodipine besylate composition containing an antioxidant and a preparation method and an application thereof, which belong to the technical field of pharmaceutical preparations. The levamlodipine besylate composition includes levamlodipine besylate, the antioxidant and a pharmaceutically acceptable excipient. Wherein, the antioxidant includes one or more of citric acid, DL-tartaric acid, thiourea, disodium edetate, L-cysteine, vitamin E, vitamin C, anhydrous sodium sulfite, sodium thiosulfate, sodium metabisulfite, BHT and BHA. By adding the antioxidant in the pharmaceutical composition of the present invention, effective protection of levamlodipine besylate is achieved, the generation of oxidative degradation impurities is reduced, the stability of the levoamlodipine besylate during the preparation process and storage period of a preparation is increased, the quality consistency and bioequivalence with an original developer (Norvasc) is ensured, and the product has good practical application value.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an antioxidant-containing levamlodipine besylate composition and a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Levoamlodipine besylate tablets were first developed by Pfizer Pharmaceuticals, and were approved by the US FDA in 1992 under the trade name Norvasc. Levoamlodipine besylate is an antihypertensive drug with independent intellectual property rights in my country. The drug adopts chiral drug resolution technology to remove the dextrorotatory component of amlodipine besylate, and only retains...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/12A61K47/20A61K47/18A61K47/22A61K47/02A61K47/10A61K9/20A61K31/4422A61P9/12
CPCA61K9/2009A61K9/2013A61K31/4422A61K47/02A61K47/10A61K47/12A61K47/183A61K47/20A61K47/22A61P9/12
Inventor 江鸿赵利军吕传涛蔺孟瑶刘玉芹
Owner JIANGXI SHIMEI PHARM CO LTD