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Novel preparation process for oral solid preparation of aliskiren and amlodipine/levamlodipine

A technology of levamlodipine and amlodipine, applied in the field of new methods and medicines, galenic preparations, can solve the problems of reducing patient compliance, difficulty in taking medicine, and rising costs, so as to increase medication compliance, The effect of reducing dosage and reducing tablet weight

Inactive Publication Date: 2013-05-01
河南省健康伟业生物医药研究股份有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Due to the characteristics of Aliskiren hemifumarate and amlodipine besylate, in the tablet made of therapeutic dose (aliskiren 300mg+amlodipine 10mg), the amount of excipients is twice that of the raw drug, It not only wastes excipients, but also increases the cost, and makes it difficult for patients to take medicine, reducing patient compliance

Method used

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  • Novel preparation process for oral solid preparation of aliskiren and amlodipine/levamlodipine
  • Novel preparation process for oral solid preparation of aliskiren and amlodipine/levamlodipine
  • Novel preparation process for oral solid preparation of aliskiren and amlodipine/levamlodipine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1 Aliskiren Granules

[0058] Take Aliskiren or its pharmaceutically acceptable salt and binder (povidone) according to the ratio (weight ratio) of 8 to 12:1 and mix them uniformly by equal-volume incremental method, and adjust the gap between the two pressure rollers of the dry granulator to be 1mm , the roller pressure is 80~100×100Pa, the screw speed is 80r·min -1 , compaction speed 19r·min -1 , Vacuum ~ 0.4×1.01 5 Pa, choose 16 mesh for the upper screen, choose 18 mesh for the lower screen, and dry granulate. The content of aliskiren (free base) in the granules was determined.

Embodiment 2

[0059] Example Diamlodipine Granules

[0060] Take amlodipine or its pharmaceutically acceptable salt, filler (microcrystalline cellulose), and disintegrant (sodium hydroxyethyl starch) in the ratio (weight ratio) of 1 to 3: 3 to 5: 1 in equal amounts. Addition and mixing evenly, adjust the gap between the two pressure rollers of the dry granulator to 1mm, the pressure of the pressure rollers to 60~80×100Pa, and the screw speed to 80r min -1 , compaction speed 19r·min -1 , Vacuum ~ 0.4×1.01 5 Pa, choose 16 mesh for the upper screen, choose 18 mesh for the lower screen, and dry granulate. The content of amlodipine (free base) in the granules was determined.

Embodiment 3

[0061] Embodiment 3 Levoamlodipine Granules

[0062] Take levamlodipine or its pharmaceutically acceptable salt, filler (microcrystalline cellulose), disintegrant (sodium hydroxyethyl starch) and adopt equal amounts according to the ratio (weight ratio) of 1~3:3~5:1 Mix evenly by incremental method, adjust the gap between the two pressure rollers of the dry granulator to 1mm, the pressure of the pressure rollers to 60~80×100Pa, and the screw speed to 80r min -1 , compaction speed 19r·min -1 , Vacuum ~ 0.4×1.01 5 Pa, choose 16 mesh for the upper screen, choose 18 mesh for the lower screen, and dry granulate. The content of amlodipine (free base) in the granules was determined.

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Abstract

The invention relates to a novel preparation process for a solid oral preparation which comprises the active components consisting of an oral active renin inhibitor (aliskiren) in an appropriate carrier medium or a medicinal salt thereof and a calcium channel blocker (CCB) amlodipine / levamlodipine or a medicinal salt thereof. Particularly, the invention provides a galenical preparation which comprises a composition of aliskiren hemifumarate and amlodipine or levamlodipine and a novel preparation process. The invention also relates to novel preparation methods for the above-mentioned preparations and application of the preparations as medicines. According to the invention, the method of dry granulation is employed, the problem that the method of wet granulation easily causes increase of relevant substances is overcome, and drug stability is improved; through optimization of the process, the usage amount of excipients is reduced, the purpose of reducing the weight of a tablet is achieved, cost is saved, and the preparations can be easily taken; through particle coating, unwanted reaction of two drugs after mixing is prevented.

Description

technical field [0001] The present invention relates to a novel process for the preparation of a solid oral dosage form comprising an orally active renin inhibitor (aliskiren) or a pharmaceutically acceptable salt thereof and a calcium channel blocker (CCB) ammonium chloride in a suitable carrier medium Amlodipine / levamlodipine or a pharmaceutically acceptable salt thereof is used as the active ingredient. In particular, the present invention provides a galenic formulation comprising aliskiren hemi-fumarate in combination with amlodipine or levamlodipine and a new preparation process. The invention also relates to novel processes for their preparation and their use as medicaments. Background technique [0002] Renin released from the kidneys cleaves angiotensinogen in the circulation to form the decapeptide angiotensin I. It is then cleaved by angiotensin-converting enzymes in the lungs, kidneys, and other organs to form the octapeptide angiotensin II. The octapeptide can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4422A61K31/165A61K9/28A61K9/48A61P9/12A61P9/04
Inventor 李建勋陈蕴张发亮黄福生叶乾堂于振艳臧孝廉康建党刘浩梁建华李进进韩宏涛苗向阳
Owner 河南省健康伟业生物医药研究股份有限公司
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