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Pharmaceutical formulation

A technology of pharmaceutical preparations and renin inhibitors, applied in the field of pharmaceutical preparations, can solve the problems of not providing the cumulative effect of combined preparations and the decline in the effect of aliskiren, and achieve the effect of improving the problem of simultaneous administration and effective curative effect

Inactive Publication Date: 2011-03-23
HANALL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Concomitant administration of the renin inhibitor aliskiren and the angiotensin-II-receptor blocker irbesartan is known to result in a 50% decrease in blood aliskiren levels, so this can lead to a decrease in the effect of aliskiren , and may not provide an additive effect of combined formulations

Method used

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Examples

Experimental program
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Embodiment I

[0141]

Embodiment I-1

[0142] Embodiment I-1: the preparation of biphasic matrix tablet

[0143] According to the ingredient composition and content shown in Table 1 below, it was prepared through the following steps.

[0144] 1) Preparation of sustained-release compartments containing aliskiren

[0145] Aliskiren hemifumarate, microcrystalline cellulose, crospovidone, and sodium chloride were sieved through a No. 35 sieve and mixed in a high speed mixer for 5 minutes to prepare a mixture. Meanwhile, polyvinylpyrrolidone was dissolved in purified water to prepare a binding solution (10 w / w%). The binding solution and the mixture of the main ingredients are placed in a high-speed mixer, and then kneaded. After completing the kneading process, the kneaded material was granulated using a shaker with a No. 20 sieve, and the granules were dried in a hot water drier at 60°C. Meanwhile, cellulose acetate (acetyl 32%), cellulose acetate (acetyl 39.8%), and hydroxypropylmethylcellulose were dissolved ...

Embodiment I-2

[0150] Embodiment 1-2: the preparation of biphasic matrix tablet

[0151] According to the ingredient composition and content shown in Table 1 below, it was prepared through the following steps.

[0152] 1) Preparation of sustained-release compartments containing aliskiren

[0153] Aliskiren hemifumarate and microcrystalline cellulose were sieved through a No. 35 sieve and mixed in a high-speed mixer for 5 minutes to prepare a mixture. Meanwhile, polyvinylpyrrolidone was dissolved in purified water to prepare a binding solution (10 w / w%). The mixture of the binding solution and the main ingredients is placed in a high-speed mixer and then kneaded. After completing the kneading process, the kneaded material was granulated using a shaker with a No. 20 sieve, and the granules were dried in a hot water drier at 60°C. Then, a mixed solution (10% w / w) of hydroxypropyl methylcellulose and hydroxypropyl methylcellulose phthalate in a 1:1 mixture of ethanol and methylene chlorid...

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Abstract

The present invention provides a pharmaceutical formulation comprising a compartment containing a rennin inhibitor as a pharmacologically active ingredient, and a compartment having an angiotensin-II-receptor blocker as a pharmacologically active ingredient. One of the compartments is an immediate-release compartment and the other one is an extended-release compartment. Since the disclosed formulation delivers the rennin inhibitor and angiotensin-II-receptor blocker at a specific delivery rate at a different time. It has an advantage in reducing the concern about side effects, improving drug effects, and simplifying the instructions for use of the drug. In addition, the formulation can pharmacologically, clinically, scientifically, and economically achieve more useful effects than the complex prescription case of taking the ingredients separately or each at once, in preventing and treating metabolic syndrome, cardiovascular disease and renal disease.

Description

technical field [0001] The invention relates to pharmaceutical preparations containing renin inhibitors and angiotensin-II-receptor blockers. Background technique [0002] Renin inhibitors are drugs developed to have a mechanism of inhibiting the splitting of angiotensinogen by binding to renin, thereby inhibiting the conversion of angiotensinogen into angiotensin-I, and examples of renin inhibitors include Aliskiren, Remigillen, Enaziren, Zhangiren, etc. Among them, Aliskiren is chemically defined as 2(S), 4(S), 5(S), 7(S)-N-(3-amino-2,2-dimethyl-3-oxopropyl )-2,7-bis(1-methylethyl)-4-hydroxy-5-amino-8-[4-methoxy-3-(3-methoxy-propoxy)phenyl]- octanamide, and is particularly disclosed in EP 678503 A. The hemifumarate salt of aliskiren is known to be preferred [Recent patents on Cardiovascular Drug Discovery 2006; Nov 1(3):233-40]. [0003] Renin synthesized in the kidney migrates into the bloodstream and splits angiotensinogen by the action of angiotensin-converting enzy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/165A61K9/48A61K31/41A61K31/4196A61K31/4178A61P9/10
CPCA61K9/2081A61K9/2027A61K9/5084A61K9/5042A61K31/165A61K9/5015A61K9/2054A61K9/2059A61K9/209A61K45/06A61K9/4808A61K9/5078A61K9/1623A61K9/5047A61K9/1635A61K31/41A61K9/2866A61K9/5026A61K9/1652A61K31/4196A61K31/4178A61K9/0004A61K9/2018A61P3/00A61P9/00A61P9/10A61P9/12A61K2300/00
Inventor 金圣旭田圣树具滋星金镇昱孙载云曹英观
Owner HANALL PHARMA CO LTD
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