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Pharmaceutical composition containing angiotensin receptor blocker

A technology of receptor antagonists and angiotensin, which is applied in the direction of active ingredients of heterocyclic compounds, medical preparations containing active ingredients, and pharmaceutical formulations to achieve the effect of increasing bioavailability and improving dissolution rate

Inactive Publication Date: 2019-01-04
DAE WON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, among the organic solvents used in the above-mentioned patents, dichloromethane and methanol are classified as Class 2 in the ICH guideline Q3C (ICHguideline Q3C) (solvents whose use is restricted in pharmaceuticals due to inherent toxicity, so The approved daily dose is about 0.1 mg), and it is well known that ethanol, etc. cause hepatotoxicity, nephrotoxicity, and gastrointestinal disturbance

Method used

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  • Pharmaceutical composition containing angiotensin receptor blocker
  • Pharmaceutical composition containing angiotensin receptor blocker
  • Pharmaceutical composition containing angiotensin receptor blocker

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0032] Experimental example 1. Solubility improvement effect of valsartan

[0033] Compositions of Examples 1 to 4 and Comparative Examples 1 to 2 of Table 1 below were prepared.

[0034] In the case of using only a dispersant, the main component is dispersed in the dispersant.

[0035] Add the main ingredient to the mixture of dispersant and dissolution aid, and mix until the main ingredient is completely dispersed.

[0036] When the polymer is also mixed, the polymer is added while the mixture of the dispersant and the dissolution aid is heated, mixed completely and cooled, then the main component is added and mixed until the main component is completely dispersed.

[0037] Unless otherwise stated, other comparative examples and examples described below were produced by the same or similar production steps as above.

[0038] [Table 1] Composition of Examples and Comparative Examples

[0039] (unit: mg)

[0040]

[0041] Into 50 ml of the solution and 50 ml of water ha...

experiment example 2

[0051] Experimental example 2. Solubility improvement effect of telmisartan

[0052] Compositions of Example 5 to Example 8 and Comparative Example 3 to Comparative Example 4 of Table 3 below were prepared.

[0053] At this time, the basifying agent is first mixed with the dispersant and the dissolution aid, and the polymer is charged and mixed in a heated state. After cooling the mixture in which the polymers have been completely mixed, add the main component and mix until the main component is completely dispersed.

[0054] [table 3] the composition of embodiment and comparative example

[0055] (unit: mg)

[0056]

[0057] Examples 5 to 8 and Comparative Examples 3 to 4 prepared above were put into 50 ml of solutions and 50 ml of water having pHs of 1.2, 4.0, and 6.8, respectively, in a manner corresponding to 80 mg of telmisartan. The composition was shaken for 24 hours at 25° C. and 200 rpm (VS-8480, Vision Technology Company). Each sample was centrifuged at 13,000...

experiment example 3

[0067] Experimental example 3. Dispersant screening

[0068] In a similar manner to Experimental Example 1 above, Examples 9 to 14 and Comparative Example 1, Comparative Example 5 to Comparative Example 7 were prepared with the composition of Table 5 below.

[0069] [Table 5] Composition of Examples and Comparative Examples

[0070] (unit: mg)

[0071]

[0072] The test was carried out according to USP40 dissolution apparatus 2 (slurry method) by using a pH 1.2 dissolution solution (Korean Pharmacopoeia Dissolution Test First Solution) in which the dissolution rate of valsartan was shown to be low, and according to the experimental The analysis conditions of Example 1 were used to analyze the dissolution test solution. The experimental conditions were as follows, and the following dissolution tests of Experimental Examples 4 to 10 were also performed in the same manner as in Experimental Example 3.

[0073] · Eluate: pH1.2, 500ml

[0074] Dissolution samples: comparativ...

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PUM

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Abstract

Provided are: a pharmaceutical composition containing one or more selected from an angiotensin receptor blocker (ARB), an isomer thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof and having enhanced bioavailability by improving the solubility and dissolution rate of the ARB; and a preparation method therefor.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising at least one selected from the group consisting of angiotensin receptor blocker (ARB), its isomer, pharmaceutically acceptable salt or its prodrug. More specifically, the present invention relates to pharmaceutical compositions and methods for their preparation that enhance bioavailability by improving the solubility and dissolution of angiotensin receptor antagonists. Background technique [0002] Angiotensin receptor antagonists such as valsartan and telmisartan have low solubility in water as poorly soluble drugs, and their solubility varies greatly depending on pH, so when they are orally administered, there is a large variation in absorption among individuals. , and the problem of low bioavailability (bioavailability, BA). [0003] It is well known that when administered orally, the bioavailability of valsartan and telmisartan are about 25% and 42-58%, respectively, valsarta...

Claims

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Application Information

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IPC IPC(8): A61K31/41A61K31/4184A61K31/4178A61K9/16
CPCA61K9/16A61K31/41A61K31/4178A61K31/4184A61K9/1664
Inventor 吴东昊蔡宝蓝朴明信宋世贤孙世一
Owner DAE WON PHARMA
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