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 restr

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

Example Embodiment

[0032] Experimental Example 1. Solubility-improving effect of valsartan

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

[0034] When only a dispersant is used, the main component is dispersed in the dispersant.

[0035] The main component is put into the mixture of the dispersant and the dissolution aid, and mixed until the main component is completely dispersed.

[0036] When a polymer is also mixed, the polymer is added to completely mix and cool while the mixture of the dispersant and the dissolution aid is heated, and 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 prepared by the same or similar preparation steps as those described above.

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

[0039] (unit: mg)

[0040]

[0041] Into 50 ml of the soluti...

Example Embodiment

[0051] Experimental Example 2. Solubility Improvement Effect of Telmisartan

[0052] The compositions of Examples 5 to 8 and Comparative Examples 3 to 4 of Table 3 below were prepared.

[0053] At this time, an alkalizing agent is mixed with a dispersing agent and a dissolution auxiliary agent, and the polymer is charged and mixed in a heated state. After cooling the mixed liquid in which the polymers are completely mixed, the main component is put in and mixed until the main component is completely dispersed.

[0054] [Table 3] Composition of Examples and Comparative Examples

[0055] (unit: mg)

[0056]

[0057] Examples 5 to 8 and Comparative Examples 3 to 4 prepared in the above were put into 50 ml of a solution with pH of 1.2, 4.0 and 6.8 and 50 ml of water, respectively, in a manner equivalent to 80 mg of telmisartan. The composition was shaken for 24 hours at 25° C. and 200 rpm (VS-8480, Vision Technology Corporation). Each sample was centrifuged at 13000 rpm for...

Example Embodiment

[0067] Experimental example 3. Screening of dispersants

[0068] Examples 9 to 14 and Comparative Example 1, Comparative Example 5 to Comparative Example 7 were prepared in a similar manner to the above-described Experimental Example 1 with the compositions 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 USP 40 dissolution apparatus 2 (slurry method) by using a pH 1.2 dissolution liquid (Korean Pharmacopoeia dissolution test first liquid) showing a low dissolution rate of valsartan, and according to the experiment Analysis Conditions of Example 1 The dissolution test solution was analyzed. The experimental conditions were as follows, and the dissolution tests of the following Experimental Examples 4 to 10 were also conducted in the same manner as in the present Experimental Example 3.

[0073] ·Dissolution: pH1.2, 500ml

[0074] Dissolution samples: Comparat...

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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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