Stable olmesartan medoxomil solid preparation

A technology of olmesartan medoxomil and solid preparations, which is applied in the field of pharmaceutical preparations, can solve problems such as large influence, easy hydrolysis, and unstable properties, and achieve the effects of avoiding oxidation, preventing hydrolysis reactions, and ensuring stability

Active Publication Date: 2011-04-27
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] As an ester compound, olmesartan medoxomil is unstable in nature and can exist stably in an acidic environment, but it is unstable in an alkaline environment and is easily hydrolyzed. In the preparation process of the preparation, the excipients have a greater impact on it, such as alkaline excipients The environment causes its hydrolysis to produce corresponding acids and alcohols, and the increase of impurities affects the quality of the drug; although it can exist stably in an acidic environment, it is necessary to strictly control the pH. Esterification reaction with the hydroxyl group in the molecule to generate new impurities
[0007] After searching, no reports on inhibiting the hydrolysis reaction of olmesartan medoxomil in previous academic literature and patent literature were found

Method used

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  • Stable olmesartan medoxomil solid preparation
  • Stable olmesartan medoxomil solid preparation
  • Stable olmesartan medoxomil solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Olmesartan medoxomil 20g, BHA0.5g, BHT0.5g, citric acid 2g, lactose 60g, microcrystalline cellulose 100g, sodium carboxymethyl starch 10g, micropowder silica gel 5g, magnesium stearate 2g, absolute ethanol 60ml, poly Vitone 4.5g.

[0019] Preparation:

[0020] (1) Olmesartan medoxomil, lactose, microcrystalline cellulose, sodium carboxymethyl starch take by weighing prescription quantity, mix homogeneously;

[0021] (2) BHA, BHT, citric acid, and povidone are dissolved in absolute ethanol to make a binder solution;

[0022] (3) Add binder solution to the mixture obtained in (1), granulate, granulate, after drying, add silicon dioxide and magnesium stearate and mix uniformly;

[0023] (4) Determination of particle content, tableting.

Embodiment 2

[0025] Olmesartan medoxomil 17g, BHA0.3g, BHT0.6g, citric acid 1.6g, lactose 54g, microcrystalline cellulose 98g, low-substituted hydroxypropyl cellulose 14g, micropowder silica gel 5g, absolute ethanol 60ml, povidone 4g.

[0026] Preparation method embodiment 1

Embodiment 3

[0028] Olmesartan medoxomil 20g, BHA 0.8g, malic acid 2.4g, lactose 30g, microcrystalline cellulose 115g, croscarmellose sodium 10g, crospovidone 5g, magnesium stearate 4g, absolute ethanol 70ml, povidone 5g.

[0029] Preparation method is as embodiment 1

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PUM

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Abstract

The invention provides a stable olmesartan medoxomil solid preparation and a preparation method thereof. Olmesartan medoxomil is unstable within a certain pH range and is easy to undergo hydration reaction. The hydrolysis product as an impurity is retained in the medicine, thereby influencing the safety effectiveness of the medicine. A pH adjusting agent and a stabilizing agent are added in a prescription, active components of the preparation are ensured to be free from undergoing the hydration reaction in the production process, the impurities are avoided, and the quality of the products and the medicine application safety of patients can be ensured.

Description

technical field [0001] The invention relates to a stable pharmaceutical solid preparation, in particular to an olmesartan medoxomil solid preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Impurities in medicines are substances that exist in medicines and have no therapeutic effect, are harmful to the human body or affect the quality of medicines, and are one of the important factors affecting the safety of medicines. There are many sources of impurities, which can be brought in during the preparation of raw materials, such as impure raw materials, incomplete reaction of some raw materials; intermediates or by-products produced during the reaction process are not completely removed during refining; or Impurities may be brought in during the process. Impurities can also be produced during the production of preparations, such as the introduction of excipients, the interaction between excipients an...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/00A61K31/4178A61K47/38A61K47/10A61K47/12A61P9/12
Inventor 黄河耿玉先
Owner BEIJING WINSUNNY PHARMA CO LTD
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