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Pharmaceutical composition and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of control, complicated preparation process, and undisclosed specific surface area of ​​magnesium stearate, etc., and achieve the effect of improving stability, simple process, and good uniformity

Active Publication Date: 2021-04-23
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, WO2004 / 067003 and EP1604664 disclose compound preparations of olmesartan medoxomil and amlodipine, but do not disclose specific prescriptions and preparation methods
WO2008 / 032107 discloses the specific prescription of olmesartan medoxomil and amlodipine tablets, but it does not disclose how to control the particle size of the raw material drug, nor does it disclose the specific surface area of ​​magnesium stearate, and it adopts dry granulation Tablets are prepared in the same way, and the preparation process is complicated

Method used

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  • Pharmaceutical composition and preparation method thereof
  • Pharmaceutical composition and preparation method thereof
  • Pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Embodiment 1: Comparing the impact of different bulk drug particle sizes on various properties of the product

[0079] Prepare the prescription composition of 1000 tablets (specification 20mg / 5mg)

[0080]

[0081]

[0082] Wherein the specific surface area of ​​the magnesium stearate is 5.6m 2 / g.

[0083] Preparation: mechanically pulverize olmesartan medoxomil and amlodipine besylate to the target particle size range, then pregelatinized starch, olmesartan medoxomil, amlodipine besylate, silicified microcrystalline cellulose and Croscarmellose sodium is mixed, then passed through a 20-mesh sieve, and then the prescription amount of magnesium stearate is added for total blending. After the mixing is finished, perform direct tablet compression, the main compression pressure is 8.0-20.0kN, and the tablet hardness is 30N-75N (punching: a flat hole with a diameter of 6.0mm). Prepare the coating solution, add purified water into the mixing tank, turn on the stirri...

Embodiment 2

[0103] Embodiment 2. investigate the impact of the magnesium stearate of different contents on industrialized scale-up production

[0104] The specific surface area and feed ratio of magnesium stearate in the small test scale and the enlarged batch were studied respectively, so as to ensure that the dissolution of the final product was qualified on the basis of ensuring no sticking and punching.

[0105] Table 5: The amount and specific surface area of ​​different magnesium stearate investigated in the small test scale (batch 2-1~2-5)

[0106]

[0107] Table 6: Investigate the amount of magnesium stearate and the specific surface area of ​​the enlarged batch of products (batch 2-6~2-9)

[0108]

[0109] The preparation method was prepared according to the preparation method disclosed in Example 1, wherein the particle size d(0.9) of olmesartan medoxomil was 23.101 μm, and the particle size d(0.9) of amlodipine was 60.321 μm.

[0110] Prepare each batch of products accor...

Embodiment 3

[0117] Example 3. Tablets made by batches 2-6, 2-7 are compared with commercially available formulations

[0118] Commercially available preparation 1 (manufacturer: Daiichi Sankyo Pharmaceutical (Shanghai) Co., Ltd., product produced by the original manufacturer, trade name: ), commercially available preparation 2 (manufacturer: Daiichi Sankyo Europe GmbH, the product produced by the original manufacturer in Germany, trade name: ) self-made preparations (batches 2-6, 2-7) to carry out the accelerated test, the accelerated test conditions are 40 ℃ ± 2 ℃, 75% RH ± 5% RH, measured the self-made tablets and commercially available preparations respectively after 6 months Related substances and dissolution rates.

[0119] Table 8: Comparison of quality between self-made batches 2-6, 2-7 samples and commercially available preparations

[0120]

[0121] It can be seen from the data in the above table that the level of related substances in the tablet prepared according to the ...

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Abstract

The invention provides a pharmaceutical composition and a preparation method thereof. According to the pharmaceutical composition and the preparation method thereof, particle sizes of olmesartan medoxomil and amlodipine and a specific surface area of magnesium stearate are limited, so that problems of sticking and unsmooth blanking in a preparation process are solved, and stability of a product is improved on the basis of ensuring dissolution of the product.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition of a compound preparation containing two kinds of antihypertensive drugs and a preparation method thereof. Background technique [0002] Amlodipine besylate is the leading drug of the third generation of calcium ion antagonists. It inhibits the transmembrane entry of calcium ions into vascular smooth muscle and cardiomyocytes, thereby reducing the intracellular calcium ion concentration and relaxing vascular smooth muscle. It was developed by Pfizer, and excipients in oral tablets include microcrystalline cellulose, dicalcium phosphate anhydrous, sodium carboxymethyl starch, and magnesium stearate. [0003] Olmesartan medoxomil belongs to angiotensin Ⅱ receptor antagonist (ARB), which is a prodrug, which can be hydrolyzed into an active metabolite olmesartan (RNH-6270) after gastrointestinal absorption. Developed by the company, the exci...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/36A61K47/38A61K47/36A61K47/12A61K31/4422A61K31/4178A61P9/12
CPCA61K9/2095A61K9/2866A61K9/2054A61K9/2059A61K9/2013A61K31/4422A61K31/4178A61P9/12A61K2300/00
Inventor 王丽双温雅静章晓骅朱春霞徐丹田舟山
Owner NANJING CHIA TAI TIANQING PHARMA
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