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Tablet containing azilsartan kamedoxomil and preparation method thereof

A technology for azilsartan medoxomil and potassium salt tablets, which is applied to medical preparations containing active ingredients, pill delivery, and pharmaceutical formulations, and can solve problems such as low bioavailability, low drug encapsulation rate, and fragile structure , to achieve the effect of simple preparation method, simple preparation method and improved shelf life

Active Publication Date: 2021-11-12
青岛市黄岛区人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Patent CN201110065253 introduces a liposome solid preparation of azilsartan, which improves the stability of the drug through the protective effect of the liposome, and the sealing of the liposome structure The system can protect the active ingredients of the drug to a certain extent, but the liposome structure is fragile and the encapsulation rate of the drug is low, resulting in low bioavailability of the product

Method used

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  • Tablet containing azilsartan kamedoxomil and preparation method thereof
  • Tablet containing azilsartan kamedoxomil and preparation method thereof
  • Tablet containing azilsartan kamedoxomil and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1: the preparation method that contains azilsartan medoxomil potassium salt tablet

[0034] Composition Component parts by weight Azilsartan medoxomil potassium salt 10mg Polyethylene glycol 4000-polyglutamic acid 6000 60mg Crospovidone 40mg Mannitol 3mg Magnesium stearate 0.7mg

[0035] 1) Add the above-mentioned polyethylene glycol 4000-polyglutamic acid 6000 into the aqueous solution, mix well and set aside;

[0036] 2) Dissolving the above-mentioned azilsartan medoxomil potassium salt in methanol solution and stirring at room temperature to obtain azilsartan medoxomil potassium salt solution;

[0037] 3) Slowly add the azilsartan medoxomil potassium salt solution into the ethylene glycol 4000-polyglutamic acid 6000 aqueous solution, slowly spin evaporate to remove the methanol, and transfer the spin evaporated solution to a dialysis bag with a molecular weight cut off of 3000 for dialysis , dialyze in dis...

Embodiment 2

[0039] Embodiment 2: Azilsartan medoxomil potassium salt tablet

[0040] Composition Component parts by weight Azilsartan medoxomil potassium salt 10mg Polyethylene glycol 6000-polyglutamic acid 10000 40mg Crospovidone 30mg Mannitol 2mg Magnesium stearate 0.5mg

[0041] Concrete component and component weight are as above table, and concrete preparation method is the same as embodiment 1

Embodiment 3

[0042] Embodiment 3: Azilsartan medoxomil potassium salt tablet

[0043] Composition Component parts by weight Azilsartan medoxomil potassium salt 10mg Polyethylene glycol 6000-polyglutamic acid 12000 40mg Low-substituted hydroxypropyl cellulose 30mg Mannitol 2mg Magnesium stearate 0.4mg

[0044] Concrete component and component weight are as above table, and concrete preparation method is the same as embodiment 1

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Abstract

The invention discloses a tablet containing azilsartan kamedoxomil and a preparation method thereof, the tablet is composed of an azilsartan kamedoxomil polymeric micelle composition, a disintegrating agent, a filler and a lubricant, the azilsartan kamedoxomil polymeric micelle composition is composed of azilsartan kamedoxomil and an amphiphilic block copolymer, a hydrophilic segment of the amphiphilic block copolymer is polyethylene glycol, a hydrophobic segment of the amphiphilic block copolymer is polyglutamic acid, the azilsartan kamedoxomil with low solubility is embedded in a polymer micelle by constructing the azilsartan kamedoxomil and the amphiphilic block copolymer, and the solubility of an active component is improved by utilizing the amphipathy of the polymer micelle, so that the medicinal effect of azilsartan medoxomil is obviously improved.

Description

technical field [0001] The invention relates to the technical field of western medicine preparations, in particular to a tablet containing azilsartan medoxomil potassium salt and a preparation method thereof. Background technique [0002] The English name of Azilsartan medoxomil is Azilsartan medoxomil, which is a new type of angiotensin II receptor blocker developed by Takeda Pharmaceutical Company in Japan. It usually exists in the form of potassium salt in pharmaceutical preparations, and its structural formula is: [0003] [0004] Azilsartan medoxomil is the prodrug of Azilsartan, which is mainly used for the treatment of hypertension and related complications. Taken together, it not only has a good blood pressure lowering effect, but also reduces the risk of concurrent vascular diseases and diabetes. The improved product has been approved by the FDA since 2011, and the trade name is EDARBI. [0005] Azilsartan medoxomil is unstable in a neutral pH environment, almo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/34A61K47/10A61K47/38A61K31/4245A61P9/12
CPCA61K9/2045A61K9/2031A61K31/4245A61P9/12
Inventor 刘东伟陈晓阳逄淑秀王坤李义亭陈伟李桂欣
Owner 青岛市黄岛区人民医院
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