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Olmesartan medoxomil dispersible tablet and preparation method thereof

A technology of olmesartan medoxomil and dispersible tablets, which is applied in the field of pharmaceutical preparations, can solve the problems that there are no sustained-release dispersible tablets of olmesartan medoxomil, and achieve the effects of reducing the amount of the main drug, less stimulation, and rapid disintegration

Inactive Publication Date: 2021-07-16
江苏宇锐医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no relevant report on olmesartan medoxomil sustained-release dispersible tablets

Method used

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  • Olmesartan medoxomil dispersible tablet and preparation method thereof
  • Olmesartan medoxomil dispersible tablet and preparation method thereof
  • Olmesartan medoxomil dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-5

[0035] The preparation method of embodiment 1-5 olmesartan medoxomil sustained-release dispersible tablet, the steps are as follows:

[0036] (1) After mixing microcrystalline cellulose, sodium alginate and other qualities, mix them with olmesartan medoxomil and binders that account for a therapeutically effective amount, use water as a solvent, and prepare by centrifugal granulation or extrusion spheronization into olmesartan medoxomil pellets;

[0037] (2) adopt fluidized bed method, in pellet surface coating, the coating liquid that adopts is HPMC coating film; Obtain coating olmesartan medoxomil pellet after coating process;

[0038] (3) The coated olmesartan medoxomil pellets and the remaining olmesartan medoxomil bulk drug and the binder solution in the adjuvant are wet granulated and dried, and lubricants, disintegrants, correction agents are added to the dry pellets. Flavoring agent, glidant, whole grain, compressed tablet.

[0039] performance appraisal

[0040] Appe...

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PUM

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Abstract

The invention discloses an olmesartan medoxomil sustained-release dispersible tablet and a preparation method thereof. The olmesartan medoxomil sustained-release dispersible tablet comprises: coated olmesartan medoxomil pellets (a sustained-release part) obtained from olmesartan medoxomil with 50% effective treatment dose, the rest olmesartan medoxomil raw material medicines (a quick-release part) to be physically mixed with the pellets and other pharmaceutically acceptable auxiliary materials. The pellets are obtained by adopting an equal-mass mixture of microcrystalline cellulose and sodium alginate as a base material, preparing a pellet core from the base material and the olmesartan medoxomil through a centrifugal granulation method or an extrusion spheronization method, and coating an HPMC sustained-release coating through a fluidized bed. The pharmaceutically acceptable auxiliary materials comprise diluents, adhesives, disintegrating agents, flavoring agents, lubricants and glidants. The olmesartan medoxomil sustained-release dispersible tablet prepared by the invention can be rapidly disintegrated and be completely disintegrated within 2 minutes, with good stability.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dispersible tablet of olmesartan medoxomil for treating hypertension and a preparation method thereof. Background technique [0002] Olmesartan Medoxomil (Candesartan Cilexetil), chemical name: 2,3-dihydroxy-2-butenyl-4-(1-hydroxy-1-methylethyl)-2-propyl-1-[p- (o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-carboxylate, cyclic 2,3-carbonate. Molecular formula: C 29 h 30 N 6 o 6 , the structural formula is as follows: [0003] [0004] Olmesartan is a selective angiotensin II type 1 receptor (AT1) antagonist, which blocks the vasoconstrictive effect of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor of vascular smooth muscle. It acts independently of the AT II synthesis pathway. The affinity of olmesartan for AT1 is more than 12500 times greater than that for AT2. The use of ACE inhibitors to block the renin-angiotensin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/38A61K47/36A61K31/4178A61P9/12
CPCA61K9/2095A61K9/2081A61K9/2054A61K9/205A61K31/4178A61P9/12
Inventor 胡小艳丁南南殷学治计莹
Owner 江苏宇锐医药科技有限公司
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