Candesartan cilexetil composition

A technology of candesartan cilexetil and its composition, which is applied in the field of candesartan cilexetil granules and its composition, and can solve the problems of small particle size and the like

Active Publication Date: 2015-07-08
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solid preparations of these candesartan cilexetils have the disadvantages of using special solubilizers, the raw materials need to be ultrafine powdered, and the particle size of the candesartan cilexetils used is extremely small (nanoscale). Therefore, it is necessary to study the candesartan cilexetil. The nature of desartan cilexetil, looking for a suitable particle size range that is suitable for formulation and easy to obtain, so that a formulation with higher bioavailability can be obtained

Method used

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preparation example Construction

[0013] The second aspect provides candesa whose particle size (D90) corresponding to the cumulative particle size distribution number reaches 90% is less than 16 μm and the particle size (D90) corresponding to the cumulative particle size distribution number reaches 90% is higher than 11 μm. A method for preparing tansylate granules, which comprises: heating candesartan cilexetil to reflux and dissolving it in a solvent containing acetone, controlling the stirring speed to be V1, adding water; Removal of the solvent afforded the product.

[0014] The acetone-containing solvent may or may not contain water. In some embodiments, the mass ratio of acetone to water in the acetone-containing solvent is 10:1-15:1. In some embodiments, the mass ratio of acetone to water in the acetone-containing solvent is 12:1-15:1.

[0015] The mass ratio of acetone to candesartan cilexetil is 3:1-5:1.

[0016] When water is added, the mass ratio of the added water to the candesartan cilexetil i...

specific Embodiment approach

[0053] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0054] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0055] In the present invention, min means minute, μm means micron, f2 means similarity factor, r / m means revolution / minute, mL means milliliter, kg means kilogram, mg means milligram, and parts refer to parts by weight.

Embodiment 1

[0057] prescription:

[0058]

[0059]

[0060] Note: " / " means no such component.

[0061] Preparation:

[0062] Candesartan cilexetil, lactose monohydrate, corn starch (if any), pregelatinized starch (if any), hydroxypropyl cellulose, croscarmellose sodium (if any) weighed according to the prescription ), add water and mix evenly; then add polyethylene glycol, carboxymethylcellulose calcium (if any), and magnesium stearate; sieve; dry at 50-60°C, sieve for granulation, and compress into tablets.

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Abstract

The invention provides a candesartan cilexetil granule with a specific particle size range, and a preparation method and a composition thereof, belonging to the technical field of pharmacy. When the cumulative particle size distribution number of the candesartan cilexetil granule reaches 90%, a corresponding particle size is less than 16 [mu]m and higher than 11[mu]m; and the candesartan cilexetil composition including candesartan cilexetil in such a particle size range comprises 1 to 20 parts of the candesartan cilexetil granule, 65 to 80 parts of a filler, 1 to 20 parts of an adhesive, 1 to 10 parts of a disintegrating agent and 1 to 5 parts of a lubricant. The composition has good dissolution performance.

Description

technical field [0001] The invention relates to candesartan cilexetil granules with a specific particle size range and a composition thereof, belonging to the technical field of pharmacy. Background technique [0002] Candesartan cilexitil (Candesartan cilexitil), chemical name: (±)-1-[[(cyclohexyloxy)carbonyl]oxo]ethyl-2-ethoxy-1-[[2'-( 1H-tetrazolyl-5)-[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylate; a prodrug of candesartan, It is hydrolyzed into candesartan in the body; candesartan is a selective angiotensin Ⅱ receptor antagonist, which can reduce peripheral vascular resistance and has antihypertensive effect; it does not affect the degradation of bradykinin, and is effective for patients with cerebrovascular disorders There is no effect on cerebral blood flow in essential hypertension; it can be used to treat diseases such as hypertension. [0003] Candesartan cilexetil has low solubility in water, slow absorption and distribution in the body, and relative...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4184A61K47/38A61K47/34A61K47/32A61P9/12
Inventor 胡相靖王天明刘经国
Owner SUNSHINE LAKE PHARM CO LTD
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