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Oral candesartan cilexetil solid preparation and preparation method thereof

A technology of candesartan medoxomil and solid preparation, applied in the field of pharmacy, can solve the problems of low bioavailability, poor stability of candesartan medoxomil, easy hydrolysis and the like, and achieves the effects of high bioavailability and good stability

Inactive Publication Date: 2013-09-18
邓俐丽
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the problems of poor stability, easy hydrolysis, low bioavailability and complex production process of candesartan cilexetil in the existing candesartan cilexetil preparations, and to provide a kind of candesartan cilexetil which can produce good stability and bioavailability Candesartan cilexetil solid preparation solution with high density and simple production process

Method used

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  • Oral candesartan cilexetil solid preparation and preparation method thereof
  • Oral candesartan cilexetil solid preparation and preparation method thereof
  • Oral candesartan cilexetil solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Candesartan cilexetil - preparation of β-cyclodextrin

[0030] 4 g of candesartan cilexetil and 8 g of β-cyclodextrin were mixed and crushed and passed through a 100-mesh sieve to obtain a candesartan cilexetil-β-cyclodextrin composition.

[0031]

Embodiment 2

[0032] Example 2 Candesartan cilexetil tablets formula

[0033]

[0034] Preparation Process:

[0035] 1. Pass the original and auxiliary materials through a 100-mesh sieve, and set aside;

[0036] 2. Weigh the raw materials and auxiliary materials according to the prescription quantity;

[0037] 3. Mix lactose, pregelatinized starch and microcrystalline cellulose evenly;

[0038] 4. Take candesartan cilexetil and red iron oxide and mix well;

[0039] 5. Mix the above two powders with croscarmellose sodium and magnesium stearate;

[0040] 6. Determine the content of the mixed powder and calculate the tablet weight;

[0041] 7. Tablet;

Embodiment 3

[0058] Example 3 Candesartan cilexetil capsule formula

[0059]

[0060] Preparation Process:

[0061] 1. Pass the original and auxiliary materials through a 100-mesh sieve, and set aside;

[0062] 2. Weigh the raw materials and auxiliary materials according to the prescription quantity;

[0063] 3. Mix lactose, pregelatinized starch and microcrystalline cellulose evenly;

[0064] 4. Take candesartan cilexetil and red iron oxide and mix well;

[0065] 5. Mix the above two powders with magnesium stearate evenly;

[0066] 6. Measure the content of the mixed powder and calculate the grain weight;

[0067] 7. Capsules;

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Abstract

The invention discloses an oral candesartan cilexetil solid preparation and a preparation method thereof. The oral solid preparation is prepared from candesartan cilexetil, stabilizer and pharmaceutically acceptable auxiliary ingredients, wherein the stabilizer is beta-cyclodextrin, and the weight of the stabilizer is 0.3 to 3 times that of the candesartan cilexetil. The preparation method comprises the steps of mixing candesartan cilexetil, beta-cyclodextrin or derivatives thereof and red iron oxide and sieving twice with a 100-mesh sieve, and then adding proper pharmaceutical auxiliary ingredients to obtain the candesartan cilexetil preparation. According to the oral candesartan cilexetil solid preparation and the preparation method thereof, the candesartan cilexetil can be inhibited from decomposing and keep long-time stabilizing and the expiry date of the candesartan cilexetil preparation can be prolonged.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a candesartan cilexetil oral solid preparation and a preparation method thereof. [0002] Background technique [0003] The chemical name of candesartan cilexetil is: (±)-1-[[(cyclohexyloxy)carbonyl]oxo]ethyl-2-ethoxy-1-[[2'-(1H-tetrazazo Azolyl-5)-[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylate, its structural formula is: [0004] [0005] Candesartan cilexetil is a non-peptide angiotensin II receptor antagonist, because it increases the specificity and selectivity of angiotensin II receptor level blockade in the circulatory system and tissues, it has a higher specificity and selectivity than angiotensin II The more superior characteristics of converting enzyme (ACE) inhibitors do not increase the action of bradykinin caused by ACE enzymes, so they will not cause coughing side effects. [0006] Candesartan cilexetil is rapidly hydrolyzed into the active met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4184A61K47/40A61K9/20A61K9/48A61P9/12
Inventor 邓俐丽
Owner 邓俐丽
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