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Capsule preparation containing candesartan cilexetil and preparation method of capsule preparation

A technology of candesartan cilexetil and capsules, which is applied in the field of capsule preparations containing candesartan cilexetil and its preparation, and can solve the problems of inability to improve bioavailability, low oral bioavailability, slow absorption and onset time, etc. , to achieve the effect of improving bioavailability, high dissolution, and good reproducibility of production process

Inactive Publication Date: 2020-03-27
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] After investigation, it was found that candesartan cilexetil is a poorly soluble drug with low oral bioavailability
Invention patent CN1086998A discloses a preparation method of candesartan cilexetil tablet that adds an oily compound with a low melting point to increase the drug stability of candesartan cilexetil, but the original candesartan cilexetil tablet (8mg) prepared according to this method The relative bioavailability is only 34% (95% CI: 28-40%), and the absorption and onset time are relatively slow
CN101623275A discloses a candesartan cilexetil capsule and a preparation method thereof, adopting a hydroxypropyl cellulose capsule shell, intending to solve the problem of dissolution decline during storage, but unable to improve the in vivo bioavailability of the preparation

Method used

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  • Capsule preparation containing candesartan cilexetil and preparation method of capsule preparation
  • Capsule preparation containing candesartan cilexetil and preparation method of capsule preparation
  • Capsule preparation containing candesartan cilexetil and preparation method of capsule preparation

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Experimental program
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Effect test

Embodiment 1

[0035] Candesartan cilexetil capsules (batch of 1000 capsules)

[0036]

[0037] Usage and dosage: once a day, 4~8mg each time.

[0038] Preparation:

[0039] a: Add candesartan cilexetil, microcrystalline cellulose, corn starch, hydroxypropyl cellulose, carmellose calcium, and polyethylene glycol 6000 into a wet granulator and stir to make the mixture uniform;

[0040] b: adding purified water to the mixture in step a to make a soft material;

[0041] c: Prepare pellets by extrusion spheronization, dry the pellets in a fluidized bed, and measure the water content below 4%;

[0042] d: adding magnesium stearate to the pellets and mixing evenly;

[0043] e; filling the mixture obtained in step d into the No. 3 gelatin capsule shell to prepare capsules containing candesartan cilexetil.

[0044] The extrusion spheronization method adopts a screen with an aperture of 1200 μm, the rotation speed of the spheronizer in the extrusion spheronization method is 1000 rpm, and the s...

Embodiment 2

[0046] Candesartan cilexetil capsules (batch of 1000 capsules)

[0047]

[0048] Preparation:

[0049] a: Add candesartan cilexetil, microcrystalline cellulose, lactose, hydroxypropyl cellulose, croscarmellose sodium, and polyethylene glycol into a wet granulator and stir to make 6000 mix evenly;

[0050] b: adding purified water to the mixture in step a to make a soft material;

[0051] c: Prepare pellets by extrusion spheronization, dry the pellets in a fluidized bed, and measure the water content below 4%;

[0052] d: adding magnesium stearate to the pellets and mixing evenly;

[0053] e; filling the mixture obtained in step d into the No. 3 gelatin capsule shell to prepare capsules containing candesartan cilexetil.

[0054] The binder solution is obtained by adding hydroxypropyl cellulose to water and stirring evenly;

[0055] The extrusion spheronization method adopts a screen with an aperture of 600 μm, and the rotation speed of the spheronizer in the extrusion sp...

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Abstract

The invention belongs to the technical field of medicines and in particular discloses a capsule preparation containing candesartan cilexetil and a preparation method of the capsule preparation. The preparation method comprises the following steps: mixing the following components in parts by weight: 2-32 parts of candesartan cilexetil, 10-150 parts of a diluent 1, 10-150 parts of a diluent 2, 0.5-8parts of a disintegrant, 1-10 parts of an adhesive and 0.5-10 parts of a low melting point oily compound, preparing pellets by using an extrusion and rolling method, mixing 0.05-4 parts of a lubricant with the pellets, and filling a capsule shell with the mixture, so as to obtain the capsule preparation. The capsule preparation containing candesartan cilexetil, which is disclosed by the invention, is prepared by using an extrusion and rolling preparation process and has good dissolution performance, and the bioavailability of candesartan cilexetil of the capsule preparation is greatly improved when being compared with that of a candesartan cilexetil preparation in the market.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a capsule preparation containing candesartan cilexetil and a preparation method thereof. Background technique [0002] Candesartan cilexetile is a new type of angiotensin Ⅱ receptor antagonist for hypertension and chronic heart failure. Candesartan cilexetil is its inactive prodrug, which is almost completely hydrolyzed into candesartan after gastrointestinal absorption. Antagonizing AT1 blocks the vasoconstriction, sympathetic nerve excitation and baroreceptor sensitivity caused by AT1 in the circulation and local tissues, and increases the effects to achieve the antihypertensive effect. [0003] After investigation, it was found that candesartan cilexetil is a poorly soluble drug with low oral bioavailability. Invention patent CN1086998A discloses a preparation method of candesartan cilexetil tablet that adds an oily compound with a low melting point to increase t...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K47/36A61K47/38A61K47/10A61K31/4184A61P9/12A61P9/04
CPCA61K9/1641A61K9/1652A61K31/4184A61P9/04A61P9/12
Inventor 周小梅高丹丹江云霞
Owner QINGDAO HUANGHAI PHARM CO LTD
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