Candesartan cilexetil double-release capsule and preparation method thereof

A technology of candesartan medoxomil and double-release capsules is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., and can solve the problem of poor maintenance of blood drug concentration, decreased blood pressure, and slow dissolution rate. and other problems, to achieve the effect of high maintenance of blood drug concentration, effective antihypertensive effect and fast onset time

Inactive Publication Date: 2013-01-23
TAIZHOU VOCATIONAL & TECHN COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the good selectivity of candesartan cilexetil (the affinity for the AT1 receptor is more than 10,000 times higher than that of the AT2 receptor), it has superior characteristics than angiotensin converting enzyme (ACE) inhibitors and does not increase the ACE enzyme. Bradykinin effect, thus will not cause cough side effects, strong antihypertensive effect and the advantages of small dosage, but, due to the poor water solubility of candesartan cilexetil, the dissolution rate is slow, and it is difficult to make common oral preparations. The absorption and onset time are relatively slow, and the bioavailability is low (absolute bioavailability is 15%, relative bioavailability is 42%)
Although the antihypertensive effect of candesar...

Method used

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  • Candesartan cilexetil double-release capsule and preparation method thereof
  • Candesartan cilexetil double-release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Preparation of immediate-release candesartan cilexetil solid dispersion

[0067] prescription:

[0068] Candesartan cilexetil: 6g

[0069] PEG6000: 30g

[0070] Poloxamer 188: 6g

[0071] Absolute ethanol: 90mL

[0072] Acetone: 15mL

[0073] The quick-release candesartan cilexetil solid dispersion is specifically prepared as follows:

[0074] Add 30g of PEG6000 and 6g of poloxamer 188 weighed into the reaction flask, then add 75mL of absolute ethanol, heat to 35°C and stir until dissolved to obtain the first solution;

[0075] Add the weighed 6g of candesartan cilexetil into another reaction flask, then add a mixed solvent of 15mL of absolute ethanol and 15mL of acetone, stir at room temperature until dissolved and clear, and obtain the second solution;

[0076] Slowly add the second solution obtained above into the first solution, stir for 15 minutes to make the mixture uniform, heat up to 45°C and carry out vacuum distillation to remove the solvent in the syste...

Embodiment 2

[0096] Preparation of immediate-release candesartan cilexetil solid dispersion

[0097] prescription:

[0098] Candesartan cilexetil: 6g

[0099] PEG6000: 24g

[0100] Poloxamer 188: 12g

[0101] Absolute ethanol: 90mL

[0102] Acetone: 15mL

[0103] The quick-release candesartan cilexetil solid dispersion is specifically prepared as follows:

[0104] Add 24g of PEG6000 and 12g of poloxamer 188 weighed into the reaction flask, then add 75mL of absolute ethanol, heat to 35°C and stir until dissolved to obtain the first solution;

[0105] Add the weighed 6g of candesartan cilexetil into another reaction flask, then add a mixed solvent of 15mL of absolute ethanol and 15mL of acetone, stir at room temperature until dissolved and clear, and obtain the second solution;

[0106] Slowly add the second solution obtained above to the first solution, stir for 15 minutes to make the mixture uniform, heat up to 55°C and carry out vacuum distillation to remove the solvent in the syste...

Embodiment 3

[0125] Preparation of immediate-release candesartan cilexetil solid dispersion

[0126] prescription:

[0127] Candesartan cilexetil: 3g

[0128] PEG6000: 15g

[0129] Poloxamer 188: 3g

[0130] Absolute ethanol: 45mL

[0131] Acetone: 5mL

[0132] The concrete of quick-release candesartan cilexetil solid dispersion is prepared according to the following method:

[0133] Add 15g of PEG6000 and 3g of poloxamer 188 weighed into the reaction flask, then add 40mL of absolute ethanol, heat to 35°C and stir until dissolved to obtain the first solution;

[0134] Add the weighed 3g of candesartan cilexetil into another reaction flask, then add a mixed solvent of 5mL of absolute ethanol and 5mL of acetone, stir at room temperature until dissolved and clear, and obtain the second solution;

[0135] Slowly add the second solution obtained above to the first solution, stir for 15 minutes to make the mixture uniform, and then heat up to 50°C to conduct vacuum distillation to remove t...

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Abstract

The invention relates to a candesartan cilexetil double-release capsule and a preparation method thereof, belonging to the technical field of pharmaceutical formulations and solving the technical problems of low dissolution speed of a candesartan cilexetil formulation, short effectiveness time and poor blood drug concentration continuity in the prior art. Each capsule of the candesartan cilexetil double-release capsule comprises quick release particles and slow release particles, wherein the weight ratio of the active components of candesartan cilexetil in the quick release particles and the slow release particles is 1.0: (0.5-2.0). The preparation method comprises the steps of: uniformly mixing the quick release particles and the slow release particles; filling into the capsule body of a capsule shell; and covering a capsule cover to obtain the candesartan cilexetil double-release capsule. The candesartan cilexetil double-release capsule has high dissolution speed, the effectiveness time is quickened, the stable blood drug concentration effect is realized, and the corresponding preparation method has the advantages of simplicity in process and easiness in operation.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a candesartan cilexetil double-release capsule and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Candesartan cilexetil is an angiotensin II receptor (AT1) antagonist, which blocks the vasoconstriction, sympathetic nerve excitation and baroreceptor sensitivity caused by AT1 in the circulation and local tissues to lower blood pressure by antagonizing AT1. In addition to clinically used for the treatment of hypertension, heart failure, myocardial infarction, etc., it is also used for hypertension with left ventricular hypertrophy, diabetic nephropathy, etc. Due to the good selectivity of candesartan cilexetil (the affinity for the AT1 receptor is more than 10,000 times higher than that of the AT2 receptor), it has superior characteristics than angiotensin converting enzyme (ACE) inhibitors and does not incr...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61K9/52A61P9/04A61P9/10A61P9/12A61P13/12
Inventor 范长春陈建军朱燕妮傅璐仙徐飞瑶张戈辉
Owner TAIZHOU VOCATIONAL & TECHN COLLEGE
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