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Candesartan cilexetil and amlodipine tablet composition and preparation method thereof

A technology for candesartan medoxomil and amlodipine besylate, applied in the field of medicine, can solve the problems of reduced drug efficacy, increased impurity content, poor stability and the like

Active Publication Date: 2012-09-26
石药集团中诺药业(石家庄)有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The candesartan cilexetil amlodipine composition disclosed above has poor stability. After long-term storage, the content of active ingredients will decrease and the amount of impurities will increase, resulting in decreased drug efficacy and increased side effects.

Method used

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  • Candesartan cilexetil and amlodipine tablet composition and preparation method thereof
  • Candesartan cilexetil and amlodipine tablet composition and preparation method thereof
  • Candesartan cilexetil and amlodipine tablet composition and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 Excipient compatibility test

[0040] Table 1

[0041]

[0042] According to the results of related substances (maximum single impurity, total amount of impurities), except for PEG6000, other excipients have good compatibility with the two active ingredients, but the dosage of PEG6000 needs to be further screened.

Embodiment 2

[0043] The screening of embodiment 2 PEG dosage

[0044] Primary selection of croscarmellose sodium 4%, microcrystalline cellulose 15%, micropowder silica gel 0.5%, magnesium stearate 1%, formula candesartan cilexetil besylate amlodipine (8 parts by weight / 6.93 parts by weight), the remaining mannitol 200SD supplements the total amount of the prescription to 100%, and the dosage of PEG6000 is screened by the results of related substances with an influencing factor of 60 degrees and 10 days.

[0045] Table 2

[0046]

[0047] As can be seen from the results in Table 2, when the dosage range of PEG6000 is 2%-4%, the product impurity amount is low, and when the dosage is 3%, the impurity amount is the lowest, and the degradation products of candesartan cilexetil increase below this dosage range, and above this Amlodipine degradation products increased in the dosage range, and the total amount of impurities increased significantly.

Embodiment 3

[0048] Example 3 Prescription Screening

[0049] With reference to the situation of candesartan cilexetil tablets on the market, it is preliminarily determined that the tablet weight of the combination of candesartan cilexetil and amlodipine besylate is 0.130g.

[0050] Mannitol is non-hygroscopic and is an excellent diluent for moisture-sensitive active ingredients. Its dosage is adjusted to 100% according to the ratio of other excipients.

[0051] The 30-minute dissolution rate of candesartan cilexetil under the dissolution conditions in the quality standard is selected as the main index, and at the same time, the angle of repose reflects the fluidity of the particles, which has a certain relationship with the uniformity of the tablet, so the angle of repose of the mixed powder is secondary index. Since the smaller the angle of repose is better, its weight is set to -1, and the weight of the dissolution rate is 1, that is, the comprehensive score = dissolution rate (%) - an...

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Abstract

The invention discloses a candesartan cilexetil and amlodipine besylate tablet composition. According to the formula, the tablet composition contains 2 to 4 weight parts of polyethylene glycol (PEG) 6000 serving as a stabilizer; and the active ingredients of the composition, namely the candesartan cilexetil and the amlodipine besylate, have high stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a pharmaceutical composition and a preparation method thereof, in particular to a tablet composition of candesartan cilexetil and amlodipine besylate and a preparation method thereof. Background technique [0002] Hypertension is one of the most common cardiovascular diseases and a major public health problem worldwide. At present, the prevalence of hypertension in the world is as high as 31.3%, and the number of people who die from hypertension-related diseases every year accounts for about 100% of the world's death population. 6%. At present, drugs for the treatment of hypertension are roughly divided into the following six categories: diuretics, beta-blockers, angiotensin-converting enzyme inhibitors (ACEI), angiotensin II receptor blockers (ARBs), and calcium antagonists. , α receptor blockers. If in order to maximize the effect of treating hypertension, simply increasing the...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K9/20A61K47/34A61K47/38A61P9/12A61K31/4184
Inventor 姚振江陈维华张芳
Owner 石药集团中诺药业(石家庄)有限公司
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