Carvedilol sustained-release capsule

A slow-release layer and slow-release pellet technology, which can be applied to non-active ingredients in medical preparations, cardiovascular system diseases, organic active ingredients, etc. bigger problems

Inactive Publication Date: 2014-04-30
HEFEI HEYUAN PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The carvedilol sustained-release capsule preparations prepared by the above patents are all prepared by mixing and filling three different speed pellets, and the dosage is greatly affected by the mixing uniformity of the three pellets and the content of each pellet. The ratio of the three and the changes in their respective contents all affect the quality and release degree of the final product, thereby affecting the efficacy of the drug
Moreover, the sustained-release pellets in the disclosed sustained-release preparat

Method used

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  • Carvedilol sustained-release capsule
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  • Carvedilol sustained-release capsule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation of drug-containing pellet cores

[0044]Get carvedilol 80g, polyoxyethylene hydrogenated castor oil 10g is placed in 400ml75% ethanol aqueous solution, stir to make it suspend, adopt fluidized bed (multifunctional fluidized bed test machine WBF-1, Chongqing Yingge coat coating manufacture) Granule Technology Co., Ltd.) on the blank pellet core 400g (0.3 ~ 0.5mm), the spray speed is 5rpm / min, the air inlet temperature is 40℃, and the air inlet volume is 80m 3 / min, the material temperature is 28°C, and the atomization pressure is 0.2Mpa. Keep the solution in a stirring state during the spraying process, and continue to maintain the fluidized state for 15 minutes after the drug is applied.

Embodiment 2

[0046] Preparation of pill-containing cores

[0047] Get carvedilol 80g, polyoxyethylene hydrogenated castor oil 10g is placed in 400ml75% ethanol aqueous solution, stir to make it suspend, adopt fluidized bed (multifunctional fluidized bed test machine WBF-1, Chongqing Yingge coat coating manufacture) Granule Technology Co., Ltd.) on the blank pellet core 400g (0.3 ~ 0.5mm), the spray speed is 5rpm / min, the air inlet temperature is 40℃, and the air inlet volume is 80m 3 / min, the material temperature is 28°C, and the atomization pressure is 0.2Mpa. Keep the solution in a stirring state during the spraying process, and continue to maintain the fluidized state for 15 minutes after the drug is applied.

Embodiment 3

[0049] Get Eudragit NE30D aqueous dispersion 100g, wherein solid content is 30%, solvent is water, adds plasticizer triethyl citrate 7.5g wherein, antitack agent glyceryl monostearate 7.5g, porogen Eudragit L100-553g and Eudragit S1006g were uniformly dispersed at high speed, and the drug-containing pellets prepared in Example 1 were used as pellet cores, and the fluidized bed equipment was used for coating. The air inlet temperature is 25°C, and the air inlet volume is 80m 3 / min, the material temperature is 20°C, the atomization pressure is 0.25Mpa, the pumping speed of the peristaltic pump is 8rpm / min, and the coating weight gain is 10.8%. After the coating is completed, put it into an oven for aging at 40°C and sprinkle 0.5% micropowder silica gel into it. During the aging process, the pellets stick together, take them out after 2 hours, measure the content, and put the pellets into capsules.

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a carvedilol sustained-release capsule. The carvedilol sustained-release capsule is characterized by consisting of a drug-containing pill core and a sustained-release layer, wherein the drug-containing pill core contains a blank pill core and carvedilol; the sustained-release layer contains a film-forming material and a pore-forming agent; the drug-containing pill core also contains a solubilizer; a weight ratio of the solubilizer to the active ingredients is (1:8)-(3:8); the sustained-release layer accounts for 12.6-16.1 percent of the total weight of the micro pill; the pore-forming agent consists of a methacrylic acid-ethyl acrylate (1:1) copolymer and a methacrylic acid-ethyl acrylate (1:2) copolymer; the pore-forming agent accounts for 6-11 percent of the total weight of the sustained-release layer. According to the carvedilol sustained-release preparation, only a micro pill is needed to be prepared, and a sustained-release effect can be achieved. Moreover, the medicine is slowly and fully released in main absorption parts at the pH of 5.5-6.8, the drug action time is prolonged, and the phenomenon that the safety risk of a patient is increased due to the local drug overdose caused by drug short-rate pulse release is avoided.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to carvedilol sustained-release capsules. Background technique [0002] Carvedilol was developed by the Boehringer Mannhei company in Germany. It was first approved by the FDA for marketing in the United States on September 14, 1995. Its chemical name is (±) 1-carbazole-4-oxyl-3-[2 -(2-methoxyphenoxy)ethylamino]-2-propanol. Carvedilol has nonselective beta-blocker, alpha-blocker and antioxidant properties. Dilates blood vessels by selectively blocking alpha1 adrenergic receptors. Carvedilol reduces peripheral resistance through vasodilation and inhibits the renin-angiotensin-aldosterone system through β-blockade. Vasorenin activity is reduced and fluid retention rarely occurs. Carvedilol has no intrinsic sympathomimetic activity and, like propranolol, is membrane stable. [0003] WO2005051322 discloses a sustained-release preparation of carvedilol and its salts. The p...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/52A61K31/403A61K47/44A61K47/32A61K47/18A61P9/08
Inventor 高署王欲斌
Owner HEFEI HEYUAN PHARM TECH CO LTD
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