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Sustained-release pellets containing captopril serving as active ingredient and preparation method thereof

A technology of sustained-release pellets and active ingredients, applied in the field of sustained-release pellets containing captopril active ingredients and its preparation, can solve problems such as major side effects, and achieve easy industrialization, increased safety, high yield and reproducible effect

Inactive Publication Date: 2011-05-18
TIANJIN TIANCHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The elimination half-life of captopril in the blood is 2.2 to 5 hours. In order to maintain the trough concentration and still be effective, the dosage must be increased, and long-term medication may bring greater side effects

Method used

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  • Sustained-release pellets containing captopril serving as active ingredient and preparation method thereof
  • Sustained-release pellets containing captopril serving as active ingredient and preparation method thereof
  • Sustained-release pellets containing captopril serving as active ingredient and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1, the preparation of drug-containing pellets

[0030]

[0031]

[0032] Mix the prescription amount of lactose (or microcrystalline cellulose) and starch evenly, add the binder prepared by sucrose or hypromellose, use a granulator (or coating pan) to start and roll the pellets to the required The mesh number is 15-30 mesh (lubricant and glidant are added while rolling the pellets), dried, and the best 18-25 mesh is screened out.

[0033]

[0034] Preparation:

[0035] Add captopril, hypromellose (or polyvinylpyrrolidone) and talcum powder described in the prescription into water or 70% ethanol respectively, and stir for 20 minutes to form a uniform mixed solution. In the fluidized bed (or coating pan), keep the temperature of the pellets at 30° C., spray the mixture evenly on the outer layer of the blank pellets obtained in the previous step to prepare drug-containing pellets.

Embodiment 2

[0036] Embodiment 2, preparation of drug-containing pellets

[0037]

[0038] Preparation

[0039] Mix the prescription amount of lactose (or microcrystalline cellulose), starch and medicine evenly, add sucrose and polyethylene glycol or (hypromellose and polyethylene glycol) prepared binder, and use a granulator ( or coating pan) and roll the balls to the required mesh number of 15-30 (adding lubricant and glidant while rolling the balls), sieve out the best 18-25 mesh, and dry to get.

Embodiment 3

[0040] Embodiment 3, the preparation of sustained-release pellets

[0041] prescription

[0042]

[0043] Preparation:

[0044] The pellets obtained in Example 1 were put into a fluidized bed (or coating pan), and the temperature of the pellets was kept at 25°C. Add triethyl citrate and talcum powder to the acrylic resin NE30D aqueous dispersion, stir evenly, and spray on the outer layer of drug-containing pellets at a flow rate of 5ml / min to make sustained-release pellets.

[0045]Embodiment 3, the preparation of sustained-release pellets

[0046] prescription

[0047]

[0048] Preparation

[0049] The pellets obtained in Example 1 are put into a fluidized bed (or coating pan), and the temperature of the pellets is kept at 25°C-28°C. Add triethyl citrate and talcum powder to the aqueous dispersion, stir evenly, and spray on the outer layer of the drug-containing pellets at a flow rate of 5ml / min to make sustained-release pellets.

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PUM

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Abstract

The invention discloses sustained-release pellets containing captopril serving as an active ingredient, which consist of medicament-containing pellets and sustained-release layers. The preparation method of the sustained-release pellets comprises: preparing the medicament-containing pellets by coating captopril on blank pellet cores, or by mixing an auxiliary material and the medicament and forming the mixture into pellets; and preparing coating liquid from a retarder, a pore forming agent and a plasticizer or an antisticking agent, spraying the coating liquid onto the outer layers of the medicament-containing pellets in a coating pan or fluidized bed to obtain sustained-release pellets. The sustained-release pellets prepared by the invention can effectively control the medicament to release in a certain period to maintain stable effective medicament concentration in blood and can avoid sudden release.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and more specifically relates to a sustained-release pellet containing an active ingredient of captopril and a preparation method thereof. Background technique [0002] Hypertension refers to increased arterial systolic and / or diastolic blood pressure in a resting state, often accompanied by disturbances in fat and glucose metabolism, as well as functional or organic changes in heart, brain, kidney, retina and other organs. Characterized systemic disease. Clinically, many hypertensive patients, especially obese patients, are often accompanied by diabetes, and diabetes is often accompanied by hypertension, so the two are called homologous diseases. The reasons are as follows: high blood pressure and diabetes may have a common genetic gene; blood vessels in diabetic patients are sensitive to angiotensin, which has a pressurizing effect; diabetes can easily cause kidney ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/401A61K47/32A61K47/38A61K47/44A61P9/12
Inventor 张国基
Owner TIANJIN TIANCHENG PHARMA
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