Clonidine hydrochloride sustained release micropill preparation

A technology of clonidine hydrochloride and sustained-release pellets, which can be used in cardiovascular system diseases, block delivery, drug combination, etc. The incidence of reaction, the effect of high and stable blood concentration

Active Publication Date: 2012-09-05
HEFEI COSOURCE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Patients with high blood pressure need long-term medication, taking too many times a day will cause great obstacles to medication compliance, and there may be missed doses, which will affect the curative effect

Method used

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  • Clonidine hydrochloride sustained release micropill preparation
  • Clonidine hydrochloride sustained release micropill preparation
  • Clonidine hydrochloride sustained release micropill preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] (1) Preparation of pill-containing core (A)

[0047] Clonidine hydrochloride

4.0g

Blank pellet core (sucrose type)

1600g

Opadry (CLEAN)

40.0g

purified water

760.0g

[0048] Preparation Process:

[0049] Weigh Opadry (CLEAN), add it to purified water and stir to dissolve, pass a 100-mesh sieve just before use, then add the prescription amount of clonidine hydrochloride raw material, stir and dissolve, to obtain a coating liquid. Weigh the blank pellets and add them to the fluidized bed coating machine (WBF-5G, Chongqing Yingge Granulation Coating Technology Co., Ltd.), and use the low spray coating system (Wurster system) for coating. The coating parameters of the equipment are :Inlet air volume 250m 3 / hr, inlet air temperature 50℃, atomization pressure 2kg / cm 2 , The flow rate of the coating liquid is 7rpm. After the coating liquid is sprayed, it is fluidized and dried for 10 minutes and then discharged to obtain a pill-containing core.

[0050] (2) Isol...

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Abstract

The invention relates to the field of medicinal preparations, in particular to a clonidine hydrochloride sustained release preparation and a preparation method thereof. The clonidine hydrochloride sustained release preparation is characterized in that: a sustained release coating membrane is divided into two layers, wherein a sustained release coating membrane of an inner layer contains a pore-forming agent, and a sustained release coating membrane on an outer layer does not contain the pore-forming agent; and a weight ratio of a sustained release coating on the inner layer to a sustained release coating of the outer layer is (1:1)-(2:5), and the weight of sustained release coatings on inner and outer layers are increased by 7 to 8 percent. In the sustained release preparation, two sustained release layers are coated, so that medicaments are released slowly, safely and effectively.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sustained-release preparation of clonidine hydrochloride and a preparation method thereof. Background technique [0002] Clonidine hydrochloride has a chemical name: 2-[(2,6-dichlorophenyl)imino]imidazolidine hydrochloride. It is an antihypertensive drug that is well absorbed in the gastrointestinal tract. After oral administration, 70% to 80% is absorbed and quickly distributed to various organs. The concentration of the drug in the tissue is higher than that in the plasma, and it can accumulate in the blood-brain barrier. brain tissue. The protein binding rate is 20%-40%. Half an hour to 1 hour after oral administration, the blood pressure will be lowered, and the blood concentration will reach the peak at 3 to 5 hours, usually 1.35 ng / ml, and the effect will last for 6 to 8 hours. The elimination half-life is 12.7 (6-23) hours, and it is prolonged with renal insuffic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/4168A61K47/38A61P9/12
Inventor 高署
Owner HEFEI COSOURCE PHARMA CO LTD
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