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Nicergoline sustained-release dropping pill and preparation method thereof

A technology of sustained-release dropping pills and nicergoline, which is applied in the field of pharmaceutical compositions and oral sustained-release dropping pill preparations, which can solve the problems of low dissolution rate, unstable blood drug concentration, and easy occurrence of toxicity, etc., and achieve accelerated dissolution and absorption , improve bioavailability, increase the effect of stability

Inactive Publication Date: 2008-09-24
北京博智绿洲医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to preparation technology and other reasons, most oral preparations of drugs have long dissolution time, low dissolution rate, poor absorption, unstable blood drug concentration, many times of taking drugs, and have hepatic and intestinal first-pass effects and bioavailability after taking. Lower problems, which affect the efficacy of the drug, also directly affect the therapeutic effect
In addition, conventional oral dosage forms, such as tablets, capsules, etc., will produce relatively large dust pollution due to the granulation process in the preparation process, which will cause harm to the health of the staff to a certain extent, and will also cause harm to the human body. some pollution to the environment
Furthermore, the production process of conventional oral preparations is complicated and the production cost is high, so that the cost of medication for patients is also increased, which is not conducive to improving the ability of patients to seek medical treatment, and is also not conducive to improving the overall health level of society.
[0006] Although the injection has the advantages of fast onset of action and high bioavailability, its production process is complicated, the cost is higher, and it is also accompanied by inconvenient use, prone to toxicity, side effects, and great pain for patients. Looking for a more suitable oral preparation of nicergoline to meet the health needs of the majority of patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0030] Now with several groups of specific examples, the preparation method of Nicergoline sustained-release dripping pills of the present invention will be further described.

[0031] First group:

[0032] Based on the total weight of 100g, weigh the matrix PEG4000 40%, PEG6000 10%, PEG10000 5%, polyoxyl (40) stearate 10%, stearic acid 15%, glyceryl monostearate 10%, raw material nylon Ergoline 10%; prepared according to the above preparation method.

[0033] The obtained product has a 2-hour cumulative release percentage of 33-51%, a 6-hour cumulative release percentage of 64-77%, a 10-hour cumulative release percentage of 80-91%, good roundness and good hardness.

[0034] Second Group:

[0035] Based on a total weight of 100g, weigh 35% of the matrix PEG4000, 25% of PEG6000, 10% of PEG10000, 10% of stearic acid, 7% of glyceryl monostearate, and 13% of the raw material nicergoline; prepared according to the above-mentioned preparation method.

[0036] The obtained product...

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PUM

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Abstract

The invention relates to a drug compound playing the role of retarding Alpha-receptors and expanding blood vessels, and is used for improving low desires and affective disorders due to cerebral arteriosclerosis and stroke sequelae and treating vascular dementia. The drug compound aims to supplement the deficiency of the prior oral pharmaceutical formulation used for hemangiectasis and provide a drug compound oral formulation, sustained-release nicergoline dropping pill which has high bioavailability, steady plasma concentration, low frequency of drug taking, low cost and absence of contamination during the production. The sustained-release nicergoline dropping pill adopts nicergoline as the ingredient and is prepared jointly with the medicinal carrier used as the stroma.

Description

technical field [0001] The present invention relates to a pharmaceutical composition with α-receptor blocking effect and vasodilator effect, which is used to improve cerebral arteriosclerosis and cerebral apoplexy sequelae caused by depression and affective disorder, and is used for treating vascular dementia. Nicergoline is a pharmaceutical composition prepared as a raw material, which is an oral sustained-release drop pill preparation. Background technique [0002] Existing nicergoline is a semi-synthetic ergot derivative, which has a-receptor blocking effect and vasodilation effect, and is clinically used to improve cerebral arteriosclerosis and cerebral apoplexy sequela caused by depression and affective disorder. Or for the treatment of acute and chronic peripheral circulatory disorders (such as: limb vaso-occlusive disease, Raynaud's syndrome, other poor symptoms of peripheral circulation), and can be used for the treatment of vascular dementia, especially in the early...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/48A61K47/34A61P25/28A61P9/10A61P9/14A61K47/10A61K47/14
Inventor 曲韵智
Owner 北京博智绿洲医药科技有限公司
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