Nimesulide sustained-release dropping pill and preparation method thereof

A technology of slow-release dripping pills and skeleton materials, applied in the field of Shuli as raw materials, can solve the problems of unstable blood drug concentration, low dissolution rate, large dust pollution, etc., and achieve improved bioavailability, accelerated dissolution and absorption, and automation high degree of effect

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

The controlled-release composition can control the active ingredients of the drug to release the drug at a fixed time and quantity at a zero-order rate, and the processing is complicated and the cost is high.
[0008] Due to reasons such as preparation technology, the oral preparations of most drugs all have long dissolution time, low dissolution rate, poor absorption, unstable blood drug concentration, many times of taking medicine, hepatic and intestinal first-pass effect and bioavailability after taking. Low-level problems, which affect the efficacy of the drug and 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.
[0009] 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 formulation of nimesulide to meet the health needs of the majority of patients

Method used

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  • Nimesulide sustained-release dropping pill and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0037]Now with several groups of specific examples, the preparation method of the nimesulide sustained-release dropping pills of the present invention will be further described.

[0038] First group:

[0039] Based on the total weight of 100g, weigh 10% of the matrix PEG10000, 10% of PEG6000, 40% of PEG4000, 15% of stearic acid, 5% of glyceryl monostearate, and 20% of the raw material nimesulide; prepared according to the above-mentioned preparation method.

[0040] The obtained product has a cumulative release percentage of 42-54% in 2 hours, a cumulative release percentage of 67-83% in 6 hours, and a cumulative release percentage of 79-94% in 10 hours, with better hardness and roundness.

[0041] Second Group:

[0042] Based on the total weight of 100g, weigh the matrix PEG10000 16%, PEG4000 50%, microcrystalline cellulose 4%, stearic acid 10%, glyceryl monostearate 7%, brazilian palmitic acid 3%, raw material Nimesul Profit 10%; prepared according to the above-mentioned p...

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Abstract

The invention relates to a drug compound playing the role of diminishing inflammation, alleviating pain and eliminating fever and being used for treating arthritis, odynolysis and pyrexia caused by upper respiratory tract infection, and particularly relates to a drug compound oral pharmaceutical formulation adopting nimesulide as the ingredient and being prepared jointly with the medicinal carrier used as the stroma. The drug compound aims to supplement the deficiency of the prior oral nimesulide pharmaceutical formulation and provide a drug compound oral formulation, sustained-release nimesulide dropping pill which has high bioavailability, controllable release time, long-acting effect, reduced frequency of drug taking for a patient, low cost and absence of contamination during the production. The sustained-release nimesulide dropping pill adopts nimesulide as the chemical ingredient and is prepared jointly with the medicinal carriers of hydrophilic frame ingredients and hydrophobic frame ingredients used as the stroma.

Description

technical field [0001] The invention belongs to the technical field of sustained-release pharmaceuticals, and relates to a pharmaceutical composition with anti-inflammatory, analgesic and antipyretic effects for treating arthritis, pain relief and fever caused by upper respiratory tract infection-nimesulide sustained-release drops Pills and their preparation methods, particularly related to the preparation of nimesulide as a raw material, mixed with a hydrophilic skeleton material and a hydrophobic skeleton material as a matrix and a pharmaceutically acceptable carrier. Background technique [0002] Nimesulide is a non-microbial anti-inflammatory drug with antipyretic and analgesic activity. The therapeutic effect is mainly due to its ability to inhibit the synthesis of prostaglandins by inhibiting cyclooxygenase. But this action also inhibits gastroprotective prostaglandins, leading to gastrointestinal intolerance. [0003] Nimesulide (nimesulide) was developed by Boehrin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/34A61K47/38A61K31/18A61P29/00A61P19/02A61P11/00A61K47/10
Inventor 曲韵智
Owner 北京博智绿洲医药科技有限公司
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