Ibuprofen preparation and preparation method thereof

A preparation and diluent technology, applied in anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of no sudden release effect, affect the therapeutic effect, fast release speed, etc., achieve great clinical application value, reduce The number of doses, the effect of solving the slow onset

Inactive Publication Date: 2014-12-31
SHANGHAI SUNTECH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the half-life of ibuprofen is about 2 hours, ordinary preparations need to be taken several times a day to maintain the blood concentration level, which will obviously reduce the patient's compliance with taking, and the phenomenon of forgetting or missing doses will affect the therapeutic effect; At the same time, the initial release dose of ordinary preparations is relatively large, the release r

Method used

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  • Ibuprofen preparation and preparation method thereof
  • Ibuprofen preparation and preparation method thereof
  • Ibuprofen preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061]

[0062]

[0063] Dissolve 30 grams of hypromellose in 345 grams of purified water to make an aqueous solution, mix 600 grams of ibuprofen and 300 grams of microcrystalline cellulose evenly, and use an aqueous solution of 8% hypromellose to rapidly wet granulate The wet material is prepared in the SHK-4B machine, and the wet material is made into drug-containing pellets by using the extrusion spheronizer of Chongqing Yingge, and the drug-containing pellets are dried to obtain immediate-release pellets. The received immediate-release pellets were divided into three parts. 90 grams of acrylic resin and 40 grams of talcum powder, 6 grams of triethyl citrate are made into the coating solution of 20% solid content, and two parts of micropills in the micropills collected are carried out using Gladt GPCG-2 fluidized bed Sustained-release coating to prepare sustained-release coated pellets.

[0064] Mix the sustained-release coated pellets with another part of the immedi...

Embodiment 2

[0066] According to Chinese Pharmacopoeia Dissolution Determination Method (appendix XC first method), with phosphate buffer (pH7.2) 900ml as dissolution medium, rotating speed is 100 revolutions per minute, the capsule produced in Example 1 is carried out dissolution detection, in The release rate at each set time point is as follows: 40% release in 30 minutes, 45% release in 1 hour, 65% release in 4 hours, 77% release in 8 hours, 88% release in 12 hours, 96% release in 16 hours, and 98% release in 20 hours , and compared it with the release of commercially available sustained-release tablets (Ibuprofen Sustained-release Tablets Shanghai Xinyi Pharmaceutical Co., Ltd.) and ordinary tablets (Ibuprofen Tablets Shanghai Xinyi Pharmaceutical Co., Ltd.). (See figure 1 )

Embodiment 3

[0068]

[0069]

[0070] Dissolve 15 grams of polyvinylpyrrolidone in the slow-release part in 60 grams of purified water to prepare a 20% aqueous solution, mix it with 500 grams of ibuprofen and 250 grams of microcrystalline cellulose, and use 20% polyvinylpyrrolidone solution in the rapid Granulate in a wet granulator, dry, and mix the dried granules after sieving, 150 grams of hypromellose, 6 grams of silicon dioxide, and 5 grams of magnesium stearate to make a slow-release matrix, which is set aside.

[0071] Dissolve 20 grams of polyvinylpyrrolidone in the immediate release part in 60 grams of purified water to form a 25% aqueous solution, mix 150 grams of microcrystalline cellulose and 300 grams of ibuprofen evenly, and use 25% polyvinylpyrrolidone solution in the rapid Granulate in a wet granulator SHK-4B, dry, mix the sieved dry granules, 40 grams of crospovidone, 4 grams of silicon dioxide, and 3 grams of magnesium stearate to make an immediate-release matrix, re...

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Abstract

The invention provides a novel ibuprofen preparation comprising a fast release part and a sustained release part. The ibuprofen as an active component in the fast release part accounts for 20% to 60% by weight of the active component ibuprofen in the novel ibuprofen preparation, and preferably accounts for 30% to 50%, and the ibuprofen as an active component in the sustained release part accounts for 80% to 40%by weight of the active component ibuprofen in the novel ibuprofen preparation, and preferably accounts for 70% to 50%. Single dose of the novel ibuprofen preparation contains 200-1000mg of ibuprofen, and preferably contains 300mg or 600mg of ibuprofen. After the product is taken, according to Chinese pharmacopoeia releasing rate detection method, the fast release part reach the maximum release value in 30 minutes, the slow release time of the sustained release part can maintain 12 to 20 hours. Drugs can relatively much release during the early stage of medication, effective drug concentration in the blood can be rapidly reached, the problem of two slow drug effect can be solved, because of the existence of the sustained-release part, the drugs can slowly and sustainedly release in the body, maintain proper blood drug concentration, play the role of continue treatment and reduce administration times.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a novel ibuprofen preparation and a preparation method thereof. Background technique [0002] Ibuprofen is a non-steroidal anti-inflammatory drug, which mainly inhibits the synthesis of cyclooxygenase and prostaglandins to achieve anti-inflammatory and analgesic effects, and plays an antipyretic effect through the hypothalamic thermoregulation center, and has a greater promotional effect. Clinically, it is generally suitable for relieving the acute attack or persistent joint swelling and pain symptoms of various chronic arthritis such as rheumatoid arthritis, osteoarthritis, spondyloarthropathy, gouty arthritis, rheumatoid arthritis, etc. Etiological treatment and control of the course of the role. For the treatment of various non-articular soft tissue rheumatic pains, such as shoulder pain, tenosynovitis, bursitis, myalgia and post-exercise injury pain, etc.; acute mild and modera...

Claims

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Application Information

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IPC IPC(8): A61K47/38A61K47/32A61K47/34A61K31/192A61P29/00A61P19/02
Inventor 何平周林伟
Owner SHANGHAI SUNTECH PHARMA
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