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A kind of indomethacin solid dispersion sustained-release preparation and preparation method thereof

A technology for indomethacin and solid dispersion, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, anti-inflammatory agents, etc., and can solve the problem of short half-life of the drug and cumulative drug release of less than 87%. problems, to achieve the effect of low moisture absorption rate, stable drug release, and long-lasting effect

Active Publication Date: 2020-11-13
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Third, the biological half-life of indomethacin is short, and conventional preparations include tablets and capsules, which are taken three times a day
CN201710188638.6 (indomethacin sustained-release tablets and its preparation method) discloses that hypromellose, carbomer, and polyvinyl alcohol are used as the hydrophilic gel skeleton, and behenate and magnesium stearate are combined Sustained-release tablets of lubricants, the paddle method is only mentioned for in vitro release, no specific release conditions, and the cumulative drug release in 24 hours is less than 87%

Method used

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  • A kind of indomethacin solid dispersion sustained-release preparation and preparation method thereof
  • A kind of indomethacin solid dispersion sustained-release preparation and preparation method thereof
  • A kind of indomethacin solid dispersion sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Hot-melt extrusion sustained-release preparation with single HPC as retarder

[0045]

[0046] Preparation: Mix indomethacin and HPC according to the above ratio, dry in an oven at 50°C, measure 1.5% moisture, extrude with a hot melt extruder at 160°C, extrude at 50 rpm to obtain a strip, which is cut into 40 mg containing drug with a sharp knife of strips.

[0047] Determination of release degree: Take indomethacin hot-melt extrudate, approximately equivalent to indomethacin containing 40mg, paddle method, 50rpm, pH5.8 PBS 900ml is the release medium, UV method, the content of indomethacin at 320nm, And calculate the cumulative drug release, the results are as follows figure 1 shown.

[0048] from figure 1 It can be seen that the molecular weights of HPCEF, HPCL and HPCGF (GXF) are 80,000, 171,000 and 370,000, respectively. When the molecular weight of HPC is 171,000 and below, and the drug loading ratio is 10:90, the zero-order kinetic drug release ti...

Embodiment 2

[0049] Embodiment 2HPCEF and HPCGF are the hot melt extrusion sustained-release preparation of combined retarder

[0050]

[0051] The preparation method and the method for measuring the release degree are the same as in Example 1, and the results are as follows figure 2 shown.

[0052] from figure 2 It can be seen that when HPCEF and HPCGF (GXF) are used in combination, when the dosage of HPC-EF (EXF) is 5% to 20%, both prescription 5 and prescription 6 can maintain zero-order kinetic drug release for 14h, and the cumulative drug release is complete in 24h. When the drug-loading ratio was increased, zero-order kinetic drug release was maintained for 24 hours, but the rate was slightly slower.

Embodiment 3

[0053] Example 3HPCEF and HPCMF are combined blocker hot melt extrusion sustained-release preparation

[0054]

[0055] The preparation method and the method for measuring the release degree are the same as in Example 1, and the results are as follows image 3 shown.

[0056] from image 3 It can be seen that when HPCEF and HPCMF (MXF) are used in combination, when the dosage of HPC-EF (EXF) is 20% to 45%, the drug release shows zero-order kinetics. The cumulative drug release was complete within 10 24h of the prescription, and the drug release rate was slightly slower in other prescription ratios.

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Abstract

The invention discloses a solid dispersion slow-release preparation of indometacin prepared by adopting a hot melt extrusion method (HME), and adopting hydroxy propyl cellulose as a carrier or hydroxypropyl cellulose and hydroxypropyl methylcellulose as a combined carrier through one step, meanwhile, phosphate buffer with the pH being 5.8 is adopted as a release medium, and a medicine release curve with zero-order kinetics is obtained. Compared with the existing method, the method provided by the invention has the advantages that (1) the slow-release preparation is prepared by utilizing the thermoplastic property of hydroxy propyl cellulose, and the one-step hot-melt extrusion with hydroxypropyl methylcellulose and medicines; (2) the medicine release curve is in zero-order kinetics, and the medicine release is stable; (3) no organic solvent is adopted in the preparation process; (4) an appropriate shape can be designed according to requirements; (5) the moisture rate of the prepared preparation is low compared with that of a physical mixture; (6) no medicine release exists in acid, medicine release begins under the pH environment of the small intestines, so that the degradation ofindometacin in acid is avoided, meanwhile, the defects that the existing indometacin slow-release preparation slowly releases medicines in the pH environment of the small intestine, the release degree is low, and the medicine release is not complete in the later period, are overcome, and the oral slow-release preparation taking effect rapidly, being stable in medicine release, and being long in effect keeping time is obtained.

Description

technical field [0001] The invention relates to an indomethacin solid dispersion sustained-release preparation and its preparation. Background technique [0002] Indomethacin is a non-steroidal anti-inflammatory drug with analgesic and antipyretic effects. It is clinically used for rheumatoid arthritis, rheumatoid arthritis, tumor pain relief and tumor blood disease antipyretic. Indomethacin pKa 4.2, the solubility is pH-dependent, the solubility is 0.00mg / ml in pH1.2 and pH4.0, 0.71mg / ml in pH6.8 PBS, and 0.01mg / ml in water (Japan "Medical Medicines"). Quality Information Collection, Orange Book). [0003] The conventional commercially available formulations of indomethacin are capsules and tablets, with doses of 25 mg and 50 mg. Due to the solubility problem, the dissolution of commercially available ordinary capsules was determined by the rotating basket method, 100 rpm, pH 7.2 phosphate buffer-water (1:4) 750 ml as the medium. Iroko Pharmaceuticals uses micronization ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/405A61K47/38A61P29/00
CPCA61K9/0002A61K9/2054A61K31/405
Inventor 熊素彬刘永娇伊珊
Owner ZHEJIANG UNIV OF TECH