Preparation method of ibuprofen transdermal sustained-release preparation

A slow-release preparation and transdermal technology, which is applied in the fields of anti-inflammatory agents, pharmaceutical formulations, rayon manufacturing, etc., can solve problems such as difficult to inhibit the crystallization of drugs, and achieve the effects of good conductivity, crystallization inhibition, and low cost

Inactive Publication Date: 2019-07-19
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, for highly crystalline drugs such as ibuprofen, simple blending electrospinning is difficult to inhibit the crystallization of drugs from the electrospinning matrix.

Method used

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  • Preparation method of ibuprofen transdermal sustained-release preparation
  • Preparation method of ibuprofen transdermal sustained-release preparation
  • Preparation method of ibuprofen transdermal sustained-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A preparation method of ibuprofen transdermal slow-release preparation, the steps are as follows:

[0040] (1) Polylactic acid (PLA, viscosity average molecular weight Mv is 10 0000) is dissolved in the mixed solvent of chloroform and N,N-dimethylformamide (DMF), and described chloroform and N,N- The volume ratio of dimethylformamide is 9:1, and the polylactic acid solution that makes concentration is 8% (w / v) is used as electrospinning sheath solution;

[0041] (2) Polyvinylpyrrolidone (PVP, weight-average molecular weight Mw is 1300000) is dissolved in the mixed solvent of dehydrated alcohol and DMF, and the volume ratio of described dehydrated alcohol and DMF is 1:1, makes concentration be 4 % (w / v) polyvinylpyrrolidone solution;

[0042] (3) Add the ibuprofen bulk drug to the polyvinylpyrrolidone solution of step (2), the addition of the ibuprofen bulk drug is 20% by mass of the polyvinylpyrrolidone, and stir magnetically at room temperature until dissolved to obta...

Embodiment 2

[0046] A preparation method of ibuprofen transdermal slow-release preparation, the steps are as follows:

[0047] (1) Polylactic acid (PLA, viscosity average molecular weight Mv is 10 0000) is dissolved in the mixed solvent of chloroform and N,N-dimethylformamide (DMF), and described chloroform and N,N- The volume ratio of dimethylformamide is 10:1, and the polylactic acid solution that makes concentration is 6% (w / v) is used as electrospinning sheath solution;

[0048] (2) Polyvinylpyrrolidone (PVP, weight-average molecular weight Mw is 1300000) is dissolved in the mixed solvent of dehydrated alcohol and DMF, and the volume ratio of described dehydrated alcohol and DMF is 2: 1, makes concentration be 6 % (w / v) polyvinylpyrrolidone solution;

[0049] (3) Add the ibuprofen bulk drug to the polyvinylpyrrolidone solution in step (2), the addition of the ibuprofen bulk drug is 15% by mass of the polyvinylpyrrolidone, and stir magnetically at room temperature until dissolved to ob...

Embodiment 3

[0053] A preparation method of ibuprofen transdermal slow-release preparation, the steps are as follows:

[0054] (1) Polylactic acid (PLA, viscosity average molecular weight Mv is 120000) is dissolved in the mixed solvent of chloroform and N,N-dimethylformamide (DMF), and described chloroform and N,N- The volume ratio of dimethylformamide is 8:1, and the polylactic acid solution that makes concentration is 8% (w / v) is used as electrospinning sheath solution;

[0055] (2) Polyvinylpyrrolidone (PVP, weight-average molecular weight Mw is 1000000) is dissolved in the mixed solvent of dehydrated alcohol and DMF, and the volume ratio of described dehydrated alcohol and DMF is 3: 1, and making concentration is 8 % (w / v) polyvinylpyrrolidone solution;

[0056] (3) Add the ibuprofen bulk drug to the polyvinylpyrrolidone solution in step (2), the addition of the ibuprofen bulk drug is 30% by mass of the polyvinylpyrrolidone, stir magnetically at room temperature until dissolved to obt...

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Abstract

The invention relates to a preparation method of an ibuprofen transdermal sustained-release preparation. According to the method, a biodegradable high-molecular material of polylactic acid is used asa shell layer material, a high-molecular material of polyvinylpyrrolidone is used as a core layer material, ibuprofen which is a medicament with strong crystallinity is loaded on the core layer of fiber by using a coaxial electrostatic spinning means, and the prepared ibuprofen transdermal sustained-release preparation has a core-shell structure. The invention utilizes the double-layer shielding function established by the special core-shell structure of the coaxial electrostatic spinning fiber to realize the inhibition of ibuprofen crystallization, and the coaxial electrostatic spinning fiberhas larger specific surface area, thereby improving the transdermal penetration effect and the drug treatment effect of the ibuprofen. The ibuprofen transdermal sustained-release preparation preparedby the method can flexibly adjust and control the drug loading ratio by adjusting the quality of the added drug, does not contain a penetration enhancer, can be directly applied to skin, has good usecomfort and drug sustained-release performance, and is beneficial to drug transdermal penetration and treatment.

Description

technical field [0001] The invention relates to a preparation method of an ibuprofen transdermal sustained-release preparation, belonging to the technical field of biomedical materials. Background technique [0002] Ibuprofen has anti-inflammatory, analgesic, and antipyretic pharmacological effects, and is mainly used clinically to treat rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and neuritis. However, traditional ibuprofen oral preparations show severe gastrointestinal side effects, accompanied by adverse reactions such as palpitations, nausea, and dizziness, and the oral ibuprofen preparations are limited due to lack of pertinence in the local area. play. The development of transdermal formulations of iprofen can effectively overcome the hepatic first-pass effect of oral administration, avoid damage to the gastrointestinal tract, and reduce drug toxicity and adverse reactions. Pediatric medicine has always been a blank in the medi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/34A61K47/32A61K31/192A61P29/00D01F8/14D01F8/10D01F1/10
CPCA61K9/7023A61K31/192A61K47/32A61K47/34A61P29/00D01F1/10D01F8/10D01F8/14
Inventor 张平平刘鲁娅孙月张梦莹路文娟王延风孙敬勇毛娉婷
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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