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Small molecule drug in-situ phase-change gel sustained release system and preparation method thereof

A technology of in-situ gel and drug activity, applied in the field of medicine, can solve the problems of accelerated drug release rate, short sustained release time, and more burst release, etc., and achieve the effect of good sustained release effect.

Active Publication Date: 2017-08-18
SICHUAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fat-soluble drugs have good compatibility with phospholipids, and are easy to penetrate, diffuse and release in phospholipid carriers, resulting in a significantly faster release rate, a relatively short sustained release time, and more burst releases. For some drugs with a narrow therapeutic window, may raise security concerns
[0006] Therefore, for small molecule drugs, it is necessary to find a drug carrier with a wide application range, small burst release, and long sustained release time to solve the problem of long-acting sustained release for injection.

Method used

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  • Small molecule drug in-situ phase-change gel sustained release system and preparation method thereof
  • Small molecule drug in-situ phase-change gel sustained release system and preparation method thereof
  • Small molecule drug in-situ phase-change gel sustained release system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Take 50 mg of 2,4-dinitrophenol, dissolve it in 2.0 g of 85% (v / v) ethanol-pH 7.6 phosphate buffer, filter through a 0.22 μm microporous membrane to obtain a drug solution, and then in sterile conditions Next, add 4.5 g of injection-grade soybean lecithin S100 and 3.5 g of Span 80, and stir magnetically for about 1 h under aseptic conditions until the S100 is completely dissolved to obtain a liquid containing a large number of bubbles, which is left to stand until the bubbles completely disappear, then packaged. Seal and serve.

Embodiment 2

[0064] Take 200 mg of dabigatran etexilate, dissolve it in 1.0 g of absolute ethanol to obtain a drug solution, filter it through a 0.22 μm microporous membrane, and then add 5.0 g of injection-grade egg yolk lecithin E80 under sterile conditions. Disc 80 4.0 g, magnetically stirred for about 1 h under aseptic conditions, until S100 was completely dissolved to obtain a liquid containing a large number of bubbles, left to stand until the bubbles completely disappeared, subpackaged, sealed, and ready to serve.

Embodiment 3

[0066] Under aseptic conditions, an appropriate amount of ebiprazole is ground and pulverized in a mortar to obtain ebiprazole powder. Take 1.5 g of absolute ethanol, 4.0 g of Span 80 and 4.5 g of injection-grade soybean lecithin S100, and magnetically stir for about 1 h under sterile conditions until S100 is completely dissolved, and a milky yellow liquid containing a large number of bubbles is obtained. Under aseptic conditions, take 200 mg of ebiprazole powder and mix it with the above-mentioned liquid evenly, let it stand until the air bubbles completely disappear, divide it into packages, seal it, and get ready.

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Abstract

The invention provides a small molecule drug in-situ phase-change gel sustained release agent with phospholipid and span as matrices and a preparation method thereof. By the adoption of the simple method, the phospholipid and span sustained release agent is prepared from phospholipid, span, active pharmaceutical ingredients and ethanol solutions of different concentrations, and has the advantages that the biocompatibility is good, the adverse reaction is low, the burst-release and inhibition capability is high, and the releasing time is prolonged; the sustained release agent is suitable for various drug administration modes such as subcutaneous injection and external drug administration, the amount of carried drugs can be adjusted conveniently according to the clinical medication dosage of the drugs, and the sustained release agent and the preparation method thereof have broad application prospects.

Description

technical field [0001] The invention relates to an in-situ phase-change gel slow-release system suitable for small-molecular drugs, which uses phospholipids and spans as substrates and ethanol as a solvent, and belongs to the technical field of medicine. Background technique [0002] Small molecule drugs play an important and irreplaceable role in human health. They have the advantages of small molecular weight, clear physical and chemical properties, simple structure, good stability, low price, and no antigenicity. However, there are also some problems. There are obvious peaks and troughs in the blood concentration of small molecule drugs after administration, making them more toxic and side effects and reducing drug efficacy; for chronic diseases, long-term continuous administration is required, which increases the physical, psychological and economic burden of patients. Therefore, the drug can be released slowly through the sustained-release preparation to obtain a stable...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/26A61K47/24A61K47/10A61K45/00A61K31/06
CPCA61K9/0002A61K9/0019A61K9/0024A61K9/06A61K9/08A61K31/06A61K31/496A61K31/519A61K45/00A61K47/10A61K47/22A61K47/24A61K47/26A61K9/0014A61K31/155A61K31/17A61K31/175A61K31/192A61K31/401A61K31/4164A61K31/4422A61K31/4439A61K31/445A61K31/4545A61K31/4748A61K31/515A61K31/522A61K31/5415A61K31/549A61K31/55A61K31/5513A61K31/573A61K31/616A61K31/635A61K31/704
Inventor 龚涛宋旭张志荣尉广飞胡梅陈体佳孙逊符垚
Owner SICHUAN UNIV
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