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In-situ phase change gel slow release system taking phospholipid as substrate and preparation method thereof

A technology of sustained-release preparations and phospholipids, which is applied in the field of in-situ injection phase-change gel sustained-release systems, which can solve problems such as drug concentration differences, small molecule drug leakage, and small injection volumes.

Active Publication Date: 2012-07-04
成都师创生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at the same time, there are many problems: on the one hand, protein and polypeptide drugs have large molecular weight, poor stability, and are easily degraded by proteolytic enzymes in the gastrointestinal tract. Injection administration; on the other hand, these drugs have a short biological half-life and are quickly degraded by the body, requiring continuous injection or intravenous infusion to ensure the efficacy of the drug, which increases the physical, psychological and economic burden on patients
[0010] Although multivesicular liposomes have a variety of administration routes and have good sustained release and depot effects, they also have many shortcomings: first, to prepare MVL, at least they must contain amphiphilic lipids (such as phospholipids) and neutral lipids. Substances (such as triglycerides)
Secondly, due to the difference in drug concentration in the inner and outer water phases of MVL, the leakage of small molecule drugs still exists, and the phospholipid bilayer will also be partially ruptured during storage, and the problem of sedimentation and aggregation during storage has not been resolved. , may affect the stability of the formulation
Third, the currently developed MVL product is a suspension, which is not convenient for storage and transportation
Fourth, the preparation process of MVL is complicated, and the production conditions are very strict, so it is not easy to expand production
[0015] More critically, the application did not carry out in vivo experiments, and there is no data to prove that it can achieve the expected sustained release effect. Those skilled in the art know from its composition of lower phospholipid concentration, less injection volume, combined with the prior art Tried it, it is safe to assume that its sustained release effect is poor

Method used

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  • In-situ phase change gel slow release system taking phospholipid as substrate and preparation method thereof
  • In-situ phase change gel slow release system taking phospholipid as substrate and preparation method thereof
  • In-situ phase change gel slow release system taking phospholipid as substrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Take 50 mg of octreotide acetate, dissolve it in 1.5 g of 85% (v / v) ethanol-pH4.0 lactic acid buffer solution to obtain a drug solution, filter it through a 0.22 μm microporous membrane, add 7.0 g of egg yolk lecithin E80, and then add After filtering 1.5g of soybean oil through a 0.22μm microporous membrane, stir it magnetically for about 0.5h in a sterile environment until the E80 is completely dissolved to obtain a milky yellow opaque liquid containing a large number of air bubbles. Let it stand until the air bubbles completely disappear. Seal and serve.

[0075]

Embodiment 2

[0077] Take 20 mg of thymopentin, dissolve it in 2.0 g of absolute ethanol to obtain a drug solution, filter it through a 0.22 μm microporous membrane, add 6.0 g of egg yolk lecithin E80, and then add medium-chain fatty acid glycerides filtered through a 0.22 μm microporous membrane 2.0g, magnetically stirred for about 0.5h, until E80 was completely dissolved, and a milky yellow opaque liquid containing a large number of bubbles was obtained, which was left to stand until the bubbles completely disappeared, then packaged and sealed to obtain a high-concentration thymopentin sustained-release preparation of phospholipids.

[0078]

Embodiment 3

[0080] Take 100 mg of insulin, dissolve it in 2.0 g of 90% (v / v) ethanol-physiological saline solution to obtain a drug solution, filter it through a 0.22 μm microporous membrane, add 5.5 g of soybean lecithin, and then add 0.22 μm microporous membrane to filter 2.5g of soybean oil, stirred by magnetic force for about 0.5h, until the soybean lecithin was completely dissolved to obtain a milky yellow opaque liquid containing a large number of air bubbles, left to stand until the air bubbles completely disappeared, subpackaged and sealed to obtain a high-concentration insulin phospholipid sustained-release preparation.

[0081]

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Abstract

The invention provides an in-situ phase change gel slow release system taking a phospholipid as a substrate, and provides a preparation method thereof. A high-concentration phospholipid slow release preparation is prepared from a high-concentration (50-85 percent) phospholipid, a bioactive ingredient, ethanol solutions of different concentrations and / or injection oil with a simple method, and has the characteristics of high biocompatibility, small untoward effect, remarkable slow release effect and suitability for various administration forms such as hypodermic injection, intramuscular injection, external administration and the like; the amount of a coated medicament can be conveniently adjusted according to the clinical dosage of a medicament; and the in-situ phase change gel slow release system has a wide application prospect.

Description

technical field [0001] The invention relates to an in-situ injection phase-change gel sustained-release system, in particular to a high-concentration phospholipid sustained-release preparation prepared by using phospholipids, ethanol solutions of different concentrations and / or oil for injection, and belongs to the technical field of medicine. [0002] Background technique [0003] With the rise and development of biotechnology, more and more protein and polypeptide drugs have been developed and used for the diagnosis and treatment of diseases. Compared with small molecule chemical drugs, protein peptide drugs are closer to normal physiological substances in the body, and have the advantages of high pharmacological activity, low toxic and side effects, small dosage, definite curative effect, and strong specificity. But at the same time, there are many problems: on the one hand, protein and polypeptide drugs have large molecular weight, poor stability, and are easily degrade...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/44A61K47/24A61K47/10A61K47/14A61K9/06
Inventor 龚涛张志荣孙逊
Owner 成都师创生物医药科技有限公司
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