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Application of low-concentration vesicular phospholipid gel as slow release carrier for small-molecule peptide drug

A technology of small molecular peptides and low concentration, which is applied in the field of slow-release carriers, can solve the problem of low phospholipid content in slow-release effects, and achieve the effects of reducing toxic and side effects, improving encapsulation efficiency, and good slow-release effects

Active Publication Date: 2011-07-20
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

[0010] In summary, there is no vesicular phospholipid gel for small molecule peptide drugs with good sustained release effect and relatively low phospholipid content, which is easy to inject.

Method used

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  • Application of low-concentration vesicular phospholipid gel as slow release carrier for small-molecule peptide drug
  • Application of low-concentration vesicular phospholipid gel as slow release carrier for small-molecule peptide drug
  • Application of low-concentration vesicular phospholipid gel as slow release carrier for small-molecule peptide drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Take 150 mg of octreotide acetate, dissolve it in 6.5 ml of pure water to obtain a drug solution, add egg yolk lecithin E80 3.5 g, magnetically stir for 1 hour, and mix well to obtain vesicular phospholipid gel of octreotide acetate.

Embodiment 2

[0058] Take 100 mg of leuprolide acetate and dissolve it in 7 ml of acetate buffer (20 mM, pH 6.0) to obtain a drug solution, add egg yolk lecithin E803 g, stir for 1 h, mix well, and mix the mixture under high pressure at 70 MPa for 3 Once, the vesicular phospholipid gel of leuprolide acetate was obtained. Its particle size distribution is between 60nm and 800nm.

Embodiment 3

[0060] Take thymosin a1300mg, dissolve it in 6ml of pure water to obtain a drug solution, add egg yolk lecithin E804g, magnetically stir for 30min, mix well, and mix the mixture under high pressure at 70Mpa for 6 times to obtain the vesicular phospholipid gel of thymosin a1 agent.

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Abstract

The invention provides a low-concentration vesicular phospholipid gel formulation of a small-molecule peptide drug and also provides a preparation method of the vesicular phospholipid gel formulation of the small-molecule peptide drug. In the low-concentration vesicular gel formulation, the content of phospholipids ranges from 20% to 40%, and the small-molecule peptide drug with a molecular weight ranging from about 300 D to about 3300 D is encapsulated in the phospholipids. The low-concentration vesicular phospholipid gel formulation is available in various drug administration forms suitable for injection drug administration, external drug administration and the like, has good biocompatibility, high drug-carrying capacity and good stability, and particularly has a long-acting slow release effect.

Description

technical field [0001] The present invention relates to a slow-release carrier for the delivery of small-molecule peptide drugs, more specifically, the present invention relates to a vesicular phospholipid with sustained-release small-molecule peptide drugs that can be widely used in the industrial production of medicine A gel and a preparation method thereof belong to the technical field of medicine. Background technique [0002] Many promising new drugs now belong to peptide or protein drugs, which provide a new direction for the treatment of diseases. However, the wide application of this type of drugs still faces many challenges. Peptide drugs are easily degraded by deamidation, Maillard reaction, oxidation or hydrolysis and other reactions to lose their activity. Moreover, under extreme conditions such as low pH, this type of degradation reaction will be accelerated, thereby reducing the bioavailability of this type of drug. In addition, the relatively high molecular ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/24
Inventor 龚照墉刘振谧
Owner 成都师创生物医药科技有限公司
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