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GnRH analogue slow release composition and preparation method thereof

A sustained-release composition and analog technology, applied in the field of medicine, can solve problems such as complex implant technology, achieve the effects of overcoming the need for long-term frequent injections, high production yield, and strong practicability

Active Publication Date: 2019-01-04
艾伟伦
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As above, it is more complicated in the process of preparing the implant

Method used

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  • GnRH analogue slow release composition and preparation method thereof
  • GnRH analogue slow release composition and preparation method thereof
  • GnRH analogue slow release composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: the synthesis of triptorelin-succinyl-chitosan (TPR-S-CS):

[0051] Dissolve 0.5g triptorelin and 0.12g succinic anhydride in 6mL CH 2 Cl 2 After stirring and reacting at room temperature for 24 h, add 9 mL of anhydrous N,N-dimethylformamide (DMF), and then add 0.1 mL of N,N-diisopropylethylamine (DIPEA), and react at room temperature for 4 h. After adding 88mL of DMF, add 0.66g of chitosan while stirring, continue to react at room temperature for 12h, ultrafilter and freeze-dry to obtain white solid TPR-S-CS.

Embodiment 2

[0052] Embodiment 2: the synthesis of triptorelin-glutaryl-chitosan (TPR-G-CS):

[0053] Dissolve 0.5g triptorelin and 0.2g glutaric anhydride in 6mL CH 2 Cl 2 After stirring for 12 hours at room temperature, add 9 mL of DMF, then 0.1 mL of DIPEA, and react for 4 hours at room temperature. After adding 88 mL of DMF, add 0.66 g of chitosan while stirring, continue to react at room temperature for 12 hours, ultrafilter, freeze Dry to obtain white solid TPR-G-CS.

Embodiment 3

[0054] Embodiment 3: Synthesis of BM106-succinoyl-chitosan (BM106-S-CS):

[0055] Dissolve 0.52g BM106 and 0.12g succinic anhydride in 6mL CH 2 Cl 2 After stirring for 12 hours at room temperature, add 9 mL of DMF, then 0.1 mL of DIPEA, and react for 4 hours at room temperature. After adding 88 mL of DMF, add 0.66 g of chitosan while stirring, continue to react at room temperature for 12 hours, and purify by ultrafiltration. Freeze-dried to obtain a white solid BM106-S-CS.

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Abstract

The invention discloses a GnRH analogue slow release composition and a preparation method thereof and belongs to the technical field of medicines. The GnRH analogue slow release composition is composed of a GnRH analogue and chitosan molecues connected to the GnRH analogue through covalent bonds. The GnRH analogue slow release composition is simple in synthetic process, and can be produced on a large scale by adopting conventional synthetic conditions. As an oral long-acting slow release preparation, the GnRH analogue slow release composition not only can solve the problem that the GnRH analogue which is easy to degrade in gastrointestinal tract cannot be orally taken, but also prolongs the action time of the GnRH analogue in vivo, so that the problem that GnRH analogue must be frequentlyinjected and administrated for a long time is solved, and the GnRH analogue slow release composition is of very high practicality.

Description

technical field [0001] The invention relates to GnRH analogues, belonging to the technical field of medicine, in particular to a GnRH analogue slow-release composition and a preparation method thereof. Background technique [0002] Gonadotropin-releasing hormone (GnRH) is a polypeptide hormone secreted by the hypothalamus. The natural GnRH molecule consists of 10 amino acids, and its molecular structure is Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro- Gly-NH 2 . A large number of studies have confirmed that GnRH regulates the endocrine system and reproductive system in the body by stimulating the secretion of luteinizing hormone and follicle generating hormone. Moreover, GnRH also participates in the occurrence and development of various benign and malignant tumors through auto / paracrine regulation. Therefore, for decades, many artificially synthesized GnRH analogues have been used to: (1) inhibit the secretion of sex hormones and treat hormone-dependent diseases, such as prostate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K47/61A61P15/00A61P35/00
CPCA61K38/09A61K47/61A61P15/00A61P35/00
Inventor 艾伟伦艾时斌冯运斌
Owner 艾伟伦
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