Glicetin -1 slow release microspheric preparation and its use

A technology of slow-release microsphere preparations and glucagon, which is applied in the field of medicine and can solve the problems of restricting the development and utilization of drugs and short half-life

Inactive Publication Date: 2004-09-01
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life of GLP-1 in vivo (less than 2 minutes) (DeaconCF, Knudsen LB, MadsenK, et al. Dipeptidyl peptidase IV resistant analogues of glucagons-likepeptide-1 which have extended metabolic stability and improved biological activity. Diabetologia 1998 41:271-278), which restricts its development and utilization as a drug, so it has not been used in clinical practice so far

Method used

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  • Glicetin -1 slow release microspheric preparation and its use
  • Glicetin -1 slow release microspheric preparation and its use
  • Glicetin -1 slow release microspheric preparation and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033]Embodiment 1: GLP-1 sustained-release microsphere preparation prepared by w / o / w solvent volatilization method

[0034] Dissolve 100 mg of PLGA (RG502H, PLA:PGA=50:50, Mw=34000) in 1.0 ml of dichloromethane to make an oil phase; dissolve 3 mg of GLP-1 (SIGMA company, the same below) in 0.1 ml of double distilled water (Containing 3% trehalose, 5% mannitol) to form the inner water phase, add it to the above oil phase, ultrasonic emulsification, form w / o colostrum, 30ml of 3% PVA solution (containing NaCl 2% and F- 68 0.5%) in a stirring container, quickly add the colostrum into the external water phase under stirring at 1000rpm to fully homogenize, after three minutes, lower the rotation speed to 400rpm and add 30ml of distilled water to the external water phase, stir at room temperature for 4 hours, After hardening, the microspheres were centrifuged, washed, and freeze-dried. Subpackaged and sealed, then irradiated and sterilized. The encapsulation efficiency of GLP-1 m...

Embodiment 2

[0035] Embodiment 2: s / o / o solvent volatilization method prepares GLP-1 sustained-release microsphere preparation

[0036] Disperse 24 mg of PEG (PEG6000), 3 mg of GLP-1 and 5 mg of protective agent zinc carbonate in 1 ml of double-distilled water, vortex and mix for about 3 minutes, freeze-dry, wash with dichloromethane, and centrifuge to remove PEG to obtain GLP-1 Micronized. PLGA (RG502H, PLA:PGA=50:50, M w =34000) 200 mg was dissolved in 1.0 ml of acetonitrile to make an oil phase, the above micropowder was added into the oil phase, ultrasonically dispersed, it was added dropwise into cottonseed oil to fully homogenize, stirred at 600 rpm for 1 hour, and then an appropriate amount of petroleum ether was added to Continue to stir at 400rpm for 2 hours to obtain GLP-1 microspheres, centrifuge, wash with petroleum ether, collect, freeze-dry, subpackage and seal, and then irradiate and sterilize. The encapsulation efficiency of the GLP-1 microspheres is 90%, and the particle...

Embodiment 3

[0037] Embodiment 3: Preparation of GLP-1 sustained release microsphere preparation by spray drying method

[0038] Dissolve 8 mg of GLP-1 and 30 mg of protective agent human serum albumin in 10 ml of double distilled water, spray into liquid nitrogen, and volatilize the liquid nitrogen at low temperature to obtain GLP-1 micropowder. PLGA (RG502H, PLA:PGA=50:50, M w =34000) 600 mg was dissolved in 10 ml of dichloromethane to make an oil phase, the micropowder was added into the oil phase for ultrasonic dispersion, and spray-dried, the inlet temperature was 40°C, the outlet temperature was 30°C, the spray pressure was 5Pa, the nozzle diameter was 0.5mm, and the flow rate was 1 ~2ml / min. The collected microspheres were vacuum-dried at room temperature for 6 hours, subpackaged and sealed, and then sterilized by irradiation. The encapsulation efficiency of GLP-1 microspheres is 80%, and the particle size is less than 60 μm.

[0039] Animal experiment: choose 16 adult wister rat...

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Abstract

The invention relates to a slow release microballoon agent of hyperglycemic factor sample peptide and the use as antihypelipidemic medicine or body weight control, wherein GLP-1 is a kind of inner source polypeptide excreted from the secretory cell of the small intestine and large intestine and nerve cells of the brain, having the effects of stimulating insuline secretion and inhibition pancreatic glucagons secretion .

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a sustained-release microsphere preparation of glucagon-like peptide-1 (GLP-1) and an application thereof. Background technique [0002] Glucagon-like peptide-1 (GLP-1) is a polypeptide secreted by the secretory cells of the small intestine and large intestine and the nerve cells of the brain. It consists of 37 amino acids, and its amino acid sequence is: His- Asp-Glu-Phe-Glu-Arg-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys- Glu-Phe-Lle-Ala-Trp-Leu-Val-Lys-Gly-Arg-Gly. (Lopez LC, Frazier ML, Su C-J, et al. Mammalian pancreatic proglucangon contains three glucanguon-related peptides. Proc Nalt Acad Sci USA 1983, 80:5485-5489). GLP-1 can stimulate the secretion of insulin, and can inhibit the secretion of glucagon, reduce fasting or postprandial blood sugar, its role has been confirmed in clinical studies of healthy humans ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/52A61K38/17A61P3/10
Inventor 钟延强蔡在龙尹东锋鲁莹吴诚杨生生毛积芳焦炳华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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