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Organism degradable star-type structure poly (glycolide-lactide) medicine carrier microsphere and preparation method thereof

A technology of polyglycolide and drug-carrying microspheres, which is applied in the directions of pharmaceutical formulations and medical preparations with inactive ingredients, can solve the problems of complicated experimental process, etc., so as to improve the poor packaging ability, improve the drug-carrying capacity and the packaging capacity. Buried rate effect

Inactive Publication Date: 2007-03-14
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But their shortcomings are that the experimental process is relatively complicated due to the large changes in the structure of the wrapping material or the experimental system.

Method used

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  • Organism degradable star-type structure poly (glycolide-lactide) medicine carrier microsphere and preparation method thereof
  • Organism degradable star-type structure poly (glycolide-lactide) medicine carrier microsphere and preparation method thereof
  • Organism degradable star-type structure poly (glycolide-lactide) medicine carrier microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: 0.3mol lactide, 0.1mol glycolide, 2×10 -3 mol pentaerythritol and 4×10 -5 mol of stannous isooctanoate was mixed and put into a sealed tube, melted and sealed the nozzle under vacuum condition (30Pa), and reacted at 160°C for 8h. The obtained product was dissolved in dichloromethane and then filtered, anhydrous methanol was added dropwise to precipitate, and the precipitate was vacuum-dried to obtain four-armed star polylactide. Its number average molecular weight was 9000. Its structure consists of 13 C NMR (VARIAN UNITY-plus400) nuclear magnetic spectrum confirmed, Figure 1. In the spectrogram, the peak f (δ=62.25ppm) of the quaternary carbon atom and the peak g (δ=15.71ppm) of the methylene carbon atom in the pentaerythritol molecule can be found respectively, thus proving the star structure of the polymer.

Embodiment 2

[0024] Example 2: 70 mg of bovine serum albumin (molecular weight: 67,000) was dissolved in 0.3 mL of an aqueous solution of 0.05% (w / v) polyvinyl alcohol (17-88, Beijing Organic Chemical Factory) to form an internal water phase. Dissolve 0.6 g of four-armed star polylactide in 12 mL of dichloromethane to form a medium oil phase. Under the condition of heating at 60°C, mix the inner water phase and the middle oil phase, and mix evenly under ultrasonic (Sonics & Materials VCX, 400W, 30s) to form W / O colostrum. 250 mL of 0.2% (w / v) polyvinyl alcohol aqueous solution was used as the external aqueous phase. Inject W / O colostrum into the external water phase under high-speed stirring, emulsify to form a W / O / W emulsion, stir until all the dichloromethane volatilizes, and solidify into balls; centrifuge and collect the obtained microspheres, and After freeze-drying, the drug-loaded microspheres of biodegradable star polylactide can be obtained. The drug loading amount is 37.85μg / mg...

Embodiment 3

[0025] Example 3: The operation steps of this example are the same as those of Example 2, except that the amount of star polylactide used is 0.8 g, and the drug loading of the obtained drug-loaded microspheres is 31.18 μg / mg microspheres, the embedding rate was 33.41%.

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Abstract

The present invention relates to one kind of biodegradable medicine-carrying polyglycolide-lactide microsphere in star structure and its preparation process. The biodegradable medicine-carrying polyglycolide-lactide microsphere has coating material of star polyglycolide-lactide, coated protein polypeptide medicine of bovine serum albumin or leuteinizing hormone-releasing homone (LH-RH) analog, medicine carrying amount of 17.56-67.51 mcg / mg microsphere and embedding rate of 28.68-78.39 wt%. It is prepared through a W / O / W composite emulsifying process to coat protein polypeptide medicine into star polyglycolide-lactide to form microsphere. Compared with linear medicine-carrying polyglycolide-lactide microsphere, the present invention has obviously increased medicine carrying amount and embedding rate and obvious long-acting and slowly releasing effect.

Description

technical field [0001] The invention relates to a protein polypeptide drug-loaded microsphere and a preparation method thereof, in particular to a star-shaped biodegradable polylactide drug-loaded microsphere and a preparation method thereof. Background technique [0002] With the development of biomedicine and biotechnology, protein peptide drugs are becoming a very important class of therapeutic agents. They have broad application prospects in the treatment of cancer, autoimmune diseases, memory loss, mental disorders, hypertension and certain cardiovascular and metabolic diseases, and have become important diagnostic, monitoring, preventive and therapeutic drugs. This type of drug is characterized by small dosage and strong biological activity. However, this type of drug is very sensitive to strong acid and proteolytic enzymes in the gastrointestinal tract after oral administration, and peptide and protein drugs are mostly hydrophilic macromolecular substances, which are ...

Claims

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Application Information

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IPC IPC(8): C08G63/08A61K47/34
Inventor 张政朴刘倩刘苗苗吴学丹
Owner NANKAI UNIV
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