Method for preparing sustained-release miniball

A technology of slow-release microspheres and active ingredients, applied in the direction of powder transportation, etc., can solve the problems of large burst release, insufficient release volume, unsatisfactory slow-release results, etc.

Active Publication Date: 2006-02-15
SHANGHAI HUAYI BIO LAB CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The result is either low encapsulation efficiency, or unsatisfactory sustained release ...

Method used

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  • Method for preparing sustained-release miniball
  • Method for preparing sustained-release miniball
  • Method for preparing sustained-release miniball

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1: Typical protein, polypeptide powder and protein powder particle size comparison obtained by anti-solvent method

[0055] 1) Take a 1ml eppendorf centrifuge tube, add 1ml of alcohol, then add 5mg of porcine insulin freeze-dried powder (purchased from Jiangsu Wanbang Biochemical Co., Ltd.), mix by ultrasonic for 15s, then take 1 drop of the suspension and drop it on a glass slide, place it under a microscope observe. picture

[0056] 2(a) is the observed image.

[0057]2) The above lyophilized porcine insulin powder was dissolved in DMSO at a concentration of 50 mg / ml. Take 100 μl of the solution and add it to 900 μl of ethanol, vortex quickly to mix, then take 1 drop of the suspension and drop it on a glass slide, and place it under a microscope for observation. figure 2 (b) is the observed image.

[0058] From figure 2 It can be seen from the results that the average particle size of insulin freeze-dried powder is about 20-30 μm, and the anti-solvent m...

Embodiment 2

[0060] Comparison of preparation of microspheres by traditional W1 / O / W2 double emulsification method, traditional S / O / W double emulsification method and improved S / O / W method

[0061] The polymer used in this example is polylactide-co-glycolide (polylactide-co-glycolide), wherein polylactide / glycolide (lactide / glycolide) = 50 / 50, namely PLGA (50:50) , with an intrinsic viscosity (ie IV) of 0.39, purchased from Birmingham Polymers, USA.

[0062] 1) W1 / O / W2 method: prepare 25mg / ml and 50mg / ml porcine insulin aqueous solutions, respectively take a certain volume of solution and add 2ml of dichloromethane (DCM) dissolved with 100mgPLGA (50:50), use high-speed homogenizer Homogenize for 1.5 minutes with a machine (F6 / 10 model, Fluko, Germany) at 10,000-15,000 rpm. Then, the W1 / O primary emulsion was added into 200 ml of 1.0% (W / V) polyvinyl alcohol (PVA, sigma, USA) solution, and stirred by a magnetic stirrer for 3 hours (1000 rpm). Afterwards, the microspheres were collected by ...

Embodiment 3

[0076] Embodiment 3: Encapsulate GLP-1(7-36)OH with improved S / O / W method

[0077] According to the method shown in Experiment 3) in Example 2, PLGA with different internal viscosities (molecular weights) were selected to prepare microspheres encapsulated with GLP-1(7-36)OH. The results are shown in Table 3.

[0078] Numbering

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Abstract

The invention provides a method for preparing sustained-release miniball, which comprises dissolving polypeptides or micromolecular proteins into DMSO, charging the solution into DCM containing PLGA, forming fine particles of the medicament by utilizing anti-solvent, charging the formed suspension into outer aqueous phase, finally volatilizing the organic solvent to obtain slow release microballoons.

Description

technical field [0001] The invention relates to a method for encapsulating protein and polypeptide drugs into polymers to obtain microspheres capable of sustaining release of drugs. Background technique [0002] Sustained-release microspheres are an important sustained-release drug delivery system (Drug Delivery System, DDS). By encapsulating the active ingredient in the polymer, the active ingredient can be released from the microspheres stably for a long time, so as to achieve the purpose of slow release and controlled release. [0003] There are various methods for preparing microspheres, such as solvent evaporation, coacervation, spray drying, and spray freeze drying (Protein delivery from biodegradable microspheres, by J.L.Clelandin Protein Delivery, edited by L . Sanders and W. Hendren, Plenum Press, N.Y. 1997). Among them, the solvent evaporation method in the water phase is the most used method, which can be subdivided into single emulsification method (Oil / Water, ...

Claims

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Application Information

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IPC IPC(8): A61K9/14
Inventor 周加祥包文超伍登熙
Owner SHANGHAI HUAYI BIO LAB CO LTD
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