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Polypeptide drug sustained-release microsphere preparation and preparation method thereof

A slow-release microsphere preparation and drug technology, which is applied in the direction of drug combination, pharmaceutical formula, peptide/protein composition, etc., can solve the problems of rising production cost and low drug encapsulation rate, and achieve weight control and increase drug encapsulation rate , the effect of uniform particle size

Active Publication Date: 2012-09-26
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the membrane emulsification method can produce microspheres with relatively uniform particle size, most of the polypeptide drugs are easily soluble in water. It is also a key factor in the production process of microsphere formulations

Method used

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  • Polypeptide drug sustained-release microsphere preparation and preparation method thereof
  • Polypeptide drug sustained-release microsphere preparation and preparation method thereof
  • Polypeptide drug sustained-release microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] A preparation method for exenatide slow-release microspheres, comprising the following steps:

[0056] (1) 1.0 g of polylactic acid-glycolic acid copolymer (molecular weight 15000, glycolide:lactide=75:25, carboxyl terminal) was dissolved in 5 ml of anhydrous acetic acid to form polylactic acid-glycolic acid copolymer solution;

[0057] (2) Weigh 50 mg of exenatide and dissolve 30 mg of sucrose in 0.5 mL of sterile water;

[0058] (3) Mix the polylactic acid-glycolic acid copolymer solution in step (1) with the exenatide solution in step (2), and stir with a magnetic stirrer until a completely uniform, clear, transparent mixed solution is formed as the organic phase ;

[0059] (4) prepare 50ml of liquid paraffin containing 2wt% lecithin, as the oil phase;

[0060] (5) Homogeneously emulsifying the mixed solution of step (3) and the oil phase of step (4) for 5-15 minutes to form an O / O type emulsion;

[0061] (6) Stir and volatilize the emulsion of step (5) to remove ...

Embodiment 2

[0063] Except that PLGA is replaced by carboxyl-terminated PLGA with end-blocked PLGA, the specific steps are the same as in Example 1, and the particle size of exenatide sustained-release microspheres is in the range of 5 to 30 microns, the drug loading is 4.58%, and the encapsulation efficiency is 90.49%. %.

Embodiment 3

[0065] Except that PLGA was replaced by MPEG-PLGA with end-blocked PLGA, the specific steps were the same as in Example 1, and the obtained exenatide sustained-release microspheres had a particle size in the range of 5 to 30 microns, a drug loading of 4.22%, and an encapsulation efficiency of 88.45. %.

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Abstract

The invention discloses a polypeptide drug sustained-release microsphere preparation and a preparation method thereof. The method comprises the following steps of: dissolving the polylactic acid-glycollic acid copolymer or polylactic acid, a protective agent and a polypeptide drug in an organic solvent to form a completely uniform mixed solution; adding the mixed solution into an oil phase to form emulsion; removing the organic solvent; and performing centrifugal washing and freeze drying to obtain the polypeptide drug sustained-release microsphere. In the invention, an O / O method is adopted, the problem that the drug spreads toward the outer aqueous phase in the multiple-emulsion preparation method is solved, and the drug encapsulation efficiency is improved to 60-95%. The biological active polypeptide drug is degraded in the body and slowly released with the polymer material of the microsphere through the pores on the microsphere surface; the release time can be as long as several weeks and even several months; and the in-vitro release test indicates that the release conforms to similar zero-order release.

Description

technical field [0001] The invention belongs to the research field of biomedical polymer materials and bioactive drug controlled-release preparations. Specifically, the invention relates to a polypeptide drug sustained-release microsphere preparation and a preparation method thereof. Background technique [0002] Most protein and polypeptide drugs have very low oral bioavailability, so that they cannot produce a sufficiently high effective blood concentration after oral administration, and such drugs cannot be administered orally. Due to the presence of proteases in the body during subcutaneous injection, the half-life of the drug in the body is very short, requiring frequent injections, which increases the pain of the patient and reduces the patient's compliance. [0003] Biocompatible degradable materials (such as polymer materials) are used to wrap active pharmaceutical ingredients to make microsphere preparations, and the drug release is controlled through the gradual de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/42A61K47/44
CPCA61K38/17A61K38/26A61K38/00A61K9/16A61K47/34A61K9/1647A61P3/04A61P3/10
Inventor 刘锋曹付春
Owner AC PHARMA CO LTD
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