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A biodegradable microsphere composition suitable for the controlled release of glucose controlling peptide and formulation thereof

A technology of biodegradation and glucose, which is applied in the field of preparation of the microspheres, can solve the problems of uncontrolled release rate, incomplete release of encapsulated drugs, complex and low efficiency, etc., and achieves simplicity, economy, high stability, Effect of High Encapsulation Efficiency

Inactive Publication Date: 2010-02-24
DONG A PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dosage form containing polyester microspheres encapsulated with protein drugs has the following defects: initial burst release effect (initial burst release effect), uncontrolled release rate within a certain period of time due to various factors, or encapsulation Incomplete release of blocked drug
However, conventional methods are complex and inefficient, as evidenced by several examples: the large amount of organic solvents used and removed during phase separation, the degradation of peptides due to the high energy used in sonication, and the use of a variety of excipients , these excipients include stabilizers (such as sugars) and release enhancers (such as inorganic acids and salts)

Method used

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  • A biodegradable microsphere composition suitable for the controlled release of glucose controlling peptide and formulation thereof
  • A biodegradable microsphere composition suitable for the controlled release of glucose controlling peptide and formulation thereof
  • A biodegradable microsphere composition suitable for the controlled release of glucose controlling peptide and formulation thereof

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Experimental program
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Effect test

preparation example Construction

[0029] Preparation methods of biodegradable polymer microspheres include:

[0030] adding an organic solvent to the polymer to obtain a polymer solution (step 1);

[0031] Disperse the glucose-regulating peptide in the polymer solution described in step 1 to obtain a dispersion, and then add alcohol or a mixture of alcohol and organic acid to the dispersion to obtain a drug-dispersed solution. solution) (step 2); and

[0032] Microspheres are formed from the drug-dispersed solution described in step 2 (step 3).

[0033] A detailed description of the method will be given step by step.

[0034] First, step 1 is to prepare a polymer solution.

[0035] In step 1, the polymer is dissolved in an organic solvent. The polymer is biodegradable and can be used as a carrier, preferably a biodegradable polyester polymer. Any volatile organic solvent may be used without particular limitation as long as the biodegradable polymer carrier has high solubility therein and can be easily rem...

Embodiment 1

[0063] Embodiment 1: Carry out the preparation of microsphere according to polymer kind and mixing ratio (oil-in-water O / W type lotion)

[0064] 300 mg of polymer (Boehringer Ingelheim) were completely dissolved in dichloromethane. 9 mg of exendin-4 (American Peptide) was dispersed in the polymer solution to obtain an exendin-4 dispersion. The polymers used are shown in Table 1, which are one polymer product or a mixture of two different polymer products in various mixing ratios. A predetermined amount of methanol (the volume ratio of alcohol to drug dispersion is 1:4) was added to each of the drug dispersions having different polymer types and mixing ratios to obtain a drug-dispersed solution. 10 ml of each drug-dispersed solution was taken and emulsified by a stirrer or a homogenizer using 250 ml of a 1% (w / v) polyvinyl alcohol aqueous solution saturated with dichloromethane to form microspheres. The microspheres were solidified while stirring at room temperature and a...

Embodiment 2

[0067] Embodiment 2: Carry out the preparation of microsphere according to the ratio of alcohol and drug dispersion (oil-in-water O / W type lotion)

[0068] 300 mg of polymer (RG502H, Boehringer Ingelheim) were completely dissolved in dichloromethane. 9 mg of exendin-4 (American Peptide) was dispersed in the polymer solution to obtain an exendin-4 dispersion. To this drug dispersion was added a predetermined amount of methanol (the volume ratio of alcohol to drug dispersion was 1:1 to 1:7, as shown in Table 2) to obtain a drug-dispersed solution. This was emulsified and dried in the same manner as in Example 1 to obtain microspheres.

[0069] Table 2

[0070]

[0071] As shown in Table 2, when the volume ratio of drug dispersion to methanol is 7 or more, no solution can be formed.

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Abstract

Disclosed are biodegradable microspheres, capable of releasing a glucose-regulating peptide in a controlled manner, comprising a biodegradable polymer carrier with the glucose-regulating peptide encapsulated therein, and methods for the preparation thereof. In addition to ensuring high encapsulation efficiency and high stability of the encapsulated drug, the microspheres shows neither an initial burst effect nor incomplete release and allows the zero-order release of drugs over a prolonged period of time, thus improving the therapeutic effect of the drug.

Description

technical field [0001] The present invention relates to a biodegradable polymer microsphere comprising a biodegradable polymer carrier in which glucose-regulating peptide is encapsulated, said microsphere is capable of releasing glucose-regulating peptide in a controlled manner Peptides; the invention also relates to a process for the preparation of said microspheres. Background technique [0002] After oral administration, most protein drugs and peptide drugs lose their active structures in the acidic environment of the stomach or under the action of enzymatic degradation. In addition, their rate of absorption through the gastric or intestinal mucosa is very low. For these reasons, protein drugs or peptide drugs are usually administered in a non-oral route, that is, injection. Since most protein drugs or peptide drugs administered non-orally have a short half-life and low bioavailability in the body, the non-oral administration of protein drugs or peptide drugs must be re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52
CPCA61K9/1647A61K38/26A61P3/04A61P3/08A61P3/10Y02A50/30A61K9/48A61K38/17A61K47/32A61K9/16
Inventor 郭贤姬李建日朴容满孙美京梁熙昌金泰亨金胤池金炳文李圣熙姜寿亨刘武姬
Owner DONG A PHARMA
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