Temperature-sensitive hydrogel containing exendin-4 and injection thereof

A temperature-sensitive, hydrogel technology, used in medical preparations containing active ingredients, medical preparations without active ingredients, metabolic diseases, etc., can solve problems such as side effects and inconvenience, and achieve less irritation and application. Convenience and improved bioavailability

Active Publication Date: 2012-03-14
BEIJING GENETECH PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recombinant exendin-4, as a national first-class new drug, is mainly used clinically for the treatment of diabetes. Like all protein drugs, exendin-4 is rapidly eliminated in the circulatory system. In order to maintain a therapeutically effective blood concentration, it is often required to Dosage or frequent administration, this method is inconvenient and has potential side effects (Chung Y M et al. Biomacromolecules, 2002, 3(3):511-516.)

Method used

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  • Temperature-sensitive hydrogel containing exendin-4 and injection thereof
  • Temperature-sensitive hydrogel containing exendin-4 and injection thereof
  • Temperature-sensitive hydrogel containing exendin-4 and injection thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Weigh 0.88g Na 2 HPO 4 12H 2 O, 2.74 g NaH 2 PO 4 2H 2 O, 1.0g potassium benzoate, 30.0g glycine, dissolved in 800ml ultrapure water, adjusted to pH 6.0, fixed to 1000ml, filtered with 0.25mM microporous membrane, prepared into 200mM phosphate buffer, placed in 4 °C refrigerator.

[0064] In a polypropylene tube placed in an ice bath, the weighed 6g PLGA-PEG-PLGA (MW=6000) copolymer was slowly added to cooling (0-4°C) 20ml ultrapure water, and stirred under magnetic force ( 400-600rpm) until the polymer is completely dissolved, fully swelled and dispersed, prepared into a PLGA-PEG-PLGA copolymer with a concentration of 300mg / ml, and placed in a 4°C refrigerator for use.

Embodiment 2

[0066] Take 1.5ml of the 300mg / ml PLGA-PEG-PLGA prepared in Example 1, put it in a centrifuge tube, then add 300 μl of 10mg / ml exendin-4 aqueous solution, and add the 200mM phosphate of pH 6.0 prepared in Example 1 at the same time Buffer 300μl, make up 3ml with ice-bath ultrapure water, during the addition process, the centrifuge tube has been placed on the shaker, the oscillation frequency is 100-200rpm, so that it is mixed evenly, divided into 3 parallel tubes, placed in 4 °C refrigerator overnight. The final concentration of PLGA-PEG-PLGA copolymer was 150 mg / ml and the concentration of exendin-4 was 1.0 mg / ml.

Embodiment 3

[0068] Same operation as in Example 2, take 2ml of the 300mg / ml PLGA-PEG-PLGA prepared in Example 1, place it in a centrifuge tube, then add 300 μl of 10mg / ml exendin-4 aqueous solution, and add the pH6. 0 200mM phosphate buffer solution 300μl, fill up 3ml with ice-bath ultrapure water, during the addition process, the centrifuge tube has been placed on the shaker, the oscillation frequency is 100-200rpm, so that it is evenly mixed, and divided into parallel 3 Tubes were placed in a 4°C refrigerator overnight. The final concentration of PLGA-PEG-PLGA copolymer was 200 mg / ml and the concentration of exendin-4 was 1.0 mg / ml.

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Abstract

The invention relates to a temperature-sensitive hydrogel containing exendin-4, comprising exendin-4 as an effective ingredient and an amphiphilic copolymer as a medicine slow release carrier, wherein, the amphiphilic copolymer comprises polyester and polyethylene glycol, preferred PLGA-PEG-PLGA. The temperature-sensitive hydrogel is a liquid at room temperature, and is a solid water insoluble gel at the temperature of 37 DEG C, can be used for treating diabetes, and has good drug release property, environmental protection, little irritation, convenient application, and obvious effect. Compared with preparations with a large dose of exendin-4, the hydrogel disclosed herein has the advantages of in vivo formation of gel, easy operation, and continuous release property, and improves bioavailability, reduces administration times, and enhances patient compliance.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular, the invention relates to a temperature-sensitive hydrogel containing insulin secretory hormone (exendin-4) and an injection thereof. Background technique [0002] Diabetes is a disease that seriously threatens human health and life. There are more than 150 million diabetics in the world, of which 90% are type 2 diabetics. There are nearly 40 million type 2 diabetes patients in my country. With the improvement of living standards, the incidence rate is getting higher and higher, and a series of complications caused by diabetes seriously affect the quality of life of patients. [0003] Insulin secretagogue-1 (glucagon-like peptide-1, GLP-1) has the functions of lowering blood sugar, promoting insulin secretion, promoting the growth, proliferation and differentiation of pancreatic beta cells and inhibiting their apoptosis, etc. It was once used as an effective treatment2 Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K38/22A61P3/10
Inventor 韩为跃付四海王为张仁怀何凯阳勇杨立明叶学君闻亚磊
Owner BEIJING GENETECH PHARML
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