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Oral slow release preparation, entrapment material and preparation method

A technology for encapsulating materials and slow-release drugs, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. It can solve problems such as short duration of action, improve compliance, prolong Action time, high biocompatibility effect

Inactive Publication Date: 2012-09-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The object of the present invention is to provide a protein polypeptide oral sustained-release preparation, and a packaging material used for encapsulating protein polypeptide drugs, so as to solve the problem of short duration of action of protein polypeptide oral preparations in the prior art; the present invention Another object is to provide the preparation method of this oral sustained-release preparation

Method used

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  • Oral slow release preparation, entrapment material and preparation method
  • Oral slow release preparation, entrapment material and preparation method
  • Oral slow release preparation, entrapment material and preparation method

Examples

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Effect test

Embodiment 1

[0042] Weigh 5mg of exenatide, sodium alginate:sodium hyaluronate=2:3, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three distilled water, the concentration is 25mg / ml, stir and dissolve To obtain the water phase, add 2% Span-80 to 20ml of liquid paraffin to obtain the oil phase, add the water phase to the oil phase drop by drop, and magnetically stir at 500rpm / min to disperse the water phase evenly in the oil phase; add to the oil phase 2ml of 25% glutaraldehyde solution and 10ml of 1M dilute hydrochloric acid were reacted at 20°C; after the reaction was completed, 20ml of ethanol was added and stirred at room temperature for 15 minutes. The preparation is complete after freeze-drying. Weigh 100 mg of drug-loaded exenatide microspheres and 100 mg of blank microspheres prepared under the same conditions, and place each in a 20ml system to measure the encapsulation efficiency, and place them in a hydrochloric acid solution with pH 1.2 for the fir...

Embodiment 2

[0044] Weigh 10mg of exenatide, sodium alginate: sodium hyaluronate=1:1, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three distilled water, the concentration is 20mg / ml, stir and dissolve To obtain the water phase, add 1% Span-80 to 50ml of liquid paraffin to obtain the oil phase, add the water phase to the oil phase drop by drop, and stir the water phase at 700rpm / min to uniformly disperse the water phase in the oil phase; add 20ml 25% glutaraldehyde solution and 10ml 1M dilute hydrochloric acid, react at 50°C; after the reaction, add 20ml absolute ethanol, stir at room temperature for 15 minutes, discard the upper layer after standing for separation, and wash the lower layer with ethanol after suction filtration times, the preparation is complete after freeze-drying. The encapsulation rate of exenatide microspheres determined by BCA method was 78%, and the particle size was <200 μm.

Embodiment 3

[0046] Weigh exenatide 10mg, sodium alginate: sodium hyaluronate=1:3, dissolve the mixture of exenatide, sodium alginate and sodium hyaluronate in three distilled water, the concentration is 40mg / ml, stir and dissolve To obtain the water phase, add 1% Span-80 to 20ml of liquid paraffin to obtain the oil phase, add the water phase to the oil phase drop by drop, and magnetically stir at 500rpm / min to disperse the water phase evenly in the oil phase; add to the oil phase 5ml 25% glutaraldehyde solution and 5ml 1M dilute hydrochloric acid, react at 25°C, add 20ml ethanol after the reaction, stir at room temperature for 15 minutes, discard the upper layer after static separation, wash the lower layer with ethanol several times after suction filtration, freeze After drying, the preparation is complete. The encapsulation rate of exenatide microspheres determined by BCA method was 86%, and the particle size was <220 μm.

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Abstract

The invention discloses an oral slow release preparation, an entrapment material and a preparation method. A sodium alginate-sodium hyaluronate mixture is taken as an entrapment material; and a prepared protein polypeptide medicament oral slow release preparation consists of the following components in percentage by mass: 0.5-10 percent of medicament and 90-99.5 percent of sodium alginate-sodium hyaluronate mixture. According to the oral slow release preparation, the conventional administration way of a protein polypeptide medicament is changed, the acting time of the protein polypeptide medicament is prolonged, the normal blood sugar level is maintained successfully for 12 hours when exenatide oral microspheres are taken as an example, the administration compliance of a diabetes patient is improved remarkably, and the treatment effect is enhanced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to the preparation of oral sustained-release preparations, in particular to oral sustained-release preparations of protein and polypeptide drugs with a sodium alginate-sodium hyaluronate combination as a carrier and its preparation and application. Background technique [0002] With the development of biotechnology and genetic engineering, the use of protein and polypeptide drugs in clinical treatment is on the rise, but complex preparation processes, low delivery efficiency, and poor bioavailability have become bottlenecks in the clinical application of protein and polypeptide drugs. Among them, the route of administration of protein and polypeptide drugs is particularly important. Compared with injection preparations, oral preparations have better patient compliance and are more convenient to take, but the research on oral preparations of protein and polypeptide drugs is mo...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K38/00A61K38/22A61P3/10
Inventor 陈依军范宇刘楠
Owner CHINA PHARM UNIV
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