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Intestinal absorption promoting liraglutide salt for preparing oral enteric-coated preparations

A technology of liraglutide salt and liraglutide, which is applied in the field of liraglutide salt to achieve the effects of improving blood drug concentration, insignificant hypoglycemic rate, and suitable for large-scale industrial production

Inactive Publication Date: 2015-10-28
哈尔滨吉象隆生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Whether liraglutide can be used orally, whether liraglutide can improve oral bioavailability after salt formation, and whether it can be prepared into enteric-coated preparations for oral administration, there is no report in the prior art. Therefore, the present invention uses liraglutide Combined with an intestinal absorption enhancer to form a salt, using liraglutide salt as the active ingredient of the drug, a liraglutide enteric-coated preparation was prepared, which achieved unexpected results

Method used

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  • Intestinal absorption promoting liraglutide salt for preparing oral enteric-coated preparations
  • Intestinal absorption promoting liraglutide salt for preparing oral enteric-coated preparations
  • Intestinal absorption promoting liraglutide salt for preparing oral enteric-coated preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1, Preparation of Liraglutide Sodium Caprate, Liraglutide Sodium Laurate, and Liraglutide Sodium Caprylate

[0054] According to the patent method that our company has applied for (public application number: CN 103864918 A), the crude product of liraglutide was synthesized, and the crude product was purified by preparative liquid chromatography, concentrated by rotary evaporation to obtain a high-purity liraglutide concentrated solution, and then used The mobile phase containing sodium caprate is subjected to salt conversion treatment on the preparation liquid phase to obtain a sodium liraglutide caprate solution, which is concentrated by rotary evaporation and then freeze-dried to obtain sodium liraglutide caprate.

[0055] The preparation process of liraglutide sodium caprate is as follows:

[0056] An aqueous solution of sodium caprate with a concentration of 0.1% was prepared as mobile phase A, and acetonitrile was used as mobile phase B to be used for salt ...

Embodiment 2

[0086] Example 2 Oral enteric-coated preparation of liraglutide sodium caprate

[0087] main formula

[0088] Liraglutide Sodium Caprate 1g

[0089] Trehalose 5g

[0090] Preparation:

[0091] 1) Add the prescribed amount of microcrystalline cellulose and talcum powder at a weight ratio of 8:1, and prepare blank pellet cores with a centrifugal granulator.

[0092] Weigh the prescribed amount of microcrystalline cellulose and talcum powder, mix them with a three-dimensional mixer for 30 minutes, take half of them and put them in the centrifugal pellet machine, and put the other half in the feeder, and take an appropriate amount of purified water and put them in the liquid supply tank , turn on the centrifugal pellet making machine, turn on the turntable, air supply, and spray, wait until the material on the turntable is made into pellets, turn on the powder supply, until the material in the feeder is used up, turn off the spray, powder supply, discharge, and finally turn off...

Embodiment 3

[0099] Example 3 Preparation of oral enteric-coated preparations of liraglutide sodium caprylate

[0100] main formula

[0101] Liraglutide Octanoate Sodium 1g

[0102] Trehalose 5g

[0103] Preparation

[0104] 1) Add the prescribed amount of microcrystalline cellulose and talcum powder at a weight ratio of 8:1, and prepare blank pellet cores with a centrifugal granulator.

[0105] Weigh the prescribed amount of microcrystalline cellulose and talcum powder, mix them with a three-dimensional mixer for 30 minutes, take half of them and put them in the centrifugal pellet machine, and put the other half in the feeder, and take an appropriate amount of purified water and put them in the liquid supply tank , turn on the centrifugal pellet making machine, turn on the turntable, air supply, and spray, but for small pellets made of materials on the turntable, turn on the powder supply until the material in the feeder is used up, turn off the spray, powder supply, discharge, and fin...

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Abstract

The invention discloses an intestinal absorption promoting liraglutide salt for preparing oral enteric-coated preparations, and belongs to the field of medicines. The liraglutide salt is selected from salts formed through reacting liraglutide with sodium caprate, potassium caprate, benzene sulfonic acid, sodium dodecyl benzene sulfonate, potassium dodecyl benzene sulfonate, sodium octanoate, potassium octanoate, sodium laurate, potassium laurate, sodium oleate and potassium oleate.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a liraglutide salt with an intestinal absorption-promoting effect for the preparation of oral enteric-coated preparations, which can obviously improve the oral absorption bioavailability of liraglutide. application in diabetes treatment. Background technique [0002] Diabetes is a common and frequently-occurring disease, and its prevalence is increasing rapidly with the improvement of people's living standards, population aging, and changes in lifestyle. According to statistics, there are more than 90 million diabetic patients in my country, of which type II diabetes patients account for about 90%, and the incidence of type II diabetes is tending to be younger. Diabetes has become the third largest non-communicable disease after cardiovascular diseases and tumors, bringing a heavy burden to society and economy. Therefore, it is of great significance to find safe and effectiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26A61P3/10
Inventor 冷国庆苏宏健刘新宇张琪田辉王丽莉余荣熹杨文龙冷宁
Owner 哈尔滨吉象隆生物技术有限公司
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