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Oral insulin compound medicine preparation and its preparing method

A compound preparation and insulin technology, applied in the field of medicine, can solve problems such as troublesome use and drug effect destruction

Active Publication Date: 2007-10-31
TONGHUA GOLDEN-HORSE PHARM IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a new oral insulin compound preparation in view of the defects that the existing injection insulin preparations are troublesome to use and easily cause drug resistance and the drug effect is destroyed during the use of oral preparations

Method used

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  • Oral insulin compound medicine preparation and its preparing method
  • Oral insulin compound medicine preparation and its preparing method
  • Oral insulin compound medicine preparation and its preparing method

Examples

Experimental program
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Effect test

example 1

[0093] 1. Dissolve 100 mg of recombinant human insulin lyophilized powder in 5 ml of 0.01 mol / L HCl solution, add 100 ml of 1% PEG 3350 (polyethylene glycol, or one or more of molecular weight 2000-8000, the following same);

[0094] 2. Add 5ml 125mmol / L CaCl in sequence 2 (or other calcium-containing compounds such as calcium nitrate, etc.) and 1ml of 165mmol / L Na 3 C 6 h 5 o 7 , the pH is adjusted to 6-9 to make A solution;

[0095] 3. Dissolve 1000mg of casein in the buffer solution of phosphorus-containing compounds (such as phosphoric acid, phosphate solution) to make B solution with a casein concentration of 3mg / ml;

[0096] 4. Add solution B to solution A, stir for 24-48 hours, and the reaction temperature is 4-5°C;

[0097] 5. Vacuum freeze-drying to prepare the oral insulin compound preparation of the present invention.

example 2

[0099] 1. Dissolve 100mg of recombinant human insulin lyophilized powder in 5ml of 0.01mol / L HCl solution, add 100ml of 1% PEG 3350;

[0100] 2. Add 5ml 125mmol / L CaCl in sequence 2 and 1ml of 165mmol / L Na 3 C 6 h 5 o 7 , adjust the pH to be 6-9;

[0101] 3. Mix 5ml 125mmol / L Na 2 HPO 4 Add to the above solution, stir for 24-48 hours; vacuum freeze-dry to make freeze-dried product;

[0102] 4. Dissolve 1000mg casein in phosphate buffer solution, the concentration is 3mg / ml;

[0103] 5. Add the freeze-dried product to casein phosphate buffer, stir and mix well, and the reaction temperature is 4-5°C;

[0104] 6. Vacuum freeze-drying to prepare the oral insulin compound preparation of the present invention.

[0105] Add 600-800 mg of the absorption promoter sodium deoxycholate to the lyophilized product of the oral insulin compound preparation described in Example 1-2, and fill 200 mg of the disintegrating agent microcrystalline cellulose into enteric-coated capsules to pr...

example 3

[0113] 1. Dissolve 20umol of insulin in 10ml of 60%DMF / 40%H at room temperature 2 O (pH9.6);

[0114] 2. Dissolve 28umol of mPEG-SPA in 1.5ml of DMF, and add it to the insulin solution for reaction, add 1mol / L NaOH to maintain the reaction pH, react at room temperature for about 30 minutes, then add 25ml H 2 O ends the reaction;

[0115] 3. Use 0.01% NH in the reaction mixture 4 HCO 3 Dialysis, lyophilization after dialysis to obtain monomethoxypolyethylene glycol derivative-insulin composite preparation;

[0116] 4. Dissolve the monomethoxypolyethylene glycol derivative-insulin compound preparation in 5ml of water, add 100ml of 1% PEG 3350, mix well, then add 5ml of 125mmol / L CaCl in turn 2 and 1ml of 165mmol / L Na 3 C 6 h 5 o 7 , adjust the pH value to 6-9 to make A solution;

[0117] 5. Dissolve 1000mg of casein in phosphate buffer to make B solution with a casein concentration of 3mg / ml;

[0118] 6. Add solution B into solution A, stir for 24-48 hours, and the rea...

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Abstract

The invention discloses an oral insulin complexing preparation, which is characterized by the following: allocating 1-15% insulin raw material, 50-97% stable protecting agent, 1-15% carrying medicine carrier, 1-20% absorption promoting agent; setting the stable protecting agent as one or several of carbowax and casein, protamine, albumin and protease inhibitor; setting the carrying medicine carrier as calcium phosphate salt; setting the absorption promoting agent as one or several of salicylic acid, cholate and fatty acid; setting the insulin raw material as human retooling insulin or human retooling insulin chemical trimmed by single methoxy carbowax derivant. This invention also relates to a preparing method of oral insulin complexing preparation. This invention can increase biostability of human retooling insulin and can resist degradation of gastrointestinal tract enzyme.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to an oral insulin compound preparation and a preparation method thereof. Background technique [0002] Diabetes is a common chronic disease that threatens human beings. There are currently 130 million diabetic patients in the world. With the enrichment of material life and the reduction of physical activity, the number of people with diabetes is increasing year by year. The incidence of diabetes has increased from 1% more than ten years ago to 2.5% at present. Various complications of diabetes, such as cardiovascular, kidney, fundus and nerve lesions, are the main factors causing loss of labor, disability and death of patients, and its mortality rate has also risen to the third place after cardiovascular disease and cancer. [0003] Insulin is the drug of choice for the treatment of diabetes. Since insulin is a protein polypeptide substance, it is easily degraded by prote...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K9/28A61K9/48A61K47/48A61K47/34A61K47/42A61P3/10A61K47/10A61K47/60
Inventor 邓柳红张春发杨卫帆
Owner TONGHUA GOLDEN-HORSE PHARM IND CO LTD
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