Insulin sustained-release oral preparation and preparation method thereof

A technology for sustained-release preparations and insulin, which is applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve the problems of hypertrophic lipodystrophy, subcutaneous lipoatrophy, induration and drug resistance, etc., and achieves good results. Sustained release effect, blood sugar concentration reduction, effect of broad clinical application prospects

Inactive Publication Date: 2008-04-30
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Insulin is a protein polypeptide drug with hypoglycemic effect. Direct oral administration can be degraded by proteolytic enzymes in the gastrointestinal tract, and it is difficult to enter the body through the intestinal mucosa to exert its effect. Therefore, it is generally administered by subcutaneous injection in clinical practice. This method of administration needs to be injected once or several times a day, and long-term medication has brought great pain and inconvenience to the patient, and is accompanied by various adverse reactions: (1) insulin edema; (2) hypoglycemic reaction; (3) ) hypertrophic lipodystrophy; (4) subcutaneous lipoatrophy; (5) injection site inflammation, induration and drug resistance

Method used

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  • Insulin sustained-release oral preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0017] Dissolve 3 g of dragon's blood in 100 mL of ethanol solution, filter to remove impurities, and obtain dragon's blood ethanol solution (3%, w / v) for later use. Weigh insulin and add to 100mL aqueous solution (pH3.0) containing 2% (w / v) dextran-70 to make the insulin concentration 2.0IU·mL -1 , drop 0.25mL Tween-20 in it, adjust the pH with 0.01M NaOH solution until the solution turns milky white, at this time the pH is 5.3, then slowly add 2mL of Dracaena ethanol solution dropwise under constant stirring, and continue stirring After 30 minutes, a colloidal solution of brick-red dragon's blood insulin nanoparticles was obtained. Take the colloidal solution of brick red dragon's blood insulin nanoparticles and heat it at 10000r min -1 centrifuge at 4°C for 30 min, add the resulting precipitate to an acidic solution of pH 3.0, and then centrifuge under the same conditions to collect the precipitate and freeze-dry to obtain an oral sustained-release preparation of insulin w...

Embodiment 2

[0019] Dissolve 2 g of dragon's blood in 100 mL of ethanol solution, filter to remove impurities, and obtain dragon's blood ethanol solution (2%, w / v) for later use. Weigh insulin and add to 100mL aqueous solution (pH3.0) containing 2% (w / v) dextran-70 to make the insulin concentration 4.0IU·mL -1 , drop 0.25mL Tween-20 in it, adjust the pH with 0.01M NaOH solution until the solution turns milky white, at this time the pH is 5.32, then slowly add 2mL of Dracaena ethanol solution dropwise under constant stirring, and continue stirring After 30 minutes, a colloidal solution of brick-red dragon's blood insulin nanoparticles was obtained. Take the colloidal solution of brick red dragon's blood insulin nanoparticles and heat it at 10000r min -1 centrifuge at 4°C for 30 min, add the resulting precipitate to an acidic solution of pH 3.0, and then centrifuge under the same conditions to collect the precipitate and freeze-dry to obtain an oral insulin sustained-release preparation wit...

Embodiment 3

[0021] Dissolve 1.5 g of dragon's blood in 100 mL of ethanol solution, filter to remove impurities, and obtain dragon's blood ethanol solution (0.5%, w / v) for later use. Add insulin to 100ml of acidic aqueous solution (pH3.0) containing 0.4% (w / v) dextran-70 and 0.6% (v / v) Tween-20, so that the concentration of insulin is 4.0IU ml -1 ; Adjust the pH to 5.31 with 0.01M NaOH solution until the solution turns milky white. Then, under continuous stirring, slowly add 8 ml of ethanol solution (0.5%, w / v) of dragon's blood into the milky white colloid solution, and react for 10 minutes to obtain brown-red dragon's blood insulin nanoparticles colloidal solution. Take the brown-red dragon's blood insulin nanoparticle colloidal solution, and use it at 10000r·min -1 centrifuge at 4°C for 30min, add the obtained precipitate to an acidic solution of pH 3.0, and then centrifuge under the same conditions, take the precipitate, freeze-dry to obtain insulin oral sustained-release preparation...

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Abstract

A sustained releasing medicament of insulin for oral administration and a process for preparation relates to insulin for oral administration. The invention provides insulin sustained releasing medicament for oral administration and a process for preparation for the diabetic to reduce blood sugars. The invention is made of nanometer grains of dragon's blood insulin, which contains dragon's blood and insulin. The nanometer grain of dragon's blood insulin takes the insulin as the core, and the dragon's blood as the coating layer. The process comprises getting miscible liquids by confecting the dragon's blood alcohol solution with the concentration of 1-5%, and filtering, charging 1-3g of insulin with the activity unit of 26.7 IU / mg to 100ml dextran-70, and charging tween 20 or tween 80, regulating the pH level of the miscible liquids by NaOH solution until the solution become lacte, charging the dragon's blood alcohol solution after filtration to the lacte solution, getting the lateritious colloidal solution of nanometer grain of dragon's blood insulin by churning up, getting the deposition by centrifugation, washing the deposition with acid solution. The insulin sustained releasing medicament for oral administration is made by freezing and drying the deposition.

Description

technical field [0001] The invention relates to an oral insulin, in particular to an oral slow-release preparation of dragon's blood jelly insulin with hypoglycemic effect mainly used for diabetic patients and a preparation method thereof. Background technique [0002] Insulin is a protein polypeptide drug with hypoglycemic effect. Direct oral administration can be degraded by proteolytic enzymes in the gastrointestinal tract, and it is difficult to enter the body through the intestinal mucosa to exert its effect. Therefore, it is generally administered by subcutaneous injection in clinical practice. This method of administration needs to be injected once or several times a day, and long-term medication has brought great pain and inconvenience to the patient, and is accompanied by various adverse reactions: (1) insulin edema; (2) hypoglycemic reaction; (3) ) hypertrophic lipodystrophy; (4) subcutaneous lipoatrophy; (5) injection site inflammation, induration and drug resista...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K38/28A61K47/46A61P5/48A61P3/10A61K36/889
Inventor 侯振清张其清王鑫娟
Owner XIAMEN UNIV
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