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A kind of preparation method of insulin sustained-release oral preparation

A technology for oral preparations and insulin, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of subcutaneous fat atrophy, inconvenience and pain of patients, etc. Controllable appearance, good biocompatibility and water solubility

Active Publication Date: 2017-02-22
YANGZHOU UNIV
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  • Abstract
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Problems solved by technology

However, subcutaneous injection will cause subcutaneous fat atrophy, which will bring inconvenience and pain to patients

Method used

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  • A kind of preparation method of insulin sustained-release oral preparation
  • A kind of preparation method of insulin sustained-release oral preparation
  • A kind of preparation method of insulin sustained-release oral preparation

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Experimental program
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Embodiment Construction

[0029] 1. Preparation process

[0030] 1. Synthesis of PEGylated Chitosan

[0031] Weigh 1g CS (CS is chitosan, molecular weight 500000), dissolve it in 6 ml acetic acid, the volume concentration of acetic acid (v / v) is 2%, dilute it with 20 ml TEMED•HCL, add it into a three-necked flask, and measure the pH The value is about 5, then add a certain amount of EDC and NHS, after 30 minutes, weigh mPEG-COOH according to the molar ratio of mPEG-COOH:CS=1:1, add it to a three-necked flask, keep the constant temperature water bath at 35°C, and stir for 36 hours. pH 4-6 was controlled during the reaction.

[0032] The obtained crude product was placed in a dialysis bag for dialysis for 4 days, and freeze-dried to obtain PEGylated chitosan.

[0033] 2. Preparation of Insulin-Loaded PEGylated Chitosan Microspheres

[0034] (1) Take a certain amount of PEG-CS (polyethylene glycolated chitosan) and TPP (sodium tripolyphosphate) and dissolve them in distilled water respectively to obtai...

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Abstract

The invention relates to a preparation method of an insulin slow-release oral preparation, which belongs to the technical field of biomedicine. The present invention uses polyethylene glycol chitosan (PEG-CS) as encapsulation material, adopts ion gel method to prepare insulin-loaded polyethylene glycol chitosan microspheres, that is, a certain concentration of PEG-CS solution and insulin Mix the solutions, add low-concentration sodium tripolyphosphate (TPP) dropwise under magnetic stirring, and adjust the pH to 5.5 with hydrochloric acid. After the reaction is completed, centrifuge the suspension to collect the microspheres. The preparation method of the present invention is simple, the conditions are mild, the obtained microspheres have good biocompatibility, can be stably released in simulated intestinal fluid for 7 days, have a sustained release function, and can ensure the biological activity of the drug, and are expected to realize the oral administration of insulin.

Description

technical field [0001] The invention relates to a method for encapsulating insulin, in particular to a preparation method for insulin slow-release oral preparations, and belongs to the technical field of biomedicine. Background technique [0002] Basal insulin is the main drug for the treatment of diabetes, and it plays an important role in the treatment of type 1 and type 2 (including other types) diabetes patients. The evaluation of basal insulin therapy in the guidelines of the American Diabetes Association is "the most effective". Subcutaneous injection of insulin has been the main route of administration for diabetic patients since the technology of recombinant human insulin made the wide application of insulin possible. However, subcutaneous injection can cause subcutaneous fat atrophy, which brings inconvenience and pain to patients. In order to overcome the disadvantages of subcutaneous injection, improve patient compliance, and improve patient quality of life, it i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/28A61K47/10A61K47/36A61K9/16A61K9/50A61P5/48
Inventor 宋晓丽许春兰闫彩凤朱爱萍郭荣
Owner YANGZHOU UNIV
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