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Insulin oral nano-preparation and preparation method thereof

A nano-preparation and insulin technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of being easily damaged by the gastrointestinal environment, poor patient compliance, and short biological half-life, etc. problems, achieve good development prospects, good biocompatibility, and prolong the effect of validity

Inactive Publication Date: 2015-02-18
FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commonly used insulin dosage form in clinic is subcutaneous injection dosage form, which has problems such as poor patient compliance, inconvenience of long-term medication, and many adverse reactions. Therefore, it is of great clinical significance to develop an oral dosage form of insulin
[0003] However, insulin, as a protein and polypeptide drug, has obstacles such as large molecular weight, strong water solubility, poor membrane permeability, short biological half-life, and easy to be destroyed by the gastrointestinal environment, which make its oral bioavailability Only 0.1%-2%

Method used

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  • Insulin oral nano-preparation and preparation method thereof
  • Insulin oral nano-preparation and preparation method thereof
  • Insulin oral nano-preparation and preparation method thereof

Examples

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preparation example Construction

[0023] (1) Preparation of nanosuspension: Weigh thiolated hyaluronic acid and insulin and dissolve them in the water phase, wherein the mass ratio of thiolated hyaluronic acid to insulin is 0.5:1-10:1; add surface The active agent can be Tween 80, soybean lecithin, egg yolk lecithin, macrogolglyceride oleate, macrogolglyceride caprylate, macrogol 40 hydrogenated castor oil, polyoxyethylene 35 castor oil , one or more mixtures of polyethylene glycol 15 hydroxystearate, the dosage is 0.1%-10% (w / v); the organic phase is dichloromethane, acetone, cyclohexane, n-hexane, One or more mixtures of diethyl ether; surfactants added to the organic phase are macrogol glyceride oleate, Span 80, macrogol glyceride caprate caprylate, macrogol 40 hydrogenated castor oil , polyoxyethylene 35 castor oil, polyethylene glycol 15 hydroxystearate or a mixture of more than one, the dosage is 0.1%-10% (w / v); the volume ratio of the aqueous phase to the organic phase is 5 :1-1:20; the ultrasonic powe...

Embodiment 1

[0025] Example 1 Preparation of Oral Nano-Preparation of Insulin

[0026]

[0027] Preparation process: Dissolve mercapto-hyaluronic acid and insulin in distilled water, add Tween 80, mix evenly as the water phase, slowly add the water phase into acetone containing polyoxyethylene 35 castor oil under magnetic stirring, and ultrasonic probe 300W , 5min, to obtain W / O type colostrum; remove acetone by rotary evaporation at 40°C, add distilled water to 200ml, and then ultrasonically probe at 300W, 5min, to obtain insulin nanoparticle suspension; add lactose and mannose to insulin nanoparticle suspension Alcohol is used as a lyoprotectant, pre-frozen at -70°C for 8 hours, and freeze-dried for 48 hours.

Embodiment 2

[0028] Example 2 Preparation of Oral Nano-Preparation of Insulin

[0029]

[0030] Preparation process: Dissolve thiolated hyaluronic acid and insulin in distilled water, add Tween 80, mix evenly as the water phase, slowly add the water phase into dichloromethane containing soybean lecithin under magnetic stirring, ultrasonic probe at 250W for 3min , to obtain W / O type colostrum; remove acetone by rotary evaporation at 40°C, add distilled water to 200ml, and then ultrasonically probe at 250W for 3min to obtain insulin nanoparticle suspension; add glucose and mannitol to the insulin nanoparticle suspension as The lyoprotectant was pre-frozen at -70°C for 8 hours, and then freeze-dried for 48 hours.

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Abstract

The invention discloses an insulin oral nano-preparation and a preparation method thereof. Polymer sulfhydrylated hyaluronic acid with biocompatibility and bio-adhesion is adopted as a carrier to prepare an insulin-entrapped nano-suspension, and a lyophilized preparation is finally prepared. According to the method, the bio-adhesive material sulfhydrylated hyaluronic acid is firstly used as the carrier to prepare sulfhydrylated hyaluronic acid nano-particles, the insulin oral bioavailability can be improved by the preparation, and the preparation has the characteristic of excellent stability, is easy to store and transport, is convenient for patient using, and is a preparation with wide development prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to an oral insulin nano-preparation and a preparation method thereof. Background technique [0002] There are 350 million people with diabetes in the world, and there is an increasing trend year by year. About 1 / 4 of the sick people suffer from type 1 diabetes and need to use insulin for life. At present, the commonly used insulin dosage form in clinic is subcutaneous injection dosage form, which has problems such as poor patient compliance, inconvenience of long-term medication, and many adverse reactions. Therefore, it is of great clinical significance to develop an oral dosage form of insulin. [0003] However, as a protein and polypeptide drug, insulin has obstacles such as large molecular weight, strong water solubility, poor membrane permeability, short biological half-life, and easy to be destroyed by the gastrointestinal environment, which make its o...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K47/36A61K9/19A61P5/48
Inventor 宋洪涛黄爱文赵佳丽刘莹于西全
Owner FUZHOU GENERAL HOSPITAL OF NANJING MILITARY COMMAND P L A
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