Exenatide oral preparation and preparation method thereof

A technology of exenatide and oral preparations, which is applied in the field of exenatide oral preparations and its preparation, can solve the problems of patients' physical, psychological and economic burdens, poor patient compliance, and low bioavailability, so as to improve bioavailability , lowering blood sugar, lowering the effect of fasting blood sugar

Inactive Publication Date: 2015-07-01
东莞市麦亘生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the frequent injection of exenatide, the patient's compliance is poor, causing a great burden on the patient's body, mind and economy.
At present, there is no oral dosage form of exenatide in the market, and the development of oral dosage forms of exenatide has the following technical difficulties: (1) Exenatide is a protein polypeptide drug, which is easily degraded by various proteases in the gastrointestinal tract Out of action
(2) Exenatide is a macromolecular drug with a large molecular weight, which makes it difficult to absorb into the blood through the gastrointestinal barrier
3) Drugs absorbed into the blood through the gastrointestinal tract face the first-pass action of the liver, resulting in low bioavailability

Method used

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  • Exenatide oral preparation and preparation method thereof
  • Exenatide oral preparation and preparation method thereof
  • Exenatide oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of exenatide-charged excipient particles

[0042] S1. Take a certain amount of charged auxiliary chitosan (molecular weight: 20,000-100,000) and place it in 5% (v / v) glacial acetic acid aqueous solution to fully dissolve it so that the concentration of chitosan is 4 mg / ml ( m / v); configure exenatide aqueous solution so that the concentration is 8 mg / ml;,

[0043] S2. measure the chitosan solution of 10ml in the vial, add 2ml exenatide solution and stir, add cross-linking agent sodium tripolyphosphate after 3h, stir for 24h, get exenatide-chitosan microparticle solution;

[0044] S3. Stop stirring, remove the supernatant, and centrifuge at 15,000 rpm for 5 minutes; add the lyoprotectant lactose, freeze-dry, and exenatide-chitosan microparticles.

Embodiment 2

[0045] Example 2 Preparation of exenatide-charged excipient particles

[0046] S1. Take a certain amount of charged auxiliary material acrylic resin EudragitL100 and place it in a mixed solvent of methanol and dichloromethane to fully dissolve it so that the concentration of EudragitL100 is 0.5 mg / ml (m / v); prepare an aqueous solution of exenatide to make the concentration 0.5 mg / ml; The two solutions are mixed and homogeneous at 8000rpm / 1min at low temperature. The mixed solution was transferred to liquid paraffin containing Span 80, and the solvent evaporated rapidly under stirring.

[0047] S2. Wash the obtained particles with petroleum ether and ultrapure water, and filter.

[0048] S3. The microparticles were dispersed in pure water, centrifuged at 8000 rpm for 20 minutes, and the supernatant was removed; the freeze-drying protective agent mannitol was added and freeze-dried to obtain exenatide-acrylic resin microparticles.

Embodiment 3

[0049] Example 3 Preparation of exenatide-charged excipient particles

[0050] S1. Take a certain amount of charged excipient sodium alginate (molecular weight: 20,000-100,000), fully dissolve it in water, so that the concentration of sodium alginate is 2 mg / ml (m / v); configure exenatide aqueous solution, so that the concentration is 2 mg / ml;

[0051] S2. Measure 10ml of sodium alginate solution in a vial, add 0.5ml of exenatide solution and stir, add cross-linking agent glutaraldehyde after 0.5h, and stir for 12h to obtain exenatide-sodium alginate particle solution;

[0052] S3. Stop stirring, remove the supernatant, and centrifuge at 8000 rpm for 20 min; add lyoprotectant sucrose, freeze-dry, exenatide-sodium alginate microparticles.

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Abstract

The invention relates to the technical field of oral preparations containing bio-polypeptides and in particular discloses an exenatide oral preparation and a preparation method thereof. The exenatide oral preparation contains exenatide-charged auxiliary material particles, wherein the exenatide-charged auxiliary material particles are prepared from exenatide accounting for 0.1-20% of the total weight of solids of the oval preparation and a charged auxiliary material accounting for 0.5-50% of the solids of the oval preparation. The exenatide oral preparation is capable of reducing postprandial blood sugar and properly reducing fasting blood glucose, can be used for treating type II diabetes and can also be applied to the patients with treatment failure in medicines of metformin and sulphonylurea.

Description

technical field [0001] The invention relates to the technical field of oral administration preparations of biological polypeptides, in particular to an exenatide oral preparation and a preparation method thereof. Background technique [0002] Diabetes is the most important chronic non-communicable disease after cardiovascular and cerebrovascular diseases, which seriously endangers human health. In recent years, with the change of people's lifestyle, the prevalence of diabetes has shown a sharp upward trend. At present, my country is the largest country with diabetes, with an incidence rate of 6.4%, which is much higher than that of developed countries in Europe and America. There are more than 94 million diabetic patients in my country, and type 2 diabetes (Type 2 Diabetes, T2DM) is the main body of diabetes, accounting for about 90% of diabetic patients. T2DM is caused by the interaction of genetics and various environmental factors, resulting in the defect of insulin secr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/22A61P3/10
Inventor 李相鲁于为常解玉玲张严冬
Owner 东莞市麦亘生物科技有限公司
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