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Polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation containing same, and preparing methods and application of polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation

A solid particle, protease inhibitor technology, applied in peptide/protein components, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of complex preparation process, difficulty, cell damage, etc. The preparation process is simple, the cost is low, and the effect of promoting absorption

Inactive Publication Date: 2018-10-16
SCI RAINBOW BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In the above methods, some absorption enhancers have irreversible damage to cells, and the preparation process of some drug carriers is relatively complicated, which leads to many difficulties in practical application.

Method used

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  • Polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation containing same, and preparing methods and application of polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation
  • Polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation containing same, and preparing methods and application of polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation
  • Polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation containing same, and preparing methods and application of polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0062] Preparation Example 1 Preparation of Insulin Granules Encapsulated by Pluronic F127 / PLGA

[0063] Dissolve 10mg of SNAC in 0.5mL of 0.01M NaOH aqueous solution, and dissolve 1mg of insulin (Ins) and 1mg of aprotinin in 0.5mL of 0.01M NaOH aqueous solution (containing 1% Tween 20) and add them to the SNAC solution to form a uniform Solution (A); 80mg Pluronic F127 / and 10mg PLGA were added to 4mL of ethanol / dichloromethane (ethanol:dichloromethane=1:4), which was fully dissolved to form a homogeneous solution (B); slowly added A to In B, after vortex mixing at 500r / min to form W / O emulsion (C), slowly add (C) dropwise into 20mL liquid paraffin (containing 1% Span 80) to form W / O / O microspheres; add The microspheres were solidified with n-hexane, continued to stir for 1.5 h, washed with n-hexane for 3 times, put the microspheres into a vacuum drying oven to dry for 24 h, and obtained Pluronic F127 / PLGA-coated insulin granules.

preparation Embodiment 2

[0064] Preparation Example 2 Preparation of Insulin Granules Encapsulated by Pluronic F127 / Eudragit S100

[0065] Dissolve 100mg of SNAC in 1mL of 0.01M NaOH aqueous solution, and dissolve 10mg of Ins and 10mg of aprotinin in 1mL of 0.01M NaOH aqueous solution, and add them to the SNAC solution to form a homogeneous solution (A); mix 200mg of Pluronic F127 and 200mg of Eudragit S100 Add to 48mL 95% ethanol (containing 10mL H 2 O) fully dissolved to form a solution (B); slowly add A to B, and vortex mix at 500r / min to form a homogeneous solution, and then use spray drying technology to prepare insulin granules wrapped in Pluronic F127 / Eudragit S100.

preparation Embodiment 3

[0066] Preparation Example 3 Preparation of Insulin Granules Encapsulated by Pluronic F127 / Eudargit S100

[0067] Dissolve 200mg of SNAC in 1mL of 0.01M NaOH aqueous solution, and dissolve 10mg of Ins and 10mg of aprotinin in 1mL of 0.01M NaOH aqueous solution, and add them to the SNAC solution to form a homogeneous solution (A); mix 200mg of Pluronic F127 and 200mg of Eudragit S100 Add to 48mL 95% ethanol (containing 10mL H 2 O) fully dissolved to form a solution (B); slowly add A to B, and vortex mix at 500r / min to form a homogeneous solution, and then use spray drying technology to prepare insulin granules wrapped in Pluronic F127 / Eudragit S100.

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Abstract

The invention relates to a polypeptide-protein-drug-carried solid particulate matter with mucous penetrability and a preparation containing the same, and preparing methods and application of the polypeptide-protein-drug-carried solid particulate matter with the mucous penetrability and the preparation. The solid particulate matter comprises, by weight, 0.5-90 parts, preferably 1-50 parts, of polypeptide protein drugs, 0.5-90 parts, preferably 5-50 parts, of absorption enhancers, 0-50 parts, preferably 1-30 parts, of protease inhibitors, and 5-90 parts, preferably 10-90 parts, of mucous penetrability materials. The provided mucous penetrability solid preparation contains the solid particulate matters wrapped with the mucous penetrability materials and colon-specific materials. A prepared drug delivery system can resist degradation of gastric acid and gastric intestinal enzymes to the polypeptide protein drugs during oral administration and meanwhile has the mucous penetrability and colon-specific effects, and absorption of polypeptide proteins in an intestinal tract can be effectively promoted; and a preparation technology is simple, the required cost is low, and the polypeptide-protein-drug-carried solid particulate matter with the mucous penetrability and the preparation are suitable for industrial production.

Description

technical field [0001] The present invention relates to the field of biopharmaceuticals, and more specifically relates to a mucus-penetrating solid particle containing polypeptide protein drugs, a preparation containing the solid particle, a preparation method and an application thereof. The mucus-penetrating solid preparation of the present invention is mainly used for preparing oral polypeptide and protein medicines, and has a better effect of improving the biological efficacy of polypeptide and protein medicines. Background technique [0002] Peptide protein drugs, such as insulin, human growth hormone, and calcitonin, are administered by injection. However, there are many disadvantages in injection administration, such as the short biological half-life of insulin, and 1-2 insulin injections per day will cause side effects such as local redness and swelling, subcutaneous nodules, subcutaneous fat atrophy, etc., which bring great pain and pain to patients. inconvenient. ...

Claims

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Application Information

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IPC IPC(8): A61K38/28A61K38/23A61K38/22A61K9/50A61K9/54A61K47/18A61K47/12A61K47/10A61K47/32
CPCA61K9/5026A61K9/5031A61K9/5073A61K38/2278A61K38/23A61K38/28A61K47/12A61K47/18A61K47/42
Inventor 刘彦其他发明人请求不公开姓名
Owner SCI RAINBOW BIOPHARMA CO LTD
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