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Oral administration system capable of promoting trans-mucus penetration of protein drug and preparation of oral administration system

A protein drug and drug delivery system technology, applied in the field of oral drug delivery system and its preparation, can solve the problems of weakening, complicated production process, induration and inflammation of injection site

Active Publication Date: 2020-07-28
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Protein drugs have been widely used in the clinical treatment of various diseases due to their advantages such as high pharmacological activity, strong specificity, and less toxic and side effects. Currently, injections are the main route of clinically administered biological drugs, but this method of administration is often Accompanied by the following problems: 1. The pain associated with the injection weakens the patient's compliance
2. Strict preparation requirements for injection forms, complex production process and high cost
3. Repeated injections cause symptoms such as induration and inflammation at the injection site
However, when protein drugs are administered orally, they are easily degraded by various proteolytic enzymes in the gastrointestinal tract. At the same time, protein drugs have high molecular weight and low fat solubility, and it is difficult to achieve transmembrane absorption in the gastrointestinal tract, which leads to the oral biogenesis of drugs. Very limited availability (<1%)

Method used

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  • Oral administration system capable of promoting trans-mucus penetration of protein drug and preparation of oral administration system
  • Oral administration system capable of promoting trans-mucus penetration of protein drug and preparation of oral administration system
  • Oral administration system capable of promoting trans-mucus penetration of protein drug and preparation of oral administration system

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0053] Example 1 Preparation of Hydrophobic Modified Mesoporous Silica

[0054] sample 1

[0055] Weigh 0.5g CTAB and dissolve it in 160mL double-distilled water, stir in a 60°C water bath at a speed of 600rpm for 0.5h to fully dissolve, add 70mL n-octane dropwise to the above clear solution, and connect to a condensing reflux device , and continued to stir for 2h to obtain a uniform emulsion. Slowly add 18 mL of styrene monomer dropwise to the emulsion. Under nitrogen protection, 0.11 g of lysine, 5.0 mL of tetraethyl orthosilicate, and 0.181 g of azobisisobutylamidine hydrochloride were sequentially added to the reaction solution. After reacting for 3 hours, the suspension was naturally cooled, left to stand for about 10 hours, an equal volume of absolute ethanol was added, centrifuged at 10000 rpm for 8 minutes, and the precipitate was washed 3 times with absolute ethanol. After the precipitate was dried at 60°C for 12h, it was calcined at 550°C for 6h to remove the pore...

example 2

[0059] Example 2 Preparation of self-assembled nanoparticles loaded with insulin

[0060] sample 1

[0061] Weigh 3 mg of the carrier prepared in sample 1 in Example 1, 3 mg of insulin and 3 mg of dodecyl betaine and dissolve them in 0.2 mL of DMSO, slowly add the above suspension into 5 ml of distilled water, and centrifuge at 10,000 rpm for 8 min to obtain the carrier Drug System (MSN-S@TSB).

[0062] sample 2

[0063] Weighed 3 mg of the carrier prepared in sample 2 in Example 1, 3 mg of insulin and 3 mg of dilauroyl lecithin were dissolved in 0.2 mL of DMSO, slowly added the suspension to 5 ml of distilled water, and centrifuged at 10,000 rpm for 8 min to obtain the carrier Drug System (MSN-DC@TSB).

[0064] sample 3

[0065] Weighed 3 mg of the carrier prepared in sample 1 in Example 1, 3 mg of insulin and 3 mg of dilauroyl lecithin were dissolved in 0.2 mL of DMSO, slowly added the suspension to 5 ml of distilled water, and centrifuged at 10,000 rpm for 8 min to obta...

example 3

[0069] Example 3 Cell Uptake Experiment

[0070] Caco-2 cells were treated with 1×10 5 / mL concentration was cultured in a 12-well plate, and the cells were cultured until the confluence reached 90%. After the cells were washed with PBS, the vector was dispersed into a serum-free medium and incubated with Caco-2 cells at 37°C for 4 hours. After the incubation, the nanoparticle dispersion was discarded, and the cells were washed 3 times with ice-cold PBS to terminate cell uptake. Add 0.25% trypsin to digest cells, suspend with 0.3mL PBS, use blank cells as negative control, set 3 wells for each sample, collect 10,000 cells each, measure the average fluorescence intensity, MSN-S@DLPC, MSN-S@ Compared with MSN-NH, TSB, MSN-DC@DLPC, and MSN-DC@TSB respectively 2 Increased to 1.2, 2, 20 and 13 times (average fluorescence intensity as attached Figure 4 ). This result shows that the drug delivery system prepared by the present invention can significantly improve the uptake of t...

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Abstract

The invention belongs to the field of biomedicine, and relates to an oral administration system capable of promoting trans-mucus penetration of a protein drug and preparation of the oral administration system, in particular to preparation of a drug carrying system capable of promoting trans-gastrointestinal tract mucus layer penetration of the protein medicine and application of the drug carryingsystem in oral administration of the protein drug. The preparation of the drug carrying system comprises the following steps: taking cetyl trimethyl ammonium bromide as a template, tetraethoxysilane as a silicon source and styrene as a pore-enlarging agent, and removing the temperature through high-temperature calcination to prepare a mesoporous silica carrier; and after the carrier adsorbs and carries the protein drug, carrying out hydrophobization modification on the surface of the drug-carrying silicon dioxide with stearic acid or cholic acid, and further using hydrophobic acting force anda zwitterionic surfactant dodecyl dimethyl betaine or dilauroyl phosphatidylcholine to form self-assembly nanoparticles. The oral administration system can promote penetration of the protein drug in the gastrointestinal tract mucus layer and improve transmembrane absorption of the drug, has the advantages of low toxicity, high drug loading capacity and the like, and has broad application prospectsin oral administration of the protein drug.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to an oral drug delivery system for promoting transmucus penetration of protein drugs and its preparation. Background technique [0002] Protein drugs have been widely used in the clinical treatment of various diseases due to their advantages such as high pharmacological activity, strong specificity, and less toxic and side effects. Currently, injection is the main route of administration of biological drugs in clinical practice, but this method of administration is often Accompanied by the following problems: 1. The pain associated with the injection weakens the patient's compliance. 2. The requirements for the preparation of injection forms are strict, the production process is complicated and the cost is high. 3. Repeated injections cause symptoms such as induration and inflammation at the injection site. Compared with injection administration, oral administration is more compliant, ec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K38/28A61P3/10B82Y5/00A61K38/38A61K38/47
CPCA61K38/28A61K47/6949B82Y5/00A61K47/544A61K47/54A61P3/10A61K38/47C12Y302/01017A61K38/385
Inventor 高亦鲲王思玲何叶
Owner SHENYANG PHARMA UNIVERSITY
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