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Oral and injection dual-effect protein or polypeptide drug controlled-release vesicle and preparation method thereof

A technology of polypeptides and proteins, which is applied in medical preparations of non-active ingredients, drug delivery, pharmaceutical formulations, etc., can solve problems such as human injury, achieve the effects of avoiding inconvenience and injury, facilitating long-term storage, and prolonging drug efficacy

Inactive Publication Date: 2014-04-16
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to prepare a kind of insulin nanoparticle with oral hypoglycemic effect, to solve the inconvenience caused by traditional diabetes treatment muscle or intravenous injection of insulin and the damage to the human body, only need to take medicine regularly, you can Treat diseases, thereby reducing or even avoiding the pain and inconvenience of medication for patients during the treatment process

Method used

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  • Oral and injection dual-effect protein or polypeptide drug controlled-release vesicle and preparation method thereof
  • Oral and injection dual-effect protein or polypeptide drug controlled-release vesicle and preparation method thereof
  • Oral and injection dual-effect protein or polypeptide drug controlled-release vesicle and preparation method thereof

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Experimental program
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Effect test

specific Embodiment approach 1

[0033]Accurately weigh 3 mg of the above-mentioned silicisome precursor lipid with an electronic balance, put it into a 25 mL round bottom flask, add 2 mL of chloroform, and then depressurize with a rotary evaporator under the conditions of 40 °C and 120 r / min The organic solvent, chloroform, was removed by rotary evaporation, and a lipid film was observed to form on the walls of the round-bottomed flask. Then add a certain amount of prepared insulin mother liquor and polyvinylpyrrolidone solution to the round bottom flask according to different drug-to-lipid ratios, make up to 4 mL with deionized water, and then place the round bottom flask in a water bath for 30 minutes at 40°C. , and then sonicated in a water bath for 5 minutes to form multilamellar vesicles. Finally, use a probe-type ultrasonic instrument to sonicate in an ice bath with 27W ultrasonic treatment for 3 minutes (over 3 seconds and stop for 3 seconds), so that it can be fully dispersed to form a stable system ...

specific Embodiment approach 2

[0034] This embodiment is different from Embodiment 1 in that before adding chloroform, after weighing the organic-inorganic composite lipid, a certain amount of acidic ethanol solution is added to acidify for 30 minutes. Others are the same as the first embodiment.

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Abstract

The invention discloses an oral and injection dual-effect polypeptide drug controlled-release preparation and a preparation method thereof. Moreover, the insulin controlled-release preparation can continuously display the medicinal effect in vivo for a long time in a stable manner. The oral and injection dual-effect polypeptide drug controlled-release preparation uses a non-toxic silica material with superstability as a carrier; polypeptide drug molecules are embedded into the carrier to form nanoscale microspheres; the nanoscale polypeptide drug microspheres have an average particle size of about 200nm. One layer of adhesion molecules is adsorbed to the surfaces of the nanoscale microspheres under the action of electrostatic adsorption, so that the drug nanoscale microspheres can be easily adhered to the wall of the small intestine and detention time is prolonged, so that more polypeptide drug molecule nanoscale microspheres permeate the intestinal mucosa and enter the blood circulation and the lymphatic system by intra-intestinal cells through an epithelial barrier; in the carrier manner, no matter intraperitoneal injection or oral administration, the oral and injection dual-effect polypeptide drug controlled-release preparation can take a good treatment effect so as to display high bioavailability and a continuous medicinal effect.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation of protein or polypeptide drug carriers, in particular to an insulin drug carrier capable of treating diabetes, a preparation method thereof, and an application as a drug carrier in oral and injection administration. Background technique [0002] With the emergence of human gene recombination technology and the development of gene recombination technology in the 1980s, more and more protein and polypeptide drugs have achieved large-scale production. The welcome of doctors and patients has aroused the research and attention of the scientific community. However, there are many limiting factors in the administration of protein and polypeptide drugs, such as relatively large molecular weight, difficult to penetrate biomembranes, easy to be degraded by enzymes in the body, and easy to be affected by various physical and chemical factors in the body, resulting i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/52A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
Inventor 戴志飞靳玉慎梁晓龙
Owner PEKING UNIV
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