Novel oral micelle preparation of pegylated phosphatide-entrapped insulin

A technology of pegylated phospholipids and polyethylene glycol, applied in the field of medicine, can solve the problems affecting the quality of life of patients and their families, malnutrition of subcutaneous fat, hypoglycemia, etc., to protect smooth entry into blood circulation and improve solubility , the effect of reducing contact

Active Publication Date: 2014-05-14
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This not only brings a great economic burden to patients, but also affects the quality of life of patients and their families. At the same time, frequent long-term injections of drugs will also cause many adverse reactions such as: insulin edema, hypoglycemia, hypertrophic lipodystrophy and subcutaneous fat. Atrophy, etc.

Method used

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  • Novel oral micelle preparation of pegylated phosphatide-entrapped insulin
  • Novel oral micelle preparation of pegylated phosphatide-entrapped insulin
  • Novel oral micelle preparation of pegylated phosphatide-entrapped insulin

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Embodiment Construction

[0013] The invention provides an oral insulin micelle preparation, which contains therapeutically effective doses of insulin, pegylated phospholipids, and pharmaceutically acceptable adjuvants.

[0014] The insulin micelles involved in the present invention can be in solution or freeze-dried form as required.

[0015] According to the present invention, the molar ratio of insulin and pegylated phospholipid is 1:2 to 1:20, preferably 1:4 to 1:10.

[0016] The pegylated phospholipid of the present invention is formed by combining polyethylene glycol molecules with nitrogen-containing bases on the phospholipid molecules through covalent bonds.

[0017] For the PEGylated phospholipid of the present invention, the number of carbon atoms contained in the fatty acid in the phospholipid part of the structure is 10 to 24, preferably 12, 14, 16, 18, 20, 22, 24 carbon atoms, fatty acid The chain can be saturated or partially saturated, especially the fatty acids that need to be pointed ...

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Abstract

The invention provides an oral nanometer insulin micelle preparation, comprising a therapeutically effective amount of insulin, pegylated phosphatide and pharmaceutically acceptable adjuvant. The insulin micelle preparation is prepared by using a one-step self-assembly method; particles with a uniform size can be formed, and the entrapment rate of insulin reaches more than 99.0%. In the micelle preparation, polyethylene glycol long chains can be distributed on the surface of a hydrophobic nucleus of an entrapment drug to form a hydrophilic protection film, which is favorable for overcoming a slime layer barrier, an enzyme barrier and an epidermal barrier in an alimentary canal system and protecting smooth entering of insulin into a blood circulation system for performance of hypoglycemic activity.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to an oral insulin micelle preparation and a preparation method thereof. Background technique [0002] Insulin (Insulin, INS) is the drug of choice for insulin-dependent diabetic patients so far due to its unique hypoglycemic effect. Currently, almost all insulin preparations are administered by injection. This not only brings a great economic burden to patients, but also affects the quality of life of patients and their families. At the same time, frequent long-term injections of drugs can also cause many adverse reactions such as: insulin edema, hypoglycemia, hypertrophic lipodystrophy and subcutaneous fat. atrophy etc. [0003] Oral administration is the most common way of administration, and it is the most easily accepted by patients among many routes of administration, especially for those patients who need long-term or frequent medication. Compliance is much better than other routes o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/19A61K38/28A61K47/34A61P3/10
Inventor 魏秀莉于继兵梁伟
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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