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Self-emulsifying agglomerant of oral polypeptide medicine

A polypeptide and self-emulsification technology, which is applied in the fields of pharmaceutical formulation, emulsion delivery, peptide/protein composition, etc., can solve the problems of bioavailability not exceeding 5%, unsatisfactory results, etc.

Inactive Publication Date: 2003-11-19
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many studies on the oral administration of polypeptide drugs such as INS, including liposomes, emulsions, enteric-coated preparations, etc., but the bioavailability has not exceeded 5%. In recent years, some new drug delivery systems have been used for oral administration of INS , such as nanoparticles (capsules), microemulsions, colon-targeted drug delivery systems, etc., but the results are still unsatisfactory

Method used

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  • Self-emulsifying agglomerant of oral polypeptide medicine
  • Self-emulsifying agglomerant of oral polypeptide medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Insulin (Insulin, INS) 1g, polysorbate 1g, polyoxyethylene hydrogenated castor oil 2.5g, caprylic / capric glyceride 2g, ethanol 0.5g, chitosan 0.5g, water 15ml, appropriate amount of pH regulator, dissolved After mixing, freeze-dry for 20 hours to obtain the oral self-emulsifying polypeptide drug agglomerates of the present invention.

Embodiment 2

[0042] Dissolve and mix 0.1g of parathyroid hormone, 1g of polysorbate, 2.5g of polyoxyethylene hydrogenated castor oil, 2g of peanut oil, 0.5g of ethanol, 2.5g of chitosan, and 30ml of water, and freeze-dry for 30 hours. The oral self-emulsifying polypeptide drug agglomerates of the present invention are obtained.

Embodiment 3

[0044] After dissolving 2g of INS, 0.5g of chitosan, and 10ml of 0.1N hydrochloric acid, add 2.5g of polyoxyethylene hydrogenated castor oil, 1g of peanut oil, and 50ml of water, after dissolving and mixing, directly spray-dry to obtain the oral self-administered drug of the present invention. Emulsifying peptide drug agglomerates.

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Abstract

An oral-applied self-emulsifying polypeptide medicine is prepared from polypeptide, gel adhesive, surfactant, co-surfactant, oil enzyme inhibitor, and diluent. Its preparing process is also disclosed. It features that after it comes in intestinal tract, it is emulsified by itself to become nano-class microemulsion, which can penetrate through intestinal mucosa and epithelial barrier into lymph and blood, and be attached on intestinal inner surface to promote its absorption.

Description

technical field [0001] The invention relates to an oral polypeptide drug preparation and a preparation method thereof. Background technique [0002] With the development of biotechnology and genetic engineering, more and more polypeptide and protein drugs are used in clinical treatment, and most polypeptide drugs are biologically active and unstable to heat and enzymes, so they are often given by injection. medicine. However, long-term injection administration brings great pain to patients, and requires special injection techniques, which makes it difficult for patients to administer medicines independently, resulting in high finished products and high medical expenses. Therefore, domestic and foreign pharmaceutical workers have been committed to the research of non-injection routes of polypeptide drugs, such as nasal cavity, rectal, oral, lung, eye, transdermal absorption and so on. Among the above-mentioned routes of administration, oral administration is particularly at...

Claims

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Application Information

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IPC IPC(8): A61K38/16A61K47/30
Inventor 金方李立民富天骄
Owner SHANGHAI INST OF PHARMA IND
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