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Oral calcitonin liposome and lyophilized preparation thereof

A technology of liposome and freeze-drying protective agent, which is applied in the direction of liposome delivery, anti-toxic agent, peptide/protein composition, etc., to achieve good drug effect, increase stability, and strong reproducibility

Inactive Publication Date: 2012-11-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for most therapeutic drugs, oral administration is the most acceptable and convenient route of administration for patients. Therefore, it is of great significance to design a preparation that can overcome various barriers of polypeptide drugs in the gastrointestinal tract and have high oral bioavailability. Important practical significance and fill the gap in the market

Method used

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  • Oral calcitonin liposome and lyophilized preparation thereof
  • Oral calcitonin liposome and lyophilized preparation thereof
  • Oral calcitonin liposome and lyophilized preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Dissolve 1.6g of soybean lecithin, 0.4g of DSPG, and 0.3g of cholesterol in a mixed solution of chloroform and methanol, remove the organic solvent by rotary evaporation, put it in a vacuum desiccator overnight, add calcitonin solution, hydrate for 30min, and ultrasonically probe at 400W, 200 Once, after passing through a 450nm microporous membrane for use, the obtained calcitonin liposome was added dropwise to the Arg8 solution, and magnetically stirred to obtain the calcitonin liposome modified by Arg8. The obtained Arg8-modified calcitonin liposomes were added dropwise into the TMC solution, and magnetically stirred to obtain Arg8-modified TMC-coated calcitonin liposomes.

Embodiment 2

[0032] Dissolve 2.0g of soybean lecithin, 0.4g of DSPG, and 0.4g of cholesterol in a mixed solution of chloroform and methanol, remove the organic solvent by rotary evaporation, put it in a vacuum desiccator overnight, add calcitonin solution, hydrate for 30min, and ultrasonically probe at 400W, 400 Once, after passing through a 450nm microporous membrane for use, the obtained calcitonin liposome was added dropwise to the Arg8 solution, and magnetically stirred to obtain the calcitonin liposome modified by Arg8. The obtained Arg8-modified calcitonin liposomes were added dropwise into the TMC solution, and magnetically stirred to obtain Arg8-modified TMC-coated calcitonin liposomes.

Embodiment 3

[0034] Dissolve 2.0g of soybean lecithin, 0.5g of DSPG, and 0.3g of cholesterol in a mixed solution of chloroform and methanol, remove the organic solvent by rotary evaporation, put it in a vacuum desiccator overnight, add calcitonin solution, hydrate for 30min, and ultrasonically probe at 200W, 400 Once, after passing through a 450nm microporous membrane for use, the obtained calcitonin liposome was added dropwise to the Arg8 solution, and magnetically stirred to obtain the calcitonin liposome modified by Arg8. The obtained Arg8-modified calcitonin liposomes were added dropwise into the TMC solution, and magnetically stirred to obtain Arg8-modified TMC-coated calcitonin liposomes. The lyoprotectant was added into the preparation, pre-frozen at -70°C for 4 hours, and freeze-dried for 48 hours to obtain Arg8-modified TMC-coated calcitonin liposomes.

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Abstract

The present invention relates to the field of pharmaceutical preparations, and particularly to an oral calcitonin liposome and a lyophilized preparation thereof. The oral calcitonin liposome is characterized in that a water-soluble polypeptide drug calcitonin is encapsulated into an inner aqueous phase of a liposome or is tightly adsorbed on the surface of liposome membrane; then cell-permeable peptide Arg8 and a high molecular TMC are sequentially adopted to modify the surface of the liposome to prepare an oral calcitonin liposome with a characteristic of mucous membrane adhesion; and then a freeze drying treatment is performed to prepare a lyophilized preparation, wherein an average particle size of the preparation is less than 180 nm, and rat in vivo experiment results show that efficacy of the preparation is increased by 103 times compared with the efficacy of oral calcitonin solutions.

Description

technical field [0001] The invention relates to the field of designing pharmaceutical preparations, in particular to N-trimethyl chitosan-coated calcitonin liposomes modified by membrane-penetrating peptide (D-Arg8) and freeze-dried preparations thereof. Background technique [0002] The research and development of non-injection drug delivery routes for protein and polypeptide drugs has long been a field of pharmacy researchers at home and abroad. Among them, oral administration has always been the main direction of researchers' efforts because of its economy, convenience, and accurate dosage. However, there are many obstacles in the oral delivery of peptide and protein drugs: ①Degradation of gastric acid. The pH of gastric acid is around 1 to 2.5, and many peptide and protein drugs lose most or even all of their biological activities in this environment; ②Enzyme degradation. The degradation of enzymes in the gastrointestinal tract is one of the important factors leading to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K38/23A61K47/28A61K47/42A61P3/14A61P5/20A61P19/08A61P19/10A61P25/00A61P39/02
Inventor 黄爱文平其能李赛肖衍宇孙敏捷
Owner CHINA PHARM UNIV
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