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A liposome preparation for nasal administration of teriparatide and its preparation method

A technology of liposome preparation and teriparatide, which is applied in the field of nasal administration liposome and its preparation, can solve the problems of reduced activity of polypeptide drugs, difficulty in realizing industrialization, and low encapsulation efficiency, and achieves low toxicity, Effect of prolonging residence time and improving bioadhesion

Active Publication Date: 2019-11-22
南京星银药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The traditional methods of liposome preparation include reverse phase evaporation method, thin film method, calcium fusion method, surfactant treatment method and extrusion container method, etc., but the liposomes prepared by these methods have the following problems: encapsulation efficiency is low, Residual organic solvents or surfactants may reduce the activity of polypeptide drugs and make it difficult to realize industrialization. For this reason, new liposome preparation methods have become a hot spot in liposome research

Method used

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  • A liposome preparation for nasal administration of teriparatide and its preparation method
  • A liposome preparation for nasal administration of teriparatide and its preparation method
  • A liposome preparation for nasal administration of teriparatide and its preparation method

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Effect test

Embodiment 1

[0030]

[0031] a) Teriparatide, soybean lecithin, cholesterol, DSPE-PEG2000 and sodium cholate were dissolved in supercritical CO 2 / ethanol solvent, and solubilize a certain amount of distilled water to form a supercritical microemulsion;

[0032] b) pre-expand the supercritical microemulsion under the conditions of set pressure (16MPa) and temperature (335K); quickly spray the phosphate buffer solution in the supercritical collection tank through a nozzle at a certain flow rate (3L / min) In the medium (pH is 5.5), through dispersion and precipitation, liposome suspension is formed;

[0033] c) CO 2 Continue to pass through the supercritical collection kettle to dissolve and remove the residual ethanol in the liposome suspension, and empty it after measuring with the rotameter to collect the nanoliposome suspension in the supercritical collection kettle, which is Teripa Peptide flexible nanoliposomes;

[0034] d) adding phosphatidylglycerol to the teriparatide flexible ...

Embodiment 2

[0037]

[0038] a) Teriparatide, egg yolk lecithin, cholesterol, DSPE-PEG2000 and sodium deoxycholate were dissolved in supercritical CO 2 / ethanol solvent, and solubilize a certain amount of distilled water to form a supercritical microemulsion;

[0039] b) The supercritical microemulsion is pre-expanded under the conditions of set pressure (20MPa) and temperature (328K); with a certain flow rate (2.5L / min), it is quickly sprayed into the phosphate buffer in the supercritical collection tank through the nozzle In the solution medium (pH is 6.5), after dispersion and precipitation, liposome suspension is formed;

[0040] c) CO 2 Continue to pass through the supercritical collection kettle to dissolve and remove the residual ethanol in the liposome suspension, and empty it after measuring with the rotameter to collect the nanoliposome suspension in the supercritical collection kettle, which is Teripa Peptide flexible nanoliposomes;

[0041] d) adding phosphatidic acid to ...

Embodiment 3

[0044]

[0045] a) Teriparatide, egg yolk lecithin, cholesterol, DSPE-PEG2000 and sodium deoxycholate were dissolved in supercritical CO 2 / ethanol solvent, and solubilize a certain amount of distilled water to form a supercritical microemulsion;

[0046] b) The supercritical microemulsion is pre-expanded under the conditions of set pressure (25MPa) and temperature (338K); with a certain flow rate (3.5L / min), it is quickly sprayed into the phosphate buffer in the supercritical collection tank through the nozzle In solution medium (pH is 7.0), after dispersion and precipitation, liposome suspension is formed;

[0047] c) CO 2 Continue to pass through the supercritical collection kettle to dissolve and remove the residual ethanol in the liposome suspension, and empty it after measuring with the rotameter to collect the nanoliposome suspension in the supercritical collection kettle, which is Teripa Peptide flexible nanoliposomes;

[0048] d) adding stearylamine to the teripar...

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Abstract

The invention discloses a teriparatide nasal administration liposome preparation and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The teriparatide nasal administration liposome preparation is mainly prepared from 0.01-0.5g of teriparatide, 0.1-1.5g of phospholipid, 0.015-0.6g of cholesterol, 0.015-0.2g of DSPE-PE2000, 0.012-0.5g of a membrane softener and 0.02-0.3g of a stabilizing agent. The teriparatide is encapsulated, and the liposome is controllable in grain size from 20nm to 100nm and uniform in distribution, the encapsulation efficiency of the liposome is higher than 90% and the activity of the liposome is stabilized above 90%. The nasal administration liposome preparation can achieve the non-injection administration of the teriparatide, and the liposome preparation can improve the bioavailability of the teriparatide, reduce the toxic and side effects of the teriparatide and improve patient's medication compliance.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a nasal administration liposome of teriparatide and a preparation method thereof. Background technique [0002] Teriparatide is a recombinant human parathyroid hormone 1-34 (rhPTH1-34), which can promote bone formation and is clinically used to treat osteoporosis. The drug was developed by Eli Lilly and Company in the United States and was approved by the FDA in 2002. The administration method of teriparatide has always been injection administration. Long-term injection administration not only increases the toxic and side effects of the drug, but also makes patients very painful and inconvenient. Adverse reactions may even occur such as allergies, induration, Inflammation etc. Therefore, it is of great clinical significance to develop a safe, effective and convenient non-injection teriparatide preparation—teriparatide nasal administration liposome. [0003] There are...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/29A61K9/127A61K47/24A61K47/28A61P19/10
CPCA61K9/0043A61K9/127A61K38/29A61K47/10A61K47/24A61K47/28
Inventor 支钦姚志勇李新宇曹演威吴丽芬
Owner 南京星银药业集团有限公司
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