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Compound phosphatide transfer body with high deformability and application thereof in preparing transdermal drug delivery preparation

A technology of compound phospholipid and transfer body, which is used in the preparation of transdermal drug delivery preparations, in the field of compound phospholipid transfer body, can solve problems such as deformation of preparations, and achieve the advantages of improving deformability, improving transdermal penetration effect, and improving drug efficacy. Effect

Inactive Publication Date: 2014-01-08
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problem of improving the deformability of preparations in the prior art, the present invention provides a composite phospholipid transfer body that can significantly improve deformability, and the technical scheme is as follows:

Method used

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  • Compound phosphatide transfer body with high deformability and application thereof in preparing transdermal drug delivery preparation
  • Compound phosphatide transfer body with high deformability and application thereof in preparing transdermal drug delivery preparation
  • Compound phosphatide transfer body with high deformability and application thereof in preparing transdermal drug delivery preparation

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Embodiment 1

[0017] The preparation of embodiment 1 complex phospholipid transfer body

[0018] The complex phospholipids consist of dipalmitoylphosphocholine (DPPC) and dimyristoylphosphatidylcholine (DMPC). Precisely weigh 0.2mmol of phospholipids (DMPC / DPPC mixed in a certain proportion) and Span 80 accounting for 15% of the total weight of phospholipids are co-dissolved in an appropriate amount of absolute ethanol, and injected into a phosphate solution of pH 7.4 in a constant temperature water bath and magnetically stirred. After the ethanol is completely evaporated, take it out and let it cool down, and make up the volume with ultrapure water; the probe ultrasonically reduces the particle size of the transfer body, and the product is obtained.

Embodiment 2

[0019] The preparation of embodiment 2 composite phospholipid transfer body gel

[0020] The complex phospholipids consist of dipalmitoylphosphocholine (DPPC) and dimyristoylphosphatidylcholine (DMPC). Accurately weigh 0.2mmol of phospholipid (DMPC / DPPC mixed in a certain proportion) and sodium cholate accounting for 10% of the total weight of phospholipids are dissolved in an appropriate amount of dichloromethane, and the organic solvent is removed by rotary evaporation at 40°C to form a film. After standing in vacuum overnight, add Physiological saline is hydrated, and the hydration solution is homogenized under high pressure to reduce the particle size of the transfer body. Another mixture of carbomer 940 and glycerin at a ratio of 1:5, adding an appropriate amount of purified water, stirring evenly, adding dropwise 4% aqueous sodium hydroxide solution to adjust the pH to 6-11, then adding ethylparaben and mixing evenly, to obtain the condensate Gel base. The prepared com...

Embodiment 3

[0021] The preparation of embodiment 3 complex phospholipid transfer body spray

[0022] The complex phospholipids consist of dipalmitoylphosphocholine (DPPC) and dimyristoylphosphatidylcholine (DMPC). Precisely weigh 0.2mmol of phospholipid (DMPC / DPPC mixed in a certain proportion) and sodium deoxycholate accounting for 12% of the total weight of phospholipids are co-dissolved in an appropriate amount of chloroform, add phosphate buffer, ultrasonically form an emulsion, evaporate under reduced pressure to remove the organic solvent The liposome suspension is formed, extruded with a polycarbonate membrane to reduce the particle size of the transfer body, filtered, filled in a spray bottle, sealed, and packaged to obtain a finished product.

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Abstract

The invention provides a compound phosphatide transfer body with high deformability. The compound phosphatide transfer body with high deformability comprises the following components in parts by weight: 0.5-5 parts of a surfactant, 1-10 parts of dipalmitoyl phosphorylcholine and 1-10 parts of dimyristoyl phosphorylcholine, wherein the surfactant is selected from sodium cholate, sodium deoxycholate, Twain and Span; the molar ratio of the dipalmitoyl phosphorylcholine to the dimyristoyl phosphorylcholine is (1: 1)-(1: 6); and the compound phosphatide transfer body with high deformability can be prepared by adopting any method of preparing lipidosome. Compared with the frequently-used granulesten and lecithin transfer bodies in the prior art, the deformability of the provided compound phosphatide transfer body is improved remarkably, the stability of a carrier is also improved remarkably, and the capability of a packaged drug of passing through a skin barrier is finally and remarkably improved, i.e. the percutaneous penetration effect is improved. By applying the transfer body technology to the transdermal drug delivery preparation, the capability of the drug of passing through a horny layer is improved obviously, and the drug effect can be improved obviously.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a highly deformable complex phospholipid transfer body and its application in the preparation of transdermal preparations. Background technique [0002] Transfersomes (transfersomes) are self-aggregating vesicles developed on the basis of liposomes, and their composition is generally that a certain surfactant is mixed into the phospholipid bilayer, thereby endowing it with special deformability and making it Under the action of external pressure, it can be squeezed and deformed to pass through the intercellular pores of the stratum corneum with a pore size of only 1 / 5 to 1 / 10 of its own particle size (Cevc G. Transfersomes, liposomes and other lipid suspensions on the skin: permeation enhancement, vesicle Penetration, and transdermal drug delivery. Crit Rev The Drug Carrier Syst.1996,13(3–4):257–388.), so as to carry the encapsulated drug through the stratum c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K31/475A61K9/06A61K9/12A61P29/00
Inventor 陈军蔡宝昌董洁顾薇陆姗姗
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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