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Percutaneous-absorption-promoting propranolol composite phospholipid transfersome, and prepartion method and application thereof

A technology of propranolol compound phospholipids and compound phospholipids, applied in the application of propranolol compound phospholipid transfer body in the treatment of infantile hemangioma, compound phospholipid transfer body and its preparation field, can solve the problem of infant hemangioma area Fixed, the skin surface is not easy to stick for a long time, and the transdermal absorption is limited, so as to achieve the effect of promoting transdermal absorption, improving bioavailability and improving curative effect

Inactive Publication Date: 2014-03-19
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Judging from the current technology, propranolol for transdermal administration has been made into dosage forms such as patches, but the area of ​​infantile hemangioma is not fixed, and the skin surface is not easy to stick for a long time, so it is undoubtedly to use liquid or semi-solid dosage forms. More suitable for clinical application needs
However, direct administration of propranolol has high polarity and limited transdermal absorption. The transfer body technology composed of a single phospholipid can promote the transdermal absorption of propranolol, but to a limited extent.

Method used

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  • Percutaneous-absorption-promoting propranolol composite phospholipid transfersome, and prepartion method and application thereof
  • Percutaneous-absorption-promoting propranolol composite phospholipid transfersome, and prepartion method and application thereof
  • Percutaneous-absorption-promoting propranolol composite phospholipid transfersome, and prepartion method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment 1 blank phospholipid transfer body

[0040] Weigh 2 to 20 parts of phospholipid materials, the total amount of which is controlled at 0.2 mmol, and co-dissolve with 0.2 to 2 parts of marginal active agent in an appropriate amount of absolute ethanol, inject it into a 0.2 mol / L ammonium sulfate aqueous solution with constant temperature water bath and magnetic stirring, and pass Ethanol was evaporated by heating or depressurization, then taken out and allowed to cool, and the volume was adjusted to 5 mL with ultrapure water; a 200 W probe was sonicated for a certain period of time to reduce the particle size of the phospholipid transfer body, and the titanium powder was removed by low-speed centrifugation before dialysis bag, and then dialyzed with pH 7.4 phosphate buffer to remove the ammonium sulfate in the outer water phase that was not encapsulated by the phospholipid transfersome to obtain a blank composite phospholipid transfersome.

Embodiment 2

[0041] Example 2 Preparation of propranolol phospholipid transfer body

[0042] On the basis of the blank phospholipid transfer body prepared in Example 1, given drug / phospholipid=19.83% by molar ratio, take a certain amount of propranolol and the blank phospholipid transfer body, and incubate for a certain period of time in a constant temperature water bath to make propranol Propranolol is encapsulated by phospholipid transfer body to make propranolol composite phospholipid transfer body.

Embodiment 3

[0043] Example 3 Determination of Encapsulation Efficiency of Propranolol Phospholipid Transfer Body

[0044] The specific operation steps are divided into three steps:

[0045] ①Sample treatment: Sephadex G-50 column was used to separate the crude propranolol phospholipid transfersome sample prepared in Example 2 to obtain the drug-containing transfersome and free drug. , 12000 rpm -1 Set aside after centrifugation.

[0046] ② Determination of the content of drug-containing transfer bodies and free drug by high-performance liquid chromatography: Precisely draw 1 mL of the sample and elute it on a high-performance liquid chromatography Kromasil C18 column (250 mm×4.6 mm, 5 μm), and the mobile phase is methanol-0.02 mol L -1 K H 2 PO 4 (50:50), flow rate 0.9 mL·min -1 , the column temperature was 35 °C, the detection wavelength was 289 nm, and the injection volume was 10 μL. Under this chromatographic condition, the drug-containing transfersome can be separated from the ...

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Abstract

The invention provides a composite phospholipid transfersome which promotes propranolol percutaneous absorption, and a preparation method thereof. According to the invention, two phospholipid materials with different phase-change temperatures, which are dipalmitoyl phosphatidyl choline and soybean lecithin, are adopted as a composite phospholipid material. Compared with a transfersome with a single phospholipid material in prior art, the propranolol composite phospholipid transfersome prepared with the phospholipid material provided by the invention has substantially improved encapsulation efficiency, reduced leakage, improved stability in rat plasma, and substantially improved bioavailability after percutaneous administration. The propranolol composite phospholipid transfersome provided by the invention is especially suitable to be used for treating infantile hemangioma. With the transfersome, propranolol percutaneous administration can be realized, and propranolol can directly act upon a hemangioma affected part. The treatment effect is improved, toxic and side effects are reduced, and children medication compliance can be improved. Also, the invention provides a preparation method of the propranolol composite phospholipid transfersome.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a composite phospholipid transfer body capable of promoting propranolol percutaneous absorption and a preparation method thereof, and also provides the propranolol composite phospholipid transfer body for treating infantile hemangioma Applications. Background technique [0002] Propranolol, as a classic non-selective β-receptor blocker, has been widely confirmed to have the exact effect in the treatment of infantile hemangiomas (Infantile Hemangiomas, IH). At present, propranolol is mostly administered orally for IH treatment, but due to the long treatment cycle of IH, this way of administration is poorly compliant for infants and young children, and may lead to bradycardia, hypotension, hypotension, etc. Extensive adverse reactions such as blood sugar, and oral administration of propranolol has been confirmed to have a serious first-pass effect and low bioav...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/138A61K47/24A61P35/00
Inventor 陈军蔡宝昌顾薇肖寒露李俊
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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