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Paclitaxel ethosome gel and preparation method thereof

A technology of ethosomes and paclitaxel, which is applied in liposome delivery, liquid delivery, aerosol delivery, etc., can solve the problems of high drug toxicity and difficulty of transdermal drug delivery, so as to increase drug loading and promote drug delivery. Transdermal penetration effect, effect of reducing irritation

Active Publication Date: 2013-06-19
STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to overcome the disadvantages of high toxicity and difficulty in percutaneous administration of paclitaxel injection in the prior art, and provide a paclitaxel ethosome gel and its preparation method

Method used

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  • Paclitaxel ethosome gel and preparation method thereof
  • Paclitaxel ethosome gel and preparation method thereof
  • Paclitaxel ethosome gel and preparation method thereof

Examples

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preparation example Construction

[0070] In addition, the present invention also provides a preparation method of the above-mentioned paclitaxel plastid gel, which comprises the following steps:

[0071] First, use the composition of the above-mentioned steroids of the present invention as raw materials to prepare paclitaxel steroids;

[0072] Secondly, use mechanical methods to sizing the paclitaxel plastids obtained;

[0073] Finally, the sized paclitaxel plastid and the gel are mixed and uniformly developed to obtain a paclitaxel plastid gel, which is a gel that does not contain paclitaxel.

[0074] Preferably, an injection method or a thin film dispersion method is used to prepare the paclitaxel plastids.

[0075] Preferably, an injection method is used to prepare the paclitaxel plastid, and the injection method includes, for example, mixing other components except water in the composition of the paclitaxel plastid of the present invention under airtight conditions, and then using the paclitaxel plastid The total w...

preparation Embodiment 1

[0101] Preparation Example 1 (preparation of paclitaxel plastid gel by injection method)

[0102] This example 1 is used to illustrate the paclitaxel plastid gel of the present invention and its preparation method.

[0103] 1. Preparation of paclitaxel plastids

[0104] Weigh out 0.04g of paclitaxel, 0.8g of phospholipids, 0.08g of cholesterol, 0.08g of stabilizers and 0.04g of antioxidants, and dissolve them in 7.0g of ethanol to form an ethanol solution containing paclitaxel, and then place the ethanol solution on a magnetic stirrer. Under 600rpm (revolutions / min) high-speed stirring and airtight conditions, distilled water (11.96g) was slowly and uniformly injected into it at a rate of 0.3mL / min. After the injection of distilled water was completed, stirring was continued for 5 minutes to obtain paclitaxel alcohol. The obtained paclitaxel alcohol plastids are sized, and the specific method is: under the condition of ice water bath, ultrasonic sonication probe (Ningbo Xinzhi JY-92...

preparation Embodiment 2

[0112] Preparation Example 2 (preparation of paclitaxel plastid gel by thin film dispersion method)

[0113] This example 2 is used to illustrate the paclitaxel plastid gel of the present invention and its preparation method.

[0114] 1. Preparation of paclitaxel plastids

[0115] Weigh 0.06g paclitaxel, 1.2g phospholipids, 0.24g cholesterol, 0.12g stabilizer, 0.06g antioxidant, and dissolve it in 100mL chloroform / methanol organic solvent with a volume ratio of 4:1; set the water bath temperature of the rotary evaporator 50℃, rotation speed 200rpm, vacuum degree 200~800mbar (mbar), rotary evaporation to fully evaporate the organic solvent; after the organic solvent evaporates, add ethanol / water (ethanol 8.0g, water 10.32g) mixed solution, vortex condition After hydration, the hydration temperature is 45℃, and the hydration time is 30min, the paclitaxel alcohol plastids are obtained. The paclitaxel alcohol plastids obtained are sized, and the specific method is: under ice-water bath...

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Abstract

The invention discloses a paclitaxel ethosome gel and a preparation method of the paclitaxel ethosome gel. The paclitaxel ethosome gel contains ethosome and gel; the ethosome and the gel are uniformly mixed; the ethosome is particles containing paclitaxel, low-molecular-weight alcohols, phospholipid, cholesterol, a stabilizing agent and an antioxidant; the gel contains a gel matrix, a penetrationaccelerator, a humectant, a preservative, a pH conditioning agent and water; the ethosome and the gel are mixed according to a certain weight proportion, and the ethosome and the gel have specific compositions respectively. According to the paclitaxel ethosome gel provided by the invention, the action of stimulation to the skin can be reduced, and the percutaneous permeation effect is good.

Description

Technical field [0001] The invention relates to a transdermal drug delivery formulation of paclitaxel and a preparation method thereof, in particular to a paclitaxel plastid gel and a preparation method thereof. Background technique [0002] Paclitaxel (Paclitaxel) is a complex secondary metabolite extracted and isolated from Taxus genus of Taxus family. It is a tetracyclic diterpenoid compound. As early as 1971, American scientists M.E.Wani and M.C.wal extracted and isolated from the bark of Taxus brevifolia, and confirmed its anti-cancer activity. In 1992, paclitaxel injection was first approved for marketing by the US Food and Drug Administration (FDA) for the treatment of ovarian cancer, and subsequently approved for marketing in Canada. At present, it has been approved for marketing in more than 50 countries in the world, and is widely used clinically in the treatment of ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, etc., and studies have shown...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K9/127A61K31/337A61P35/00
Inventor 谭剑平蒋立新常坦然周志文
Owner STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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