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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, pharmaceutical formulations, etc., can solve the problems of difficulty in transdermal administration and high toxicity of administration, and achieve the effect of promoting transdermal penetration and increasing the loading capacity. Dosage, easily deformed effect

Active Publication Date: 2012-07-18
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 the preparation method of above-mentioned paclitaxel ethosome gel, which comprises the following steps:

[0071] First, using the above-mentioned ethosome composition of the present invention as a raw material, prepare paclitaxel ethosome;

[0072] Secondly, the obtained paclitaxel elastosomes are sized by a mechanical method;

[0073] Finally, the granulated paclitaxel elastosome and the gel were mixed and ground evenly to obtain the paclitaxel elastosome gel, and the gel was a gel that did not contain paclitaxel.

[0074] Preferably, the paclitaxel ethosomes are prepared by an injection method or a film dispersion method.

[0075] Preferably, the paclitaxel ethosomes are prepared using an injection method, which includes, for example, mixing other components of the paclitaxel ethosomes of the present invention except water under airtight conditions, and then injecting the ethosomes with the ethosomes The total weight ...

preparation Embodiment 1

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

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

[0103] 1. Preparation of paclitaxel elastosomes

[0104] Take paclitaxel 0.04g, phospholipid 0.8g, cholesterol 0.08g, stabilizer 0.08g and antioxidant 0.04g, be dissolved in 7.0g ethanol, form the ethanol solution containing paclitaxel, then this ethanol solution is placed on the magnetic stirrer, 600rpm (rev / min) high-speed stirring and under airtight conditions, distilled water (11.96g) was slowly and uniformly injected thereinto at an injection rate of 0.3mL / min, and continued to stir for 5min after the injection of distilled water was completed, to obtain paclitaxel ethosomes. The obtained paclitaxel ethosomes were granulated, and the specific method was: under the condition of an ice-water bath, a probe ultrasonic instrument (Ningbo Xinzhi JY-92 2D) wa...

preparation Embodiment 2

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

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

[0114] 1. Preparation of paclitaxel elastosomes

[0115] Take paclitaxel 0.06g, phospholipid 1.2g, cholesterol 0.24g, stabilizer 0.12g, antioxidant 0.06g, be dissolved in the organic solvent of 100mL chloroform / methanol that volume ratio is 4: 1; Set the water bath temperature of rotary evaporator 50°C, rotation speed 200rpm, vacuum degree 200-800mbar (mbar), rotary evaporation to fully evaporate the organic solvent; after the organic solvent has evaporated, add ethanol / water (ethanol 8.0g, water 10.32g) mixed solution, vortex condition hydration at 45° C. and 30 minutes for hydration time to obtain paclitaxel ethosomes. The obtained paclitaxel plastid is sized, and the specific method is: under the ice-water bath condition, the digital display high-sp...

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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 paclitaxel transdermal preparation and a preparation method thereof, in particular to a paclitaxel ethosome gel and a preparation method thereof. Background technique [0002] Paclitaxel is a complex secondary metabolite extracted and isolated from Taxus genus Taxus, a tetracyclic diterpenoid compound. As early as 1971, it was extracted and isolated from the bark of Taxus brevifolia by American scientists M.E.Wani and M.C.wal, and its anticancer activity was confirmed. In 1992, paclitaxel injection was first approved by the US Food and Drug Administration (FDA) for the treatment of ovarian cancer, and was subsequently approved for marketing in Canada. At present, it has been approved for marketing in more than 50 countries in the world, and it is widely used in the treatment of ovarian cancer, breast cancer, prostate cancer, non-small cell lung cancer, etc. It also has obvious effects in the treatment of inflammation and sk...

Claims

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Application Information

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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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