Preparation method of yew alcohol micro-emulsion

A paclitaxel and microemulsion technology, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as instability, low bioavailability, toxicity, etc., and achieve bioavailability The effect of low concentration and simple preparation conditions

Inactive Publication Date: 2009-12-30
张鹏
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to provide a preparation method of paclitaxel microemulsion to solve the toxicity and sensitization caused by the current clinically used paclitaxel injection containing polyoxyethylated castor oil, and to solve the problem of diluting the current clinically used paclitaxel injection to 0.3 ~1.2mg / mL is unstable, solving the problem of low bioavailability of oral paclitaxel preparations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1) Raw materials: Prepare the following raw materials according to the preparation amount of 100 ml:

[0022] Paclitaxel (purity 99.5%): 0.2g; refined corn oil: 40mL;

[0023] Soybean lecithin: 20g; Poloxamer 188: 5g; absolute ethanol: 20mL; water: appropriate amount;

[0024] The above-mentioned ingredients are all obtained from commercially available products that meet the Chinese national pharmaceutical preparation standards.

[0025] 2) Operation steps: mix paclitaxel, refined corn oil, soybean lecithin, poloxamer 188, and absolute ethanol in the above formula, mix and stir well; then, add water while stirring until clear, then add water to The full amount, that is, 100mL paclitaxel microemulsion. The particle size of the microemulsion was determined to be about 24nm.

[0026] Note: In the above operation steps, add water while stirring until it becomes clear. When the microemulsion is formed, if the amount of water added has reached or exceeded the full amount, ...

Embodiment 2

[0028] 1) Raw materials: Prepare the following raw materials according to the preparation amount of 100 ml:

[0029] Paclitaxel (99.5% purity): 0.3g; refined corn oil and olive oil: 25mL each;

[0030] Soy lecithin: 25g; Poloxamer 188: 10g; absolute ethanol: 30mL; water: appropriate amount;

[0031] The above-mentioned ingredients are all obtained from commercially available products that meet the Chinese national pharmaceutical preparation standards.

[0032] 2) Operation steps: mix paclitaxel, refined corn oil, olive oil, soybean lecithin, poloxamer 188, and absolute ethanol as the above raw materials, mix and stir well; then, add water while stirring until clear, and then Add water to the full amount to obtain 100mL paclitaxel microemulsion. The particle size of the microemulsion was determined to be about 50nm.

Embodiment 3

[0034] 1) Raw materials: Prepare the following raw materials according to the preparation amount of 100 ml:

[0035] Paclitaxel and its derivatives (99.5% purity): 0.25g; soybean oil: 30mL;

[0036] Soy lecithin: 20g; absolute ethanol: 15mL; water: appropriate amount;

[0037] The above-mentioned ingredients are all obtained from commercially available products that meet the Chinese national pharmaceutical preparation standards.

[0038]2) Operation steps: mix the paclitaxel, soybean oil, soybean lecithin, and absolute ethanol of the above raw materials, mix and stir well; then, add water while stirring until it is clear, and then add water to the full amount to obtain 100mL paclitaxel microemulsion . The particle size of the microemulsion was determined to be about 100nm.

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Abstract

The invention relates to a preparation method of yew alcohol and derivative micro-emulsion thereof, belonging to the technical field of pharmaceutical preparations. In the preparation method, one or the mixture of two of refined corn oil, soybean oil and olive oil is used as an oil phase, one or the mixture of both of lecithin and poloxamer is used as an emulsifying agent, one or the mixture of both of anhydrous alcohol and propylene glycol is used as an emulsifying agent aid, water is used as a water phase, and the yew alcohol or the derivative self-emulsifying micro-emulsion thereof are prepared. The micro-emulsion is a medicine-carrying body of the yew alcohol or the derivative thereof, is an intermediate product, has stable quality, does not have the toxicity and sensitization of polyoxy ethyl substituted castor oil, has targeting property, high oral bioavailability and simple preparation condition, is suitable for industrialization and scale production and can be further prepared into various clinically acceptable dosage forms.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a self-emulsification preparation method of drug-carrying microemulsions, in particular to a preparation method of paclitaxel and its derivative microemulsions. Background technique [0002] Paclitaxel and paclitaxel injection have been recorded in the current United States Pharmacopoeia and Chinese National Drug Standards, and are used for the treatment of metastatic ovarian cancer, breast cancer, lung cancer, and esophageal cancer. The United States Pharmacopoeia and China National Drug Standards stipulate that paclitaxel is a white crystalline powder, odorless and tasteless, its English name is Paclitaxel, and its molecular formula is C 47 h 51 NO 14 , the molecular weight is 853.92. Paclitaxel injection is a colorless transparent or slightly yellow viscous solution, containing 6mg of paclitaxel, 527mg of polyoxyethylated castor oil and 49.7%...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/44A61K47/24A61K47/34A61K47/10A61P35/00
Inventor 张鹏
Owner 张鹏
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