Submicroemulsion injection containing polyene paclitaxel and its preparing method

A technology of docetaxel and submicroemulsion, applied in the field of medicine, can solve the problems of toxic and side effects of human body, large toxic and side effects, no major progress, etc., and achieve the effects of simple preparation process, improved solubility, and reduced toxicity

Inactive Publication Date: 2007-07-18
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Docetaxel is poorly soluble in water. Even if it is prepared as an injection, it has relatively large toxic and side effects in clinical application and is likely to cause more complications, such as allergic reactions, bone marrow suppression, neurotoxicity, cardiovascular toxicity, hair loss, etc. , while the bioavailability of the drug in vivo is low, and it needs to be used for a long time
Attempts to modify its structure to reduce adverse effects have not made much progress so far
[0004] At present, docetaxel is mainly prepared from polyoxyethylene hydrogenated castor oil and ethanol, etc., which have toxic and side effects on the human body after injection, especially before using docetaxel injection, you must first take anti-allergic drugs or inject anti-allergic Drugs are used to help alleviate the severe allergies and other toxic and side effects caused by the use of docetaxel injection, which often bring pain to patients and directly affect the use of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Docetaxel 200mg

[0041] Soy Lecithin for Injection 0.8g

[0042] Soybean oil for injection l0g

[0043] Poloxamer 188 0.4g

[0044] Oleic acid 0.3g

[0045] Glycerin 2.5g

[0046] Add water for injection to 100ml

[0047] method:

[0048] 1. Preparation of the oil phase: Add oleic acid and docetaxel to the oil for injection at 50-70°C, stir and mix well to form the oil phase.

[0049] 2. Prepare the water phase: add phospholipids, poloxamer 188, glycerin, etc. into the water for injection at 50-70°C, stir and mix well to form the water phase.

[0050] 3. Preparation of colostrum: On the premise of maintaining a constant temperature of 50-70°C and constant stirring, slowly inject the oil phase into the water phase, stir quickly, adjust the pH value to 4-9, and constant volume. Homogenized by a homogenizer to obtain colostrum.

[0051] 4. Preparation of final milk: pass the prepared colostrum through a high-pressure homogenizer or a microfluidizer, and repeatedly...

Embodiment 2

[0053] Docetaxel 200mg

[0054] Soy Lecithin for Injection 1.2g

[0055] Soybean oil for injection 10g

[0056] V E 0.2g

[0057] Glycerin 2.5g

[0058] Add water for injection to 100ml

[0059] Other experimental steps were the same as in Example 1, and the docetaxel submicroemulsion of the present invention was obtained.

Embodiment 3

[0061] Docetaxel 400mg

[0062] Yolk Lecithin 1.6g

[0063]Soybean oil for injection 15g

[0064] Tween-80 0.4g

[0065] Oleic acid 0.4g

[0066] Glycerin 2.5g

[0067] Add water for injection to 100ml

[0068] Other experimental steps were the same as in Example 1, and the docetaxel submicroemulsion of the present invention was obtained.

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Abstract

A sub-microemulsion injection of polyene taxol with a certain target performance and low poison is prepared from polyene taxol, the oil for injection, emulsifier, stabilizer, isotonic regulator, pH regulator, and emulsifying aid. Its preparing process is also disclosed.

Description

Technical field: [0001] The invention belongs to the technical field of medicine and relates to a submicroemulsion preparation for injection in the field of drug administration, more specifically a semi-synthetic taxane anticancer drug-docetaxel submicroemulsion injection and a preparation method thereof. Background technique: [0002] Docetaxel (the trade name of the imported product is Taxotere) is an inactive compound extracted from the needles of the European berry yew. This product is a semi-synthetic paclitaxel derivative developed by the French company Aventis. It is a microtubule Depolymerization inhibitor, which acts on the microtubule / tubulin system, arrests cells in G2 and M phases by promoting the assembly of microtubule dimers into microtubules and stabilizing microtubules by preventing the depolymerization process , thereby inhibiting the mitosis and proliferation of cancer cells. Docetaxel is effective for advanced breast cancer, non-small cell lung cancer, o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/337A61P35/00
Inventor 王东凯黎玲
Owner SHENYANG PHARMA UNIVERSITY
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