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Paclitaxel lipid microspheres injection and preparation method thereof

A lipid microsphere, paclitaxel technology, applied in the field of medicine, can solve the problems of high cost of paclitaxel liposome, not being widely used, unfavorable for large production, etc. Effect

Inactive Publication Date: 2008-06-25
李时海 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The paclitaxel submicroemulsion prepared by the traditional fat emulsion prescription and process will precipitate paclitaxel after being placed for two weeks; the cost of paclitaxel liposomes is high, which is not conducive to large-scale industrial production, and has not been widely used so far; The paclitaxel injection prepared by the paclitaxel solubility method cannot be widely used in clinical practice due to its high toxicity and irritation

Method used

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  • Paclitaxel lipid microspheres injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Prescription 1:

[0073] Paclitaxel 0.12%

[0074] Alpha-Tocopherol 8%

[0075] Medium Chain Fatty Acid Triglycerides (MCT) 4%

[0076] Soy Lecithin 0.6%

[0077] Tween-80 0.6%

[0078] F68 1.0%

[0079] Glycerin 2.5%

[0080] Sodium Cholesteryl Sulfate 0.06%

[0081] EDTA0.02%

[0082] Ethanol about 10%

[0083] Add water for injection to 100mL

[0084] Preparation method 1:

[0085] (1) Mix the prescribed amount of glycerin, sodium cholesteryl sulfate, EDTA, and F68 with water for injection preheated to 80°C, and stir until the ingredients are dissolved to obtain an aqueous phase;

[0086] (2) Add the prescription amount of Tween-80 to the prescription amount of α-tocopherol and MCT mixed oil, heat to 75°C, stir and mix to obtain the oil phase;

[0087] (3) Dissolve the prescribed amount of paclitaxel and soybean lecithin in an appropriate amount of ethanol under heating at 75°C, and stir until clear;

[0088] (4) Mix (2) and (3), heat at 80° C., and evapo...

Embodiment 2

[0094] Prescription 2:

[0095] Paclitaxel 0.06%

[0096] Alpha-Tocopherol 2%

[0097] Medium Chain Fatty Acid Triglycerides (MCT) 8%

[0098] Soy Lecithin 1.2%

[0099] Tween-80 0.2%

[0100] F68 0.2%

[0101] Glycerin 2.5%

[0102] EDTA0.02%

[0103] Ethanol about 10%

[0104] Add water for injection to 100mL

[0105] Preparation method 2:

[0106] (1) Mix the prescribed amount of glycerin, EDTA, and F68 with water for injection preheated to 80°C, and stir until the ingredients are dissolved to obtain an aqueous phase;

[0107] (2) Add the prescription amount of Tween-80 to the prescription amount of α-tocopherol and MCT mixed oil, heat to 75°C, stir and mix to obtain the oil phase;

[0108] (3) Dissolve the prescribed amount of paclitaxel and soybean lecithin in an appropriate amount of ethanol under heating at 75°C, and stir until clear;

[0109] (4) Mix (2) and (3), heat at 80° C., and evaporate ethanol under nitrogen flow to obtain a clear drug-containing oil ...

Embodiment 3

[0115] Prescription 3:

[0116] Paclitaxel 0.06%

[0117] Alpha-Tocopherol 0.1%

[0118] Medium Chain Fatty Acid Triglycerides (MCT) 12%

[0119] Soybean oil for injection (LCT) 3%

[0120] Soy Lecithin 3%

[0121] Oleic acid 0.03%

[0122] Tween-80 0.2%

[0123] F68 0.2%

[0124] Sodium Cholesteryl Sulfate 0.03%

[0125] Glycerin 2.5%

[0126] EDTA0.02%

[0127] Ethanol about 10%

[0128] Add water for injection to 100mL

[0129] Preparation method 3:

[0130] (1) Mix glycerin, EDTA, F68, sodium cholesteryl sulfate in the prescribed amount with water for injection preheated to 80°C, and stir until the ingredients are dissolved to obtain an aqueous phase;

[0131] (2) Add the prescription amount of oleic acid and Tween-80 to the prescription amount of α-tocopherol, MCT and LCT mixed oil, heat to 75°C, stir to mix evenly, and obtain the oil phase;

[0132] (3) Dissolve the prescribed amount of paclitaxel and soybean lecithin in an appropriate amount of ethanol unde...

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Abstract

The invention relates to a paclitaxel lipid microsphere injection and a manufacturing method thereof. In the invention, a paclitaxel lipid microsphere injection that does not contain polyoxyethylene castor oil is prepared. The medicine 90-98 per cent paclitaxel is coated in the oil phase and the oil-water interfacial film of the lipid microsphere. Thus the toxicity and stimulation of paclitaxel in clinic use are largely reduced, and the adverse reaction resulted from the excipient in the existing paclitaxel injection is prevented. With low stimulation, low toxicity and high efficiency, the preparation as a antineoplastic drug is administrated by intravenous injection.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a lipid microsphere injection containing paclitaxel and a preparation method thereof. technical background [0002] Paclitaxel is an anticancer drug extracted from the bark of the yew (Taxus chinensis), which is effective for advanced ovarian cancer, breast cancer, lung cancer, head and neck cancer, esophageal cancer, germ cell tumors, endometrial cancer, lymphoma , bladder cancer have a certain effect. Combined with other commonly used anti-tumor drugs, the curative effect can be further improved. Because paclitaxel has a unique mechanism of action for stabilizing cell microtubules, and has good therapeutic effects, strong broad-spectrum, and small side effects, it is internationally recognized as the preferred anticancer drug. But the water solubility of this medicine is extremely poor (the solubility in water is about 0.004g L -1 ), current clinical preparations, such as T...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/16A61K9/127A61K31/337A61K47/44A61K47/34A61P35/00A61K47/10A61K47/26
Inventor 李时海毕文生
Owner 李时海
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