Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof

A technology of hydroxycamptothecin and heat-sensitive liposomes, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of large side effects and low solubility, and achieve improved therapeutic index, Increase lipophilic effect

Inactive Publication Date: 2012-09-19
SUZHOU FAMO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problem of low solubility and large side effects of 7-ethyl-10-hydroxycamptothecin in most biocompatible and pharmaceutically acceptable solvents, and has prepared a long-circulation thermosensitive lipid body

Method used

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  • Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof
  • Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof
  • Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] prescription:

[0022]

[0023] Preparation Process:

[0024] Take the prescribed amount of 7-ethyl-10-hydroxycamptothecin, soybean lecithin, distearoylphosphatidylglycerol, distearylethanolamine-polyethylene glycol 2000 copolymer, cholesterol, α-tocopherol dissolved in Water ethanol, then add a small amount of PBS solution containing octadecylamine, spin the film at 40-45 ° C, hydrate with 10 mL of pH 5.0 PBS containing 3% lactose, ultrasonicate in a water bath, and cycle through the nanomachine for 6 times, with a pore size of 0.22 μm microporous filter membrane, and then divided into vials, pre-frozen at -18°C for 24 hours, transferred to a freeze dryer for freeze-drying, and obtained.

Embodiment 2

[0026] prescription:

[0027]

[0028] Preparation Process:

[0029] Take the prescribed amount of 7-ethyl-10-hydroxycamptothecin, egg yolk lecithin, distearoylphosphatidylglycerol, distearylethanolamine-polyethylene glycol 2000 copolymer, cholesterol, α-tocopherol and place in eggplant In a shaped bottle, add an appropriate amount of mixed solution of chloroform and methanol (3:1) to dissolve, then add a small amount of PBS solution containing octadecylamine, remove the organic solvent under reduced pressure in a water bath in a rotary evaporator, add an appropriate amount of PBS (pH7. 4) - Lactose solution, 50°C, hydration with rotation for 30 minutes, degassed under reduced pressure, placed in a high-pressure homogenizer, passed through polycarbonate membranes of 200 nm, 100 nm, and 80 nm in sequence, and freeze-dried to obtain the product.

Embodiment 3

[0031] prescription:

[0032]

[0033]

[0034] Preparation Process:

[0035] Dissolve the prescription amount of 7-ethyl-10-hydroxycamptothecin, soybean lecithin for injection, vitamin E, cholesterol, dipalmitoylphosphatidylcholine in chloroform: methanol (2: 1) and pour into a pear-shaped bottle, Then add a small amount of buffer solution containing octadecylamine, and evaporate the organic solvent to dryness in a water bath at 60°C to form a dry film on the wall of the glass bottle. Rotate hydration in a shaped bottle at 40 rpm at room temperature until the dry film on the wall of the bottle is completely eluted, and hydrate the resulting coarse suspension at room temperature for 1 hour. The resulting coarse suspension was passed through a 0.8 μm microporous membrane for 1 time, a 0.45 μm microporous membrane for 3 times, a 0.22 μm microporous membrane for 3 times, and a 0.1 μm microporous membrane for 3 times to obtain the final suspension. bottle, sealed with nitr...

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Abstract

The invention belongs to the technical field of medicine, and relates to a lyophilized powder for injection of a long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and a preparation method thereof. The lyophilized powder for injection comprises 1%-30% of 7-ethyl-10-hydroxycamptothecin, 10%-90% of phosphatide, 0%-10% of octadecylamine, 0%-70% of a lyophilizing protective agent, 0%-50% of accessory G, 0.001%-50% of an antioxidant, 0%-30% of cholesterol, 0%-50% of thermal sensitive accessory H, and a balanced amount of a buffer solution. The long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin has improved water-solubility and stability, and has reduced toxicity.

Description

technical field [0001] The technical field of the invention relates to the design and preparation of new dosage forms of antineoplastic drugs, and provides a 7-ethyl-10-hydroxycamptothecin long-circulation thermosensitive liposome and a preparation method. Background technique [0002] 7-Ethyl-10-hydroxycamptothecin is an active metabolite of irinotecan and belongs to the class of topoisomerase I inhibitors. Irinotecan is a product of Pfizer (Pfizer), and its trade name is Camptosar. In 2000, the FDA approved it as a first-line treatment drug for advanced colon cancer. The in vitro cytotoxicity test showed that for some tumor cell lines, the antitumor activity of 7-ethyl-10-hydroxycamptothecin was more than 1000 times that of irinotecan. Although 7-ethyl-10-hydroxycamptothecin has strong antitumor activity, it is insoluble in most biocompatible and pharmaceutically acceptable solvents, which limits its development. [0003] Liposome refers to a closed vesicle composed of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4745A61K47/28A61K47/34A61K47/36A61P35/00
Inventor 吴小明
Owner SUZHOU FAMO BIOLOGICAL TECH
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