Poorly soluble antineoplastic drug micelle preparation and preparation method thereof

An anti-tumor drug, insoluble technology, applied in the field of medicine, can solve the problems of low bioavailability, many adverse reactions, strong pain, etc., to improve the therapeutic effect, improve water solubility, and reduce drug side effects

Inactive Publication Date: 2015-08-26
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Antineoplastic drugs usually have poor water solubility. When they are made into preparations, especially injections, a large amount of organic solvents need to be added to help dissolve them. When used, they will cause intense pain, many adverse reactions, redness, swelling, erythema, allergies, itching, etc., or , made into a suspoemulsion, its preparation has poor quality stability and low bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of embodiment 1 methoxypolyethylene glycol 2000-polylactide (53 / 47) block copolymer

[0039] (1) Polymerization reaction: under the protection of dry high-purity nitrogen, weigh 2kg methoxypolyethylene glycol 2000 and 2kg D, L-lactide in a fully dry polymerization reactor, add 8.33g stannous octoate, Heat to 70°C to dissolve methoxypolyethylene glycol 2000, and carry out polymerization reaction in an oil bath at 130°C for about 10 hours under vacuum conditions.

[0040] (2) Dissolving: after the polymerization reaction finishes, add 16kg methylene chloride to the solid obtained in the reactor to dissolve.

[0041] (3) Mixed precipitation: the above solution was added to a container containing 160 kg of isopropyl ether (pre-cooled at -20° C.), and the target product precipitated.

[0042] (4) Filtration (discard the solution phase): open the valve on the isopropyl ether container to pump the above mixed precipitate into the filter through an evacuation pum...

Embodiment 2

[0048] The preparation of embodiment 2 vincristine micellar injection

[0049] (1) Dissolution: According to the formulation ratio, accurately weigh 0.01kg of vincristine raw material drug and 0.1kg of methoxypolyethylene glycol 2000-polylactide (53 / 47) diblock copolymer in the liquid preparation tank Add about 1kg of acetonitrile, control the temperature at 60-80°C, start stirring, so that vincristine and copolymer auxiliary materials are fully dissolved in acetonitrile, and a clear solution is obtained in about 30 minutes.

[0050] (2) Evaporate solvent: heat to boiling, acetonitrile is evaporated to obtain transparent gel-like vincristine and copolymer auxiliary material mixed drug film.

[0051] (3) Dissolving: Add 30 L of 5 mM phosphate buffer solution prepared with water for injection into the liquid preparation tank to fully dissolve the gel-like drug film to obtain vincristine micellar solution.

[0052] (4) Charcoal adsorption: Add 9g of activated carbon, stir and ad...

Embodiment 3

[0059] The preparation of embodiment 3 doxorubicin micellar injection

[0060] (1) Dissolution: According to the formulation ratio, accurately weigh 0.2kg of doxorubicin bulk drug and 2.0kg of methoxypolyethylene glycol 2000-polylactide (53 / 47) diblock copolymer in the dosing solution Add about 20kg of ethanol to the tank, control the temperature at 60-80°C, and start stirring to fully dissolve the doxorubicin and copolymer excipients in the ethanol, and obtain a clear solution in about 30 minutes.

[0061] (2) Evaporating the solvent: heating to boiling, and evaporating ethanol to obtain a transparent gel-like mixed drug film of doxorubicin and copolymer auxiliary materials.

[0062] (3) Dissolving: Add 30 L of 5 mM phosphate buffer solution prepared with water for injection into the liquid preparation tank to fully dissolve the gel-like drug film to obtain a doxorubicin micelle solution.

[0063] (4) Charcoal adsorption: Add 9g of activated carbon, stir and adsorb for 15min...

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Abstract

The invention provides a copolymer drug-loaded micelle preparation which comprises a poorly soluble antineoplastic drug and a copolymer carrier material. A poorly soluble antineoplastic drug micelle injection is prepared through using methoxy polyethylene glycol 2000-polylactide (53 / 47) diblock copolymer as a carrier material, embedding the poorly soluble antineoplastic drug in micelle, and performing spray drying or freeze drying. According to the invention, the poorly soluble antineoplastic drug micelle preparation not only greatly increases the solubility of poorly soluble antineoplastic drug and improves efficacy, but also prolongs the circulation time of drug in the body, improves the drug activity, reduces the burst effect and increases the bioavailability.

Description

technical field [0001] The invention relates to a micelle preparation and a preparation method thereof, in particular to a micelle preparation of an insoluble antitumor drug and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Nearly 50 years of research and development of anti-tumor drugs have made considerable progress in cancer chemotherapy, especially prolonging the survival time of patients with hematological malignancies, but the treatment of solid tumors, which seriously threaten human life and health and account for more than 90% of malignant tumors, has not yet been developed. Even if a satisfactory curative effect is achieved, half of the cancer patients still have no response or drug resistance to treatment, which eventually leads to treatment failure. Therefore, discovering and developing new antitumor drugs is still a very arduous and long-term mission and challenge that pharmacists must face. With the ra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K45/06A61K31/475A61K31/704A61K33/24A61K31/7048A61K31/4745A61P35/00
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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