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Nanometer microsphere of temozolomide polylactic acid and its preparation and preparing method therefor

A technology of temozolomide polylactic acid and nano-microspheres, which is applied in the directions of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems that have not yet been reported in the literature on the preparation method of temozolomide lactic acid, and achieve Effect of Good Sustained Release Properties

Inactive Publication Date: 2007-07-18
南京伍盛纳米科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, polylactic acid has been widely used as a drug carrier to make carrier drug preparations such as various microspheres, nanospheres, microcapsules, nanocapsules, and rod-shaped implants, but there is no preparation method for temozolomide lactic acid nanospheres and its preparations. literature reports

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) 50 mg of polylactic acid with relative molecular weight of 10000, 40000, 60000, 100000, 150000 and 200000 and 6 parts of 20 mg of temozolomide were respectively dissolved in 20 ml of dichloromethane as the oil phase; (2) 2 parts of 50 mg of Poloxamer 188, 2 parts of 200 mg of hydroxypropyl methylcellulose, and 2 parts of 500 mg of polyvinyl alcohol were respectively dissolved in 200 ml of deionized water as the water phase; (3) under 400W ultrasonic conditions, six The oil phases of polylactic acids with different molecular weights were slowly injected into the aqueous phase of six surfactants in sequence, and then magnetically stirred for 8 hours under the condition of 1000r / min to obtain six temozolomide polylactic acid nanospheres of polylactic acids with different molecular weights. Emulsion dispersion system; (4) The temozolomide polylactic acid nanosphere emulsion dispersion system of six polylactic acids with different molecular weights was centrifuged and was...

Embodiment 2

[0030] (1) 10, 25, 50, 70 mg of temozolomide and 4 parts of 50 mg of polylactic acid were dissolved in 20 ml of chloroform as the oil phase; (2) 30, 60, 100, 180 mg of poloxamer 188 were dissolved in 4 parts of 100ml of deionized water were used as the water phase; (3) 4 different oil phases were slowly injected into 4 different concentrations of poloxamer 188 water phases with a syringe in turn, and ultrasonically emulsified under the condition of 600W in an ice-water bath 1, 5, 5, and 10 minutes, and then magnetically stirred for 6 hours under the condition of 2000r / min to obtain four temozolomide polylactic acid nanosphere emulsion dispersion systems; (4) disperse the four temozolomide polylactic acid nanosphere emulsions The system was separated by centrifugation and washed with sterilized water for injection to prepare four kinds of temozolomide polylactic acid drug-loaded nanospheres with drug loadings of 4.6%, 13.6%, 27%, and 32% respectively; (5) washing with deionized ...

Embodiment 3

[0032] (1) Dissolve 50 mg of temozolomide and 50 mg of polylactic acid in 20 ml of toluene as the oil phase; (2) dissolve 20 mg of Poloxamer 188 in 400 ml of deionized water as the water phase; (3) separate the oil phases with syringes Slowly inject the water phase, ultrasonically emulsify under the condition of 200W in the ice-water bath, and then magnetically stir under the condition of 400r / min for 10 hours to obtain the temozolomide polylactic acid nanosphere emulsion dispersion system; (4) the temozolomide polylactic acid nanosphere The emulsion dispersion system was subjected to centrifugal ultrafiltration at 20000r / min, and washed with deionized water to obtain temozolomide polylactic acid drug-loaded nanospheres; Lactic acid nanosphere freeze-dried powder is made of temozolomide polylactic acid nanosphere dry powder and sterile water for injection, relying on the excipient performance of polylactic acid microsphere itself, through temozolomide polylactic acid nanosphere...

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Abstract

A nanoball of temozolomide-sodium polylactate is proportionally prepared from temozolomide and sodium polylactate. Its product may be injection, freeze-dried powder injection, slow-release micropills, tablets, or membrane for treating cancer, especially the cerebral glioma. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to temozolomide biodegradable polymer nano-microspheres, preparations and preparation methods thereof, in particular to temozolomide polylactic acid nano-microspheres, preparations and preparation methods thereof. Background technique [0002] Temozolomide is a fat-soluble, water-insoluble broad-spectrum antineoplastic drug. It is currently the best single-drug chemotherapy drug for glioma. Its appearance is considered to be a major breakthrough in anti-brain tumor chemotherapy drugs in the past 40 years. At present, the dosage form of temozolomide is mainly oral capsules. After oral administration, temozolomide is widely distributed in the whole body after entering the body. It can pass through the blood-brain barrier. The half-life is about 1.3 hours, and there is no obvious first-pass effect. Malignant tumors such as glioma, degenerative astrocytoma, malignant melanoma, leukemia and lymphoma. Due to the rapid oral absorption a...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/4188A61K47/34A61P35/00
Inventor 朱宏朱明星张雪松王玉英
Owner 南京伍盛纳米科技有限公司
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