Long-circulation nano-grain of hydroxycamptothecin and method for preparing the same

A technology of hydroxycamptothecin and long circulation, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Large, low stability and other problems, to achieve the effect of prolonging the residence time, prolonging the residence time and long residence time

Inactive Publication Date: 2010-10-13
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is a big defect in the application of hydroxycamptothecin nanoparticles: its stability is not high in the solution phase, and the drug hydroxycamptothecin is easy to precipitate
However, after freeze-drying, the encapsulation efficiency is too low and the particle size of nanoparticles becomes larger.

Method used

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  • Long-circulation nano-grain of hydroxycamptothecin and method for preparing the same
  • Long-circulation nano-grain of hydroxycamptothecin and method for preparing the same
  • Long-circulation nano-grain of hydroxycamptothecin and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～6

[0034] Embodiment 1~6 hydroxycamptothecin long circulation nanoparticles

[0035] Table 1 shows Examples 1-6 of hydroxycamptothecin long-cycle nanoparticles.

[0036] Table 1 Hydroxycamptothecin Long Circulation Nanoparticles Examples 1-6

[0037]

[0038]

preparation Embodiment 1

[0040] 10mg of hydroxycamptothecin and 150mg of PLGA were dissolved in 75ml of ethyl acetate, added to 100ml of an aqueous solution containing 5g of poloxamer 188 and 1.5g of PEG400, the pH value was 4.5, at room temperature, with a fluko shear Shear at 8,000 rpm for 10 minutes to make an emulsion, then remove ethyl acetate by rotary evaporation at 40°C, and stir at room temperature for 1 hour to obtain hydroxycamptothecin long-cycle nanoparticles with an average particle size of 50nm.

preparation Embodiment 2

[0042] Dissolve 10mg hydroxycamptothecin and 200mg PLGA in 80ml petroleum ether, add to 100ml aqueous solution containing 1g polysorbate 80 and 3g poloxamer 188, the pH value is 7.2, at room temperature, use a fluko shear Shear at 10,000 rpm for 8 minutes to make an emulsion, remove petroleum ether by rotary evaporation at 60°C, and stir at room temperature for 1 hour to obtain hydroxycamptothecin long-circulation nanoparticles with an average particle size of 30nm.

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Abstract

The invention discloses novel long-circulating nanoparticles of hydroxycamptothecine, which comprises raw material components of hydroxycamptothecine, polymer of glycolide and gactide (PLGA), a surfactant and a film modified material, and the structure is that the hydroxycamptothecine is sealed in the polymer of glycolide and gactide (PLGA) and is further covered the surfactant and the film modified material on the surface. The invention further discloses a preparation method thereof. The long-circulating nanoparticles of hydroxycamptothecine of the invention have low toxicity, high stabilityin solutions, long detention time in vivo, small particle diameter, and no obvious change after being lyophilized. The preparation method of the invention can be processed under the condition of stable hydroxycamptothecine to avoid the reduction of the drug effect, which has the advantages of simple steps, good repeatability and easy application in industrialized manufacture.

Description

technical field [0001] The invention relates to a nanoparticle and a preparation method thereof, in particular to a hydroxycamptothecin nanoparticle and a preparation method thereof. Background technique [0002] Hydroxycamptothecin is the 10-hydroxyl derivative of camptothecin, which belongs to the same class of cytotoxic anticancer drugs as camptothecin. Recently, it has been found that it can selectively inhibit DNA topoisomerase I. While killing cancer cells, it also affects normal cell metabolism. The drug is insoluble in water and has certain toxicity, which limits its clinical application. Therefore, improving the performance of hydroxycamptothecin has become one of the current hot spots. [0003] Patent application document CN 1875946A discloses a solid nanoparticle of 10-hydroxycamptothecin and its preparation method. The nanoparticle comprises 10-hydroxycamptothecin, carrier, stabilizer and water, wherein the carrier is fatty acid poloxamer cholesteryl ester and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4745A61P35/00A61K9/14A61K47/34A61K47/10A61K47/26
Inventor 奉建芳张乐乐陈满仓祝林邹凌燕
Owner SHANGHAI INST OF PHARMA IND CO LTD
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