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10-hydroxycamptothecine invisible nano-particle sustained release preparation and preparation method thereof

A technology of hydroxycamptothecin and sustained-release preparations, which is applied in the direction of pharmaceutical formulas, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc., which can solve problems such as increased disease sensitivity and MPS self-injury, and achieve Effects of reduced adsorption, high drug loading rate, and mild conditions

Inactive Publication Date: 2011-09-28
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the past, methods such as MPS inhibitors have been used to prevent nanoparticles from being quickly cleared by MPS, but such methods can easily lead to self-damage of MPS, inhibit the immune function of the host, and increase the body's sensitivity to diseases

Method used

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  • 10-hydroxycamptothecine invisible nano-particle sustained release preparation and preparation method thereof
  • 10-hydroxycamptothecine invisible nano-particle sustained release preparation and preparation method thereof
  • 10-hydroxycamptothecine invisible nano-particle sustained release preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Example 1: Preparation of 10-hydroxycamptothecin stealth nanoparticle sustained-release preparation: Weigh 40 mg of 10-hydroxycamptothecin bulk drug, polylactic acid grafted with polyethylene glycol monomethyl ether with a molecular weight of 10,000 Daltons (mPEG-PLA) 400mg, put it in a beaker and dissolve it with 10ml DMF (N,N-dimethylformamide); 1, 4, and 8 hours to replace the water phase in the bathtub to achieve complete dialysis; freeze-dry the resulting suspension to obtain 10-hydroxycamptothecin invisible nano drug-loaded microspheres, which are sterilized and subpackaged.

[0032] Utilize this method to prepare microsphere process to cause carrier material loss substantially; Simultaneously 10-hydroxycamptothecin itself is insoluble in water, and loss is little; From figure 1 The scanning electron microscope image shows that the particle size of the drug-loaded microspheres is round, the average particle size is 210nm, and the drug-loading capacity is 7.1%. f...

Embodiment 2

[0033] Example 2: Preparation of 10-Hydroxycamptothecin Stealth Nanoparticle Sustained Release Preparation: Weigh 40 mg of 10-Hydroxycamptothecin bulk drug, polylactic acid grafted with molecular weight 35000 Dalton polyethylene glycol monomethyl ether (mPEG-PLA) 400mg, put it in a beaker and dissolve it with 10ml DMF (N,N-dimethylformamide); 1, 4, and 8 hours to replace the water phase in the bathtub to achieve complete dialysis; freeze-dry the obtained suspension, sterilize and subpackage. The particle size of the drug-loaded microspheres is rounded ( Figure 4 ), the average particle size is 230nm, the drug loading capacity is 7.6%, and the average drug release time in vitro can reach more than 30 days.

Embodiment 3

[0034] Embodiment 3: Preparation of 10-hydroxycamptothecin invisible nanoparticle slow-release preparation: Weigh 40 mg of 10-hydroxycamptothecin bulk drug, and use molecular weight of 10000 Dalton polyethylene glycol monomethyl ether grafted poly( Lactic acid-glycolic acid) copolymer (mPEG-PLGA) 400mg, put in the beaker and dissolve with 10ml DMF (N, N-dimethylformamide); The above-mentioned solution is transferred to the dialysis bag of minimum permeability 8000 Dalton, Put it in a water bathtub, and replace the water phase in the bathtub every 1, 4, and 8 hours to complete the dialysis; freeze-dry the obtained suspension, and sterilize it for packaging. The particle size of the drug-loaded microspheres is rounded ( Figure 5 ), the average particle size is 224nm, the drug loading capacity is 7.3%, and the average drug release time in vitro can reach more than 30 days.

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Abstract

The invention provides a 10-hydroxycamptothecine invisible nano-particle sustained release preparation and a preparation method thereof, relating to a new preparation of medical antitumor medicaments. The invention provides the 10-hydroxycamptothecine invisible nano-particle sustained release preparation which has long sustained drug release time, stable drug release and high bioavailability, and the preparation method thereof. The 10-hydroxycamptothecine invisible nano-particle sustained release preparation is composed of 10-hydroxycamptothecine and a medical carrier, wherein the mass ratio of the 10-hydroxycamptothecine to the medical carrier is 1:(2-20). The preparation method comprises the steps of: dissolving the 10-hydroxycamptothecine and the medical carrier in the mass ratio of 1:(2-20) in an organic solvent to obtain a solution A; transferring the solution A into a dialysis bag to dialyze; and freeze drying the obtained suspension to obtain the 10-hydroxycamptothecine invisible nano-particle sustained release preparation.

Description

technical field [0001] The invention relates to a new pharmaceutical antitumor drug preparation, in particular to a 10-hydroxycamptothecin (hereinafter referred to as 10-hydroxycamptothecin) invisible nanoparticle slow-release preparation for preventing the growth and recurrence of malignant tumors and its preparation method. Background technique [0002] 10-Hydroxycamptothecin ((S)-4,9-dihydroxy-4-ethyl-1H-pyrano[3',4':6,7]indolizine[1,2b]quinoline-3, 14-(4H, 12H)-diketone) is a topoisomerase I inhibitor, which can inhibit the enzymatic activity of topoisomerase I and inhibit the participation of topoisomerase in DNA replication, repair, genetic recombination and transcription [1] . 10-Hydroxycamptothecin mainly acts on the DNA synthesis phase, on G 0 Phase cells have no effect on G 1 , G 2 , Has slight lethality to cells in M ​​phase. It has a broad anti-tumor spectrum and no cross-resistance with commonly used anti-tumor drugs. It is mainly used clinically for the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61P35/00A61K31/4745
Inventor 侯振清张其清常迪罗颖李乐蒋琦玮王衍戈
Owner XIAMEN UNIV
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