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A broom-shaped hydroxycamptothecin-loaded sustained-release particle and its preparation method

A hydroxycamptothecin and hydroxyl-carrying technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of increasing adverse reactions, reducing curative effect, and easy decomposition

Active Publication Date: 2015-12-30
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, because HCPT sodium salt injection is unstable, it is easy to decompose when exposed to light, which may reduce the curative effect and increase adverse reactions

Method used

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  • A broom-shaped hydroxycamptothecin-loaded sustained-release particle and its preparation method
  • A broom-shaped hydroxycamptothecin-loaded sustained-release particle and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] After co-dissolving 20mg10-HCPT and 20mgMePEG-PLGA in 80mL of acetone, inject it into the disperse phase feed port of the membrane emulsifier, and inject the aqueous solution containing 0.25% PVA into the continuous phase of the membrane emulsifier, using a 1.1μm SPG membrane as a template, at 100KPa Under the pressure of pure nitrogen, the dispersed phase solution quickly entered the continuous phase to obtain a MePEG-PLGA-HCPT suspension. After the above suspension was vacuum rotary evaporated to remove acetone, it was filtered with a 1 μm microporous membrane, and then the obtained suspension was filtered. Placed in a freeze dryer for 24 hours of vacuum freeze drying to obtain MePEG-PLGA-HCPT powder with a drug loading of 38.3%, figure 1 The scanning electron microscope image of the nanoparticles prepared in Example 1 is given.

Embodiment 2

[0015] After co-dissolving 20mg10-HCPT and 20mgMePEG-PLGA in 80mL acetone, inject it into the disperse phase feed port of the membrane emulsifier, and inject the aqueous solution containing 0.25% PVA into the continuous phase of the membrane emulsifier, using 0.6μm SPG membrane as template, at 100KPa Under the pressure of pure nitrogen, the dispersed phase solution quickly entered the continuous phase to obtain a MePEG-PLGA-HCPT suspension. After the above suspension was vacuum rotary evaporated to remove acetone, it was filtered with a 1 μm microporous membrane, and then the obtained suspension was filtered. The MePEG-PLGA-HCPT powder was obtained by vacuum freeze-drying in a freeze dryer for 24 hours, and its drug loading was 32.7%.

Embodiment 3

[0017] After co-dissolving 20mg10-HCPT and 40mgMePEG-PLGA in 80mL acetone, inject it into the disperse phase feed port of the membrane emulsifier, and inject ultrapure water containing 0.25% PVA into the continuous phase of the membrane emulsifier, using 0.4μm SPG membrane as template, Under the pressure of 50KPa pure nitrogen, the disperse phase solution was rapidly entered into the continuous phase to obtain a MePEG-PLGA-HCPT suspension. The above suspension was vacuum rotary evaporated to remove acetone, filtered with a 1 μm microporous membrane, and then the obtained suspension was The liquid was placed in a freeze dryer for 24 hours under vacuum to obtain MePEG-PLGA-HCPT powder with a drug loading of 21.4%.

[0018] Example 3

[0019] After co-dissolving 20mg10-HCPT and 40mgMePEG-PLGA in 80mL acetone, inject it into the disperse phase feed port of the membrane emulsifier, and inject the aqueous solution containing 0.25% PVA into the continuous phase of the membrane emulsi...

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Abstract

The invention discloses a broom-shaped hydroxycamptotecin-loaded sustained-release particle and a preparation method thereof. The preparation method comprises the following steps: dissolving hydroxycamptothecine (10-HCPT) and methoxyl-terminated polyethylene glycol- poly(dl-lactide-co-glycolide) (MePEG-PLGA) in an organic solvent, injecting into a disperse phase of a membrane emulsifier, and injecting an aqueous solution containing little polyvinyl acetate (PVA) into a continuous phase of the membrane emulsifier; leading the solution of the disperse phase to quickly enter the continuous phase at nitrogen pressure by adopting a porous glass membrane as a template to obtain suspension of the hydroxycamptotecin-loaded sustained release particle (MePEG-PLGA-HCPT); distilling the suspension in vacuum, removing the organic solvent, removing uncoated square medicinal crystal by ultrafiltration of a microporous filter membrane, and lyophilizing the suspension in vacuum in a lyophilizer for 24 hours to obtain the broom-shaped MePEG-PLGA-HCPT sustained-release particle. The method is reliable, and convenient to operate; the prepared irregular particle is high in drug-loading amount and encapsulation rate, is excellent in sustained release effect, and is particularly suitable for tumor local medication and tumor post-operation medication.

Description

technical field [0001] The invention belongs to the field of pharmacy, in particular to the preparation of hydroxycamptothecin into "broom"-shaped nanoparticles and a preparation method thereof. Background technique [0002] Hydroxycamptothecin (HCPT, also known as hydroxycamptothecin, 10-hydroxycamptothecin) is an indole alkaloid (ie, camptothecin) isolated from China's endemic dovetaceae plant, Camptotheca Derivatives are pure natural anticancer drugs. It has a broad anti-cancer spectrum, has a significant inhibitory effect on the synthesis of nucleic acids, especially DNA, and has no cross-resistance with commonly used anti-tumor drugs. At present, it is mainly used for the treatment of ascites-type liver cancer, colorectal cancer, gastric cancer, non-small cell lung cancer and leukemia. [0003] The toxic and side effects of 10-hydroxycamptothecin are relatively large, mainly manifested as: bone marrow suppression, causing leukopenia, gastrointestinal reactions, urinar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4745A61K47/34A61P35/00
Inventor 侯振清杨向瑞侯鲁贾梦梦江倩
Owner XIAMEN UNIV
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