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Broom-shaped hydroxycamptotecin-loaded sustained-release particle and preparation method thereof

A technology for carrying hydroxyl and camptothecin, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., and can solve the problems of increasing adverse reactions, easy decomposition, and reducing efficacy.

Active Publication Date: 2014-05-21
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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  • Broom-shaped hydroxycamptotecin-loaded sustained-release particle and preparation method thereof
  • Broom-shaped hydroxycamptotecin-loaded sustained-release particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] After co-dissolving 20mg of 10-HCPT and 20mg of MePEG-PLGA in 80mL of acetone, inject it into the dispersed phase inlet of the membrane emulsifier, and inject the aqueous solution containing 0.25% PVA into the continuous phase of the membrane emulsifier, using 1.1 μm SPG membrane as a template, in Under the pressure of 100KPa pure nitrogen, the dispersed phase solution quickly enters the continuous phase to obtain a MePEG-PLGA-HCPT suspension. After the above suspension is vacuum rotary evaporated to remove acetone, it is filtered with a 1 μm microporous membrane, and then the obtained suspension is The solution was vacuum freeze-dried in a freeze dryer for 24 hours to obtain MePEG-PLGA-HCPT powder with a drug loading of 38.3%. figure 1 The scanning electron micrographs of the nanoparticles prepared in Example 1 are given.

Embodiment 2

[0015] After co-dissolving 20mg of 10-HCPT and 20mg of MePEG-PLGA in 80mL of acetone, inject it into the dispersed 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 a template, in Under the pressure of 100KPa pure nitrogen, the dispersed phase solution quickly enters the continuous phase to obtain a MePEG-PLGA-HCPT suspension. After the above suspension is vacuum rotary evaporated to remove acetone, it is filtered with a 1 μm microporous membrane, and then the obtained suspension is The solution was vacuum freeze-dried in a freeze dryer for 24 hours to obtain MePEG-PLGA-HCPT powder with a drug loading of 32.7%.

Embodiment 3

[0017] After co-dissolving 20mg of 10-HCPT and 40mg of MePEG-PLGA in 80mL of acetone, inject it into the dispersed phase inlet of the membrane emulsifier, and inject ultrapure water containing 0.25% PVA into the continuous phase of the membrane emulsifier, using a 0.4μm SPG membrane as a template , under the pressure of 50KPa pure nitrogen, the dispersed phase solution quickly enters the continuous phase to obtain the MePEG-PLGA-HCPT suspension, the above suspension is vacuum rotary evaporated to remove acetone, filtered with a 1 μm microporous membrane, and the resulting mixture The suspension was vacuum freeze-dried in a freeze dryer for 24 hours to obtain MePEG-PLGA-HCPT powder with a drug loading of 21.4%.

[0018] Example 3

[0019] After co-dissolving 20mg10-HCPT and 40mg MePEG-PLGA in 80mL acetone, inject it into the dispersed 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, and in particular relates to preparing hydroxycamptothecin into "broom"-shaped nanoparticles and a preparation method thereof. Background technique [0002] Hydroxycamptothecin (HCPT, alias hydroxycamptothecin, 10-hydroxycamptothecin) is an indole alkaloid (i.e. camptothecin) isolated from the endemic Chinese Davidiaceae Eclipta plant Camptothecin Derivatives, which are pure natural anticancer drugs. It has a wide anticancer spectrum, has obvious inhibitory effect on the synthesis of nucleic acid, especially DNA, and has no cross-resistance with commonly used antitumor drugs. At present, it is mainly used clinically for the treatment of ascites-type liver cancer, colorectal cancer, gastric cancer, non-small cell lung cancer and leukemia. [0003] 10-Hydroxycamptothecin has relatively high toxic and side effects, mainly manifested as: bone marrow suppression, leukopenia, gastrointestinal reactions, urina...

Claims

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Application Information

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Patent Type & Authority Applications(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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