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Hydroxycamptothecin sustained-release microsphere and preparation method thereof

A technology of hydroxycamptothecin and slow-release microspheres, which is applied in the direction of microcapsules, pharmaceutical formulas, and medical preparations containing active ingredients, etc., can solve the problems of poor system reproducibility, low production efficiency, and wide distribution range, and achieve The effect of low cost, small dosage and simple preparation method

Inactive Publication Date: 2011-01-26
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional emulsification methods such as colloid mill, mechanical stirring, ultrasonic, etc. generally have disadvantages such as high energy consumption, low production efficiency, large particle size and wide distribution range, poor system reproducibility, etc., and most of the achievements are in the laboratory research stage

Method used

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  • Hydroxycamptothecin sustained-release microsphere and preparation method thereof
  • Hydroxycamptothecin sustained-release microsphere and preparation method thereof
  • Hydroxycamptothecin sustained-release microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: take by weighing 30mg of HCPT crude drug, polylactic acid (PLA) 300mg that molecular weight is 5000, put in the beaker with 30ml DMF and CH Cl mixed solution dissolves; With 5% polyvinyl alcohol (PVA) and 1% dodecyl Sodium sulfate (SDS) mixed aqueous solution was used as the continuous phase, and the drug-loaded particles were prepared through a membrane emulsifier; the obtained emulsion was centrifuged at 2000r / min, the precipitate was collected and freeze-dried to obtain the drug-loaded microspheres before modification; Microspheres. Add 10 ml of 0.5% N-succinyl chitosan in PBS solution during stirring, coat for 1 hour, collect the precipitate after centrifugation, wash with water for 3 times, place in a 40°C oven and vacuum-dry to obtain a powder preparation. figure 1 Provide the composition schematic diagram of the hydroxycamptothecin microsphere of the embodiment of the present invention, carrier 2 is polylactic acid (PLA), wraps anticancer drug hydro...

Embodiment 2

[0026] Embodiment 2: take by weighing 20mg of HCPT crude drug, polylactic acid (PLA) 400mg that molecular weight is 10000, put in beaker with 40ml DMF and CH 2 Cl 2 The mixed solution is dissolved; the mixed aqueous solution of 0.5% polyvinyl alcohol (PVA) and 0.5% sodium dodecyl sulfate (SDS) is used as the continuous phase, and the drug-loaded particles are prepared by a membrane emulsifier; the obtained emulsion is centrifuged at a speed of 1800r / min, Collect the precipitate and lyophilize to obtain the drug-loaded microspheres before modification; then weigh 50 mg of the drug-loaded microspheres. Add 10 ml of 0.5% N-succinyl-O-carboxymethyl chitosan in PBS solution during stirring, coat for 1 hour, collect the precipitate after centrifugation, wash with water for 3 times, and vacuum-dry in an oven at 45°C to obtain a powder preparation.

Embodiment 3

[0027] Embodiment 3: take by weighing 20mg of HCPT crude drug, polylactic acid (PLA) 300mg that molecular weight is 15000, put in beaker with 40ml DMF and CH 2 Cl 2 The mixed solution is dissolved; the mixed aqueous solution of 1% polyvinyl alcohol (PVA) and 0.5% sodium dodecyl sulfate (SDS) is used as the continuous phase, and the drug-loaded particles are prepared by a membrane emulsifier; the obtained emulsion is centrifuged at a speed of 2500r / min, Collect the precipitate and lyophilize to obtain the drug-loaded microspheres before modification; then weigh 30 mg of the drug-loaded microspheres. Add 20 ml of 0.2% N-lactose acylated succinyl chitosan in PBS solution during stirring, coat for 1 hour, collect the precipitate after centrifugation, wash with water for 3 times, place in a 50°C oven and vacuum-dry to obtain a powder preparation.

[0028] The drug in vitro cumulative release curve of embodiment 3 is shown in image 3 ,From image 3 It can be seen that the releas...

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Abstract

The invention discloses a hydroxycamptothecin slow-release microsphere and a preparation method thereof, relates to an anti-tumor pharmaceutical preparation and provides a hydroxycamptothecin slow-release microsphere and a preparation method thereof with long time of continuous drug release, stable drug release and high drug utilization; a carrier is polylactic acid, anti-cancer drug of hydroxycamptothecin is packed in the carrier and a modifying layer of water soluble derivative of chitosan is arranged on the surface of the carrier; the hydroxycamptothecin and the polylactic acid are dissolved in an organic solvent so as to obtain solution A; polyvinyl alcohol solution with the concentration of 0.5 percent to 5 percent is prepared and sodium dodecyl sulfate is added to prepare mixed solution B with the concentration of 0.5 percent to 1 percent; the solution A is transferred into a disperse phase container of a film emulsifier, the mixed solution B is added into a continuous phase container, a water suction pump is started to lead the continuous phase to be cycled, a mobile phase is collected, a certain pressure is maintained and a pressure indicating value which is operated to the film emulsifier is reduced to 0kPa. The collected mobile phase is centrifugated, precipitation is collected and freeze-dried to obtain the unmodified drug-carrying microsphere and then the surface modifying of the microsphere is carried out.

Description

technical field [0001] The invention relates to an antitumor drug preparation, in particular to a hydroxycamptothecin (hereinafter referred to as HCPT) sustained-release microspheres for postoperative recurrence of malignant solid tumors and a preparation method thereof. Background technique [0002] Hydroxycamptothecin (HCPT) has a broad anti-tumor spectrum and has no cross-resistance with commonly used anti-tumor drugs. Clinically, it is mainly used for the treatment of liver cancer, colorectal cancer, lung cancer and leukemia, but the drug has relatively serious side effects, mainly manifested as bone marrow suppression, leukopenia, gastrointestinal reactions and urinary tract irritation. HCPT is a topoisomerase I inhibitor, which can inhibit the enzymatic activity of topoisomerase I. It mainly acts on the DNA synthesis phase and has the effect on G 0 Phase cells have no effect on G 1 , G 2 Slightly lethal to M phase cells. HCPT is a water-insoluble and fat-insoluble ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/50A61K31/4745A61P35/00
Inventor 张其清侯振清韩晶王衍戈
Owner XIAMEN UNIV
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