Hydroxycamptothecin sustained-release microsphere and preparation method thereof

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 ...

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