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Hydroxycamptothecin (hydroxycampothecin, HCPT) is extracted from the Chinese Camptotheca acuminata antineoplastic agents, which selectively inhibits topoisomerase I and interfere with DNA replication efficiency and low toxicity, broad-spectrum anti-cancer characteristics, and no cross-resistance with other commonly used anticancer. Clinically for bladder cancer, colorectal cancer, liver cancer, stomach cancer, ovarian cancer, leukemia, and head and neck tumors, etc., are made good effect. The advantage lies mainly from bile excretion, small irritation of the urinary system, had no effect on the renal. Hydroxycamptothecin of the a-hydroxy inner alicyclic activity essential group, the clinical use of its lactone ring-opened sodium injection, the formulation is not only less effective, and can cause serious side effects, and therefore need improve clinically formulations. Liposomes as a novel pharmaceutical carrier, can improve the stability of the drug to be wrapped, and make drug targeting to a specific organization, activate the body's own immune function to reduce or lower the toxicity of drugs. Hydroxy camptothecin as a model drug, first be prepared as a liposome, effective to alter the stability of the drug, reached improve bioavailability hydroxycamptothecin. Further added lyoprotectant, lyophilization, in order to improve the storage stability of the liposomes. First, after the carrier and the screening process for the carrier with hydrogenated soybean lecithin (HSPC), using a thin film - the ultrasonic dispersion prepared Hydroxycamptothecin liposomes, and the liposome preparation process was optimized to encapsulate rate and the appearance of the trait of the indicators, and ultimately determine the following factors: hydroxycamptothecin HSPC molar ratio of the concentration of F68, phosphate buffer concentration. Take three levels of each factor, the choice of L9 (34) table hydroxycamptothecin liposome encapsulation rate indicators orthogonal test, and ultimately to determine the best prescription: hydroxycamptothecin: HSPC = 1:10 , F68 the concentration was 0.8%, phosphate buffer at a concentration of 0.05mol / L. Then, after the investigated formulations appearance, the dispersibility and stability as a standard, investigated several different lyophilized stent agent and different usage case, the protective effect of the formulation of lyophilized. Finally, the differential thermal analysis (DSC), infrared France (IR), X-ray diffraction method carried out to identify and check the quality of the hydroxycamptothecin-HSPC liposomes, the results show that the hydroxycamptothecin in the carrier to amorphous exist. Laboratory three batches of preparations in accordance with the Chinese Pharmacopoeia 2005 edition two appendices relevant requirements, quality evaluation methodology and stability studies, to develop quality standards, preclinical research foundation for of pharmaceuticals reporting and industrial production. Hydroxycamptothecin liposomes quality standards include character, identification, inspection, assay and stability test preparation for injection, in which content and related substances was determined by high performance liquid chromatography (HPLC), fumble after chromatographic conditions and method inspection of the school, to the precise and accurate determination of the content of the sample developed on this basis injection hydroxycamptothecin liposomes quality standards; quality inspection this standard, three batches of preparations, the indicators are in line with the requirements. Study on the stability of the preparation of the laboratory three batches include: impact factor test (high temperature, high humidity, light) accelerated testing and long-term test. The influencing factors test results show that the injection hydroxycamptothecin liposomes unstable under conditions of high temperature, high humidity should be at room temperature, dried save.
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