| Glioma cells is the furthest familiar tumour of nerve centre system, and is also one refractory disease in neurosurgery, and TMZ is one of the most effective chemical remedy in curing glioma cells. TMZ is prone to decompose, its half life in body environment is 1.24 hours. As a alkyl antitumour medicine, TMZ's toxicity in causing abnormal, causing cancer, and causing mutation is higher. Via changing the medicine preparation form, to prolong medicine's effective time, to play down medicine dosage in order to increase security, it has realistic significance. This paper did some research in the preparation technics using polylactic Acid to prepare microcapsule to carry medicine, medicine in microcapsule releasing capability and cell toxicity.We used polylactic acid as the microcapsule wall's material, liquid paraffin is oil phase, DMF is water phase, using the simple water-in-oil (W/O) emulsion solvent evaporation method to prepare Temozolomide Polylactic Acid Microcapsule. Research indicate :(1) The effect on microcapsule of experimental equipment, affirm reactive condition is: size of agitate oar to container inner is 0.75:1, the distance of agitate oar to the container bottom to the height of liquid is 1:3.(2) Preparation temperature, agitating rate, concentration of polylactic acid, emulsifier concentration, ratio of oil phase and water phase, agitating volatilizing time, medicine quantity have do some effect to microcapsule's shape, grain diameter and grain diameter distributing, enveloped ratio, harvest ratio, quantity of medicine carrying.(3) Optimize experiment receive the furthest fit technics parameters: preparation temperature is 40℃, rotate speed is 1200r/min, emulsifier concentration is 2.0g/100ml, ratio of TMZ/PLA is 1/15, volume ratio of water phase to oil phase is 10/100, agitating volatilizing time is 12h. preparing temperature 40℃. Microcapsule harvest ratio is 89.1%, enveloped ratio is 86.2%, quantity of medicine carrying is 86.5mg/g, average diameter of microcapsule is100.8μm, 50% microcapsule distributing range from 83.2to 118.4μm.(4) According as TMZ's character, basing measuring method in pharmacopoeia, improve the method of measuring released medicine.(5) Using the improved method to measure self-making microcapsule, taking orally microcapsule preparation, TMZ's releasing amortized solution, indicate that they have obviously difference each other, self-making microcapsule's releasing time is 66h, and that the selling TMZ's taking orally preparation is only 9h.(6) Measuring self-making microcapsule in PBS-HCl buffers (pH =3.0) system is different from its in rabbit's brain organizing system. Under the environment of Rabbit's brain , making the microcapsule by myself will have very good result to the preparation slowly.self-making microcapsule releasing time reach 32h in rabbit's brain organize environment, selling TMZ oral capsule release time as 20hr in rabbit(7) The toxic experiment of the big glue tumour cell of mouse's brain of C6...
|
PDF Full Text Request