Anti-cancer pellet and colonic targeting agent
A technology of colon targeting and micropills, which is applied in the direction of antineoplastic drugs, pharmaceutical formulations, bulk delivery, etc. It can solve the problems of low level of preparations, obvious adverse reactions, poor quality controllability, and poor stability, so as to improve compliance , Improve anti-tumor activity, improve the effect of drug activity
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Embodiment 1
[0034] The preparation of embodiment 1 micropill of the present invention
[0035] (1) Raw material formula
[0036] Emodin: Sophoridine: Matrine=1:20:25;
[0037] (2) Take a total of 50g of the above formula raw materials and 50g of microcrystalline cellulose passed through a 100-mesh sieve, mix well, moisten with 50% ethanol in an appropriate amount, prepare a soft material, pass through a 20-mesh sieve, and put it in a centrifugal coating granulator, At 30°C, the rotating speed is 35 rev / min, the wind speed is 8cfm, the pellets are rounded for 4 minutes, taken out and dried at 50°C to obtain the pellets of the present invention.
Embodiment 2
[0038] Embodiment 2 Preparation of colon targeting agent of the present invention
[0039](1) Take 10g of EudragitⅢ, add about 100ml of ethanol, soak and swell for 12 hours, stir to fully disperse and dissolve evenly. Dissolve 2g of diethyl phthalate in 100ml of ethanol, then add 1g of micropowdered silica gel, and homogenize at high speed for 20 minutes. Add the suspension of plasticizer and micropowder silica gel into the Eudragit III solution, stir to disperse evenly, and obtain the coating liquid, and keep stirring during the coating process.
[0040] (2) Take the pellets prepared in Example 1, put them in a centrifugal coating granulator, adjust the parameters as wind speed 8cfm, speed 35 rpm, wind temperature 30°C, peristaltic pump 1-2, spray pressure 0.25MPa Spray the above-mentioned coating solution for coating to increase the weight of the pellets by 30%.
Embodiment 3
[0041] Embodiment 3 Micropill preparation technology research of the present invention
[0042] According to the properties and dosage of the material, it is planned to use a centrifugal coating granulator to prepare vegetarian pills first, and then coat a layer of colon-targeting coating to prepare the colon-targeting pellets of the present invention.
[0043] In the early stage, the starch blank pellet core was used as the mother core, and the method of spraying wetting agent and powder to increase the layer size and spheroidization was investigated. The results found that the following problems existed: ①The drug powder was very viscous, and it was easy to stick to the pills during the process of adding powder and spheronizing, and a large amount of excipients needed to be added, resulting in a large amount of finished product, which was difficult to meet the needs of preparing capsules; ②The combination of powder and wetting agent Proportion coordination control is difficu...
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