Pharmaceutical composition containing trifluridine and tipiracil hydrochloride, and application thereof
A composition and drug technology, applied in the field of pharmaceutical preparations, can solve problems such as degradation
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Embodiment 1
[0042] Embodiment 1 Compatibility experiment of raw materials and auxiliary materials
[0043] The API (API) composed of FTD and TPI was mixed with microcrystalline cellulose 102 (MCC 102) and lactose (200mg:40mg) respectively, and the API was mixed with pregelatinized starch and micropowdered silica gel (SiO 2 ), stearic acid, magnesium stearate (MS), glyceryl behenate, talcum powder, polyethylene glycol 8000 (PEG 8000) according to (75mg: 75mg), mixed at high temperature and high humidity (40±2℃ / 75%±5%RH), light (4500±500lx), high temperature (60°C), high humidity (25°C / 92.5%RH) for 28 days, and inspected on the 0th, 7th, 14th and 28th day The change of total impurity content is shown in Table 1.
[0044] Table 1
[0045]
[0046]
[0047] The above experimental results show that the API (API) composed of FTD and TPI has poor compatibility stability with the commonly used diluent MCC102, and has poor compatibility with the commonly used lubricant micropowder silica ...
Embodiment 2-3
[0049] Weigh an appropriate amount of FTD and TPI, mix them at a molar ratio of 2:1, and grind them to particle size D 90 ≤100 μm, a mixed API is obtained. Mix lactose monohydrate (purchased from German Meiji Leversberg Dairy Co., Ltd.) and pregelatinized starch (from Shanghai Colorcon Coating Technology Co., Ltd.) in equal increments, and then add stearic acid (purchased from BASF Shanghai Co., Ltd.) and glyceryl behenate (purchased from Jiafashi Trading Co., Ltd.), mixed according to the prescription ratio shown in Table 2, and compressed into tablets.
[0050] Get some of the tablets prepared in Examples 2 and 3, place them under 40°C ± 2°C / 75% ± 5%RH (open) conditions for 28 days respectively, and investigate the total impurity content in 7 days, 14 days and 28 days Changes. The test results are shown in Table 3.
[0051] Table 2
[0052]
[0053] table 3
[0054]
[0055] The above results show that plain tablets prepared with stearic acid or glyceryl behenate ...
Embodiment 4
[0057] The plain tablet of embodiment 2 and 3 is coated with the HPC-SSL solution of about 7% solid content and the Opadry solution of about 7% respectively (the HPC-SSL solution preparation of about 7% solid content: weigh hydroxypropyl Add 24 g of cellulose-SSL (HPC-SSL) (purchased from Nippon Soda Co., Ltd.), add 318.86 g of absolute ethanol, and stir magnetically for 2 hours to obtain HPC-SSL solution; Opadry solution with a solid content of about 7% is prepared by weighing 54g of 295F680027 (purchased from Shanghai Colorcon Coating Technology Co., Ltd.), 720g of purified water was added, magnetically stirred for 2h, filtered through a 120-mesh sieve, and the filtrate was taken to obtain Opadry solution), to obtain the coated tablet of Example 2 and Example 3 coated tablets.
[0058] Take some of the coated tablets of Example 2 and Example 3 prepared in Example 4, and place them under the conditions of 40°C ± 2°C / 75% ± 5% RH (open) for 17 days respectively to investigat...
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