Talazoparib-containing medicinal composition and application thereof
A composition and drug technology, which is applied in the PARP enzyme inhibitor Talazoparib pharmaceutical composition, in the field of cancer treatment, can solve the problems of high blood drug concentration fluctuation range, dose boosting blood drug concentration, and no patent of public preparations, etc., to avoid adverse effects Response, control of blood concentration level and fluctuation range, and effect of reducing toxicity
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preparation example Construction
[0042] The preparation method of the multivesicular liposome of the present invention adopts conventional methods in the art, such as adopting the double emulsion method, specifically, it needs to include the following 5 steps: (1) first dissolve the lipid component of the prescription amount in easy Volatile organic solvents (usually chloroform or a mixture of chloroform and ether) form an oil phase, and the talazoparib of the prescribed amount is dissolved in water to form a drug-containing aqueous solution (the first water phase), and then with a suitable oil-water volume ratio (volume ratio) 1:10-12:10, v / v) Mix the drug-containing aqueous solution (the first water phase) with the organic phase of the lipid (oil phase), and prepare a uniform mixture at room temperature by ultrasonic or mechanical shearing for a certain period of time. Water-in-oil (W / O) type colostrum; (2) absorb the formed W / O type colostrum, and inject the second aqueous phase buffer solution according to...
Embodiment 1
[0075] The preparation of embodiment 1 talazoparib gel preparation in situ
[0076]
[0077] After dissolving PLA with N-methylpyrrolidone, and then dissolving the drug talazoparib, the in situ gel injection can be obtained.
[0078] The quick-release capsule of comparative example 1 (self-made gelatin quick-release capsule, 25wt% talazoparib tosylate, 33wt% microcrystalline cellulose, 22wt% lactose, 15% mannitol 2wt% micropowder silica gel, 1wt% magnesium stearate After mixing evenly with 2% sodium lauryl sulfate, directly pack into 0# hard capsule and make); Its dissolution measurement adopts the first method device of the dissolution measurement method (Chinese Pharmacopoeia 2010 edition two appendix X C), 37 Under the condition of ℃, use 900mL of hydrochloric acid aqueous solution with pH 1.2 as the release medium, the rotation speed is 75 rpm, operate according to the law, take 6mL of the solution according to the predetermined time point, centrifuge, take the supernat...
Embodiment 2
[0083] Embodiment 2: Preparation of talazoparib microspheres
[0084]
[0085] Dissolve Talazoparib and PLGA in dichloromethane, and inject it into BUCHI B-290 spray-drying static electricity with a drying temperature of 65°C, a spray frequency of 120kHz, and a ventilation rate of 70L / min at an injection rate of 0.2ml / min of 0.5ml / min. Collect the system to prepare microspheres with uniform particle size, and 80% of the microspheres have a particle size of 0.5-10um.
[0086] The release test of the talazoparib microsphere of test embodiment 2 embodiment 2
[0087] The talazoparib microspheres of Example 2 were incubated in a release medium containing 0.2% Tween 80 in a physiological isotonic PBS solution (pH 7.4), at 37° C., under the condition of 100 r / min, at a predetermined time point, 5 ml of the dissolution medium was taken, After centrifugation at 10,000 rpm for 5 minutes, 20 μl of filtrate from the supernatant was accurately measured and injected into a liquid chrom...
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