A reconstitutable teverelix-tfa composition
A technology of Tivereq and -TFA, applied in drug delivery, dry solid materials, active ingredients of anhydrides/acids/halides, etc., can solve problems such as increasing shelf life, increasing or decreasing the rate of deamidation, etc., to achieve The effect of long shelf life
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Embodiment 1
[0055] Example 1: Preparation of Tivereq-TFA Compositions with Different Molar Ratio
[0056] A custom batch (batch A) of Tiverelix with low TFA content was obtained. The properties of this batch A are shown in Table 1.
[0057] Table 1
[0058] purity 99.3％ Content of Tivereq 85.56% by weight TFA content 10.9% by weight Acetate content 0.3% by weight water content 4.3% by weight
[0059] If a composition containing 75 mg of Tivereq is desired (composition A), 88.28 mg of batch A must be used, calculated as follows:
[0060]
[0061] The molar ratio of Tivereq to TFA in Composition A can then be calculated.
[0062] The TFA content in 88.28mg batch A can be calculated as:
[0063] 88.28 mg x 10.9 / 100 (% content of TFA) = 9.62 mg.
[0064] Due to the molar mass of TFA (M TFA ) is 114g / mol, and the molar mass (M TEV ) is 1459 g / mol, it can be calculated that the molar concentration of TFA in the 75 mg Tivereq composition is 0....
Embodiment 2
[0075] Example 2: The relationship between the content and molar ratio of soluble and insoluble tiverelix
[0076] To determine the amount of soluble versus insoluble Tiverelix in the respective tubes, tubes No. 2 and No. 3 of each molar ratio were centrifuged at 10,000 rpm for 10 to 20 minutes and the supernatant was measured using HPLC analysis and the concentration of telvirec in the pellet.
[0077] Chromatographic conditions for HPLC analysis are shown in Table 4.
[0078] Table 4
[0079]
[0080] Two 100% standards were prepared by weighing 59.9 mg of Tivereq Acetate (Batch 080113) into a volumetric flask and making up the volume to 100 ml with water:acetonitrile 65:35 v / v. 10 ml of this solution was made up to 50 ml with the same solvent to provide a concentration of 0.1 mg / ml of telviracide.
[0081] A 1% standard solution was prepared by diluting 2 ml of the 100% standard to 200 ml with the same solvent to provide a concentration of 0.001 mg / ml ticavirectide. ...
Embodiment 3
[0091] Embodiment 3: the relation of plasma concentration and molar ratio
[0092] In order to assess the correlation of the molar ratio to the plasma concentration of tiverelix, five glass vials containing different molar ratios were prepared as described in Example 1 to provide aqueous Test tube of composition:
[0093] Table 7
[0094] test tube I II III IV V The molar ratio of 1:1.64 1:2.1 1:2.36 1:2.61 1:2.86
[0095] Five rats were tested for each molar ratio. Each rat was injected with 60 μl of the corresponding solution using a 25 mm 21 G luer 6% regular bevel needle (available from Terumo, Leuven, Belgium) and a 100 μl luer slide syringe (available from Hamilton, Reno, USA). Plasma concentrations were measured before administration and then at 1 hour, 6 hours, 24 hours, 48 hours, 7 days, 10 days, 14 days, 21 days and 28 days after administration.
[0096] The peak plasma concentrations (Cmax) of Tivereq after injection into each i...
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