Tranexamic acid fatty alcohol ester and application of gel preparation of tranexamic acid fatty alcohol ester in sclerotherapy
A technology of tranexamic acid and fatty alcohol esters, which is applied in the field of medicine, can solve the problems of unstable foam volume, short foam half-life, shortened action time, etc., and achieve the advantages of rapid formation, prolonged action time, and improved retention Effect
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Embodiment 1
[0069] Synthesis and Characterization of Fatty Alcohol Tranexamic Acid Ester
[0070] Tranexamic acid (5 g, 31.84 mmol) was dissolved in dichloromethane, and thionyl chloride (3.23 mL, 44.58 mmol) was added dropwise under ice-cooling conditions, and the temperature was raised to 25° C. for 12 h. The corresponding alcohol (n-hexanol (4.79mL, 38.21mmol), n-octanol (6.01mL, 38.21mmol), n-nonanol (6.66mL, 38.21mmol)) was added dropwise, the reaction was continued at 25°C for 24h, and distilled off under reduced pressure. Chloromethane was used to obtain a white solid, which was washed with methyl tert-butyl ether and dried in vacuum for 24 hours to obtain the following three products respectively. The NMR spectrum is as Figure 1-6 shown.
[0071] Tranexamic acid n-hexyl alcohol ester (TA6): 1 H NMR (600MHz,D 2 O) δ3.99(t, J=6.7Hz, 2H), 2.82(d, J=7.1Hz, 2H), 2.31-2.17(m, 1H), 1.92(d, J=5.4Hz, 2H), 1.84 (d,J=12.2Hz,2H),1.67-1.60(m,1H),1.58-1.49(m,2H),1.37(qd,J=13.0,3.2Hz,2H),1...
Embodiment 2
[0075] Preparation of Tranexamic Acid Long-chain Alcohol Ester Gel Preparation
[0076] (1) At room temperature, weigh 1.3, 1.4, 1.5, 1.6 g of n-hexanol tranexamic acid (TA6) and place them in 1 g of water for injection, stir to dissolve them all, and let stand to obtain 56.5%, 58.3%, 60.0%, 61.5% (w / w) serial concentration TA6 gel.
[0077] (2) At room temperature, weigh 0.9, 1.0, 1.1, 1.2 g of n-octyl tranexamic acid (TA8) and place them in 1 g of water for injection, stir to dissolve them all, and let stand to obtain 47.4%, 50.0% , 52.4%, 54.5% (w / w) series concentration TA8 gel.
[0078] (3) At room temperature, weigh 0.7, 0.8, 0.9, 1.0 g of n-nonyl tranexamic acid (TA9) and place them in 1 g of water for injection, stir to dissolve them all, and let stand to obtain 41.2%, 44.4% , 47.4%, 50.0% (w / w) series concentration TA9 gel.
Embodiment 3
[0080] Performance Test of Tranexamic Acid Long-chain Alcohol Ester Gel Preparation
[0081] (1) Determination of gel-sol transition temperature (T gel )
[0082] Measuring method: the critical gelling temperature is measured by the falling ball method. Three kinds of gels with different concentrations prepared in Example 2 are respectively placed in 10 mL test tubes, and a stainless steel ball with a diameter of 0.28 mm and 0.096 g is placed on the surface of the gel, and Put the test tube in an oil bath, start to heat up from room temperature, and the temperature rise rate is 1°C / min. Measure the temperature at which the stainless steel ball falls to the bottom of the test tube, which is the T of the gel with different concentrations. gel .
[0083] Measurement results and conclusions: if Figure 7 Shown, Gel T gel All are greater than 37°C, fully meeting the requirements for administration in the human body. T gel The changes of the three gels show that the thermal st...
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