Amorphous telmisartan-pimelic acid eutectic crystal and preparation method and application thereof
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A technology of telmisartan and pimelic acid is applied in the field of medicine to achieve the effects of improving bioavailability, low production cost and simple preparation method
Active Publication Date: 2017-05-31
SHANDONG UNIV
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Therefore, it is an effective means to improve its solubility by studying the co-crystal of telmisartan.
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Embodiment 1
[0053] Put 51.4mg (0.1mmol) telmisartan raw material and 15.8mg (0.1mmol) pimelic acid into a mortar, drop a few drops of ethanol at room temperature, and grind for 3 to 4 hours to obtain 67.2mg of amorphous telmisartan Cocrystal of sartan and pimelic acid.
Embodiment 2
[0055] Put 102.8 mg (0.2 mmol) of telmisartan raw material and 31.6 mg (0.2 mmol) of pimelic acid into a mortar, drop a few drops of ethanol at room temperature, and grind for 3 to 4 hours to obtain 134.4 mg of amorphous telmisartan Cocrystal of sartan and pimelic acid.
Embodiment 3
[0057] The eutectic of the amorphous telmisartan prepared in Example 1 and pimelic acid uses Cu-kα radiation, and its X-ray diffraction pattern is as follows: figure 1 shown. Specifically, a Bruker D8 Advance diffractometer was used, and the measurement conditions were as follows: Cu-Kα, 40KV, 40mV light source, step size 0.02°, scanning speed 1° / min, scanning range 2-40°, room temperature. The X-ray diffraction pattern of Telmisartan is as follows figure 2 As shown, the X-ray diffraction pattern of pimelic acid is image 3 shown.
[0058] The eutectic infrared absorption spectrum of the amorphous telmisartan prepared in embodiment 1 and pimelic acid is as follows Figure 4 shown. The wave numbers of its IR characteristic peaks are: 3060.0, 3029.7, 2933.4, 2871.1, 2520.5, 1706.4, 1616.5, 1599.1, 1567.7, 1515.8, 1459.8, 1409.6, 1334.9, 1230.1, 1131.8, 1089.08, 1458.9.6 The carboxyl characteristic peak wave number of telmisartan is 1694.7, while in the infrared spectrum of...
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Abstract
The invention discloses an amorphous telmisartan-pimelic acid eutectic crystal and a preparation method and application thereof. The amorphous telmisartan-pimelic acid eutectic crystal and the preparation method and application thereof have the advantages that the amorphous telmisartan-pimelic acid eutectic crystal is prepared through a solid-state grinding method for the first time, the amorphous telmisartan-pimelic acid eutectic crystal is better in dissolution performance (solubility and dissolving speed) as compared with telmisartan, dissolution equilibrium can be achieved in an extremely short time (10 minutes) in a pH 2.0 phosphate buffer solution, the equilibrium solubility of the amorphous telmisartan-pimelic acid eutectic crystal is increased by above 7 times as compared with that of telmisartan, dissolution equilibrium can be achieved in an extremely short time (10 minutes) in a pH 7.5 phosphate buffer solution, the equilibrium solubility of the amorphous telmisartan-pimelic acid eutectic crystal is increased by above 1 time as compared with that of telmisartan, the high equilibrium solubility can be kept without 1 hour, great benefits are provided for the fast dissolution of the telmisartan and the increasing of the dissolution speed of the telmisartan, and medicine biological utilization efficiency is increased favorably.
Description
technical field [0001] The invention relates to a co-crystal of amorphous telmisartan and pimelic acid and a preparation method thereof, and also relates to a pharmaceutical composition comprising the co-crystal of amorphous telmisartan and pimelic acid, which belongs to the technical field of medicine. Background technique [0002] Telmisartan (Telmisartan), chemical name: 4'-[4-methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazole Methyl] biphenyl-2-carboxylic acid, molecular formula: C 33 h 30 N 4 o 2 , molecular weight: 514.63, structural formula is as shown in following formula I: [0003] [0004] Telmisartan (Telmisartan) is a hypotensive drug developed by Boehringer Ingelheim Pharmaceutical Company in Germany. It was granted the patent EP502314 in 1991. It was first approved for marketing in the United States in November 1998, and then in Germany, the Philippines, Australia, Belgium, the United Kingdom, etc. listed in the country. Telmisartan is...
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