Aclatacit pharmaceutical co-crystal and preparation method thereof
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A technology for actarid and medicine, which is applied in the field of actali drug co-crystal and preparation thereof, can solve problems such as decreased solubility, and achieve the effects of low cost, improved oral absorption efficiency, and simple process
Pending Publication Date: 2022-04-29
SOUTHEAST UNIV
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Problems solved by technology
Although drug co-crystals have obvious advantages in improving the solubility of drugs, it is not that the solubility of drugs will be improved after forming co-crystals, and the solubility of some drugs will decrease after forming co-crystals.
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Embodiment 1
[0036] Weigh 193.2mg of actarit and 122.1mg of nicotinamide, dissolve in 10mL of acetone and cyclohexane mixed solvent with a volume ratio of 1:1, ultrasonically react for 50min, filter and place in a constant temperature incubator at 35°C After cultivating at a medium constant temperature for 8 days, the drug co-crystal of actaritide-nicotinamide was obtained. Using SXRD to characterize and analyze the crystal, the obtained actarit-nicotinamide crystal structure is as follows figure 1 As shown, its crystal structure belongs to the monoclinic crystal system, and the space group is P2 1 / n, axis length: Angle: α / °=90, β / °=98.9990(10), γ / °=90, Z=4.
Embodiment 2
[0038] Weigh 193.2mg of actarit and 183.2mg of nicotinamide, dissolve in 20mL of acetonitrile and chloroform mixed solvent with a volume ratio of 2:1, react with ultrasound for 70min, filter and place in a constant temperature incubator at 30°C After culturing for 10 days, the drug co-crystal of Actarit-Nicotinamide was obtained. The drug co-crystal was characterized by differential scanning calorimetry, and the actaritide-nicotinamide co-crystal had an absorption peak at 115.96°C, and the DSC figure was as follows figure 2 shown.
Embodiment 3
[0040] Weigh 96.6mg of actarit and 122.1mg of nicotinamide, dissolve in 15mL of a mixed solvent of methanol and chloroform with a volume ratio of 1:6, react with ultrasound for 40min, filter, and place in a constant temperature incubator at 40°C for constant temperature After culturing for 14 days, the drug co-crystal of Actarit-Nicotinamide was obtained. Using PXRD to characterize the obtained crystals, the actarityl-nicotinamide co-crystals were at 2θ=8.6°, 13.7°, 15.4°, 16.4°, 17.3°, 19.3°, 20.5°, 22.6°, 24.1°, 24.9° , 26.2°, 26.8°, 27.3°, 27.6°, 28.6°, 30.5°, 31.3°, 33.2°, 34.8°, 36.9°, 38.7° and 40.1° have characteristic peaks, and the characteristic curves are as follows image 3 shown.
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Abstract
The invention discloses an acclathril pharmaceutical co-crystal which is formed by taking acclathril as a pharmaceutical active ingredient and taking a pyridine carboxamide micromolecule as a co-crystal former through an intermolecular hydrogen bond. The solubility of the acclathril medicine and the two co-crystals of the acclathril medicine in water and a simulated duodenum solution is investigated, and it is found that the solubility of the acclathril medicine is obviously improved through the two co-crystals of the medicine, and the bioavailability of the acclathril medicine is improved. The invention also discloses a preparation method of the actacitride pharmaceutical co-crystal, nicotinamide and isonicotinamide are respectively selected to form two new actacitride pharmaceutical co-crystals with actacitride pharmaceutical active ingredients through a pharmaceutical co-crystal technology, so that the solubility and bioavailability of the actacitride pharmaceutical co-crystal are remarkably improved, and the oral absorption efficiency of actacitride is improved. The method is simple in process, low in cost and beneficial to further production.
Description
technical field [0001] The invention belongs to the field of organic drug co-crystals, in particular to actaride drug co-crystals and a preparation method thereof. Background technique [0002] Rheumatoid arthritis is a chronic inflammatory disease that often affects the various moving joints of the body. Its clinical symptoms are mostly manifested as morning stiffness, multi-joint involvement, joint deformity, etc., which are more harmful to the human body. In severe cases, it can lead to the loss of joint movement function, and even affect the heart, kidneys and respiratory system. [0003] The chemical name of actarit is 4-acetylaminophenylacetic acid, which is an oral immunomodulator developed by Mitsubishi Chemical Corporation of Japan, and is clinically used for the treatment of rheumatoid arthritis. It has an inhibitory effect on the delayed allergic reaction, and can improve the early symptoms of rheumatoid arthritis by reducing the concentration of nitric oxide in...
Claims
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