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Ketorolac and 4-pyridine carboxamide eutectic crystal and preparation method thereof

A technology of pyridinecarboxamide and ketorolac, which is applied in the field of co-crystal of ketorolac and 4-pyridinecarboxamide and its preparation, can solve the problems that the crystal form solubility and stability need to be further improved, and achieve easy control of the crystallization process , high yield and good reproducibility

Pending Publication Date: 2022-04-22
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the solubility and stability of the existing crystal forms need to be further improved

Method used

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  • Ketorolac and 4-pyridine carboxamide eutectic crystal and preparation method thereof
  • Ketorolac and 4-pyridine carboxamide eutectic crystal and preparation method thereof
  • Ketorolac and 4-pyridine carboxamide eutectic crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 255 mg of ketorolac acid (1 mmoL) and 122 mg of 4-pyridinecarboxamide (1 mmoL) dissolved in 40 mL acetone and 40 mL of methanol, heated and dissolved at 40 °C, dissolved in solution, cooled to 10 °C, left to crystallization for 24 hours, filtered and dried to obtain ketorolac acid and 4-pyridineformamide eutectic, yield 96.8%, HPLC: 99.92%.

Embodiment 2

[0048] 255 mg of ketorolac acid (1 mmoL) and 146 mg of 4-pyridinecarboxamide (1.2 mmoL) were dissolved in 30 mL of acetonitrile and 30 mL of acetone, heated and dissolved at 55 °C, after the solution was clarified, cooled to 15 °C, left to crystallography for 48 hours, filtered and dried to obtain ketorolac acid and 4-pyridinecarboxamide eucrystalline, yield 98.2%, HPLC: 99.96%.

Embodiment 3

[0050] 255 mg of ketorolac (1 mmoL) and 183 mg of 4-pyridinecarboxamide (1.5 mmoL) were dissolved in 40 mL acetonitrile, heated and dissolved at 60 °C, dissolved in solution, cooled to 30 °C, left to crystallize for 36 hours, filtered and dried to obtain ketorolac acid and 4-pyridineformamide eutectic, yield 98.0%, HPLC: 99.93%.

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals, and provides a ketorolac and 4-pyridinecarboxamide co-crystal and a preparation method thereof.The prepared ketorolac and 4-pyridinecarboxamide co-crystal is radiated through Cu-K alpha, and an X-ray diffraction pattern expressed by 2 theta has characteristic peaks at the positions of 5.7 + / -0.2 degrees, 6.6 + / -0.2 degrees, 11.5 + / -0.2 degrees, 13.4 + / -0.2 degrees, 15.7 + / -0.2 degrees, 17.5 + / -0.2 degrees, 18.3 + / -0.2 degrees and 27.4 + / -0.2 degrees; according to the ketorolac and 4-pyridine carboxamide eutectic crystal prepared by the invention, the yield is greater than 93%, the purity is higher than 99.80%, the preparation method is simple, the crystallization process is easy to control, and the reproducibility is good; compared with the existing ketorolac crystal form or ketorolac standard substance, the ketorolac crystal form or ketorolac standard substance has higher solubility in a phosphoric acid buffer solution with pH of 6.8.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical eutectic technology, specifically to a ketorolac and 4-picolinicamide eutectic and preparation method and application thereof. Background [0002] Ketorolac is a powerful analgesic, moderate anti-inflammatory nonsteroidal anti-inflammatory drug that has analgesic effects comparable to morphine and is stronger than aspirin, indomethacin, and naproxen. At present, there are more reports on ketorolac, mainly on its preparation, preparation, physicochemical properties and pharmacology, and less reports on its crystal structure. There is a polymorphic phenomenon in ketorolac, the article Crystal Forms of Ketorolac (Arch Pharm Res, 2004, 27, 357-360) disclosed the crystal form characterization data and preparation methods of ketorolac crystal forms I, crystalline II, crystal form III, crystal form IV, and studied the solubility and stability of crystal forms I. to IV. The results show that the solubili...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D213/81A61K31/407A61P29/00
CPCC07D487/04C07D213/81A61P29/00C07B2200/13
Inventor 翟立海许秀艳朱志英余军厚
Owner LUNAN PHARMA GROUP CORPORATION
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