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Tizanidine phenylacetate crystal form A and preparation method and applications thereof

A technology of tizanidine and phenylacetic acid, applied in the field of medicinal chemistry, can solve the problems affecting the stability of pharmaceutical preparations, solubility and hygroscopicity, bioavailability, drug quality and clinical efficacy differences, etc. The effect of good performance and high yield

Active Publication Date: 2019-03-29
SICHUAN CREDIT PHARMA
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

And different crystal forms may have different colors, melting points, stability, apparent solubility, dissolution rate, etc. These properties will directly affect the stability, solubility, hygroscopicity, bioavailability, etc. of pharmaceutical preparations, and resulting in differences in drug quality and clinical efficacy

Method used

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  • Tizanidine phenylacetate crystal form A and preparation method and applications thereof
  • Tizanidine phenylacetate crystal form A and preparation method and applications thereof
  • Tizanidine phenylacetate crystal form A and preparation method and applications thereof

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Embodiment 1

[0037] The preparation of embodiment 1 tizanidine phenylacetate crystal form A

[0038] Weigh 10g of tizanidine, add 500mL of isopropanol, heat up to 65-70°C and stir, add 5.37g of phenylacetic acid and stir for reaction, stop heating when the reaction is complete, slowly cool down to room temperature, continue to stir and crystallize for 1 hour , and then stand still for crystallization for 2 hours. Filter, wash, and vacuum-dry at 35° C. to obtain 14.9 g of white powdery crystals of tizanidine phenylacetate, with a yield of 97.0% and an HPLC purity of 99.97%. Mass spectrum shows its MS (m / z): 253 (M + ).

[0039] Adopt DX-2700 type X-ray powder diffractometer to analyze the crystal phase of the sample, Cu-Kα radiation, tube voltage 35KV, tube current 30mA, record the X-ray powder diffraction pattern of tizanidine phenylacetate crystal form A, see figure 1 , and the diffraction related data are shown in Table 1. Among them, the 2θ measurement error is ±0.2°, and the relative...

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Abstract

The invention provides a tizanidine phenylacetate crystal form A and a preparation method thereof, and applications. The provided tizanidine phenylacetate crystal form A uses a Cu-K[alpha] radiation source to perform X-ray powder diffraction, and a 2[theta] diffraction angle has characteristic absorption peaks at 8.0 + / - 0.2, 16.2 + / - 0.2, 19.6 + / - 0.2, 21.4 + / - 0.2 and 25.4 + / - 0.2 degrees. The crystal form A has high product chemical purity, stable properties and low hygroscopicity, and effective solutions can be provided for the improvement of the security and validity of drugs; and in addition, the crystal form A is simple in preparation technology, short in reaction time, high in yield, good in reproducibility and suitable for industrial production.

Description

technical field [0001] The invention relates to a crystal form A of tizanidine phenylacetate, a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. Background technique [0002] Tizanidine is a central skeletal muscle relaxant with an imidazoline structure, and its chemical name is 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2, 1,3-Benzothidiazol-4-amine, molecular formula: C 9 h 8 ClN 5 S, molecular weight: 253.71, its chemical structure is as follows: [0003] [0004] Formula I [0005] Tizanidine is the only new type of central skeletal muscle relaxant and central α2 adrenergic receptor agonist with gastrointestinal protective effect on the market. It was first developed by Swiss Novartis and first launched in Denmark in 1988. and Switzerland, and then successively obtained sales licenses in more than 20 countries including Europe, the United States, and Japan. It is clinically used to treat diseases such as incre...

Claims

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Application Information

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IPC IPC(8): C07D417/12A61K31/433A61P19/00
CPCC07D417/12C07B2200/13
Inventor 刘强维李晓莉傅霖陈刚
Owner SICHUAN CREDIT PHARMA
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