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Tizanidine nitrate crystal form A, and preparation method and applications thereof

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

Active Publication Date: 2019-03-29
SICHUAN CREDIT PHARMA
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  • Abstract
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  • 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 nitrate crystal form A, and preparation method and applications thereof
  • Tizanidine nitrate crystal form A, and preparation method and applications thereof
  • Tizanidine nitrate crystal form A, and preparation method and applications thereof

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Embodiment 1

[0035] The preparation of embodiment 1 tizanidine nitrate crystal form A

[0036] Weigh 10g of tizanidine, add 400mL of methanol and 2.53mL of concentrated nitric acid, heat up to 40-45°C and stir to react. After the reaction is complete, stop heating, slowly cool down to 5-10°C, and continue to stir and crystallize for 4 hours. After filtration, washing, and vacuum drying at 35° C., 12.07 g of crystal form A of tizanidine nitrate was obtained as a white powder, with a yield of 96.7% and an HPLC purity of 99.98%. Mass spectrum shows its MS (m / z): 253 (M + ).

[0037] Adopt DX-2700 type X-ray powder diffractometer to analyze sample crystal phase, Cu-Kα radiation, tube voltage 35KV, tube current 30mA, record the X-ray powder diffraction pattern of tizanidine nitrate 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 intensity measurement error is ±5%, sometimes even up to ±20%.

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Abstract

The invention provides a tizanidine nitrate crystal form A, and a preparation method and applications thereof. The provided tizanidine nitrate 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 11.4 + / - 0.2, 20.8 + / - 0.2, 21.8 + / - 0.2, 23.2 + / - 0.2 and 26.7 + / - 0.2 degrees; the crystal formA is high in chemical purity, stable in property and low in hygroscopicity, and an effective solution can be provided for the improvement of the availability and security of drugs; and in addition, the crystal form A is simple in preparation technology, short in reaction time and high in product yield, and has no special requirements on equipment, so that the crystal form A is suitable for industrial production.

Description

technical field [0001] The invention relates to a crystal form A of tizanidine nitrate, a preparation method and application of the crystal form, and belongs to the technical field of medicinal chemistry. Background technique [0002] Tizanidine is an imidazoline diazoline derivative with the chemical name 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3 -Benzothiadiazol-4-amine, molecular formula: C 9 h 8 ClN 5 S, molecular weight: 253.71, its chemical structure is as follows: [0003] [0004] 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 increased skeletal muscle tension, muscle spasm an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
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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