Unlock instant, AI-driven research and patent intelligence for your innovation.

Tizanidine hydrochloride compound

A technology for tizanidine hydrochloride and a compound, which is applied in the field of preparation of the compound crystal I, can solve the problems that the quality of the finished product is difficult to meet the standard, difficult to remove colored impurities, and there are many impurities in tizanidine hydrochloride, so as to achieve stable properties and improve biological performance. Availability and safety, good water solubility

Active Publication Date: 2016-05-11
SICHUAN CREDIT PHARMA
View PDF4 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the tizanidine hydrochloride prepared by the existing process has more impurities, and the finished product is mostly yellow or light yellow solid, with many colored impurities that are not easy to remove, making the quality of the finished product difficult to reach the standard

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tizanidine hydrochloride compound
  • Tizanidine hydrochloride compound
  • Tizanidine hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation of embodiment 1 tizanidine hydrochloride compound

[0034] Weigh 50g of tizanidine hydrochloride, add a mixed solution of 125mL ethanol and 125mL water, heat up to 75°C, after the dissolution is complete, add an appropriate amount of activated carbon, filter while hot, and slowly cool the filtrate to room temperature at 0.5°C / min, continue Stir for 1 hour, then stand at room temperature for 8 hours, filter with suction, wash, and dry to obtain 49.1 g of tizanidine hydrochloride compound crystal I in the form of white powder, with a yield of 98.2%. Mass spectrum showed its ESI m / z: 254.

[0035] The measured melting point of tizazidine hydrochloride compound crystal I is 285.0-286.5°C. Using CuKα radiation, the X-ray powder diffraction pattern of tizanidine hydrochloride compound crystal I is measured in figure 1 , and the diffraction related data are shown in Table 1 (2θ measurement error is ±0.2).

[0036] Table 1 X-ray powder diffraction data of tiz...

Embodiment 2

[0038] The preparation of embodiment 2 tizanidine hydrochloride compound

[0039] Weigh 50g of tizanidine hydrochloride, add a mixed solution of 350mL ethanol and 50mL water, heat up to 50°C, after the dissolution is complete, add an appropriate amount of activated carbon, filter while hot, and slowly cool the filtrate to room temperature at 0.5°C / min, continue Stir for 0.5 hour, then stand at room temperature for 24 hours, filter with suction, wash, and dry to obtain 48.4 g of crystal I of tizanidine hydrochloride compound in the form of white powder, with a yield of 96.8%. The structural analysis results and X-ray powder diffraction patterns of the obtained product are not significantly different from those in Example 1.

Embodiment 3

[0040] The preparation of embodiment 3 tizanidine hydrochloride compound

[0041]Weigh 50g of tizanidine hydrochloride, add a mixed solution of 690mL ethanol and 60mL water, heat up to reflux, after the dissolution is complete, add an appropriate amount of activated carbon, filter while hot, and slowly cool the filtrate to room temperature at 0.8°C / min, then continue to stir After 2.5 hours, it was allowed to stand at room temperature for 16 hours, filtered with suction, washed, and dried to obtain 48.5 g of crystals of tizanidine hydrochloride compound I in the form of white powder, with a yield of 97.0%. The structural analysis results and X-ray powder diffraction patterns of the obtained product are not significantly different from those in Example 1.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Melting pointaaaaaaaaaa
Login to View More

Abstract

The invention provides a tizanidine hydrochloride compound. The invention also provides a preparation method of the tizanidine hydrochloride compound, a pharmaceutical composition and a use of the tizanidine hydrochloride compound. The tizanidine hydrochloride compound is in a crystal I form. In X ray powder diffraction based on Cu and K alpha radiation sources, characteristic absorption peaks of the tizanidine hydrochloride compound form at 2 theta diffraction angles of 10.7+ / -0.2, 11.1+ / -0.2, 12.4+ / -0.2, 17.0+ / -0.2, 20.3+ / -0.2, 21.2+ / -0.2, 24.0+ / -0.2 and 24.8+ / -0.2 degrees. The tizanidine hydrochloride compound has stable properties and good water solubility and provides an effective method for improving drug bioavailability and safety. The tizanidine hydrochloride compound has the advantages of simple processes, high purity and good yield and is suitable for industrial production.

Description

technical field [0001] The present invention relates to a tizanidine hydrochloride compound, in particular to the crystal I form of the compound, as well as the preparation method, pharmaceutical composition and application of the compound crystal I. Background technique [0002] Tiazanidine Hydrochloride (TiazanidineHydrochloride) is a central skeletal muscle relaxant with an imidazoline structure, the chemical name is 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2 , 1,3-benzothiadiazol-4-amine hydrochloride, its molecular structure is as follows: [0003] [0004] Tizanidine hydrochloride is the only new type of central skeletal muscle relaxant and central α 2 Adrenergic receptor agonists were first developed by Novartis in Switzerland. They were first launched in Denmark and Switzerland in 1988, and subsequently obtained sales licenses in more than 20 countries including Europe, the United States, and Japan. They are used clinically Treatment of diseases such as increas...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D417/12A61K31/433A61P21/02
Inventor 傅霖邓丽敏李文婕陈刚
Owner SICHUAN CREDIT PHARMA