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Novel formulation of Tizanidine and derivative thereof and preparation method thereof

A technology of tizanidine and its derivatives, which can be applied to medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc., and can solve problems such as high risks

Active Publication Date: 2011-02-09
SICHUAN CREDIT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, the risk of hypotension and orthostatic hypotension is greater when the patient is turned from a supine to a standing position

Method used

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  • Novel formulation of Tizanidine and derivative thereof and preparation method thereof
  • Novel formulation of Tizanidine and derivative thereof and preparation method thereof
  • Novel formulation of Tizanidine and derivative thereof and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The preparation of embodiment 1 tablet of the present invention (tizanidine molar ratio 70: 30 in the regular release part and the sustained release part)

[0045] Raw materials: tizanidine hydrochloride 2g, hydroxypropyl methylcellulose (HPMC K4M) 64.8g, lactose 110g, starch 100g, microcrystalline cellulose 5g, 75% ethanol appropriate amount (1000 pieces), the preparation method is as follows:

[0046] A, get tizanidine hydrochloride 0.6g, add hydroxypropyl methylcellulose (HPMC K4M) and lactose, be prepared into sustained-release part inner layer tablet core;

[0047] B. Get 1.4g of tizanidine hydrochloride, add microcrystalline cellulose to make the constant release part, and coat the outer layer of the tablet core obtained in step a to obtain a coating;

[0048]c. Take the coating obtained in step b, add starch and press into tablets according to the conventional method.

Embodiment 2

[0049] Embodiment 2 Preparation of tablet of the present invention (tizanidine molar ratio 65: 35 in the regular release part and the sustained release part)

[0050] Raw materials: 4g of tizanidine hydrochloride, 20g of tragacanth gum, 1.5g of flavoring agent, appropriate amount of distilled water, 80g of starch, 20g of dextrin (1000 tablets), the preparation method is as follows:

[0051] a. Get 1.4 g of tizanidine hydrochloride, add tragacanth gum, and prepare the slow-release part inner layer tablet core;

[0052] B. Get 2.6g of tizanidine hydrochloride, add dextrin to make a constant release part, and coat the outer layer of the tablet core obtained in step a to obtain a coating;

[0053] c. Take the coating obtained in step b, add starch and flavoring agent, and press into tablets according to the conventional method.

Embodiment 3

[0054] Embodiment 3 Preparation of tablet of the present invention (tizanidine molar ratio 75: 25 in the regular release part and the sustained release part)

[0055] Raw materials: 4g of tizanidine hydrochloride, 50g of hydroxypropyl methylcellulose (HPMC K100M), 45g of methylcellulose, 80g of starch, 20g of microcrystalline cellulose (1000 pieces), the preparation method is as follows:

[0056] a, get tizanidine hydrochloride 1.0g, add hydroxypropyl methylcellulose (HPMC K100M), methylcellulose and starch, be prepared into sustained-release part inner layer tablet core;

[0057] B. Get 3.0 g of tizanidine hydrochloride, add microcrystalline cellulose to make a constant release part, and coat the outer layer of the tablet core obtained in step a to obtain a coating;

[0058] c. Take the coating obtained in step b, add starch and press into tablets according to the conventional method.

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PUM

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Abstract

The invention relates to a nizatidine and it's derivate, wherein it contains the general-release paret whose active compotents are nizatidine and its derivate, and the slow-release part, while the mol ratio between nizatidine and derivate are 5-95:5-95. The invention also provides a relative preparation. The test has proves that its effect is higher than slow-release agent, and its rate of side effect is lower than general-release agent.

Description

technical field [0001] The invention relates to new dosage forms of tizanidine and derivatives thereof, belonging to the field of medicines. Background technique [0002] The structural formulas of tizanidine and derivatives thereof are shown in formula 1 and formula 2: [0003] Wherein Formula 1 is the structural formula of tizanidine, and Formula 2 is the structural formula of tizanidine derivatives. [0004] [0005] Formula 1 [0006] [0007] Formula 2 [0008] Wherein R is available organic or inorganic acids such as hydrochloric acid, nitric acid, sulfuric acid, fumaric acid, citric acid, methanesulfonic acid, p-toluenesulfonic acid. [0009] Tizanidine hydrochloride, the chemical name is 5-chloro-4-(2-imidazoline-2-amino)-2,1,3 thiothiazine hydrochloride. As a central skeletal muscle relaxant, it is used to reduce the increase of skeletal muscle tension, muscle spasm and muscle rigidity caused by brain and spinal cord trauma, cerebral hemorrhage, encephalit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/20A61K9/48A61K31/433A61P21/02
Inventor 陈刚陈功政刁健代竹青
Owner SICHUAN CREDIT PHARMA
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