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Stable novel crystal form of dimemorfan phosphate

A technology of dimethylphene phosphate and crystal form, which is applied in the field of preparing antitussive drugs and can solve problems such as description of recrystallization method

Active Publication Date: 2011-03-30
贵州阜康仁制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The literature Chem.Pharm.Bull. (1972, 20, 1706-1710) reported that dimethylorphinyl phosphate can be obtained quantitatively from the salt formation of dimethylorphinyl and phosphoric acid, but did not describe its recrystallization method

Method used

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  • Stable novel crystal form of dimemorfan phosphate
  • Stable novel crystal form of dimemorfan phosphate
  • Stable novel crystal form of dimemorfan phosphate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Dissolve 21.8g of dimethyrphane in 60ml of acetone by heating in a water bath, add 9.8ml of 85% phosphoric acid dropwise under stirring, stir at room temperature for 2 hours after dropping, filter, wash twice with an appropriate amount of acetone, and dry under reduced pressure at 50°C to obtain 27g of white solid , that is, dimethylorphantyl phosphate crystal I.

[0020] 1 H-NMR (CD 3 OD, ppm): 2.198~2.223(d, 1H), 2.306(s, 3H), 2.865(s, 3H), 3.530(s, 1H), 7.022~7.038(d, 1H), 7.095~7.110(d, 1H), 7.159 (s, 1H). ESI-MS: 256.2.

Embodiment 2

[0022] Take 17.3 g of dimethylorphinyl phosphate, add 400 ml of methanol, heat to reflux to dissolve, filter while hot, and place the filtrate at room temperature to crystallize completely. Filter and dry under reduced pressure at 50°C to obtain 12.4 g of dimethylmorphyl phosphate crystal I.

Embodiment 3

[0024] Tablets each containing 10 mg of the new crystal form of dimetyl phosphate were prepared as follows:

[0025] Prescription: 10 g of dimethylorphinyl phosphate, 44 g of microcrystalline cellulose (PH-102), 35 g of lactose, 0.5 g of croscarmellose sodium, and 0.5 g of magnesium stearate, made into 1000 tablets.

[0026] Method: crush the main drug through 80-mesh sieve, pass other auxiliary materials through 60-mesh sieve, mix evenly, inspect the semi-finished product, measure the content, determine the average tablet weight; press into tablets, and coat with film.

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Abstract

The invention provides a stable novel crystal form of dimemorfan phosphate, which is characterized in that basically the diffraction spectrum, which is presented by 2 theta, of the X-ray Cu-Ka powder has characteristic peaks at about 5.3 nanometers, about 13.5 nanometers, about 16.3 nanometers and about 24.5 nanometers.

Description

technical field [0001] The present invention relates to new crystal forms of dimethylorphinyl phosphate, pharmaceutical compositions containing these new crystal forms and their use in the preparation of antitussive drugs. Background technique [0002] The chemical name of dimethylmorphan phosphate is (9α, 13α, 14α)-3,17-dimethylmorphinan phosphate, and its structural formula is as follows: [0003] [0004] This product is a non-addictive central antitussive drug, and its antitussive effect is slightly better than that of dextromethorphan, which is about twice that of codeine. The advantages are low toxicity, high safety, no inhibition of respiration in the therapeutic dose, and no side effect of constipation. Dimethylorphantyl phosphate has been on the market in Japan for more than 30 years without any report of serious adverse reactions. It has definite curative effect and is safe and reliable. [0005] The document Chem.Pharm.Bull. (1972, 20, 1706-1710) reported tha...

Claims

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Application Information

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IPC IPC(8): C07D221/28A61K31/485A61P11/14
Inventor 姚勇敢
Owner 贵州阜康仁制药有限公司
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