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Methocarbamol salt
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A technology of methocarbamol and solvent, applied in the field of methocarbamol salt, can solve the problems of low bioavailability of methocarbamol, swelling of patients, large oral dose, etc., to improve water solubility and bioavailability , The effect of water solubility improvement
Active Publication Date: 2010-10-20
天津市美索药物研发有限公司
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[0006] On the basis of the original product research, we conducted a comprehensive analysis of Methocarbamol, and found that the shortcoming of Methocarbamol itself is that it is insoluble in water
Because of this shortcoming of being insoluble in water, only polyethylene glycol and water were used as solvents to make injections, so some patients experienced adverse reactions of swelling at the intramuscular injection site in clinical practice; it is also because of this insoluble The disadvantage of water makes the bioavailability of methocarbamol low, so its oral dose is relatively large, 0.75-1.0 g each time, 3-4 times a day
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[0029] 1. Synthesis of Methocarbamol Dihydrogen Phosphate:
[0030] In the cooling pool, install a reaction bottle, an electric stirrer, a thermometer, and a dropping funnel, put in 120.62 grams of methocarbamol and 1,500 mL of chloroform, stir, cool down to -15°C, and dropwise add 153 grams of phosphorus oxychloride and 153 mL of chloroform solution , keep the low temperature, add 90mL of pyridine dropwise, the temperature is not higher than 20°C. After adding, react for 120 minutes. 100 mL of water was added, and the organic solvent was distilled off under reduced pressure. Add 2400 mL of water, precipitate crystals, cool down, filter, wash the filter layer with water, and dry. Obtain 132 grams of dihydrogen phosphate, mP120~124°C.
[0034] 1. Synthesis of Methocarbamol Dihydrogen Phosphate:
[0035] In the cooling pool, install a reaction bottle, an electric stirrer, a thermometer, and a dropping funnel, put 120.62 grams of methocarbamol and 1,200 mL of chloroform, stir, cool down to -15°C, and dropwise add 153 grams of phosphorus oxychloride and 153 mL of trichloride Methane liquid, keep the low temperature, add 160mL of triethylamine dropwise, the temperature is not higher than 20°C. After adding, the reaction is 120 points. Add 1000mL of water, pour the reaction solution into a separatory funnel, let it stand, separate the chloroform layer, collect the water extract, add 800mL of water, extract, add 800mL of water, extract, combine the water extract, cool down, filter, wash the filter layer with water, and dry . 137 grams of dihydrogen phosphate was obtained, mP120~123°C.
[0036] 2. Synthesis of Dipotassium Methocarbamol Phosphate...
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Abstract
The invention relates to methocarbamol salt, belonging to the technical field of chemicals, wherein methocarbamol is a central muscle relaxant and a medicine for treating common diseases and frequently-occurring diseases; and the methocarbamol has exact curative effects and high safety, but the shortcoming of water insolubility thereof is a key obstacle for development and improvement. The methocarbamol salt solves the problem and changes the water solubility of methocarbamol from 1:210 into that of the methocarbamol salt of 1:1; the methocarbamol salt is easily dissolved in water and the bioavailabilityin vivo is improved; and on the basis of comprehensive and deep experimental study, the invention explores a novel process route for synthesizing the water-soluble methocarbamol salt.
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technical field [0001] The invention belongs to the technical field of chemicals, in particular to methocarbamol salts with improved bioavailability. Background technique [0002] Drugs are special commodities related to life and safety. New drug research and development has a large investment; the development cycle is long, generally takes about 10 years; the development of new drugs must be based on multidisciplinary basic theories, and use various modern scientific and technological means to follow up and study. To discover and innovate. The market is highly competitive, and many studies in developed countries start with modified lead compounds, which is a shortcut method among the multi-research strategies of developed countries. For example, there are quite a few derivatives of erythromycin, some of which are combined into double salts by using the intermolecular acid-base or van der Waals force, and some of which are new compounds obtained by modifying the structure o...
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