Skeletal muscle relaxant compositions comprising .alpha.,.alpha.-diphenyl-3-tropidineethanol and methods of producing skeletal muscle relaxation

#This invention relates to pharmaceutical compositions which are useful for spastic disorders of skeletal muscles and to a method of producing skeletal muscle relaxant activity by administering said compositions. The compositions of this invention help relieve myopathic disorders such as, for example, myotonia, night cramps, or motor deficiencies resulting from disorders of muscle cell metabolism. More specifically, the compounds of this invention comprise .alpha.,.alpha.-diphenyl-3-tropidineethanol as the active medicament.

#Most advantageously the compositions of this invention are in dosage unit form and comprise a nontoxic pharmaceutical carrier and a tropidineethanol having the following formula: ##STR1##

#The compound of this invention has been demonstrated as having direct acting spastic skeletal muscle relaxation activity without tropane-like side effects when tested against chemically induced myotonia in mice. The skeletal muscle effects induced by the administration of anthracene-9-carboxylic acid have been reported to be markedly similar to hereditary myotonia in the goat and to myotonia congentia in humans (J. Physiol. 219, 367-383, 1971).

#The following examples are not limiting but are illustrative of compounds of this invention and the procedures for their preparation. Other variations of this invention will be obvious to those skilled in the art.

#Under an atmosphere of dry nitrogen, 1.5 gm. of lithium wire in 20 ml. of ether is reacted with 5.65 gm. of bromobenzene in 50 ml. of ether. A solution of 1.5 gm. of ethyl 3-tropidineacetate in 30 ml. of ether is added and mild reflux maintained throughout the addition. The reaction mixture is then stirred under reflux for about four hours, cooled and treated with saturated ammonium chloride solution and extracted several times with ether. The extracts are dried and concentrated to give an oil which is treated with citric acid in acetone-ether (1.1 mole ratio) to yield .alpha.,.alpha.-diphenyl-3-tropidineethanol citrate as white crystals having a melting point of 195.degree.-199.degree. C.

#______________________________________ Ingredients Amounts ______________________________________ .alpha.,.alpha.-Diphenyl-3-tropidineethanol 75.00 mg. Magnesium Stearate 2.00 mg. Lactose 130.00 mg. ______________________________________