Novel water-soluble lubricant for the preparation of tiemonium methylsulfate fast-dissolving tablets

Abstract

The rapid delivery and self-administration of antispasmodics are very essential for the treatment of pain associated with smooth muscle spasms. Tiemonium methylsulfate (TMS) is a well-known antispasmodic drug used in the treatment of muscle spasms of different organs. New oral dissolving tablets (ODTs) of the drug were formulated using l-leucine as a new and highly water-soluble lubricant and evaluated. The obtained tablets were of sufficient mechanical strength and low friability and disintegrated and dissolved rapidly. About 98% of the drug was dissolved in the first 15 min without any solid residues in the buccal cavity. There was no difference observed between the dissolution profiles of pure drug and drug formulated in ODTs. The in vitro antispasmodic effect of TMS was not affected by incorporation of the drug in the tablet form. The obtained results strongly support the development of ODTs containing TMS for rapid and noninvasive treatment of painful smooth muscle spasms.