1.Effects of automated external lubrication on tablet properties and the stability of eprazinone hydrochloride.
Yamamura T1, Ohta T, Taira T, Ogawa Y, Sakai Y, Moribe K, Yamamoto K. Int J Pharm. 2009 Mar 31;370(1-2):1-7. doi: 10.1016/j.ijpharm.2008.11.007. Epub 2008 Nov 18.
We investigated the advantages of an external lubrication technique for tableting. A newly developed external lubricating system was applied to tableting in a rotary tablet press using magnesium stearate. The resulting tablets were compared with tablets produced by the conventional internal lubrication method, in which lubricant is blended before tableting. As a model API, we chose eprazinone hydrochloride, because it is easily hydrolyzed by alkaline lubricant. The amount of lubricant required to prevent sticking with external lubrication was only 1/13th of that required with internal lubrication. External lubrication increased tablet crushing strength by 40%, without prolonging tablet disintegration time, and improved the residual ratio of eprazinone hydrochloride in tablets stored under stress conditions for 4 weeks by 10%. The distribution of lubricant on the surface of externally lubricated tablets was observed by scanning electron microscopy after the preparation by focused ion beam milling.
2.[Eprazinone exanthema with subcorneal pustulosis].
Faber M, Maucher OM, Stengel R, Goerttler E. Hautarzt. 1984 Apr;35(4):200-3.
A drug eruption with subcorneal pustulation is presented, occurring in a patient during treatment with eprazinone . The biopsy of the initial lesions showed changes as in pustulosis subcornealis . The aetiopathogenetic relationship between administration of eprazinone and the pustular eruption was confirmed by patch test.
3.Eprazinone alters lung lavage lipid levels and transtracheal ion transport.
Thrall RS1, Cloutier MM, Guernsey L, Swayne E, Gionfriddo M. Exp Lung Res. 1992 May-Jun;18(3):409-20.
Eprazinone therapy improves pulmonary function and arterial pO2 in patients with chronic bronchitis; however, the mechanism of action is unknown. The purpose of this study was to determine if eprazinone alters either lung surfactant levels in bronchoalveolar lavage fluid (BAL) of normal rats, or ion transport across canine tracheal epithelium mounted in Ussing chambers. In the surfactant studies, normal rats were force fed three doses (50, 100, and 200 mg/kg) of eprazinone for 4 days. Eprazinone at a dose of 200 mg/kg significantly increased total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreased total neutral lipids. Lower doses of eprazinone significantly decreased neutral lipid levels without affecting the phospholipids. There was no change in BAL levels of protein or cells and no abnormal histology. In airway epithelial studies, mucosal addition of eprazinone produced a dose-dependent partially reversible decrease in short-circuit current (Isc).