Malotilate - CAS 59937-28-9
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Not Intended for Therapeutic Use. For research use only.
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Malotilate, diisopropyl 1,3-dithiol-2-ylidenemalonate, is a drug used for the treatment of liver cirrhosis.
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1.[Drugs inhibiting the hepatic fibrogenesis].
Tariciotti G1, Festuccia F, Lauria V, Attili AF. Minerva Gastroenterol Dietol. 1998 Mar;44(1):23-42.
The treatment of chronic liver disease represents still now an open problem in medicine. The first objective of therapy has to be the causal agent removal; however, there are many cases (viral infections, autoimmunity, genetic disease) in which it is not possible to reach this issue; in these situations the secondary objective of the therapy is to inhibit the hepatic fibrogenesis, in attempt of easing or blocking the transformation of chronic liver disease in cirrhosis. The aim of this work is to review the various compounds which showed an antifibrotic activity, using a simple classification model, allowing a fast setting of different compounds. These last, on the basis of their main action, can be divided into two main groups: drugs with direct action, which interfere with collagen metabolism (for instance interferons, glucocorticoids, prolyl 4-hydroxylase inhibitors, cyclosporin A, colchicine, D-penicillamine, phosphatidylcholine and so on) and drugs with indirect action, that decrease the inflammatory stimuli, capable of stirring up the fibrogenetic hepatic process (S-adenosylmethionine, malotilate, ursodeoxycholic acid, ribavirin and so on).
2.[Effect of tanshinone IIA on CCl4-induced liver fibrosis in rats].
Liu Y1, Chen H, Jiang Y. Zhong Yao Cai. 2002 Jan;25(1):31-3.
OBJECTIVE: To study the effect of tanshinone IIA on liver fibrosis in rats induced by CCl4.
3.Gene-CYP11B2 expression in rat liver in hepatic fibrogenesis induced by CCl4.
Li X1, Yang X, Wu P, Meng Y, Li S, Lai W. Chin Med J (Engl). 2001 Jan;114(1):64-8.
OBJECTIVE: To identify aldosterone synthase gene-CYP11B2 mRNA expression in normal and fibrotic liver in rats and evaluate the curative effect of antisterone.
4.Physicochemical and pharmacokinetic characterization of a spray-dried malotilate emulsion.
Zhang J1, Gao Y, Qian S, Liu X, Zu H. Int J Pharm. 2011 Jul 29;414(1-2):186-92. doi: 10.1016/j.ijpharm.2011.05.032. Epub 2011 May 17.
Malotilate (MT) is a hepatoprotective drug administered orally. However, MT was found to be a poorly water-soluble drug with low oral bioavailability. In the present investigation, a novel spray-dried emulsion (SDE) loaded with MT was prepared, and its physicochemical properties were characterized by rheological evaluation, particle size measurement, in vitro release, and surface morphology. The pharmacokinetic study of SDE, in comparison to MT suspension with the pure MT powder homogeneously dispersed in 0.5% CMC-Na solution, was also performed in rats after a single oral dose. It was found that SDE exhibited a 2.9-fold higher peak plasma concentration (C(max)) and 2.3-fold higher area under the curve (AUC) than MT suspension.
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CAS 59937-28-9 Malotilate

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