Lafutidine - CAS 118288-08-7
Catalog number: 118288-08-7
Category: Inhibitor
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Histamine Receptor
Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
FRG-8813; FRG 8813; FRG8813
1.Changes in the mucus barrier during cisplatin-induced intestinal mucositis in rats.
Yamamoto H1, Ishihara K2, Takeda Y2, Koizumi W1, Ichikawa T2. Biomed Res Int. 2013;2013:276186. doi: 10.1155/2013/276186. Epub 2013 Dec 23.
AIM: Gastrointestinal mucositis is a frequent complication of antineoplastic chemotherapy, but the effects of chemotherapy on mucosal defense mechanisms remain poorly understood. We studied the effects of cisplatin on mucin, one of the principal defense factors of the gastrointestinal mucosa, and evaluated the efficacy of two different types of H2-receptor antagonists against cisplatin-induced mucositis.
2.Retrospective cohort study on combination therapy with the histamine H2-receptor antagonist lafutidine for antihistamine-resistant chronic urticaria.
Ogawa Y1, Ichinokawa Y, Hiruma M, Machida Y, Funakushi N, Sadamasa H, Hiruma M. J Dermatolog Treat. 2013 Dec;24(6):463-5. doi: 10.3109/09546634.2013.800183. Epub 2013 May 21.
We conducted a retrospective cohort study evaluating the efficacy and usefulness of the addition of lafutidine, a novel histamine H2-receptor antagonist, in treatment of patients with idiopathic chronic urticaria whose disease was not well controlled with histamine H1-receptor antagonists. Based on the assessment of global improvement, moderate or better improvement was achieved in 39 of 46 patients (85%) after 1-3 weeks of additional administration of lafutidine and 35 patients (76%) after 3 months. No incidence of drug-related adverse reactions was reported in any patient. Lafutidine was rated as useful or better in 34 patients (74%) after 3 months of treatment. The usefulness of the drug was not affected by differences in background factors, such as disease duration, previous treatment duration and the number of concomitant H1-receptor antagonists. Lafutidine appears to be a promising addition to histamine H1-receptor antagonist therapy for the treatment of chronic urticaria resistant to treatment with H1-receptor antagonists alone.
3.Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability.
Patil S1, Talele GS. Drug Deliv. 2015 May;22(3):312-9. doi: 10.3109/10717544.2013.877099. Epub 2014 Jan 29.
Lafutidine a newly developed histamine H2-receptor antagonist having biological half-life of 1.92 ± 0.94 h due to its selective absorption from upper part of gastrointestinal tract the development of mucoadhesive sustained release drug delivery system is recommended in order to enhance the bioavailability. A mucoadhesive tablets was developed using the natural polymer, sodium alginate, xanthan gum and karaya gum. Mucoadhesion is a complex phenomenon which involves wetting, adsorption and interpenetration of polymer chains. The prepared tablets of various formulations were evaluated for a total mucoadhesion time, buoyancy lag time and percentage drug released. The formulation with xanthan gum showed better results. Thus, it may be useful for prolonged drug release in stomach to improve the bioavailability and reduced dosing frequency. Non-fickians release transport was confirmed as the drug release mechanism from the optimized formulation by Korsmeyer-Peppas.
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CAS 118288-08-7 Lafutidine

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