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. The optimized formulation (B3) showed a mucoadhesive strength >35 g. In vivo study was performed using rabbits by X-ray imaging technique. Radiological evidences suggest that, a formulated tablet was well adhered for >10 h in rabbit's stomach. Optimized lafutidine mucoadhesive tablets showed no significant change in physical appearance, drug content, mucoadhesive properties and in vitro dissolution pattern after storage at 40 °C temperature 75 ± 5% relative humidity for 3 months.
This study was aimed at evaluating the anti-inflammatory and gastromucosal protective effect of chloroform extract (CH) and hydroalcoholic extract (HE) of the stem bark of Calotropis procera obtained successively by cold maceration. The anti-inflammatory effect of the CH and HE extracts of the stem bark of Calotropis procera against carrageenan-induced paw oedema and also its gastromucosal protective effect has been studied by using two acute models: aspirin (100 mg/kg, p.o.) and ethanol (96%) in albino rats. CH and HE extracts showed significant anti-inflammatory activity at 200 and 400 mg/kg, while CH extract at 400 mg/kg was also found to have a significant gastromucosal protective effect. As part of investigations to obtain compounds with anti-inflammatory and gastromucosal protective effects in this work, a bioassay was carried out with fractions obtained from the CH extract with n-hexane (NF1), 1-butanol (BF1), ethyl acetate (EF1) and chloroform (CF1). The HE extract of the stem bark was fractionated with n-hexane (NF2), 1-butanol (BF2), ethyl acetate (EF2), chloroform (CF2) and water (WF2). The fractions were evaluated for their anti-inflammatory and gastromucosal protective effects. Fractions NF1, CF1, BF2 and EF2 (20 mg/kg) showed significant anti-inflammatory activity, while NF1 and BF2 (20 mg/kg) also showed gastromucosal protective effects. The results obtained for gastromucosal protective effects were also well supported by histopathological examination of the open excised rat stomach.
Bombax ceiba bark extract was evaluated for its hypoglycemic and hypolipidemic potential through normal and streptozotocin-induced diabetic rats administered with graded oral doses (200, 400, 600 mg/kg/day) for 21 days. The results showed that a dose of 600 mg/kg of B. ceiba extract is the most effective to cause significant (p<0.001) hypoglycemic and/or hypolipidemic effects on streptozotocin-induced diabetic rats. This dose also significantly (p<0.001) lowered the total cholesterol and triglyceride level in severely diabetic rats. Phytochemical and GC-MS studies confirmed the presence of the triterpenoid compounds in the extract, which may account for its significant hypoglycemic activity. The present study thus provides a scientific rationale for the traditional use of this plant in the management diabetes. This ork is li e sed u der a Creati e Co o s Attri utio 3.0 Li e se. You are free to opy, distri ute a d perfor the ork. You ust attri ute the ork i the a er spe ified y the author or li e sor.
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