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.
Studies on influence of lipid lowering therapies have generated wide controversial results on the role of cholesterol on memory function. However recent studies revealed that cholesterol lowering treatment substantially reduce the risk of dementia. The objectives of this study were to analyze the effect of statins on memory function and to establish the relationship between increase/decrease in cholesterol synthesis, total cholesterol level and memory function in animals. We examined the relationship between biosynthesis of cholesterol and memory function using two statins (lipophilic simvastatin and hydrophilic pravastatin) and high cholesterol diet in mice for 15 days and 4 months. Memory performance was evaluated with two different behavioral tests and various biochemical parameters such as serum cholesterol, whole brain cholesterol, brain 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) activity and brain acetylcholine esterase (AChE) activity. We found that statin treatment for 4 months, but not for 15 days, showed significant improvement in memory function whereas high cholesterol diet showed significant impairment of memory. However long-term statin treatment showed significant decrease in serum cholesterol level as well as brain AChE level. Moreover high cholesterol diet showed significant decrease in memory function with an increase in serum cholesterol level as well as brain AChE level. There is no direct correlation between brain cholesterol level, as well as HMG-CoA activity with memory function regulation. However there is definite link between plasma cholesterol level and AChE level. A long-standing plasma cholesterol alteration may be essential to regulate memory function which in turn might be mediated through AChE modulated pathway.
Abstract:In recent years, a widespread search has been launched to identify new antiinflammatory and antiulcer-drugs from natural sources. The study was aimed at evaluating the antiinflammatory and antiulcer activity of chloroform extract (CH) and hydroalcoholic extract (HE) of the stem bark of Calotropis procera (Aiton) W.T. Aiton, Apocynaceae, obtained successively by cold maceration. The antiinflammatory effect of the CH and HE extracts of the stem bark of the C. procera against carrageenan-induced paw oedema and also its antiulcer activity by using two acute models: Aspirin (100 mg/kg, p.o.) and ethanol (96%, 1 mL/200 g) in albino rats have been studied and found to be significant at 200 and 400 mg/kg when compared to the standard drugs. As a part of investigations to obtain compounds with antiinflammatory and antiulcer activity in this work, a bioassay was carried out with fractions obtained from chloroform extract with n-hexane (NF1), 1-butanol (BF1), ethyl acetate (EF1) and chloroform (CF1). The hydroalcoholic extract (HE) of the stem bark was fractionated with n-hexane (NF2), 1-butanol (BF2), ethyl acetate (EF2), chloroform (CF2) and water (WF2). The fractions were freezedried and evaluated for its antiinflammatory and antiulcer activity. Fractions NF1, CF1, BF2 and EF2 (20 mg/kg) showed significant antiinflammatory and antiulcer activity. The results obtained for antiulcer activity were also supported well by the histopathological examination of the open excised rat stomach. Further experiments are underway to determine which phytoconstituents are involved in antiinflammatory and antiulcer activities as well as mechanisms involved in gastroprotection.
In the present work, orodispersible tablets of Tramadol hydrochloride were prepared using novel co-processed superdisintegrants consisting of crospovidone and sodium starch glycolate in the different ratios (1:1, 1:2 & 1:3). The developed superdisintegrants were evaluated for angle of repose, Carr's index and Hausner's ratio in comparison with physical mixture of superdisintegrants. The angle of repose of the developed excipients was found to be < 25 o , Carr's index in the range of 11-15% and Hausner's ratio in the range of 1.12-1.17. Orodispesible tablets of Tramadol hydrochloride were prepared using the above coprocessed superdisintegrants and evaluated for pre-compression and post-compression parameters. Based on in vitro disintegration time (approximately 18 sec), promising formulation CP1 was tested for in vitro drug release pattern in 0.1N HCl and drug excipients interaction (FT-IR spectroscopy, DSC) were studied. Among the designed formulations, the formulation (CP1) containing 4% w/w of co-processed superdisintegrant (1:1 mixture of crospovidone and sodium starch glycolate) emerged as the overall best formulation (t50% 1.46 min) based on drug release characteristics in 0.1N HCl compared to commercial conventional tablet formulation (t50%> 8 min).
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