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Background and Objectives: There is increase prevalence of gastric ulcer in the society, but the drugs that are sensitive for radical cure are not screened with physiologic markers such which affect proper management of the disease. The objective of the study is to relate various sources or organ specific templates: gastrin, histamine and prostaglandin relating with the disease in evaluating the potencies of cimetidine, ranitidine and omeprazole for best choice of the drugs in gastric ulcer disease treatment.Material and Methods: Plasma, gastric and antral prostaglandins, histamine and gastrin levels were studied in ninety-six (96), male and female Swiss albino rats for 28 days, using high performance liquid chromatography.Results: Male and female rats with gastric ulcer treated with cimetidine, omepraszole and ranitidine showed no significant difference (P>0.5) in gastrin and the drug groups in plasma, gastric and antral concentrations. But, there was significant difference (P<0.05) in histamine levels between cimetidine, omeprazole and ranitidine in their gastric and plasma concentration. There was no significant difference (P>0.05) in prostaglandin values between cimetidine, omeprazole and ranitidine. Also there was no significant difference (P>0.05) in gastric and plasma levels of gastrin, histamine and prostaglandin between 7, 14, 21 and 28 days treatment period. But, there was significant difference (P<0.05) in antral concentration of gastrin, histamines and prostaglandin between the drug groups. However, there was no significant difference (P>0.05) in antral gastrin between male and female rats in cimetidine and ranitidine treatment. The three drugs were associated with high levels of gastrin, histamine, low prostaglandin though cimetidine showed higher concentration of prostaglandin.Conclusion: It is concluded that gastrin, histamine and prostaglandin are sensitive indicators in evaluating anti-ulcerogenic drugs efficacies.
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The utilization of the peels of the widely popular pomegranate fruit is the subject of this study. This bio waste product, which has been under study for some time as a source of potential bioactive constituents is investigated for its biological activity. A method for the extract standardization was developed using HPLC and ellagic acid as a reference standard. Results revealed that the pomegranate methanolic extract exhibited potent analgesic and anti-inflammatory activity comparable to indomethacin, used as a reference, and furthermore, caused no gastric ulcer formation.
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Introduction: species of the family Cyperaceae are commonly used by the population to treat gastric disorders.However, there are a few ethnopharmacological studies about this family Lagenocarpus rigidus (Kunth) Ness, Cyperaceae, is one of the most widespread swamp species. Objective: evaluate the gastric activity of L. rigidus and its chemical characterization. Methods: ethanolic extract of L. rigidus (ELR) leaves prepared by percolation was subjected to total polyphenol and flavonoid quantification, as well as HPLC quantification of some flavonoids. Angiotensin converting enzyme (ACE) inhibition was determined by colorimetric assays.The gastric effects of ELR were tested in male Wistar rats (n = 6 each group) treated with different doses (600, 60 and 6 mg/kg i.p.) ELR.Gastric lesions were induced by administration of indomethacin (30 mg/kg s.c.).The number of ulcers and the index of mucosal damage (IMD) were determined taking into account the color, edema and bleeding of gastric lesions, the number of petechiae, and the number and size of the ulcers. Statistical analysis of data was performed with one-way ANOVA followed by Tukey's test; significance was p < 0.05. Results: ELR inhibited the ACE (68.5±18.1%) at a concentration of 100 mg/mL.Oral administration of ELR (6, 60 and 600 mg/kg) showed protective activity against indomethacin-induced gastric injury. Total polyphenols in ELR were 157.7 ± 5.8 mg pirogalol/mg equivalent flavonoids and 66.9 ± 3.1 µg equivalent quercetin/mg. Conclusion: L. rigidus protects against acute gastric damage induced by indomethacin in an independent dose manner.
Introducción: las especies de la familia Cyperaceae popularmente se utilizan para tratar trastornos gástricos. Sin embargo, hay pocos estudios etnofarmacológicos sobre esta familia. Lagenocarpus rigidus (Kunth) Ness, Cyperaceae, es una de las especies más grandes de población en pantano. Objetivo: evaluar la actividad gástrica de L. rigidus, junto a su caracterización química. Métodos: el extracto etanólico de hojas de L. rigidus (ELR), preparado por percolación fue objeto de cuantificación de polifenoles y flavonoides totales, cuantificación por HPLC de algunos flavonoides. La inhibición de la enzima convertidora de angiotensina (ECA) se realizó por ensayos colorimétricos. Los efectos gástricos de ELR se llevó a cabo en ratas Wistar macho (n = 6, cada grupo), el tratamiento con diferentes dosis (600, 60 y 6 mg/kg ip) de ELR. Las lesiones gástricas se indujeron mediante la administración de indometacina (30 mg/kg sc). El número de úlceras y signos de puntuación del índice de lesión de las mucosas (IMD) se evaluó teniendo en cuenta el color, edema y hemorragia de las lesiones gástricas, el número de petequias, y el número y tamaño de las úlceras. El análisis estadístico de los datos se realizó mediante ANOVA 1 vía, seguido por el test de Tukey y significación fue de p < 0,05. Resultados: ELR inhiben la ACE (68,5 ± 18,1 %) a una concentración de 100 mg/mL. La administración oral de ELR (6, 60 y 600 mg/kg) mostró un efecto protector gástrico contra inducido por indometacina. Los polifenoles totales de ELR fue 157,7 ± 5,8 mg equivalente de pirogalol/mg de flavonoides y 66,9 ± 3,1 μg equivalentes de quercetina/mg. Conclusiones: L. rigidus protege contra el daño gástrico agudo inducido por la indometacina en una organización independiente de la dosis.
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Naproxen, an anti-inflammatory drug, exhibits poor aqueous solubility, which limits the pharmacological effects. The present work was carried out to study the effect of agglomeration on micromeritic properties and dissolution. Naproxen agglomerates were prepared by using a three solvents system composed of acetone (good solvent), water (non-solvent) and dichloromethane (bridging liquid). Differential Scanning Calorimetry (DSC) results showed no change in the drug after crystallization process. X-Ray Powder Diffraction (XRPD) studies showed the sharp peaks are present in the diffractograms of spherical agglomerates with minor reduction in height of the peaks. The residual solvents are largely below the tolerated limits in the agglomerates. Scanning Electronic Microscopy (SEM) studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates exhibited improved solubility, dissolution rate and micromeritic properties compared to pure drug. Anti-inflammatory studies were conducted in Wistar strain male albino rats and naproxen agglomerates showed more significant activity than the pure drug.
Naproxeno, fármaco anti-inflamatório, apresenta baixa solubilidade em água, o que limita os efeitos farmacológicos. O presente trabalho foi realizado para estudar o efeito da aglomeração nas propriedades micromeríticas e na dissolução. Aglomerados de naproxeno foram preparados por meio da utilização de sistema de três solventes composto de acetona (bom solvente), água (não-solvente) e diclorometano (líquido de ligação). A DSC não resulta mostrou nenhuma mudança na droga depois de processo de cristalização. Estudos de difração de Raios X do Pó (XRPD) mostraram picos agudos nos difratogramas de aglomerados esféricos, com redução mínima dea altura dos picos. Os solventes residuais estão amplamente abaixo dos limites tolerados nos aglomerados. Os estudos de Microscopia Eletrônica de Varredura (SEM) mostraram que esses aglomerados eram de estrutura esférica e formados por grupos de pequenos cristais. Os aglomerados apresentaram solubilidade, taxa de dissolução e propriedades micromeríticas aprimoradas em comparação com o fármaco puro. Estudos anti-inflamatórios foram conduzidos em ratos Wistar albinos masculinos e os aglomerados de naproxeno mostraram atividade mais significativa do que o fármaco puro.
Subject(s)
Dissolution/methods , Naproxen/analysis , Anti-Inflammatory Agents/pharmacokinetics , Calorimetry, Differential Scanning/classification , Methylene Chloride/analysis , Solvents/classificationABSTRACT
Carpolobia lutea leaves (CLL) (Polygalaceae) were earlier screened and the antiulcer ethnomedicinal claim established. This article seeks to quantitatively isolate, elucidate the active compounds from most active CLL fraction. Fractionation was by semi-preparative HPLC; the active fraction was subjected to radical scavenging assays (RSA) and quantification of the total phenolic content (TPC) were also executed. Results: Ethyl acetate fraction (EAF) was observed to be the most pharmacologically active antiulcer fraction when screened using acute ulcer models induced in rodents. The EAF demonstrated significant (p < 0.05-0.001) antiulcer activity in various in vivo induced ulceration models by reducing the ulcer index and increasing the preventive ratio. The EAF demonstrated > 70% in TPC and < 20 % in RSA. Cinnamic and coumaric acids derivatives were isolated from EAF. Cinnamic acids have been implicated and patented as antiulcer agent. Isolated compounds could in part mediate the observed pharmacological activities which lend credence to its ethnobotanical uses.
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Ethanolic extract of Annona muricata L., Annonaceae, leaf (AML) was used to investigate its antinociceptive and anti-ulcerogenic activities and the involvement of the mechanism of ethanolic leaves extract of AML in various animal models. Antinociceptive activity of AML extract was done using acetic acid-induced abdominal writhing in mice, formalin test in rats and hot plate test in mice. Furthermore, the anti-ulcerogenic effect of AML extract was studied in ethanol-induced ulcer model in rats, ethanol-induced gastric lesions in L-NAME-pre-treated rats as well as ethanol-induced gastric lesions in NEM-pre-treated rats test model to determine its mechanism. AML exhibited significant and dose-dependent antinociceptive activity. It also significantly decreased the ulcerative lesion produced by ethanol in rats in a dose-dependent manner. Pre-treatment with N-ethymaleimide, a thiol blocker, including mucosal nonprotein sulfhydryl groups, reduced the anti-ulcerogenic effect of AML extract in the same ulcer model, suggesting that AML extract may have active substances such as tannins, flavanoids and triterpenes that increase the mucosal nonprotein sulfhydryl group content.
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BACKGROUND: The incidence of upper gastrointestinal bleeding has decreased in the general population but has increased in geriatric patients worldwide. The aim of this study was to evaluate the clinical characteristics and outcomes of geriatric patients (aged 65 or older) with upper gastrointestinal bleeding and to compare them with non-geriatric patients (less than 65 years old). METHODS: We conducted a retrospective study of 288 patients with upper gastrointestinal bleeding from January 2007 to August 2010. We compared the clinical characteristics and outcomes of geriatric patients (n=148, 51.4%) with those of non-geriatric patients (n=140, 48.6%). RESULTS: Cardiovascular disease, hypertension, and cerebrovascular accidents were more prevalent in the geriatric group, compared with those in the non-geriatric group (p<0.05). Vital signs were more unstable in the geriatric group than those in the non-geriatric group (p<0.05). The geriatric group had taken more ulcerogenic drugs than those in the non-geriatric group (p<0.05). The most common cause of upper gastrointestinal bleeding was peptic ulcer (72.3%) in the geriatric group, whereas it was variceal bleeding (41.4%) in the non-geriatric group. Treatment methods, transfusion volume, operation rate, and mortality were not different between the two groups. The length of hospital stay and length of intensive care unit (ICU) stay were significantly longer in geriatric patients than those in the non-geriatric group (p<0.05). CONCLUSION: Geriatric patients with upper gastrointestinal bleeding had longer ICU and hospital stays than those of non-geriatric patients. Important emerging etiologies such as ulcerogenic drugs and associated chronic illness should be monitored and treated early in these patients.
Subject(s)
Humans , Cardiovascular Diseases , Chronic Disease , Geriatrics , Hemorrhage , Hypertension , Incidence , Intensive Care Units , Length of Stay , Peptic Ulcer , Retrospective Studies , Stroke , Vital SignsABSTRACT
From Hippophae rhamnoides L.oil free seed, acylated ?-sitosterol ?-D-glucoside was isolated.By alkaline hydrolysis, acylated steryl glucoside yielded ?-sitosterol-?-D-glucoside and fatty acids which were identified as palmitic, stearic, oleic, linoleic, linolenic and decadecylenic acids.These results suggest that acylated steryl glucoside may be esterified forms of ?-sitosterol-?-D-glucoside which was identified by means of physicochemical properties, spectral analysis and synthesis, ?-sitosterol ?-D-glucoside in relatively small doses (i. e. 12mg/kg) was found to be an effective agent in the treatment of acetic acid-induced chronic ulcer in mice.