Formulation of stomach-specific floating microparticles of nizatidine and their radiographic evaluation

Nizatidine is an anti-secretogogue and a gastroprotective drug with a half-life of 1-2 h and is well absorbed in the stomach. This study aimed to optimize the process and develop floating microparticles of nizatidine that are based on low methoxyl pectin. Oil-in-oil dispersion method and Taguchi orthogonal array design were employed, and the prolonged residence time of the microparticles in the stomach was demonstrated. The constraints for independent variables, viz. A-polymer, B-internal solvent volume, C-surfactant, D-stirring rate and E-stirring time were set to generate the experimental runs. Particle size, percentage yield, micromeritic properties, entrapment efficiency, in vitro buoyancy and in vitro release were characterized. Surface morphology, zeta potential, in vitro release kinetics and in vivo floating performance of the optimized formulation was examined. The microparticles were free-flowing, irregular in shape and had a mean particle size distribution of 73-187 µ. Low methoxyl pectin played a predominant role in achieving buoyancy and optimum gastric retention for the modified release of the drug, suggesting Korsmeyer-Peppas model as the possible release mechanism. In vivo radiographic study in rabbits revealed that the drug was retained in the stomach for a period of 6 h. These results indicate that nizatidine floating microparticulate system provides modified drug release for the effective treatment of gastric ulcer

Comparative stomach tissue distribution profiles of four major bio-active components of Radix Astragali in normal and gastric ulcer mice

Numerous studies have demonstrated that Radix Astragali can inhibit gastric ulcers in mice. Anhydrous ethanol (0.01 mL/g) administered to mice by intragastric infusion can induce gastric ulcer injury. This study was performed to compare the stomach tissue distribution profiles of four major bioactive constituents of Radix Astragali(calycosin-7-O-ß-d-glucoside, calycosin, ononin and formononetin) after oral administration of extract of Radix Astragali (ERA)in normal and gastric ulcer mice. The abundance of Radix Astragali constituents was determined using an ultra-pressure liquid chromatograph with a photodiode array detector (UPLC-PDA), after which histograms were drawn. In comparison with normal mice, the contents of calycosin- 7-O-ß-d-glucoside, calycosin, ononin and formononetin in the stomach tissue samples of gastric ulcer mice showed significant differences at the selected time points (P < 0.05).The abundance of each of the four tested constituents in the normal groups was higher than that of the gastric ulcer groups. This study provides an empirical foundation for future studies focused on developing clinical applications of Radix Astragali

Effects of acute oral exposure to acrylamide on histological structures of the stomach in Wistar rats / Efectos de la exposición oral aguda a la acrilamida sobre las estructuras histológicas del estómago en ratas Wistar

SUMMARY: Acrylamide is a toxic chemical substance with wide implementation in chemical industry. In 2002 the presence of acrylamide was discovered in foods rich in starch which are prepared at high temperatures. The aim of this study was to investigate the histopathological changes in the gastric tissue in Wistar rats induced with injection of oral acrylamide. The research was carried out 6 groups of 5 animals (Wistar rats), two control groups and four experimental groups. Histological changes in the stomach tissue of Wistar rats are seen as a direct slight damage of the surface epithelium, accompanynig inflammatory reaction and renewal of the epithelium. Examined inflammatory and degenerative parameters show a positive correlation with respect to dose and time of exposition to acrylamide. Knowing the mechanism of action of these toxic substances, allows to apply adequate prevention in nutrition and make an appropriate choice of therapeutic methods.

RESUMEN: La acrilamida es una sustancia química tóxica con amplia aplicación en la industria química. En el año 2002 se determinó la presencia de acrilamida en alimentos ricos en almidón preparados a altas temperaturas. El objetivo de este estudio fue investigar los cambios histopatológicos en el tejido gástrico en ratas Wistar inducidos con inyección de acrilamida oral. La investigación se llevó a cabo en 6 grupos de 5 animales, dos grupos control y cuatro grupos experimentales. Los cambios histológicos en el tejido del estómago de las ratas Wistar se ven como un ligero daño directo del epitelio superficial, que acompaña a la reacción inflamatoria y la renovación del epitelio. Los parámetros inflamatorios y degenerativos examinados muestran una correlación positiva con respecto a la dosis y el tiempo de exposición a la acrilamida. El conocimiento del mecanismo de acción de estas sustancias tóxicas permite aplicar una prevención adecuada en nutrición y hacer una elección oportuna de los métodos terapéuticos.

Antiulcerogenic effects of selected African nightshades (Solanum nigrum Linn. ) genotypes on the rat stomach: a morphologic and morphometric study / Efectos antiulcerogénicos de genotipos seleccionados de solanáceas Africanas (Solanum nigrum Linn. m) en el estómago de ratas: un estudio morfológico y morfométrico

Solanum nigrum (SLN), commonly known as African nightshade, is used as a vegetable as well as in the management and treatment of various ailments including gastric ulcers. We analyzed, both grossly and microscopically using H&E, Masson's trichrome and PSA staining methods, the protective effects of aqueous leaf extracts of three Kenyan SLN genotypes namely S. scabrum (SSB), S. sarrachoides (SSR) and S. villosum (SVL) on ethanol-induced gastric lesions in rats. There was evidence of gastro-protection by all the three genotypes with the SSB showing the highest ulcer inhibition score (76.37 %) followed by SSR (72.51 %) and SVL (63.30 %). SLN-pretreated rats showed less areas of gastric mucosal surface erosion. Additionally in the pretreated animals, the depth of the ulcers were markedly reduced, reaching only the gastric pit region except in those treated with SVL where the ulcers penetrated slightly more deeply to affect the gastric glands. Compared with controls, the mean microscopic ulcer index decreased 5.07, 3.55 and 2.37-fold in rats pretreated with SSB, SSR and SVL extracts respectively. Results of this work show extracts of the three SLN genotypes to have antiulcerogenic potential but at varied strengths, thus confirming earlier reports that phytoconstituents and hence the efficacy of a medicinal plant may be influenced by genetic factors.

Solanum nigrum (SLN), comúnmente conocida como la solanácea africana, se usa como vegetal, para el tratamiento de diversas dolencias incluyendo las úlceras gástricas. Analizamos de forma macro y microscópica, de forma macroscópica y microscópica, utilizando para ello tinciones de H&E, tricrómico de Masson y PSA los efectos protectores de extractos acuosos de hojas de tres genotipos SLN de Kenia: S. scabrum (SSB), S. sarrachoides (SSR) and S. villosum (SVL) en lesiones gástricas inducidas por etanol en ratas. Hubo evidencia de gastroprotección por parte de los tres genotipos con el SSB mostrando el puntaje más alto de inhibición de la úlcera (76,37 %) seguido de SSR (72,51 %) y SVL (63,30 %). Las ratas tratadas previamente con SLN mostraron menos áreas de erosión de la superficie de la mucosa gástrica. Además, en los animales pretratados, la profundidad de las úlceras se redujo notablemente, llegando solo a la región del fondo gástrico, excepto en aquellos tratados con SVL donde las úlceras penetraron un poco más profundamente para afectar las glándulas gástricas. En comparación con los controles, el índice medio de úlcera microscópica disminuyó 5,07, 3,55 y 2,37 veces en ratas pretratadas con extractos de SSB, SSR y SVL, respectivamente. Los resultados de este trabajo muestran que los extractos de los tres genotipos de SLN tienen potencial antiulcerogénico en diferentes concentraciones, lo que confirma informes anteriores que los fitoconstituyentes y la eficacia de una planta medicinal pueden estar influenciados por factores genéticos.

Chemical composition by HPLC-ESI-QTOF-MS/MS: Estrogenic and antioxidant effects of Mangifera indica L. cv. "Kent" leave extracts on ovariectomized rats / Composición química por HPLC-ESI-QTOF-MS/MS: efectos estrogénicos y antioxidantes de extractos de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas

The chemical composition of Mangifera indica L. cv. "Kent" leaves was determined by HPLC-ESI-QTOF-MS/MS. Polyphenolic compounds characterized as benzophenone derivatives were the main components found in extracts (1, maclurin 3-C-(2-O-galloyl)-D- glucoside isomer; 2, maclurin 3-C---D-glucoside; 3, iriflophenone 3-C---D-glucoside; 5, maclurin 3-C-(2,3-di-O-galloyl)---D-glucoside; 6, iriflophenone 3-C-(2-O-galloyl)---D-glucoside; 7, methyl-iriflophenone 3-C-(2,6-di-O-galloyl)---D-glucoside) and xanthones (4, mangiferin and 8, 6-O-galloyl-mangiferin). The estrogenic and antioxidant effects of aqueous extracts from Mangifera indica L. cv. "Kent" leaves on ovariectomized rats were determined by uterotrophic assay and malondialdehyde (MDA) levels in erythrocytes, bone, liver, and stomach. We conclude that the polyphenolic compounds from extracts act as exogenous antioxidant agents against oxidative damage in ovariectomized rats.

La composición química de las hojas de Mangifera indica L. cv. "Kent" se determinó por HPLC-ESI-QTOF-MS/MS. Compuestos polifenólicos caracterizados como derivados de benzofenona fueron los componentes principales encontrados en los extractos (1, isómero de la maclurina 3-C-(2-O-galoyil)-D-glucósido; 2, maclurina 3-C-ß-D-glucósido; 3, iriflofenona 3-C-ß-D-glucósido; 5, maclurina 3-C-(2,3-di-O-galloíl)-ß-D-glucósido; 6, iriflofenona 3-C-(2-O-galloil)-ß-D-glucósido; 7, metil-iriflofenona 3-C-(2,6-di-O- galloyl)-ß-D-glucósido) y xantonas (4, mangiferina y 8, 6-O-galoyil-mangiferina). Los efectos estrogénicos y antioxidantes de los extractos acuosos de hojas de Mangifera indica L. cv. "Kent" en ratas ovariectomizadas se determinaron mediante ensayo uterotrófico y la medición de los niveles de malondialdehído (MDA) en eritrocitos, huesos, hígado y estómago. Concluimos que los compuestos polifenólicos de los extractos actúan como agentes antioxidantes exógenos contra el daño oxidativo en ratas ovariectomizadas.

Regularity of prescription medication of Xin'an Wang's internal medicine in treating stomach cramps based on data mining / 中国中药杂志

The study analyzes the medication rules of Xin'an Wang's internal medicine for treating stomach cramps by data mining technology,in order to provide reference for clinical medication. Through the summarization of the medical cases of stomach cramps treated by Xin'an Wang's doctors( Wang Ren-zhi,Wang Zhong-qi,Wang Le-tao),statistics was made for the frequency of symptoms,signs,syndromes and drugs in Office 2010. Apriori algorithm in IBM SPSS Modeler 14. 1,and SPSS Statistics 22. 0 were used for association rule analysis and cluster analysis. The results showed that the 310 prescriptions collected involved totally 322 syndromes( including symptoms and signs) and 336 drugs,with the cumulative dose of 4 072 times; the symptoms were correlated to the spleen and stomach,liver and gallbladder,and the heart system; syndrome differentiation was mainly based on liver-Qi invasion of the stomach,diet impairment to the stomach,deficiency of spleen and stomach and cold syndrome; commonly used drugs were Qi regulating drugs,phlegm eliminating drugs and blood circulation promoting and stasis removing drugs; high-frequency drug complex network diagram showed that Pinelliae Rhizoma,Aurantii Fructus,Trichosanthis Fructus,Allii Macrostemonis Bulbus were closely related; the analysis showed 12,20,and 17 two,three,and four association rules; cluster analysis showed 10 pairs of Trichosanthis Fructus-Allii Macrostemonis Bulbus,Pinelliae Rhizoma-Aurantii Fructus,and Aspongopus-Toosendan Fructus drug combinations. According to Xin' an Wang's doctors,stomach cramps are closely related to liver and spleen,Qi stagnation,phlegm and blood stasis are the standard.Xin'an Wang's doctors give the first priority on " deoppilation",focus on soothing the liver and spleen,activating Qi and eliminating phlegm,and promoting blood circulation,and refer to use modified Xiaoxianxiong Decoction and modified Gualou Xiebai Banxia Decoction based on symptoms.

Histological and ultrastructural studies on the effect amoxicillin on the stomach of mouse fetuses

Introduction: B-Lactam antibiotics are widely used because of their lack of toxicity in humans. However, during pregnancy, exposure of the fetus is likely to occur due to b-lactam antibiotics cross the placenta. The potential adverse effects of amoxicillin were examined in stomach of mice fetuses

Material and Methods: This study was aimed to evaluate the possible side effects produced by amoxicillin prenatal administration on the stomach of fetuses. Twenty pregnant mice were used in this study; and were divided into two groups: the first group served as a control group and injected by saline solution [the drug solvent]; the second group treated with amoxicillin dose of 205 mg/kg body weight. The treatment was daily administered interperitoneally, from the 7[th] day of gestation till the 14[th] day of gestation [GDs 7-14]. The developing 19-days old fetuses were examined histologically and ultrastructurally to determine any disorders in the stomach

Results: This study illustrated marked deleterious consequences in the gastric wall of 19 day old fetus, following the treatment with amoxicillin, ranging from marked vacuolations and erosions in the epithelial and glandular cells of the gastric mucosa to conspicuous necrosis of glandular [parietal and zymogenic] cells. The electron microscopical examination of the gastric mucosal cells of fetuses maternally treated with amoxicillin, revealed conspicuous alterations, in the cytoplasmic organelles of gastric mucosal cells [surface epithelial, peptic and parietal cells]. The cisternae of RER were dilated and fragmented. The mitochondria displayed gradual devastations

Conclusions: Therefore, the destructive impacts of amoxicillin on the stomach of mice fetuses indicated that it should be used under restricted precautions in the medical fields to protect the pregnant women from its hazardous impact

Ultrastructural and immunohistochemical effects of aqueous leave extract of Xylopia aethiopica on the stomach in streptozotocin-induced diabetic rats / Efectos ultraestructurales e inmunohistoquímicos del extracto acuoso de la hoja Xylopia aethiopica en el estómago de ratas diabéticas inducidas por estreptozotocina

Gastrointestinal pathology in diabetic patients has become a source of concern in recent times. The aim of this study was to investigate the ultrastructural and immunohistochemical effects of aqueous leaf extract of Xylopia aethiopica on the stomach in streptozotocin-induced diabetic rats. This study was conducted using thirty adult Wistar rats. The animals were divided into three groups (n= 10). Group A was the control animals (administered with equivalent volume of citrate buffer), group B was diabetic animals induced by a single intraperitoneal injection of streptozotocin dissolved in citrate buffer (65 mg/kg) and group C was diabetic animals treated with 200 mg/kg body weight of aqueous leave extract of X. aethiopica for twenty five days. At the expiration of the study, all the animals in each of the groups were sacrificed and the stomach excised and fixed in both 10 % formol and karnovsky fixatives immunohistochemical, light microscopic and electron microscopic studies respectively. The results showed a gradual decline (P<0.05) in the blood glucose level in the extract treated group as against the increment in untreated diabetic group. There was a distortion of the glandular mucosa and epithelium in the untreated diabetic group vis-à-vis the extract treated and control groups. The immunohistochemical staining and percentage immunoreactivity of the stomach of untreated diabetic group showed that the immunoexpression of H+/K+-ATPase were sparse and significantly (p<0.000) lower compared with the control group. There was a better staining pattern for H+/K+-ATPase gastric proton pump in the group treated with aqueous leaf extract of X. aethiopica as compared with the untreated diabetic group. The ultrastructural studies of untreated diabetic group revealed a reduction in the density of mitochondria as compared with the control group. Treatment with leaf extract of X. aethiopica increased the mitochondrial density as well as uniform dispersal of chromatin. It is concluded that diabetes causes gastric pathology thus resulting in morphological changes in the gastric histo-architecture and parietal cells. The aqueous leaf extract of X. aethiopica enhances the recovery/restoration of these defects in streptozotocin induced diabetic rats and as such, may play a significant role in the management of complications associated with diabetes mellitus.

La enfermedad gastrointestinal en pacientes diabéticos se ha convertido en una fuente de preocupación en los últimos tiempos. El objetivo fue investigar los efectos ultraestructurales e inmunohistoquímicos de extracto acuoso de la hoja de Xylopia aethiopica en el estómago de ratas con diabetes inducida por estreptozotocina. Se utilizaron 30 ratas Wistar adultas, divididas en tres grupos (n= 10). El Grupo A, control (se le administró un volumen equivalente de tampón de citrato); el Grupo B, animales diabéticos inducidos por una sola inyección intraperitoneal de estreptozotocina disuelta en tampón de citrato (65 mg/kg) y el Grupo C, animales diabéticos con 200 mg/kg peso corporal tratados con extracto acuoso de X. aethiopica durante 25 d. Luego, todos los animales fueron sacrificados, se les extirpó el estómago y fijó en formol al 10 % y en fijador Karnovsky para anticuerpos monoclonales contra la bomba de protones gátrica H+/K+-ATPasa; las muestras se observaron mediante microscopías óptica y electrónica. Los resultados mostraron una disminución gradual (P<0,05) en el nivel de glucosa en sangre del grupo tratado con el extracto, contra un incremento en el grupo diabético no tratado. Hubo una distorsión de la mucosa glandular y el epitelio en el grupo diabético no tratado vis-à-vis los grupos tratados con extracto y el de control. La tinción inmunohistoquímica del estómago del grupo diabético no tratado, mostró escasas células parietales inmunorreactivas en el grupo diabético no tratado comparado con el grupo control. Hubo un mejor patrón de tinción en la bomba de protones gátrica H+/K+-ATPasa en el grupo tratado con el extracto de hoja acuosa de X. aethiopica, en comparación con el grupo diabético no tratado. Los estudios ultraestructurales del grupo diabético no tratado revelaron una reducción en la densidad de las mitocondrias en comparación con el grupo control. El tratamiento con extracto de hoja de X. aethiopica aumentó la densidad mitocondrial, así como la dispersión uniforme de la cromatina. Se concluye que la diabetes causa una enfermedad gástrica que genera cambios morfológicos en la histoarquitectura de las células parietales gástricas. El extracto de hoja acuosa de X. aethiopica mejora la recuperación/restauración de estos defectos en ratas diabéticas inducidas por estreptozotocina y, como tal, puede jugar un rol significativo en el tratamiento de las complicaciones asociadas con la diabetes mellitus.

Association of terpinolene and diclofenac presents antinociceptive and anti-inflammatory synergistic effects in a model of chronic inflammation

Pharmacological treatment of inflammatory pain is usually done by administration of non-steroidal anti-inflammatory drugs (NSAIDs). These drugs present high efficacy, although side effects are common, especially gastrointestinal lesions. One of the pharmacological strategies to minimize such effects is the combination of drugs and natural products with synergistic analgesic effect. The monoterpene terpinolene (TPL) is a chemical constituent of essential oils present in many plant species, which have pharmacological activities, such as analgesic and anti-inflammatory. The association of ineffective doses of TPL and diclofenac (DCF) (3.125 and 1.25 mg/kg po, respectively) presented antinociceptive and anti-inflammatory effects in the acute (0, 1, 2, 3, 4, 5 and 6 h, after treatment) and chronic (10 days) inflammatory hyperalgesia induced by Freund's complete adjuvant (CFA) in the right hind paw of female Wistar rats (170-230 g, n=6-8). The mechanical hyperalgesia was assessed by the Randall Selitto paw pressure test, which determines the paw withdrawal thresholds. The development of edema was quantified by measuring the volume of the hind paw by plethismography. The TPL/DCF association reduced neutrophils, macrophages and lymphocytes in the histological analysis of the paw, following a standard staining protocol with hematoxylin and eosin and the counts were performed with the aid of optical microscopy after chronic oral administration of these drugs. Moreover, the TPL/DCF association did not induce macroscopic gastric lesions. A possible mechanism of action of the analgesic effect is the involvement of 5-HT2A serotonin receptors, because ketanserin completely reversed the antinociceptive effect of the TPL/DCF association. These results suggest that the TPL/DCF association had a synergistic anti-inflammatory and analgesic effect without causing apparent gastric injury, and that the serotonergic system may be involved in the antinociceptive effect of this association.

Histological evaluation of the effects of borax obtained from various sources in different rat organs / Evaluación histológica de los efectos del borax obtenido de diversas fuentes en diferentes órganos de rata

Boron is an essential element for life and intake via different sources into the body. Because effects of boron and compounds on the body has not been studied enough especially in tissue level, we planned this study to evaluate the effects of borax the most intaken form of boron compound on different intraabdominal organs histologically and also clinically. 42 male rats divided into equal 7 groups and different toxicological doses consistent with its LD50 dose (5000 mg/kg/d) were administered by gavage except control and sham groups. In the study, 2 different kinds of borax one of which was produced for research and the other for agriculture but the same formulation, were used and their effects were also compared. As a result it was found that borax did not cause any histological changes in kidney, large intestine, liver and stomach in lower doses. But if doses were increased, a slightly inflammatory cell migration was detected without clinical signs in liver and large intestine. However, when a single very high dose of borax was administered, very high edema, inflammatory cell migration and neovascularization was observed and clinically 2 out of 6 rats died within 5 hours. We suggested that very high dose intake of borax may cause sudden death and also during long periods and higher dose intake may pave the way of inflammatory bowel diseases. At the same time, in boron related studies we advice that the kind of boron and also their source should be evaluated carefully and the most suitable compound should be chosen in case of faulty results.

El boro es un elemento esencial para la vida e ingresa a través de diferentes fuentes al cuerpo. Dado que los efectos del boro y sus compuestos en el cuerpo no se han estudiado lo suficiente, especialmente a nivel tisular, se planificó este estudio para evaluar sus efectos y la forma de consumo más común del compuesto de boro sobre diferentes órganos intraabdominales a nivel histológico y clínico. Cuarenta y dos ratas macho divididas en 7 grupos, con diferentes dosis toxicológicas de acuerdo con su dosis DL50 (5000 mg/kg/d) administradas por sonda, excepto en los grupos control y simulado. En el estudio fueron usados 2 tipos diferentes de boro, uno producido para la investigación y el otro para la agricultura, pero de la misma formulación, y sus efectos fueron comparados. Se encontró que el boro no causó cambios histológicos en el riñón, intestino grueso, hígado y estómago en dosis bajas. Sin embargo, al aumentar la dosis, se detectó una leve migración de células inflamatorias, sin signos clínicos, en el hígado e intestino grueso. Por otra parte, cuando se administró una sola dosis muy alta de boro, se observó un amplio edema, migración de células inflamatorias y neovascularización; clínicamente 2 de 6 ratas murieron dentro de 5 horas. Sugerimos que la ingesta de dosis muy altas de bórax pueden causar la muerte súbita, además la ingesta de dosis altas y durante periodos de tiempo prolongado puede causar enfermedades inflamatorias del intestino. Es recomendable que en los estudios relacionados con el boro, el tipo de boro así como su fuente sean evaluados cuidadosamente, eligiendo el compuesto más adecuado en caso de resultados erróneos.

Clinical implications of proliferation activity in T1 or T2 male gastric cancer patients

Proliferation activity has already been established as a prognostic marker or as a marker for anticancer drug sensitivity. In gastric cancer, however, the prognostic significance of proliferation activity is still being debated. Several studies evaluating proliferation activity using Ki-67 have shown controversial results in terms of the relationship between proliferation activity and overall survival (OS) or drug sensitivity in gastric cancer patients. Because cytoskeleton-associated protein 2 (CKAP2) staining has recently been introduced as a marker of proliferation activity, we analyzed 437 gastric cancer tissues through CKAP2 immunohistochemistry, and we evaluated the chromatin CKAP2-positive cell count (CPCC) for proliferation activity. Although the CPCC did not show any significant correlation with OS in the male, female or total number of cases, it did show a significant correlation in the T1 or T2 male patient subgroup, according to log-rank tests (P=0.001) and univariate analysis (P=0.045). Additionally, multivariate analysis with the Cox proportional hazard regression model showed a significant correlation between the CPCC and OS (P=0.039) for the co-variables of age, gender, T stage, N stage, histology, tumor location, tumor size and adjuvant chemotherapy. In male gastric cancer cell lines, faster-growing cancer cells showed higher sensitivity to cisplatin than slow-growing cells. Thus our study indicates that CPCC-measured proliferation activity demonstrates a significantly worse prognosis in T1 or T2 male gastric cancer patients. The CPCC will help to more precisely classify gastric cancer patients and to select excellent candidates for adjuvant chemotherapy, which in turn will facilitate further clinical chemotherapeutic trials.

Is Lipase Supplementation before a High Fat Meal Helpful to Patients with Functional Dyspepsia?

No abstract available.

Lipase Supplementation before a High-Fat Meal Reduces Perceptions of Fullness in Healthy Subjects

BACKGROUND/AIMS: Postprandial symptoms of fullness and abdominal discomfort are common after fatty meals. Gastric lipases hydrolyze 10% to 20% of dietary triglycerides during the stomach trituration period of digestion. The aim of this study was to evaluate the effects of acid-resistant lipase on upper gastrointestinal symptoms, including fullness and bloating, as well as on gastric myoelectrical activity after healthy subjects ingested a high-fat, liquid meal. METHODS: This study utilized a double-blind, placebo-controlled, crossover design with 16 healthy volunteers who ingested either a capsule containing 280 mg of acid-resistant lipase or a placebo immediately before a fatty meal (355 calories, 55% fat). Participants rated their stomach fullness, bloating, and nausea before and at timed intervals for 60 minutes after the meal. Electrogastrograms were obtained to assess the gastric myoelectrical activity. RESULTS: Stomach fullness, bloating, and nausea increased significantly 10 minutes after ingestion of the fatty meal (p<0.01), whereas normal gastric myoelectrical activity decreased and tachygastria increased (p<0.05). With lipase, reports of stomach fullness were significantly lower compared with placebo (p<0.05), but no effect on gastric myoelectrical activity or other upper gastrointestinal symptoms was observed. CONCLUSIONS: The high-fat meal induced transient fullness, bloating, nausea, and tachygastria in healthy individuals, consistent with post-prandial distress syndrome. Acid-resistant lipase supplementation significantly decreased stomach fullness.

Cicatrização gástrica com uso do extrato da Euphorbia Tirucalli L.: estudo em ratos / Gastric healing process with raw extract of Euphorbia tirucalli L.: study in rats

RACIONAL: A utilização de plantas na prevenção e no tratamento de doenças é prática milenar. O aveloz (Euphorbia tirucalli) é uma planta originária da África e tem sido relacionada com efeitos antimicrobiano, antiulceroso, anticarcinogênico, antivirais, cicatrizante, antihelmíntico e antisifilítico. OBJETIVO: Avaliar o uso do extrato bruto de Euphorbia tirucalli no processo de cicatrização de estômago de camundongo. MÉTODOS: Dezesseis camundongos da espécie Swiss, adultos, fêmeas foram submetidos à incisão longitudinal de 1 cm no corpo gástrico e síntese em plano único com pontos separados de polipropilene 6-0. Após o procedimento os animais foram distribuídos aleatoriamente em dois grupos de oito. Eles foram redistribuídos em quatro subgrupos: Aveloz (GA7) e Controle (GC7) com morte programada para 7º dia de pós-operatório e Aveloz (GA14) e Controle (GC14) com morte programada para 14º dia de pós-operatório. No seguimento o grupo GA utilizou-se 1 mL de solução hidroalcoólica do extrato bruto de Euphorbia tirucalli L. na concentração de 30 mg/ml por via oral através de gavagem e no GC, soro fisiológico 0,9%, no mesmo volume e via. Após a morte, foi realizado o inventário da cavidade abdominal e procedeu-se a retirada do estômago, fixação no formol e enviado para a análise microscópica. Na análise comparativa entre os dois grupos foram avaliados parâmetros macroscópicos e microscópicos da cicatrização. RESULTADOS: Não foram detectados sinais de peritonite, fístulas ou hematomas nos animal. Houve aderências do estômago, principalmente, com o fígado e omento, nos animais dos 7º e 14º dias do período pós-operatório nos dois grupos. A análise dos parâmetros histológicos não demonstrou diferença estatisticamente significante em nenhum dos parâmetros avaliados. CONCLUSÃO: A avaliação do uso do extrato bruto de Euphorbia tirucalli L. em cicatrização de lesões em estômago de camundogos mostrou equivalência em comparação ao grupo controle.

BACKGROUND: The use of plants in the prevention and treatment of disease is age-old practice. The aveloz (Euphorbia tirucalli) is a plant native of Africa and has been associated with antimicrobial, antiulcers, anticarcinogenic, antiviral, healing, anti-helminthic, antisiphilitic effects. AIM: To analyze the effect of the crude extract of Euphorbia tirucalli L. in the stomach healing process of mice. METHODS: Sixteen Swiss mice, adult females were subjected to 1 cm longitudinal incision in the gastric body and sutured with 6-0 polypropylene stitches. After the procedure, the animals were randomly divided into two groups of eight animals. These were redistributed into four subgroups: Aveloz (GA7) and Control (CG7) with programmed death for 7th day postoperatively and Aveloz (GA14) and Control (GC14) with programmed death for 14 days postoperatively. The group GA used 1 ml of hydroalcoholic solution of the crude extract of Euphorbia tirucalli at 30 mg/ml orally by gavage route and the CG, 0.9% saline solution at the same volume and route. After death, the inventory of the abdominal cavity was conducted and the stomach removal was performed, fixing in formalin and sent for microscopic analysis. In the comparative analysis between the two groups were evaluated the macroscopic and microscopic parameters of healing. RESULTS: There were no signs of peritonitis, fistulas or hematomas in the animals. There were adhesions of the stomach, especially with the liver and omentum in the animals at 7 and 14 days postoperatively in both groups. The analysis of histological parameters showed no statistically significant difference between groups in any of the parameters evaluated. CONCLUSION: The evaluation of the use of the crude extract of Euphorbia tirucalli L. on stomach wound healing in mice showed equivalence in comparison to the control group.

[ effect of diclofenac sodium injection on stomach of male rats]

Diclofenac sodium is a non-steroidal anti-inflammatory drug [NSAID]. It is widely used because of its analgesic, anti-inflammatory and antipyretic effects. The aim of this experimental study is to investigate the effects of intramuscular injection of diclofenac sodium in therapeutic and high doses for different periods on the stomach of rats. Forty young adult male albino rats ranging from 180-220 g body weight were used. They were divided into 5 groups of 8 animals for each. Group A and B were the control groups, they received intramuscular injection of normal saline for 7 and 14 weeks respectively. Group C received intramuscular injection of therapeutic doses of diclofenac sodium [2.2 mg/kg/day] for 7 weeks. Group D received therapeutic doses of diclofenac sodium intramuscularly for 14 weeks, while group E was administered intramuscular injection of high doses of diclofenac sodium [11 mg/kg/day] for 7 weeks. At the end of the experiment, the animals were sacrificed and the stomachs were obtained from all groups for light microscopic examinations. No changes were observed in stomachs of groups A, B and C, while in group D there were destruction of glandular architecture, damage of surface epithelium and submucosal blood vessels congestion. Group E reveals destruction and shedding of surface epithelium, necrosis in the gastric mucosa with mononuclear inflammatory cells infiltration, in addition to submucosal blood vessels congestion, edema and hemorrhage. Diclofenac sodium is safe and cause no gastric damage when administered intramuscularly as a single daily therapeutic dose in young adult rats for 7 weeks or less, but it causes gastric damage when the period of administration or the dose of the drug increase [i.e gastric damage depends on the period of exposure and the dose of the drug]

morphometeric study of the effects of ibuprofen on the stomach of albino rats under light microscope

To observe the effects of ibuprofen on the stomach of the albino rats under light microscope and its morphometeric analysis. A prospective experimental study. This study was conducted at the Department of Anatomy, Basic Medical Sciences Institute, Jinnah Postgraduate Medical Centre Karachi during 01.04.2008 to 31.05.2008. Thirty male adult albino rats were taken for the study and were divided into two groups containing 15 animals each. Each group was divided in to three sub groups according to the time of sacrifice i.e. 4,6 and 8 weeks. Group A served as control. Group B received ibuprofen at the dose of 70 mg per kilogram body weight per day orally with feed. After completion of respective period of treatment animals were sacrificed, abdomen was opened. The stomach was removed and opened along the greater curvature, divided into cardiac, body and pyloric parts and was fixed in Buffered neutral formalin for 24 hours. After that tissues were processed in ascending strength of alcohol, cleared in xylene and infiltrated and embedded with paraffin. Five micron thick sections were made on the rotatory microtome, were stained with Haematoxylin and eosin [for general morphology and morphometric study], and with Periodic Acid Schiff Orange-G [for the mucus content of the surface mucus cells and the mucus neck cells], randomly selected every seventh stained section, in three fields were studied. In stained sections of all parts of stomach the lining epithelium was disrupted, exfoliated, and ulcers and erosions were present. The erosive areas contained red blood cells and extended deep in to lamina propria. The results of mucosal thickness and the mean values of number of surface mucous cell count was moderately significant [P < 0.001] to highly significant [[P < 0.0001] in all parts of stomach when compared to control. The mucous content of the surface mucous cell in subgroups 'B'1, 'B'2 and 'B'3 of cardiac and pyloric parts were same marked [++++], while in body part of stomach it was moderate [+++] same as in control animals respectively. Based on present study, it is concluded that Ibuprofen induces gastric mucosal damage

Histological, biochemical and pharmacologycal characterization of the gastric muscular layer in Chagas disease / Caracterização histológica, bioquímica e farmacológica da musculatura gástrica na doença de Chagas

PURPOSE: To assess in vitro the correlation between the number of neurons and the sensitivity to cholinergic drugs and acetylcholinesterase activity in chagasic patients. METHODS: A 3x1 cm strip of the muscle layer of the anterior part of the stomach, always close to the angular incisure, was removed from 10 chronic chagasic patients (6 men) submitted to megaesophagus or megacolon surgery and from 10 non-chagasic patients (4 men) submitted to other types of surgery (control group), aged on average 52.3 and 50.1 years, respectively, for histological and pharmacological studies. The action of cholinergic drugs was investigated in isolated preparations according to the superfusion method of Ferreira and Costa, and acetylcholinesterase activity was determined by the method of Ellman. For neuron count, the strips were cut into 8 µm sections according to the method standardized by Alcântara. RESULTS: There was a difference in number of neurons between the chagasic (5,6) and control (7,3) groups. Acetylcholinesterase activity, in moles of hydrolyzed substrate per minute per gram tissue, was reduced in chagasic patients (4,32) compared to the controls (7,30). No hypersensitivity of the gastric musculature to cholinergic drugs was detected, with a reduced maximum response to carbachol and betanechol in the chagasic group. CONCLUSIONS: The reduction of neurons in the myenteric plexus of the stomach of chronic chagasic patients can be demonstrated even in the absence of clinical chagasic gastropathy. The hypersensitivity of the gastric musculature to cholinergic drugs probably depends on intense denervation. The reduced acetylcholinesterase activity demonstrates the involvement of the cholinergic innervation in the stomach of chronic chagasic patients. There was no correlation between number of neurons, sensitivity to cholinergic drugs and acetylcholinesterase activity in the gastric musculature of chagasic and non-chagasic patients.

OBJETIVO: Avaliar in vitro a correlação entre o número de neurônios e a sensibilidade a drogas colinérgicas e a atividade da acetilcolinesterase em pacientes chagásicos. MÉTODOS: Em 10 pacientes chagásicos crônicos (6 homens) submetidos à cirurgia de megaesôfago ou de megacólon e em 10 pacientes não chagásicos (4 homens) submetidos a outros tipos de cirurgia (grupo controle), respectivamente com idade média de 52,3 e 50,1 anos, retirou-se uma tira de 3x1 cm da camada muscular da parede anterior do estômago, sempre junto á cisura angular, que serviu para os estudos histológicos e farmacológicos. A ação de drogas colinérgicas foi feita em preparação isolada de acordo com o método de superfusão de Ferreira e Costa, e a determinação da atividade da acetilcolinesterase pelo método de Ellman. Para a contagem de neurônios a tira muscular foi submetida a cortes de 8 micra segundo método padronizado por Alcântara. RESULTADOS: Houve diferença do número de neurônios entre os grupos chagásico (5,6) e controle (7,3). A atividade da acetilcolinesterase mostrou-se diminuída nos chagásicos (4,32) expressa como número de moles do substrato hidrolisado por minuto por grama de tecido, em relação aos controles (7,30). Não se encontrou hipersensibilidade da musculatura gástrica a drogas colinérgicas, encontrando-se inclusive efeito máximo reduzido ao carbacol e betanecol no grupo chagásico. CONCLUSÕES: A redução de neurônios no plexo mioentérico do estômago de pacientes chagásicos crônicos pode ser demonstrada mesmo na ausência de gastropatia chagásica clínica. A hipersensibilidade da musculatura gástrica a drogas colinérgicas provavelmente depende de desnervação intensa. A redução da atividade da acetilcolinesterase demonstra o comprometimento da inervação colinérgica no estômago de pacientes chagásicos crônicos. Não houve correlação entre número de neurônios, sensibilidade a drogas colinérgicas e atividade da acetilcolinesterase na musculatura gástrica de pacientes chagásicos ou não chagásicos.

effect of Cedrus deodara root oil on the histopathology of rat stomach

The aim of this study was to observe the anti-ulcer effects of Cedrus deodara root oil on the rat's stomach and compare it with standard anti-ulcer drugs, femotidine and protonix. The study was conducted on 50 albino Wistar rats in three different doses i.e. 30, 40, and 50 mg/kg. The animals were divided into five groups, each group comprised of 10 rats [5 male and 5 female]. The oil was extracted from the plant root by dry destructive distillation method and the dose was calculated by dissolving 1.25 gms of Cedrus deodara in 25ml of 10% ethanol. The drugs were administered to the treated animals orally through feeding tube for two weeks. Animals received the dose of 50 mg cedar oil only, showed the healing effects on the mucosal epithelium of stomach, decreased inflammatory cells and granulation tissues on the submucosal layer upon histopathological examination. Therefore it may be concluded that Cedrus deodara root oil has anti-ulcerative effects and may be used in the management of gastrointestinal disorders particularly in peptic ulcer

Assessment of the stability of novel antibacterial triazolyl oxazolidinones using a stability-indicating high-performance liquid chromatography method

To evaluate the stability of 12 triazolyl oxazolidinone [TOZ] derivatives in simulated gastric and intestinal fluids as well as in human plasma at 37 +/- 1°C. A stability-indicating high-performance liquid chromatography [HPLC] procedure with a C8 column [250 +/- 40 mm, 5 micro m particle size] and a mobile phase of acetonitrile/H2O [50/50 v/v] at 1.0 ml/min was used. Accelerated stability studies were conducted at 37 +/- 1°C in 0.1 M HCl solution as simulated gastric fluid and in phosphate buffer solution [pH about 7.4] as simulated intestinal fluid. The stability of TOZs in human plasma at a simulated biological temperature of 37 +/- 1°C was evaluated as well. The stability studies indicated that the examined TOZs were stable in the above media, with the exception of compounds 1a [tert- butyl 4-[4-[[R]-5-[[1H-1,2,3-triazol-1-yl]methyl]-2-oxooxazolidin-3-yl]-2-fluorophenyl]piperazine-1-carboxylate] and 1b [tert-butyl 4-[2-fluoro-4-[[R]-5-[[4-methyl-1H-1,2,3-triazol- 1-yl]methyl]-2-oxooxazolidin-3-yl]phenyl] piperazine-1-carboxylate], which underwent degradation in simulated gastric fluid. The degradation kinetics revealed degradation parameters [kdeg, t1/2, t90] of 0.180 h-1, 3.85 h, and 0.58 h for 1a and of 0.184 h-1, 3.76 h and 0.57 h for 1b, respectively. Furthermore, the degradation products were identified by mass-spectrometric analysis at mass-to-charge ratios 347.5 and 361.5, respectively, and proton nuclear magnetic resonance analysis. With the exception of compounds 1a and 1b, the TOZs are stable in simulated gastric and intestinal fluids as well as in human plasma. Being carbamate derivatives, compounds 1a and 1b underwent fast and complete degradation in simulated gastric fluid. The obtained results should be considered for future studies of formulation of structurally related TOZs in oral dosage forms

Carcinogenesis of the upper gastrointestinal tract induced by N-methyl-N'-nitro-nitrosoguanidine and reflux of duodenal contents in the rat / Carcinogênese do trato gastrointestinal alto induzida pelo N-methyl-N'-nitro-nitrosoguanidina e pelo refluxo duodenogástrico no rato

PURPOSE: To investigate the combined effects of reflux of duodenal contents through the pylorus and treatment with N-methyl-N'-nitro-nitrosoguanidine (MNNG) on the development of lesions in the glandular stomach, at the gastrojejunal anastomosis and in the forestomach of rats. METHODS: Eighty Male Wistar rats were divided into 4 groups: G1: MNNG + Reflux, G2: Reflux, G3: MNNG and G4: Gastrostomy. MNNG was given in the drinking water (100 mg/ml) for 12 weeks and then two groups (G1 and G2) were submitted to a gastrojejunal anastomosis followed by section of the afferent loop and suture of both stumps to allow reflux of duodenal contents through the pylorus. The animals were sacrificed 18 and 36 weeks after surgery. The lesions obtained in the antral mucosa, at the gastrojejunal anastomosis and in the forestomach were analysed histologically. RESULTS: Duodenal reflux induced proliferative lesions at both glandular and squamous mucosa of the stomach. In the antrum, adenomatous hyperplasia (AH) was observed in 20% and 50% of the animals at the 18th and 36th weeks respectively. Aditionally 85% of the animals presented AH at the gastrojejunal anastomosis and 60% developed squamous hyperplasia at the squamous portion of the stomach. MNNG treatment plus duodenal reflux enhanced the development of malignant tumors at both glandular and squamous mucosa, since there were 30% of antral adenocarcinomas and 45% of squamous carcinomas at the 18th week and the frequency of these malignant tumors rose to 50% in the antrum and 65% in the squamous mucosa at the 36th week. CONCLUSION: The reflux of duodenal contents through the pylorus enhanced the development of proliferative lesions, benign and malignant, in the glandular stomach and in the forestomach of rats.

OBJETIVO: Investigar os efeitos do refluxo duodenogástrico e sua interação com o cancerígeno químico N-methil-N'-nitro-nitrosoguanidina (MNNG) no desenvolvimento de lesões no estômago glandular, anastomose gastrojejunal e no estômago escamoso do rato. MÉTODOS: Foram utilizados 80 ratos Wistar divididos em 4 grupos: G1: MNNG + Refluxo, G2: Refluxo, G3: MNNG e G 4: Gastrostomia. O MNNG foi oferecido na água de beber (100mg/ml) por 12 semanas. A seguir foi feita anastomose gastrojejunal na porção glandular do estômago nos grupos G1 e G2, com secção da alça aferente junto ao estômago e sutura de ambos os cotos para permitir o refluxo do conteúdo duodenal para o estômago pelo piloro. Os animais foram sacrificados 18 e 36 semanas após a cirurgia. As lesões identificadas foram submetidas à exame histopatológico. RESULTADOS: O refluxo duodenogástrico levou ao desenvolvimento de lesões proliferativas no estômago glandular e na porção escamosa. No antro, hiperplasia adenomatosa (HA) foi diagnosticada em 20 e 50% dos animais (G2) na 18ª e 36ª semanas, respectivamente. Na anastomose gastrojejunal 85 por cento dos animais (G2) apresentaram HA e 60% apresentaram hiperplasia escamosa no estômago escamoso, na 36ª semana. No grupo MNNG+Refluxo foram identificados na 18ª semana, 30% adenocarcinomas no antro e 45%carcinomas escamosos. A freqüência destas lesões malignas aumentou, respectivamente, para 50% e 65% na 36ª semana. CONCLUSÃO: O refluxo duodenogástrico potencializou o desenvolvimento de lesões proliferativas benignas e malignas no estômago glandular e em sua porção escamosa, no rato.