Bioavailability augmentation of silymarin using natural bioenhancers: An in vivo pharmacokinetic study

Abstract Pharmacokinetic studies were carried out in male and female rats to quantify silymarin as silybin (A+B) after the oral administration of various silymarin formulations combined with three bioenhancers, namely, lysergol, piperine, and fulvic acid, and compared with plain silymarin formulation (control). A non-compartmental analysis, model independent analysis, was utilized, and various pharmacokinetic parameters (C max, T max, and AUC 0-t) were calculated individually for each treatment group, and the values were expressed as mean ± SEM (n = 6). Plasma samples obtained from the rats were analyzed for the concentration of silymarin through a validated RP-HPLC method and on the basis of data generated from the pharmacokinetic studies. Results indicated that the bioenhancers augmented pharmacokinetic parameters and bioavailability increased 2.4-14.5-fold in all the formulations compared with the control. The current work envisages the development of an industrially viable product that can be further subjected to clinical trials and scientifically supports the development of silymarin as a contemporary therapeutic agent with enhanced bioavailability and medicinal values.

HPLC quantitative analysis of protocatechuic acid contents in 11 Phellinus mushroom species collected in Thailand

Abstract Phellinus mushrooms have been traditionally used for various medicinal purposes. Protocatechuic acid, which was previously reported to be a component in some Phellinus mushrooms, has some pharmacological effects. This study aimed to validate a HPLC method for the quantitative analysis of the protocatechuic acid contents in the extracts from different Phellinus mushroom species collected in Thailand. HPLC was carried out using a C18 column and the gradient mobile phases of 0.1% formic acid in water and 0.1% formic acid in acetonitrile. Method validation was performed to assure the linearity, accuracy, precision, limit of detection and limit of quantitation of the analytical method. The linearity range of protocatechuic acid was 1 - 10 µg/ml. The average recovery was 104.16%. The method was shown to be precise with the RSD of repeatability and intermediate precision at less than 3%. The protocatechuic contents in 11 Phellinus mushrooms were in the range of less than 0.0099 - 0.4121 %w/w of the extract. The developed HPLC method was reliable and suitable for the quantitative analysis of protocatechuic acid content in Phellinus mushrooms.

Acrocarpus fraxinifolius Wight and Arn. Bark; phenolics, toxicity studies, antioxidant and anti-inflammatory activities

The purpose of the survey was to determine acute & chronic toxicity; in vivo antioxidant and anti-inflammatory actions of the different extracts of A. fraxinifolius Wight and Arn bark; along with estimation of the phenolic, flavonoidal contents and investigation of phenolic metabolites that may attribute to the activities. LD50 of the total ethanol extract (TEE) was 7.1 g/kg b. wt, the radical scavenging activity of DPPH showed 60.31% inhibition, FRAP ability and ABTS+ activity showed 55.024 and 67.217 µmol Trolox/100 g dry weight, respectively. TEE followed by ethyl acetate extract (EAE) at 100 mg/kg b.w exhibited the highest in vivo antioxidant activity (94.51% and 91.08% potency, respectively) compared with Vit E (100%). The TEE & EAE exhibited the highest anti-inflammatory activity (3.81±0.08 & 3.79±.0.04) respectively in comparison with indomethacin 3.83±0.01 measured as edema diameter after 4 hours of extract administration. The total phenolic and total flavonoid contents in the total ethanol extract (TEE) estimated as gallic acid and catechin equivalents were 61.06± 0.08 µg eq GA/g, 40.33± 0.20 µg CE/g extract respectively. EAE revealed five phenolic acids and eight flavonoid compounds isolated for the first time from the plant

In vitro evaluation of the microhardness of bovine enamel exposed to acid solutions after bleaching

Acid erosion is a superficial loss of enamel caused by chemical processes that do not involve bacteria. Intrinsic and extrinsic factors, such as the presence of acid substances in the oral cavity, may cause a pH reduction, thus potentially increasing acid erosion. The aim of this study was to evaluate the microhardness of bleached and unbleached bovine enamel after immersion in a soda beverage, artificial powder juice and hydrochloric acid. The results obtained for the variables of exposure time, acid solution and substrate condition (bleached or unbleached enamel) were statistically analyzed by the ANOVA and Tukey tests. It was concluded that a decrease in microhardness renders dental structures more susceptible to erosion and mineral loss, and that teeth left unbleached show higher values of microhardness compared to bleached teeth.

Surface and subsurface erosion of primary enamel by acid beverages over time

This study evaluated the influence of a cola-type soft drink and a soy-based orange juice on the surface and subsurface erosion of primary enamel, as a function of the exposure time. Seventy-five primary incisors were divided for microhardness test (n=45) or scanning electron microscopy (SEM) analysis (n=30). The specimens were randomly assigned to 3 groups: 1 - artificial saliva (control); 2 - cola-type soft drink; and 3 - soy-based orange juice. Immersion cycles in the beverages were undertaken under agitation for 5 min, 3 times a day, during 60 days. Surface microhardness was measured at 7, 15, 30, 45 and 60 days. After 60 days, specimens were bisected and subsurface microhardness was measured at 30, 60, 90, 120, 150 and 200 µm from the surface exposed. Data were analyzed by ANOVA and Tukey’s test (a=0.05). Groups 2 and 3 presented similar decrease of surface microhardness. Regarding subsurface microhardness, group 2 presented the lowest values. SEM images revealed that after 60 days the surfaces clearly exhibited structural loss, unlike those immersed in artificial saliva. It may be concluded that erosion of the surfaces exposed to the cola-type soft drink was more accentuated and directly proportional to the exposure time.

Este estudo avaliou a influência de um refrigerante a base de cola e um suco de laranja a base de soja na erosão da superfície e subsuperfície do esmalte do dente decíduo, em função do tempo de exposição. Setenta e cinco incisivos decíduos foram divididos para o teste de microdureza (n=45) ou para a análise em microscópio eletrônico de varredura (MEV) (n=30). Os espécimes foram alocados aleatoriamente em 3 grupos: I - saliva artificial (controle); II - refrigerante a base de cola; e III - suco de laranja a base de soja. Ciclos de imersão nas bebidas foram realizados sob agitação durante 5 min, 3 vezes ao dia, durante 60 dias. A microdureza superficial foi mensurada aos 7, 15, 30, 45 e 60 dias. Após 60 dias, os espécimes foram seccionados e a microdureza subsuperficial foi mensurada aos 30, 60, 90, 120, 150 e 200 μm. Os dados foram analisados pelos testes ANOVA e Tukey (α=5 por cento). Os grupos II e III apresentam uma diminuição similar da microdureza superficial. O grupo II apresentou menores valores de microdureza subsuperficial. As imagens de MEV revelaram que após 60 dias as superficies mostraram perdas de estruturas claramentes identificadas, diferentemente das superfícies imersas em saliva artificial. Pode-se concluir que a erosão das superficies expostas ao refrigerante a base de cola foi mais acentuada e diretamente proporcional ao tempo de exposição à bebida.

[ effect of pH on the erosive potential of Iranian and imported soft drinks using atomic absorption spectrophotometry]

An increase in pH can affect the erosive potential of soft drinks, but the possible role of calcium salts and phosphate has not been fully recognized. The aim of the present investigation was to evaluate the effect of pH on the erosive potential of soft drinks on permanent tooth enamel. This experimental in vitro study was performed on 8 beverages and 240 intact premolars extracted for orthodontic purposes. Two Iranian soft drinks [Cola and Orange Zamzam] and 2 imported ones [Pepsi and Mirinda] constituted the case group and 4 solutions with the same pH served as the control group. The teeth were divided into 3 groups [A, B and C] and further subdivided into 8 subgroups and immersed in 20 ml of one of the 8 beverages for 15 minutes [A], 45 minutes [B] and 12 hours [C]. The amount of Ca[++] released in each soft drink or solution was estimated by AA-spectrophotometry at the end of each exposure time. A statistically significant difference was found in the extent of erosion between the case and control groups which increased with exposure time [P<0.001]. The pattern of Ca[++] concentration changes were similar in both study groups [p=0.3915], but the case group revealed a higher erosive potential than the control group [P<0.001]. The percentage of titratable acids seems to have a greater effect on the erosive potential of beverages when compared to pH. Measuring pH alone could not accurately estimate the erosive potential of different soft drinks

Extraesophageal manifestations associated with gastroesophageal reflux

Approximately 25 per cent of the patients with gastroesophageal reflux disease (GERD) present only extraesophageal manifestations. GERD may be defined as clinical manifestations and tissue lesions associed to gastroesophageal reflux. GERD results from excessive exposure of the mucosa to aggressors, prominently acid and pepsin, associated with diminished esophageal defense mechanisms. This review aims to characterize extraesophageal GERD symptoms. Most patients with reflux-related otolaryngologic symptoms present relatively preserved motor function and esophageal clearance, but exhibit poor upper esophageal sphincter function, which leads to a "high" (pharyngeal) symptom. Acidification in the distal esophagus is likely to activate vagovagal reflexes. These reflexes. These reflexes also induce respiratory symptoms and bronchoconstriction. Nonspecific laryngitis, granuloma, posterior comissure hypertrophy, cricoarytenoid arthritis and come cases of globus pharyngeus have been attributed to larynx and pharynx irritations produced by repeated GER episodes. Otolaryngologic patients with reflux respond better to treatment than those patients whose symptoms are typically gastrointestinal.

Reaçäo pulpar aos condicionadores ácidos / Pulp responses induced by acid etchants

O efeito de materiais restauradores colocados em contato e a 1 mm da polpa dental foi avaliado. Essa análise foi realizada em polpas inflamadas onde foi feita induçäo de cárie e em polpas sadias. Os materiais usados foram os adesivos dentinários One Step de quinta e última geraçäo, o Scotchbond Multi-Uso Plus e o Acido Poliacrílico. A biocompatibilidade desses materiais na estrutura pulpar foi mostrada por meio de análise histológica. Constatou-se que a agressäo pulpar é uma evidência histológica independentemente ou näo da presença de bactérias e do contato ou näo com a polpa. Os resultados mostraram que todos os materiais possuem potencial irritativo à polpa. Em ordem crescente de agressividade podem ser assim dispostos: One Step, ácido poliacrílico e o Scotchbond Multi-Uso Plus. O uso de tais produtos podem levar a problemas clínicos como perda da vitalidade pulpar

Análise comparativa, ao microscópio eletrônico de varredura, de esmalte bovino exposto a diferentes soluçöes ácidas: um estudo in vitro / Scanning electron microscopy analysis of bovine enamel exposed to different acid solutions: an in vitro study

O presente estudo teve por objetivo analisar as possíveis alteraçöes ocorridas na superfície de esmalte bovino, hígido ou desmineralizado, exposto por 40 minutos à Coca-cola em fórmula original, ao suco de limäo diluído em água destilada na razäo 1:5 e ao suco de laranja natural integral (Parmalat). Com esse fim, 40 blocos de esmalte bovino de 16 mm² foram previamente limpos com pedra-pomes e água destilada, em baixa rotaçäo. Desse total, 20 foram artificialmente descalcificados. Tanto os blocos hígidos quando os descalcificados foram colocados 6 a 6 em dispositivos de cera, perfazendo um total de 3 dispositivos com 6 blocos de esmalte hígido (Grupo I) e 3 dispositivos com 6 blocos de esmalte descalcificado (Grupo II). Análises comparativas ao Microscópio Eletrônico de Varredura demonstraram que o suco de limäo foi o responsável por padröes de erosäo mais acentuados, seguido pela Coca-cola e pelo suco de laranja, tanto no esmalte hígido quanto no desmineralizado. Os resultados evidenciam o potencial erosivo do suco de limäo, da Coca-cola e do suco de laranja

Erosäo dental: estudo "in vitro" da erosäo causada por refrigerantes e suco de limäo no esmalte de dentes decíduos humanos: análises bioquímicas / Dental erosion: \"in vitro\" study of erosion caused by soft drinks and lemon juice on the enamel deciduous teeth: biochemical analysis

A erosäo dental provocada "in vitro" pelo suco de limäo e por refrigerantes do tipo Cola e Guaraná sobre o esmalte de dentes decíduos humanos, foi analisada sob parâmetros bioquímicos. Períodos de incubaçäo variáveis de 15 e 45 minutos e de 3, 6, 9, e 12 horas foram utilizados. As análises bioquímicas dos produtos testados para incubaçäo dos dentes decíduos incluíram a determinaçäo de seus pHs, a espectrofotometria de absorçäo atômica para determinaçäo das concentraçöes de cálcio e a Colorimetria de Fiske & Subbarow para determinaçäo das concentraçöes do fosfato inorgânico, íons estes liberados a partir da dissoluçäo da hidroxiapatita dental humana. Os pHs médios dos produtos foram respectivamente 2,50, 2,60 e 3,30, para o suco de limäo, refrigerante tipo Cola e Guaraná. A acidez demonstrada pelos produtos näo foi modificada pela incubaçäo dos dentes. Todos os produtos testados demonstraram ser potencialmente erosivos, sendo que o suco de limäo causou as maiores perdas de cálcio e fosfato inorgânico pelos dentes incubados, seguido pelo refrigerante tipo Cola e pelo Guaraná. Foi observada uma relaçäo direta entre o aumento do tempo de incubaçäo dos dentes e a perda iônica sofrida pelos mesmos. Näo foi encontrada uma relaçäo de proporcionalidade entre os íons cálcio e fosfato inorgânico perdidos

histological and ultrastructural study on the effects of aquarium - acidity on the liver of the catfish, clarias lazera

This study assessed the adverse effects of aquarium - acidity [pH = 4] on the histology and ultrastructure of the liver of the lover of the catfish, Clarias lazera after 2, 5 and 7 days of exposure. In fish inhabiting the acidified water for 2 days, venous congestion was prevalent in the liver tussue and liver cell cytoplasm became glassy and less eosinophilic. The nuclei of such cells displayed dense basophilic stainability. In fish inhabiting acidified water for 5 days, paraffin sections of the liver showed lymphocytic infiltration. The hepatocytes displayed mottled stainability and a number of vacuoles appeared in the cytoplasm of some liver cells. Some liver cells were necrotic, lysed and their nuclei displayed deformity or pyknosis. Ultrastructurally, some mitochondria became elongated and displayed irregular contours. The endoplasmic reticulum showed mild fragmentation. Increased fat vacuoles of different sizes appeared in the cytoplasm. Some liver cell nuclei were deformed. In fish inhabiting acidified water for 7 days, paraffin sections showed that some liver cells were severely dissociated, lysed and necrotic. A number of liver cell nuclei were deformed or pyknotic. Lymphocytic infiltration and venous congestion were pronounced. In electron micrographs of the liver,certain areas of the cytoplasm of the liver cells were electron - lucent and structureless. The endoplasmic reticulum was severely fragmented into large number of small vesicles. Besides the increased fat vacuoles, the ground cytoplasm showed hydropic degeneration and the mitochondira exhibited bizzare shapes

Erosäo dental: estudo in vitro da erosäo causada por refrigerantes e suco de limäo no esmalte de dentes decíduos humanos: análises morfológicas / Dental erosion: an \"in vitro\" study caused by soft beverages and lemon juice on the enamel of human deciduous teeth: morphological analysis

A erosäo in vitro provocada por refrigerantes do tipo Coca-Cola e guaraná e por um suco de limäo enlatado sobre o esmalte de dentes decíduos humanos, foi analisada sob parâmetros morfológicos. Períodos de incubaçäo variáveis de 15 e 45 minutos e de 12 horas foram utilizados. As análises morfológicas do esmalte afetado pela açäo dos produtos incluiram a estereomicroscopia e a microscopia optica comum, de luz transmitida, tendo sido demonstrado claramente o efeito prejudicial dos produtos testados sobre o esmalte decíduo humano. A estereomicroscopia demonstrou perda do brilho e alteraçäo da coloraçäo normal do esmalte, com perdas irregulares do tecido dental em graus variáveis, as quais agravaram-se com o aumento no tempo de incubaçäo dos dentes. A microscopia optica comum, de luz transmitida demonstrou alteraçöes do tipo erosäo dental no perfil da superfície do esmalte dos dentes analisados, com diferentes graus de profundidade. O aumento do tempo de incubaçäo causou um agravamento das características adquiridas pelo perfil do esmalte, em todos os produtos testados. O suco de limäo foi o produto que demonstrou maior potencial erosivo sobre o esmalte dental decíduo humano, seguido pela Coca-Cola e depois pelo guaraná

Condicionamento ácido do esmalte: estudo pela microscopia eletrônica de varredura / Acid conditioned dental enamel: electron scanning microcospic study

O propósito deste trabalho foi a comprovaçäo das descalcificaçöes seletivas do esmalte dental, dentro dos padröes já determinados. Analisando-se 72 fotomicrografias obtidas pelo MEV, das superfícies de esmalte condicionadas pelos ácidos do Adaptic, Esticid e Simulate, foi possível estabelecer porcentagens de cada padräo obtido: 53 por cento para o padräo tipo I, 18 por cento para o tipo II e 29 por cento para o tipo III

Queimadura dos olhos por cáusticos: rotina de atendimento

A recuperaçäo das estruturas oculares lesadas por substâncias cáusticas, alcalinas ou ácidas, depende essencialmente da rapidez do atendimento e da terapia específica para cada caso. As queimaduras por álcalis säo sabidamente mais freqüentes e muito mais graves. Säo apresentadas, em forma de gráficos de fácil manuseio, as etapas que devem ser seguidas para cada um dos casos destas queimaduras oculares