Equivalencia terapéutica in vitro de tabletas de enalapril maleato 20 mg de producción nacional / In vitro therapeutic equivalence of 20 mg enalapril maleate tablets of national production

Los ensayos de equivalencia terapéutica tienen como objetivo demostrar que los medicamentos genéricos aportan la misma cantidad de principio activo en comparación con el medicamento innovador. El objetivo de la investigación fue evaluar la equivalencia terapéutica del medicamento enalapril maleato en tabletas de 20 mg, según la clasificación biofarmacéutica que le corresponde, ya que este es un medicamento representativo de la clase III, para demostrar que tienen un perfil de tolerabilidad adecuado y que son eficaces para su prescripción médica. Por otro lado, al demostrarse la equivalencia terapéutica se puede recurrir con toda seguridad al medicamento genérico y reducir los costos de los tratamientos, con lo cual la población tendrá una oferta de medicamentos confiables, seguros y a precios económicos. Se utilizó un medicamento innovador y tres de los ocho medicamentos genéricos de fabricación y comercialización nacional, a los cuales se les determinó perfiles de disolución (F2: 45.41, 92.42, 71.04), uniformidad de contenido (AV: 7.37, 2.97, 2.50) y valoración de principio activo (%: 107.14, 98.89, 101.71) para determinar la cantidad de principio activo en las muestras. Los análisis se realizaron con base en los criterios establecidos en la Farmacopea de los Estados Unidos. Se aplicó un modelo estadístico independiente, y se estableció que dos de los tres lotes analizados de los medicamentos genéricos son equivalentes terapéuticos con el lote del medicamento innovador. Con las pruebas de disolución in vitro realizadas a lo largo de este estudio, se puede concluir que los tres lotes analizados de dos medicamentos genéricos pueden ser considerados intercambiables con respecto al lote del medicamento innovador.

The therapeutic equivalence essays to demonstrate that generic medicine can provide the same amount of active ingredient compared to the innovative medicine. The objective of this research was to evaluate the therapeutic equivalence of enalapril maleate 20 mg, according to the biopharmaceutical classification, given that this is a representative class III drug. This to demonstrate that it has an acceptable tolerability profile and that it is effective for medical prescription. Once the therapeutic equivalence is stablished, the use of therapeutic bioequivalence products can reduce treatment costs, so that the general public can have access to reliable, safe and affordable medicines. For this study an innovative medicine and three of the eight generic medicines of national manufacture and commercialization were used for each medicine, the dissolucion profiles (F2: 45.41, 92.42, 71.04), the uniformity of content (AV: 7.37, 2.97, 2.50) and percentage of active ingredient (%: 107.14, 98.89, 101.71) were determined. The essays were performed based on the criteria established in The United States Pharmacopeia and were satisfactory in all the analyzed batches. An independent statistical model was carried out it was established, that two of the three analyzed batches for generic medicine are therapeutic equivalents with the batch of the innovative drug. In vitro dissolution tests obtained throughout this study, concluded that the three analyzed batches of two generic medicines can be considered interchangeable in respect to the batch of the innovative medicine.

The Medicinal Usage and Restriction of Ginseng in Britain and America, 1660–1900 / 의사학

This article demonstrates the medicinal usage of ginseng in the West from 1660 to 1914. Asian[Korea] ginseng was first introduced into England in the early 17th century, and North American ginseng was found in the early 18th century. Starting from the late 17th century doctors prescribed ginseng to cure many different kinds of ailments and disease such as: fatigue general lethargy, fever, torpidity, trembling in the joints, nervous disorder, laughing and crying hysteria, scurvy, spermatic vessel infection, jaundice, leprosy, dry gripes and constipation, strangury, yellow fever, dysentery, infertility and addictions of alcohol, opium and tobacco, etc. In the mid-18th century Materia Medica began to specify medicinal properties of ginseng and the patent medicines containing ginseng were widely circulated. However, starting in the late 18th century the medicinal properties of ginseng began to be disparaged and major pharmacopoeias removed ginseng from their contents. The reform of the pharmacopoeia, influenced by Linnaeus in botany and Lavoisier in chemistry, introduced nomenclature that emphasized identifying ingredients and active constituents. Western medicine at this period, however, failed to identify and to extract the active constituents of ginseng. Apart from the technical underdevelopment of the period, the medical discourses reveal that the so-called chemical experiment of ginseng were conducted with unqualified materials and without proper differentiation of various species of ginseng.

Bioinformatics Analysis on Proteomics of Rat Bone Marrow Mesenchymal Stem Cells Intervened by Active Principle Region of Yang-Xin Tong-Mai Formula / 世界科学技术-中医药现代化

This study was aimed to analyze the bioinformatics of proteomics of rat bone marrow mesenchymal stem cells (MSCs) intervened by active principle region of Yang-Xin Tong-Mai Formula (apr-YTF). The latest versions of bioinformatics tools including DAVID (http://david.abcc.ncifcrf.gov/) and GO (http://www.geneontology.org/) were combined to assign a precise function to rat bone marrow MSCs intervened by apr-YTF. KEGG and VISANT were assigned with a precise function to rat bone marrow MSCs intervened by apr-YTF. The results showed that a total of 102 biological processes were mainly involved, with 35 cellular components and 6 molecular functions. These proteins interacted in 3 signal transduction pathways. It was concluded that the following proteins and signal transduction pathways played an important role in the process of apr-YTF inducing BMSCs differentiation into cardiomyocytes. Presenilin-1 and Presenilin-2 were in the Notch signaling pathway. And syntaxin-4 protein was in soluble N-ethylmaleimide sensitive fusion protein attachment protein (SNARE). The apr-YTF played a role on MSCs from multiple sites, with multiple links through different biological processes. The bioinformatics of proteomics can predict action mechanism of traditional Chinese medicine (TCM) from the holism concept. The validation in combination with molecularbiology was a good way for TCM modernization.

Regulation of Acrylamide Induced µ-Class Glutathione-S-Transferases in Mice Testis by the Treatment of Hybanthus Enneaspermus Active Principles.

The present study was aimed to analyse the effect of acrylamide and Hybanthus enneaspermus leaf extract active principles on mice testis glutathione-s-transferases (GST; EC 2.5.1.18). These enzymes play a role in biotransformation of electrophilic compounds that cause damage to cells by conjugating with the substrate glutathione. Hybanthus enneaspermus, a spade flower, is an erect shrub of violaceae family, having free radical scavenging activity. Acrylamide is a known neurotoxicant that cause damage to almost all cells including liver, testis, brain and kidney. The GSTs purified from mice testis using glutathionyl linked agarose affinity chromatography were analyzed by using SDS-PAGE and were resolved into four sub units i.e. Yc, Yb, Yβ &Yδ. Also these subunits expression were confirmed by western blot analysis. During experimentation to analyze the effect of Hybanthus enneaspermus active principle (HE) mice were subjected to both acrylamide (AC) and also mixture of HE and AC. This exposure significantly altered the specific activity of mice GSTs in testis. Polyclonal antibodies produced against purified GSTs of mice testis on immunoblot analysis showed significant increase of μclass GSTs (Yb & Yβ) based on dose and time dependent manner. Therefore the present research of Hybanthus enneaspermus treatment on mice testis showed that, regulation of synthesis of μ-GSTs was depending on the dose of acrylamide concentration and also the active principles of HE. Hence it is proposed that μ-GSTs may be used as tumour markers for testis carcinoma, since their production is variable due to the increased dose concentration of synthetic chemical acrylamide and its regulation by plant product, HE.

Study on anticancer active principle in lignum Caesalpinia sappan / 肿瘤研究与临床

Objective To search for the anticancer active substance from Caesalpinia sappan wood extractions. Methods Crude extracts were extracted from Caesalpinia sappan wood with different solvents.Liquid chromatography was applied to analyze the content of each essential component in the extraction fractions. Trypan blue exclusion test was performed to detect the growth suppression rate of human bladder carcinoma cell line T24 treated by the extraction fractions at different time course (20,40,60,80,100 min).The main component positively correlated with the cell suppression rate was separated out using repeated chromatography, thus the anticancer active monomer was obtained, with purity over 98 ％. The chemical constitution was determined using NMR (nuclear magnetic resonance), mass spectrum and infrared spectrum methods. T24 cell line, human ovarian cancer cell line SKOV3, mice sarcoma S180 and hepatic carcinoma H22 cell were chosen as target subjects, with mitomycin, hydroxycamptothecin as positive control drug, the inhibitory activity of the monomer was tested by trypan blue chromophobia method. Results Among the extraction fractions, R12 has a positive correlation with the cell suppression rate (r100 min=0.941, P＜0.001).Brazilin is the key component in R12.The inhibition rate of brazilin could reach 90.89 ％,98.65 ％,99.82 ％ and 100.00 ％ on T24,SKOV3,S180 and H22 respectively in 40 min at the concentration of 1.2 mg/ml,and its effect is much superior to that of the control drug mitomycin and hydroxycamptothecin. Conclusion Brazilin is one of the essential anticancer principles in Caesalpinia sappan wood.

Determinação de óleos essenciais de alfavaca (Ocimum gratissimum L. ), orégano (Origanum vulgare L. ) e tomilho (Thymus vulgaris L.) / Determination of essential oils of basil (Ocimum gratissimum L. ), oregano (Ocimum gratissimum L. ) and thyme (Thymus vulgaris L.)

O presente trabalho teve como objetivo a caracterização de plantas frescas e secas (comerciais) de alfavaca, orégano e tomilho, a obtenção dos óleos essenciais através do método de arraste a vapor e a quantificação dos compostos químicos por CG/EM. As plantas frescas e as secas comerciais foram submetidas às análises de umidade, extrato etéreo, proteína, fibra bruta, cinzas, extrato não nitrogenado, valor calórico, teor de óleo essencial e identificação dos compostos majoritários através da cromatografia gasosa-espectrometria de massas. Dentre a caracterização obtida os resultados na base seca mostraram-se promissores, sendo o teor de proteína e de cinzas na alfavaca seca comercial com 17,34 g 100 g-1 e 8,12 g 100 g-1, respectivamente; a fibra bruta no orégano seco comercial com 15,65 g 100 g-1; o extrato etéreo, o extrato não nitrogenado e o valor calórico no tomilho seco comercial com 9,30 g 100 g-1, 52,72 g 100 g-1 e 356,74 Kcal 100 g-1, respectivamente. Obteve-se o maior rendimento de óleo essencial na alfavaca seca comercial com 1,02%, enquanto a alfavaca fresca apresentou o menor rendimento, com apenas 0,13%. Na alfavaca fresca encontrou-se 87,38% de eugenol e 6,27% de timol, enquanto na alfavaca seca comercial observou-se redução no eugenol (71,12%) e aumento do timol (13,28%). No orégano fresco foram quantificados quatro picos o γ-terpineno (33,45%), 4-terpineol (25,59%), timol (14,21%) e carvacrol (2,30%). Já no óleo essencial de orégano seco comercial houve redução no γ-terpineno (28,73%) e aumento no 4-terpineol (27,58%), timol (19,71%) e carvacrol (3,67%). No óleo essencial do tomilho fresco foram quantificados três picos o borneol (66,66%), timol (13,41%) e linalol (3,24%). Por outro lado, no óleo essencial do tomilho seco comercial houve redução no borneol (37,90%) e aumento no timol (20,61%) e linalol (10,34%). Pode-se concluir que as folhas secas comerciais analisadas de alfavaca, orégano, e tomilho apresentam potencial para o enriquecimento dos alimentos ou para a obtenção dos óleos essenciais.

This study aimed to characterize commercial fresh and dry medicinal plants (basil, oregano and thyme), to obtain essential oil by the steam distillation method and to quantify chemical compounds by means of GC/MS. The fresh and dry plants were subjected to the following analyses moisture, ether extract, protein, crude fiber, ash, non-nitrogenous extract, caloric value, essential oil content and identification of major compounds by gas chromatography-mass spectrometry. Considering the obtained characterization, the following results on dry basis proved promising: protein and ash content in commercial dry basil with 17.34 g 100 g-1 and 8.12 g 100 g-1, respectively; crude fiber in commercial dry oregano with 15.65 g 100 g-1; ether extract, non-nitrogenous extract and caloric value in commercial dry thyme with 9.30 g 100 g-1, 52.72 g 100 g-1 and 356.74 Kcal 100 g-1, respectively. The highest essential oil yield was obtained for commercial dry basil with 1.02% and the lowest yield was obtained for fresh basil with only 0.13%. Chromatography indicated 87.38% eugenol and 6.27% thymol in fresh basil. For commercial dry basil, the chromatogram showed a reduction in eugenol (71.12%) and an increase in thymol (13.28%). Four peaks were quantified for fresh oregano the γ-terpinene (33.45%), 4-terpineol (25.59%), thymol (14.21%) and carvacrol (2.30%). For the essential oil of commercial dry oregano, there was a decrease in γ-terpinene (28.73%) and an increase in 4-terpineol (27.58%), thymol (19.71%) and carvacrol (3.67%). In the chromatogram of the essential oil of fresh thyme, three peaks were quantified: borneol (66.66%), thymol (13.41%) and linalool (3.24%). On the other hand, in the chromatogram of the essential oil of commercial dry thyme, there was a decrease in borneol (37.90%) and an increase in thymol (20.61%) and linalool (10.34%). It can be concluded that commercial dry leaves of basil, oregano and thyme are feasible to enrich foods or to obtain essential oils.

Could the products of Indian medicinal plants be the next alternative for the treatment of infections.

Indian medicinal plants are now recognized to have great potential for preparing clinically useful drugs that could even be used by allopathic physicians. Traditionally, practitioners of Indian medicine have used plant products in powder, syrup or lotion forms, without identification, quantification and dose regulation, unlike their allopathic counterparts. The present review explores the immense potential of the demonstrated effect of Indian medicinal plants on microbes, viruses and parasites. In the present context, with the available talent in the country like pharmaceutical chemists, microbiologists, biotechnologists and interested allopathic physicians, significant national effort towards identification of an "active principle" of Indian medicinal plants to treat human and animal infections should be a priority.

Current status of Indian medicinal plants with antidiabetic potential：a review

In India, indigenous remedies have been used in the treatment of diabetes mellitus since the time of Charaka and Sushruta. Plants have always been an exemplary source of drugs and many of the currently available drugs have been derived directly or indirectly from them. The ethnobotanical information reports that about 800 plants may possess anti-diabetic potential. Out of several Indian medicinal plants 33 plants were reviewed. The most effective antidiabetic Indian medicinal plants are Acacia arabica, Aegle marmelose, Agrimonia eupatoria, Allium cepa, Allium sativum, Aloe vera, Azadirachta indica, Benincasa hispida, Beta vulgaris, Caesalpinia bonducella, Citrullus colocynthis, Coccinia indica, Eucalyptus globules, Ficus bengalenesis, Gymnema sylvestre, Hibiscus rosasinesis, Ipomoea batatas, Jatropha curcus, Mangifera indica, Momordica charantia, Morus alba, Mucuna pruriens, Ocimum sanctum, Pterocarpus marsupium, Punica granatum, Syzigium cumini, Tinospora cordifolia, Trigonella foenum graecum. A wide array of plant derived active principles representing numerous chemical compounds has demonstrated activity consistent with their possible use in the treatment of diabetes.

Antineoplasic activity of Agaricus brasiliensis basidiocarps on different maturation phases

The fungus Agaricus brasiliensis is a Basidiomycete studied because of its immunomodulation and/or antitumor substances. The objective of this study was to verify the Agaricus brasiliensis antineoplasic activity in vivo on different basidiocarp maturation phases on Sarcoma 180 cells implanted in mice. Sarcoma cells were implanted in mice and after seven days mice were divided in three groups. The first group was treated with saline solution, the second group was treated with closed basidiocarp extract solution and the third group was treated with opened basidiocarp extract solution. After 30 days of being daily orally treated with these three solutions all animals suffered euthanasia, and the splenic index, tumor mass and volume were determined. No significant differences of the tumor growth inhibition in function of the different basidiocarp maturation phases for the Agaricus brasiliensis strain were observed. The in vivo basidiocarp antineoplasic average activity was 89.22 percent.