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1.
Acta Biochim Pol ; 69(1): 123-129, 2022 Feb 28.
Artículo en Inglés | MEDLINE | ID: mdl-35225498

RESUMEN

The active ingredients of the Pyretrin-D trichological cosmetic series, namely benzyl benzoate, Dalmatian pyrethrum daisy, Cistus incanus, tea tree oil and geranium oil, almond acid and arginine were tested in respect to the treatment of seborrheic dermatitis. The paper describes the application of Dalmatian pyrethrum daisy and the excipient. Methods and devices used to confirm the effectiveness of the tested formulations included the TrichoScope Polarizer Dino-Lite (MEDL4HM) and the scanning electron microscope (SEM).


Asunto(s)
Chrysanthemum cinerariifolium/química , Dermatitis Seborreica/tratamiento farmacológico , Excipientes/uso terapéutico , Extractos Vegetales/uso terapéutico , Administración Cutánea , Adolescente , Adulto , Arginina/uso terapéutico , Benzoatos/uso terapéutico , Cistus/química , Cosméticos/uso terapéutico , Femenino , Geranium/química , Humanos , Microscopía Electrónica de Rastreo/métodos , Persona de Mediana Edad , Prunus dulcis/química , Aceite de Árbol de Té/uso terapéutico , Adulto Joven
2.
PLoS One ; 16(4): e0250599, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33905453

RESUMEN

The objective of this study is to improve and optimize the formulation of Genistein in capsules in order to result in a better pharmacokinetic profile comparing to existing commercial products. In order to do this, five different formulations of Genistein capsules were developed and examined by reviewing their disintegration and dissolution properties. Furthermore, flowability of the powder along with potent incompatibilities between Genistein and its excipients were monitored through their thermal properties. The final formulation of Genistein was quantified using HPLC analysis and then its stability was evaluated thoroughly in real time and accelerated conditions. Finally, with the target to have a product with actual results, in vitro and in vivo studies were conducted. The final product proved to have better results in disintegration and dissolution. Moreover, R.G.C.C.'s capsules exhibited enhanced action in human cell lines as well as impressive pharmacokinetic results in animal models. The in vitro results showed an advantage of the R.G.C.C. product compared to the commercial one, whereas its maximum concertation in vivo was determined 34% higher than the commercial one.


Asunto(s)
Química Farmacéutica , Suplementos Dietéticos , Genisteína/uso terapéutico , Cápsulas/química , Cápsulas/uso terapéutico , Cromatografía Líquida de Alta Presión , Excipientes/química , Excipientes/uso terapéutico , Genisteína/química , Humanos , Equivalencia Terapéutica
3.
Med Hypotheses ; 144: 110027, 2020 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-32758873

RESUMEN

There currently is no specific antiviral drug or a vaccine for SARS-CoV-2/COVID-19 infections; now exceeding 10,300,000 infections worldwide. In the absence of animal models to test drugs, we need to find molecular explanations for any unforeseen peculiarities in clinical data, especially the recent reports describing an unexpected asthma paradox. Asthma is considered a high medical risk factor for susceptibility to SARS-CoV-2/COVID-19 infection, yet asthma is not on the list of top 10 chronic health problems suffered by people who died from SARS-CoV-2/COVID-19. Resolving this paradox requires looking beyond the binary model of a viral receptor-binding domain (RBD) attaching to the ACE-2 receptor. A NCBI pBlast analysis revealed that the SARS-CoV-2 surface spike protein contains key two calcium-dependent fusion domains that are almost identical to those that were recently discovered SARS-CoV-1. These viral calcium-dependent binding domains can facilitate membrane fusion only after cleavage by the host surface protease TMPRSS2. Importantly, TMPRSS2 also requires calcium for its SRCR (scavenger receptor cysteine-rich) domain and itsLDLRA(LDL receptor class A) domain. Thus, the presence of EDTA excipients in nebulized ß2-agonist medicines can disrupt SARS-CoV-2/COVID-19 infection and can explain the asthma paradox. This model validates repurposing EDTA in nebulizer solutions from a passive excipient to an active drug for treating COVID-19 infections. Repurposed EDTA delivery to respiratory tissues at an initial target dose of 2.4 mg per aerosol treatment is readily achievable with standard nebulizer and mechanical ventilator equipment. EDTA warrants further investigation as a potential treatment for SARS-CoV-2/COVID-19 in consideration of the new calcium requirements for virus infection and the regular presence of EDTA excipients in common asthma medications such as Metaproterenol. Finally, the natural history of Coronavirus diseases and further analysis of the fusion loop homologies between the Betacorona SARS-CoV-2 virus and the less pathogenic Alphacorona HC0V-229E virus suggest how to engineer a hybrid virus suitable for an attenuated alpha-beta SARS-CoV-2/COVID-19 vaccine. Thus, replacing SARS-CoV-2 fusion loops (amino acids 816-855) with the less pathogenic HCoV-229E fusion loop (amino acids 923-982) may provide antigenicity of COVID-19, but limit the pathogenicity to the level of HCoV-229E.


Asunto(s)
Asma/complicaciones , Asma/epidemiología , COVID-19/complicaciones , COVID-19/epidemiología , Reposicionamiento de Medicamentos , Ácido Edético/uso terapéutico , Antivirales/uso terapéutico , Broncodilatadores/uso terapéutico , Vacunas contra la COVID-19 , Calcio/química , Susceptibilidad a Enfermedades , Excipientes/uso terapéutico , Humanos , Metaproterenol/uso terapéutico , Modelos Teóricos , Nebulizadores y Vaporizadores , Prevalencia , Receptores de LDL/química , Factores de Riesgo , Serina Endopeptidasas/metabolismo
4.
Int J Pharm ; 431(1-2): 149-60, 2012 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-22265913

RESUMEN

The aim of present investigation was to evaluate the potential of clotrimazole as antimalarial drug. Due to poor aqueous solubility and high lipophilicity, it was previously formulated in a nanoemulsion based system. The intrinsic effects of nanoemulsion on improvement of antimalarial activity of clotrimazole were assessed in mice infected with Plasmodium berghei and compared to its suspension formulation. In four-day suppressive test, mice treated with 10mg/kg clotrimazole nanoemulsion showed the highest suppression of parasitemia and; parasitemia was significantly lower than that of 10mg/kg clotrimazole suspension. In onset of activity and recrudescence test, percent reduction of parasitemia was significantly higher in 10 and 15 mg/kg clotrimazole nanoemulsion groups compared to 15 mg/kg suspension group. In both murine models, survival of mice treated with nanoemulsion was significantly prolonged compared to suspension at equivalent doses. The inhibition of parasite growth by clotrimazole in the nanoemulsion was dose dependent as determined by test for linear trend. In repeated dose oral toxicity, levels of serum liver enzymes and biomarkers of hepatotoxicity did not vary significantly from control. Six-month stability testing of the clotrimazole nanoemulsion exhibited no changes in various physiochemical attributes of drug product compared to initial analysis.


Asunto(s)
Antimaláricos/uso terapéutico , Clotrimazol/uso terapéutico , Malaria/tratamiento farmacológico , Nanoestructuras/química , Animales , Antimaláricos/química , Antimaláricos/toxicidad , Clotrimazol/química , Clotrimazol/toxicidad , Modelos Animales de Enfermedad , Estabilidad de Medicamentos , Almacenaje de Medicamentos , Emulsiones , Excipientes/química , Excipientes/uso terapéutico , Excipientes/toxicidad , Femenino , Humedad , Masculino , Ratones , Plasmodium berghei , Ratas , Ratas Wistar , Solubilidad , Temperatura
5.
Neuroscience ; 160(1): 149-55, 2009 Apr 21.
Artículo en Inglés | MEDLINE | ID: mdl-19409205

RESUMEN

N-methyl-D-aspartate (NMDA) receptor and nitricoxide syntheses are the emerging target sites for development of novel drug molecules because their modulation affects the long term potentiation (LTP) process. NMDA receptor antagonists and nitric oxide synthase inhibitors induce amnesia in animals and therefore have been employed for evaluation of efficacy of several novel antiamnesic agents.Bacopa monniera Linn (syn. Brahmi) is commonly used in the ancient Indian medical system for improvement of memory deficit.We have earlier described the involvement of GABAergic and cholinergic system to account for the antiamnesic effects of B. monniera on diazepam- and scopolamine-induced amnesia.In extension to our previous study this study was designed to investigate the downstream mechanism of B. monniera by evaluation of its effect on MK-801 (an NMDA receptor antagonist) and N(w)-nitro-L-arginine (L-NNA) (a nitric oxide inhibitor)induced memory deficit. We used a Morris water maze scale and compared the degree of reversal of amnesia induced by the two agents. Male Swiss albino mice were subjected to a Rotarod muscle incoordination test followed by water maze tasks.Our data revealed that L-NNA and MK-801 produced anterograde and retrograde amnesia and B. monniera significantly attenuated the L-NNA-induced anterograde amnesia, partially reversing L-NNA-induced retrograde amnesia. On the other hand, B. monniera neither attenuated the MK-801-induced anterograde amnesia nor improved retrograde amnesia caused by it.


Asunto(s)
Amnesia/inducido químicamente , Amnesia/tratamiento farmacológico , Bacopa , Fitoterapia , Preparaciones de Plantas/uso terapéutico , Amnesia Anterógrada/inducido químicamente , Amnesia Anterógrada/tratamiento farmacológico , Amnesia Retrógrada/inducido químicamente , Amnesia Retrógrada/tratamiento farmacológico , Análisis de Varianza , Animales , Maleato de Dizocilpina , Excipientes/uso terapéutico , Masculino , Aprendizaje por Laberinto/efectos de los fármacos , Memoria/efectos de los fármacos , Ratones , Actividad Motora/efectos de los fármacos , Nitroarginina , Polisorbatos/uso terapéutico
6.
Dis Colon Rectum ; 47(9): 1506-9, 2004 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-15486748

RESUMEN

PURPOSE: Water for colostomy irrigation is largely absorbed by the colon, which may result in less efficient expulsion of stool. This study compared the outcome of colonic cleansing with water and polyethylene glycol solution. METHODS: In a cross-over study, 41 colostomy irrigators were randomly assigned to water or polyethylene glycol solution irrigation first and then the other regimen, each for one week. Patients recorded fluid inflow time, total washout time, cramps, leakage episodes, number of stoma pouches used, and satisfaction scores (Visual Analog Scale, 1-10: 1 = poor, and 10 = excellent). The median and interquartile range for each variable was calculated, and the two treatments were compared (Wilcoxon's test). RESULTS: Eight patients failed to complete the study. Thirty-three patients (20 females; mean age, 55 (range, 39-73) years) provided 352 irrigation sessions: water (n = 176), and polyethylene glycol solution (n = 176). Irrigation was performed every 24, 48, and 72 hours by 17, 9, and 7 patients respectively, using 500 ml (n = 1), 750 ml (n = 2), 1,000 ml (n = 16), 1,500 ml (n = 11), 2,000 ml (n = 2), and 3,500 ml (n = 1) of fluid. The median and interquartile range for water vs. polyethylene glycol solution were: fluid inflow time (6 (range, 4.4-10.8) vs. 6.3 (range, 4.1-11) minutes; P = 0.48), total washout time (53 (range, 33-69) vs. 38 (range, 28-55) minutes; P = 0.01), leakage episodes (2.3 (range, 1.7-3.8) vs. 0.7 (range, 0.2-1); P < 0.001), satisfaction score (5.8 (range, 4-7.5) vs. 8.8 (range, 8.3-10); P < 0.001), and stoma pouch usage per week (75 (range, 45-80) vs. 43 (range, 0-80); P = 0.008). No difference was demonstrated for frequency of cramps ( P = 0.24). CONCLUSIONS: Polyethylene glycol solution performed significantly better than water and may be a superior alternative fluid regimen for colostomy irrigation.


Asunto(s)
Colostomía , Excipientes/uso terapéutico , Polietilenglicoles/uso terapéutico , Adulto , Anciano , Estudios Cruzados , Heces , Femenino , Humanos , Masculino , Persona de Mediana Edad , Calidad de Vida , Irrigación Terapéutica/métodos , Agua/administración & dosificación
7.
Phytother Res ; 17(5): 537-41, 2003 May.
Artículo en Inglés | MEDLINE | ID: mdl-12748993

RESUMEN

A previous study demonstrated that an extract of Salvia miltiorrhiza, a medicinal herb highly valued in Chinese folk medicine for the treatment of different pathologies, including insomnia, was capable of reducing voluntary alcohol intake in selectively bred Sardinian alcohol-preferring (sP) rats. The present study was designed to evaluate the suitability of different emulsifying, suspending agents and solvents as vehicles through which Salvia miltiorrhiza extracts can exert their reducing effect on alcohol intake. A single dose (100 mg/kg) of a standardised extract of Salvia miltiorrhiza was dissolved in either pure Polysorbate 80, arachis oil, PEG 400, or Polyoxyl 35 castor oil, or suspended in 0.5% CMC in water, and administered acutely by gavage to sP rats. A significant and specific reduction in alcohol intake was recorded only in rats treated with the combination of Polysorbate 80 plus the Salvia miltiorrhiza extract. A further experiment demonstrated that the ability of the combination of Polysorbate 80 in water plus the Salvia miltiorrhiza extract to decrease alcohol intake was dependent upon the concentration of Polysorbate 80. The results of the present study demonstrate that Polysorbate 80 is a proper vehicle for unravelling the reducing effect of Salvia miltiorrhiza extracts on alcohol intake. The ability of Polysorbate 80 to form micelles with the active ingredient(s) of the Salvia miltiorrhiza may explain these results. They may also offer relevant information for pharmaceutical preparation of Salvia miltiorrhiza extract to be used in future clinical trials.


Asunto(s)
Consumo de Bebidas Alcohólicas/prevención & control , Extractos Vegetales/uso terapéutico , Salvia miltiorrhiza , Animales , Medicamentos Herbarios Chinos , Excipientes/uso terapéutico , Masculino , Modelos Animales , Fitoterapia , Raíces de Plantas/química , Polisorbatos/uso terapéutico , Ratas , Solventes/uso terapéutico
8.
Dakar Med ; 45(2): 113-6, 2000.
Artículo en Francés | MEDLINE | ID: mdl-15779163

RESUMEN

In a former study, it was proved that the alcoholic solution of hydro-alcoholic extract of Khaya senegalensis barks had an anti-inflammatory activity on animals after a local application. In this work, ointments made from the same extract and three different excipients (vaseline, lanoline and shea butter (crude and refined)) have been prepared and tested by the method of the croton oil inhibited ear oedema. Results showed inhibition percentages of the ear oedema of 58.8%, 66.7% and 75.4% when the hydro-alcoholic extract was tested at respective doses of 1%, 2% and 3% in shea butter. The two other excipients, (vaceline and Lanoline) tested at the dose of 3% showed between 52% and 58% of inhibitions. The interest of this study was to demonstrate the possibility to maintain the anti-inflammatory activity of Khaya senegalensis barks by using them in a galenic form, easy to prepare and which is, in addition, more adapted than the extract to possible clinical trials.


Asunto(s)
Antiinflamatorios/uso terapéutico , Excipientes/uso terapéutico , Medicinas Tradicionales Africanas , Meliaceae , Ácidos Oléicos/uso terapéutico , Fitoterapia/métodos , Aceites de Plantas/uso terapéutico , Administración Cutánea , Animales , Antiinflamatorios/farmacología , Aceite de Crotón , Dexametasona/uso terapéutico , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Enfermedades del Oído/inducido químicamente , Enfermedades del Oído/tratamiento farmacológico , Edema/inducido químicamente , Edema/tratamiento farmacológico , Excipientes/farmacología , Indometacina/uso terapéutico , Lanolina/uso terapéutico , Ratones , Pomadas , Ácidos Oléicos/farmacología , Vaselina/uso terapéutico , Fitoterapia/normas , Corteza de la Planta , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Aceites de Plantas/farmacología , Senegal
9.
Posit Health News ; (No 17): 4-7, 1998.
Artículo en Inglés | MEDLINE | ID: mdl-11366556

RESUMEN

AIDS: Chondroitin sulfate, a fusion inhibitor found in human milk, appears to work by blocking the ability of a virus, such as HIV, to infect a cell. There are questions about whether cow or goat milk can offer the same fusion-inhibiting benefits. One sulfated monosaccharide, glucosamine 6-sulfate, appears to have significant anti-HIV activity. Carrageenan, a seaweed derivative, shows promise as a vaginal microbicide, and should be tested further to determine its effectiveness against HIV transmission.^ieng


Asunto(s)
Carragenina/uso terapéutico , Sulfatos de Condroitina/uso terapéutico , Terapias Complementarias , Excipientes/uso terapéutico , Infecciones por VIH/tratamiento farmacológico , VIH-1/efectos de los fármacos , Polisacáridos/farmacología , Sulfatos/farmacología , Agar/uso terapéutico , Antígenos CD4/metabolismo , Quimioterapia Combinada , Glucosamina , Proteína gp120 de Envoltorio del VIH/metabolismo , Infecciones por VIH/inmunología , Humanos , Leche Humana/química , Algas Marinas , Dióxido de Silicio/uso terapéutico , Linfocitos T/virología
10.
J Am Coll Nutr ; 15(4): 377-82, 1996 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-8829093

RESUMEN

OBJECTIVE: To assess whether the addition of gum arabic (GA) to oral rehydration solutions (ORS) of either 60 or 90 mM sodium enhances net water and sodium absorption in rats. METHODS: Perfusion of a jejunal segment of male juvenile rats under anesthesia, and determination of net water and sodium absorption, and unidirectional fluid movements using appropriate markers. RESULTS: Addition of 5 and 10 g/L of GA increased the rates of sodium removal from the intestinal lumen perfused with ORS containing either 60 or 90 mM sodium. Net water absorption was unaffected, although GA tended to facilitate bidirectional fluid movement. The alteration of solute transport rates by the addition of 10 g/L GA was associated with an expansion of the basolateral intercellular spaces. CONCLUSIONS: A soluble fiber such as GA appears to be an effective enhancer of sodium absorption from ORS when tested in experimental animals. Since GA does not affect viscosity, an alteration of solute diffusibility through the brush border membrane and changes in intercellular compartments may underlie the observed improvement of sodium absorption.


Asunto(s)
Excipientes/uso terapéutico , Fluidoterapia/métodos , Goma Arábiga/uso terapéutico , Yeyuno/metabolismo , Soluciones para Rehidratación/química , Sodio/farmacocinética , Agua/metabolismo , Animales , Absorción Intestinal/fisiología , Yeyuno/ultraestructura , Masculino , Microscopía Electrónica , Perfusión , Ratas , Ratas Sprague-Dawley
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