Effect of processing excipient suet oil on formation and absorption of baohuoside Ⅰ-bile salt self-assembled micelles / 中国中药杂志

The fried method with suet oil,which can strengthen the effect of Epimedium in warming kidney and enhancing Yang,has been widely used in the processing of Epimedium in traditional Chinese medicine. Based on the formation mechanism of Epimedium flavonoids self-assembled micelles in vivo,the synergistic mechanism of processing excipient suet oil was investigated in this paper from the perspective of pharmaceutics. Baohuoside Ⅰ,as representative component of processed Epimedium,was selected as model drug.Average size and zeta potential were measured and the morphology of micelles was observed under transmission electron microscopy. Caco-2 monolayer cell model,rat intestinal perfusion model and in vivo serum drug concentration method were established to investigate the effect of suet oil on the formation and absorption of the baohuosideⅠ bile salt self-assembled micelles. Baohuoside Ⅰ can form selfassembled micelles under the action of sodium deoxycholate. While,adding suet oil into the baohuoside Ⅰ-bile salt micelles( BSDOC) can make it form a more stable system with a smaller average size,higher Zeta potential,lower polydispersity index( PDI) value,significantly improved encapsulation efficiency and drug loading,indicating that suet oil could significantly improve the micelle formation in vivo. In addition,the permeability coefficient of baohuoside Ⅰ in Caco-2 monolayer cells and the four intestinal organs( duodenum,jejunum,ileum and colon) was increased and the oral bioavailability was also improved after adding the suet oil to BS-DOC.All the results demonstrated that the suet oil can promote the formation and absorption of baohuoside Ⅰ self-assembled micelles,so as to enhance its synergistic effects.

Shock séptico en unidad de cuidados intensivos: Enfoque actual en el tratamiento / Septic shock in intensive care units: Current focus on treatment

Los pilares terapéuticos del niño con shock séptico se mantienen en el tiempo, sin embargo, se han incorporado nuevos conceptos, siendo importante que el pediatra y el intensivista tengan conocimiento a cabalidad de ellos. La reanimación con fluidos es una intervención fundamental, no obstante, aún no se ha establecido un tipo de fluido ideal, presentando cada uno limitaciones específicas, no existiendo evidencia sobre la superioridad de un tipo de fluido. Si a pesar de una adecuada resucitación con fluidos persiste el shock, el inicio de inótropos y/o vasopresores está indicado. En caso de refractariedad al uso de vasopresores, nuevos fármacos vasoactivos pueden ser empleados y el uso de hidrocortisona debe considerarse en niños con sospecha de insuficiencia suprarrenal. Existe controversia respecto a la transfusión de glóbulos rojos o el nivel óptimo de glucemia, no existiendo consenso en el valor umbral para el uso de estos hemocomponentes o el inicio de insulina, respectivamente. Asimismo, la utilización de la hemofiltración de alto volumen (HFAV)aún permanece controversial, requiriendo mayores estudios para su recomendación en forma rutinaria en el curso de un shock séptico refractario. El soporte nutricional es primordial, ya que la desnutrición es una grave complicación que debe ser prevenida y tratada adecuadamente. El objetivo de la presente revisión es entregar una actualización en los más recientes avances en tratamiento del shock séptico en la población pediátrica.

Essential therapeutic principles in children with septic shock persist over time, although some new concepts have been recently incorporated, and fully awareness of pediatricians and intensivists is essential. Fluid resuscitation is a fundamental intervention, but the kind of ideal fluid has not been established yet, as each of these interventions has specific limitations and there is no evidence supportive of the superiority of one type of fluid. Should septic shock persists despite adequate fluid resuscitation, the use of inotropic medication and/or vasopressors is indicated. New vasoactive drugs can be used in refractory septic shock caused by vasopressors, and the use of hydrocortisone should be considered in children with suspected adrenal insufficiency, as it reduces the need for vasopressors. The indications for red blood cells transfusion or the optimal level of glycemia are still controversial, with no consensus on the threshold value for the use of these blood products or the initiation of insulin administration, respectively. Likewise, the use of high-volume hemofiltration is a controversial issue and further study is needed on the routine recommendation in the course of septic shock. Nutritional support is crucial, as malnutrition is a serious complication that should be properly prevented and treated. The aim of this paper is to provide update on the most recent advances as concerns the treatment of septic shock in the pediatric population.

Dissolution rate enhancement of piroxicam by ordered mixing

Micronized piroxicam was mixed with lactose, mannitol, sorbitol, maltitol and sodium chloride to produce ordered mixture in a glass vial by manual hand shaking method. The effect of excipients, surfactant, superdisintegrant, drug concentration and carrier particle size on dissolution rate was investigated. Dissolution rate studies of the prepared ordered mixtures revealed that all water soluble excipients increased the dissolution rate of piroxicam when compared to the dissolution rate of piroxicam or its suspension. Ordered mixture formulation PLF4, consisting of lactose as water soluble excipient, SSG [8% w/s] and SLS [1% w/w], released piroxcam at a very fast rate so much so that about 90% of the composition had passed into solution within 2 min. The order of the dissolution rate enhancement for ordered mixtures of various water soluble excipients was: lactose > mannitol > maltitol > sorbitol > sodium chloride. Carrier granules of size 355-710 micro m were most effective in increasing the dissolution rate of drug from ordered mixtures. Decreasing the carrier particle size reduced drug dissolution from ordered mixtures. The dissolution rate of ordered mixtures consisisting of 1-5% w/w piroxicam was superior to dissolution rate of piroxicam suspension. The dissolution data fitting and the resulting regression parameters indicated Hixson Crowell, cube root law, as the best fit to drug release data of ordered mixtures

Formulation and evaluation of ficus glomerata mucilage sustained release matrix tablets of gliclazide

The main aim of present investigation was to develop sustained release matrix tablets of Gliclazide using fruit mucilage from the plant Ficus glomerata. Varying ratios of drug and polymer viz. 1:0.25, 1:0.5, 1:0.75, 1:1.0 and 1:1.25 were selected for the study. The flow properties of powdered mucilage and physical properties of matrix tablets were performed. The swelling behavior and release rate characteristics were studied. The in vitro drug release data was analyzed by zero order, first order, Higuchi plot, Peppas plot and Hixon-Crowell Models. It was observed that as the proportion of mucilage increased the release of drug from the matrix tablets was retarded. Stability studies were conducted at 40 +/- 2°C and RH 75 +/- 5% for 3 months indicates that Gliclazide was stable in the matrix tablets. The Differential Scanning Calorimetric [DSC] and Fourier Transform Infrared [FTIR] study revealed that there was no negative chemical interaction between drug and the mucilage used. From the dissolution study, it was concluded that dried Ficus glomerata mucilage can be used as an excipient for making sustained release matrix tablets

Formulation and evaluation of cetirizine dihydrochloride orodispersible tablet

Cetirizine orodispersible tablets were prepared to achieve quick onset of action and for maximum bioavailability. Tablets were prepared using cetirizine along with camphor and mannitol in the proportion of 1:1:1, 1:1:3, and 1:1:6. The flow property of granules was found to be good for the formulation CZ2 [1:1:3]. The hardness and friability of all the formulations were found to be within the standard limit for orodispersible tablets. Disintegration time was found to be rapid in formulation CZ2 [1:1:3].The in vitro dissolution time was found to be 100% in 11 minutes for the formulation CZ2 [1:1:3]