Autoimmune hepatitis unmasked by nimesulide. Presenting with a MELD score of After a clinical improvement with supportive care and acetylcysteine, a liver biopsy was executed.
The histology revealed micronodular cirrhosis associated with acute hepatitis, with features suggestive of autoimmune hepatitis. Twenty eight months after treatment, another liver biopsy was performed, showing Alejandra menassa toc homosexual full remission of the disease, with only mild fibrosis and no significant inflammatory infiltrate. Supercritical antisolvent precipitation of nimesulide:
Alejandra menassa toc homosexual purpose of this preliminary study was to investigate the physico-chemical properties of nimesulide precipitated by continuous supercritical antisolvent SAS from different organic solvents like acetone, chloroform and dichloromethane at 40 degrees C and 80, 85 and 88 respectively.
Scanning electron microscopy, differential scanning calorimetry, X-Ray diffractometry and in vitro dissolution tests were employed to study how the technological process and the solvent nature would affect the final product. SAS-processed nimesulide particles showed dramatic morphological change in crystalline structure if compared to native nimesulideresulting in needle and thin rods shaped crystals.
The solid state analysis showed that using chloroform or dichloromethane as a solvent the drug solid
Alejandra menassa toc homosexual remained substantially unchanged, whilst if using acetone the applied method caused a transition Alejandra menassa toc homosexual the starting form I to the meta-stable form II.
So as to identify which process was responsible this result, nimesulide was further precipitated from the same solvent by conventional evaporation method RV-sample.
On the basis of this comparison, the solvent was found to be responsible for the re-organization into the different polymorphic form and the potential of the SAS process to produce micronic needle shaped particles, with an enhanced dissolution rate if compared to the to the pure drug, was ascertained.
Finally, the stability of the nimesulide form II, checked by DSC analysis, was ruled on over a period of 15 Genotoxicity of nimesulide in murine bone marrow cells.
The genotoxic potentiality of nimesulide was evaluated in vivo in murine bone marrow cells. Metaphase chromosome
Alejandra menassa toc homosexual revealed the significant increase in the incidence of chromosomal aberrations with preference to structural over the numerical ones. It therefore suggested the clastogenic effect the nimesulide.
The molecular mechanism of mutagenesis is yet to be determined. Comparison of the transdermal absorption of nimesulide from three commercially available
Alejandra menassa toc homosexual formulations.
Nimesulide is a non-steroidal anti-inflammatory drug NSAID applied topically for a variety of Alejandra menassa toc homosexual characterized by pain and inflammation. One of the aims of this study was to compare the permeation profile of nimesulide from the commercially available transdermal gel formulations across dermatomed porcine and human skin.
The in vitro transdermal absorption of nimesulide formulations across porcine skin and human skin was studiedfor 24 hr using a continuous flow-through diffusion cell. The three commercial gels used in this study were Nimulid, Nise Gel, and Orthobid. infinite dose of nimesulide gel about mg was applied on the skin over 0.
The rank order for the drug permeation from these formulations using porcine skin was: The rank order of the permeation across human skin was: The permeation profiles followed zero-order kinetics without any significant lag time. The steady-state flux of nimesulide from Nimulid was significantly higher than that of Nise Gel and Orthobid in both porcine Alejandra menassa toc homosexual human skin p nimesulide 24 hr from Nise Gel and Orthobid across both human and Alejandra menassa toc homosexual skins.
The results suggest that the Nimulid gel may have a greater bioavailability of nimesulide compared to the other gels. In addition, permeation profiles of the various gels across porcine skin did Alejandra menassa
Alejandra menassa toc homosexual homosexual a positive profile behavior to human skin. However, the in vitro drug release of nimesulide Alejandra menassa toc homosexual across a synthetic membrane did not correlate with skin permeation profiles.
In-vitro assessment and Alejandra menassa toc homosexual of nimesulide incorporated Aloe vera transemulgel. The aim of the investigation was to prepare nimesulide emulsion for incorporation in Aloe vera gel base to formulate ' nimesulide - Aloe vera transemulgel' NAE and to carryout in-vitro assessment and in-vivo anti-inflammatory studies of the product. Although the use of nimesulide is banned for oral administration, Alejandra menassa toc homosexual to its potential for inducing hepatotoxicity and thrombocytopenia, the use of nimesulide for topical delivery is prominent in Alejandra menassa toc homosexual treatment of many inflammatory conditions including rheumatoid arthritis.
The drug loading capacity of transdermal Alejandra menassa toc homosexual is low for
Alejandra menassa toc homosexual drugs such as nimesulide.
Nimesulide can be effectively incorporated into emulgels a combination of emulsion and gel. Aloe vera has a mild anti-inflammatory effect and in the present study Aloe vera gel was formulated and used as a gel base prepare NAE. The emulgels thus Alejandra menassa toc homosexual were evaluated for viscosity, pH, in-vitro permeation, stability and skin irritation test.
anti-inflammatory studies were performed using carrageenan induced hind paw edema method in Wistar rats. The results were compared with that of commercial nimesulide gel CNG. From the in-vitro studies, effective permeation of nimesulide from NAE Topical application of the emulgel found no skin Alejandra menassa toc homosexual. Stability studies proved the integrity of the formulation.
The percentage of inhibition of edema was highest for the prepared NAE From our results, it was concluded that the Aloe vera gel acts as an effective gel base to prepare nimesulide emulgel with high drug loading capacity Guaifenesin enhances the analgesic potency of ibuprofen, nimesulide and celecoxib in mice.
Previously, we found Alejandra menassa toc homosexual guaifenesin enhances analgesia Alejandra menassa toc homosexual by paracetamol. The aim of the present study was to determine whether guaifenesin is able to also increase analgesic activity in the non-steroid anti-inflammatory drugs ibuprofen, nimesulide and celecoxib. In addition we investigated the influence of guaifenesin on plasma levels of nimesulide.
A of visceral pain consisting of intraperitoneal injection of acetic acid test was used. Levels
Alejandra menassa toc homosexual Alejandra menassa toc homosexual in plasma were by HPLC.
All Alejandra menassa toc homosexual were given orally and tested in mice. Guaifenesin alone did not produce any antinociceptive effect. The plasma levels of nimesulide were significantly higher in combination with guaifenesin at 30, 60 and 90 min after oral administration in comparison Alejandra menassa toc homosexual nimesulide monotherapy.
The present results suggest that guaifenesin might enhance the analgesic activity of various
Alejandra menassa toc homosexual anti-inflammatory drugs. Photoacoustic study of the penetration kinetics of nimesulid into human skin. The photoacoustic
Alejandra menassa toc homosexual effect is observed when modulated or pulsed light is absorbed by a sample inside a closed chamber and converted in heat, generating acoustic waves; PA measurements have been employed to evaluate transdermal penetration of topically applied drugs.
Phonophoresis is the utilization of ultrasonic US energy to enhance absorption of drugs across the epidermal barrier, and its usefulness has been shown by PA measurements. The aim of the present Alejandra menassa toc homosexual was to determine the characteristic absorption times of the anti-inflammatory Nimesulid gel in human skin, with and without help of therapeutic phonophoresis. After local cleaning, measurements were performed in the forearm of each volunteer before Nimesulid application and for different times after application through massage with the US equipment head; the protocol was repeated for the opposite forearm, but without US emission.
No significant gain was observed in Nimesulid absorption with the utilization of US radiation, indicating that topic application of Nimesulid does not require the use of phonophoresis, due to the natural fast penetration of the Nimesulid gel. Liposomal Aloe vera trans-emulgel drug delivery of naproxen and nimesulide: The present aim of this study was to formulate naproxen and nimesulide liposomal formulation for incorporation in Aloe vera transemulgel and to carry out in vitro and in vivo evaluation of the formulation.
Carbopol is used as a gelling agent and Methyl Alejandra menassa toc homosexual was used as a preservative for the formulation of the gel. Liposomes was formulated by using hydration method. The formulated naproxen and nimesulide Alejandra menassa toc homosexual formulation using A. Paw edema method in Wistar rats induced by carrageenan is used to study in vivo anti-inflammatory action. In vivo data shows that formulated liposomal transemulgel formulation are superior in their efficacy compared to commercial and A.
The results are compared with the commercial formulations. From our results, it is concluded Alejandra
Alejandra menassa toc homosexual toc homosexual the A.
Natural lipid nanoparticles containing nimesulide: Lipid nanoparticles are drug delivery systems able to increase bioavailability of poorly soluble drugs. They can Alejandra menassa toc homosexual prepared with different lipid materials, especially natural lipids. Shea butter is natural lipid obtained from the Butyrospermum parkii seed and rich in oleic and stearic acids.
Nimesulide is a COX 2 selective anti-inflammatory that is poorly soluble in water. The purpose of this study was to develop and characterize shea butter lipid nanoparticles using a new technique and evaluate the in vivo activity of these nanoparticles. Lipid nanoparticles were prepared by melting shea butter and mixing with an aqueous phase using a high shear mixer.
The nanoparticles presented pH of 6. Zeta potential was around mV and the encapsulation efficiency was Antinociceptive activity was performed by
Alejandra menassa toc homosexual acetic acid model. Both nimesulide and nimesulide -loaded nanoparticles presented significant activity compared to the control. The in vivo anti-inflammatory activity was evaluated by paw edema and was statistically different for the nanoparticles containing nimesulide compared to free nimesulideblank nanoparticles and saline.
In conclusion, the use of shea butter as encapsulating
Alejandra menassa toc homosexual was very successful and allowed nanoparticles to be prepared with a very simple technique. The nanoparticles presented significant pharmacological effects that were not seen for free drug administration. Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide. In vitro, the inhibitory effect of nimesulide on nitrite and prostaglandin E2 production by lipopolysaccharide-activated J cell line was reversed by ZM and APCP.
Our data demonstrate that the anti-inflammatory effect of nimesulide in part is mediated by CD Thirty-three healthy Alejandra menassa toc homosexual nude mice were randomly divided into 4 groups: Rapeseed
Alejandra menassa toc homosexual diet alters in vitro menadione and nimesulide hepatic mitochondrial toxicity.
Diet-induced changes in the lipid composition of mitochondrial membranes Alejandra menassa toc homosexual been shown to influence physiological processes. However, the modulation effect of diet on mitochondrially-active drugs has not yet received the deserved attention. Our hypothesis is that modulation of membrane dynamics by diet impacts drug-effects on liver mitochondrial functioning.
In a previous work, we have shown that a diet rich in rapeseed oil altered mitochondrial membrane composition and bioenergetics in Wistar rats. In the present work, we investigated the influence of the modified diet on hepatic mitochondrial activity of two drugs, menadione and nimesulideand FCCP,
Alejandra menassa toc homosexual classic protonophore, was used for comparison.
The results showed that the effects of menadione and nimesulide were less severe on Alejandra menassa toc homosexual mitochondria for rats fed the modified diet than on rats fed the control diet. A specific effect on complex I seemed to be involved in drug-induced mitochondria dysfunction.
Liver mitochondria from the modified diet group were more susceptible to nimesulide effects on MPT induction. The present work demonstrates that diet Alejandra menassa toc homosexual aimed at modifying mitochondrial membrane properties alters the toxicity of mitochondria active agents. This work highlights that diet may potentiate mitochondrial pharmacologic effects increase drug-induced liabilities.