Evaluation of in vivo anti-inflammatory activity of Ariflex tablet in comparison with diclofenac and aceclofenac tablet in carrageenan induced rat paw edema model

Background: Osteoarthritis is a major cause of pain and locomotor disability worldwide. Though various pharmacological, mechanical and surgical interventions are used, there is no known cure for OA. The present study was conducted to evaluate anti-inflammatory activity of Ariflex tablet (conceptualized and developed by Ari Healthcare Pvt. Ltd.) in comparison with diclofenac and aceclofenac tablet in carrageenan induced rat paw edema model.Methods: Wistar rats of either sex weighing 150-180 g were taken and divided into 4 groups with 6 animals in each group i.e. group 1 (control group), group 2 (diclofenac tablet), group 3 (aceclofenac tablet) and group 4 (ariflex tablet). The study drugs were orally administered with feeding needle, 30 minutes prior to carrageenan injection. After 30 min 1% w/v of 0.05 ml carrageenan was injected subcutaneously in the rat paw. The paw was marked with ink at the level of lateral malleolus and immersed in mercury up to lateral malleolus mark. The paw volume was measured plethysmographically after injection at 30 minutes, 1 hour, 2 hour, 3 hour, 4 hour and eventually at 5 hour.Results: All the test formulations possess statistically significant (p<0.05) anti-inflammatory activity as compared to control group. The maximum percentage inhibition for Ariflex tablet was 96.97% at the end of 5 hours. When compared to control group, statistically significant reduction of paw edema was observed. The anti-inflammatory activity of Ariflex tablet from 2 hours onwards is comparable to that of diclofenac tablet and aceclofenac tablet.Conclusions: Ariflex tablet possesses significant anti-inflammatory activity

Evaluation of analgesic (in vivo) activity of Ariflex liniment in comparison with diclofenac gel by acetic acid induced writhing model

Background: Adverse effects of available medications for osteoarthritis (OA) and rheumatoid arthritis (RA) necessitate development of safer and effective alternative medicinal substitutes. The present study was conducted to evaluate analgesic activity of Ariflex liniment (conceptualized and developed by Ari Healthcare Pvt. Ltd.) in comparison with diclofenac gel by using acetic acid induced writhing model.Methods: Albino mice of either sex weighing 20-25 g were taken and divided into 3 groups with 5 animals in each group, i.e., group 1 (control group), group 2 (diclofenac gel) and group 3 (Ariflex liniment). After 1 hour of topical application of study drugs writhing was induced in mice using intra-peritonial injection of 1% acetic acid in volume of 0.1 ml/10 g body weight. Then the writhing episodes were recorded for 30 minutes and results were noted.Results: In the control group, the total number of  writhes were 260±29.73 (mean±S. E. M.). The total number of writhes was 12.17±11.81 (mean ± S. E. M.) in diclofenac group. In Ariflex liniment group, not a single animal felt pain, hence there were no writhes recorded. When compared to control group, the difference in number of writhes was statistically significant. The analgesic activity of Ariflex liniment was found to be superior to that of diclofenac gel used as standard drug.Conclusions: It can be concluded that Ariflex liniment possesses analgesic activity

Application of quality by design approach to optimize process and formulation parameters of rizatriptan loaded chitosan nanoparticles

The purpose of present study was to optimize rizatriptan (RZT) chitosan (CS) nanoparticles using ionic gelation method by application of quality by design (QbD) approach. Based on risk assessment, effect of three variables, that is CS %, tripolyphosphate % and stirring speed were studied on critical quality attributes (CQAs); particle size and entrapment efficiency. Central composite design (CCD) was implemented for design of experimentation with 20 runs. RZT CS nanoparticles were characterized for particle size, polydispersity index, entrapment efficiency, in-vitro release study, differential scanning calorimetric, X-ray diffraction, scanning electron microscopy (SEM). Based on QbD approach, design space (DS) was optimized with a combination of selected variables with entrapment efficiency > 50% w/w and a particle size between 400 and 600 nm. Validation of model was performed with 3 representative formulations from DS for which standard error of − 0.70-3.29 was observed between experimental and predicted values. In-vitro drug release followed initial burst release 20.26 ± 2.34% in 3-4 h with sustained drug release of 98.43 ± 2.45% in 60 h. Lower magnitude of standard error for CQAs confirms the validation of selected CCD model for optimization of RZT CS nanoparticles. In-vitro drug release followed dual mechanism via, diffusion and polymer erosion. RZT CS nanoparticles were prepared successfully using QbD approach with the understanding of the high risk process and formulation parameters involved and optimized DS with a multifactorial combination of critical parameters to obtain predetermined RZT loaded CS nanoparticle specifications

Dataset of 2-(2-(4-aryloxybenzylidene) hydrazinyl) benzothiazole derivatives for GQSAR of antitubercular agents

Fragment based Quantitative structure activity relationship (QSAR) analysis on reported 25 2-(2-(4-aryloxybenzylidene) hydrazinyl) benzothiazole dataset as antitubercular agents were carried out. Molecules in the current dataset were fragmented into six fragments (R1, R2, R3, R4, R5, R6).Group based QSAR Models were derived using Multiple linear regression (MLR) analysis and selected on the basis of various statistical parameters. Dataset of benzothiazole reveled importance of presence of halogen atoms on is essential requirement. The generated models will provide structural requirements of benzothiazole derivatives which can be used to design and develop potent antitubercular derivatives

A Review on Impact of Pegylation on Biopharmaceuticals

Covalent conjugation of polyethylene glycol (PEG) molecules to biopharmaceutical molecules is known to increase the pharmacological and medicinal characteristics of proteins and other big molecules and has been utilized effectively in 12 authorized medications. PEG reagents with straight and branched chains up to 40 kDa were utilized with a variety of PEG derivatives with varied linker chemistries. This article discusses the characteristics of PEG, the history and evolution of &nbsp;PEGylation chemistry, and examples of PEGylated pharmaceuticals with a proven track record. They prefer to employ bigger PEG polymers and complicated PEG structures, although they use extremely pure and well-characterized PEG reagents. The preclinical toxicity data for PEG in PEGylated biologics that have been authorized are summarised. Microscopically detected cell vacuolization in phagocytes, which is connected to the biological function of absorption and elimination of particles and macromolecules from blood and tissues. It's possible. Side effects in toxicity tests typically relate to the active moiety of the medicine, not the PEG moiety, according to experience with commercially available PEGylated pharmaceuticals