ALLERGIC RHINITIS AND IMPORTANCE OF FEXOFENADINE HCL SUSTAINED RELEASE MICROSPHERE AS ITS TREATMENT APPROACH

The current treatment approaches for allergic rhinitis are practiced over decades, but the patient quality of life has not yet changed so much. The reasons are research gaps in pathophysiology of the disease, proper management of the disease. Fexofenadine HCl is a second-generation antihistamine drug which has a half-life of about 14.4 h. It is useful in the management of common symptoms like sneezing, itchy throat, and red eyes in individuals suffering from allergic rhinitis. Fexofenadine immediate release or sustained release formulations are available in the market as suspension, tablet and capsule. In this research paper, we have discussed the symptoms associated with allergic rhinitis and treatment approaches. Fexofenadine HCl is being used for the treatment of this disease. But as it has a long half-life, we have discussed the importance of the introduction of sustained-release microsphere formulation of Fexofenadine HCl in the market.

Measurement and modeling of clemastine fumarate (antihistamine drug) solubility in supercritical carbon dioxide

The solubilities of clemastine fumarate in supercritical carbon dioxide (ScCO2) were measured for the first time at temperature (308 to 338 K) and pressure (12 to 27 MPa). The measured solubilities were reported in terms of mole faction (mol/mol total) and it had a range from 1.61 × 10–6 to 9.41 × 10–6. Various models were used to correlate the data. The efficacy of the models was quantified with corrected Akaike’s information criterion (AICc). A new cluster salvation model was derived to correlate the solubility data. The new model was able to correlate the data and deviation was 10.3% in terms of average absolute relative deviation (AARD). Furthermore, the measured solubilities were also correlated with existing K.-W. Chen et al., model, equation of state model and a few other density models. Among density models, Reddy and Garlapati model was observed to be the best model and corresponding AARD was 7.57% (corresponding AICc was − 678.88). The temperature independent Peng–Robinson equation of state was able to correlate the data and AARD was 8.25% (corresponding AICc was − 674.88). Thermodynamic parameters like heats of reaction, sublimation and solvation of clemastine fumarate were calculated and reported.

Safety of Cyproheptadine, an Orexigenic Drug. Analysis of the French National Pharmacovigilance Data-Base and Systematic Review

Objectives: Cyproheptadine is a first-generation H1-antihistamine drug first that was distributed in the 1960s. While its orexigenic effect was observed early, cyproheptadine is not yet authorized for this indication in all countries today. There is an increasing medical interest and demand for the orexigenic effect of cyproheptadine, especially in children with poor appetite. As cyproheptadine might be evaluated in future clinical trials, we wanted to assess its safety profile.Methods: Using the French national pharmacovigilance database, we retrospectively analyzed all pediatric and adult reports of adverse effects of cyproheptadine recorded since its first distribution in France. Next, we performed a systematic review of the literature of cyproheptadine adverse effects.Results: Since 1985, 93 adverse effects were reported in the French pharmacovigilance database (adults 81.7%, children 18.3%); these were mainly neurological symptoms (n = 38, adults 71%, children 28.9%), and hepatic complications (n = 15, adults 86.7%, children 13.3%). In the literature, the most frequent adverse effect reported was drowsiness in adults or children, and five case reports noted liver complications in adults. We estimated the frequency of hepatic adverse effects at 0.27 to 1.4/1000, regardless of age.Conclusion: Cyproheptadine can be considered a safe drug. Mild neurological effects appear to be frequent, and hepatotoxicity is uncommon to rare. Randomized controlled trials are needed to evaluate the safety and efficacy of cyproheptadine before authorization for appetite stimulation, especially in young children as studies at this age are lacking. Possible hepatic complications should be monitored, as very rare cases of liver failure have been reported.

Measurement and Modeling of Clemastine Fumarate (Antihistamine Drug) Solubility in Supercritical Carbon Dioxide

The solubilities of clemastine fumarate in supercritical carbon dioxide) ScCO2( were measured for the first time at temperature (308 to 338 K) and pressure (12 to 27 MPa). The measured solubilities were reported in terms of mole faction and it is ranged from 1.61 ×10− 6 to 9.41×10− 6. Various models were used to correlate the data. The efficacy of the models was quantified with corrected Akaike’s information criterion (AICc). A new cluster salvation model was derived to correlate the solubility data. The new model was able to correlate the data and deviation was 10.3% in terms of average absolute relative deviation (AARD). Furthermore, the measured solubilities were also correlated with existing K.-W. Chen et al., cluster salvation model, equation of state (EoS) model and few density models. Among density models, Tippana and Garlapati model was observed to be the best model and corresponding AARD% was 7.57 (corresponding AICc is -678.88). The Peng-Robinson equation of state as temperature independent was able to correlate the data and deviation was 8.25% in terms of AARD% (corresponding AICc is -674.88). Moreover, thermodynamic enthalpies of clemastine fumarate were estimated.

Design, Synthesis, and Validation of a Novel [11C]Promethazine PET Probe for Imaging Abeta Using Autoradiography

Promethazine, an antihistamine drug used in the clinical treatment of nausea, has been demonstrated the ability to bind Abeta in a transgenic mouse model of Alzheimer’s disease. However, so far, all of the studies were performed in vitro using extracted tissues. In this work, we report the design and synthesis of a novel [11C]promethazine PET radioligand for future in vivo studies. The [11C]promethazine was isolated by RP-HPLC with radiochemical purity >95% and molar activity of 48 TBq/mmol. The specificity of the probe was demonstrated using human hippocampal tissues via autoradiography.

Poly (DL-valine) electro-polymerized carbon nanotube paste sensor for determination of antihistamine drug cetirizine

Poly (DL-valine) modified multiwalled carbon nanotube paste sensor (PVLMCNTPS) was prepared by electro-polymerization route. PVLMCNTPS and bare multiwalled carbon nanotube paste sensor (BMCNTPS) morphologies and sensing properties for cetirizine (CTZ) were confirmed through a field emission scanning electron microscope (FE-SEM) and electrochemical studies, respectively. In contrast to BMCNTPS, PVLMCNTPS surface composite creates an electrocatalytic impact on the oxidation of CTZ. PVLMCNTPS properties were optimized using parameters such as accumulation time, number of polymerization cycles, solution pH, and scan rate. The optimized PVLMCNTPS was applied for the determination of cetirizine in 0.1 M phosphate buffer solution (PBS) of pH 7.0, using cyclic voltammetry (CV). It is shown that PVLMCNTPS provided analytical linearity from 2.0 to 80 µM, with a detection limit of 0.11 µM for CTZ determination. PVLMCNTPS is found highly selective for CTZ in presence of some interfering organic molecules. The stable and selective PVLMCNTPS was applied for CTZ determination in pharmaceutical pills with satisfactory results.