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.

Evaluation of the Influence of Stirring Speed on the Release Kinetics of Fexofenadine HCl Polymeric Microspheres

Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period with a high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres was significantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.

Fexofenadine HCl Microspheres – Can it be the First Line therapy for Allergic Disorders ?

Fexofenadine HCl is a second-generation antihistamine which is commonly used for allergic disorders. But it has low bioavailability. Intranasal corticosteroids (INCs) and Immunotherapy and Allergen Specific Immunotherapy (ASIT) are now commonly being suggested for the treatment of allergic disorders. Despite the fact that current treatment alternatives have been in use for decades, patient quality of life has remained static. The treatment options are not much explored for their respective adverse effects. Therefore, they are in desperate need of research. Fexofenadine HCl is available in the form of a suspension, tablet, or capsule. In our current study, we have explored whether microspheres can be the perfect dosage form of Fexofenadine HCl to treat allergic disorders considering the pharmacokinetics of the drug, available dosage forms options and the probable side effects of the current therapies.

Effect of fexofenadine hydrochloride on allergic rhinitis aggravated by air pollutants

In recent decades, seasonal allergic rhinitis (SAR) prevalence has increased and recent studies have shown that air pollutants, such as diesel exhaust particles (DEP), can increase inflammatory and allergic biomarkers. The aim of this study was to investigate the effects of DEP on SAR symptoms induced by ragweed and to evaluate the efficacy and safety of fexofenadine HCl 180 mg versus placebo.This Phase 3, single-centre, sequential, parallel-group, double-blind, randomised study (NCT03664882) was conducted in an environmental exposure unit (EEU) during sequential exposures: Period 1 (ragweed pollen alone), Period 2 (ragweed pollen+DEP), and Period 3 (ragweed pollen+DEP+single-dose fexofenadine HCl 180 mg or placebo). Efficacy and safety were evaluated in Period 3. Primary endpoints were the area-under-the-curve of Total Nasal Symptom Score (TNSS) from baseline to hour 12 (AUC0–12) during Period 1 and Period 2; and the AUC of the TNSS from hour 2 to 12 (AUC2–12) during Period 3.251/257 evaluable subjects were included in the modified intent-to-treat population. Least squares (LS)-mean difference (95% confidence interval [CI]) for TNSS Log AUC0−12 in Period 2 versus Period 1 was 0.13 (0.081, 0.182; p<0.0001). LS-mean difference in TNSS Log AUC2−12 for fexofenadine HCl versus placebo during Period 3 was −0.24 (−0.425, −0.047, p=0.0148). One fexofenadine HCl-related AE was observed.SAR symptoms evoked by ragweed were aggravated by DEP. Fexofenadine HCl 180 mg was effective in relieving pollen-induced, air pollution-aggravated allergic rhinitis symptoms.

Quality by Design for the Development and Analysis of Enhanced In-Situ Forming Vesicles for the Improvement of the Bioavailability of Fexofenadine HCl In Vitro and In Vivo

Drug absorption from the gastrointestinal tract (GIT) is one of the major problems affecting the bioavailability of orally absorbed drugs. This work aims to enhance Fexofenadine HCl oral bioavailability in vivo, the drug used for allergic rhinitis. In this study, novel spray-dried lactose-based enhanced in situ forming vesicles were prepared using different absorption enhancer by the slurry method. Full factorial design was used to obtain an optimized formulation, while central composite design was used to develop economic, environment-friendly analysis method of Fexofenadine HCl in plasma of rabbits. The optimized formulation containing Capryol 90 as absorption enhancer has a mean particle size 202.6 ± 3.9 nm and zeta potential −31.6 ± 0.9 mV. It achieved high entrapment efficiency of the drug 73.7 ± 1.7% and rapid Q3h release reaches 71.5 ± 2.7%. The design-optimized HPLC assay method in rabbit plasma could separate Fexofenadine HCl from endogenous plasma compounds in less than 3.7 min. The pharmacokinetic study and the pharmacological effect of the fexofenadine-loaded optimized formulation showed a significant increase in blood concentration and significantly higher activity against compound 48/80 induced systemic anaphylaxis-like reactions in mice. Therefore, enhanced in situ forming vesicles were effective nanocarriers for the entrapment and delivery of Fexofenadine HCl.

Green Analytical Methods for the Separation of Seven Antihistamines: Application in Separation of Azelastine and Related Impurities in Nasal Solution

Antihistamines are widely used to alleviate the symptoms caused by allergic reactions. Most of these drugs have zwitteriónicas and/or amphoteric characteristics, which confer additional analytical challenges. This work aimed to develop a single eco-friendly and efficient chromatographic methods for analysis of seven antihistamines, namely, azelastine HCl, desloratadine, ebastine, fexofenadine HCl, ketotifen, loratadine, and olopatadine HCl. The separations were obtained using RP C-18 LUNA (150x4.6mm, 5 μm) column. The mobile phase consisted of acetonitrile and acidified water (pH 2.1) in the following proportion: 15:85, v/v for desloratadine, 25:75, v/v for ketotifen and olopatadine, 32:68, v/v for fexofenadine, 35:65, v/v for azelastine and loratadine, and 45:55, v/v for ebastine. All separations were obtained in less than 7.0 min. A prototype method was fully validated and applied in the assay of azelastine HCl in nasal solutions. The proposed methods for analysis of seven antihistamines are highly efficient, selective, and sensitive. Moreover, all methods can be considered excellent in terms of greenness, with total organic residue < 2.5 mL/analysis. An improved gradient method is also described for separation of azelastine HCl and its related impurities.

A Validated RP-HPLC Method and Force Degradation Studies of Fexofenadine Hydrochloride in Pharmaceutical Dosage Form

A stability indicating HPLC method was developed and validated for the quantitative determination of fexofenadine hydrochloride. An isocratic separation was achieved using phenomenex (C18) column (250×4.6 mm, 5 μm) with flow rate of 1.0 ml/min and UV detection at 254 nm. The mobile phase consists of 5Mm acetate buffer: acetonitrile (50:50; v/v) with pH 9.4 adjusted with acetic acid. The drug was subjected to oxidative, acidic, basic, neutral, photolytic and thermal degradation. All degradation products were eluted in an overall analytical run time of approximately 40 min with the parent compound fexofenadine hydrochloride at a flow rate of approximately 3.3±0.3 min. The method was linear over the concentration range of 31.5-500 μg/ml (r2 = 0.999) with limit of detection and quantification of 3.5 μg/ml and 10.1 μg/ml, respectively. The method has the requisite accuracy, selective, precision and robustness to assay fexofenadine HCl in tablets.Dhaka Univ. J. Pharm. Sci. 17(1): 43-50, 2018 (June)