Fexofenadine HCl

Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.

Design, characterization and in vitro evaluation of HPMC K100 M CR loaded Fexofenadine HCl microspheres.[Pubmed:27350925]

Springerplus. 2016 May 25;5(1):691.

The aim of the current study was to formulate Fexofenadine hydrochloride loaded sustained release microspheres using HPMC K100 M CR, a release retardant hydrophilic polymer by solvent evaporation method. The effect of different drug loading on drug content, drug encapsulation efficiency and release of drug was monitored. The studies on in vitro release mechanism were performed using USP paddle method with 900 ml of phosphate buffer (pH 6.8) for 10 h at 100 rpm. The mechanism of the drug release was determined by fitting in vitro release data to various release kinetic models such as the zero order, first order, Higuchi, Hixson Crowell and Korsemeyer-Peppas model and finding R(2) values for the release profile corresponding to each model. The results confirm that the release rate of the drug from the microspheres is highly affected by the drug to polymer ratio. The study finds that Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics were the major release mechanism. The release mechanism was found to be non-Fickian with increase of polymer content. Scanning electron microscopic technique was performed to obtain the morphological changes due to different drug loading. Differential scanning calorimetry and Fourier transform infra-red spectroscopy was performed to determine any interaction of drug with the polymer. A statistically significant variation in release rate was observed for variation in the amount of HPMC K100 M CR. In the present study, a series of sustained release formulations of Fexofenadine hydrochloride were developed with different drug loading so that these formulations could further be evaluated from the in vivo studies. The formulations were found to be stable and reproducible.

Fast Dissolving Tablets of Fexofenadine HCl by Effervescent Method.[Pubmed:20336204]

Indian J Pharm Sci. 2009 Mar;71(2):116-9.

In the present work, fast dissolving tablets of Fexofenadine HCl were prepared by effervescent method with a view to enhance patient compliance. Three super-disintegrants viz., crospovidone, croscarmellose sodium and sodium starch glycolate along with sodium bicarbonate and anhydrous citric acid in different ratios were used and directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on the in vitro dispersion time (approximately 20 s), three formulations were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability at 40 degrees /75% RH for 3 mo and drug-excipient interaction (IR spectroscopy). Among the three promising formulations, the formulation ECP(3) containing 8% w/w of crospovidone and mixture of 24% w/w sodium bicarbonate 18% w/w of anhydrous citric acid emerged as the best (t(50%) 4 min) based on the in vitro drug release characteristics compared to conventional commercial tablet formulation (t(50%) 15 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (P<0.05).

Spectrofluorimetric determination of etodolac, moxepril HCl and fexofenadine HCl using europium sensitized fluorescence in bulk and pharmaceutical preparations.[Pubmed:21853256]

J Fluoresc. 2012 Jan;22(1):247-52.

A simple, selective and sensitive luminescence method has been developed for the assay of etodolac (I), moxepril HCl (II) and Fexofenadine HCl (III) in bulk drug and pharmaceutical formulations. The method is based on the luminescence sensitization of europium (Eu(3+)) by complexation with the studied drugs. The fluorescence intensities of the products were measured at 667 nm for (I) and at 615 for (II) and (III) while exciting at 276 for all the studied drugs. The fluorescence intensity was directly proportional to the concentration over the range (20-280), (40-240) and (30-80) ng/ml with limits of detection (LOD) = 0.93, 0.92 and 0.95 mug/ml for drugs I, II and III respectively. Optimum conditions for the formation of the complex in methanol were carefully studied. The proposed method was successfully applied for the assay of the studied drugs in pharmaceutical formulations with excellent recovery.

Simultaneous quantitation of Ofloxacin, Fexofenadine HCl and Diclofenac Potassium in affixed dose combinative formulation by HPLC-UV method.[Pubmed:26639475]

Pak J Pharm Sci. 2015 Nov;28(6):1979-84.

A high-pressure liquid chromatography (HPLC-UV) based simple and specific method for simultaneous quantitative determination of Ofloxacin, Fexofenadine HCl and Diclofenac Potassium has been developed and validated according to ICH guidelines. Chromatographic separation of the three drugs was carried out on 4.6 x 250 mm x 5 micro Licrospher RP Select B Column, using mobile phase constituted of methanol and phosphate buffer pH 3.5 (650: 350), pH adjusted to 3.5 +/- 0.05 with dilute ortho-phosphoric acid and delivered at a flow rate of 1 ml/min. The eluents were detected at UV wavelength of 220 nm and the retention times for Ofloxacin, Fexofenadine HCl and Diclofenac Potassium were 2.5 minutes, 4 minutes and 11.5 minutes, respectively. This method is suitable and specific for the three drugs and was found to be linear (R(2) > 0.996), accurate, specific, reproducible and robust over a concentration range of 0.05 to 0.15 mg/ml for Ofloxacin, 0.015 to 0.045 mg/ml for Fexofenadine HCl and 0.0125 to 0.0375 mg/ml for Diclofenac Potassium. The proposed method is simple and convenient, hence easily utilized for the characterization and quantitation of the three drugs in a single formulation for combination therapy of rheumatoid arthritis, sepsis, infection with fever and flu.

Changes in pH differently affect the binding properties of histamine H1 receptor antagonists.[Pubmed:16388798]

Eur J Pharmacol. 2006 Jan 20;530(3):205-14.

We investigated the effect of acidic pH, a condition that can be encountered during inflammation accompanying allergic reaction, on the binding properties of histamine H1 receptor antagonists, including levocetirizine ((2-(4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl)ethoxy)acetic acid; Xyzal ), fexofenadine (rac-2-[4-[1-Hydroxy-4-[4-(hydroxydiphenylmethyl) piperidin-1-yl]butyl]phenyl]-2-methylpropionic acid hydrochloride; Allegra) and desloratadine (8-Chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridi ne; Clarinex ). Lowering the pH from 7.4 to 5.8 decreased the affinity of [3H]mepyramine for histamine H1 receptors from 1.7 to 7.5 nM while the opposite was observed with [3H]levocetirizine, whose affinity increased from 4.1 to 1.5 nM. Competition curves with [3H]mepyramine indicated that decreasing the pH from 7.4 to 5.8 led to a 2- to 5-fold increase in the affinity of fexofenadine and levocetirizine, no change in affinity for desloratadine and a 5- to 10-fold decrease in affinity for mepyramine and histamine. Kinetic experiments showed that the increase in affinity of levocetirizine and, to a lesser extent, fexofenadine were totally attributable to a lower dissociation rate at acidic pH (t1/2 increasing from 77 to 266 min and from 71 to 135 min, respectively). Although the affinity of desloratadine remained unchanged, lowering the pH caused a decrease in its dissociation rate (t1/2 of 50 and 256 min at pH 7.5 and 5.8, respectively) accompanied by a concomitant 3.5-fold decrease in its association rate constant. The loss of affinity of mepyramine at acidic pH was driven by a decrease in its association rate constant. Interaction between the carboxylic moiety of levocetirizine and Lys191 is responsible for its slow dissociation rate from the receptor. We found that the magnitude of the pH effect on the dissociation rate of levocetirizine was maintained after mutating Lys191 into alanine, suggesting that a tighter interaction of levocetirizine with Lys191 at lower pH is not the cause of its even slower dissociation rate from the receptor. Although these changes may seem limited in amplitude, we show that they may have substantial effects on receptor occupancy in vivo.

Effects of fexofenadine hydrochloride in a guinea pig model of antigen-induced rhinitis.[Pubmed:16037679]

Pharmacology. 2005 Oct;75(2):76-86.

Allergic rhinitis is an inflammatory disease of the nasal mucosa, induced by histamine, leukotrienes, and other substances released from mast cells. Fexofenadine hydrochloride, the active metabolite of terfenadine, is a novel, nonsedating antiallergic drug having H1 receptor antagonistic activity. Fexofenadine is effective for the treatment of allergic rhinitis. However, its mechanism of action in attenuating nasal congestion has not yet been elucidated. Therefore, we first examined the effects of fexofenadine on a guinea pig model of antigen-induced rhinitis. We also evaluated the effects of mepyramine, zafirlukast and ramatroban in this model; these drugs are an H1 receptor antagonist, a selective leukotriene antagonist and a selective thromboxane antagonist, respectively. Rhinitis was induced by ovalbumin (OVA) instillation into the nasal cavity of animals that had been sensitized by two earlier OVA injections (s.c. and i.p.). The nasal airway resistance was measured for 45 min after the challenge. Fexofenadine hydrochloride (20 mg/kg) and terfenadine (20 mg/kg) administered orally 70 min prior to the challenge significantly inhibited (fexofenadine, p < 0.001, terfenadine, p < 0.05) the increase in nasal airway resistance. Ramatroban (30 mg/kg) administered orally 60 min prior to the challenge also significantly inhibited (p < 0.05) the increase in nasal airway resistance. In contrast, mepyramine (3 mg/kg i.v.) and zafirlukast (3 mg/kg p.o.) failed to reduce the increase in nasal airway resistance. These results suggest that thromboxane may be involved in the increase in the nasal airway resistance in this model. Accordingly, fexofenadine may reduce the increase in nasal airway resistance by inhibiting the release of chemical mediators, including thromboxane, that are involved in the increase in nasal airway resistance in this model.

Fexofenadine.[Pubmed:9506246]

Drugs. 1998 Feb;55(2):269-74; discussion 275-6.

The nonsedating histamine H1 receptor antagonist fexofenadine is the active metabolite of terfenadine. It reduced the allergic response in animal models of allergy and did not prolong the QT interval (QTc) in dogs or rabbits at plasma concentrations many times higher than those seen after administration of therapeutic dosages. Similarly, relative to placebo, fexofenadine did not affect mean QTc in patients given dosages of up to 480 mg/day for 2 weeks or in volunteers who received up to 800 mg/day for 6 days or 240 mg/day for 12 months. In a double-blind clinical trial, oral fexofenadine 120 or 180mg once daily controlled symptoms in patients with seasonal allergic rhinitis as effectively as cetirizine. Other double-blind clinical trials showed that fexofenadine 40 to 240mg twice daily was significantly more effective than placebo. Fexofenadine 180 or 240mg once daily was significantly more effective than placebo in patients with chronic idiopathic urticaria. The drug was well tolerated in these clinical trials, with an adverse event profile similar to that seen with placebo. The most common adverse events were headache, throat irritation, viral infection, nausea, dysmenorrhoea, drowsiness, dyspepsia and fatigue.

Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years).

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