Levocetirizine Research Articles

Formulation and Evaluation of Orally Disintegrating Films of Levocetirizine Dihydrochloride

The present investigation was undertaken with the objective of formulating taste-masked orally-disintegrating films of the bitter levocetirizine dihydrochloride to enhance the convenience and compliance by the elderly or paediatric or bedridden and non-cooperative patients due to its ease of administration. Scope of this study was to explore the film forming properties of various film formers like modified starch, pullulan, hydroxypropyl methylcellulose and polyvinyl alcohol-polyethylene glycol based polymers. Plasticizers like glycerin, propylene glycol, sorbitol and polyethylene glycol 400 were evaluated by studying their effect on folding endurance, peelablity and in vitro disintegration time. Films were prepared by solvent casting method. Drug loaded films, which composed of the selected polymers with the suitable plasticizer showed excellent film forming capacity along with good folding endurance, in vitro disintegration time within 22 s and >95% drug release in 10 min as compared to marketed immediate release tablets, which showed on 30.4% at the end of 10 min The films prepared were 30-40 mg in weight with pleasant taste with bitter active being successfully taste masked by a mixture of sucralose and monoammonium glycerrhizinate producing an extended sweetness profile. Furthermore, the orally disintegrating films were stable for at least 3 mon when stored at 40° and 75% relative humidity. The formulation developed is simple, easy to prepare and economical with great applicability during the emergency cases such as allergic reactions, whenever immediate onset of action is desired.

Combined ozone hydrotherapy for atopic dermatitis: evaluation of efficacy and detection of interleukin-4 and nerve growth factor levels in peripheral blood from patients before and after treatment

Objective To evaluate the clinical efficacy and safety of combined ozone hydrotherapy for the treatment of atopic dermatitis (AD). Methods A total of 60 patients with moderate or severe AD aged from 6 to 65 years were enrolled, and randomly and equally divided into a test group and a control group. Both the two groups were treated with oral levocetirizine capsules 5 mg once a day, topical tacrolimus ointment twice a day, and topical moisturizers. The test group was additionally treated with ozone hydrotherapy 3-5 times every week. The treatment lasted 2 weeks. The severity scoring of atopic dermatitis (SCORAD) score, visual analog scale (VAS) score, dermatology life quality index (DLQI) or children's dermatology life quality index (CDLQI) score were assessed before and after the treatment, and compared between the two groups. Enzyme-linked immunosorbent assay (ELISA) was performed to measure the levels of interleukin-4 (IL-4) and nerve growth factor (NGF) in peripheral blood from the patients before and after the treatment. Results After 2-week treatment, the SCORAD scores, VAS scores and DLQI/CDLQI scores significantly decreased from 42.13 ± 16.03, 7.14 ± 2.12 and 14.92 ± 5.94 before the treatment to 27.3 ± 11.01, 2.23 ± 1.31 and 9.69 ± 4.17 respectively in the test group (all P 0.05). Conclusion Combined ozone hydrotherapy can effectively and safely improve the condition of patients with AD, likely by decreasing the levels of IL-4 in peripheral blood. Key words: Dermatitis, atopic; Ozone; Interleukin-4; Nerve growth factor; Treatment outcome

Experimental and quantum mechanical studies on the ion–pair of levocetirizine and bromocresol green in aqueous solutions

In the present work, levocetirizine dihydrochloride (LEV) was found to interact with bromocresol green (BCG) via ion–pair formation. UV–vis and FTIR spectroscopy were used to validate the data obtained from quantum mechanical calculations (QMC). The electrostatic potential maps show that the reaction is preferred through the interaction of the sulfonic acid group of BCG and the quaternary ammonium group of LEV. The optimized geometry of the product shows that there are six different intermolecular hydrogen bonds between the studied molecules resulting from the ionic attraction between the oppositely charged groups. The UV–vis spectra suggest the formation of an ion–pair. This finding is contradicting with the previous charge–transfer hypothesis.

Olopatadine hydrochloride for the treatment of chronic idiopathic urticaria: a multicentre, double-blind, randomized, parallel-group, controlled clinical trial

Objective To evaluate the efficacy and safety of olopatadine hydrochloride for the treatment of chronic idiopathic urticaria (CIU). Methods A multicentre, double-blind, randomized, parallel-group, controlled clinical trial was conducted. A total of 144 patients with CIU from 3 research centers were enrolled into this study, and randomly and equally divided into a test group and a control group. The test group administrated olopatadine hydrochloride 5 mg twice a day for 28 consecutive days, while the control group administrated levocetirizine hydrochloride 5 mg in the forenoon and a placebo tablet of olopatadine hydrochloride 5 mg in the afternoon for 28 consecutive days. The symptom score reducing index (SSRI) served as the primary outcome, and global assessment score for efficacy and total response rates as the secondary outcome. Results Totally, 137 patients completed the trial, including 70 in the test group and 67 in the control group. As intention-to-treat analysis showed, there were no significant differences in the total response rate between the test group and control group on day 7 (64.29% (45/70) vs. 56.72% (38/67), P> 0.05), 14 (82.86%(58/70) vs. 74.63%(50/67), P> 0.05), or 28 (87.14% (61/70) vs. 77.61% (52/67), P> 0.05) after start of treatment. The SSRI was significantly higher in the test group than in the control group after 4 weeks of treatment (82.67% ± 22.70% vs. 70.51% ± 32.07%, P 0.05), and adverse reactions mainly included lethargy, dry mouth, fatigue, etc. Conclusion Olopatadine hydrochloride is effective and safe for the treatment of CIU. Key words: Urticaria; Randomized controlled trial; Olopatadine; Levocetirizine

A SINGLE HPLC-DAD METHOD FOR SIMULTANEOUS ANALYSIS OF PARACETAMOL, PHENYLEPHRINE, CAFFEINE AND LEVOCETIRIZINE IN BULK POWDER AND TABLET FORMULATION: APPLICATION TO IN-VITRO DISSOLUTION STUDIES

ABSTRACT Present work describes development and validation of HPLC–DAD method for the analysis of a complex mixture consisting phenylephrine hydrochloride (PHE), paracetamol (PAR), caffeine (CAF) and levocetirizine (LEV). Chromatographic separation was achieved using a Kinetex-C18 column involving gradient elution, the mobile phase composed of 10mM phosphate buffer (pH 3.3) and methanol. The three step gradient program started with step-1 initially with 2% (by volume) methanol and 98 % phosphate buffer (pH 3.3) for first 5 minutes. In step-2 methanol concentration changed linearly to 80% in next 12 minutes the analysis was concluded by step-3 changing methanol to 2% in next 8 minutes. The method was linear in concentration ranges of 50 to 200 % of labeled claims with r 2 near to 1. Developed method proved to be precise for inter and intra-day studies the %RSD values were < 2 , accuracy studies by standard addition at 80, 100 and 120% levels resulted in recoveries of standard near to 100%. The method was selective with no interferences from placebo; robustness of method was proved by no significant alteration in system suitability parameters. The LOD values for PHE, PAR, CAF and LEV were 0.13, 0.51, 0.05 and 0.05 and LOQ were 0.39, 1.53, 0.15 and 0.15 respectively. The study concluded a validated HPLC method for analysis of complex mixture consisting PHE, PAR, CAF and LEV in bulk, tablet and dissolution samples in simulated gastric fluid (SGF).

Validated derivative and ratio derivative spectrophotometric methods for the simultaneous determination of levocetirizine dihydrochloride and ambroxol hydrochloride in pharmaceutical dosage form

Three simple, precise, accurate and validated derivative spectrophotometric methods have been developed for the simultaneous determination of levocetirizine dihydrochloride (LCD) and ambroxol hydrochloride (ABH) in bulk powder and in pharmaceutical formulations. The first method is a first derivative spectrophotometric method (1D) using a zero-crossing technique of measurement at 210.4nm for LCD and at 220.0nm for ABH. The second method employs a second derivative spectrophotometry (2D) where the measurements were carried out at 242.0 and 224.4nm for LCD and ABH, respectively. In the third method, the first derivative of the ratio spectra was calculated and the first derivative of the ratio amplitudes at 222.8 and 247.2nm was selected for the determination of LCD and ABH, respectively. Calibration graphs were established in the ranges of 1.0–20.0μgmL−1 for LCD and 4.0–20.0μgmL−1 for ABH using derivative and ratio first derivative spectrophotometric methods with good correlation coefficients. The developed methods have been successfully applied to the simultaneous determination of both drugs in commercial tablet dosage form.

DEVELOPMENT AND VALIDATION OF ABSORBANCE CORRECTION METHOD FOR SIMULTANEOUS DETERMINATION OF LEVOCETIRIZINE AND AMBROXOL IN COMBINED TABLET DOSAGE FORM

A new, s imple, accurate and sensitive U V - Spectrophotometric absorbance correction method has been develop ed and validated for simultaneous estimation of Levocetirizine ( LEV ) and Ambroxol ( AMB ) in a combined tablet dosage form. Distill water was used as solvent. In this method, two wave lengths on Ambroxol curve were selected where it showed same absorbance, w hich were 261 nm and 303 nm. At 303 nm, Levocetirizine showed zero absorbance while at 261 nm it gave considerable absorbance. At 261 nm, both the drugs showed some absorbance . The absorbance of Levocetirizine was corrected at 261 nm. The method was found to be linear between the range of 4 - 28 μg/ml for Levocetirizine and Ambroxol . The mean percentage recovery was found in the range of 99.4 ± 1.11 % and 100 . 2 ± 1 % for Levocetirizine and Ambroxol respectively at three different levels of standard additions . The precision (intra - day, inter day) of method were found within limits (RSD < 2 %). The met h od was validated according to ICH guidelines. Thus the proposed method was simple, precise, economic, rapid and accurate and can be successfully applied for simultaneous determination of Levocetirizin e and Ambroxol in combined tablet dosage form.

Elimination of bitter, disgusting taste of Levocetrizine di hydrochloride by HPβ-Cyclodextrin

Levocetrizine Di Hydrochloride is second generation piperazine derivative, a potent H1 selective anti-histaminic or anti-allergic agent. It has bitter taste. So, the taste has to be masked in order to reduce its bitterness, to increase its palatability and to improve patient compliance. The purpose of this research work to prepare tasteless complexes of levocetrizine di hydrochloride. Conventional taste masking techniques such as use of sweeteners and amino acids and flavoring agents often are unsuccessful in masking the taste of highly bitter drugs. The purpose of this research was to mask the intensely bitter taste of Levocetrizine Di Hydrochloride adopting inclusion complex formation array using HP β-cyclodextrin by Kneading method. The study conclusively demonstrated the complete masking of bitter taste of Levocetrizine Di Hydrochloride with HP Beta cyclodextrin in 1: 1 Kneaded ratio.

Assessment of the efficacy and safety of total glucosides of paeony combined with levocetirizine and tacrolimus ointment for the treatment of severe facial corticosteroid-dependent dermatitis

Objective To evaluate the efficacy and safety of total glucosides of paeony combined with levocetirizine and tacrolimus ointment for the treatment of severe facial corticosteroid-dependent dermatitis.Methods Ninety-eight patients with severe facial corticosteroid-dependent dermatitis were enrolled in this study,and assigned into the test group (n =63) and control group (n =35).The test group were treated with oral total glucosides of paeony capsules and levocetirizine as well as topical 0.03％ tacrolimus ointment,and the control group with oral levocetirizine and topical 0.03％ tacrolimus ointment only.The facial symptoms and signs of patients were observed and scored at week 2 and 4 after starting treatment as well as at week 2 after drug withdrawal.The response rate in these patients was calculated.Results Totally,8 patients (3 in the test group and 5 in the control group) were lost to follow up,and the remaining 90 patients completed the treatment finally.The response rate in the test group was significantly higher than that in the control group at week 2 (50.0％ (30/60) vs.16.7％ (5/30),P ＜ 0.05)and 4 (93.3％ (56/60) vs.60.0％ (18/30),P ＜ 0.05) after starting treatment.During the 2 weeks after drug withdrawal,total symptom scores continuously decreased in all the patients in the test group and in 53.3％ (16/30) of the patients in the control group,maintained unchanged in 26.7％ (8/30) and increased in 20.0％ (6/30) of the patients in the control group.No severe adverse reactions were observed in either of the two groups during the study period.Conclusion Total glucosides of paeony capsules can improve the efficacy of levocetirizine and topical tacrolimus ointment for the treatment of severe facial corticosteroid-dependent dermatitis. Key words: Dermatitis, corticosteroid-dependent; RADIX PAEONIAE ALBA; Treatment outcome

COMPARISON OF DIFFERENT WAYS OF CHROMATOGRAPHIC SPOTS VISUALIZATION IN DETERMINATION OF ANTYHISTAMINE SUBSTANCES

Importance of compounds investigated (loratadine, desloratadine, cetirizine dihydrochloride, levocetirizinedihydrochloride) i n contemporary pharmacy causes necessity of finding the fast and easy method for their identifi cation. The aim of this work is to find the best way of visualization of chromatographic spots in qualitative determination of compounds investigated during analysis by thin layer chromatography. The standard solution s of compounds investigated were prepar ed in ethanol or methanol. The different mobile phases for particular compounds were used. There were also used many ways of spot visualization i.e. exposure to UV light, dipping in solution of visualizing agents, visualization in iodine vapour and photo c atalytic visualization. The best visualization effect gave exposure to UV light and dipping in solution of bromophenol blue in the case of loratadine and desloratadine, respective ly; and visualization in iodine vapour in the case of cetirizine and levoceti rizine. Using photo catalytic degradation had no use in the case all of compounds investigated.

Simultaneous Estimation of Paracetamol, Ambroxol Hydrochloride, Levocetirizine Dihydrochloride, and Phenylephrine Hydrochloride in Combined Tablet Formulation by First-Order Derivative Spectrophotometry

Paracetamol, ambroxol hydrochloride, levocetirizine dihydrochloride, and phenylephrine hydrochloride are used in combination for the treatment of chronic sinusitis, rhinitis, fever, nasal discharge, sore throat, and wheezing. The present work deals with method development for simultaneous estimation of paracetamol, ambroxol hydrochloride, levocetirizine dihydrochloride, and phenylephrine hydrochloride in tablet formulation by first-order derivative spectrosphotometry. For determination of sampling wavelength, 10 μg/mL of each of paracetamol, ambroxol hydrochloride, levocetirizine dihydrochloride, and phenylephrine hydrochloride was scanned in 200–400 nm ranges and sampling wavelengths were found to be 305.5 nm for paracetamol, 321 nm for ambroxol hydrochloride, 244 nm for levocetirizine dihydrochloride, and 280 nm for phenylephrine hydrochloride in first-order derivative spectrophotometry. In this method, linearity was observed in the ranges of 20–140 μg/mL for paracetamol and 10–70 μg/mL for ambroxol hydrochloride, levocetirizine dihydrochloride, and phenylephrine hydrochloride. The % recovery was within the range between 98 and 102%, and % relative standard deviation for precision and accuracy of the method was found to be less than 2%. The method is validated as per International Conference on Harmonization Guidelines. The method can be successfully applied for the simultaneous analysis of these drugs in pharmaceutical dosage forms.

Fast Disintegrating Combination Tablet of Taste Masked Levocetrizine Dihydrochloride and Montelukast Sodium: Formulation Design, Development, and Characterization.

The aim of this study was to prepare fast disintegrating combination tablet of taste masked Levocetrizine dihydrochloride and Montelukast sodium by using direct compression method. To prevent bitter taste and unacceptable odour of the Levocetrizine dihydrochloride drug, the drug was taste masked with ion exchange resins like Kyron-T-104 and Tulsion-412. Among the two resins, Kyron-T-104 was selected for further studies because of high drug loading capacity, low cost, and better drug release profile. An ion exchange resin complex was prepared by the batch technique and various parameters; namely, resin activation, drug: resin ratio, pH, temperature, and stirring time, and swelling time were optimized to successfully formulate the tasteless drug resin complex (DRC). The tablets were prepared using microcrystalline cellulose (MCC) PH 102 as diluent along with crospovidone (CP), croscarmellose sodium (CCM), and sodium starch glycolate (SSG) as a superdisintegrants. The tablets were evaluated for weight variation, hardness, friability, wetting time, water absorption ratio, disintegration time (DT), and dissolution study and it was concluded that the tablet formulation prepared with 2% SSG + CCS showed better disintegration time in comparison with other formulation and good drug release. The stability studies were carried out for the optimized batch for three months and it showed acceptable results.

SIMULTANEOUS ANALYSIS OF LEVOCETIRIZINE DIHYDROCHLORIDE, AMBROXOL HYDROCHLORIDE, AND MONTELUKAST SODIUM BY RP-HPLC - PDA METHOD

A simple, specific, and accurate reverse-phase liquid chromatographic method was developed for the estimation of Levocetirizine (LCZ), Ambroxol Hydrochloride (AMB), and Montelukast Sodium (MONT) in bulk and pharmaceutical dosage forms. A C18 reverse phase column (Phenomenox- RP Aqueous) of 250 × 4.6 mm dimensions and 5 µm particle size with mobile phase containing 15 mm of Ammonium acetate:acetonitrile (40:60%, v/v) was used at isocratic mode and eluents were monitored at 215 nm. The retention times for LCZ, AMB, and MONT are 2.21, 4.46, and 13.35 nm, respectively, and showed a good linearity in the concentration range of 4–20 µg/mL of LCZ, 30–150 µg/mL of AMB, and 8–40 µg/mL of MONT with a correlation coefficient (R) of 0.998, 0.999, and 0.995. The percentage assays were found to be LCZ (99.1), AMB (98.5), and MONT (102.5), respectively. The proposed method was validated as per ICH guidelines and successfully applied to the simultaneous estimation of LCZ, AMB, and MONT in commercial formulations.

Development and Validation of First-Order Derivative Spectrophotometry for Simultaneous Determination of Levocetirizine Dihydrochloride and Phenylephrine Hydrochloride in Pharmaceutical Dosage Form

A simple, precise, accurate, and economical spectrophotometric method has been developed for simultaneous estimation of levocetirizine dihydrochloride (LCT) and phenylephrine hydrochloride (PHE) by employing first-order derivative spectrophotometric method. The first-order derivative absorption at 240 nm (zero crossing point of PHE) was used for quantification of LCT and 283.2 nm (zero crossing point of LCT) for quantification of PHE. The linearity was established over the concentration range of 4–24 μg/mL and 8–48 μg/mL for LCT and PHE with correlation coefficients (r2) 0.9964 and 0.9972, respectively. The mean % recoveries were found to be in the range of 99.14%–100.43% for LCT and 98.73%–100.83% for PHE. The proposed method has been validated as per ICH guideline and successfully applied for the simultaneous estimation of LCT and PHE in combined tablet dosage form.

Ефективність левоцетиризину при алергічному риніті в дітей

Проблемі кращого лікування легкого персистуючого або помірно тяжкого інтермітуючого алергічного риніту присвячене дослідження, у якому взяли участь 62 дитини молодшого шкільного віку. Дітям призначали левоцетиризин перорально (5 мг/день) або назальну/очну форму кромоглікату натрію (20 мг/мл, 1–2 впорскування/краплі 4 рази на день) упродовж 2 тижнів. У кінці дослідження був зроблений висновок про те, що левоцетиризин на 1-му і 2-му тижні лікування був відповідно на 28 і 29 % (р &lt; 0,05) ефективнішим за кромоглікат натрію. Препарати були порівнянні щодо зменшення вираженості очних симптомів у дітей із супутнім кон’юнктивітом (–45 vs –45 % і –55 vs –59 % відповідно, p &gt; 0,05). При використанні левоцетиризину комплайєнс підвищувався на 38 %, якість життя — на 46 % (р &lt; 0,05) порівняно з натрію кромоглікатом. Автори дослідження дійшли висновку, що при лікуванні легкого персистуючого або помірно тяжкого інтермітуючого алергічного риніту в дітей перевагу слід надавати левоцетиризину.

TASTE MASKING AND FORMULATION DEVELOPEMENT &amp;EVALUATION OF MOUTH DISSOLVING TABLETS OF LEVOCETRIZINE DIHYDROCHLORIDE

Levocetrizine dihydrochloride is the active R (-) enantiomer of cetrizine. It is an orally active and selective H1 receptor antagonist used medically as an Antiallergic. Allergic rhinitis is a symptomatic disorder of the nose induced by inflammation mediated by immunoglobulin E (IgE) in the membrane lining the nose after allergen exposure. Thus formulating Levocetirizine dihydrochloride into a mouth dissolving tablets would provide fast relief. Levocetirizine dihydrochloride is bitter in taste so the Kyron T-134 (ion exchange resin) was used to mask the taste and formulated a mouth dissolving tablets using drug resin complex. Results show that effective taste masking is achieved for Levocetrizine dihydrocloride by preparing drug-resin complex using Kyron T-134. The tablets have evaluated for the drug content, weight variation, and water absorption ratio, wetting time, in vitro disintegration, hardness, friability, thickness uniformity and in-vitro dissolution. The tablets disintegrated in- vitro within 21 to 33 seconds. . The % drug content of tablets in all formulations was found to be between 90-110% which complied with limits established in Indian Pharmacopoeia. In vitro drug release profile of tablets is shown 99% drug release in 10 minutes. The results show that Levocetirizine dihydrochloride is successfully formulated into a mouth dissolving tablet. Key words: Levocetirizine dihydrochloride, Allergic rhinitis, Super disintegrants, Ion exchange resin, Mouth dissolving tablets.

English

The study aims to develop a microparticulate casein based delivery system by the&nbsp;controlled drug delivery approach using Levocetirizine dihydrochloride as the&nbsp;model drug. Fourier transform infrared spectroscopy&nbsp;(FTIR), X-ray and differential scanning calorimetry (DSC) studies substantially indicates the presence of molecularly dispersed drug within the particles with preserved stability during microencapsulation.&nbsp;In vitro&nbsp;release studies of&nbsp;levocetirizine dihydrochloride&nbsp;loaded microparticles&nbsp;were performed by simulating the condition of gastrointestinal tract, and showed the minimal drug leakage (less than 5%) at acidic pH (1.2) and significantly higher release at basic pH (7.4).&nbsp;The results were found to be critical in confirming the role of casein microparticles as potential candidate for the controlled and targeted release of levocetirizine dihydrochloride. &nbsp; Key words:&nbsp;Extended release, casein, levocetirizine dihydrochloride, steric stabilization. &nbsp;

Efficacy of fluticasone furoate nasal spray and levocetirizine in patients with Japanese cedar pollinosis subjected to an artificial exposure chamber

Objective:This study investigated the clinical efficacy of a combination therapy of levocetirizine (LCTZ) and fluticasone furoate nasal spray (FFNS), compared with LCTZ monotherapy, for the suppression of seasonal allergic rhinitis (SAR) symptoms induced in an artificial exposure chamber.Methods:This study was a single-center, placebo-controlled, randomized, 3-way cross-over comparative study performed in 42 Japanese cedar pollinosis patients. These subjects received (1) LCTZ plus FFNS (combination group), (2) LCTZ plus FFNS placebo (monotherapy group), or (3) LCTZ placebo plus FFNS placebo (placebo group) once on the night prior to exposure, with a 1-week washout period between exposures. Nasal (sneezing, rhinorrhea, nasal congestion, and itchy nose) and ocular (eye itching and tearing) symptoms were recorded every 15 min, and the number of sneezes, nose blowing events, and the amount of nasal secretions were measured during exposure. The primary end-point was the cumulative incidence of SAR symptoms during exposure and the ‘ime to occurrence of symptoms’. The secondary end-points were the total nasal symptom score, the ocular symptom score, the amount of nasal discharge, and the number of sneezes and nose blowing events.Results:At all the measurement points, the lowest cumulative incidences for the nasal symptoms were observed in the combination group, followed by the monotherapy and placebo groups. All the subjects in the placebo group developed nasal symptoms within 2 h after pollen exposure, while three and eight subjects in the monotherapy and combination groups, respectively, did not develop any nasal symptoms during exposure. In addition, combination therapy delayed the onset of symptoms.Conclusions:The results demonstrated that combination therapy with FFNS and LCTZ significantly suppressed the induced SAR symptoms and delayed the onset of symptoms compared with LCTZ monotherapy and placebo. Although the conditions of the allergen challenge study using an exposure chamber are different from those in real life, combination therapy with FF and LCTZ was confirmed to be an effective treatment for SAR.

Suppression of osteopontin functions by levocetirizine, a histamine H1 receptor antagonist, in vitro.

Objectives. Osteopontin (OPN), a multifunctional glycoprotein secreted from a wide variety of cells after inflammatory stimulation, is well accepted to contribute to the development of allergic diseases. However, the influence of histamine H1 receptor antagonists (antihistamines) on OPN functions is not well understood. The present study was undertaken to examine the influence of antihistamines on OPN functions in vitro. Methods. Human nasal epithelial cells (5 × 105 cells) were stimulated with 250 ng/mL OPN in the presence of either desloratadine (DL), fexofenadine (FEX), or levocetirizine (LCT). The levels of OPN, GM-CSF, Eotaxin, and RANTES in 24 h culture supernatants were examined by ELISA. The influence of LCT on mRNA expression and transcription factor activation in cells were also examined by real-time RT-PCR and ELISA, respectively. Key Findings. The antihistamines examined significantly suppressed the production of GM-CSF, Eotaxin, and RANTES from cells after OPN stimulation. LCT also exhibited the suppression of mRNA expression for chemokines and transcription factor, NF-κB and AP-1, activation, which were increased by the stimulation of cells with OPN. Conclusions. The suppressive activity of LCT on OPN functions on nasal epithelial cells may be responsible for the attenuating effect of the agent on allergic diseases.

Levocetirizine dihydrochloride and ambroxol hydrochloride oral soluble films: Design, optimization, and patient compliance study on healthy volunteers

Objective: The aim of this study was to develop taste masked oral soluble films (OSFs) for levocetirizine dihydrochloride (LCT) and ambroxol hydrochloride (AMB) using different combination of polymers such as polyvinyl pyrrolidone (PVP) K30, propylene glycol (PG), gelatin, sodium alginate (SA), pectin, gaur gum (GG), and hydroxypropyl methylcellulose (HPMC) K15M and super disintegrants like carboxymethyl cellulose (CMC) and sodium starch glycolate (SSG). Materials and Methods: The different basic formulations were developed using solvent casting method for with and without drugs loading and prepared films were evaluated different morphological and mechanical parameters facilitated the screening of a formulation with best characteristics. Results: The films made from HPMC K15M (42.2% w/w) and pectin (35.2% w/w) and considered as an optimized batch among the other formulations. The addition of (titanium dioxide) (TiO 2 ) films was shown opaque nature. The optimized films were subjected to further of drugs content, drugs release profile, stability, and organoleptic properties by human volunteers. The percentage release at end of 90 th s found 73.11 ± 5.2% in pH 6.0 and 81.07 ± 5.6% in water for LCT and 89.2 ± 4.5% in pH 6.0 and 86.22 ± 4.2% in water for AMB, respectively and there were insignificant changes showed at stability study. The organoleptic properties revealed that by complexing drugs with hydroxypropyl β-cyclodextrin (HPβ-CD) in 1:1.5 ratios masked the bitter taste of drugs. Conclusion: Developed OSFs can be considered as one of the promising formulation to administer bitter drugs such as LCT and AMB especially for pediatric, geriatric, and non-cooperative patients.