Georgeta Pavalache, Nicoleta Matei, Antoanela Popescu and Verginica Schroder
The aim of research is to assess the active substance by a HPLC method for the separation and quantitative determination of loratadine. The method has been developed and validated on the standard solutions, in previous research. The current study was undertaken to present the results obtained from loratadine determination in biological samples (human serum, urine and breast milk). These results may be applicable on patients with different physiological conditions (aging, pregnancy or recently giving birth, etc.) and pathological conditions which may interfere with the metabolism of loratadine. The used HPLC method detected loratadine concentrations in human serum samples, respectively urine samples, at 2 hours after drug administration. The method detected traces of loratadine which passed into breast milk, as well. Data were statistically interpreted using MED CALC 10.2 software. These results show that the applied method can be used for quantitative analysis of loratadine in biological fluids (all permissible limits of quality specifications being in the range 95- 105%).
Georgeta Pavalache, Nicoleta Matei and Antoanela Popescu
The spectrophotometric method for determination of loratadine using tetraiodomercurate has been applied in various pharmaceutical formulations. The results confirmed that recovery value is optimum and the method is valid, thus it can be used in quality control and evaluation of loratadine tablets, oral formulations of mixed composition, oral solutions, etc. The method is easy and simple to apply, does not require complicated equipment and spectrophotometric reading time is reduced, which allows a large number of analyzes in a relatively short time.
Adriana Ciurba, Emőke Rédai, Ioana Pop, Paula Antonoaea and Nicoleta Todoran
Objective: The aim of this study is to develop lactose-free orodispersible tablets with loratadine for patients with lactose intolerance. Materials and methods: Seven compositions (F1-F7) of 10 mg loratadine were prepared in form of orally disintegrating tablets, by direct compression, using croscarmellose sodium and pre-gelatinized starch in various concentrations as superdisintegrants, diluted with microcrystalline cellulose and combined with mannitol and maltodextrin as binder agents. The tablets had been studied in terms of their pharmacotechnical characteristics, by determining: the weight uniformity of the tablets, their friability, breaking strength and disintegration time, drug content and the dissolution profile of loratadine. The statistical analyses were performed with GraphPad Prism Software Inc. As dependent variables, both the hardness of the tablets and their disintegration ability differ between batches due to their compositional differences (as independent variables). DDSolver were used for modeling the kinetic of the dissolution processes by fitting the dissolution profiles with time-dependent equations (Zero-order, First-order, Higuchi, Korsmeyer-Peppas, Peppas-Sahlin). Results: All proposed formulas shows rapid disintegration, in less than 15 seconds, and the dissolution loratadine spans a period of about 10 minutes. Akaike index as well as R2 adjusted parameter have demonstrated that the studied dissolution profiles are the best fitted by Zero-order kinetic. Conclusion: In conclusion, association of croscarmellose sodium (7.5%) with pre-gelatinized starch (6%) as superdisintegrants and mannitol as the binder agent (35%), positively influences the dissolution properties of loratadine from orally fast dispersible tablets.
Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine
A gastro retentive controlled release system of loratadine was formulated to increase the residence time in stomach and to modulate the release behaviour of the drug. Oil entrapped floating microbeads prepared by the emulsion gelation method were optimized by 23 factorial design and a polymer ratio of 2.5:1.5 (pectin/sodium alginate) by mass, 15% (m/V) of oil (mineral oil or castor oil) and 0.45 mol L-1 calcium chloride solution as the optimized processing conditions for the desired buoyancy and physical stability. In vitro drug release in the fed state conditions demonstrated sustained release of loratadine for 8 h, which best fitted the Peppas model with n < 0.45. The ethyl cellulose coating on microbeads optimized by 22 factorial design resulted in a controlled release formulation of loratadine that provided zero-order release for 8 h.
Katarzyna Bober, Marlena Płonka and Marek Miszczyk
extractive spectrophotometric determination of loratadine, desloratadine and rupatadine from pharmaceutical formulations. Int. J. Pharma Bio Sci. 3(2), 89, 2012.
11. Renger B., Vegh Z., Ferenczi-Fodor K.: Validation of thin layer and high performance thin layer chromatographic methods. J. Chromatogr. A, 1218, 2712, 2011.
12. Srinubabu G. et al.: Development and validation of high-throughput liquid chromatography-tandem mass spectrometric method for simultaneous quantification of loratadine and desloratadine in human plasma. J. Chromatogr. B
Nona-Aura Florincescu-Gheorghe, Florica Popescu and D.O. Alexandru
1. Ebbo D. Allergic rhinitis in primary care: Results of the ORA survey in France. Rev Fr Allergol. 2011;doi:10.1016/j.reval.2011.05.009
2. Bousquet J, Khaltaev N, Cruz AA, et al. Allergic Rhinitis and its Impact on Asthma (ARIA) 2008 Update (in collaboration with the World HealthOrganization, GA (2)LEN and AllerGen). Allergy. 2008;63 Suppl 86:8-160.
3. Anolik R. Mometasone Furoate Nasal Spray with Loratadine Study Group. Clinical benefits of combination treatment with mometasone furoate nasal spray
Māris Bukovskis, Madara Tirzīte, Gunta Strazda, Normunds Jurka, Renāte Ligere, Sergejs Isajevs and Immanuels Taivans
levocetirizine and loratadine on histamine-induced wheal, flare, and itch in human skin. Allergy , 56 (10), 985-988.
Denham, K.J., Boutsiouki, P., Clough, G.F., Church, M.K. (2003). Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skin. Inflamm. Res. 52 , 424-427.
Deruaz, C., Leimgruber, A., Berney, M., Pradervand, E., Spertini, F. (2004). Levocetirizine better protects than desloratadine in a nasal provocation with allergen. J. Allergy Clin. Immunol
Antonin Lojek, Milan Číž, Michaela Pekarová, Gabriela Ambrožová, Ondřej Vašíček, Jana Moravcová, Lukáš Kubala, Katarína Drábiková, Viera Jančinová, Tomáš Perečko, Jana Pečivová, Tatiana Mačičková and Radomír Nosáľ
Modulation of metabolic activity of phagocytes by antihistamines
The purpose of the study was to investigate the effects of H1-antihistamines of the 1st generation (antazoline, bromadryl, brompheniramine, dithiaden, cyclizine, chlorcyclizine, chlorpheniramine, clemastine) and the 2nd generation (acrivastine, ketotifen, and loratadine) on the respiratory burst of phagocytes. Reactive oxygen species generation in neutrophils isolated from rat blood was measured using luminol-enhanced chemiluminescence. Changes in nitrite formation and iNOS protein expression by RAW 264.7 macrophages were analysed using Griess reaction and Western blotting. The antioxidative properties of drugs in cell-free systems were detected spectrophotometrically, luminometrically, fluorimetrically, and amperometrically. The majority of the H1-antihistamines tested (bromadryl, brompheniramine, chlorcyclizine, chlorpheniramine, clemastine, dithiaden, and ketotifen) exhibited a significant inhibitory effect on the chemiluminescence activity of phagocytes. H1-antihistamines did not show significant scavenging properties against superoxide anion and hydroxyl radical, thus this could not contribute to the inhibition of chemiluminescence. H1-antihistamines had a different ability to modulate nitric oxide production by LPS-stimulated macrophages. Bromadryl, clemastine, and dithiaden were the most effective since they inhibited iNOS expression, which was followed by a significant reduction in nitrite levels. H1-antihistamines had no scavenging activity against nitric oxide. It can be concluded that the effects observed in the H1-antihistamines tested are not mediated exclusively via H1-receptor pathway or by direct antioxidative properties. Based on our results, antihistamines not interfering with the microbicidal mechanisms of leukocytes (antazoline, acrivastine and cyclizine) could be used preferentially in infections. Other antihistamines should be used, under pathological conditions accompanied by the overproduction of reactive oxygen species.
-221; DOI: 10.2478/v10007-009-0019-6.
S. T. Prajapati, L. D. Patel and D. M. Patel, Gastric floating matrix tablets: Design and optimization using combination of polymers, Acta Pharm. 58 (2008) 221-229; DOI: 10.2478/v10007-008-0006-3.
S. K. Mishra and K. Pathak, Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine, Acta Pharm. 58 (2008) 187-197; DOI: 10.2478/v10007-008-0001-8.
J. G. Hardman, L. E. Limbird, A. G. Gilman (Eds.), Goodman and Gilman
Guo-Qing Wang, Jin-Long Hou, Huan-Yu Huang and Chao-Wen Yuan
.J., Czarlewski W., Campbell A.M., Bousquet J., Davies R.J.: Effect of loratadine on nitrogen dioxide–induced changes in electrical resistance and release of inflammatory mediators from cultured human bronchial epithelial cells. J Allergy Clin Immunol 1999, 104, 93–99.
5. Chapwanya A., Meade K.G., Narciandi F., Stanley P., Mee J.F., Doherty M.L., Callanan J.J.: Endometrial biopsy: a valuable clinical and research tool in bovine reproduction. Theriogenology 2010, 73, 988–994.
6. Cruz M.A., Gonzalez C., Sepulveda W.H., Rudolph M.I.: Effect of histamine on human