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  1. Sivadasan D, Venkatesan K, Mohamed JMM, Alqahtani S, Asiri YI, Faisal MM, et al.
    Sci Rep, 2024 Mar 16;14(1):6361.
    PMID: 38493177 DOI: 10.1038/s41598-024-55953-2
    Loratadine (LoR) is a highly lipophilic and practically insoluble in water, hence having a low oral bioavailability. As it is formulated as topical gel, it competitively binds with the receptors, thus reducing the side-effects. The objective of this study was to prepare LoR loaded nanosponge (LoR-NS) in gel for topical delivery. Nine different formulations of emulsion were prepared by solvent evaporation method with polyvinyl alcohol (PVA), ethyl cellulose (EC), and dichloromethane (DCM). Based on 32 Full Factorial Design (FFD), optimization was carried out by varying the concentration of LOR:EC ratio and stirring rate. The preparations were subjected for the evaluation of particle size (PS), in vitro release, zeta potential (ZP) and entrapment efficiency (EE). The results revealed that the NS dispersion was nanosized with sustained release profiles and significant PS. The optimised formulation was formulated and incorporated into carbopol 934P hydrogel. The formulation was then examined to surface morphological characterizations using scanning electron microscopy (SEM) which depicted spherical NS. Stability studies, undertaken for 2 months at 40 ± 2 °C/75 ± 5% RH, concluded to the stability of the formulation. The formulation did not cause skin irritation. Therefore, the prepared NS hydrogel proved to be a promising applicant for LoR as a novel drug delivery system (NDDS) for safe, sustained and controlled topical application.
    Matched MeSH terms: Loratadine*
  2. Zeeshan F, Bukhari NI
    AAPS PharmSciTech, 2010 Jun;11(2):910-6.
    PMID: 20496016 DOI: 10.1208/s12249-010-9456-2
    Modified-release multiple-unit tablets of loratadine and pseudoephedrine hydrochloride with different release profiles were prepared from the immediate-release pellets comprising the above two drugs and prolonged-release pellets containing only pseudoephedrine hydrochloride. The immediate-release pellets containing pseudoephedrine hydrochloride alone or in combination with loratadine were prepared using extrusion-spheronization method. The pellets of pseudoephedrine hydrochloride were coated to prolong the drug release up to 12 h. Both immediate- and prolonged-release pellets were filled into hard gelatin capsule and also compressed into tablets using inert tabletting granules of microcrystalline cellulose Ceolus KG-801. The in vitro drug dissolution study conducted using high-performance liquid chromatography method showed that both multiple-unit capsules and multiple-unit tablets released loratadine completely within a time period of 2 h, whereas the immediate-release portion of pseudoephedrine hydrochloride was liberated completely within the first 10 min of dissolution study. On the other hand, the release of pseudoephedrine hydrochloride from the prolonged release coated pellets was prolonged up to 12 hr and followed zero-order release kinetic. The drug dissolution profiles of multiple-unit tablets and multiple-unit capsules were found to be closely similar, indicating that the integrity of pellets remained unaffected during the compression process. Moreover, the friability, hardness, and disintegration time of multiple-unit tablets were found to be within BP specifications. In conclusion, modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride was successfully developed and evaluated.
    Matched MeSH terms: Loratadine/administration & dosage*; Loratadine/chemistry*
  3. Lee ST, Amin MJ
    Singapore Med J, 1994 Dec;35(6):591-4.
    PMID: 7761882
    Nonsedating selective peripheral H1 receptor antagonists are an important advance in antihistaminic therapy in allergic patients. This is a randomised, double-blind parallel group study comparing the use of two such agents viz loratadine 10mg daily and astemizole 10mg daily for two weeks in 39 Malaysian allergic rhinitis patients. At these dosages, both drugs were demonstrated to be efficacious (p < 0.05) for controlling nasal symptoms and safe in terms of short term biochemical and haematological changes and adverse effects noted. Evaluating efficacy criteria utilised in this study loratadine and astemizole were comparable but loratadine was significantly more effective in three areas viz: (i) in diminishing nasal symptoms after 2 weeks of treatment (p = 0.03); (ii) physician's efficacy evaluation after 2 weeks' treatment (p = 0.009); (iii) patient's efficacy evaluation after 2 weeks' treatment (p = 0.019).
    Study site: Allergy clinic, University Malaya Medical Centre (UMMC), Kuala Lumpur, Malaysia
    Matched MeSH terms: Loratadine/adverse effects; Loratadine/therapeutic use*
  4. Asha'ari ZA, Ahmad MZ, Jihan WS, Che CM, Leman I
    Ann Saudi Med, 2013;33(5):469-75.
    PMID: 24188941 DOI: 10.5144/0256-4947.2013.469
    BACKGROUND AND OBJECTIVES: The role of honey in the treatment of allergic rhinitis (AR) is controversial. We studied the complementary effect of ingestion of a high dose of honey, in addition to standard medications, on AR.

    DESIGN AND SETTINGS: Prospective randomized placebo-controlled study. Subjects were recruited from an otolaryngology clinic in 2 tertiary referral centers in the East coast of Peninsular Malaysia. The study period ranged from April 2010-April 2011.

    METHODS: Forty AR patients were divided equally into a case group and a control group. All the subjects received a daily dose of 10 mg of loratadine for 4 weeks. The case group ingested 1 g/kg body weight of honey daily in separate doses for the 4-week period. The control group ingested the same dose of honey-flavored corn syrup as placebo. AR symptoms were scored at the start, week 4, and week 8 of the study.

    RESULTS: There were no significant differences between the mean total symptom score of the case and the control groups at the start of the study. At week 4, both groups showed progressive improvement in the symptoms; at week 8, only the case group showed a continuous improvement in the symptom score. Only the group that ingested honey showed a significant improvement in individual AR symptoms. The improvement persisted for a month after the cessation of the treatment.

    CONCLUSION: Honey ingestion at a high dose improves the overall and individual symptoms of AR, and it could serve as a complementary therapy for AR.

    Matched MeSH terms: Loratadine/administration & dosage; Loratadine/therapeutic use*
  5. Wong TW, Deepak KG, Taib MN, Anuar NK
    Int J Pharm, 2007 Oct 1;343(1-2):122-30.
    PMID: 17597317
    The capacity of microwave non-destructive testing (NDT) technique to characterize the matrix property of binary polymeric films for use as transdermal drug delivery system was investigated. Hydroxypropylmethylcellulose (HPMC) and polyethylene glycol (PEG) 3000 were the choice of polymeric matrix and plasticizer, respectively with loratadine as the model drug. Both blank and drug loaded HPMC-PEG 3000 films were prepared using the solvent-evaporation method. These films were conditioned at the relative humidity of 25, 50 and 75% prior to physicochemical characterization using the established methods of ultra-violet spectrophotometry, differential scanning calorimetry and Fourier transform infrared spectroscopy methods, as well as, novel microwave NDT technique. Blank films exhibited a greater propensity of polymer-polymer interaction at the O-H domain upon storage at a lower level of relative humidity, whereas drug loaded films exhibited a greater propensity of polymer-polymer, polymer-plasticizer and/or drug-polymer interaction via the O-H, C-H and/or aromatic C=C functional groups when they were stored at a lower or moderate level of relative humidity. The absorption and transmission characteristics of both blank and drug loaded films for microwave varied with the state of polymer-polymer, polymer-plasticizer, and/or drug-polymer interaction of the matrix. The measurements of microwave NDT test at 8 and 12 GHz were sensitive to the polar fraction of film involving functional group such as O-H moiety and the less polar environment of matrix consisting of functional groups such as C-H and aromatic C=C moieties. The state of interaction between polymer, plasticizer and/or drug of a binary polymeric film can be elucidated through its absorption and transmission profiles of microwave.
    Matched MeSH terms: Loratadine/chemistry*
  6. Anuar NK, Wui WT, Ghodgaonkar DK, Taib MN
    J Pharm Biomed Anal, 2007 Jan 17;43(2):549-57.
    PMID: 16978823
    The applicability of microwave non-destructive testing (NDT) technique in characterization of matrix property of pharmaceutical films was investigated. Hydroxypropylmethylcellulose and loratadine were selected as model matrix polymer and drug, respectively. Both blank and drug loaded hydroxypropylmethylcellulose films were prepared using the solvent-evaporation method and were conditioned at the relative humidity of 25, 50 and 75% prior to physicochemical characterization using microwave NDT technique as well as ultraviolet spectrophotometry, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) techniques. The results indicated that blank hydroxypropylmethylcellulose film exhibited a greater propensity of polymer-polymer interaction at the O-H and C-H domains of the polymer chains upon conditioned at a lower level of relative humidity. In the case of loratadine loaded films, a greater propensity of polymer-polymer and/or drug-polymer interaction via the O-H moiety was mediated in samples conditioned at the lower level of relative humidity, and via the C-H moiety when 50% relative humidity was selected as the condition for sample storage. Apparently, the absorption and transmission characteristics of both blank and drug loaded films for microwave varied with the state of polymer-polymer and/or drug-polymer interaction involving the O-H and C-H moieties. The measurement of microwave NDT test at 8GHz was sensitive to the chemical environment involving O-H moiety while it was greatly governed by the C-H moiety in test conducted at a higher frequency band of microwave. Similar observation was obtained with respect to the profiles of microwave NDT measurements against the state of polymer-polymer and/or drug-polymer interaction of hydroxypropylmethylcellulose films containing chlorpheniramine maleate. The microwave NDT measurement is potentially suitable for use as an apparent indicator of the state of polymer-polymer and drug-polymer interaction of the matrix.
    Matched MeSH terms: Loratadine/administration & dosage; Loratadine/chemistry
  7. Dong AN, Ahemad N, Pan Y, Palanisamy UD, Yiap BC, Ong CE
    Curr Mol Pharmacol, 2020;13(3):233-244.
    PMID: 31713493 DOI: 10.2174/1874467212666191111110429
    BACKGROUND: There is a large inter-individual variation in cytochrome P450 2C19 (CYP2C19) activity. The variability can be caused by the genetic polymorphism of CYP2C19 gene. This study aimed to investigate the molecular and kinetics basis for activity changes in three alleles including CYP2C19*23, CYP2C19*24 and CYP2C19*25found in the Chinese population.

    METHODS: The three variants expressed by bacteria were investigated using substrate (omeprazole and 3- cyano-7-ethoxycoumarin[CEC]) and inhibitor (ketoconazole, fluoxetine, sertraline and loratadine) probes in enzyme assays along with molecular docking.

    RESULTS: All alleles exhibited very low enzyme activity and affinity towards omeprazole and CEC (6.1% or less in intrinsic clearance). The inhibition studies with the four inhibitors, however, suggested that mutations in different variants have a tendency to cause enhanced binding (reduced IC50 values). The enhanced binding could partially be explained by the lower polar solvent accessible surface area of the inhibitors relative to the substrates. Molecular docking indicated that G91R, R335Q and F448L, the unique mutations in the alleles, have caused slight alteration in the substrate access channel morphology and a more compact active site cavity hence affecting ligand access and binding. It is likely that these structural alterations in CYP2C19 proteins have caused ligand-specific alteration in catalytic and inhibitory specificities as observed in the in vitro assays.

    CONCLUSION: This study indicates that CYP2C19 variant selectivity for ligands was not solely governed by mutation-induced modifications in the active site architecture, but the intrinsic properties of the probe compounds also played a vital role.

    Matched MeSH terms: Loratadine
  8. Lee LM, Gendeh BS
    Med J Malaysia, 2003 Mar;58(1):17-20.
    PMID: 14556322
    Allergic rhinitis causes an impairment of the mucociliary function in the nose. It is hoped that treatment of perennial allergic rhinitis would be able to revert mucociliary function to normal. This study aims to compare pre and post treatment mucociliary transport time in 3 different treatment modalities. Ninety-two newly diagnosed patients with allergic rhinitis were randomised into 3 groups and started on different treatment regimes. At the end of 8 weeks, the group treated with only intranasal beclomethasone showed some, though not significant, improvement in the mucociliary function. There were no changes in the mucociliary function in the other two groups treated with beclomethasone and loratidine or loratidine alone.

    Study site: ENT clinic in Pusat Perubatan Universiti Kebangsaan Malaysia (PPUKM)
    UKM
    Matched MeSH terms: Loratadine/administration & dosage; Loratadine/therapeutic use*
  9. Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y
    Ther Clin Risk Manag, 2016;12:585-97.
    PMID: 27110120 DOI: 10.2147/TCRM.S105189
    Allergic rhinitis and urticaria are common allergic diseases that may have a major negative impact on patients' quality of life. Bilastine, a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. This agent does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans, suggesting that it has very low potential for drug-drug interactions, and does not require dose adjustment in renal impairment. As bilastine is not metabolized and is excreted largely unchanged, hepatic impairment is not expected to increase systemic exposure above the drug's safety margin. Bilastine has demonstrated similar efficacy to cetirizine and desloratadine in patients with seasonal allergic rhinitis and, in a Vienna Chamber study, a potentially longer duration of action than fexofenadine in patients with asymptomatic seasonal allergic rhinitis. It has also shown significant efficacy (similar to that of cetirizine) and safety in the long-term treatment of perennial allergic rhinitis. Bilastine showed similar efficacy to levocetirizine in patients with chronic spontaneous urticaria and can be safely used at doses of up to fourfold higher than standard dosage (80 mg once daily). The fourfold higher than standard dose is specified as an acceptable second-line treatment option for urticaria in international guidelines. Bilastine is generally well tolerated, both at standard and at supratherapeutic doses, appears to have less sedative potential than other second-generation antihistamines, and has no cardiotoxicity. Based on its pharmacokinetic properties, efficacy, and tolerability profile, bilastine will be valuable in the management of allergic rhinitis and urticaria.
    Matched MeSH terms: Loratadine
  10. Abdullah B, Snidvongs K, Recto M, Poerbonegoro NL, Wang Y
    Multidiscip Respir Med, 2020 Jan 28;15(1):726.
    PMID: 33376593 DOI: 10.4081/mrm.2020.726
    Background: In primary care, general practitioners (GPs) and pharmacists are tasked with the frontline responsibility of identifying and managing allergic rhinitis (AR) patients. There are currently no consolidated data on current treatment practices, patient compliance, and usage of guidelines within Southeast Asian Nations (ASEAN). Objective: To assess the attitudes and practices on AR of GPs and pharmacists in 4 ASEAN countries (Philippines, Indonesia, Thailand, and Malaysia).

    Methods: A cross-sectional survey of 329 GPs and 548 pharmacists was conducted from May to November 2019. Participants answered a questionnaire focused on their i) current practice in the management of AR, ii) views on patient compliance, iii) understanding and usage of guidelines.

    Results: Clinical history was the most preferred method to diagnose AR by 95.4% of GPs and 58.8% of pharmacists. Second-generation antihistamines were the most widely available treatment option in GP clinics and pharmacies (94.8% and 97.2%) and correspondingly the most preferred treatment for both mild (90.3%, 76.8%) to moderatesevere rhinitis (90.3%, 78.6%) by GPs and pharmacists, respectively. Loratadine was ranked as the most preferred 2nd generation antihistamines (GP vs pharmacists: 55.3% vs 58.9%). More than 90% of GPs and pharmacists ranked length and efficacy of treatment as important factors that increase patient compliance. Awareness of the ARIA guidelines was high among GPs (80%) and lower among pharmacists (48.4%). However, only 63.3% of GPs and 48.2% of pharmacists knew how to identify AR patients.

    Conclusions: The survey in the 4 ASEAN countries has identified a need to strengthen the awareness and use of ARIA guidelines among the primary care practitioners. Adherence to ARIA guidelines, choosing the appropriate treatment option and prioritizing factors that increases patient compliance may contribute to better management outcomes of AR at the primary care practice.

    Matched MeSH terms: Loratadine
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