Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new nasacort research articles will be listed here shortly after becoming available to us.
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Medical research on nasacort
Drug Dev Ind Pharm. 2003 Oct; 29(9): 1005-12
Sharpe SA, Sandweiss V, Tuazon J, Giordano M, Witchey-Lakshmanan L, Hart J, Sequeira J
Many aqueous suspension corticosteroid nasal sprays become less viscous when shaken and sprayed, then return to a more viscous state after application. This time-dependent, reversible loss of viscosity under shear (e.g., shaking or spraying) can be quantified in the rheological property of thixotropy. The flow properties of 5 corticosteroid nasal sprays were measured over a range of shear rates. The formulations tested included Nasonex, Vancenase AQ, Nasacort AQ, Rhinocort Aqua, and Flonase. The yield stress values, as well as an estimate of thixotropy, were compared by using three different sampling techniques, including one that simulated patient use (shaking for 30 sec, spraying, and immediately transferring the sample to the rheometer). The rheological properties of all products indicated that when initially shaken and dispensed, they flowed more freely, followed by recovery of viscosity that would likely inhibit the suspensions from flowing out of the nasal cavity. Under all three tested conditions, Nasonex exhibited the highest yield stress, the largest apparent initial and final viscosities, and the highest apparent thixotropy. The study protocol that simulated patient-use conditions produced the following rank order of measured thixotropy: Nasonex > Flonase > Vancenase AQ > Rhinocort Aqua > Nasacort AQ. The thixotropy of Nasonex was 3.4 to 21.4 times greater and the final viscosity was 3.2 to 17.4 times greater than the values of the other tested products.
J Clin Pharmacol. 2002 Jun; 42(6): 662-9
Hochhaus G, González MA, Dockhorn RJ, Shilstone J, Karafilidis J
The present study was undertaken to describe the pharmacokinetics of a new solution-based intranasal triamcinolone acetonideformulation (Tri-Nasal) in patients with perennial allergic rhinitis and to use a pharmacokinetic/pharmacodynamic (PK/PD) simulation approach to compare the potential effects on plasma cortisol with that of an aqueous suspension-based nasal triamcinolone acetonide formulation (Nasacort AQ). Data from an open-label, randomized, three-way crossover study in patients with perennial allergic rhinitis receiving three doses (100, 200, and 400 microg) of a nasal solution-based triamcinolone acetonide formulation (Tri-Nasal) over 7 days were used to describe the pharmacokinetics of this formulation. Available literature data for a suspension-based aqueous triamcinolone acetonide formulation (Nasacort AQ) were used to describe its pharmacokinetic profile after similar single doses of 110, 220, and 440 microg. A PK/PD simulation approach was used to predict the anticipated cumulative cortisol suppression (CCS) of these two formulations. These simulations suggested a cortisol suppression of 8% to 16% for the single and steady-state doses of the solution-based product. Similar CCS estimates were predicted for equivalent doses of the aqueous suspension-based triamcinolone acetonide formulation with no difference between both formulations. Post hoc power analysis suggested that the predicted cortisol suppression is not likely to be significant for either preparation, including the clinically recommended doses of 200 and 220 microg of the solution-based and suspension-based formulations, respectively. In summary, based on the results of this PK/PD simulation, the plasma levels observed afternasal administration of the solution or the aqueous suspension are unlikely to induce a clinically relevant cortisol suppression, especially for the recommended dosing regimens of 200 and 220 microg/day.
J Pharm Pharmacol. 2000 Oct; 52(10): 1223-32
Eccleston GM, Hudson NE
The rheological profiles of four commercial nasal spray suspensions (Beconase, Flixonase, Nasacort and Nasonex) were compared using rotational viscometry. Two of the nasal sprays (Beconase and Nasonex) were further examined in both shear and extension using a capillary rheometer under conditions similar to those experienced at the spray nozzle (i.e. extremely high shear rates with significant stretching or extensional flow). In rotation, the shear viscosity fell rapidly with increase in shear rate. Plots of the viscosity derived at the lower shear rates in rotation were extrapolated to include the high-shear rate capillary values. At very high shear rates, the shear viscosity of Beconase was higher than that of Nasonex with the cross-over occurring in the extrapolated region at approximately 10,000 s(-1). In the transition region between laminar and turbulent flow (shear rate 6-8 x 10(4) s(-1)) there was a minimum in the shear viscosity to less than that of water for Nasonex and similar to water for Beconase, and a plateau region in extensional viscosity for Beconase but not Nasonex. These anomalies were due to the extensive aeration of both samples when sprayed. Whereas Beconase had de-aerated within 30 min of the experiment, Nasonex had not de-aerated completely after six weeks. The very low viscosity at the shear rates at the nozzle imply that it is unlikely that the low viscosity of the spray on delivery to the nose is a key factor in prolonging its residence time. The extensional viscosity for these rather fluid samples was over 1000-times the shear viscosity (not 3-times as with Newtonian fluids) and both sprays exhibited strain hardening over the range covered. The high extensional stress in the nozzle enables the fluid to form as reasonably sized droplets rather than fine atomized droplets, which rather than settling in the nose, would be prone to redistribution through the normal respiratory function. Both sprays resisted degradation despite the high shear rates and extensional stresses experienced.
Rheological behavior of nasal sprays in shear and extension.
Drug Dev Ind Pharm. 2000 Sep; 26(9): 975-83
Eccleston GM, Bakhshaee M, Hudson NE, Richards DH
The rheological profiles of commercial corticosteroid nasal spray suspensions (Beconase, Nasacort, Flixonase, and Nasonex) were compared using shear and extensional techniques. Thixotropy/shear thinning was investigated (Carri-Med CSL100, concentric cylinder geometry) by (a) the generation of flow curves at low (100 sec-1) and high (1200 sec-1) maximum shear rates and (b) determination of equilibrium shear viscosities at constant shear rates of 10 sec-1, 100 sec-1, or 1200 sec-1. Extensional properties, on which droplet breakup and size depend, were examined using digital camera photography of droplet evolution and the length any trailing filament formed when the suspension was extruded from a 10-ml syringe at 500 microliters/min. All the nasal suspensions were shear thinning and were also thixotropic to varying degrees. The absence of significant thixotropic recovery at short times (5 min) for all the sprays implies that thixotropy is not necessarily the controlling factor for prolonged residence of the spray in the nasal cavity, but rather that it is the high viscosities present in all four sprays, even after structure breakdown. Preliminary extensional flow data identified differences among the four sprays, with extensional filament lengths increasing in the same rank order as the lowest shear rate (10 sec-1) equilibrium viscosities.
Am J Rhinol. 1998 Nov-Dec; 12(6): 427-33
Rosenthal R, Berger W, Bronsky E, Dockhorn R, Korenblat P, Lampl K, Lumry W, Pollard S, Raphael G, Rohr C, Shapiro G, Valentine M, Wanderer A, Fleming L, LaVallee N, Stepanians M, Karafilidis J, Shilstone J, Ellis E
Tri-Nasal Nasal Spray is an investigational solution of triamcinolone acetonide (TAA) currently being evaluated as a treatment for allergic rhinitis. The safety and efficacy of 200 and 400 micrograms once daily doses of Tri-Nasal Nasal Spray, an active control (440 micrograms once daily of Nasacort Nasal aerosol), and Tri-Nasal Nasal Spray placebo were compared over a 2-week treatment period in a double-blind (the Nasacort treatment was not blinded), parallel design trial. A total of 377 adult patients in 13 centers were enrolled during the grass pollen season. The primary efficacy variable was the weekly average of the SSI (Symptom Severity Index), the sum of daily nasal congestion, rhinorrhea, and sneezing severity scores from the patient diary. A total of 355 patients completed the study. All active treatments were significantly more effective than placebo in relieving nasal symptoms at each treatment week. The 400 micrograms Tri-Nasal Nasal Spray and Nasacort treatments had a rapid onset of action, demonstrating significant improvement in the SSI versus placebo by the second day of treatment. Results for the individual nasal symptoms and other secondary efficacy measures paralleled those of the primary efficacy variables. Tri-Nasal Nasal Spray and Nasacort were comparable in safety, and in treating the nonocular symptoms of seasonal allergic rhinitis.
Biodistribution and kinetics of nasal carbon-11-triamcinolone acetonide.
J Nucl Med. 1998 Nov; 39(11): 1972-7
Berridge MS, Heald DL, Muswick GJ, Leisure GP, Voelker KW, Miraldi F
PET is a technique with a strong potential for use in drug evaluation and development. In particular, the distribution and pharmacokinetics of locally administered drugs may be advantageously explored noninvasively using labeled compounds. This pilot study was performed to demonstrate the effectiveness of PET for drug development and to determine the human biodistribution and kinetics of triamcinolone acetonide, labeled with 11C, formulated and nasally administered as Nasacort AQ nasal inhalant. METHODS: Carbon-11-labeled triamcinolone acetonide was formulated as the commercial product, and PET scans of the heads of four volunteers were performed in a vertical orientation. Region-of-interest analysis with MRI coregistration was used to analyze the distribution and kinetics in nasal tissues. RESULTS: Deposition of the majority of the dose on target tissues was immediate. Penetration into sinuses was observed. There was moderate redistribution and slow migration of the drug through nasal passages to the throat. Significant amounts of the drug remained in target regions for several hours. CONCLUSION: PET is an effective means to determine local drug distribution and kinetics.
Ann Allergy. 1992 Mar; 68(3): 228-32
Findlay S, Huber F, Garcia J, Huang L
A 4-week, double-blind, parallel group study compared the safety and efficacy of once-a-day intranasal administration of triamcinolone acetonide (Nasacort) versus placebo in 304 patients (155 adult and 149 adolescent) with seasonal allergic rhinitis. Patients were randomized to receive triamcinolone acetonide (110, 220, or 440 microgram) or placebo once daily each morning. Daily rhinitis symptoms scores, weekly patient and physician global assessments, and weekly nasal eosinophil smears were obtained. In each triamcinolone acetonide group, significant (P less than .05) improvement over placebo was noted in the nasal index (sum of ratings for stuffiness, discharge, and sneezing) by week 1, the first point of analysis, and maintained throughout the study. Triamcinolone acetonide groups also demonstrated significant (P less than .05) improvement over placebo in all individual rhinitis symptoms evaluated. The greatest improvement in symptoms was observed at the 440 microgram dose. A significant decrease in eosinophil counts paralleled clinical improvement in all triamcinolone acetonide groups. Physicians and patients rated triamcinolone acetonide significantly (P less than .05) more effective than placebo. Responses of adult and adolescent patients were comparable. Adverse experiences, clinical laboratory values, and results of physical examinations were unremarkable and comparable between the triamcinolone acetonide and placebo groups. We conclude that triamcinolone acetonide is safe, well tolerated, and superior to placebo as a once-a-day treatment for seasonal allergic rhinitis.