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Howard I. Maibach - One of the best experts on this subject based on the ideXlab platform.
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Simultaneous Diffusion and Metabolism of Betamethasone 17-Valerate in the Living Skin Equivalent
Journal of pharmaceutical sciences, 1995Co-Authors: Klyoshi Kubota, John I. Ademola, Howard I. MaibachAbstract:Simultaneous diffusion and metabolism of Betamethasone 17-valerate was studied using Betamethasone 17-valerate, Betamethasone 21-valerate, and Betamethasone as permeants. These corticosteroids were suspended in silicone adhesive and applied to an artificial living skin equivalent (LSE) for 72 h. When Betamethasone was applied, no metabolites were detected in the receptor medium. Conversely, with Betamethasone 21-valerate application, only Betamethasone but no Betamethasone 21-valerate was detected in the receptor medium indicating the metabolism of the latter by skin esterases. When tested with the theory for simultaneous diffusion and metabolism, the result is consistent with the enzyme rate constant in the LSE homogenate measured in a previous study. When Betamethasone 17-valerate was applied to the LSE, more than half of the total amount of corticosteroids detected in the receptor medium was unchanged, consistent with the previously reported chemical (as opposed to enzymatic) degradation half-life of about 8 h. This result also indicated that very little metabolism of Betamethasone 17-valerate occurred in the skin.
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Metabolism and degradation of Betamethasone 17-valerate in homogenized living skin equivalent.
Dermatology (Basel Switzerland), 1994Co-Authors: Kiyoshi Kubota, John I. Ademola, Howard I. MaibachAbstract:The metabolism of Betamethasone 17-valerate was estimated using an artificial living skin equivalent (LSE). Betamethasone 17-valerate, Betamethasone 21-valerate and Betamethasone were measured by a normal-phase high-performance liquid chromatographic (HPLC) method. Betamethasone 17-valerate was added to the culture medium with or without LSE homogenate. Degradation profiles (%) of Betamethasone 17-valerate remaining in the culture medium with skin homogenate did not differ from those without homogenate. However, the conversion of Betamethasone 21-valerate to Betamethasone was accelerated by skin homogenate, indicating that LSE has a sufficient level of esterase.
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Plasma concentrations of Betamethasone after topical application of Betamethasone 17-valerate: comparison with oral administration.
British journal of clinical pharmacology, 1994Co-Authors: Kiyoshi Kubota, G. Huttinot, P. H. Andersen, Howard I. MaibachAbstract:Plasma concentrations of Betamethasone were measured by r.i.a. after oral administration of 0.6 mg Betamethasone and topical application of Betamethasone 17-valerate in the same five healthy subjects. Betamethasone 17-valerate was prepared as a suspension in medical grade pressure sensitive adhesive and applied to a 100 cm2 area on the back for 28 h. Mean maximum plasma concentrations were 5.0 and 0.24 ng ml-1 and mean AUC values were 75.4 and 7.74 ng ml-1 h after oral and topical administrations, respectively. The mean plasma elimination half-life of Betamethasone after the removal of topical Betamethasone 17-valerate was 16.6 h which was twice that after oral administration, 8.1 h. Betamethasone 17-valerate may require application to the skin more than twice daily.
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In Vitro Percutaneous Permeation of Betamethasone and Betamethasone 17-Valerate
Journal of pharmaceutical sciences, 1993Co-Authors: Kiyoshi Kubota, Howard I. MaibachAbstract:The percutaneous permeation and sorption isotherm (equilibrium) profiles of Betamethasone and Betamethasone 17-valerate were estimated in an in vitro study with excised human skin. Corticosteroids were measured by HPLC. The stratum corneum (dry weight)/water partition coefficient of Betamethasone 17-valerate was 20 times greater than that of Betamethasone. Nevertheless, when aqueous saturation was maintained in the donor solution, the mean steady-state flux of Betamethasone 17-valerate through split-thickness skin was 57.6 ng/cm2/h, whereas that of Betamethasone was 15.2 ng/cm2/h. This was presumably because the aqueous saturation concentration of Betamethasone (60 micrograms/mL) was 11 times greater than that of Betamethasone 17-valerate (5.4 micrograms/mL), so that the calculated saturation concentrations of the two corticosteroids in stratum corneum were within a factor of 2. However, the drug amounts or concentrations of the more lipophilic corticosteroid (Betamethasone 17-valerate) attained in viable layers (viable epidermis and dermis) at steady state were predicted to be greater than those of the less lipophilic corticosteroid (Betamethasone) when the results in the permeation and equilibrium studies were interpreted by a mathematical model. The drug distribution pattern predicted (i.e., that a more lipophilic corticosteroid preferentially partitions into viable layers) was reasonable when compared with that observed in the permeation study. The mean drug amount of Betamethasone 17-valerate in dermis was four times greater than that of Betamethasone, whereas the drug amounts of both corticosteroids in epidermis were similar to each other.
Solange Maria Dieterich Rabelo Junqueira - One of the best experts on this subject based on the ideXlab platform.
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Influencia da betametasona, empregada na forma de preparações farmaceuticas distintas, sobre alguns valores de auto-hemostasia, em ratos
2017Co-Authors: Solange Maria Dieterich Rabelo JunqueiraAbstract:Resumo: Este trabalho teve por objetivo avaliar os efeitos da betametasona, empregada na forma de duas preparações farmacêuticas distintas, sobre alguns valores de auto-hemostasia. Para tanto,foram utilizados 30 ratos Wistar,machos,divididos em 3 grupos experimentais,tratados (via 1M) com solução de NaCI a 0,9% (Grupo Controle), fosfato dissódico de betametasona ou com a associação deste mesmo sal ao acetato de betametasona, que possibilita uma ação farmacológica de maior duração do glucocorticóide. Nos tempos de .1, 24, 48 e 168 horas após o tratamento, foram obtidas amostras de sangue e avaliado o tempo de coagulação sangüínea e o número de plaquetas circulantes. Os resultados obtidos demonstraram que o fosfato dissódico de betametasona, na dose única de 0,1mg/kg, não alterou os parâmetros de auto-hemostasia estudados. Quando a mesma dose da preparação farmacêutica de depósito de Betametasona foi empregada, observou-se apenas um Discreto aumento do Tempo de coagulação e uma pequena diminuição da contagem respectivamente nos tempos de 168 e 24 horas. de plaquetas , Apesar destas alterações serem estatisticamente significantes (p < 0,05), os valores encontrados situaram-se dentro das faixas de normalidade biológica do tempo de coagulação sangüínea e contagem de plaquetas, em ratosAbstract: The aim of this paper was to study the effeets of two distinet pharmaceutieal preparations of Betamethasone, values of auto-hemostasis. To do so, 30 male Wistar rats were used, divided in 3 upon the experimental groups, dissodium phosphate betametasone acetate. Treated with normal saline, betametasone or with this salt associated with After 1, 24, 48 and 168 hours of these distinct treatments, blood samples were obtained and avaliated the clotting time and platelet count.The results showed no interference of the Betamethasone Dissodium phosphate (0,1 mg / kg) , In the values of the auto-hemostasis parameters studied. In the animals treated with the depot preparati ns of Betamethasone, there was a discret increase of the c clotting time and a little decrease of the platelet count, in the times of 168 and 24 hours, respectively. In spite of this alterations are statisticaly significant (p < 0,05), these values are situated in biological normal ranges for the clotting time and platelet count, in rat
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Influencia da betametasona, empregada na forma de preparações farmaceuticas distintas, sobre alguns valores de auto-hemostasia, em ratos
Universidade Estadual de Campinas. Faculdade de Odontologia de Piracicaba, 1992Co-Authors: Solange Maria Dieterich Rabelo JunqueiraAbstract:Este trabalho teve por objetivo avaliar os efeitos da betametasona, empregada na forma de duas preparações farmacêuticas distintas, sobre alguns valores de auto-hemostasia. Para tanto,foram utilizados 30 ratos Wistar,machos,divididos em 3 grupos experimentais,tratados (via 1M) com solução de NaCI a 0,9% (Grupo Controle), fosfato dissódico de betametasona ou com a associação deste mesmo sal ao acetato de betametasona, que possibilita uma ação farmacológica de maior duração do glucocorticóide. Nos tempos de .1, 24, 48 e 168 horas após o tratamento, foram obtidas amostras de sangue e avaliado o tempo de coagulação sangüínea e o número de plaquetas circulantes. Os resultados obtidos demonstraram que o fosfato dissódico de betametasona, na dose única de 0,1mg/kg, não alterou os parâmetros de auto-hemostasia estudados. Quando a mesma dose da preparação farmacêutica de depósito de Betametasona foi empregada, observou-se apenas um Discreto aumento do Tempo de coagulação e uma pequena diminuição da contagem respectivamente nos tempos de 168 e 24 horas. de plaquetas , Apesar destas alterações serem estatisticamente significantes (p < 0,05), os valores encontrados situaram-se dentro das faixas de normalidade biológica do tempo de coagulação sangüínea e contagem de plaquetas, em ratosThe aim of this paper was to study the effeets of two distinet pharmaceutieal preparations of Betamethasone, values of auto-hemostasis. To do so, 30 male Wistar rats were used, divided in 3 upon the experimental groups, dissodium phosphate betametasone acetate. Treated with normal saline, betametasone or with this salt associated with After 1, 24, 48 and 168 hours of these distinct treatments, blood samples were obtained and avaliated the clotting time and platelet count.The results showed no interference of the Betamethasone Dissodium phosphate (0,1 mg / kg) , In the values of the auto-hemostasis parameters studied. In the animals treated with the depot preparati ns of Betamethasone, there was a discret increase of the c clotting time and a little decrease of the platelet count, in the times of 168 and 24 hours, respectively. In spite of this alterations are statisticaly significant (p < 0,05), these values are situated in biological normal ranges for the clotting time and platelet count, in rat
L. Vaillant - One of the best experts on this subject based on the ideXlab platform.
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Topical rapamycin versus Betamethasone dipropionate ointment for treating oral erosive lichen planus: a randomized, double‐blind, controlled study
Journal of the European Academy of Dermatology and Venereology, 2020Co-Authors: Mahtab Samimi, A. Le Gouge, F. Boralevi, T. Passeron, F. Pascal, P. Bernard, S Agbo‐godeau, S. Leducq, Jc Fricain, L. VaillantAbstract:Background Although superpotent topical corticosteroids are the first-line treatment for oral erosive lichen planus (OELP), topical rapamycin was found efficient in a previous case series. Objectives To compare the efficacy and safety of topical rapamycin and Betamethasone dipropionate ointment for OELP in a randomized, double-blind trial. Methods Patients were randomized to receive treatment with Betamethasone dipropionate ointment 0.05% in Orabase(R) or topical rapamycin solution (1 mg/mL) on lesions twice daily for 3 months, followed by 3 months of observation. The primary outcome was clinical remission after 3 months of treatment. Secondary outcomes were clinical remission after 1 and 2 months, reduced oral pain and reduced impact on food intake after 3 months, clinical recurrence after treatment withdrawal, and adverse events. Results During a 4-year period, 76 patients were randomized and 75 received treatment (rapamycin, n = 39; Betamethasone, n = 36). At 3 months, 39.4% of patients with Betamethasone and 27.3% with rapamycin showed clinical remission (odds ratio 0.68, 95% CI [0.24; 1.89]; P = 0.46). Rates of remission after 1 and 2 months, reduction in pain and impact on food intake after 3 months, were higher with Betamethasone than rapamycin. Recurrence of oral erosions was similar between groups. Adverse events occurred in 43.6% of patients with rapamycin (mostly burning sensation, impaired taste) and 27.8% with Betamethasone (mostly oral candidiasis). Conclusion Although the study was limited by insufficient recruitment, we did not find any superiority of topical rapamycin over Betamethasone dipropionate ointment for OELP. Given the rapid remission and pain improvement in the Betamethasone group, it appears that superpotent topical corticosteroids should remain the first-line treatment for OELP.
Andreas Katsambas - One of the best experts on this subject based on the ideXlab platform.
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efficacy and safety of tacrolimus ointment 0 1 vs Betamethasone 17 valerate 0 1 in the treatment of chronic paronychia an unblinded randomized study
British Journal of Dermatology, 2009Co-Authors: Dimitris Rigopoulos, George Larios, Stamatios Gregoriou, E Belyayeva, Georgios Kontochristopoulos, Andreas KatsambasAbstract:Summary Background Recent studies have established the pivotal role of irritants and allergens in development of chronic paronychia and the significant improvement with corticosteroid therapy. Objectives The objective of this randomized, unblinded, comparative study was to compare the efficacy of tacrolimus ointment 0·1% vs. Betamethasone 17-valerate 0·1% in the treatment of chronic paronychia. Methods Forty-five patients with chronic paronychia were randomized 1 : 1 : 1 to apply twice daily either Betamethasone 17-valerate 0·1% or tacrolimus 0·1% ointment or emollient. Protective measures were counselled to all patients. Treatment duration was 3 weeks and patients were followed for an additional 6 weeks. Results Eight patients in the Betamethasone group were considered as cured, two as improved and four as nonresponders at the end of the treatment period. Thirteen patients in the tacrolimus group were considered as cured and one as improved at the end of the treatment period. Nine patients in the emollient group were considered as stable and six failed to respond. Both Betamethasone and tacrolimus groups presented statistically significantly greater cure or improvement rates when compared with the emollient group (P < 0·001). Conclusions Tacrolimus ointment appears to be a more efficacious agent than Betamethasone 17-valerate or placebo for the treatment of chronic paronychia.
Mahtab Samimi - One of the best experts on this subject based on the ideXlab platform.
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Topical rapamycin versus Betamethasone dipropionate ointment for treating oral erosive lichen planus: a randomized, double‐blind, controlled study
Journal of the European Academy of Dermatology and Venereology, 2020Co-Authors: Mahtab Samimi, A. Le Gouge, F. Boralevi, T. Passeron, F. Pascal, P. Bernard, S Agbo‐godeau, S. Leducq, Jc Fricain, L. VaillantAbstract:Background Although superpotent topical corticosteroids are the first-line treatment for oral erosive lichen planus (OELP), topical rapamycin was found efficient in a previous case series. Objectives To compare the efficacy and safety of topical rapamycin and Betamethasone dipropionate ointment for OELP in a randomized, double-blind trial. Methods Patients were randomized to receive treatment with Betamethasone dipropionate ointment 0.05% in Orabase(R) or topical rapamycin solution (1 mg/mL) on lesions twice daily for 3 months, followed by 3 months of observation. The primary outcome was clinical remission after 3 months of treatment. Secondary outcomes were clinical remission after 1 and 2 months, reduced oral pain and reduced impact on food intake after 3 months, clinical recurrence after treatment withdrawal, and adverse events. Results During a 4-year period, 76 patients were randomized and 75 received treatment (rapamycin, n = 39; Betamethasone, n = 36). At 3 months, 39.4% of patients with Betamethasone and 27.3% with rapamycin showed clinical remission (odds ratio 0.68, 95% CI [0.24; 1.89]; P = 0.46). Rates of remission after 1 and 2 months, reduction in pain and impact on food intake after 3 months, were higher with Betamethasone than rapamycin. Recurrence of oral erosions was similar between groups. Adverse events occurred in 43.6% of patients with rapamycin (mostly burning sensation, impaired taste) and 27.8% with Betamethasone (mostly oral candidiasis). Conclusion Although the study was limited by insufficient recruitment, we did not find any superiority of topical rapamycin over Betamethasone dipropionate ointment for OELP. Given the rapid remission and pain improvement in the Betamethasone group, it appears that superpotent topical corticosteroids should remain the first-line treatment for OELP.