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Dr_Dan ★★ Germany, 2015-02-05 15:24 (3360 d 08:16 ago) Posting: # 14380 Views: 3,145 |
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Hi everyone In oral pharmaceutical formulations, combinations of methylparaben and propylparaben are applied with concentrations generally ranging from 0.015 to 0.2% for methylparaben and 0.02% to 0.06% for propylparaben. Due to possible endocrine-disrupting effects in humans parabenes are no longer allowed for use as a food additive within the European Union and in pharmaceutical preparations wherever possible the use of parabens should be avoided, particularly in case of paediatric formulations and/or the concentration used should be at the lowest feasible level according to the reflection paper on the use of methyl- and propylparaben as excipients in human medicinal products for oral use EMA/CHMP/SWP/272921/2012. Does by chance anybody know if for a generic test formulation a difference in the content of parabens in comparison to an oral liquid reference formulation could have an influence on bioavailability/bioequivalence of a drug? I am looking forward to your replies and a fruitful discussion. Kind regards Dr_Dan — Kind regards and have a nice day Dr_Dan |
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luvblooms ★★ India, 2015-02-19 06:59 (3346 d 16:41 ago) @ Dr_Dan Posting: # 14459 Views: 2,306 |
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Hi Dr_Dan ❝ Does by chance anybody know if for a generic test formulation a difference in the content of parabens in comparison to an oral liquid reference formulation could have an influence on bioavailability/bioequivalence of a drug? I do not have any practical experience on this but I have read an article where paraben acted by inhibiting the metabolism pattern of some of the prodrugs. "Coincubation of tenofovir DF with this mixture also resulted in an enhancement of its absorption in the in vitro Caco-2 system as well as in rat ileum" Full test is available here Also this one is worth reading "A study on the absorption mechanism of drugs through biomembranes" Hope this would be of some help. Regards — ~A happy Soul~ |
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nobody nothing 2015-02-19 09:57 (3346 d 13:43 ago) @ luvblooms Posting: # 14460 Views: 2,234 |
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Hi! No data here, too, but by all means, an interaction is likely, due to the nature of the parabens to act as disinfectants, which inherently requires a strong interaction with biomembranes. If I were a regulator, the question would be quite obvious and I would like to see some hard data, before I accept the conclusion that there is no influence of parabens on absorption. However, such an effect might be highly unlikely to have any relevant effect on highly permeable compounds at somewhat high concentrations, rushing into circulation virtually at the moment you put the spoon in your mouth... — Kindest regards, nobody |
Ing. Helmut Schütz