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BIOAVAILABILITY OF DRUGS FROM SUPPOSITORIES IN CLINICAL PRACTICE AFTER 1995

100%
Hermann J., Hermann T. W.
Acta Poloniae Pharmaceutica - Drug Research
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2020
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vol. 77
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issue 3
417-421
EN
Abstract: A review has been supposed to be arranged on the literature published between 1996 and 2018 concerning applications of suppositories in clinical practice. The rectal route of drug administration has been in use for centuries particularly in children, elderly and comatose patients as well as in palliative care and preterm infants undergoing painful procedures. Morphine, salbutamol, methadone, lidocaine, propranolol, theophylline, and mianserin, which allow to avoid the hepatic first-pass effect, are examples of preference of rectal route over oral one. Only two main classes of antibiotics (β-lactams and macrolides) have been studied recently after the rectal route of their administration. With the help of modern pharmaceutics and novel RDDS, higher bioavailability and controlled release of the drug have become possible. A number of antiepileptic drugs can be given rectally either for acute seizure control or in maintenance therapy. UC can be effectively treated with topical formulations and is superior to rectal corticosteroids. To suppositories most often used in Europe and the United States for their local treatments belong: bisacodyl, glycerol, mesalazine, diclofenac, glyceryl trinitrate, budesonide, prednisolone, and hydrocortisone. Suppositories applied for treatment of systemic conditions are more numerous.
2
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Bioavailability of mesalazine from two coated formulation tablets

81%
Hermann T. W., Główka F. K., Hermann J., Zabel M.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 1
67-73
EN
HPLC methodology with a fluorescent detector is suitable for bioavailability studies of investigated generic tablets Mesalazine 250 mg (Jelfa, Poland) versus standard Salofalk tablets (Dr. Falk, Germany). The investigations were completed in ten healthy subjects in a double way crossover design. Only one bioavailability parameter – time for maximum mesalazine plasma concentration (tmax ) and overall elimination rate constants are significantly greater for the above standard tablets. The parameters like maximum plasma drug concentration (Cmax), lag time for absorption (Tlag), biological half-life time (t1/2 ) are also more favorable for the standard, but these values are not significantly different.
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