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Transdermal delivery of erythromycin lactobionate—implications for the therapy of gastroparesis
Author(s) -
Brand R. M.,
Lof J.,
Quigley E. M. M.
Publication year - 1997
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1046/j.1365-2036.1997.00165.x
Subject(s) - transdermal , medicine , pharmacology , erythromycin , gastric emptying , in vivo , gastroparesis , human skin , hairless , drug , gastrointestinal tract , anesthesia , stomach , gastroenterology , antibiotics , biology , genetics , microbiology and biotechnology
Background: The treatment of many diseases may be complicated by abnormalities in gastric emptying. Gastric motor dysfunction may lead to unpredictable food and medication delivery to the small intestine, their site of absorption. Prokinetic agents improve gastric motility, but orally administered drugs are unreliably absorbed, thereby limiting their effectiveness. A method of delivering prokinetic agents which bypasses the gastrointestinal tract could lead to more effective treatment. Methods: Skin samples from rat, hairless mouse and man were placed in an in vitro diffusion chamber. The epidermal side of the skin was exposed to erythromycin lactobionate and passage of the drug across the skin sample monitored and quantitated by high‐performance liquid chromatography with UV detection. Results: Erythromycin passed across all skin types tested. Steady‐state flux across hairless mouse skin was greater than for rat, full thickness human skin and human epidermis. In the first 3 h following introduction of erythromycin lactobionate, 1.85 mg/cm 2 crossed human epidermis. Given that a dose of 50 mg may exert prokinetic effects in vivo in man, increasing the patch size to ≈28 cm 2 should provide therapeutic levels of drug within 3 h. Conclusions: Erythromycin lactobionate, when administered transdermally, can be delivered at levels sufficient to treat gastroparesis. This technique warrants in vivo investigation.