Abstract：
:Recently, single-dose drug packaging systems, allowing the administration of multiple drugs in a single pill, have become popular for the convenience of the patient. The quality of drugs and an accurate measurement of their photostabilities within this system, however, have not been carefully addressed. Drugs that are unstable in light should be carefully handled to protect their potency and ensure their safety. Propranolol (1), a beta-adrenergic receptor antagonist, is widely used for angina pectoris, arrhythmia, and hypertension. Due to its naphthalene skeleton, this drug may be both light unstable and a photosensitizing agent. In this study, we isolated three photodegraded products of propranolol (1): 1-naphthol (2), N-acetylpropranolol (3), and N-formylpropranolol (4). The structures of these compounds were determined by spectroscopic methods and chemical syntheses. We also examined the acute toxicities of these substances in mice and their binding to beta-adrenergic receptors using rat cerebellum cortex membranes. Although the photoproducts isolated in this study did not exhibit any acute toxicity or significant binding to beta-adrenergic receptors, these results serve as a warning to single-dose packaging systems, as propranolol (1) must be handled carefully to protect the compound from light-induced degradation.
journal_name
Life Scijournal_title
Life sciencesauthors
Uwai K,Tani M,Ohtake Y,Abe S,Maruko A,Chiba T,Hamaya Y,Ohkubo Y,Takeshita Mdoi
10.1016/j.lfs.2005.04.033subject
Has Abstractpub_date
2005-12-12 00:00:00pages
357-65issue
4eissn
0024-3205issn
1879-0631pii
S0024-3205(05)00670-3journal_volume
78pub_type
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