期刊
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
卷 51, 期 3, 页码 723-727出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jpba.2009.08.010
关键词
Cialis (R); Counterfeit; Tadalafil; trans-Tadalafil; Liquid chromatography-mass spectrometry (LC-MS); Nuclear magnetic resonance (NMR)
Four blisters with suspect Cialis (R) (tadalafil) 20 mg tablets were screened for authenticity using near infrared spectroscopy (NIRS) and for the presence of phosphodiesterase 5 (PDE-5) inhibitors using LC-DAD-MS. All samples were identified as counterfeit Cialis (R) and contained sildenafil or a combination of tadalafil and sildenafil. Although the tablets contained efficacious amounts of PDE-5 inhibitors, neither the active ingredient nor the dosage corresponded to the description on the blister. This is the first reported case of a diastereomeric mixture of tadalafil and trans-tadalafil (3:1) being identified in a counterfeit medicine. The LC-DAD-CD revealed that both diastereomers had a high optical purity. The optical rotation of the diastereomeric mixture was measured indicating the presence of (-)-trans-tadalafil, which is the only other stereoisomer with some PDE-5 inhibitory activity. As no safety profiles are known for the stereoisomers of tadalafil, there is a potential health risk. In addition, the optical purity of tadalafil needs to be taken into account when calculating the dosage in illegal medicines. (C) 2009 Published by Elsevier B.V.
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