Biopharmaceutical evaluation of methylcellulose as an excipient for nitroglycerin tablets.
To examine the bioavailability of nitroglycerin in sublingual tablet, 5 healthy adult volunteers underwent simultaneous sublingual administration of a tablet prepared with methylcellulose and a tablet prepared with lactose containing 0.15 mg of nitroglycerin and 0.15 mg of nitroglycerin-15N3, respectively. In 4 of 5 volunteers, no difference in plasma concentration determined by gas chromatography-mass spectrometry (GC-MS) was observed between 2 tablets described above, so it was well accepted that nitroglycerin in tablets prepared with methylcellulose had a similar bioavailability to that in tablets prepared with lactose. The simultaneous administration of the 2 nitroglycerin tablets to a healthy volunteer, one of which containing the drug labeled with a stable isotope followed by GC-MS assay, seems to be the most suitable method for a precise comparison of bioavailability of the formulations.
D000328:Adult; D001682:Biological Availability; D005079:Excipients / Q000008:administration & dosage*; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage*; D008875:Middle Aged; D005996:Nitroglycerin / Q000008:administration & dosage* / Q000378:metabolism / Q000494:pharmacology; D013607:Tablets
D005079:Excipients; D013607:Tablets; D008747:Methylcellulose; D005996:Nitroglycerin