Table 3.
Papers describing the application of stable isotope technology to assess the bioavailability or release profile of drug products and delivery systems
| Author | Year | System (reference) | Labelled substance | System (test) | Study objective | Reference |
|---|---|---|---|---|---|---|
| Strong et al. | 1975 | Intravenous injection | 13C-N-Acetylprocainamide | Capsule (immediate release) | ABA | [45] |
| Heck et al. | 1979 | Oral solution | 2H2-Imipramine | Tablet (immediate release) | RBA | [79] |
| Eichelbaum et al. | 1981 | Intravenous infusion | 2H3-Verapamil | Oral solution | ABA | [80] |
| Eichelbaum et al. | 1981 | Oral solution | 2H3-Verapamil | Tablet (prolonged release) | RBA | [81] |
| Meresaar et al. | 1981 | Intravenous injection | 2H2-Methadone | Tablets | ABA | [82] |
| Rigby et al. | 1983 | Pro-banthine, 15 mg | Propantheline bromide | Tablet (new formulations) | RBA | [83] |
| Gammans et al. | 1984 | Oral solution | 2H4-Trazodone | Tablet (immediate release) | RBA | [47] |
| Vogelgesang et al. | 1984 | Intravenous injection | 2H7-Verapamil | ABA | [84] | |
| Marvola et al. | 1985 | Tablet (extended release) | 2H7-Verapamil | Tablet (extended release) | RBA | [85] |
| Shibuya et al. | 1985 | Tablet (excipient lactose) | 15N3-Nitroglycerin | Tablet (excipient methylcellulose) | RBA | [46] |
| Hatch et al. | 1986 | Oral solution | 2H3-Verapamil | Tablet (immediate release) | RBA | [86] |
| Fujioka | 1987 | Endogenous testosterone | 2H3-17α-Testosterone | Intramuscular injection | RP | [87] |
| Looareesuwan et al. | 1987 | Oral solution | 2H-Mefloquine | Tablet (immediate release) | RBA | [88] |
| Mikus et al. | 1987 | Intravenous injection | 13C4-Nitrendipine | Oral solution and tablet (immediate release) | ABA | [89] |
| Hallen et al. | 1988 | Tablet | 2H2-Terodiline | Tablet | RP | [90] |
| Atkinson et al. | 1989 | Intravenous injection | 13C-N-Acetylprocainamide | Capsule (immediate release) | ABA | [91] |
| Fujioka | 1989 | Endogenous testosterone | 2H3-17α-Testosterone proprionate | Intramuscular injection | RP | [92] |
| Shinohara & Baba | 1990 | Solution | 2H3-17α-Testosterone | Tablet | RBA | [93] |
| Aronoff et al. | 1991 | Intraveous infusion | 15N2-Cibenzoline | Capsule (immediate release) | ABA | [94] |
| Benowitz et al. | 1991 | Intravenous infusion | 2H2-Nicotine | Capsule (immediate release) | ABA | [95] |
| Benowitz et al. | 1991 | NA | 2H2-Nicotine | Transdermal delivery system | RP | [96] |
| Wilding et al. | 1991 | Intravenous infusion | 15N-Carbamazepine | Tablet (extended release) | ABA | [49] |
| Oral suspension | Tablet (extended release) | RP | ||||
| Bredberg et al. | 1992 | Intravenous infusion | 2H6-Terbutaline | Tablet | ABA | [97] |
| Oral solution | Tablet | RBA | ||||
| Browne et al. | 1993 | Intravenous infusion (sodium salt of phenytoin) | 15N2-13C3-Phenytoin (sodium salt) and 13C3-phenytoin phosphate | Intravenous infusion (phosphate-ester of phenytoin) | ABA | [98] |
| Hall et al. | 1993 | Intravenous injection | S-2H4-Ibuprofen | Tablet (immediate release) and intravenous injection | ABA | [99] |
| Le Houezec et al. | 1993 | NA | 2H2-Nicotine | Subcutaneous injection | RP | [100] |
| Richard et al. | 1994 | Tablet (immediate and slow release) | H2-Metoprolol | Tablet (extended release) | ABA | [101] |
| Hage et al. | 1995 | Oral solution | 2H3-Flecainide | Tablet (controlled release) | ABA | [102] |
| Sun et al. | 1995 | Intravenous infusion | 15N-Nitroglycerin | Transdermal delivery system | ABA | [103] |
| Voortman & Paanakker | 1995 | Intravenous infusion | 13C-Mirtazapine | Tablet (immediate release) | ABA | [104] |
| Bode et al. | 1996 | Intravenous infusion | 13C4-Nifedipine | Intrajenunal and intracolonic delivered solution | ABA | [105] |
| Cummings et al. | 1996 | NA | 13C-Glucose | Capsule (delayed release) | RP | [50] |
| Gross et al. | 1997 | Capsule (immediate release) | S-2H2-Gallopamil | Capsule (immediate release) | RBA | [106] |
| Benech et al. | 1998 | Intravenous injection | 25Mg and 26Mg | Tablets | ABA | [107] |
| Fromm et al. | 1998 | Intravenous injection | 2H7-Verapamil | Tablet (prolonged release) | ABA | [108] |
| Dilger et al. | 1999 | Intravenous infusion | 2H7-Verapamil | Tablet (prolonged release) | ABA | [109] |
| Pieniaszek et al. | 1999 | Oral solution | 13C6-Moricizine | Tablet (immediate release) | RBA | [110] |
| Yeh et al. | 1999 | Intravenous injection | 2H6-Indinavir | Capsule (immediate release) | ABA | [111] |
| Gross et al. | 2000 | Capsule (immediate release) | S-2H2-Gallopamil | Capsule (immediate release) | RBA | [108] |
| Heikkinen et al. | 2001 | Intravenous injection | 13C-Entacapone | Oral solution | ABA | [112] |
| Glaeser et al. | 2004 | Intravenous injection | 2H7-Verapamil | Intrajenunal delivered solution | ABA | [113] |
| Kasuya et al. | 1985 | Intravenous injection | 2H10-Phenytoin | Tablet | ABA | [114] |
| Verbeke et al. | 2005 | NA | 13C-Urea/15N-urea | Capsule (delayed release) | RP | [52] |
| Foster et al. | 2006 | Intravenous injection | 2H6-Methadone | Oral solution | ABA | [115] |
| Majumdar et al. | 2006 | Intravenous infusion | 13C2-15N3-Aprepitant | Capsule (immediate release) | ABA | [116] |
| Schultz et al. | 2006 | Intravenous injection | 13C-Dichloroacetate | Oral solution | ABA | [117] |
| Schellekens et al. | 2008 | Capsule (immediate release) | 13C-Glucose | Capsule (delayed release) | RP | [51] |
| Schellekens et al. | 2009 | Capsule (immediate release) | 13C-Urea | Capsule (delayed release) | RP | [54] |
| Schellekens et al. | 2010 | Capsule (immediate release) | 13C-Urea | Capsule (delayed release) | RP | [53] |
Abbreviations: ABA, absolute bioavailability; NA, not applicable; RBA, relative bioavailability; and RP, release profile.