Extended hildebrand solubility approach: Testosterone and testosterone propionate in binary solvents

✍ Scribed by A. Martin; P. L. Wu; A. Adjei; M. Mehdizadeh; K. C. James; Carl Metzler

• Publisher: John Wiley and Sons
• Year: 1982
• Tongue: English
• Weight: 831 KB
• Volume: 71
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600711207

✦ Synopsis

value for 8-chloro-6-phenyl-4H-s-triazolo[4,3-a J\1,4] benzodiazepine (estazolam) was reported to be 2.84 from the UV absorption spectral change (23). Considering the structural difference mentioned, the estimated pKa value for triazolam, 1.52, is reasonable.

The bioavailability or the pharmacological effect of a drug would greatly depend on the formation rate in the cyclization reaction from the opened form to the closed form because only the cyclized 1,4-benzodiazepines possess pharmacological CNS activity (24), which are discussed in reports on diazepam (8) and desmethyldiazepam (12). The half-time of the forward reaction of I at pH 7.4, which was calculated to be 80.6 min (Fig. 5), indicates that much time is required to convert I into the closed form 11, only if the in uiuo reaction proceeds chemically.

REFERENCES

(1) H.