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Phosphate buffer interferes dissolution of prazosin hydrochloride in compendial dissolution testing.

Hiroshi Sudaki1, Katsuyoshi Fujimoto1, Koichi Wada1

  • 1Nippon Boehringer Ingelheim Co. Ltd., 6-7-5 Minatojima-minamimachi, Chuo-ku, Kobe, Hyogo, 650-0047, Japan.

Drug Metabolism and Pharmacokinetics
|July 2, 2023
PubMed
Summary

Prazosin hydrochloride (PRZ-HCl) dissolution shows no supersaturation in phosphate buffers due to salt formation. This impacts in vivo predictions, as intestinal fluid uses a bicarbonate system, not phosphate.

Keywords:
Equilibrium solubilityPhosphate precipitatesPoorly water-soluble drugspH-dependent solubility

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Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry
  • Drug Delivery

Background:

  • Supersaturation is crucial for oral drug absorption.
  • Prazosin hydrochloride (PRZ-HCl) exhibits unusual dissolution behavior.
  • Understanding PRZ-HCl dissolution is key for predicting in vivo performance.

Purpose of the Study:

  • To investigate the absence of supersaturation in prazosin hydrochloride (PRZ-HCl) dissolution.
  • To identify the solid-state transformations occurring during PRZ-HCl dissolution.
  • To evaluate the suitability of phosphate buffers for simulating in vivo dissolution.

Main Methods:

  • Equilibrium solubility determined using the shake-flask method.
  • Dissolution testing performed with the compendial paddle method.
  • Solid-state analysis of residual particles via Raman spectroscopy.

Main Results:

  • PRZ-HCl formed a phosphate salt in phosphate buffers below pH 6.5, reducing solubility.
  • Above pH 6.5, PRZ-HCl transformed into its freebase (PRZ-FB), matching unbuffered solubility.
  • In dissolution tests, PRZ-HCl rapidly converted to a phosphate salt, then slowly to PRZ-FB.

Conclusions:

  • Phosphate buffers do not accurately reflect in vivo dissolution due to different buffering systems (bicarbonate vs. phosphate).
  • The formation of PRZ phosphate salt inhibits supersaturation, affecting dissolution profiles.
  • Drug formulation and dissolution testing require consideration of physiological buffer systems for accurate in vivo predictions.