Kinetic Study of a 2‐Hydroxypropyl‐β‐Cyclodextrin‐Based Formulation of all‐trans‐Retinoic Acid in Sprague‐Dawley Rats After Oral or Intravenous Administration

all‐trans‐Retinoic acid (ATRA, vitamin A acid, or tretinoin) is a potent chemotherapeutic agent for the treatment of acute promyelocytic leukemia (APL). Its poor aqueous solubility not only affects its oral absorption but also prevents it from forming an aqueous parenteral formulation. Recently, we...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2000-02, Vol.89 (2), p.260-267
Main Authors: Lin, Hai‐Shu, Chan, Sui Yung, Low, Kerwin Siew Yang, Shoon, Mei Leng, Ho, Paul C.
Format: Article
Language:English
Subjects:
2-Hydroxypropyl-beta-cyclodextrin
Administration, Oral
Animals
Antineoplastic agents
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - pharmacokinetics
beta-Cyclodextrins
Biological and medical sciences
Biological Availability
Body Fluid Compartments
Cyclodextrins - administration & dosage
Cyclodextrins - pharmacokinetics
General aspects
General pharmacology
Injections, Intravenous
Intestinal Absorption
Male
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Solubility
Tretinoin - administration & dosage
Tretinoin - pharmacokinetics
Water - chemistry
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Summary:all‐trans‐Retinoic acid (ATRA, vitamin A acid, or tretinoin) is a potent chemotherapeutic agent for the treatment of acute promyelocytic leukemia (APL). Its poor aqueous solubility not only affects its oral absorption but also prevents it from forming an aqueous parenteral formulation. Recently, we developed a water‐soluble formulation of ATRA with 2‐hydroxypropyl‐β‐cyclodextrin (HPβCD). In present study, this formulation was tested in Sprague‐Dawley rats. Kinetic study of ATRA was carried out after oral or intravenous administration. Though there were no statistical differences in any of the estimated pharmacokinetic parameters between ATRA sodium salt and HPβCD‐based ATRA after intravenous administration, inclusion of ATRA into HPβCD was found to greatly improve the oral absorption of ATRA. © 2000 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 89: 260–267, 2000
ISSN:0022-3549
1520-6017
DOI:10.1002/(SICI)1520-6017(200002)89:2<260::AID-JPS13>3.0.CO;2-Q