Evaluation of subcutaneous forms in the improvement of pharmacokinetic profile of warfarin

We attempted to prepare a subcutaneous pharmaceutical form of warfarin based on a suspension or poly(ɛ-caprolactone) microparticles to improve patient adherence. The warfarin suspension had a mean particle size of 20.0μm and in vitro release close to 100% in 72h. Microparticle size and encapsulation...

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Bibliographic Details
Published in:International journal of pharmaceutics 2012-07, Vol.431 (1-2), p.33-38
Main Authors: Scala-Bertola, J., Javot, L., Camargo, J.A., Bonneaux, F., Lecompte, T., Maincent, P., Sapin, A.
Format: Article
Language:English
Subjects:
Animals
Anticoagulants - administration & dosage
Anticoagulants - blood
Anticoagulants - pharmacokinetics
bioactive properties
Bioavailability
Delayed-Action Preparations
drug formulations
Drug release
drugs
encapsulation
Injections, Subcutaneous
Life Sciences
Microparticles
monitoring
Particle Size
patients
pharmacokinetics
Polycaprolactone
Polyesters - administration & dosage
Polyesters - chemistry
Polyesters - pharmacokinetics
Povidone - administration & dosage
Povidone - chemistry
Povidone - pharmacokinetics
prothrombin
Prothrombin time monitoring
Rabbits
Suspensions
warfarin
Warfarin - administration & dosage
Warfarin - blood
Warfarin - pharmacokinetics
Warfarin delivery
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Summary:We attempted to prepare a subcutaneous pharmaceutical form of warfarin based on a suspension or poly(ɛ-caprolactone) microparticles to improve patient adherence. The warfarin suspension had a mean particle size of 20.0μm and in vitro release close to 100% in 72h. Microparticle size and encapsulation efficiencies ranged from 54.0 to 80.0μm and 37.0 to 47.0%, respectively. After 72h, warfarin microparticles exhibited in vitro drug release ranging from 62.0 to 80.0%. Warfarin subcutaneous dosage forms were administered to rabbits. Plasma concentration of warfarin was determined and biological activity was measured by prothrombin time monitoring. The observed relative bioavailabilities calculated from plasma concentrations and prothrombin times were 54.2 and 92.1%, and 61.8 and 61.4% for suspension and microparticles, respectively.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2012.03.053