Role of in vitro release models in formulation development and quality control of parenteral depots.
This review article provides an assessment of advantages/limitations of the use of current in vitro release models to predict in vivo performance of parenteral sustained release products (injectable depots). As highlighted, key characteristics influencing the in vivo drug fate may vary with the route of administration and the type of sustained release formulation. To this end, an account is given on three representative injection sites (intramuscular, subcutaneous and intra-articular) as well as on in vitro release mechanism(s) of drugs from five commonly investigated depot principles (suspensions, microspheres, hydrogels, lipophilic solutions, and liposomes/other nano-size formulations). Current in vitro release models are, to a different extent, able to mimic the rate, transport and equilibrium processes that the drug substance may experience in the environment of the administration site. Their utility for the purpose of quality control including in vitro-in vivo correlations and formulation design is discussed.
Larsen
Claus
C
University of Copenhagen, Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen, Denmark. csl@farma.ku.dk
Larsen
Susan Weng
SW
Jensen
Henrik
H
Yaghmur
Anan
A
Ostergaard
Jesper
J
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D006801:Humans; D007270:Injections, Intra-Articular; D007273:Injections, Intramuscular; D007279:Injections, Subcutaneous; D008954:Models, Biological; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000378:metabolism; D011786:Quality Control
D003692:Delayed-Action Preparations; D004364:Pharmaceutical Preparations