Photostability of extended-release matrix formulations.
The photostability of drugs has been widely studied while less attention is devoted to the possible modifications that UV light may induce on the excipients of a dosage form, in particular, on the functional polymers used to modulate drug delivery. In this work we have evaluated the effect of UV light on the release characteristics of extended-release matrix tablets containing hydroxypropylmethylcellulose (HPMC) or polyethylene oxide (PEO) as retarding polymers. Two different model drugs have been used: nifedipine (insoluble and photolabile drug) and diltiazem (soluble and photostable drug). Photodecomposition of nifedipine was evaluated and the formation of the photoproducts was followed during the dissolution process. Regarding the dissolution stability, the matrix tablets containing HPMC exposed to UV light have not shown significant differences in drug release profiles compared to the same non-irradiated formulation, while the matrix tablets containing PEO and exposed to the same conditions of UV light have shown a remarkable increase of drug release rate within the first minutes of the dissolution test (burst effect) which is particularly critical because it can cause the loss of the desired therapeutic control.
Maggi
L
L
Department of Pharmaceutical Chemistry, University of Pavia, Pavia, Italy. lauretta.maggi@unipv.it
Ochoa Machiste
E
E
Fasani
E
E
Albini
A
A
Segale
L
L
Conte
U
U
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004110:Diltiazem / Q000737:chemistry / Q000528:radiation effects*; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D009543:Nifedipine / Q000737:chemistry / Q000528:radiation effects*; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013997:Time Factors; D014466:Ultraviolet Rays
D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D008747:Methylcellulose; D004110:Diltiazem; D009543:Nifedipine