The use of 13C labeling to enhance the sensitivity of 13C solid-state CPMAS NMR to study polymorphism in low dose solid formulations.
(13)C labeling was used to enhance the sensitivity of (13)C solid-state NMR to study the effect of tabletting on the polymorphism of a steroidal drug. The steroidal drug Org OD 14 was (13)C labeled and formulated into tablets containing only 0.5-2.5% active ingredient. The tablets were subsequently studied by solid-state (13)C CPMAS NMR. The crystalline form present in tablets could readily be analyzed in tablets. No change in crystalline form was observed as a result of formulation or in subsequent stability studies. Solid-state NMR in combination with (13)C labeling can, in suitable cases, be used as a strategy to study the effect of formulation on the polymorphism of low dose drugs.
Booy
Kees-Jan
KJ
Pre- and early Clinical Development, Organon, P.O. Box 20, 5340BH Oss, The Netherlands.
Wiegerinck
Peter
P
Vader
Jan
J
Kaspersen
Frans
F
Lambregts
Dorette
D
Vromans
Herman
H
Kellenbach
Edwin
E
D002247:Carbon Isotopes / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D004304:Dosage Forms; D020847:Estrogen Receptor Modulators / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D012680:Sensitivity and Specificity; D013607:Tablets / Q000737:chemistry
D002247:Carbon Isotopes; D004304:Dosage Forms; D020847:Estrogen Receptor Modulators; D013607:Tablets