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The use of 13C labeling to enhance the sensitivity of 13C solid-state CPMAS NMR to study polymorphism in low dose solid formulations

✍ Scribed by Kees-Jan Booy; Peter Wiegerinck; Jan Vader; Frans Kaspersen; Dorette Lambregts; Herman Vromans; Edwin Kellenbach

Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
99 KB
Volume
94
Category
Article
ISSN
0022-3549

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✦ Synopsis

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. ß 2004

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