Evaluation of the impact of sodium lauryl sulfate source variability on solid oral dosage form development.
OBJECTIVE
The objective of this study was to investigate the effects of sodium lauryl sulfate (SLS) from different sources on solubilization/wetting, granulation process, and tablet dissolution of BILR 355 and the potential causes.


METHODS
The particle size distribution, morphology, and thermal behaviors of two pharmaceutical grades of SLS from Spectrum and Cognis were characterized. The surface tension and drug solubility in SLS solutions were measured. The BILR 355 tablets were prepared by a wet granulation process and the dissolution was evaluated.


RESULTS
The critical micelle concentration was lower for Spectrum SLS, which resulted in a higher BILR 355 solubility. During wet granulation, less water was required to reach the same end point using Spectrum than Cognis SLS. In general, BILR 355 tablets prepared with Spectrum SLS showed a higher dissolution than the tablets containing Cognis SLS. Micronization of SLS achieved the same improved tablet dissolution as micronized active pharmaceutical ingredient.


CONCLUSIONS
The observed differences in wetting and solubilization were likely due to the different impurity levels in SLS from two sources. This study demonstrated that SLS from different sources could have significant impact on wet granulation process and dissolution. Therefore, it is critical to evaluate SLS properties from different suppliers, and then identify optimal formulation and process parameters to ensure robustness of drug product manufacture process and performance.
Qiang
Dongmei
D
Department of Pharmaceutics, Boehringer Ingelheim Pharmaceuticals, Ridgefield, CT 06877, USA. dongmei.qiang@boehringer-ingelheim.com
Gunn
Jocelyn A
JA
Schultz
Leon
L
Li
Z Jane
ZJ
D001381:Azepines / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D008823:Micelles; D010316:Particle Size; D011725:Pyridines / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry* / Q000592:standards; D012995:Solubility; D013500:Surface Tension; D013501:Surface-Active Agents / Q000737:chemistry* / Q000592:standards; D013607:Tablets
C548654:5,11-dihydro-11-ethyl-5-methyl-8-(2-(1-oxido-4-quinolinyl)ethyl)-6H-dipyrido(3,2-B,2',3'-E)(1,4)diazepin-6-one; D001381:Azepines; D008823:Micelles; D011725:Pyridines; D018894:Reverse Transcriptase Inhibitors; D013501:Surface-Active Agents; D013607:Tablets; D012967:Sodium Dodecyl Sulfate