Improving the hardness of dry granulated tablets containing sodium lauryl sulfate.
The impact of the addition of a wetting agent, the surfactant sodium lauryl sulfate (SLS), on the tablet hardness of a dry granulated, solid oral dosage form was investigated. In three batches, SLS was added concurrently with: (1) a poorly soluble, highly hydrophobic active pharmaceutical ingredient (API) and the other excipients prior to the initial blending step, (2) magnesium stearate prior to roller compaction, or (3) magnesium stearate prior to tableting. A fourth batch, which did not contain SLS, served as a control. The maximum hardness of 100 mg, 1/4″-SRC tablets for the four batches--SLS added initially, prior to roller compaction, prior to tableting, and no SLS--were 61±3, 71±3, 89±5, and 86±3N, respectively, suggesting reduced processing of SLS improves tablet hardness by ∼50%. Dissolution of the tablets in 900 ml of simulated gastric fluid with paddles at 75 rpm showed that: (1) there was no impact on the insertion point of SLS into the process on API dissolution, and (2) that the presence of SLS improved dissolution by 5% compared to the control tablets. Adding SLS just prior to tableting can improve tablet hardness and yield similar dissolution performance relative to SLS addition prior to the initial blending step.
Moore
Francis
F
Pfizer Global Research and Development, Groton, CT 06340, United States.
Okelo
Geoffrey
G
Colón
Ivelisse
I
Kushner
Joseph
J
D019245:Compressive Strength; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006244:Hardness; D010316:Particle Size; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*; D013607:Tablets; D013678:Technology, Pharmaceutical
D005079:Excipients; D013501:Surface-Active Agents; D013607:Tablets; D012967:Sodium Dodecyl Sulfate