Design and characterization of a surfactant-enriched tablet formulation for oral delivery of a poorly water-soluble immunosuppressive agent

The feasibility of incorporating significant quantities of the anionic surfactant, sodium lauryl sulfate (SDS), into an immediate release tablet formulation of a poorly water-soluble immunosuppressive agent was investigated. Despite the extremely poor compressibility of SDS and poor chemical stabili...

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Bibliographic Details
Published in:	International journal of pharmaceutics Vol. 182; no. 2; pp. 173 - 186
Main Authors:	Ruddy, Stephen B., Matuszewska, Bozena K., Grim, Yvetta A., Ostovic, Drazen, Storey, David E.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier B.V 25-05-1999 Elsevier
Subjects:	Administration, Oral Biological and medical sciences Chemistry, Pharmaceutical Drug Delivery Systems General pharmacology Imidazoles - administration & dosage Imidazoles - chemistry Immunomodulators Immunosuppressive agent Immunosuppressive Agents - administration & dosage Medical sciences Micellar solubilization Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Poorly water-soluble drug Sodium Dodecyl Sulfate - administration & dosage Sodium lauryl sulfate Solubility Surface-Active Agents - administration & dosage Surfactant Tablet formulation Tablets Tacrolimus - administration & dosage Tacrolimus - analogs & derivatives Tacrolimus - chemistry Poorly water-soluble drug Tablet formulation Sodium lauryl sulfate Immunosuppressive agent Surfactant Micellar solubilization Compression Pharmaceutical technology Solubilization Dissolution In vitro Lauryl sulfate Mannitol Dosage form Active ingredient Coated tablet Release
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Summary:	The feasibility of incorporating significant quantities of the anionic surfactant, sodium lauryl sulfate (SDS), into an immediate release tablet formulation of a poorly water-soluble immunosuppressive agent was investigated. Despite the extremely poor compressibility of SDS and poor chemical stability of the drug, a commercializable, direct-compression tablet formulation with satisfactory mechanical properties and acceptable chemical stability was achieved. Optimal in vitro release of the drug from the tablet formulation was achieved by establishing the minimum molar uptake ratio necessary to achieve complete micellar solubilization of the drug, after which formulation studies were conducted to determine the influence of formulation and process variables on the rate and extent of drug release. A model-independent analysis of dissolution results in a reduced volume (250 ml) of modified simulated gastric fluid demonstrated that the rate and extent of drug release was highly dependent on the mean particle size of the bulk drug, but independent of compression force above that required to achieve a compact of acceptable mechanical strength. Employing the Korsmeyer–Peppas model of Fickian and non-Fickian drug release, it was further shown that release of the drug from the dosage form was governed largely by surface erosion of the surfactant-enriched tablet matrix.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0378-5173 1873-3476
DOI:	10.1016/S0378-5173(99)00056-3