Abstract
PurposeTo develop tablet formulations by adsorbing liquid self-emulsifying drug delivery systems (SEDDS) onto Neusilin®US2, a porous silicate.MethodsNine SEDDS were prepared by combining a medium chain monoglyceride, Capmul MCM EP, a medium chain triglyceride, Captex 355 EP/NF, or their mixtures with a surfactant Cremophor EL, and a model drug, probucol, was then dissolved. The solutions were directly adsorbed onto Neusilin®US2 at 1:1 w/w ratio. Content uniformity, bulk and tap density, compressibility index, Hausner ratio and angle of repose of the powders formed were determined. The powders were then compressed into tablets. The dispersion of SEDDS from tablets was studied in 250 mL of 0.01NHCl (USP dissolution apparatus; 50 RPM; 37°C) and compared with that of liquid SEDDS.ResultsAfter adsorption of liquid SEDDS onto Neusilin®US2, all powders demonstrated acceptable flow properties and content uniformity for development into tablet. Tablets with good tensile strength (>1 MPa) at the compression pressure of 45 to 135 MPa were obtained. Complete drug release from tablets was observed if the SEDDS did not form gels in contact with water; the gel formation clogged pores of the silicate and trapped the liquid inside pores.ConclusionLiquid SEDDS were successfully developed into tablets by adsorbing them onto Neusilin®US2. Complete drug release from tablets could be obtained.Electronic supplementary materialThe online version of this article (doi:10.1007/s11095-013-1106-4) contains supplementary material, which is available to authorized users.
Highlights
The lipid-based delivery system is a highly promising approach to enhance bioavailability of poorly watersoluble compounds since it presents the drug to the gastro-intestinal tract in a solubilized state
Tabletability, which is characterized by the plot of tablet tensile strength as a function of compaction pressure, may be defined as the capacity of a powder to be transformed into a tablet of specified strength under the effect of compaction pressure [34]
Several investigators incorporated large amounts of binders and diluents to increase tabletability of silicate formulations [22,23,24]. This approach may often defeat the purpose of solidifying the lipid-based formulations as the added excipients increase the tablet size and, only limited amount of the liquid self-emulsifying drug delivery systems (SEDDS) can be incorporated in a tablet of convenient size
Summary
The lipid-based delivery system is a highly promising approach to enhance bioavailability of poorly watersoluble compounds since it presents the drug to the gastro-intestinal tract in a solubilized state. One of the primary reasons for the lack of widespread application of lipid-based formulations is that the most commonly used lipids and surfactants are liquid and, not amenable to the development of solid dosage forms They usually lead to liquid-filled bottles (Agenerase®, GSK; Sustiva Oral Solution, BMS) and, if the solubility of drug is high enough or the dose is low, to liquid-filled soft or hard gelatin capsule formulations (Avodart®, GSK; Aptivus®, Boehringer Ingelheim; Glakay® Capsules and Juvela®N Soft Capsules, Eisai) [2]. Such formulations, have many limitations and challenges. Since most of the major pharmaceutical companies do not have soft gelatin
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