Development of Solid SEDDS, V: Compaction and Drug Release Properties of Tablets Prepared by Adsorbing Lipid-Based Formulations Onto Neusilin® US2

Overview

Journal Pharm Res

Specialties Pharmacology
Pharmacy

Date 2013 Jun 26

PMID 23797463

Citations 15

Authors

Suhas G Gumaste

Damon M Dalrymple

Abu T M Serajuddin

Affiliations

Soon will be listed here.

Abstract

Purpose: To develop tablet formulations by adsorbing liquid self-emulsifying drug delivery systems (SEDDS) onto Neusilin®US2, a porous silicate.

Methods: Nine 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.

Results: After 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.

Conclusion: Liquid SEDDS were successfully developed into tablets by adsorbing them onto Neusilin®US2. Complete drug release from tablets could be obtained.

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References

Nazzal S, Khan M . Controlled release of a self-emulsifying formulation from a tablet dosage form: stability assessment and optimization of some processing parameters. Int J Pharm. 2006; 315(1-2):110-21. DOI: 10.1016/j.ijpharm.2006.02.019. View

Milovic M, Djuris J, Djekic L, Vasiljevic D, Ibric S . Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release. Int J Pharm. 2012; 436(1-2):58-65. DOI: 10.1016/j.ijpharm.2012.06.032. View

Yi T, Wan J, Xu H, Yang X . A new solid self-microemulsifying formulation prepared by spray-drying to improve the oral bioavailability of poorly water soluble drugs. Eur J Pharm Biopharm. 2008; 70(2):439-44. DOI: 10.1016/j.ejpb.2008.05.001. View

Agarwal V, Siddiqui A, Ali H, Nazzal S . Dissolution and powder flow characterization of solid self-emulsified drug delivery system (SEDDS). Int J Pharm. 2008; 366(1-2):44-52. DOI: 10.1016/j.ijpharm.2008.08.046. View

Van Speybroeck M, Williams H, Nguyen T, Anby M, Porter C, Augustijns P . Incomplete desorption of liquid excipients reduces the in vitro and in vivo performance of self-emulsifying drug delivery systems solidified by adsorption onto an inorganic mesoporous carrier. Mol Pharm. 2012; 9(9):2750-60. DOI: 10.1021/mp300298z. View

Fell J, Newton J . Determination of tablet strength by the diametral-compression test. J Pharm Sci. 1970; 59(5):688-91. DOI: 10.1002/jps.2600590523. View

Mullertz A, Ogbonna A, Ren S, Rades T . New perspectives on lipid and surfactant based drug delivery systems for oral delivery of poorly soluble drugs. J Pharm Pharmacol. 2010; 62(11):1622-36. DOI: 10.1111/j.2042-7158.2010.01107.x. View

Kang M, Jung S, Song W, Park J, Choi S, Oh K . Immediate release of ibuprofen from Fujicalin®-based fast-dissolving self-emulsifying tablets. Drug Dev Ind Pharm. 2011; 37(11):1298-305. DOI: 10.3109/03639045.2011.571695. View

Cole E, Cade D, Benameur H . Challenges and opportunities in the encapsulation of liquid and semi-solid formulations into capsules for oral administration. Adv Drug Deliv Rev. 2007; 60(6):747-56. DOI: 10.1016/j.addr.2007.09.009. View

10.

Li P, Hynes S, Haefele T, Pudipeddi M, Royce A, Serajuddin A . Development of clinical dosage forms for a poorly water-soluble drug II: formulation and characterization of a novel solid microemulsion preconcentrate system for oral delivery of a poorly water-soluble drug. J Pharm Sci. 2008; 98(5):1750-64. DOI: 10.1002/jps.21547. View

11.

Nazzal S, Nutan M, Palamakula A, Shah R, Zaghloul A, Khan M . Optimization of a self-nanoemulsified tablet dosage form of Ubiquinone using response surface methodology: effect of formulation ingredients. Int J Pharm. 2002; 240(1-2):103-14. DOI: 10.1016/s0378-5173(02)00130-8. View

12.

Shah A, Serajuddin A . Development of solid self-emulsifying drug delivery system (SEDDS) I: use of poloxamer 188 as both solidifying and emulsifying agent for lipids. Pharm Res. 2012; 29(10):2817-32. DOI: 10.1007/s11095-012-0704-x. View

13.

Nielsen F, Gibault E, Ljusberg-Wahren H, Arleth L, Pedersen J, Mullertz A . Characterization of prototype self-nanoemulsifying formulations of lipophilic compounds. J Pharm Sci. 2007; 96(4):876-92. DOI: 10.1002/jps.20673. View

14.

Prajapati H, Dalrymple D, Serajuddin A . A comparative evaluation of mono-, di- and triglyceride of medium chain fatty acids by lipid/surfactant/water phase diagram, solubility determination and dispersion testing for application in pharmaceutical dosage form development. Pharm Res. 2011; 29(1):285-305. PMC: 3246583. DOI: 10.1007/s11095-011-0541-3. View

15.

Strickley R . Solubilizing excipients in oral and injectable formulations. Pharm Res. 2004; 21(2):201-30. DOI: 10.1023/b:pham.0000016235.32639.23. View

16.

Shah R, Tawakkul M, Khan M . Comparative evaluation of flow for pharmaceutical powders and granules. AAPS PharmSciTech. 2008; 9(1):250-8. PMC: 2976911. DOI: 10.1208/s12249-008-9046-8. View

17.

Sander C, Holm P . Porous magnesium aluminometasilicate tablets as carrier of a cyclosporine self-emulsifying formulation. AAPS PharmSciTech. 2009; 10(4):1388-95. PMC: 2799606. DOI: 10.1208/s12249-009-9340-0. View

18.

Liao C, JAROWSKI C . Dissolution rates of corticoid solutions dispersed on silicas. J Pharm Sci. 1984; 73(3):401-3. DOI: 10.1002/jps.2600730330. View

19.

Bauer J, Spanton S, Henry R, Quick J, Dziki W, Porter W . Ritonavir: an extraordinary example of conformational polymorphism. Pharm Res. 2001; 18(6):859-66. DOI: 10.1023/a:1011052932607. View

20.

Gumaste S, Pawlak S, Dalrymple D, Nider C, Trombetta L, Serajuddin A . Development of Solid SEDDS, IV: Effect of Adsorbed Lipid and Surfactant on Tableting Properties and Surface Structures of Different Silicates. Pharm Res. 2013; . PMC: 3841658. DOI: 10.1007/s11095-013-1114-4. View