Development of solid SEDDS, III: Application of Acconon® C-50 and Gelucire® 50/13 as both solidifying and emulsifying agents for medium chain triglycerides

Journal of Excipients and Food Chemicals

Volumn 3, Issue 2, 2012, Pages 83-92

  Patel, Nrupa ^a   Dalrymple, Damon M ^b   Serajuddin, Abu T M ^a  

^a ST JOHN'S UNIVERSITY   (United States)

^b AB Enzymes GmbH   (Germany)

Author keywords

Acconon C 50; Dispersion testing; Gelucire 50 13; Probucol; Solid SEDDS; Stearoyl polyoxyl glycerides

Indexed keywords

ACCONON C 50; EMULSIFYING AGENT; GELUCIRE 50 13; MEDIUM CHAIN TRIACYLGLYCEROL; PROBUCOL; STEAROYL POLYOXYL GLYCERIDE; UNCLASSIFIED DRUG;

ARTICLE; CONFOCAL FLUORESCENCE ANALYSIS; COOLING; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG MIXTURE; DRUG SOLUBILITY; FLUORESCENCE ANALYSIS; HARD GELATIN CAPSULE; HEATING; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; LIPID COMPOSITION; LIQUID; MELTING POINT; MICROSCOPY; PARTICLE SIZE; POLARIZATION; ROOM TEMPERATURE; SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM; X RAY POWDER DIFFRACTION;

EID: 84863817743     PISSN: None     EISSN: 21502668     Source Type: Journal    
DOI: None     Document Type: Article

References (28)

1. Charman S.A., Charman W.N., Rogge M.C., Wilson T.D., Dutko F.J., Pouton C.W., Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound, Pharm. Res., 9:87-93, 1992
2. Shah N.H., Carvajal M.T., Patel C.I., Infeld M.H., Malick A.W., Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs, Int. J. Pharm., 106:15-23, 1994
3. Porter C.J.H., Trevaskis N.L., Charman W.N., Lipids and lipid-based formulations: Optimizing the oral delivery of lipophilic drugs, Nature Rev., 6:231-248, 2007
4. O'Driscoll C.M., Griffin B.T., Biopharmaceutical challenges associated with drugs with low aqueous solubility-the potential impact of lipid-based formulations, Adv. Drug Del. Rev., 60:617-624, 2008
5. Serajuddin A.T.M., Li P., Haefele T.F., Development of lipid-based drug delivery systems for poorly watersoluble drugs as viable oral dosage forms, American Pharmaceutical Review, 11:34-42, 2008
6. Prajapati H.N., Dalrymple D.M., Serajuddin A.T.M., 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., 29:285-305, 2012
7. Prajapati H.N., Patel D.P., Patel N.G., Dalrymple D.M., Serajuddin A.T.M., Effect of difference in fatty acid chain lengths of medium-chain lipids on lipidsurfactant-water phase diagrams and drug solubility, J. Excipients Food Chem., 2(3):73-87, 2011
8. Vasanthavada M., Serajuddin A.T.M., Lipid-based self-emulsifying solid dispersions, in Hauss D (ed.), Lipid-based formulations for oral drug delivery: Enhancing bioavailability of poorly water-soluble drug; Informa Healthcare, New York, NY, pp. 149-184, 2007
9. Jannin V., Musakhanian J., Marchaud D., Approaches for the development of solid and semi-solid lipidbased formulations, Adv. Drug. Del. Rev., 60:734-746, 2008
10. Li P., Hynes S.R., Haefele T.F., Pudipeddi M., Royce A.E., Serajuddin A.T.M., 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., 98:1750-1764, 2009
11. Shah A., Serajuddin A.T. M., Development of Solid SEDDS, I: Use of Poloxamer 188 as both solidifying and emulsifying agent, Pharm. Res., DOI 10.1007/s11095-012-0704-x (published online: 28 February, 2012)
12. Patel N., Prajapati H., Dalrymple D., Serajuddin A., Development of solid SEDDS, II: Application of Acconon® C-44 and Gelucire® 44/14 as Solidifying Agents for Self-emulsifying Drug Delivery Systems of Medium Chain Triglyceride, J. Excipients Food Chem., 3 (2), 54-66, 2012
13. Khan N., Craig D.Q.M., The influence of drug incorporation on the structure and release properties of solid dispersions in lipid matrices, J. Cont. Rel., 93:355-368, 2003
14. Passerini N., Perissutti B., Moneghini M., Voinovich D., Albertini B., Cavallari C., Rodriguez L., Characterization of carbamazepine-Gelucire® 50/13 microparticles prepared by a spray congealing process using ultrasounds, J. Pharm. Sci., 91:699-707, 2002
15. Vippagunta S.R., Maul K.A., Tallavajhala S., Grant D.J.W., Solid-state characterization of nifedipine solid dispersions, Int. J. Pharm., 236:111-123, 2002
16. Fini A., Moyano J.R., Gines J.M., Perez-Martinez J.I., Rabasco A.M., Diclofenac salts, II. Solid dispersions in PEG6000 and Gelucire® 50/13, Eur. J. Pharm. Biopharm., 60:99-111, 2005
17. Shrivastava A.R., Ursekar B., Kapadia C.J., Design, optimization, preparation and evaluation of dispersion granules of valsartan and formulation into tablets, Current Drug Delivery 6:28-37, 2009
18. Qi S., Marchaud D., Craig D.Q.M., An investigation into the mechanism of dissolution rate enhancement of poorly water soluble drugs from spray chilled Gelucire® 50/13 microspheres, J. Pharm. Sci., 99:262-274, 2010
19. Shimpi S.L., Chauhan B., Mahadik K., Paradkar A., Stabilization and improved in vivo performance of amorphous etoricoxib using Gelucire® 50/13, Pharm. Res. 22:1727-1734, 2005
20. Dhumal R.S., Biradar S.V., Aher S., Paradkar A.R., Cefuroxime axetil solid dispersion with polyglycolized glycerides for improved stability and bioavailability, J. Pharm. Pharmacol., 61:743-751, 2009
21. Serajuddin A.T.M., Solid dispersion of poorly water soluble drugs: early promises, subsequent problems, and recent breakthroughs, J. Pharm. Sci. 88:1058-1066, 1999
22. Yagi N., Terashima Y., Kenmotsu H., Sekikawa H., Takada M., Dissolution behavior of probucol from sol id dispe r sion sy stems of probucol polyvinylpyrrolidone, Chem. Pharm. Bull., 44:241-244. 1996
23. Zaghloul A., Khattab I., Nada K.A., Al-Saidan S., Preparation, characterization and optimization of probucol self-emulsified drug delivery system to enhance solubility and dissolution, Pharmazie, 9: 654-660, 2008
24. Greenspan P., Fowler S.D., Spectrofluorometric studies of the lipid probe, Nile red, J. Lipid Res., 26: 781-9. 1985
25. Strawhecker K., Manias E., Crystallization behavior of poly (ethylene oxide) in the presence of Na montmorillonite fillers, Chemistry of Materials, 15:844-849, 2003
26. Gines J., Arias M., Moyano J., Sanchez-Soto P., Thermal investigation of crystallization of polyethylene glycols in solid dispersions containing oxazepam, Int. J. Pharm., 143:247-53, 1996
27. Gránásy L., Pusztai T., Tegze G., Warren J.A., Douglas J.F., Growth and form of spherulites. Physical Review E, 72:011605, 2005
28. Li S., He H., Parthiban L.J., Yin H., Serajuddin A., IV IVC considerations in the development of immediate release oral dosage form, J. Pharm. Sci., 94:1396-1417, 2005