Formulation and in vivo evaluation of self-nanoemulsifying granules for oral delivery of a combination of ezetimibe and simvastatin

Drug Development and Industrial Pharmacy

Volumn 34, Issue 12, 2008, Pages 1285-1296

  Dixit, Rahul P ^a   Nagarsenker, M S ^a  

^a BOMBAY COLLEGE OF PHARMACY   (India)

Author keywords

Colloidal silicon dioxide; Ezetimibe; Hyperlipidemia; Self nanoemulsifying granules; Simvastatin

Indexed keywords

AEROSIL; CAPRYOL 90; CHOLESTEROL; CREMOPHOR; DODECYL SULFATE SODIUM; EXCIPIENT; EZETIMIBE; LABRAFIL 1944; LABRASOL; LAUROGLYCOL 90; MACROGOL 400; MIGLOYL 812; NEOBEE M 5; POLYSORBATE 80; SILICON DIOXIDE; SIMVASTATIN; SOLUTOL HS 15; SURFACTANT; TRANSCUTOL P; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ADSORPTION; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG GRANULE; DRUG STABILITY; EVALUATION; HYDROPHILICITY; HYPERCHOLESTEROLEMIA; IN VIVO STUDY; MALE; NANOEMULSION; NONHUMAN; PARTICLE SIZE; POWDER; RAT; SCANNING ELECTRON MICROSCOPY; TRIACYLGLYCEROL BLOOD LEVEL; X RAY DIFFRACTION;

ADMINISTRATION, ORAL; ANIMALS; ANTICHOLESTEREMIC AGENTS; AZETIDINES; CHEMISTRY, PHARMACEUTICAL; CHOLESTEROL; EMULSIONS; MALE; MICROSCOPY, ELECTRON, SCANNING; NANOPARTICLES; RATS; RATS, SPRAGUE-DAWLEY; SIMVASTATIN; SOLUBILITY; X-RAY DIFFRACTION;

EID: 57349119914     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.1080/03639040802071570     Document Type: Article

References (34)

1. Ahmed, I. S., & Aboul-Einien, H. A. (2007). In vitro and in vivo evaluation of a fast- disintegrating lyophilized dry emulsion tablet containing griseofulvin. Eur. J. Pharm. Sci., 32, 58-68.
2. Alvarez-Lueje, A., Valenzuela, C., Squella, J. A., & Núñez-Vergara, L. J. (2005). Stability study of simvastatin under hydrolytic conditions assessed by liquid chromatography. J AOAC Int., 88, 1631-1636.
3. Ambike, A. A., Mahadik, K. R., & Paradkar, A. R. (2005). Spray-dried amorphous solid dispersions of Simvastatin, a low Tg drug: In vitro and in vivo evaluations. Pharm. Res., 22, 990-998.
4. Bays, H. E., Ose, L., Fraser, N., Tribble, D. L., Quinto, K., Reyes, R., Johnson-Levonas, A. O, Sapre, A., & Donahue, S. R. (2004). A multicenter, randomized, double-blind, placebo-controlled, factorial design study to evaluate the lipid-altering efficacy and safety profile of the Ezetimibe/Simvastatin tablet compared with Ezetimibe and Simvastatin monotherapy in patients with primary hypercholesterolemia. Clin. Ther., 26, 1758-1773.
5. Chambin, O., Bellone, C., Champion, D., Rochat-Gonthier, M. H., & Pourcelot, Y. (2000). Dry adsorbed emulsion: 1 Characterization of an intricate physicochemical structure. J. Pharm. Sci., 89, 991-999.
6. Chambin, O., Berard, V., Rochat-Gonthier, M. H., & Pourcelot, Y. (2002). Dry adsorbed emulsion: 2. Dissolution behaviour of an intricate formulation. Int. J. Pharm., 235, 169-178.
7. Christensen, K. L., Pedersen, G. P., & Kristensen H. G. (2001). Preparation of redispersible dry emulsion by spray drying. Int. J. Pharm., 212, 187-194.
8. Christensen, K. L., Pedersen, G. P., & Kristensen, H. G. (2002). Physical stability of redispersible dry emulsions containing amorphous sucrose. Eur. J. Pharm. Biopharm., 53, 147-153.
9. Cornaire, G., Woodley, J., Hermann, P., Cloarec, A., Arellano, C., & Houin G. (2004). Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int. J. Pharm., 278, 119-131.
10. Corveleyn, S., & Remon, J. P. (1998a). Formulation of a lyophilized dry adsorbed emulsion tablet for the delivery of poorly soluble drugs. Int. J. Pharm., 166, 65-74.
11. Corveleyn, S., & Remon, J. P. (1998b). Bioavailability of hydrochlorothiazide: Conventional versus freeze-dried tablets. Int. J. Pharm., 173, 149-155.
12. Corveleyn, S., & Remon, J. P. (1999). Stability of freeze-dried tablets at different relative humidities. Drug Dev. Ind. Pharm. 25, 1005-1013.
13. Cui, F., Wang, Y., Wang, J., Feng, L., & Ning, K. (2007). Preparation of redispersible dry emulsions using Eudragit E100 as both solid carrier and unique emulsifier. Coll. Surf. A: Physicochem. Eng. Asp., 307, 131-141.
14. Davis, H. R., Pula, K. K, Alton, K. B, Burrier, R. E., & Watkins, R. W. (2001). The synergistic hypocholesterolemic activity of the potent cholesterol absorption inhibitor, ezetimibe, in combination with 3-Hydroxy-3-Methylglutaryl Coenzyme A reductase inhibitors in dogs. Metabolism, 50, 1234-1241.
15. Dollo, G., Corre, P. L., Guerin, A., Chevanne, F. O., Burgot, J. L., & Leverge, R. (2003). Spray-dried redispersible oil-in-water emulsion to improve oral bioavailability of poorly soluble drugs. Eur. J. Pharm. Sci., 19, 273-280.
16. Dollo, G., Corre, P. L., Chevanne, F., & Verge, R.L. (2004). Bupivacaine containing dry adsorbed emulsion can prolong epidural anesthetic effects in rabbits. Eur. J. Pharm. Sci., 22, 63-70.
17. Farah, N., Bouzan, J., Rollet, M., Taverdet, J. L., & Vergnaud, J. M. (1987). 'Dry emulsion' - a sustained release form: modelling of drug transfers in liquids. Int. J. Pharm., 36, 81-88.
18. Formiga, F. R., Fonseca, I. A. A., Souza, K. B., Silva, A. K. A., Macedo, J. P. F., Aráujo, I. B., Soares, L. A. L., Socrates, E., & Egito T. (2007). Influence of a lipophilic drug on the stability of emulsions: An important approach on the development of lipidic carriers. Int. J. Pharm., 344, 158-160.
19. Hansen, T., Holm, P., & Schultz, K. (2004). Process characteristics and compaction of spray-dried emulsions containing a drug dissolved in lipid. Int. J. Pharm., 287, 55-66.
20. Hansen. T., Holm, P., Rohde. M., & Schultz, K. (2005). In vivo evaluation of tablets and capsules containing spray-dried o/w emulsions for oral delivery of poorly soluble drugs. Int. J. Pharm., 293, 203-211.
21. Hauss, D. J. (2007). Oral lipid based formulations. Adv. Drug Del. Rev., 59, 667-676.
22. Heinzelmann, K., & Franke, K. (1999). Using freezing and drying techniques of emulsions for the microencapsulation of fish oil to improve oxidation stability. Colloids Surf. B., 12, 223-229.
23. Humberstone, A. J., & Charman W. N. (1997). Lipid- based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug Del. Rev., 25, 103-128.
24. Jang, D. J., Jeong, E. J., Lee, H.M., Kim, B.C., Lim, S. J., & Kim, C. K. (2006). Improvement of bioavailability and photostability of amlodipine using redispersible dry emulsion. Eur. J. Pharm. Sci., 28, 405-411.
25. Kang, B. K., Lee, J. S., Chon, S. K., Jeong, S. Y., Yuk, S. H., Khang, G., Lee, H. B., & Cho S. H. (2004). Development of self microemulsifying drug delivery system (SMEDDS) for oral bioavailability enhancement of Simvastatin in beagle dogs. Int. J. Pharm., 274, 65-73.
26. Kosoglou, T., Statkevich, P., Johnson- Levonos, A.O., Paolini, J. F., Bergman, A. J., & Alton, K. B. (2005). Ezetimibe: A review of its metabolism, pharmacokinetics and drug interaction. Clin. Pharmaco., 44, 467-494.
27. McKenney, J. M., Jones, P. H., Bays, H. E., Knopp, R. H., Kashyap, M. L., Ruoff, G. E., & McGovern, M. E. (2007). Comparative effects on lipid levels of combination therapy with a statin and extended-release niacin or ezetimibe versus a statin alone (the COMPELL study). Atherosclerosis, 192, 432-437.
28. Myers S. L., & Shively M. L. (1993). Solid state emulsion: the effect of maltodextrin on microcrystalline aging. Pharm. Res., 10, 1389-1391.
29. Nazzal, S., Smalyukh, I. I., Lavrentovich, O.D., & Khan, M. A. (2002). Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: Mechanism and progress of emulsion formation. Int. J. Pharm., 235, 247-265.
30. Newton, M., Petersson, J., Podczeck, F., Clarke, A., & Booth S. (2001). The influence of formulation variables on the properties of pellets containing a self-emulsifying mixture. J. Pharm. Sci., 90, 987-995.
31. Patil, P., Patil, V., & Paradkar A. (2007). Formulation of a self-emulsifying system for oral delivery of simvastatin: In vitro and in vivo evaluation. Acta Pharm., 57, 111-122.
32. Pedersen, G. P., Faldt, P., Bergenstahl, B., & Kristensen, H. G. (1998). Solid state characterizations of a dry emulsion: a potential drug delivery system. Int. J. Pharm., 171, 257-270.
33. Toorisaka, E., Hashida, M., Kamiya, N., Ono, H, Kokazu, Y., & Goto, M. (2005). An enteric-coated dry emulsion formulation for oral insulin delivery. J. Cont. Rel., 107, 91-96.
34. Wandel, C., Kim, R.B., & Stein, M. (2003). "Inactive" excipients such as Cremophor can affect in vivo drug disposition. Clin. Pharmacol. Ther., 73, 394-396.