Self nano-emulsifying simvastatin based tablets: Design and in vitro/in vivo evaluation

Pharmaceutical Development and Technology

Volumn 18, Issue 6, 2013, Pages 1294-1304

  Abdelbary, Ghada ^a   Amin, Maha ^a   Salah, Salwa ^a  

^a CAIRO UNIVERSITY   (Egypt)

Author keywords

in vivo study; LC MS MS; Liquisolid powder; Self nanoemulsification; Simvastatin

Indexed keywords

DIETHYLENE GLYCOL MONOETHYL ETHER; PEGLICOL 5 OLEATE; POLYSORBATE 80; SIMVASTATIN; UNCLASSIFIED DRUG; DRUG CARRIER; EMULSIFYING AGENT; EMULSION; ETHYLENE GLYCOL DERIVATIVE; EXCIPIENT; NANOPARTICLE; POLYSORBATE; POWDER; TABLET;

ADULT; ARTICLE; DRUG DESIGN; DRUG FORMULATION; DRUG SCREENING; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; LIQUID CHROMATOGRAPHY; MALE; NANOEMULSION; NORMAL HUMAN; PARTICLE SIZE; PRIORITY JOURNAL; TABLET; ZETA POTENTIAL; BIOAVAILABILITY; CHEMISTRY; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG DELIVERY SYSTEM; EMULSION; MEDICINAL CHEMISTRY; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; POWDER; PROCEDURES; RANDOMIZED CONTROLLED TRIAL; SOLUBILITY; SYNTHESIS;

ADMINISTRATION, ORAL; ADULT; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CROSS-OVER STUDIES; DRUG CARRIERS; DRUG DELIVERY SYSTEMS; EMULSIFYING AGENTS; EMULSIONS; ETHYLENE GLYCOLS; EXCIPIENTS; HUMANS; MALE; NANOPARTICLES; PARTICLE SIZE; POLYSORBATES; POWDERS; SIMVASTATIN; SOLUBILITY; TABLETS;

EID: 84883377214     PISSN: 10837450     EISSN: 10979867     Source Type: Journal    
DOI: 10.3109/10837450.2012.672989     Document Type: Article

References (46)

1. Cheng H, Sutton SC, Pipkin JD, Zentner GM, Rogers JD, Schwartz JI et al (Pubitemid 23325676)
2. McClelland GA, Stubbs RJ, Fix JA, Pogany SA, Zentner GM. Enhancement of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor efficacy through administration of a controlled-porosity osmotic pump dosage form. Pharm Res 1991;8:873-876
3. Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G et al. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm 2004;274:65-73 (Pubitemid 38457007)
4. USP 24/NF 19, USP Convention. (2000). Rockville. pp1942.
5. Aungst BJ. Novel formulation strategies for improving oral bioavailability of drugs with poor membrane permeation or presystemic metabolism. J Pharm Sci 1993;82:979-987
6. Burcham DL, Maurin MB, Hausner EA, Huang SM. Improved oral bioavailability of the hypocholesterolemic DMP 565 in dogs following oral dosing in oil and glycol solutions. Biopharm Drug Dispos 1997;18:737-742 (Pubitemid 27475189)
7. Serajuddin AT, Sheen PC, Mufson D, Bernstein DF, Augustine MA. Effect of vehicle amphiphilicity on the dissolution and bioavailability of a poorly water-soluble drug from solid dispersions. J Pharm Sci 1988;77:414-417 (Pubitemid 19080862)
8. Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm Res 1992;9:87-93
9. Craig DQM, Lievens HSR, Pitt KG, Storey DE. An investigation into the physicochemical properties of self-emulsifying systems using low frequency dielectric spectroscopy, surface tension measurements and particle size analysis. Int J Pharm 1993;96:147-155 (Pubitemid 23233280)
10. Shah NH, Carvajal MT, Patel CI, Infeld MH, Malick AW. Selfemulsifying drug delivery systems (SEDDS) with polyglycolysed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int J Pharm 1994;106:15-23 (Pubitemid 24110060)
11. Wakerly MG, Pouton CW, Meakin BJ, Morton FS. Self-emulsification of vegetable oil-nonionic surfactant mixtures: a proposed mechanism of action. ACS Symp Ser 1986;311:242-255
12. Kararli TT, Needham TE, Griffin M, Schoenhard G, Ferro LJ, Alcorn L. Oral delivery of a renin inhibitor compound using emulsion formulations. Pharm Res 1992;9:888-893
13. Myers RA, Stella VJ. Systemic bioavailability of penclomedine (NSC-338720) from oil-in-water emulsions administered intraduodenally to rats. Int J Pharm 1992;78:217-226
14. Palin KJ, Phillips AJ, Ning A. The oral absorption of cefoxitin from oil and emulsion vehicles in rats. Int J Pharm 1986;33:99-104 (Pubitemid 17197793)
15. Stella V, Haslam J, Yata N, Okada H, Lindenbaum S, Higuchi T. Enhancement of bioavailability of a hydrophobic amine antimalarial by formulation with oleic acid in a soft gelatin capsule. J Pharm Sci 1978;67:1375-1377 (Pubitemid 9031055)
16. Toguchi H, Ogawa Y, Iga K, Yashiki T, Shimamoto T. Gastro-intestinal absorption of ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy) phenyl]propionate from different dosage forms in rats and dogs. Chem Pharm Bull 1990;38:2792-2796 (Pubitemid 20386053)
17. Humberstone AJ, Charman WN. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv Drug Deliv Rev 1997;25:103-128
18. Tenjarla S. Microemulsions: an overview and pharmaceutical applications. Crit Rev Ther Drug Carrier Syst 1999;16:461-521 (Pubitemid 30004629)
19. Lieberman HA, Rieger MM, Banker GS, eds. (1996). Pharmaceutical dosage forms: Disperse systems. Second ed, Vol 1. New York: Marcel Decker, 211-281, 315-370
20. Kovarik JM, Mueller EA, van Bree JB, Tetzloff W, Kutz K. Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation. J Pharm Sci 1994;83:444-446 (Pubitemid 24224228)
21. Yin YM, Cui FD, Mu CF, Choi MK, Kim JS, Chung SJ et al. Docetaxel microemulsion for enhanced oral bioavailability: preparation and in vitro and in vivo evaluation. J Control Release 2009;140:86-94
22. Kanga BK, Lee JS, Chona SK, Jeong SY, Yuk SH, Khanga G, Lee HB, Choc SH. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J of Pharm 2004;274:65-73 (Pubitemid 38457007)
23. Patil P, Patil V, Paradkar A. Formulation of a self-emulsifying system for oral delivery of simvastatin: in vitro and in vivo evaluation. Acta Pharm 2007;57:111-122 (Pubitemid 46361952)
24. Spireas S, Sadu S, Grover R. In vitro release evaluation of hydrocortisone liquisolid tablets. J Pharm Sci 1998;87:867-872 (Pubitemid 28319418)
25. Staniforth JN. Pharmaceutics. (1988). In: Aulton ME, ed. The science of dosage form design. UK: Churchill, Livingstone, 610
26. Nazzal S, Nutan M, Palamakula A, Shah R, Zaghloul AA, Khan MA. Optimization of a self-nanoemulsified tablet dosage form of Ubiquinone using response surface methodology: effect of formulation ingredients. Int J Pharm 2002;240:103-114 (Pubitemid 34607707)
27. Sinko PJ, ed. (2006). Martin's physical pharmacy and biopharmaceutical sciences. 5th ed. Philadelphia: Lippincott Williams &Wilkins, 558.
28. Abdelbary G, Prinderre P, Eouani C, Joachim J, Reynier JP, Piccerelle P. The preparation of orally disintegrating tablets using a hydrophilic waxy binder. Int J Pharm 2004;278:423-433 (Pubitemid 38759514)
29. Chateau ME, Galet L, Soudais Y, Fages J. Processing a detergent powder formulation: direct compression, and high shear wet granulation followed by compression. Powder Technol 2005;157:191-198 (Pubitemid 41435534)
30. British Pharmacopeia Commission. British Pharmacopeia. (2002). London: Her Majesty's Stationary office.
31. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev 2000;45:89-121
32. US Pharmacopeia Convention. (2002). United States Pharmacopeia. 3rd ed. Rockville: US Pharmacopeia Convention.
33. Declaration of Helsinki. (2000). As amended by the 52nd World Medical Assembly (WMA). Edinburgh, Scotland: World Medical Association
34. FDA. (2002). Guidance of Industry, Food-effect Bioavailability and Bioequivalence Studies
35. Amy Y, Yang L, Donald S, Musson G, Jamie JZ. Short Application of a novel ultra-low elution volume 96-well solid-phase extraction method to the LC/MS/MS determination of simvastatin and simvastatin acid in human plasma. J Pharm Biomed Analysis 2005;38:521-527
36. Shah VP, Midha KK, Dighe S, McGilveray IJ, Skelly JP, Yacobi A et al. Analytical methods validation: bioavailability, bioequivalence and pharmacokinetic studies. Conference report. Eur J Drug Metab Pharmacokinet 1991;16:249-255
37. Shukla JB, Patel SJ. Formulation and Evaluation of self micro emulsifying system of candesartan cilexetil. Int J Pharm and Pharmaceut Sci 2010;2:143-146
38. Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, Lee HB, Cho SH. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm 2004;274:65-73 (Pubitemid 38457007)
39. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS PharmSciTech 2010;11:314-321
40. Constantinides PP, Scalart JP, Lancaster C, Marcello J, Marks G, Ellens H et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating mediumchain glycerides. Pharm Res 1994;11:1385-1390 (Pubitemid 24339642)
41. Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004;58:173-182 (Pubitemid 38479922)
42. Baboota S, Shakeel F, Ahuja A, Ali J, Shafiq S. Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib. Acta Pharm 2007;57:315-332 (Pubitemid 47429175)
43. Lu JL, Wang JC, Zhao SX, Liu XY, Zhao H, Zhang X et al. Selfmicroemulsifying drug delivery system (SMEDDS) improves anticancer effect of oral 9-nitrocamptothecin on human cancer xenografts in nude mice. Eur J Pharm Biopharm 2008;69:899-907
44. Cui J, Yu B, Zhao Y, Zhu W, Li H, Lou H et al. Enhancement of oral absorption of curcumin by self-microemulsifying drug delivery systems. Int J Pharm 2009;371:148-155
45. Balakrishnan P, Lee BJ, Oh DH, Kim JO, Hong MJ, Jee JP et al. Enhanced oral bioavailability of dexibuprofen by a novel solid selfemulsifying drug delivery system (SEDDS). Eur J Pharm Biopharm 2009;72:539-545
46. Nekkanti V, Karatgi P, Prabhu R, Pillai R. Solid self-microemulsifying formulation for candesartan cilexetil. AAPS PharmSciTech 2010;11:9-17.