Browse > Article
http://dx.doi.org/10.4333/KPS.2002.32.1.027

Improved Dissolution Characteristics of Ibuprofen Employing Self-Microemulsifying Drug Delivery System and Their Bioavailability in Rats  

Kim, Hyung-Soo (College of Pharmacy, Chung-Ang University)
Lee, Sang-Kil (College of Pharmacy, Chung-Ang University)
Choi, Sung-Up (College of Pharmacy, Chung-Ang University)
Park, Hye-Sook (College of Pharmacy, Chung-Ang University)
Jeon, Hyun-Joo (College of Pharmacy, Chung-Ang University)
Choi, Young-Wook (College of Pharmacy, Chung-Ang University)
Publication Information
Journal of Pharmaceutical Investigation / v.32, no.1, 2002 , pp. 27-33 More about this Journal
Abstract
A self-microemulsifying drug delivery system(SMEDDS) composed of Cremophor $EL^{\circledR},\;Labrasol^{circledR}$, and Lauroglycol $FCC^{circledR}$ was prepared for the enhancement of solubility, dissolution rate and bioavailability of ibuprofen(IBP), which is water-insoluble but soluble in oils and surfactants. Phase diagram with various regions including microemulsion area was depicted. The SMEDDS was encapsulated in soft gelatin capsules and their dissolution characteristics in various media were observed in comparison to the generic products commercially available in the market. Soft capsules of SMEDDS formulation showed better dissolution profiles, especially in acidic condition, than the others. For the period of 1 hr dissolution in pH 1.2 medium, it reached over 70% dissolution from soft capsules, compared to less than 40% dissolution from commercial reference tablets. On the other hand, in vivo pharmacokinetic parameters were obtained after oral administrations of different IBP preparations to Sprague Dawley rats. SMEDDS formulation showed higher $C_{max}$ and greater $AUC_{0-5hr}$ than the suspension of reference tablet or IBP powder. Therefore, it is possible to conclude that a newly developed soft capsules employing SMEDDS provides an alternative preparation to improve oral bioavailability of IBP.
Keywords
Ibuprofen; SMEDDS; Soft capsule; Dissolution; Bioavailability;
Citations & Related Records
연도 인용수 순위
  • Reference
1 S.A Charman, W.N. Charman, M.C. Rogge, T.D. Wilson, F.D. Dutko and C.W. Pouton, Self-emulsifying drug delivery systems: Formulation and biopharmaceutical evaluation of an investigational lipophilic compound, Pharm. Res., 9, 87-93 (1992)   DOI   ScienceOn
2 N.H. Shah, M.T. Carvajal, C.I. Patel, M.H. Infeld and A.W. Malick, Self-emulsifying drug delivery systems with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs, Int. J. Pharm., 106, 15-23 (1994)   DOI   ScienceOn
3 D.Q.M. Craig, S.A. Baker, D. Banning, S.W. Booth, An investigation into the mechanism of self-emulsification using particle size analysis and low frequency dielectric spectro- scopy, Int. J. Pharm., 114, 103-110 (1995)   DOI   ScienceOn
4 M.J. Groves and R.M.A. Mustafa, Measurement of the spontaneity of self-emulsifiable oils, J. Pharm. Pharmacol., 26, 671-681 (1974)   DOI
5 A.K. Bansal, R.K. Khar, R. Dubey and A.K. Sharma, Effect of group substitution on the physicochemical properties of ibuprofen prodrugs, Pharmazie, 49, 422-424 (1994)
6 P.A. Insel, Analgesic-antipyretics and antiinflammatory agents: In Goodman Gilman's the pharmacological basis of thera- peutics, A.G. Gilman, T.W. Rall, A.S. Nies and P. Taylor (Eds.), McGraw Hill, Inc., New York, U.S.A., pp 664-668 (1991)
7 식품의약품안전청고시 제2000-26호, 약효동등성시험관리지침 및 대체조제의약품지정고시안
8 J.W. Lee, E.S. Park and S.C. Chi, Solubilization of ibuprofen in aqueous solution, J. Kor. Pharm. Sci., 27, 279-286 (1997)
9 D. Attwood, C. Mallon and C.J. Taylor, D. Attwood, C. Mallon and C.J. Taylor,, Int. J. Pharm., 84, R5-R8 (1992)   DOI   ScienceOn
10 AHFP Drug Information, p1499 (1997)
11 AHFP Drug Information, p1499 (1997)
12 K.H. Kim, Y.S. Rhee, J.H. Bae, S.C. Chi and E.S. Park, Improvement of dissolution rate of poorly water soluble drug using self-microemulsifying drug delivery system, J. Kor. Pharm. Sci., 29, 37-45 (1999)
13 J.H. Choi, J.Y. Kim and Y.S. Ku, Self-emulsifying drug delivery system containing ibuprofen for oral use, J. Kor. Pharm. Sci., 29, 99-103 (1999)
14 I.J. Oh, J.G. Park, Y.B. Lee and S.C. Shin, Inclusion complex of analgesic and antiinflammatory agents with cyclodextrins(I): Enhancement of dissolution of ibuprofen by 2-hydroxypropyl-$\beta$-cyclodextrin, J. Kor. Pharm. Sci., 23, 11-18 (1993)
15 S.C. Shin, I.J. Oh and I.B. Koh, Enhancement of dissolution properties of poorly soluble drugs(V): Enhanced dissolution of furosemide by cogrinding or coprecipitating with povidone, J. Kor. Pharm. Sci., 20, 193-198 (1990)
16 C.K. Kim and H.J. Shin, Soluble complex formation of rifampicin with alginate, YakhakHoeji., 27, 11-19 (1983)
17 Y.B. Jun, S.I. Kim and Y.I. Kim, Effect of surfactants on dissolution rate of mefenamic acid capsules, J. Kor. Pharm. Sci., 20, 121-127 (1990)