Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effect of Additive of the Encapsulated Amounts and Solubility of Poorly Water-soluble Ibuprofen in Gelatin Microcapsules

  • Published : 2007.10.21
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Abstract

Poorly water-soluble ibuprofen and ethanol can be encapsulated in gelatin microcapsule by spray drying technique. To select an optimal formula of ibuprofen-loaded gelatin microcapsule which increased the ethanol content and ibuprofen solubility with the decreased amount of gelatin in the microcapsules, in this study, the effect of gelatin, ibuprofen and sodium lauryl sulfate on the ibuprofen solubility and the amount of ethanol and ibuprofen encapsulated in the gelatin microcapsule were investigated. Ibuprofen solubility and the amount of ethanol encapsulated increased as gelatin and sodium lauryl sulfate increased, reached maximum at 4% and 0.6%, respectively and then followed a rapid decrease. Furthermore, the ibuprofen solubility and the encapsulated ibuprofen content increased as the amount of ibuprofen increased, reaching maximum at 0.5% and beyond that, there was no change in the solubility and ibuprofen content. However, the encapsulated ethanol content remained same irrespective of the amount of ibuprofen. On the basis of increased ibuprofen solubility, our results showed that the formula of ibuprofen-loaded gelatin microcapsule at the ratio of gelatin/ibuprofen/sodium lauryl sulfate/water/ethanol of 4/0.5/0.6/30/70 with ibuprofen solubility of about $290\;{\mu}g/mL$ and ethanol content of about $160\;{\mu}g/mg$ could be a potential oral delivery system for poorly water-soluble ibuprofen.

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References

  1. D.J. Germhalgh, A.C. Williams, P. Timmins and P. York, Solubility parameters as predictors of miscibility in solid dispersions, J. Pharm. Sci., 88, 1182-1190 (1999) https://doi.org/10.1021/js9900856
  2. F.K. Glowka, Stereoselective pharmacokinetics of ibuprofen and its lysinate from suppositories in rabbits, Int. J. Pharm., 199, 159-166 (2000) https://doi.org/10.1016/S0378-5173(00)00377-X
  3. 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)
  4. J.L. Murtha and H.Y Ando, Synthesis of the cholesteryl ester prodrugs cholesteryl ibuprofen and cholesteryl flufenamate and their formulation into phospholipid microemulsions, J. Pharm. Sci., 83, 1222-1228 (1994) https://doi.org/10.1002/jps.2600830907
  5. M. Charoenchaitrakool, F. Dehghani and N.R. Foster, Utilization of supercritical carbon dioxIGM for complex formation of ibuprofen and methyl-beta-cyclodextrin, Int. J. Pharm., 239, 103-112 (2002) https://doi.org/10.1016/S0378-5173(02)00078-9
  6. M.K. Ghorab and M.C. Adeyeye, Enhancement of ibuprofen dissolution via wet granulation with beta-cyclodextrin, Pharm. Dev. Technol., 6, 305-314 (2001) https://doi.org/10.1081/PDT-100002611
  7. C.M. Adeyeye and J.C. Price, Development and evaluation of sustained-release ibuprofen-wax microspheres. 11. In vitro dissolution studies, Pharm. Res., 11, 575-579 (1994) https://doi.org/10.1023/A:1018931002991
  8. K. Kachrimanis, I. Nikolakakis and S. Malamataris, Spherical crystal agglomeration of ibuprofen by the solvent-change technique in presence ofmethacrylic polymers, J. Pharm. Sci., 89, 250-259 (2000) https://doi.org/10.1002/(SICI)1520-6017(200002)89:2<250::AID-JPS12>3.0.CO;2-W
  9. R. Bodmeier and J. Wang, Microencapsulation of drugs with aqueous colloidal polymer dispersions, J. Pharm. Sci., 82, 191-194 (1993) https://doi.org/10.1002/jps.2600820215
  10. G.M. Khan and Z. Jiabi, Ibuprofen release kinetics from controlled-release tablets granulated with aqueous polymeric dispersion of ethylcellulose II: Influence of several parameters and coexcipients, J. Controlled Rel., 56, 127-134 (1998) https://doi.org/10.1016/S0168-3659(98)00080-7
  11. C.S. Yong, M.K. Lee, Y.J Park, K.H. Kong, J.J. Xuan, J.H. Kim, J.A. Kim, W.S. Lyoo, S.S. Han, J.O. Rhee, J.O. Kim, C.H. Yang, C.K. Kim and H.G Choi, Enhanced oral bioavailability of ibuprofen in rats by poloxamer gel using poloxamer 188 and menthol, Drug Dev. Ind. Pharm., 31, 615-622 (2005) https://doi.org/10.1080/03639040500216113
  12. L.C. Menting and B. Hoogstad, Volatile retention during the drying aqueous carbohydrate solutions, J. Food Sci., 32, 87-90 (1967) https://doi.org/10.1111/j.1365-2621.1967.tb01965.x
  13. L.C. Menting, B. Hoogstad and H.A.C. Thijssen, Diffusion coefficient of water and organic volatiles in carbohydratewater system, J. Food Technol., 5, 111-126 (1970) https://doi.org/10.1111/j.1365-2621.1970.tb01549.x
  14. J. Sato and T. Kurusu, Process of manufacturing alcohol-containing solid matter, US Patent., 3786159 (1974)
  15. J.S. Kaka and A. Tekle, Bioavailability of ibuprofen from oral and suppository preparations in rats, Res. Commun. Chem. Pathol. Pharmacol., 76, 171-182 (1992)
  16. Z. Kokot and H. Zmidzinska, Solubility and dissolution rate of ibuprofen in ionic and non-ionic micellar systems, Acta Pol. Pharm., 58, 117-120 (2001)
  17. C.K. Kim, J.Y. Choi, Y.S. Yoon, J.P. Gong, H.G Choi, J.Y. Lee and B.J. Kong, Preparation and evaluation of dry elixir for the enhancement of dissolution rate of poorly water-soluble drugs, Int. J. Pharm., 106, 25-32 (1994) https://doi.org/10.1016/0378-5173(94)90272-0
  18. S.W Lee, M.H. Kim and C.K. Kim, Encapsulation of ethanol by spray drying technique: effects of sodium lauryl sulfate, Int. J. Pharm., 187, 193-198 (1999) https://doi.org/10.1016/S0378-5173(99)00185-4
  19. H.J. Ahn, K.M. Kim and C.K. Kim, Enhancement of bioavailability of ketoprofen using drug elixir as a novel dosage form, Drug Dev. Ind Pharm., 24(7), 697-701 (1998) https://doi.org/10.3109/03639049809082375
  20. C.K. Kim and Y.S. Yoon, Developement of digoxin dry elixir as a novel dosage form using a spray-drying technique, J. Microencapsul., 12, 547-556 (1995) https://doi.org/10.3109/02652049509006785
  21. C.K. Kim, Y.S. Yoon and lY Kong, Preparation and evaluation of flurbiprofen dry elixir as a novel dosage form using a spray-drying technique, Int. J. Pharm., 120,21-31 (1995) https://doi.org/10.1016/0378-5173(94)00375-F
  22. H.G Choi, B.J. Lee, C.S. Yong, J.D. Rhee, J.H. Han, M.K. Lee, K.M. Park and C.K. Kim, Terfenadine-${\beta}$-cyclodextrin inclusion complex with the anti-histaminic activity enhancement, Drug Dev. Ind Pharm., 27, 857-862 (2001) https://doi.org/10.1081/DDC-100107250
  23. C.S. Yong, Y.K. Oh, S.H. Jung, J.D. Rhee, H.D. Kim, C.K. Kim, J.S. Choi and H.G Choi, Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol, Eur. J. Pharm. Sci., 23, 347-353 (2004) https://doi.org/10.1016/j.ejps.2004.08.008
  24. C.S. Yong, C.H. Yang, J.D. Rhee, B.J. Lee, D.C. Kim, D.D. Kim, C.K. Kim, J.S. Choi and H.G. Choi, Enhanced rectal bioavailability of ibuprofen in rats by poloxamer 188 and menthol, Int. J. Pharm., 269, 169-176 (2004) https://doi.org/10.1016/j.ijpharm.2003.09.013