- Volume 59 Issue 2
DOI QR Code
Comparative Characterization Study on Quality Attributes of Vegetable and Gelatin as Capsule Shell of Soft Capsule
연질캡슐 피막물질로서 식물성 성분 원료와 젤라틴에 대한 품질특성 비교
- Kim, Dong Wook (A Department of Pharmaceutical Engineering, Cheongju University) ;
- Weon, Kwon Yeon (College of Pharmacy, Catholic University of Daegu)
- Received : 2015.04.02
- Accepted : 2015.04.27
- Published : 2015.04.30
A Softgel is an oral dosage form for medicine similar to capsules and softgel dosage form offers several advantages over other oral dosage forms, such as delivering a liquid matrix designed to solubilize and improve the oral bioavailability of a poorly soluble compound as a unit dose solid dosage form, delivering low and ultra-low doses of a compound. This study aimed to qualify a proprietary vegetable soft capsule which contains modified starch and carrageenan as capsule shell components compare to the conventional gelatin softgel. Four kinds of samples were prepared with vegetable and gelatin capsule shell, respectively. Morphology of capsule shell, mechanical strength of capsule, and hygroscopic properties were studied for comparing the quality attributes of softgel. Short-term stability against heat and moisture was also investigated in this study. Vegetable capsule shell showed better mechanical strength, physical stability and disintegration time for temperature and humidity than those of conventional gelatin capsule shell with four different filling materials used frequently as soft capsule form. Conclusively, this vegetable capsule shell polymer system can replace easily gelatin-shell systems and additionally allows encapsulation of lipid fills at high temperatures that are semisolid or solid-like at room temperature.
Supported by : 코스맥스바이오
- Lipinski, C. A., Lombardo, F., Dominy, B. W. and Feeney, P. J. : Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23, 3 (1997). https://doi.org/10.1016/S0169-409X(96)00423-1
- Lipinski, C. A. : Physicochemical properties in drug design/ development. 2nd International Drug Discovery and Development Summit: Novel Concepts and Technologies to Accelerate Drug Development. Honolulu, HI (2003).
- Agharkar, S., Lindenbaum, S. and Higuchi, T. : Enhancement of solubility of drug salts by hydrophilic counter-ions: Properties of organic salts of an anti-malarial drug. J. Pharm. Sci. 65, 747 (1976). https://doi.org/10.1002/jps.2600650533
- Bastin, R. J., Bowker, M. J. and Slater, B. J. : Salt selection and optimisation procedures for pharmaceutical new chemical entities. Org. Proc. Res. Dev. 4, 427 (2000). https://doi.org/10.1021/op000018u
- Serajuddin, A. T. M. : Salt formation to improve drug solubility. Adv. Drug Deliv. Rev. 59, 603 (2007). https://doi.org/10.1016/j.addr.2007.05.010
- Dannenfelser, R., He, H., Joshi, Y., Bateman, S. and Serajuddin, A. T. M. : Development of clinical dosage forms for a poorly water soluble drug I: Application of polyethylene glycolpolysorbate 80 solid dispersion carrier system. J. Pharm. Sci. 93, 1165 (2004). https://doi.org/10.1002/jps.20044
- Crew, M. D., Curatolo, W. J., Friesen, D. T., Gumkowski, M. J., Lorenz, D. A., Nightlingale, J. A. S., Ruggeri, R. B. and Shanker, R. M. : Pharmaceutical compositions of cholesteryl ester transfer protein inhibitors. US Patent Application 2007/ 0282009 (2007).
- Stella, V. J. and Nti-Addae, K. W. : Prodrug strategies to overcome poor water solubility. Adv. Drug Deliv. Rev. 59, 677 (2007). https://doi.org/10.1016/j.addr.2007.05.013
- Merisko-Liversidge, E., Liversidge, G. G. and Cooper, E. R. : Nanosizing: A formulation approach for poorly-water-soluble compounds. Eur. J. Pharm. Sci. 18, 113 (2003). https://doi.org/10.1016/S0928-0987(02)00251-8
- Kipp, J. E. : The role of solid nanoparticle technology in the parenteral delivery of poorly water-soluble drugs. Int. J. Pharm. 284, 109 (2004). https://doi.org/10.1016/j.ijpharm.2004.07.019
- Kesisoglou, F., Panmai, S. and Wu, Y. : Nanosizing-oral formulation development and biopharmaceutical evaluation. Adv. Drug Deliv. Rev. 59, 631 (2007). https://doi.org/10.1016/j.addr.2007.05.003
- Hauss, D. J. : Oral lipid-based formulations. Adv. Drug Deliv. Rev. 59, 667 (2007). https://doi.org/10.1016/j.addr.2007.05.006
- Crowley, P. J. and Martini, L. G. : Physicochemical approaches to enhancing oral absorption. Pharm. Technol. Eur. 16, 18 (2004).
- Strickley, R. G. : Solubilizing excipients in oral and injectable formulations. Pharm. Res. 21, 201 (2004). https://doi.org/10.1023/B:PHAM.0000016235.32639.23
- Gumkowski, M. J., Fournier, L. A., Tierney, N. K. and Curatolo, W. J. : Improved bioavailability through use of soft gelatin capsule formulations of terlakiren, a tripeptide rennin inhibitor. Pharm. Res. 11, S (1994).
- Yu, L., Bridgers, A., Polli, J., Vickers, A., Long, S., Roy, A., Winnike, R. and Coffin, M. : Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. J. Pharm. Sci. 16, 1812 (1999).
- Hugger, E. D., Novak, B. L., Burton, P. S., Audus, K. L. and Borchardt, R. T. : A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J. Pharm. Sci. 91, 1991 (2002). https://doi.org/10.1002/jps.10176
- Rege, B. D., Kao, J. P. and Polli, J. E. : Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur. J. Pharm. Sci. 16, 237 (2002). https://doi.org/10.1016/S0928-0987(02)00055-6
- Seeballuck, F., Ashford, M. B. and O'Driscoll, C. M. : The effects of pluronics block copolymers and cremophor EL on intestinal lipoprotein processing and the potential link with Pglycoprotein in Caco-2 cells. Pharm. Res. 20, 1085 (2003). https://doi.org/10.1023/A:1024422625596
- Wandel, C., Kim, R. B. and Stein, M. : ''Inactive'' excipients such as Cremophor can affect in vivo drug disposition. Clin. Pharmacol. Ther. 73, 394 (2003). https://doi.org/10.1016/S0009-9236(03)00010-9
- Cornaire, G., Woodley, J., Hermann, P., Cloarec, A., Arellano, C. and Houin, G. : Impact of excipients on the absorption of Pglycoprotein substrates in vitro and in vivo. Int. J. Pharm. 278, 119 (2004). https://doi.org/10.1016/j.ijpharm.2004.03.001
- Shono, Y., Nishihara, H., Matsuda, Y., Furukawa, S., Okada, N., Fujita, T. and Yamamoto, A. : Modulation of intestinal Pglycoprotein function by cremophor EL and other surfactants by an in vitro diffusion chamber method using the isolated rat intestinal membranes. J. Pharm. Sci. 93, 877 (2004). https://doi.org/10.1002/jps.20017
- Pole, D. L. : Physical and biological considerations for the use of nonaqueous solvents in oral bioavailability enhancement. J. Pharm. Sci. 97, 1071 (2008). https://doi.org/10.1002/jps.21060
- Kua, M., Li, W., Dulina, W., Donahuea, F., Cade, D., Benameur, H. and Hutchison, K. : Performance qualification of a new hypromellose capsule: Part I. Comparative evaluation of physical, mechanical and processability quality attributes of Vcaps Plus(R), Quali-V(R) and gelatin capsules. Int. J. Pharm. 386, 30 (2010). https://doi.org/10.1016/j.ijpharm.2009.10.050
- Rowe, R. C., Sheskey, P. S. and Weller, P. J. : Handbook of Pharmaceutical Excipients, 5th ed. Pharmaceutical Press (London, UK) and the American Pharmacists Association (Washington DC, USA) (2003).
- Cole, S. K., Story, M. J., Attwood, D., Laudanski, T., Robertson, J. and Barnwell, S. G. : Studies using a non-ionic surfactantcontaining drug delivery system designed for hard gelatin capsule compatibility. Int. J. Pharm. 88, 211 (1992). https://doi.org/10.1016/0378-5173(92)90318-V
- Brown, J., Madit, N., Cole, E. T., Wilding, I. R. and Cade, D. : Effect of cross-linking on the in vivo disintegration of hard gelatin capsules. Pharm. Res. 15, 1026 (1998). https://doi.org/10.1023/A:1011973909815