Formulation and evaluation of felodipine in softgels with a solubilized core

Asian Journal of Pharmaceutical Sciences

Volumn 4, Issue 3, 2009, Pages 144-160

  Aboul Einien, Mona Hassan ^a  

^a CAIRO UNIVERSITY   (Egypt)

Author keywords

Bioavailability; Dielectric constant; Felodipine; Micellar solubilization; Softgels

Indexed keywords

ANIONIC SURFACTANT; CATIONIC SURFACTANT; FELODIPINE; NONIONIC SURFACTANT;

ARTICLE; CONTROLLED STUDY; DIELECTRIC CONSTANT; DISSOLUTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG SCREENING; DRUG SOLUBILITY; DRUG SOLUTION; DRUG STORAGE; GEL; IN VITRO STUDY; IN VIVO STUDY; MICELLE; SOLUBILIZATION;

EID: 77953469678     PISSN: 18180876     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (46)

1. K. C. Yedinak, L. M. Lopez. Felodipine: a new dihydropyridine calcium channel antagonist. DICP, 1991, 25: 1193-1206.
2. T. Walton, L. R. Symes. Felodipine and isradipine: new calcium-channel-blocking agents for the treatment of hypertension. Clin. Pharm., 1993, 12: 261-275.
3. W. C. Little, C. P. Cheng, L. Elvelin, et al. Vascular selective calcium entry blockers in the treatment of cardiovascuolar disorders: focus on felodipine. Cardiovasc. Drugs Ther., 1995, 9: 657-663.
4. H. Song, W. Bao, H. Wang, G. An, J. Feny, R. Wang, Y. Zhang, F. An. Effects of extended release felodipine on endothelial vasoactive substances in patients with essential hypertension. Clin. Chem. Lab. Med., 2008, 46: 393-395.
5. R. Yao, X. Cheng, Y. H. Liao, et al. Molecular mechanisms of felodipine suppressing atheroscelerosis in high-cholesteroldiet apolipoprotein E-knockout mice. J. Cardiovasc. Pharmacol., 2008, 51: 188-195.
6. P. H. Dunselman, B. Edgar. Felodipine clinical pharmacokinetics. Clin. Pharmacokinet., 1991, 21: 418-430.
7. E. Saltiel, A. G. Ellrodt, J. P. Monk, et al. A Review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension. Drugs, 1988, 36: 387-428.
8. D. Jack. Handbook of clinical pharmacokinetic data, Macmillan Publishers, 1992, 81-82.
9. P. Kallinteri, S. G. Antimisiaris. Solubility of drugs in the presence of gelatin: effect of drug lipophilicity and degree of ionization. Int. J. Pharm., 2001, 221: 219-226.
10. S. H. Yolkowsky, S. C. Valvani. Precipitation of solubilized drugs due to injection or dilution. Drug Intell. Clin. Pharm., 1977, 11: 417-419.
11. S. H. Yalkowsky. Techniques of solubilization of drugs, Dekker, New York, 1981, 1-14.
12. J. Kerc, S. Srcic, B. Kofler. Alternative solvent-free preparation methods for felodipine surface solid dispersions. Drug Dev. Ind. Pharm., 1998, 24: 359-363.
13. E. Karavas, G. Ktistis, A. Xenakis, et al. Miscibility behavior and formation mechanism of stabilized felodipinepolyvinylpyrrolidone amorphous solid dispersions. Drug Dev. Ind. Pharm., 2005, 31: 473-489.
14. E. Karavas, G. Ktistis, A. Xenakis, et al. Effect of hydrogen bonding on the release mechanism of felodipine from nanodispersions with polyvinylpyrrolidone. Eur. J. Pharm. Biopharm., 2006,63: 103-141.
15. D. H. Won, M. S. Kim, S. Lee, et al. Improved physicochemical characteristics of felodipine solid dispersion particles by supercritical anti-solvent precipitation process. Int. J. Pharm. 2005, 301: 199-208.
16. E. J. Kim, M. K. Chun, J. S. Jang, et al. Preparation of a solid dispersion of felodipine using a solvent wetting method. Eur. J. Pharm. Biopharm., 2006, 64: 200-205.
17. A. T. Serajuddin. Solid dispersion of poorly water-soluble drugs: early promises, subsequent problems and recent breakthroughs. J. Pharm. Sci.,1999, 88: 1058-1066.
18. J. Kerc, S. Srcic, B. Kofler, et al. Micronization of drugs using supercritical carbon dioxide. Int. J. Pharm., 1999, 182: 33-39.
19. A. H. Chiou, H. C. Cheng, D. P. Wang. Micronization and microencapsulation of felodipine by supercritical carbon dioxide. J. Microencapsul., 2006, 23: 265-276.
20. M. Vogt, K. Kunath, J. B. Dressman. Dissolution improvement of four poorly water soluble drugs by cogrinding with commonly used excepients. Eur. J. Pharm. Biopharm., 2008, 68: 330-337.
21. C. K. Kim, J. S. Park. Solubility enhancers for oral drug delivery: can chemical structure manipulation be avoided? Am. J. Drug Del., 2004, 2: 113-130
22. P. Li, L. Zhao, S. H. Yalkowsky. Combined effect of cosolvent and cyclodextrin on solubilization of nonpolar drugs. J. Pharm. Sci., 1999, 88: 1107-1111.
23. J. W. Millard, F. A. Alvarez-Nunez, S. H. Yalkowsky. Solubilization by cosolvents. Establishing useful constants for the log-linear model. Int. J. Pharm., 2002, 245: 153-166.
24. P. Li, L. Zhao. Solubilization of flurbiprofen in pH-surfactant solutions. J. Pharm. Sci., 2003, 92: 951-956.
25. A. Martin, A. Paruta, A. Adjei. Extended hildebrand solubility approach: methylxanthines in mixed solvents. J. Pharm. Sci., 1981, 70: 1115-1120.
26. J. Kerc, S. Srcic, B. Kofler, et al. Molar solubility of felodipine in different aqueous systems. Int. J. Pharm., 1992, 81: R1-R4.
27. E. Söderlind, M. Wollbratt, C. V. Corswant. The usefulness of sugar surfactants as solubilizing agents in parenteral formulations. Int. J. Pharm., 2003, 252: 61-71.
28. F. S. Hom, S. A. Veresh, W. R. Ebert. Soft gelatin capsules II: Oxygen permeability study of capsule shells. J. Pharm. Sci., 1975, 64: 851-857.
29. V. Alvisi, C. Longhini, B. Bagni, et al. An improvement in digoxin bioavailability. Studies with soft gelatin capsules containing a solution of digoxin. Arzneimittelforschung, 1979, 29: 1047-1050.
30. E. Astorri, G. Bianchi, G. La Canna, et al. Bioavaiability and related heart function index of digoxin capsules and tablets in cardiac patients. J. Pharm. Sci., 1979, 68: 104-106.
31. L. M. Fuccella. Bioavailability of temazepam in soft gelatin capsules. Br. J. Clin. Pharmacol., 1979, 8: 318-358.
32. C. B. Bottom, M. Clark, J.T. Carstensen. Dissolution testing of soft shell capsules-Acetaminophen and nifedipine. J. Pharm. Sci., 1997, 86: 1057-1061.
33. S. S. Hong, S. H. Lee, Y. J. Lee, et al. Accelerated oral absorption of gliclazide in human subjects from a soft gelatin capsule containing a PEG400 suspension of glicazide. J. Control. Release, 1998,51: 185-192.
34. S. G. Yang, D. D. Kim, S. J. Chung, et al. Stable bioavailability of cycloporin A, regardless of food intake, from soft gelatin capsule containing a new self-emulsifying formulation. Int. J. Clin. Pharmacol. Ther., 2006, 44: 233-239.
35. A. Avramoff, A. Laor, R. Kitzes-Cohen, et al. Comparative in vivo bioequivalence and in vitro dissolution of two cyclosporine A soft gelatin capsule formulations. Int. J. Clin. Pharmacol. Ther., 2007, 45: 126-132.
36. M. Ahnoff. Determination of felodipine in plasma by capillary gas chromatography with electron capture detection. J. Pharm. Biomed. Anal., 1984, 2: 519-526.
37. Web site: http: // www. trimen.pl.
38. L. Augsburger. Hard and soft gelatin capsules, in: G. S. Banker, C. T. Rhodes (eds.), Modern Pharmaceutics, 4th. Ed., 2002, Marcel Dekker, Inc., pp. 371.
39. T. Amemiya, S. Misono, H. Yausa, et al. Development of emulsion type new vehicle for soft gelatin capsule. I. Selection of surfactants for development of new vehicle and its physicochemical properties. Chem. Pharm. Bull., 1998, 46: 309-313.
40. B. Abrahamsson, D. Johansson, A. Torestensson, et al. Evaluation of solubilizers in the drug release testing of hydrophilic matrix extended-release tablets of felodipine. Pharm. Res., 1994, 11: 1093-1097.
41. A. T. M. Serajuddin, P. C. Sheen, M. A. Augustine. Water migration from soft gelatin capsule shell to fill material and its effect on drug solubility. J. Pharm. Sci., 1986, 75: 62-64.
42. L. Chafetz, H. W. Hong, D. C. Tsilifonis, et al. Decrease in the rate of capsule dissolution due to formaldehyde from polysorbate 80 autoxidation. J. Pharm. Sci., 1984, 73: 1186-1189.
43. G. A. Digenis, T. B. Gold, V. P. Shah. Cross-linking of gelatin capsules and its relevance to their in vitro-in vivo performance. J. Pharm. Sci., 1994, 83: 915-921.
44. M. Weis, S. A. Mortensen, M. R. Rassing, et al. Bioavailability of four oral coenzyme Q10 fornulations in healthy volunteers. Mol. Aspects Med., 1994, 15: 273-280.
45. A. A. Zaghloul, B. Gurley, M. Khan, et al. Bioavailability assessment of oral coenzyme Q10 formulations in dogs. Drug Dev. Ind. Pharm., 2002, 28: 1195-1200.
46. B. J. Aungst. Intestinal permeation enhancers (Review). J. Pharm. Sci., 2000, 89: 429-442.