An in vitro and in vivo comparative study of directly compressed solid dispersions and freeze dried sildenafil citrate sublingual tablets for management of pulmonary arterial hypertension

1. C. W. Oakley, Primary pulmonary hypertension. Case series from the United Kingdom, Chest. 105 (1994) 29S-32S; DOI: 10.1378/chest.105.2_Supplement.29S.10.1378/chest.105.2_Supplement.29S8306805Search in Google Scholar

2. B. G. Schwartz, L. A. Levine, G. Comstock, V. J. Stecher and R. A. Kloner, Cardiac uses of Phosphodiesterase-5 Inhibitors, JACC 59 (2012) 9-15; DOI:10.1016/j.jacc.2011.07.051.10.1016/j.jacc.2011.07.05122192662Search in Google Scholar

3. G. D. Lewis, R. Shah, K. Shahzad, J. M. Camuso, P. P. Pappagianopoulos, J. Hung, A. Tawakol, R. E. Gerszten, D. M. Systrom, K. D. Bloch, M. J. Semigran, Sildenafil improves exercise capacity and quality of life in patients with systolic heart failure and secondary pulmonary hypertension, Circulation 116 (2007) 1555-1562; DOI: 10.1161/CIRCULATIONAHA.107.716373.10.1161/CIRCULATIONAHA.107.71637317785618Search in Google Scholar

4. V. Q. Chau, F. N. Salloum, N. N. Hoke, A. Abbate and R. C. Kukreja, Mitigation of the progression of heart failure with sildenafil involves inhibition of RhoA/Rho-kinase pathway, Am. J. Physiol. Heart Circ. Physiol. 300 (2011) H2272-H2279; DOI: 10.1152/ajpheart.00654.2010.10.1152/ajpheart.00654.2010311908521398594Search in Google Scholar

5. J. Nagendran, S. L. Archer, D. Soliman, V. Gurtu, R. Moudgil, A. Haromy, C. St Aubin, L. Webster, I. M. Rebeyka, D. B. Ross, P. E. Light, J. R. Dyck, E. D. Michelakis, Phosphodiesterase type 5 is highly expressed in the hypertrophied human right ventricle, and acute inhibition of phosphodiesterase type 5 improves contractility, Circulation 116 (2007) 238-248; DOI: 10.1161/CIRCULATIONAHA. 106.655266.Search in Google Scholar

6. L. Zhao, N. A. Mason, N. W. Morrell, B. Kojonazarov, A. Sadykov, A. Maripov, M. M. Mirrakhimov, A. Aldashev and M. R. Wilkins, Sildenafil inhibits hypoxia-induced pulmonary hypertension, Circulation 104 (2001) 424-428; DOI: 10.1161/hc2901.093117.10.1161/hc2901.09311711468204Search in Google Scholar

7. P. Rajagopalan, A. Mazzu, C. Xia, R. Dawkins and P. Sundaresan, Effect of high-fat breakfast and moderate-fat evening meal on pharmacokinetics of vardenafil, an oral phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, J. Clin. Pharmacol. 43 (2003) 260-267; DOI: 10.1177/0091270002250604.10.1177/009127000225060412638394Search in Google Scholar

8. A. H. Elshafeey, E. R. Bendasand O. H. Mohamed, Intranasal microemulsion of sildenafil citrate: in vitro evaluation and invivo pharmacokinetic study in rabbits, AAPSPharmSciTech. 10 (2009) 361-367; DOI: 10.1208/s12249-009-9213-6.10.1208/s12249-009-9213-6269077619333762Search in Google Scholar

9. A. H. Shajaei, Buccal mucosa as a route for systemic drug delivery. J. Pharm. Pharmaceut. Sci. 1 (1998) 15-30; http://www.ualberta.ca/~csps/JPPS1(1)/A.Shojaei/buccalreview.htm.Search in Google Scholar

10. Z. Bayrak, C. Tas, U. Tasdemir, H. Erol, C. K. Ozkan, A. Sayaser and Y. Ozkan, Formulation of zolmitriptan sublingual tablets prepared by direct compression with different polymers: In vitro and in vivo evaluation, Eur. J.Parm. Biopharm. 78 (2011) 499-505; DOI: 10.1016/j.ejpb.2011.02.014.10.1016/j.ejpb.2011.02.01421352916Search in Google Scholar

11. S. A. Randale, C. S. Dabhi, A. R. Tekade, V. S. Belgamwar, S. G. Gattani and S. J. Surana, Rapidly disintegrating tablets containing taste masked metoclopramide hydrochloride prepared by extrusion-precipitation method, Chem.Pharm. Bull, 58 (2010) 443-448; DOI: 10.1248/cpb.58.443.10.1248/cpb.58.44320410620Search in Google Scholar

12. S. Bandari, R. K. Mittapalli, R.Gannu and Y. H. Rao, Orodispersibletablets: an overview, Asian J. Pharm. 2 (2008) 2-11; DOI: 10.4103/0973-8398.41557.10.4103/0973-8398.41557Search in Google Scholar

13. G. Abdelbary, C. Eouani, P. Prinderre, J. Joachim, J. Reynier and P. Piccerelle, Determination of the in vitro disintegration profile of rapidly disintegrating tablets and correlation with oral disintegration, Int. J. Pharm. 292 (2005) 29-41; DOI:10.1016/j.ijpharm.2004.08.019.10.1016/j.ijpharm.2004.08.019Search in Google Scholar

14. J. W. Moore and H. H. Flanner, Mathematical comparison of dissolution profiles, Pharmaceutical Technology, 20 (1996) 64-74.Search in Google Scholar

15. »Declaration of Helsinki.« As amended by the 59th World Medical Assembly (WMA). World Medical Association, Seoul, South Korea, October 2008. Available at: http://www.wma.net/e/ethicsunit/helsinki.htm.Search in Google Scholar

16. V. P. Shah, K. K. Midha, S. Dighe, I. J. McGilveray, J. P. Skelly, A. Yacobi, T. Layloff, C. T. Viswanathan, C. E. Cook and R. D. McDowall, Analytical methods validation: bioavailability, bioequivalence and pharmacokinetic studies. Conference report, Eur. J. Drug Metab. Pharmacokinet. 16 (1991) 249-255; DOI: 10.1002/jps.2600810324.10.1002/jps.2600810324Search in Google Scholar

17. A. P. Simonelli, S. C. Mehta, W. I. Higuchi. Dissolution rates of high energy polyvinylpyrrolidone-sulfathiazole coprecipitates, J. Pharm. Sci. 58 (1969) 538-549; DOI: 10.1002/jps.2600580503.10.1002/jps.2600580503Search in Google Scholar

18. O. I. Corrigan, Mechanisms of dissolution of fast release solid dispersions. Drug Dev. Ind. Pharm. 11 (1985) 697-724; DOI: 10.3109/03639048509056896.10.3109/03639048509056896Search in Google Scholar

19. M. Newa, K. H. Bhandari, D. X. Li, T. H. Kwon, J. A. Kim, B. K. Yoo, J. S. Woo, W. S. Lyoo, C. S. Yong, H. G. Choi, Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with Poloxamer 188, Int. J. Pharm. 343 (2007) 228-237; DOI: 10.1016/j.ijpharm.2007. 05.031.Search in Google Scholar

20. N. Passerini, M. L. Gonzalez-Rodriguez, C. Cavallari, L. Rodriguez and B. Albertini, Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation, Eur. J. Pharm. Sci. 15 (2002) 71-78; DOI: 10.1016/S0928-0987(01)00210-X.10.1016/S0928-0987(01)00210-XSearch in Google Scholar

21. P. P. Shah and R. C. Mashru, Development and evaluation of artemether taste masked rapid disintegrating tablets with improved dissolution using solid dispersion technique. AAPS Pharm.Search in Google Scholar

Sci. Tech. 9 (2008) 494-500; DOI: 10.1208/s12249-008-9066-4. 22. S. Khan, H. Batchelor, P. Hanson, Y. Perrie and A. R. Mohammed, Physicochemical characterization, drug polymer dissolution and in vitro evaluation of phenacetin and phenylbutazone solid dispersions with polyethylene glycol 8000, J. Pharm. Sci. 100 (2011) 4281-4294; DOI: 10.1002/jps.22613.10.1002/jps.2261321560130Search in Google Scholar

23. A. Quadir and K. Kolter, A comparative study of current superdisintegrants, Pharma. Tech. Com. 2006.Search in Google Scholar

24. R. Chandrasekhar, Z. Hassan, F. Alhusban, A. M. Smith and A. R. Mohammed, The role of formulation excipients in the development of lyophilized fast-disintegrating tablets, Eur. J.Parm. Biopharm.72 (2009) 119-129; DOI: 10.1016/j.ejpb.2008.11.011.10.1016/j.ejpb.2008.11.01119073253Search in Google Scholar

25. W. L. Chiou and S. Riegelman, Pharmaceutical application of solid dispersion system, J. Pharm. Sci. 60 (1971) 1281-1302; DOI: 10.1002/jps.2600600902.10.1002/jps.26006009024935981Search in Google Scholar

26. R. A. Shoukri, I. S. Ahmed and R. N. Shamma, In vitro and in vivo evaluation of nimesulide lyophilized orally disintegrating tablets, Eur. J.Parm. Biopharm.73 (2009) 162-171; DOI: 10.1016/j.ejpb.2009.04.005.10.1016/j.ejpb.2009.04.00519406232Search in Google Scholar

27. V. B. Djagny, Z. Wang and S. Xu, Gelatin: A valuable protein for food and pharmaceutical industries: Review, Crit. Rev. Food Sci. Nutr.41 (2001) 481-492; DOI: 10.1080/20014091091904.10.1080/2001409109190411592686Search in Google Scholar

28. P. J. Dawson and D. J. Hockley, Scanning electron microscopy of freeze-dried preparations: relationship of morphology to freeze-drying parameters, Develop. Biol.Standard. 74 (1991) 185-192.Search in Google Scholar

29. D. J. van Drooge, W. L. J. Hinrichs and H. W. Frijlink, Incorporation of lipophilic drugs in sugar glasses by lyophilization using a mixture of water and tertiary butyl alcohol as solvent, J. Pharm. Sci.93 (2004) 713-725; DOI: 10.1002/jps.10590.10.1002/jps.1059014762909Search in Google Scholar

30. A. A. Mahmoud and S. Salah, Fast relief from migraine attacks using fast-disintegrating sublingual zolmitriptan tablets, Drug Dev. Ind. Pharm. (2011) 1-8; DOI:10.3109/03639045.2011.625949.10.3109/03639045.2011.62594922023340Search in Google Scholar

31. REVATIO - sildenafil citrate tablet, film coatedPfizer Labs http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfmfiarchiveid=10206.Search in Google Scholar

32. A. Abdelbary, A. H. Elshafeeyand G. Zidan, Comparative effects of different cellulosic-based directly compressed orodispersable tablets on oral bioavailability of famotidine, Carb. Polym. 77 (2009) 799-806; DOI:10.1016/j.carbpol.2009.02.030.10.1016/j.carbpol.2009.02.030Search in Google Scholar

33. M. M. Rawas-Qalaji, F. E. Simons and K. J.Simons, Sublingual epinephrine tablets versus intramuscular injection of epinephrine: Dose equivalence for potential treatment of anaphylaxis, J. Allergy Clin. Immunol. 117 (2006) 398-403; DOI:10.1016/j.jaci.2005.12.1310.10.1016/j.jaci.2005.12.131016461140Search in Google Scholar

34. G. V. Betageri and K. R. Makarla, Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques, Int. J. Pharm. 126 (1995) 155-160; DOI: 10.1016/0378-5173(95) 04114-1.Search in Google Scholar