Formulation, preparation, and evaluation of novel orally disintegrating tablets containing taste-masked naproxen sodium granules and naratriptan hydrochloride

Journal of Pharmaceutical Sciences

Volumn 103, Issue 4, 2014, Pages 1233-1245

  Stange, Ulrike ^a   Führling, Christian ^b   Gieseler, Henning ^a,c  

^a UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^b Niederbronner Pharmacy   (Germany)

^c GILYOS GmbH   (Germany)

Author keywords

excipients; fast melting tablet; formulation; freeze drying lyophilization; microparticles; migraine; oral drug delivery; orally disintegrating tablet; taste masking

Indexed keywords

ALGINIC ACID; EUDRAGIT; GELATIN; HETASTARCH; MENTHOL; METHYLCELLULOSE; NAPROXEN; NARATRIPTAN; POLOXAMER; SUCROSE;

ARTICLE; BITTER TASTE; DRUG ABSORPTION; DRUG GRANULE; DRUG RELEASE; DRUG SCREENING; DRUG SOLUBILITY; DRUG STABILITY; DRUG STORAGE; DRUG SYNTHESIS; FLAVOR; FREEZE DRYING; MIGRAINE; ORALLY DISINTEGRATING TABLET; PARTICLE SIZE; PERFORMANCE; ROOM TEMPERATURE; TABLET DISINTEGRATION; TABLET DISINTEGRATION TIME; TABLET FORMULATION; TABLET HARDNESS; TABLET MANUFACTURE; TABLET PROPERTY; TASTE;

EXCIPIENTS; FAST MELTING TABLET; FORMULATION; FREEZE DRYING/LYOPHILIZATION; MICROPARTICLES; MIGRAINE; ORAL DRUG DELIVERY; ORALLY DISINTEGRATING TABLET; TASTE MASKING;

ADMINISTRATION, ORAL; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; DRUG COMPOUNDING; DRUG STORAGE; EXCIPIENTS; FREEZE DRYING; MIGRAINE DISORDERS; NAPROXEN; PARTICLE SIZE; PIPERIDINES; POLYMETHACRYLIC ACIDS; SOLUBILITY; TABLETS; TASTE; TRYPTAMINES; VASOCONSTRICTOR AGENTS;

EID: 84896388565     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23896     Document Type: Article

References (73)

1. Carnaby-Mann G, Crary M,. 2005. Pill swallowing by adults with dysphagia. Arch Otolaryngol Head Neck Surg 131 (11): 970-975.
2. Shukla D, Chakraborty S, Singh S, Mishra B,. 2009. Mouth dissolving tablets I: An overview of formulation technology. Scientia Pharmaceutica 77 (2): 309-326.
3. Shoukri RA, Ahmed IS, Shamma RN,. 2009. In vitro and in vivo evaluation of nimesulide lyophilized orally disintegrating tablets. Eur J Pharm Biopharm 73 (1): 162-171.
4. Clarke A, Brewer F, Johnson ES, Mallard N, Hartig F, Taylor S, Corn TH,. 2003. A new formulation of selegiline: Improved bioavailability and selectivity for MAO-B inhibition. J Neural Transm 110 (11): 1241-1255.
5. Corveleyn S, Paul Remon J,. 1998. Bioavailability of hydrochlorothiazide: Conventional versus freeze-dried tablets. Int J Pharm 173 (1-2): 149-155.
6. Ibrahim HK, El-Setouhy DA,. 2010. Valsartan orodispersible tablets: Formulation, in vitro/in vivo characterization. AAPS PharmSciTech 11 (1): 189-196.
7. Ahmed IS, Hassan M,. 2007. In vitro and in vivo evaluation of a fast-disintegrating lyophilized dry emulsion tablet containing griseofulvin. Eur J Pharm Sci 32 (1): 58-68.
8. Fu YR, Yang SC, Jeong SH, Kimura S, Park K,. 2004. Orally fast disintegrating tablets: Developments, technologies, taste-masking and clinical studies. Crit Rev Ther Drug Carr Syst 21 (6): 433-475.
9. Gendolla A,. 2005. Part I: What do patients really need and want from migraine treatment? Curr Med Res Opin 21: 3-7.
10. Seager H,. 1998. Drug-delivery products and the Zydis fast-dissolving dosage form. J Pharm Pharmacol 50 (4): 375-382.
11. Corveleyn S, Remon JP,. 1998. Formulation of a lyophilized dry emulsion tablet for the delivery of poorly soluble drugs. Int J Pharm 166 (1): 65-74.
12. Ahmed IS, Nafadi MM, Fatahalla FA,. 2006. Formulation of a fast-dissolving ketoprofen tablet using freeze-drying in blisters technique. Drug Dev Ind Pharm 32 (4): 437-442.
13. Corveleyn S, Remon JP,. 1997. Formulation and production of rapidly disintegrating tablets by lyophilisation using hydrochlorothiazide as a model drug. Int J Pharm 152 (2): 215-225.
14. Lai F, Pini E, Angioni G, Manca ML, Perricci J, Sinico C, Fadda AM,. 2011. Nanocrystals as tool to improve piroxicam dissolution rate in novel orally disintegrating tablets. Eur J Pharm Biopharm 79 (3): 552-558.
15. AlHusban F, Perrie Y, Mohammed AR,. 2010. Formulation and characterisation of lyophilised rapid disintegrating tablets using amino acids as matrix forming agents. Eur J Pharm Biopharm 75 (2): 254-262.
16. Chandrasekhar R, Hassan Z, AlHusban F, Smith AM, Mohammed AR,. 2009. The role of formulation excipients in the development of lyophilised fast-disintegrating tablets. Eur J Pharm Biopharm 72 (1): 119-129.
17. AlHusban F, Perrie Y, Mohammed AR,. 2010. Preparation, optimisation and characterisation of lyophilised rapid disintegrating tablets based on gelatin and saccharide. Curr Drug Deliv 7 (1): 65-75.
18. Chandrashekar J, Kuhn C, Oka Y, Yarmolinsky DA, Hummler E, Ryba NJP, Zuker CS,. 2010. The cells and peripheral representation of sodium taste in mice. Nature 464 (7286): 297-U182.
19. AlHusban F, ElShaer AM, Kansara JH, Smith AM, Grover LM, Perrie Y, Mohammed AR,. 2010. Investigation of formulation and process of lyophilised orally disintegrating tablet (ODT) using novel amino acid combination. Pharmaceutics 2: 1-17.
20. Vennat B, Gross D, Pourrat A, Legret P,. 1993. [Oral freeze-dried forms of procyanidins]. J Pharm Belg 48 (6): 430-436.
21. Brown D,. 2003. Orally disintegrating tablets-Taste over speed. Drug Deliv Technol 3 (6): 1-5.
22. Douroumis D,. 2007. Practical approaches of taste masking technologies in oral solid forms. Expert Opin Drug Deliv 4 (4): 417-426.
23. Sugiura T, Uchida S, Namiki N,. 2012. Taste-Masking effect of physical and organoleptic methods on peppermint-scented orally disintegrating tablet of famotidine based on suspension spray-coating method. Chem Pharm Bull 60 (3): 315-319.
24. Douroumis DD, Gryczke A, Schminke S,. 2010. Development and evaluation of cetirizine HCl taste-masked oral disintegrating tablets. AAPS PharmSciTech 12 (1): 141-151.
25. Jagdale SC, Gawali VU, Kuchekar BS, Chabukswar AR,. 2011. Formulation and in vitro evaluation of taste-masked oro-dispersible dosage form of diltiazem hydrochloride. Braz J Pharm Sci 47 (4): 907-916.
26. Haware RV, Chaudhari PD, Parakh SR, Bauer-Brandl A,. 2008. Development of a melting tablet containing Promethazine HCl against motion sickness. AAPS PharmSciTech 9 (3): 1006-1015.
27. Kawano Y, Ito A, Sasatsu M, Machida Y,. 2010. Preparation of orally disintegrating tablets with masking of unpleasant taste: Comparison with corrective-adding methods. J Pharm Soc Jpn 130 (1): 75-80.
28. Kondo K, Niwa T, Ozeki Y, Ando M, Danjo K,. 2011. Preparation and evaluation of orally rapidly disintegrating tablets containing taste-masked particles using one-step dry-coated tablets technology. Chem Pharm Bull 59 (10): 1214-1220.
29. Sheshala R, Khan N, Darwis Y,. 2011. Formulation and optimization of orally disintegrating tablets of sumatriptan succinate. Chem Pharm Bull 59 (8): 920-928.
30. Yan YD, Woo JS, Kang JH, Yong CS, Choi HG,. 2010. Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets. Biol Pharm Bull 33 (8): 1364-1370.
31. Aulton ME, Dyer AM, Khan KA,. 1994. The strength and compaction of millispheres-The design of a controlled-release drug-delivery system for ibuprofen the form of a tablet comprising compacted polymer-coated millispheres. Drug Dev Ind Pharm 20 (20): 3069-3104.
32. Debunne A, Vervaet C, Mangelings D, Remon JP,. 2004. Compaction of enteric-coated pellets: Influence of formulation and process parameters on tablet properties and in vivo evaluation. Eur J Pharm Sci 22 (4): 305-314.
33. Maganti L, Celik M,. 1994. Compaction studies on pellets 2: Coated pellets. Int J Pharm 103 (1): 55-67.
34. AlHusban F, Perrie Y, Mohammed AR,. 2011. Formulation of multiparticulate systems as lyophilised orally disintegrating tablets. Eur J Pharm Biopharm 79 (3): 627-634.
35. Sznitowska M, Placzek M, Klunder M,. 2005. The physical characteristics of lyophilized tablets containing a model drug in different chemical forms and concentrations. Acta Pol Pharm 62 (1): 25-29.
36. Stange U, Führling C, Gieseler H,. 2014. Taste masking of naproxen sodium granules by fluid-bed coating. Pharm Dev Technol 19 (2): 137-147.
37. Prajapati ST, Patel PB, Patel CN,. 2012. Formulation and evaluation of sublingual tablets containing Sumatriptan succinate. Int J Pharm Investig 2 (3): 162-168.
38. Brandes JL, Kudrow D, Stark SR, O'Carroll CP, Adelman JU, O'Donnell FJ, Alexander WJ, Spruill SE, Barrett PS, Lener SE,. 2007. Sumatriptan-naproxen for acute treatment of migraine-A randomized trial. JAMA 297 (13): 1443-1454.
39. Cady R, Banks J, Nett RB, Goldstein J, Bennett N, Turner IM, Ruoff GE, Landy SH, Farmer K, Juhász M, Tarrasch J, Runken MC,. 2011. Multi-center comparison of response to a single tablet of sumatriptan 85 mg and naproxen 500 mg vs usual therapy treating multiple migraine attacks as measured by the completeness of response survey. Headache 51 (6): 961-970.
40. Haberer LJ, Walls CM, Lener SE, Taylor DR, McDonald SA,. 2010. Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine. Headache 50 (3): 357-373.
41. Khoury CK, Couch JR,. 2010. Sumatriptan-naproxen fixed combination for acute treatment of migraine: A critical appraisal. Drug Des Devel Ther 4: 9-17.
42. Stange U, Führling C, Gieseler H,. 2013. Influence of non-water-soluble placebo pellets of different sizes on the characteristics of orally disintegrating tablets manufactured by freeze-drying. J Pharm Sci 102 (6): 1786-1799.
43. Patel SM, Doen T, Pikal MJ,. 2010. Determination of end point of primary drying in freeze-drying process control. AAPS PharmSciTech 11 (1): 73-84.
44. 2012. Monographs on dosage forms: Tablets, sub-category oral lyophilisates. Eur Pharmacopoeia (7.1): 1105-1109.
45. Jones RM,. 2003. Particle size analysis by laser diffraction: ISO 13320, standard operating procedures, and Mie theory. Am Lab 35 (1): 44-47.
46. Vargas-Ubera J, Sanchez-Escobar JJ, Aguilar JF, Gale DM,. 2007. Numerical study of particle-size distributions retrieved from angular light-scattering data using an evolution strategy with the Fraunhofer approximation. Appl Optics 46 (17): 3602-3610.
47. Bora D, Borude P, Bhise K,. 2008. Taste masking by spray-drying technique. AAPS PharmSciTech 9 (4): 1159-1164.
48. 2012. Taste masking formulations. Eudragit application guidelines. Darmstadt: Evonik Industries AG pp 1-26.
49. Davis SS, Hardy JG, Taylor MJ, Whalley DR, Wilson CG,. 1984. A comparative-study of the gastrointestinal transit of a pellet and tablet formulation. Int J Pharm 21 (2): 167-177.
50. Azarmi S, Roa W, Lobenberg R,. 2007. Current perspectives in dissolution testing of conventional and novel dosage forms. Int J Pharm 328 (1): 12-21.
51. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research 2008. Guidance for industry-Orally disintegrating tablets. http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/ucm070578.pdf. Accessed online: December 2013.
52. Dawson PJ, Hockley DJ,. 1992. Scanning electron microscopy of freeze-dried preparations: Relationship of morphology to freeze-drying parameters. Dev Biol Stand 74: 185-192.
53. Searles JA, Carpenter JF, Randolph TW,. 2001. The ice nucleation temperature determines the primary drying rate of lyophilization for samples frozen on a temperature-controlled shelf. J Pharm Sci 90 (7): 860-871.
54. Widehem P, Cochet N,. 2003. Pseudomonas syringae as an ice nucleator-Application to freeze-concentration. Process Biochem 39 (4): 405-410.
55. Pikal MJ,. 2002. Freeze drying. Encyclopedia of pharmaceutical technology. Third Edition. Swarbrick J. Editor. Informa Healthcare USA Inc., New York, USA., pp 1299-1326.
56. Dupont L, Dideberg O,. 1972. Crystal-structure of hydrochlorothiazide, C7H8CLN3O4S2. Acta Crystallogr B 28: 2340-2347.
57. Florence A, Johnston A, Fernandes P, Shankland K, Stevens HNE, Osmundsen S, Mullen AB,. 2005. Powder study of hydrochlorothiazide form II. Acta Crystallogr E 61: O2798-O2800.
58. Watanabe A, Ohnuma N,. 1994. Crystal morphological and habit investigations of crystalline drugs 3: Sulfamethizole, levodopa and phenobarbital. J Pharm Soc Jpn 114 (2): 80-88.
59. Beirowski J, Inghelbrecht S, Arien A, Gieseler H,. 2012. Freeze-drying of nanosuspensions, part 3: Investigation of factors compromising storage stability of highly concentrated drug nanosuspensions. J Pharm Sci 101 (1): 354-362.
60. Pikal MJ, Shah S, Senior D, Lang JE,. 1983. Physical-chemistry of freeze-drying-Measurement of sublimation rates for frozen aqueous-solutions by a microbalance technique. J Pharm Sci 72 (6): 635-650.
61. Patapoff TW, Overcashier DE,. 2002. The importance of freezing on lyophilization cycle development. BioPharm 15 (3): 16-21.
62. Corveleyn S, Remon JP,. 1999. Stability of freeze-dried tablets at different relative humidities. Drug Dev Ind Pharm 25 (9): 1005-1013.
63. Hancock BC, Zografi G,. 1997. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci 86 (1): 1-12.
64. Pearnchob N, Siepmann J, Bodmeier R,. 2003. Pharmaceutical applications of shellac: Moisture-protective and taste-masking coatings and extended-release matrix tablets. Drug Dev Ind Pharm 29 (8): 925-938.
65. Shirai Y, Sogo K, Yamamoto K, Kojima K, Fujioka H, Makita H, Nakamura Y,. 1993. A novel fine granule system for masking bitter taste. Biol Pharm Bull 16 (2): 172-177.
66. Abed KK, Hussein AA, Ghareeb MM, Abdulrasool AA,. 2010. Formulation and optimization of orodispersible tablets of diazepam. AAPS PharmSciTech 11 (1): 356-361.
67. AlHusban FA, El-Shaer AM, Jones RJ, Mohammed AR,. 2010. Recent patents and trends in orally disintegrating tablets. Recent Pat Drug Deliv Formul 4 (3): 178-197.
68. Johnson RE, Oldroyd ME, Ahmed SS, Gieseler H, Lewis LM,. 2009. Use of manometric temperature measurements (MTM) to characterize the freeze-drying behavior of amorphous protein formulations. J Pharm Sci 99 (6): 2863-2873.
69. Parker A, Rigby-Singleton S, Perkins M, Bates D, Le Roux D, Roberts CJ, Madden-Smith C, Lewis L, Teagarden DL, Johnson RE, Ahmed SS,. 2010. Determination of the influence of primary drying rates on the microscale structural attributes and physicochemical properties of protein containing lyophilized products. J Pharm Sci 99 (11): 4616-4629.
70. Pikal MJ, Shah S,. 1990. The collapse temperature in freeze-drying- Dependence on measurement methodology and rate of water removal from the glassy phase. Int J Pharm 62 (2-3): 165-186.
71. Hoy MR, Roche EJ,. 1996. Taste mask coatings for preparation of chewable pharmaceutical tablets. Mcneil-Ppc, Inc., Ft. Washington, PA, pp 239.
72. Zhang LJ, Liu L, Qian Y, Chen Y,. 2008. The effects of cryoprotectants on the freeze-drying of ibuprofen-loaded solid lipid microparticles (SLM). Eur J Pharm Biopharm 69 (2): 750-759.
73. Searles JA,. 2010. Freezing and annealing phenomena in lyophilization. In Freeze drying/lyophilization of pharmaceutical and biological products;, Rey L, May JC, Eds. New York: Informa Healthcare, pp 52-81.