Development of novel bepotastine salicylate salt bioequivalent to the commercial bepotastine besilate in beagle dogs

Drug Development and Industrial Pharmacy

Volumn 39, Issue 6, 2013, Pages 901-908

  Cho, Kwan Hyung ^a,b   Choi, Han Gon ^a,c  

^a Yeungnam University   (South Korea)

^b Inje University   (South Korea)

^c Hanyang University   (South Korea)

Author keywords

Bepotastine salicylate; Bioavailability; Bioequivalence; Solubility; Stability

Indexed keywords

BEPOTASTINE; BEPOTASTINE SALICYLATE; MANNITOL; MICROCRYSTALLINE CELLULOSE; POVIDONE; SALICYLIC ACID; SODIUM CHLORIDE; STARCH GLYCOLATE SODIUM; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; DOG; DRUG BIOAVAILABILITY; DRUG DOSAGE FORM; DRUG GRANULATION; DRUG MARKETING; DRUG SOLUBILITY; LOADING DRUG DOSE; MALE; MELTING POINT; NONHUMAN; PH; PHYSICAL CHEMISTRY; TABLET; WETTABILITY;

ANIMALS; CROSS-OVER STUDIES; DOGS; DRUG DISCOVERY; MALE; PIPERIDINES; PYRIDINES; SALICYLIC ACID; THERAPEUTIC EQUIVALENCY;

EID: 84877067532     PISSN: 03639045     EISSN: 15205762     Source Type: Journal    
DOI: 10.3109/03639045.2012.717295     Document Type: Article

References (28)

1. Lyseng-Williamson KA. (2010). Oral bepotastine: in allergic disorders. Drugs, 70:1579-1591.
2. Williams JI, Gow JA, Klier SM, McCue SL, Salapatek AM, McNamara TR. (2010). Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate. Curr Med Res Opin, 26:2329-2338.
3. Williams JI, Kennedy KS, Gow JA, Torkildsen GL, Abelson MB, Gomes PJ et al.; Bepotastine Besilate Ophthalmic Solutions Study Group. (2011). Prolonged effectiveness of bepotastine besilate ophthalmic solution for the treatment of ocular symptoms of allergic conjunctivitis. J Ocul Pharmacol Ther, 27:385-393.
4. Otsuka M, Tanabe H. (2012). Stability test for amorphous materials in humidity controlled 96-well plates by near-infrared spectroscopy. Drug Dev Ind Pharm, 38:380-385.
5. Loeser E, Sutton P, Skorodinsky A, Lin M, Yowell G. (2012). Chemical interactions between an active pharmaceutical ingredient and its counterion in a tromethamine salt under forced degradation conditions. Drug Dev Ind Pharm, 38:357-364.
6. Loeser E, Sutton P, Skorodinsky A, Lin M, Yowell G. (2012). Chemical interactions between an active pharmaceutical ingredient and its counterion in a tromethamine salt under forced degradation conditions. Drug Dev Ind Pharm, 38:357-364.
7. Food and Drug Administration (FDA). (2000). FDA guidance for industry on bioavailability and bioequivalence studies for orally administered drug products. Silver Spring, MD: U.S. Food and Drug Administration.
8. Society of Toxicology (SOT). (2008). Guiding principles in the use of animals in toxicology. www.toxicology.org/AI/FA/ guidingprinciples.pdf
9. Kim YI, Kim KS, Suh KH, Shanmugam S, Woo JS, Yong CS et al. (2011). New clopidogrel napadisilate salt and its solid dispersion with improved stability and bioequivalence to the commercial clopidogrel bisulphate salt in beagle dogs. Int J Pharm, 415:129-139.
10. Park YJ, Xuan JJ, Oh DH, Balakrishnan P, Yang HJ, Yeo WH et al. (2010). Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability. Arch Pharm Res, 33:1217-1225.
11. Joe JH, Lee WM, Park YJ, Joe KH, Oh DH, Seo YG et al. (2010). Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. Int J Pharm, 395:161-166.
12. Kim BH, Chung JY, Kim JR, Lim KS, Lim HS, Yu KS, Jang IJ, Shin SG. (2007). Pharmacokinetic characteristics of bepotastine besilate in healthy subjects. Kor J Clin Pharmacol Ther, 15:37-45.
13. Amighi K, Timmermans J, Puigdevall J, Baltes E, Moës AJ. (1998). Peroral sustained-release film-coated pellets as a means to overcome physicochemical and biological drug-related problems. I. In vitro development and evaluation. Drug Dev Ind Pharm, 24:509-515.
14. Newa M, Bhandari KH, Li DX, Kwon TH, Kim JA, Yoo BK et al. (2007). Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188. Int J Pharm, 343:228-237.
15. Li DX, Oh YK, Lim SJ, Kim JO, Yang HJ, Sung JH et al. (2008). Novel gelatin microcapsule with bioavailability enhancement of ibuprofen using spray-drying technique. Int J Pharm, 355:277-284.
16. Oh DH, Park YJ, Kang JH, Yong CS, Choi HG. (2011). Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change. Drug Deliv, 18:46-53.
17. Cho KH, Choi YK, Kang JH, Choi HG, Yong CS, Park YJ. (2010). Development of a novel combination tablet containing trimebutine maleate and mosapride citrate for the treatment of functional dyspepsia. Int J Pharm, 400:145-152.
18. Lim HT, Balakrishnan P, Oh DH, Joe KH, Kim YR, Hwang DH et al. (2010). Development of novel sibutramine base-loaded solid dispersion with gelatin and HPMC: physicochemical characterization and pharmacokinetics in beagle dogs. Int J Pharm, 397:225-230.
19. Yan YD, Kim DH, Sung JH, Yong CS, Choi HG. (2010). Enhanced oral bioavailability of docetaxel in rats by four consecutive days of pre-treatment with curcumin. Int J Pharm, 399:116-120.
20. Sigfridsson K, Lundqvist A, Strimfors M. (2011). Co-administration of a nanosuspension of a poorly soluble basic compound and a solution of a proton pump inhibitor - the importance of gastrointestinal pH and solubility for the in vivo exposure. Drug Dev Ind Pharm, 37:1036-1042.
21. Medendorp J, Donovan B, Pennington J. (2010). Development of a highthroughput UHPLC-MS-based content uniformity method as a tool for assessing dry powder inhalers. Drug Dev Ind Pharm, 36:762-772.
22. Kanaujia P, Lau G, Ng WK, Widjaja E, Schreyer M, Hanefeld A et al. (2011). Investigating the effect of moisture protection on solidstate stability and dissolution of fenofibrate and ketoconazole solid dispersions using PXRD, HSDSC and Raman microscopy. Drug Dev Ind Pharm, 37:1026-1035.
23. Gould PL. (1986). Salt selection for basic drugs. Int J Pharm, 33:201-217.
24. David SE, Timmins P, Conway BR. (2012). Impact of the counterion on the solubility and physicochemical properties of salts of carboxylic acid drugs. Drug Dev Ind Pharm, 38:93-103.
25. Lee T, Wang YW. (2009). Initial salt screening procedures for manufacturing ibuprofen. Drug Dev Ind Pharm, 35:555-567.
26. Amidon GL, Lennernäs H, Shah VP, Crison Jr. (1995). A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res, 12:413-420.
27. Greenlees KJ. (2003). Animal drug human food safety toxicology and antimicrobial resistance - the square peg. Int J Toxicol, 22:131-134.
28. Kroes R, Kozianowski G. (2002). Threshold of toxicological concern (TTC) in food safety assessment. Toxicol Lett, 127:43-46.