Preparation and evaluation of enteric-coated delayed-release pellets of duloxetine hydrochloride using a fluidized bed coater
详细信息 查看全文
- 作者：Yong-Il Kim ; Roshan Pradhan ; Bijay K. Paudel…
- 关键词：Duloxetine hydrochloride ; Delayed ; release ; Enteric coated ; Pellet ; Pharmacokinetics
- 刊名：Archives of Pharmacal Research
- 出版年：2015
- 出版时间：December 2015
- 年：2015
- 卷：38
- 期：12
- 页码：2163-2171
- 全文大小：649 KB
- 参考文献：Abdul, S., A.V. Chandewar, and S.B. Jaiswal. 2010. A flexible technology for modified-release drugs: Multiple-unit pellet system (MUPS). Journal of Controlled Release 147: 2-6.CrossRef PubMed
Bymaster, F.P., L.J. Dreshfield-Ahmad, P.G. Threlkeld, J.L. Shaw, L. Thompson, D.L. Nelson, S.K. Hemrick-Luecke, and D.T. Wong. 2001. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology 25: 871-80.CrossRef PubMed
Cao, Q.R., J.S. Choi, Y. Liu, W.J. Xu, M. Yang, B.J. Lee, and J.H. Cui. 2013. A formulation approach for development of HPMC-based sustained release tablets for tolterodine tartrate with a low release variation. Drug Development and Industrial Pharmacy 39: 1720-730.CrossRef PubMed
Chatlapalli, R., and B.D. Rohera. 1998. Physical characterization of HPMC and HEC and investigation of their use as pelletization aids. International Journal of Pharmaceutics 161: 179-93.CrossRef
Choi, H., Y. Oh, and C. Kim. 1998. In situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability. International Journal of Pharmaceutics 165: 23-2.CrossRef
Costa, P., J.M. Sousa Lobo, M.C. Gohel, and M.K. Panchal. 2001. Modeling and comparison of dissolution profiles. European Journal of Pharmaceutical Sciences 13: 123-33.CrossRef PubMed
Costa, P., and J.M. Sousa Lobo. 2001. Influence of dissolution medium agitation on release profiles of sustained-release tablets. Drug Development and Industrial Pharmacy 27: 811-17.CrossRef
Fishbain, D.A., J. Hall, A.L. Meyers, J. Gonzales, and C. Mallinckrodt. 2008. Does pain mediate the pain interference with sleep problem in chronic pain? Findings from the studies for management of diabetic peripheral neuropathic pain with duloxetine. Journal of Pain and Symptom Management 36: 639-47.CrossRef PubMed
Frohoff-Hulsmann, M.A., B.C. Lippold, and J.W. McGinity. 1999. Aqueous ethyl cellulose dispersion containing plasticizers of different water solubility and hydroxy propyl methyl-cellulose as coating material for diffusion pellets II: properties of sprayed films. European Journal of Pharmaceutics and Biopharmaceutics 48: 67-5.CrossRef PubMed
Gibaldi, M., and D. Perrier. 1982. Pharmacokinetics, 2nd ed. New York: Marcel Dekker.
Goldstein, D.J., Y. Lu, M.J. Detke, C. Wiltse, C. Mallinckrodt, and M.A. Demitrack. 2004. Duloxetine in the treatment of depression: A double-blind placebo-controlled comparison with paroxetine. Journal of Clinical Psychopharmacology 24: 389-99.CrossRef PubMed
Goyanes, A., and R. Martinez-Pacheco. 2013. New co-processed MCC-based excipient for fast release of low solubility drugs from pellets prepared by extrusion-spheronization. Drug Development and Industrial Pharmacy (Early online:1-).
Hausner, H.H. 1967. Friction conditions in a mass of metal powder. International Journal of Powder Metallurgy 3: 7-3.
International Conference on Harmonization (ICH Q2A, Q2B), 1995. Guidelines on validation of analytical procedures.
Jansen, P.J., P.L. Oren, C.A. Kemp, S.R. Maple, and S.W. Beartschi. 1998. Characterization of impurities formed by interaction of duloxetine HCl with enteric polymers hydroxypropyl methylcellulose acetate duccinate and hydroxypropyl methylcellulose phthalate. Journal of Pharmaceutical Sciences 87: 81-5.CrossRef PubMed
Korakianiti, E.S., D.M. Rekkas, P.P. Dallas, and N.H. Choulis. 2000. Optimization of the pelletization process in a fluid- bed rotor granulator using experimental design. AAPS Pharm SciTech 1: 71-5.CrossRef
Lecomte, F., J. Siepmann, M. Walther, R.J. MacRae, and R. Bodmeier. 2004. Polymer blends used for the coating of multiparticulates: Comparison of aqueous and organic coating techniques. Pharmaceutical Research 21: 882-90.CrossRef PubMed
Mastan, S., T.B. Latha, and S. Ajay. 2011. The basic regulatory considerations and prospects for conducting bioavailability/bioequivalence (BA/BE) studies—An overview. Comparative Effectiveness Research 1: 1-5.CrossRef
Mease, P.J., I.J. Russell, D.K. Kajdasz, C.G. Wiltse, M.J. Detke, M.M. Wohlreich, D.J. Walker, and A.S. Chappell. 2010. Long term safety, tolerability, and efficacy of duloxetine in the treatment of fibromyalgia. Seminars in Arthritis and Rheumatism 39: 454-64.CrossRef PubMed
Mohamed, F.A., M. Roberts, L. Seton, J.L. Ford, M. Levina, and A.R. Rajabi-Siahboomi. 2013. The influence of HPMC concentration on release of theophylline or hydrocortisone from extended release mini-tablets. Drug Development and Industrial Pharmacy 38: 1167-174.CrossRef
Robinson, D., and L. Cardozo. 2010. New drug treatments for urinary incontinence. Maturitas 65: 340-47.CrossRef PubMed
Sharma, A., M.J. Goldberg, and B.J. Cerimele. 2000. Pharmacokinetics and safety of duloxetine, a dual-serotonin and norepinephrine reuptake inhibitor. The Journal of - 作者单位：Yong-Il Kim (1) (2)
Roshan Pradhan (1)
Bijay K. Paudel (1)
Ju Yeon Choi (1)
Ho Taek Im (2) (3)
Jong Oh Kim (1)
1. College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan, 712-749, Republic of Korea
2. Pharm. R&D Institute, Hanmi Pharm. Co., Ltd., Hwasung, 445-913, Republic of Korea
3. School of Pharmacy, Sungkyunkwan University, Jangan-gu, Suwon, 440-746, Gyeonggi-do, Republic of Korea - 刊物主题：Pharmacy; Pharmacology/Toxicology;
- 出版者：Springer Netherlands
- ISSN：1976-3786
文摘
In this study, the enteric-coated delayed-release pellets of duloxetine hydrochloride (DLX) were formulated using a fluidized bed coater. Three separate layers, the drug layer, the barrier layer, and the enteric layer, were coated onto inert core pellets. Among the three formulations (F1–F3), the dissolution profiles of formulation F2 were most similar to those of the marketed product, with similarity and difference factors of 83.99 and 3.77, respectively. In addition, pharmacokinetic parameters of AUC, Cmax, Tmax, t1/2, Kel, and MRT of DLX for the developed formulation (F2) did not differ significantly from those for the marketed product in beagle dogs, suggesting that they were bioequivalent. Our results demonstrated that the in vitro dissolution data resembled the in vivo performance of the drug. Therefore, this study has a positive scope for further scale up and development of the formulation for achievement of the generic product. Keywords Duloxetine hydrochloride Delayed-release Enteric coated Pellet Pharmacokinetics