Bilayer Matrix Tablets for Prolonged Actions of Metformin Hydrochloride and Repaglinide

详细信息    查看全文

• 作者：Wei He (1)
  Shijing Huang (2)
  Chunyan Zhou (1)
  Lin Cao (1)
  Jing Yao (1)
  Jianping Zhou (1)
  Guangji Wang (1)
  Lifang Yin (1)
  
  1. State Key Laboratory of Natural Medicines ; School of Pharmacy ; China Pharmaceutical University ; Nanjing ; 210009 ; People鈥檚 Republic of China
  2. The Third People鈥檚 Hospital of Chengdu ; Chengdu ; 610031 ; People鈥檚 Republic of China
  
• 关键词：bilayer tablets ; metformin hydrochloride ; pharmacokinetics ; repaglinide ; sustained release
• 刊名：AAPS PharmSciTech
• 出版年：2015
• 出版时间：April 2015
• 年：2015
• 卷：16
• 期：2
• 页码：344-353
• 全文大小：1,164 KB
• 参考文献：1. Berardis, G, Dttorre, A, Graziano, G, Lucisano, G, Pellegrini, F, Cammarota, S (2013) The burden of hospitalization related to diabetes mellitus: a population-based study. Nutr Metab Cardiovasc 22: pp. 605-12 CrossRef
  2. Zuo, H, Shi, Z, Hussain, A (2014) Prevalence, trends and risk factors for the diabetes epidemic in China: a systematic review and meta-analysis. Diabetes Res Clin Pract 103: pp. 176-85 CrossRef
  3. Guariguata, L, Linnenkamp, U, Beagley, J, Whiting, DR, Cho, NH (2014) Global estimates of the prevalence of hyperglycaemia in pregnancy. Diabetes Res Clin Pract 103: pp. 176-85 CrossRef
  4. Tucker, GT, Casey, C, Phillips, PJ, Connor, H, Ward, JD, Woods, HF (1981) Metformin kinetics in healthy subjects and in patients with diabetes mellitus. Br J Clin Pharmacol 12: pp. 235-46
  5. Thomas, CR, Turner, SL, Jefferson, WH, Bailey, CJ (1998) Prevention of dexamethasone-induced insulin resistance by metformin. Biochem Pharmacol 56: pp. 1145-450 CrossRef
  6. Wolffenbuttel, BHR (1999) Repaglinide: a new compound for the treatment of patients with type 2 diabetes. Neth J Med 55: pp. 229-34 CrossRef
  7. Tosi, F, Muggeo, M, Brun, E, Spiazzi, G, Perobelli, L, Zanolin, E (2003) Combination treatment with metformin and glibenclamide versus single-drug therapies in type 2 diabetes mellitus: a randomized, double-blind, comparative study. Metabolism 52: pp. 862-7 CrossRef
  8. Dailey, GE (2003) Glyburide/metformin tablets: a new therapeutic option for the management of type 2 diabetes. Expert Opin Pharmaco 4: pp. 1417-30 CrossRef
  9. Scott, LJ (2012) Repaglinide: a review of its use in type 2 diabetes mellitus. Drugs 72: pp. 249-72 CrossRef
  10. Dhana lekshmi, UM, Poovi, G, Kishore, N, Reddy, PN (2010) In vitro characterization and in vivo toxicity study of repaglinide loaded poly (methyl methacrylate) nanoparticles. Int J Pharm 396: pp. 194-203 CrossRef
  11. Lalau, JD, Azzoug, ML, Kajbaf, F, Briet, C, Desailloud, R (2014) Metformin accumulation without hyperlactataemia and metformin-induced hyperlactataemia without metformin accumulation. Diabetes Metab 40: pp. 220-3 CrossRef
  12. Klinzing, G, Zavaliangos, A (2013) Understanding the effect of environmental history on bilayer tablet interfacial shear strength. Pharm Res 30: pp. 1300-10 CrossRef
  13. Abebe, A, Akseli, I, Sprockel, O, Kottala, N, Cuitino, AM (2014) Review of bilayer tablet technology. Int J Pharm 461: pp. 549-58 CrossRef
  14. Qin, C, He, W, Zhu, C, Wu, M, Jin, Z, Zhang, Q (2014) Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet. Int J Pharm 466: pp. 276-85 CrossRef
  15. Yin, LF, Huang, SJ, Zhu, CL, Zhang, SH, Zhang, Q, Chen, XJ (2012) In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier. Drug Dev Ind Pharm 38: pp. 1371-80 CrossRef
  16. Siepmann, J, Peppas, NA (2012) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev 64: pp. 163-74 CrossRef
  17. Wu, B, Deng, D, Lu, Y, Wu, W (2008) Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: II. Influencing variables, stability and pharmacokinetics in dogs. Eur J Pharm Biopharm 69: pp. 294-302 CrossRef
  18. Chambin, O, Champion, D, Debray, C, Rochat-Gonthier, MH, Meste, M, Pourcelot, Y (2004) Effects of different cellulose derivatives on drug release mechanism studied at a preformulation stage. J Control Release 95: pp. 101-8 CrossRef
  19. Grund, J, K枚rberr, M, Bodmeier, R (2013) Predictability of drug release from water-insoluble polymeric matrix tablets. Eur J Pharm Biopharm 85: pp. 650-5 CrossRef
  20. Rujivipat, S, Bodmeier, R (2010) Modified release from hydroxypropyl methylcellulose compression-coated tablets. Int J Pharm 402: pp. 72-7 CrossRef
  21. Quinten, T, Gonnissen, Y, Adriaens, E, Beer, TD, Cnudde, V, Masschaele, B (2009) Development of injection moulded matrix tablets based on mixtures of ethylcellulose and low-substituted hydroxypropylcellulose. Eur J Pharm Sci 37: pp. 207-16 CrossRef
  22. Sotthivirat, S, Haslam, JL, Lee, PI, Rao, VM, Stella, VJ (2009) Release mechanisms of a sparingly water-soluble drug from controlled porosity-osmotic pump pellets using sulfobutylether-beta-cyclodextrin as both a solubilizing and osmotic agent. J Pharm Sci 98: pp. 1992-2000 CrossRef
  23. Palmer, D, Levina, M, Nokhodchi, A, Douroumis, D, Farrell, T, Rajabi-Siahboomi, A (2011) The influence of sodium carboxymethylcellulose on drug release from polyethylene oxide extended release matrices. AAPS PharmSciTech 12: pp. 862-71 CrossRef
  24. Conti, S, Maggi, L, Segale, L, Ochoa Machiste, E, Conte, U, Grenier, P (2007) Matrices containing NaCMC and HPMC 1. Dissolution performance characterization. Int J Pharm 333: pp. 136-42 CrossRef
  25. Maderuelo, C, Zarzuelo, A, Lanao, JM (2011) Critical factors in the release of drugs from sustained release hydrophilic matrices. J Control Release 154: pp. 2-19 CrossRef
  26. Vaidya, MP, Avachat, AM (2011) Investigation of the impact of insoluble diluents on the compression and release properties of matrix based sustained release tablets. Powder Technol 214: pp. 375-81 CrossRef
  27. Fuertes, I, Caraballo, I, Miranda, A, Milln, M (2010) Study of critical points of drugs with different solubilities in hydrophilic matrices. Int J Pharm 383: pp. 138-46 CrossRef
  28. Mandi, Z, Gabelica, V (2006) Ionization, lipophilicity and solubility properties of repaglinide. J Pharm Biomed Anal 41: pp. 866-71 CrossRef
  29. American Chemical Society. 2014. https://scifinder.cas.org/scifinder/view/scifinder/scifinderExplore.jsf.
  30. Bettini, R, Catellani, PL, Santi, P, Massimo, G, Peppas, NA, Colombo, P (2001) Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate. J Control Release 70: pp. 383-91 CrossRef
  31. Vidon, N, Chaussade, S, Noel, M, Franchisseur, C, Huchet, B, Bernier, JJ (1988) Metformin in the digestive tract. Diabetes Res Clin Pract 4: pp. 223-9 CrossRef
  32. Nayak, AK, Pal, D, Santra, K (2014) Tamarind seed polysaccharide-gellan mucoadhesive beads for controlled release of metformin HCl. Carbohydr Polym 103: pp. 154-63 CrossRef
  33. Kortejrvi, H, Mikkola, J, Bckman, M, Antila, S, Marvola, M (2002) Development of level A, B and C in vitro鈥搃n vivo correlations for modified-release levosimendan capsules. Int J Pharm 241: pp. 87-95 CrossRef
  
• 刊物主题：Pharmacology/Toxicology; Biotechnology; Biochemistry, general; Pharmacy;
• 出版者：Springer US
• ISSN：1530-9932

文摘

A combination therapy of metformin hydrochloride (MH) and repaglinide (RG) achieves a perfect glycemic control; however, the combination formulation of immediate release must be taken several times a day, compromising the therapeutic benefits and causing inconveniences to the patients. Herein, a bilayer matrix tablet that aimed at continuously releasing both MH and RG over time was developed, in which the two drugs were formulated into two separated layers. The tablets were prepared by wet granulation method, and the optimized formulation was obtained by evaluating the factors that affected the drug release. The bilayer tablets simultaneously released the two drugs over 12 h; and a better in vivo performance with a steady plasma concentration, markedly lower C max, prolonged T max, and perfect absorption was obtained. Summarily, the bilayer matrix tablets sustained both MH and RG release over time, thereby prolonging the actions for diabetic therapy and producing better health outcomes.