New Technology of Thermoplastic Coating for Osmotic Pump Tablets: Study on in vivo Drug Release

Abstract

Aim The in vivo pharmacokinetics of thermoplastic-coated tablets prepared by a new technology of thermoplastic coating in Beagle dogs were studied, and the correlation between in vitro release and in vivo absorption was analyzed.

Methods The in vitro release profiles of metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets were investigated. The single-dose pharmacokinetic study of these tablets in Beagle dogs was performed, and the obtained results were separately compared with the data of conventional osmotic pump tablets reported in the literature.

Results Metformin hydrochloride thermoplastic-coated tablets and nifedipine thermoplastic-coated tablets displayed controlled drug-release characteristics and had a good in vivo–in vitro correlation in Beagle dogs, respectively. The literature-compared results further demonstrated that both thermoplastic-coated tablets had release characteristics of osmotic pump tablets in vivo.

Conclusion The thermoplastic-coated tablets could control drug release in vivo and it was further confirmed that the new thermoplastic coating technology could replace the spray coating of osmotic pump controlled-release tablets. This study provides a theoretical basis and practical support for the industrialization and clinical application of the new thermoplastic coating technology.

Keywords

thermoplastic coating - spray coating - metformin hydrochloride - nifedipine - osmotic pump tablet - pharmacokinetics - in vivo­–in vitro correlation

• References

• 1 Yuan CP, Hou HM, Qian MY. , et al. A new thermoplastic coating for osmotic pump tablets I. Development of preparation process. Carol J Pharm 2019; 50 (01) 48-58
• 2 Yuan CP, Hou HM, Ou SY. , et al. A new thermoplastic coating for osmotic pump tablets II. Evaluation of the coating membrane. Carol J Pharm 2019; 50 (02) 165-176
• 3 Yuan CP, Hou HM, Ou SY. , et al. New technology of thermoplastic coating for osmotic pump tablets: study on in vitro drug release. Pharm Fronts 2019; 1 (01) e1-e10
• 4 Chinese Pharmacopoeia Commission. The Pharmacopoeia of the People's Republic of China 2015 ed. Vol. IV. Beijing: China Medical Science Press; 2015: 368
• 5 Pan H, Jing H, Yang X. , et al. Synchronized and controlled release of metformin hydrochloride/glipizide from elementary osmotic delivery. Drug Dev Ind Pharm 2017; 43 (05) 780-788
• 6 Yin J, Feng Y, Lu J. , et al. Preparation of novel metformin hydrochloride osmotic pump controlled release tablets and study on pharmacokinetics in Beagle dogs. Zhongguo Xin Yao Zazhi 2012; 21 (20) 2429-2433
• 7 Pan X, Zhou S, Fu Q. , et al. Determination of nifedipine in dog plasma by high-performance liquid chromatography with tandem mass spectrometric detection. Biomed Chromatogr 2014; 28 (07) 1036-1040
• 8 Zhang DL, Yuan CP, Ren XH. , et al. Determination of nifedipine in human plasma by high performance liquid chromatography-tandem mass spectrometry. Zhongguo Yiyuan Yaoxue Zazhi 2012; 32 (03) 224-227
• 9 Choi YH, Kim SG, Lee MG. Dose-independent pharmacokinetics of metformin in rats: hepatic and gastrointestinal first-pass effects. J Pharm Sci 2006; 95 (11) 2543-2552
• 10 Qin C, He W, Zhu C. , et al. Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet. Int J Pharm 2014; 466 (1–2): 276-285
• 11 He W, Li Y, Zhang R. , et al. Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro/in vivo evaluation. Int J Pharm 2014; 476 (1–2): 223-231
• 12 Bode H, Brendel E, Ahr G. , et al. Investigation of nifedipine absorption in different regions of the human gastrointestinal (GI) tract after simultaneous administration of 13C- and 12C-nifedipine. Eur J Clin Pharmacol 1996; 50 (03) 195-201
• 13 He Q, Yang J. Development of digital gastrointestinal model and its application in absorption prediction of nifedipine sustained-release tablets. J Chin Pharm Univ 2012; 43 (01) 85-91
• 14 Grundy JS, Eliot LA, Kulmatycki KM. , et al. Grapefruit juice and orange juice effects on the bioavailability of nifedipine in the rat. Biopharm Drug Dispos 1998; 19 (03) 175-183
• 15 Pollak PT, Herman RJ, Feldman RD. Therapeutic differences in 24-h ambulatory blood pressures in patients switched between bioequivalent nifedipine osmotic systems with differing delivery technologies. Clin Transl Sci 2017; 10 (03) 217-224
• 16 Yan G, Li H, Zhang R. , et al. Preparation and evaluation of a sustained-release formulation of nifedipine HPMC tablets. Drug Dev Ind Pharm 2000; 26 (06) 681-686