Drug Research, Inhaltsverzeichnis

Drug Res (Stuttg) 2013; 63(08): 414-419
DOI: 10.1055/s-0033-1343429

Original Article

© Georg Thieme Verlag KG Stuttgart · New York

The Effect of Pore-Formers and Plasticizers on the Release Kinetic of Diltiazem Hydrochloride from the Controlled Porosity Osmotic Pumps

J. Shokri

¹Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran

³Dermatology & Dermopharmacy Research Team, Tabriz University of Medical Sciences, Tabriz, Iran

,

M. H. Zarrintan

²Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

,

S. Ghanbarzadeh

²Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

⁴Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran

,

Z. Arash

²Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

⁴Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran

,

A. Farahani

²Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

⁴Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran

,

K. Adibkia

¹Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran

²Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

› Institutsangaben

Abstract

Background:

The aim of this study was to design a controlled porosity osmotic pump (CPOP) tablet of diltiazem hydrochloride (DLTZ) to deliver the drug according to the zero order kinetic model over 24 h.

Method:

CPOPs were prepared by incorporating DLTZ in the tablet core followed by coating with cellulose acetate solution containing various types of pore-formers (PVP, PEG 2000, PEG 6000 and PEG 20000) and plasticizers (glycerol, castor oil and diethylphthalate). In vitro release study was conducted for the prepared formulations and the dissolution profiles were compared throughout four parameters, namely, D₂₄ _h (cumulative release in 24 h), t_L (lag time), RSQ_zero (squared correlation coefficient of zero order kinetic) and MPD_zero (mean percent deviation from zero order equation).

Results:

Scanning electron microscopy showed formation of the pores in the semi-permeable membrane after coming in contact with dissolution medium. All formulations released more than 76% of contained drug during 24 h.

Conclusion:

Drug release rate and lag time were found to be directly proportional to the type and concentration of pore-formers as well as hydrophilicity of plasticizers. Our findings indicated that by optimizing formulation variables, CPOP tablets obeying zero order drug release kinetic could be obtained.

Key words

Key words

controlled porosity osmotic pump - diltiazem hydrochloride - pore-former - plasticizer - zero order kinetic

References
1 Bridges JF, Woodley JF, Duncan R et al. Soluble N-(2-hydroxypropyl) methacrylamide copolymers as a potential oral, controlled-release, drug delivery system. I. Bioadhesion to the rat intestine in vitro. Int J Pharm 1988; 44: 213-223
2 Gruber P, Longer MA, Robinson JR. Some biological issues in oral, controlled drug delivery. Adv Drug Del Rev 1987; 1: 1-18
3 Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Rel 2000; 63: 235-259
4 Verma RK, Krishna DM, Garg S. Formulation aspects in the development of osmotically controlled oral drug delivery systems. J Control Rel 2002; 79: 7-27
5 Waterman KC, Goeken GS, Konagurthu S et al. Osmotic capsules: A universal oral, controlled-release drug delivery dosage form. J Control Rel 2011; 152: 264-269
6 Adibkia K, Javadzadeh Y, Dastmalchi S et al. Naproxen-eudragit^® RS100 nanoparticles: Preparation and physicochemical characterization. Colloids Surf B Biointerfaces 2011; 83: 155-159
7 Barzegar-Jalali M, Adibkia K, Valizadeh H et al. Kinetic analysis of drug release from nanoparticles. J Pharm Pharm Sci 2008; 11: 167-177
8 Cook RO, Pannu RK, Kellaway IW. Novel sustained release microspheres for pulmonary drug delivery. J Control Rel 2005; 104: 79-90
9 Jaspart S, Bertholet P, Piel G et al. Solid lipid microparticles as a sustained release system for pulmonary drug delivery. Eur J Pharm Biopharm 2007; 65: 47-56
10 Lee SB, Geroski DH, Prausnitz MR et al. Drug delivery through the sclera: effects of thickness, hydration, and sustained release systems. Exp Eye Res 2004; 78: 599-607
11 Nakamura K, Nara E, Akiyama Y. Development of an oral sustained release drug delivery system utilizing pH-dependent swelling of carboxyvinyl polymer. J Control Rel 2006; 111: 309-315
12 Haslam JL, Merfeld AE, Rork GS. Surface wetting effects in the lipid osmotic pump. Int J Pharm 1989; 56: 227-233
13 Liu L, Che B. Preparation of monolithic osmotic pump system by coating the indented core tablet. Eur J Pharm Biopharm 2006; 64: 180-184
14 Liu L, Wang X. Solubility-modulated monolithic osmotic pump tablet for atenolol delivery. Eur J Pharm Biopharm 2008; 68: 298-302
15 Liu L, Xu X. Preparation of bilayer-core osmotic pump tablet by coating the indented core tablet. Int J Pharm 2008; 352: 225-230
16 Malaterre V, Ogorka J, Loggia N et al. Approach to design push–pull osmotic pumps. Int J Pharm 2009; 376: 56-62
17 Shokri J, Hanaee J, Adibkia K et al. Formulation of Nifedipine osmotic pump and evaluation of drug release from prepared formulations. Pharm Sci 2003; 2: 75-85
18 Barzegar-jalali M, Siahi-Shadbad MR, Barzegar-jalali A et al. Design and evaluation of delayed-release osmotic capsule of acetaminophen. Iran J Pharm Sci 2006; 2: 65-72
19 Herrlich S, Spieth S, Messner S et al. Osmotic micropumps for drug delivery. Adv Drug Del Rev 2012; 64: 1617-1627
20 Makhija SN, Vavia PR. Controlled porosity osmotic pump-based controlled release systems of pseudoephedrine: I. Cellulose acetate as a semipermeable membrane. J Control Rel 2003; 89: 5-18
21 Malaterre V, Ogorka J, Loggia N et al. Oral osmotically driven systems: 30 years of development and clinical use. Eur J Pharm Biopharm 2009; 73: 311-323
22 Okimoto K, Tokunaga Y, Ibuki R et al. Applicability of (SBE)7m-β-CD in controlled-porosity osmotic pump tablets (OPTs). Int J Pharm 2004; 286: 81-88
23 Xu WJ, Li N, Gao Ck. Preparation of controlled porosity osmotic pump tablets for salvianolic acid and optimization of the formulation using an artificial neural network method. Acta Pharmaceutica Sinica B 2011; 1: 64-70
24 Prabakaran D, Singh P, Kanaujia P et al. Modified push-pull osmotic system for simultaneous delivery of theophylline and salbutamol: development and in vitro characterization. Int J Pharm 2004; 284: 95-108
25 Zentner GM, Rork GS, Himmelstein KJ. The controlled porosity osmotic pump. J Control Rel 1985; 1: 269-282
26 Zhang Zh, Dong Hy, Peng B et al. Design of an expert system for the development and formulation of push–pull osmotic pump tablets containing poorly water-soluble drugs. Int J Pharm 2011; 410: 41-47
27 Junyaprasert VB, Manwiwattanakul G. Release profile comparison and stability of diltiazem-resin microcapsules in sustained release suspensions. Int J Pharm 2008; 352: 81-91
28 Klinke WP, Juneau M, Grace M et al. Usefulness of sustained-release diltiazem for stable angina pectoris. Am J Cardiol 1989; 64: 1249-1252
29 Levis SR, Deasy PB. Use of coated microtubular halloysite for the sustained release of diltiazem hydrochloride and propranolol hydrochloride. Int J Pharm 2003; 253: 145-157
30 Uekama K, Horikawa T, Horiuchi Y et al. In vitro and in vivo evaluation of delayed-release behavior of diltiazem from its O-carboxymethyl-O-ethyl-β-cyclodextrin complex. J Control Rel 1993; 25: 99-106
31 Wilding IR, Hardy JG, Maccari M et al. Scintigraphic and pharmacokinetic assessment of a multiparticulate sustained release formulation of diltiazem. Int J Pharm 1991; 76: 133-143
32 Zentner GM, McClelland GA, Sutton SC. Controlled porosity solubility- and resin-modulated osmotic drug delivery systems for release of diltiazem hydrochloride. J Control Rel 1991; 16: 237-243
33 Glasser SP, Neutel JM, Gana TJ et al. Efficacy and safety of a once daily graded-release diltiazem formulation in essential hypertension. Am J Hypertens 2003; 16: 51-58
34 Toti US, Aminabhavi TM. Modified guar gum matrix tablet for controlled release of diltiazem hydrochloride. J Control Rel 2004; 95: 567-577
35 Felicetta JV, Serfer HM, Cutler NR et al. A dose-response trial of once-daily diltiazem. Am Heart J 1992; 123 (4, Part 1) 1022-1026
36 Cataldi M. Diltiazem. xPharm: The Comprehensive Pharmacology Reference. 2009; 1-32
37 Chaudhary A, Tiwari N, Jain V et al. Microporous bilayer osmotic tablet for colon-specific delivery. Eur J Pharm Biopharm 2011; 78: 134-140
38 Okimoto K, Ohike A, Ibuki R et al. Factors affecting membrane-controlled drug release for an osmotic pump tablet (OPT) utilizing (SBE)7m-β-CD as both a solubilizer and osmotic agent. J Control Rel 1999; 60: 311-319
39 Okimoto K, Rajewski RA, Stella VJ. Release of testosterone from an osmotic pump tablet utilizing (SBE)7m-β-cyclodextrin as both a solubilizing and an osmotic pump agent. J Control Rel 1999; 58: 29-38
40 Philip AK, Pathak K, Shakya P. Asymmetric membrane in membrane capsules: A means for achieving delayed and osmotic flow of cefadroxil. Eur J Pharm Biopharm 2008; 69: 658-666
41 Verma RK, Kaushal AM, Garg S. Development and evaluation of extended release formulations of isosorbide mononitrate based on osmotic technology. Int J Pharm 2003; 263: 9-24
42 Nokhodchi A, Momin MN, Shokri J et al. Factors affecting the release of nifedipine from a swellable elementary osmotic pump. Drug Deliv 2008; 15: 43-48
43 Shokri J, Ahmadi P, Rashidi P et al. Swellable elementary osmotic pump (SEOP): An effective device for delivery of poorly water-soluble drugs. Eur J Pharm Biopharm 2008; 68: 289-297
44 Roy A, Ghosh A, Datta S et al. Effects of plasticizers and surfactants on the film forming properties of hydroxypropyl methylcellulose for the coating of diclofenac sodium tablets. Saudi Pharm J 2009; 17: 233-241
45 Chakrabarty B, Ghoshal AK, Purkait MK. Effect of molecular weight of PEG on membrane morphology and transport properties. J Membr Sci 2008; 309: 209-221
46 Barzegar-Jalali M, Valizadeh H, Siahi-Shadbad MR et al. Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide). Powder Technol 2010; 197: 150-158