Formulation Study and Evaluation of Matrix and Three-layer Tablet Sustained Drug Delivery Systems Based on Carbopols with Isosorbite Mononitrate
The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate.
- H. Ho-Wah, J. Robinson, and V. Lee. Design and fabrication of oral controlled release drug delivery systems. In J. Robinson, and V. Lee (eds.), Controlled Drug Delivery, Marcell Dekker Inc, New York, 1987, p. 373.
- U. Conte, and L. Maggi. Multi-layer tablets as drug delivery devices. Pharm. Techn. 2:18–25 (1998).
- N. Chidambram, W. Porter, K. Flood, and Y. Qiu. Formulation and characterization of new layered diffusional matrices for zero-order sustained release. J. Control. Release. 52:149–158 (1998). CrossRef
- M. Efentakis, and S. Politis. Comparative evaluation of various structures in polymer controlled drug delivery systems and the effect of their morphology and characteristics on drug release. Eur. Polym. J. 42:1183–1195 (2006). CrossRef
- L. Yang, and R. Fassihi. Accessibility of solid core tablet for dissolution in a asymmetric triple-layer matrix system. J. Pharm. Pharmcol. 55:1331–1337 (2003). CrossRef
- A. Shajahan, and S. Pondar. A flexible technology for modified release of drugs: multilayer tablets. J. Control. Release. 97:393–405 (2004).
- D. Alderman. A review of cellulose ethers in hydrophilic matrices for oral controlled release dosage forms. Int. J. Tech. Prod. Mfr. 5:1–9 (1984).
- P. Katikanemi, S. Upadrashta, S. Neau, and A. Mitra. Ethylcellulose matrix controlled release tablets of a water-soluble drug. Int. J. Pharm. 123:119–125 (1995). CrossRef
- B. F. Goodrich Bulletin. “Carbopol water soluble resins-controlled release tablets and capsules”. No 17 (1994).
- M. Meshali, G. El-Sayed, Y. El-Said, and H. Abd El-Aleem. Preparation and evaluation of theophylline sustained release tablets. Drug Dev. Ind. Pharm. 22:373–376 (1996). CrossRef
- A. Singla, M. Chawla, and A. Sigh. Potential applications of Carbomer in oral mucoadhesive controlled drug delivery systems: A review. Drug Dev. Ind. Pharm. 26:913–924 (2000). CrossRef
- M. Efentakis, A. Koutlis, and M. Vlachou. Development and evaluation of oral multiple unit and single unit hydrophilic controlled release systems. aapspharmscitech.org. 1(4) article 34 (2000).
- J. Waller. Optimal nitrate therapy with a once-daily sustained-release formulation of isosorbide mononitrate. J. Cardiovasc. Pharm. 34Suppl 2:S1–S7 (1999).
- D. Franz. Cardiovascular drugs. In A. Gennaro (ed.), Remington: The Science and Practice of Pharmacy, Mack, Pennsylvania, 1995, p. 954.
- K. Khan. The concept of dissolution efficiency. J. Pharm. Pharmacol. 27:48–49 (1975).
- R. Korsmeyer, R. Gurny, E. Doelker, P. Buri, and N. Peppas. Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. 15:25–359 (1983). CrossRef
- Formulation Study and Evaluation of Matrix and Three-layer Tablet Sustained Drug Delivery Systems Based on Carbopols with Isosorbite Mononitrate
Volume 9, Issue 3 , pp 917-923
- Cover Date
- Online ISSN
- Springer US
- Additional Links
- isosorbide mononitrate
- release kinetics
- sustained release
- three-layer tablets
- Industry Sectors