Production of of Ibuprofen Pellets Containing High Amount of Rate Retarding Eudragit RL Using PEG400 and Investigation of Their Physicomechanical Properties | ||
| Iranian Journal of Basic Medical Sciences | ||
| مقاله 11، دوره 14، شماره 4، مهر 2011، صفحه 383-390 اصل مقاله (606.01 K) | ||
| نوع مقاله: Original Article | ||
| شناسه دیجیتال (DOI): 10.22038/ijbms.2011.5028 | ||
| نویسندگان | ||
| Fatemeh Sadeghi* 1؛ Hasan Hijazi2؛ Hadi Afrasiabi Garekani1 | ||
| 1Pharmaceutical Research Center and School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran | ||
| 2School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran | ||
| چکیده | ||
| Objective(s) The aim of this study was to investigate the possibility of production of ibuprofen pellets with high amount of rate retarding polymer by aid of PEG400 as plasticizer. Materials and Methods Polyethylene glycol (PEG400) in concentrations of 1, 3 or 5% w/w with respect to Eudragit RL was used in production of pellets containing 60% ibuprofen and 40% excipient (2% polyvinylpyrrolidone (PVP), 7.6 or 0% microcrystalline cellulose (MCC) and 30.4 or 38% Eudragit RL). Physicomechanical and release properties of pellets were evaluated. Results In presence of PEG400, formulations containing 30.4% Eudragit RL and 7.6% MCC could easily form pellets. In formulations without any MCC pellets were obtained only in presence of 3 or 5% PEG400. Pellets containing MCC with 0 or 1% PEG400 showed brittle properties but those with 3% or 5% PEG400 showed plastic nature under pressure. Elastic modulus dramatically decreased with increasing PEG400 indicating softening of pellets. This was due to shift of Eudragit structure from glassy to rubbery state which was supported by DSC studies. Mean dissolution time (MDT) increased with addition of 1 or 3% PEG400 but this was not the case for pellets with 5% PEG400. Conclusion Overall PEG400 is a potential plasticizer in production of pellets based on Eudragit RL and ibuprofen. The ease in process of extrusion-spheronization, increasing the mean dissolution time and change in mechanical properties of pellets from brittle to plastic behavior were advantages of using PEG400. Changes in mechanical properties of pellets are important when pellets are intended to be compressed as tablets. | ||
| کلیدواژهها | ||
| Eudragit RL؛ Extrusion-spheronization؛ Ibuprofen؛ Microcrystalline cellulose؛ Pellets؛ PEG400 | ||
| مراجع | ||
|
1.Tho I, Arne Sande S, Kleinbudde P. Pectinic acid a novel excipiant for production of pellets by extrusion- spheronization: preliminary studies. Eur J Pharm Biopharm 2002; 54:95-99.
2.Vervaet C, Baert L, Remon JP. Extrusion-spheronization A literature review. Int J Pharm 1995; 116:131-146.
3.Abbaspour MR, Sadeghi F, Afrasiabi Garekani H. Preperation and characterization of ibuprofen pellets based on Eudragit RS PO and RL PO or their combination. Int J Pharm 2005; 303:88-94.
4.Santos H, Veign F, Pina M, Podczeck F, Sousa J. Physical properties of chitosan pellets produced by extrusion-spheronization: influence of formulation variables. Int J Pharm 2002; 246:153-169.
5.Abbaspour MR, Sadeghi F, Afrasiabi Garekani H. Thermal treating as a tool to produce plastic pellets based on Eudragit RS PO and RL PO aimed for tableting. Eur J Pharm Biopharm 2007; 67:260-267.
6.Zelko R, Orban A, Suvegh K, Riedl Z, Racz I. Effect of plasticizer on the dynamic surface tension and the free volume of Eudragit systems. Int J Pharm 2002; 244:81-86.
7.Wang CC, Zhang G,Shah NH, Infeld MH, Malick AW, McGinity JW. Influence of plasticizers on the mechanical properties of pellets containing Eudragit RS 30D. Int J Pharm 1997; 152:153-163.
8.Zhu Y, Shah NH, Malick AW, Infeld MH, McGinity JW. Solid state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate. Int J Pharm 2002; 241:301-310.
9.Costa Fo, Sousa JJS, Pais AACC, Formosinho SJ. Comparison of dissolution profiles of ibuprofen pellets. J Control Rel 2003; 89:199-212.
10.Dukic-Ott A, Thommes M, Remon JP, Kleinebudde P, Vervaet C. Production of pellets via extrusion- spheronization without the incorporation of microcrystalline cellulose: A critical review. Eur J Pharm Biopharm 2009; 71:38-46.
11.Lustig C, Kaur H, Podczeck F, Newton JM. The influence of water content and drug solubility on the formulation of pellets by extrusion and spheronization. Eur J Pharm Sci 1999; 8:147-152.
12.Felton LA, McGinity W. Influence of plasticizers on the adhesive properties of an acrylic resin copolymer to hydrophilic and hydrophobic tablet compacts. Int J Pharm 1997; 154:167-178.
13.Fujimori J, Yoshihashi Y, Yonemochi E, Terada K. Application of Eudragit RS to thermo-sensitive drug delivery systems: II. Effect of temperature on drug permeability through membrane consisting of Eudragit RS/PEG400 blend polymers.J Control Release 2005; 102:49-57.
14.Fielden KE, Newton JM, Rowe RC. The influence of moisture content on spheronization of extudate processed by a ram extruder. Int J Pharm 1993; 97:79-92.
15.Sadeghi F, Afrasiabi Garekani H, Goli F. Tableting of Eudragit RS and propranolol hydrochloride solid dispersion: Effect of particle size, compaction force and plasticizer addition on drug release. Drug Dev Ind Pharm 2004; 30:759-766.
16.Sadeghi F, Afrasiabi Garekani H, Sadr A. Influence of polymer viscosity and plasticizer addition on ethylcellulose matrix characteristics prepared from solid dispersion system, S.T.P. J Pharm Sci 2003; 13:105-110. | ||
|
آمار تعداد مشاهده مقاله: 1,397 تعداد دریافت فایل اصل مقاله: 712 |
||