Indomethacin sustained release pellets prepared by extrusion-spheronization

被引:21
|
作者
Mahrous, G. M. [1 ]
Ibarhim, M. A. [2 ]
El-Badry, M. [1 ]
Al-Anazi, F. K. [1 ,2 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11451, Saudi Arabia
[2] King Saud Univ, Coll Pharm, Kayyali Chair Pharmaceut Ind, Riyadh 11451, Saudi Arabia
关键词
Indomethacin; Pellets; Extrusion-spheronization; Hydrophilic polymers; Kinetics; MICROCRYSTALLINE CELLULOSE; OPTIMIZATION; FORMULATIONS; BEHAVIOR; DRUGS;
D O I
10.1016/S1773-2247(10)50016-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Gastrointestinal side effects was interrupt essential therapy with indomethacin, a non-steroidal anti-inflammatory drug. Formulation of this drug into sustained release multiparticulate form may reduce some of these side (fleets by avoiding,g contact of drug crystals with gastrointestinal mucosa at high concentrations, as may happen with immediate release dosage,forms. Indomethacin (IM) sustained release pellets containing 5 or 10 % w/w oldie drug were prepared using an extrusion-spheronization technique. Different concentrations of hydrophilic polymers. polyethylene glycol 4000 (PEG 4000), hvdroxypropy/methylcellulose E5 LV premium (HPMC) and polyvinyl pyrrolidone (PVP K30). were mixed at different concentrations (5,10 and 20 %) with Avicel PH 101 to prepare the sustained release formulae. Moreover, a mixer torque rheometer was used to quantitatively determine the suitable moisture content ill the pastes before the extrusion process. The resulting pellets were characterized for content, particle size, shape and dissolution profile. The studies On the (fleet of the polymers used on Avicel rheological properties revealed that the magnitude of torque for the system was decreasing as the polymer concentration increased. The in vitro release of IM from the prepared Avicel pellets was found to be dependent upon the type and concentration of the added polymer. The rank order of IM release in the presence of the investigated polymers was as follows: PEG > HPMC > PVP. Furthermore, the magnitude of release rate from the pellet formulations was found to be dependent on the magnitude oldie peak torque of the pellet formating paste, which in turn depends on the type and (concentration of the added polymer. increasing IM loading from 5 to 10 % has led to an increase in dissolution rates. At least two of the prepared pellet formulations showed dissolution profiles similar to the commercial product Bonidon 75 SR capsules. in conclusion, the formulation of IM sustained release pellets successfully controlled the drug release which might he beneficial lowering the risk of side effects and improving patient convenience as all advantage of the Pellets as a drag defivery syslem.
引用
收藏
页码:119 / 125
页数:7
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