Saleem M A, Bala Sumanji, Aeajaz A
Luqman College of Pharmacy, Behind P and T Quarters, Old Jewargi Road, Gulbarga - 585 102, India.
Indian J Pharm Sci. 2010 Nov;72(6):710-8. doi: 10.4103/0250-474X.84579.
The ability of β-cyclodextrin, hydroxypropyl-β-cyclodextrin, polyvinyl pyrrolidone and urea to influence the percutaneous absorption of meloxicam through isolated rat skin was evaluated. Carrier complex were prepared by kneading method in 1:1 and 1:2 in molar ratios for β-cyclodextrin and hydroxypropyl-β-cyclodextrin and in 1:1, 1:3 and 1:5 in weight ratios for polyvinyl pyrrolidone and urea. The complexes were characterized by IR, DSC and evaluated for solubility, dissolution and skin permeability. The solubility, dissolution and permeability of meloxicam were enhanced by using the carriers. The influence of cyclodextrins, polyvinyl pyrrolidone and urea on in vitro permeation of meloxicam through rat skin was investigated by incorporation of prepared carrier complex in 1% carbopol gel. The prepared gel was evaluated for drug content, pH and viscosity and in vitro permeation. All the percutaneous parameters like flux (Jss), amount permeated (Q(6)), diffusivity (D), permeability coefficient (K(p)), partition coefficient (K) and release rate constant (k) were calculated statistically. In vitro permeation study showed the trend that the penetration flux and enhancement factor increases with increasing concentration of β-cyclodextrin and hydroxypropyl-β-cyclodextrin and then decrease dramatically in case of hydroxypropyl-β-cyclodextrin gel formulation with the increase to 1:2 ratio. Similar changes in pattern of permeation were also observed with polyvinyl pyrrolidone and urea carrier complex. These findings concluded that the carriers cyclodextrins, polyvinyl pyrrolidone and urea could be used as transdermal permeation enhancer in topical preparation of meloxicam.
评估了β-环糊精、羟丙基-β-环糊精、聚乙烯吡咯烷酮和尿素对美洛昔康经离体大鼠皮肤的透皮吸收的影响。通过捏合法制备载体复合物,β-环糊精和羟丙基-β-环糊精的摩尔比为1:1和1:2,聚乙烯吡咯烷酮和尿素的重量比为1:1、1:3和1:5。通过红外光谱(IR)、差示扫描量热法(DSC)对复合物进行表征,并评估其溶解度、溶出度和皮肤渗透性。使用这些载体可提高美洛昔康的溶解度、溶出度和渗透性。通过将制备的载体复合物加入1%卡波姆凝胶中,研究了环糊精、聚乙烯吡咯烷酮和尿素对美洛昔康经大鼠皮肤体外渗透的影响。对制备的凝胶进行药物含量、pH值和粘度以及体外渗透评估。对所有透皮参数如通量(Jss)、渗透量(Q(6))、扩散系数(D)、渗透系数(K(p))、分配系数(K)和释放速率常数(k)进行统计学计算。体外渗透研究表明,随着β-环糊精和羟丙基-β-环糊精浓度的增加,渗透通量和增强因子呈上升趋势,然后在羟丙基-β-环糊精凝胶制剂比例增加到1:2时急剧下降。在聚乙烯吡咯烷酮和尿素载体复合物中也观察到类似的渗透模式变化。这些研究结果表明,载体环糊精、聚乙烯吡咯烷酮和尿素可作为美洛昔康局部制剂的透皮渗透促进剂使用。