Nande V S, Barabde U V, Morkhade D M, Joshi S B, Patil A T
Department of Pharmaceutical Sciences, Nagpur University Campus, Nagpur, 440 033 Maharashtra, India.
AAPS PharmSciTech. 2008;9(1):105-11. doi: 10.1208/s12249-007-9025-5. Epub 2008 Jan 16.
The purpose of the present study was to investigate the potential use of two PEGylated derivatives of rosin (PD) as sustained release film forming materials. The derivatives differed chemically by their acid numbers--PD-1 with 120.93 and PD-2 with 88.19. The derivative films were characterized for surface morphology, water uptake-weight loss, angle of contact, water vapor transmission rate, mechanical properties and permeability study. Dissolution of diclofenac sodium (DS) and propranolol hydrochloride (PHL) as model drugs was studied from coated pellets. The films of derivatives with and without plasticizers were smooth and continuous. PD-2 films developed greater numbers of pores when in contact with phosphate buffer pH 6.8. The low weight loss, low angles of contact and high water vapor transmission rate of PD-2 films were related to presence of higher concentration of PEG esters. Higher tensile strength and percent elongation of PD-2 films was due to greater degree of internal plasticization of the derivative. The permeability of films to model drugs propranolol hydrochloride and diclofenac sodium was inversely proportional to the film thickness and dibutyl phthalate concentration in them; the permeability being greatest in PD-2 films containing 10% PEG 200. Dissolution rate of propranolol hydrochloride was higher from the coated pellets. The dissolution data followed zero order, Baker-Lonsdale equation and Hixon-Crowell equation of release kinetics with high correlation coefficients. The mechanism of drug release from these coated systems however followed class II transport (n > 1.0). The derivatives investigated could successfully retard release of the model drugs and offers an alternative to the conventionally used polymers.
本研究的目的是探究两种松香聚乙二醇化衍生物(PD)作为缓释成膜材料的潜在用途。这两种衍生物在化学性质上因酸值不同而有所差异——PD - 1的酸值为120.93,PD - 2的酸值为88.19。对衍生物薄膜的表面形态、吸水失重、接触角、水蒸气透过率、机械性能和渗透性进行了表征。以双氯芬酸钠(DS)和盐酸普萘洛尔(PHL)为模型药物,研究了包衣微丸中药物的溶出情况。含和不含增塑剂的衍生物薄膜均光滑且连续。当与pH 6.8的磷酸盐缓冲液接触时,PD - 2薄膜形成了更多的孔隙。PD - 2薄膜的低失重、低接触角和高水蒸气透过率与较高浓度的PEG酯的存在有关。PD - 2薄膜较高的拉伸强度和伸长率是由于该衍生物更大程度的内增塑作用。薄膜对模型药物盐酸普萘洛尔和双氯芬酸钠的渗透性与薄膜厚度和其中邻苯二甲酸二丁酯浓度成反比;在含有10% PEG 200的PD - 2薄膜中渗透性最大。盐酸普萘洛尔从包衣微丸中的溶出速率较高。溶出数据符合零级、Baker - Lonsdale方程和Hixon - Crowell释放动力学方程,相关系数较高。然而,这些包衣体系的药物释放机制遵循II类转运(n > 1.0)。所研究的衍生物能够成功延缓模型药物的释放,并为传统使用的聚合物提供了一种替代选择。