用于脉冲药物释放的锌交联异羟肟酸海藻酸盐
Zinc cross-linked hydroxamated alginates for pulsed drug release.
作者信息
Raut Neha S, Deshmukh Prasad R, Umekar Milind J, Kotagale Nandkishor R
机构信息
Department of Pharmaceutics, Smt. Kishoritai Bhoyar College of Pharmacy, New Kamptee, Nagpur, Maharashtra, India.
出版信息
Int J Pharm Investig. 2013 Oct;3(4):194-202. doi: 10.4103/2230-973X.121292.
INTRODUCTION
Alginates can be tailored chemically to improve solubility, physicochemical, and biological properties and its complexation with metal ion is useful for controlling the drug release.
MATERIALS AND METHODS
Synthesized N,O-dimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were subsequently complexed with zinc to form beads. Hydroxamation of sodium alginate was confirmed by Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC).
RESULTS
The synthesized polymeric material exhibited reduced aqueous, HCl and NaOH solubility. The hydroxamated derivatives demonstrated pulsed release where change in pH of the dissolution medium stimulated the atenolol release.
CONCLUSION
Atenolol loaded Zn cross-linked polymeric beads demonstrated the sustained the plasma drug levels with increased half-life. Although the synthesized derivatives greatly altered the aqueous solubility of sodium alginate, no significant differences in in vitro and in vivo atenolol release behavior amongst the N,O-dimethyl, N-methyl, or N-Benzyl hydroxylamine derivatives of sodium alginate were observed.
引言
海藻酸盐可通过化学方法进行定制,以改善其溶解性、物理化学性质和生物学性质,并且其与金属离子的络合作用有助于控制药物释放。
材料与方法
合成海藻酸钠的N,O - 二甲基、N - 甲基或N - 苄基羟胺衍生物,随后与锌络合形成珠子。通过傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)确认海藻酸钠的羟肟化反应。
结果
合成的聚合材料在水、盐酸和氢氧化钠中的溶解度降低。羟肟化衍生物表现出脉冲释放,其中溶出介质pH值的变化刺激了阿替洛尔的释放。
结论
载有阿替洛尔的锌交联聚合物珠子显示出能维持血浆药物水平并延长半衰期。虽然合成衍生物极大地改变了海藻酸钠的水溶性,但在海藻酸钠的N,O - 二甲基、N - 甲基或N - 苄基羟胺衍生物之间,未观察到阿替洛尔体外和体内释放行为的显著差异。
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