Formulation and in vitro Evaluation of pH-Sensitive Cross-linked Xanthan Gum-Grafted Acrylic Acid Copolymer for Controlled Delivery of Perindopril Erbumine (PE)

A novel xanthan gum-co-acrylic acid superabsorbent hydrogel composite was formulated by free radical polymerization reaction of acrylic acid on xanthan gum. Effect of variables like dynamic swelling ratio, equilibrium swelling ratio, drug loading and drug release was investigated. Swelling ratio increases with decrease in crosslinker concentration. Drug release studies were conducted in pH 7.4 and 0.1N HCl. In acidic environment, drug release was low whereas it was sustained release in alkaline. XG4 showed significant swelling and drug release up to 24?hr. Physicochemical evaluation also confirmed it was optimized formulation. Hence XG4-co-AA was optimized for once daily dose of Perindopril Erbumine.     

培哚普利单用和与格列齐特联用治疗糖尿病肾病的临床疗效评价

目的: 评价培哚普利(perindopril) 单用和与格列齐特联用对治疗Ⅱ型糖尿病(DM) 伴高血压合并糖尿病肾病 (DN) 病人的疗效及安全性。方法: 61 例病人, 男34 例, 女27 例。随机分为两组, 培哚普利组31 例, 培哚普利 4 mg, 1 次/d;格列齐特 80 mg, 2次/d 。硝苯地平组30 例, 硝苯地平缓释片 10 mg, 1次/d;格列齐特 80 mg, 2 次/d 。以治疗 3 mon 为统计界限。结果: 两组治疗前后比较, 收缩压、舒张压、空腹血糖(FPG) 、糖化血红蛋白 (GHb) 明显降低(P<0.05), 培哚普利组尿微量白蛋白(UMA) 显著下降(P<0.01), 硝苯地平组 UMA 无明显变化(P > 0.05) 。两组治疗后, 收缩压、舒张压、空腹血糖(PLG) 、糖化血红蛋白(GHb) 比较无显著性差异(P>0.05) 。培哚普利组尿微量蛋白(UMA) 较硝苯地平组明显下降(P<0.01) 。两组治疗前后及治疗后比较, WBC 、RBC 、PLT 、血清尿素、Cr 及 K⁺ 均无明显变化(P >0.05) 。结论: 培哚普利是治疗Ⅱ型DM 伴高血压合并 DN 保护肾功能安全有效的药物;培哚普利和格列齐特联合应用效果更佳。     

培哚普利叔丁胺盐的合成

以(2S,3aS,7aS)-八氢吲哚-2-羧酸和N-[(1S)-(1-乙氧羰基)-丁基]-(S)-丙氨酸为原料,经酯化、缩合、氢化3步反应合成培哚普利叔丁胺盐,总收率为46%。产物经IR、NMR和质谱进行了确认。对文献工艺条件进行了优化,操作简便,成本低,适合工业化生产。     

Thiolation of arabinoxylan and its application in the fabrication of pH-sensitive thiolated arabinoxylan grafted acrylic acid copolymer

Current research work was conducted to synthesize Thiol modified arabinoxylan and its application in fabrication of hydrogel. Thioglycolic acid was esterified with arabinoxylan to prepare Thiolatedarabinoxylan. Appearance of peak at 2533.34?cm^?1 in FTIR and thiol content showed successful thiolation. The pH-dependent Thiolatedarabinoxylan/acrylic acid (TAX/AA) hydrogels of perindopril erbumine were prepared via free-radical co-polymerization. Perindopril erbumine (PE) was employed as model drug. Different batches with different feed ratio of TAX, AA, and MBA were prepared and their influence on swelling, solvent penetration, and consequent drug release was investigated. Swelling coefficients increased with increase in pH. TAX/AA hydrogels were characterized by Fourier-transform infrared spectroscopy (FT-IR), Thermal Analysis (TA), X-Ray diffraction (XRD), and scanning electron microscope (SEM). Dissolution studies were performed at pH 1.2 and 7.4 in which drug release showed direct correlation with TAX and AA ratio. In vivo studies showed that C_max of TAX-co-AA based hydrogel was 81.57?±?0.35?ng/ml which was maintained for a longer time after its administration. All the results of in vivo studies were significant and TAX-co-AA based hydrogel enhances the bioavailability of perindopril erbumine.     

培哚普利对慢性缺氧高二氧化碳大鼠肺血管重建的影响1

目的 探讨培哚普利对常压慢性缺氧高二氧化碳性肺动脉高压及肺血管重建的影响。方法 47只SD大鼠随机分为:对照组(A)、缺氧高二氧化碳处理4wk组(B1)、培哚普利治疗4wk组(B2)、缺氧高二氧化碳处理8wk组(C1)、培哚普利治疗8wk组(C2)。采用常压低氧高二氧化碳肺动脉高压大鼠模型,观察肺动脉平均压(mPAP),血浆血管紧张素Ⅱ(Ang Ⅱ)及肺小血管平滑肌外膜、内膜超微结构的变化,以及培哚普利对以上变化的影响。结果 缺氧高二氧化碳使mPAP,Ang Ⅱ上升,超微结构发生变化,培哚普利治疗4wk组mPAP,AngⅡ下降,平滑肌超微结构病变减轻。培哚普利治疗8wk组,平滑肌超微结构病变与对照组相似。结论 提示缺氧高二氧化碳使肺血管重建,且与AngⅡ有关;培哚普利能在一定程度上能减轻肺血管重建。