【作者】 陈关平；

【导师】 操继跃；

【作者基本信息】 华中农业大学 ， 基础兽医学， 2003， 硕士

【摘要】 控释剂以其在动物体内停留时间长持久释放药物而被广泛应用于反刍动物抗寄生虫病。本论文回顾了控释剂和缓释剂的特点、国内外研究现状以及在兽医临床上的应用，对伊维菌素和阿苯达唑的研究和应用进行了综述。以高分子材料PVC为骨架材料自制的三组复方伊维菌素瘤胃控释剂为材料，用紫外分光光度计法测定并扫描了制剂每天释放的药物量，伊维菌素和阿苯达唑在5.30μg／ml的回归方程分别为A=0.0496+0.0517C(r=0.9999)、A=0.0054+0.0555C(r=0.9996)，线性关系良好。结果表明，第Ⅰ组制剂1-5号阿苯达唑的释药量为33.724±1.890mg／d，6-10号阿苯达唑的释药量33.473±1.928mg／d；1-5号伊维菌素的释药量为10.032±0.736mg／d，6-10号伊维菌素的释药量10.676±0.705mg／d。第Ⅱ组制剂中1-5号阿苯达唑的释药量为22.080±1.216mg／d，6-10号阿苯达唑的释药量21.887±1.114mg／d；1-5号伊维菌素的释药量为5.013±0.208mg／d，6-10号伊维菌素的释药量5.193±0.431mg／d。第Ⅲ组制剂中1-5号阿苯达唑的释药量为18.519±0.498mg／d，6-10号阿苯达唑的释药量19.313±0.609mg／d；1-5号伊维菌素的释药量为4.058±0.419mg／d，6-10号伊维菌素的释药量4.521±0.504mg／d。测定并计算了三组制剂的密度，第Ⅰ组制剂的密度2.27±0.13g／cm~3，第Ⅱ组制剂的密度2.44±0.08g／cm~3，第Ⅲ组制剂的密度2.15±0.06g／cm~3。继而对三组制剂进行了稳定性试验，将常温放置的制剂1-5号与在培养箱中(37.5℃)放置30天的6-10号制剂比较其每天的释放药物量，结果表明二者之间的每天药物释放量无明显差异。然后用HPLC方法采用双波长检测器同时测定伊维菌素和阿苯达唑的血浆药物浓度，伊维菌素和阿苯达唑在40-640ng／ml范围内线性关系良好，伊维菌素的回归方程为Y=0.0077+0.0117C(r=0.9994)，阿苯达唑的回归方程为Y=0.0578+0.0027C(r=0.9680)，并测定了阿苯达唑和伊维菌素在60、240、480ng／ml的回收率分别为94.2％、97.6％、101.40％和93.5％、98.3％、98.7％，表明回收率较高。通过比较三组制剂的密度、每天释药量和稳定性，第Ⅱ组制剂最为理想，达到了课题规划的要求。更多还原

【Abstract】 Controlled released preparation has been popularly applied in ruminant for anti-parasite because it can remain and release drugs in intra-ruminant for a long time. This article summarized the characterizations, origination, research development and practical application at home and abroad, about controlled released preparation and sustained release preparation of Ivermectin and Albendozale. Three groups intraruminal controlled release preparations of containing Ivermectin and Albendozale prescription were made in laboratory with polymer PVC. Ultral-violet spectrophotometry was used for determining the quantity of released drugs of intraruminal controlled release preparation of containing4Ivermectin and Albendozale. The equation of Ivermectin and Albendozale has good lineal relation. Ivermectin is A=0.0496+0.0517C (r=0.9999), and Albendozale is A=0.0054+0.0555C (r=0.9996). The results showed that the Ivermectin and Albendozale released quantity of the number of 1-5 of group I preparation were 10.0332 ± 0. 736mg. d, 33.724±1.890mg. d, the number 6~10 of group I preparation were 10.676± 0. 705mg. d, 33.473 ±1.928mg. d, the group 11 preparation were 5.013 ± 0. 208mg. d, 22. 080± 1. 216mg. d, 5. 193 ± 0. 431mg. d, 21. 887± 1. 1 14mg. d, the group 111 preparation were 4.058 ± 0.419rng. d, 18. 519 ± 0. 498mg. d, 41.521±0. 504mg. d, 19. 313±0. 609mg. d. After this, the stability of the three group preparations were determined, the results showed that it was not obviously significant between the preparations in room temperature and in 37. 5 ℃. And then high performance liquid chromatography (HPLC) method was used to delect the blood plasma concentration of Ivermectin and Albendozale with Dual λ Absorbance Detector at the same time, which have the good lineal relation in the range of 40-640ng/ml, the equation of Ivermectin is y=0.0077+0.0117C (r=0.9994), Albendozale is Y=0.0578+0.0027C (r=0.9680). With the same method the recovery of Ivermectin and Albendozale in blood plasma concentration 60. 240. 480ng/ml were 93.5%. 98.3%, 98.7% and 94.2%, 97.6%, 101.4%. The group II preparation has reached the ideal objectiveplanned before the experiment through comparing the concentration, stability and the quantity of drug released every day among the three group preparations.更多还原