4种直肠给药剂型对家兔的局部药效学研究

Topical Pharmacodynamics of Four Rectal Dosage Forms in Rabbits

目的:分析4种直肠给药剂型在直肠中的分布特点。方法:以亚甲蓝为指示剂,制备浓度均为0.5%的栓剂、灌肠液、凝胶剂和泡沫剂,将12只家兔分为4组,将4种制剂分别经直肠给药,2h后解剖,观察家兔直肠染色部分的长度、染色的深度、黏膜皱襞是否染色及制剂在体内保留时间等指标。结果:4种剂型中,泡沫剂组着色部分最长,平均达(28.3±1.3)cm(P<0.05),且颜色最深;栓剂组着色部分最短,平均为(12.5±0.8)cm,且颜色最浅,但制剂保留时间较长。凝胶剂组与灌肠液组着色长度和保留时间介于上述2种剂型之间。结论:泡沫剂在治疗直肠结肠疾病给药方面具有显著优势,值得深入研究。

OBJECTIVE： To analyze the distribution characteristics of four rectal dosage forms in rectum. METHODS Four rectal dosage forms （0.5% suppository, enema, gels and foam） were prepared with methylene blue as indicator. A total of 12 rahbits were randomized to 4 groups to receive suppositories, enema, gel, or foam preparation per rectum. The rabbits were dissected at 2 h for the measurement of the length of stained rectum, degree of staining, whether there was staining in mucosa plica, and the retention time of the preparations in vivo etc. RESULTS： The averge length of stained intestinal tract was （28.3 ± 1.3） cm in rabbits receiving foam per rectum （P 〈 0.05） and the staining was also the deepest in color; the length of stained intestinal tract was the shortest （12.5 ±0.8） cm in rabbits receiving suppository per rectum （P 〈 0.05） and the staining was the lightest in color, but the retention time of suppository was long. The averge length of stained intestinal tract and the retention time of gels or enema in rabbits receiving gels or enema were ranged in between of the above two groups （foam and suppository）. CONCLUSION： The foam per rectum has its marked merits in treating colorectal disease, which thus deverving further investigation.