硝酸甘油口腔速崩片的研制及其药效学的初步评价

Studies on preparation and pharmaceutical evaluation of a fast-disintegrating oral nitroglycerin tablet

目的研制及评价硝酸甘油口腔速崩片。方法采用适宜的湿法制粒工艺制备硝酸甘油口腔速崩片,并对其性状、重量差异、崩解时限、含量、稳定性等进行检测。通过8例健康自愿受试者含服硝酸甘油舌下片0.5mg,比较了硝酸甘油口腔速崩片与市售片对受试者的心率(HR)、舒张压(DBP)的影响。结果在性状、重量差异、含量等符合规定情况下,硝酸甘油口腔速崩片与市售片的崩解时间(分别为1.98 s,74.0 s)之间有显著性差异(P<0.01)。服药后3m in之内,硝酸甘油口腔速崩片的显效速度(对心率的增高和舒张压的降低)明显快于市售片,两者之间亦有显著性差异(P<0.05)。结论硝酸甘油口腔速崩片的速崩特性有利于药物的快速吸收,从而对急症冠心病心绞痛患者的自救具有显著性意义。

OBJECTIVE To prepare and evaluate a fast-disintegrating oral nitroglycerin tablet. METHODS Fast-disintegrating oral nitroglycerin tablets could be prepared by wet process compression method. The properties of tablets, such as shape, weight divergence, disintegration time,the content of nitroglycerin, stability were investigated, and the effect of eight healthy volunteers on DBP, HR of the fast-dlsintegrating oral nitroglycerin tablet and commercial tablet were all examined when volunteers were given a single dose of 0. 5mg nitroglycerin via sublingual way. RESULTS When tablets had proper shape and properties,weight divergence,the content of nitroglycerin, the disintegration time of rapid-disintegrating oral nitroglycerin tablet was few than that of commercial tablet （ 1.98s and 74.0s, respectively）, and a significant difference between them was found （P 〈0.01 ）. The speed of pharmacology （on HR and DBP） of fast-disintegrating oral nitroglycerin tablet was faster than that of commercial tablet after administration for 3minutes, and a significant difference between them was found also （ P 〈 0.05 ）. CONCLUSION A fast-disintegrating oral nitroglycerin tablet having rapid disintegrating characteristics will be beneficial for the drug absorption, therefore a remarkable significance will have been made to save patients with coronary heart disease or angina pectoris by themselves.