CAJ | 학술논문

目的：研究羟丙基甲基纤维素（HPMC）亲水凝胶对托拉塞米渗透的影响。方法以HPMC为亲水凝胶的辅料，托拉塞米为模型药物，采用三室渗透装置测定药物透过中间室的速度，实验温度为37℃，测定时间为1、3、7、10、24 h，考察 HPMC 的不同质量浓度、黏度对药物渗透速度的影响，与药物本身的渗透速度比较计算阻滞率。结果半透膜本身对药物的平衡速度有一定影响，37℃下10 h透过率约50%，24 h基本达到平衡药物。在HPMC凝胶的存在下，阻滞率随着测定时间的延长而逐步减少，7 h后趋于平缓。HPMC的质量浓度越大对药物的阻滞率越大，黏度升高则阻滞率增加。合理的测定条件为HPMC K100M质量浓度分别为5、10、20 mg/mL，托拉塞米质量浓度为50μg/mL，在37℃水浴条件下，测定时间为10 h。相同型号（100M）的进口与国产HPMC在10、5 mg/mL时阻滞率基本一致，但在20 mg/mL时，国产HPMC的阻滞率明显大于进口产品。结论 HPMC溶胀形成的凝胶层对托拉塞米的渗透具有阻滞作用，对HPMC应用到缓释骨架片的研究提供参考。
목적：연구간병기갑기섬유소（HPMC）친수응효대탁랍새미삼투적영향。방법이HPMC위친수응효적보료，탁랍새미위모형약물，채용삼실삼투장치측정약물투과중간실적속도，실험온도위37℃，측정시간위1、3、7、10、24 h，고찰 HPMC 적불동질량농도、점도대약물삼투속도적영향，여약물본신적삼투속도비교계산조체솔。결과반투막본신대약물적평형속도유일정영향，37℃하10 h투과솔약50%，24 h기본체도평형약물。재HPMC응효적존재하，조체솔수착측정시간적연장이축보감소，7 h후추우평완。HPMC적질량농도월대대약물적조체솔월대，점도승고칙조체솔증가。합리적측정조건위HPMC K100M질량농도분별위5、10、20 mg/mL，탁랍새미질량농도위50μg/mL，재37℃수욕조건하，측정시간위10 h。상동형호（100M）적진구여국산HPMC재10、5 mg/mL시조체솔기본일치，단재20 mg/mL시，국산HPMC적조체솔명현대우진구산품。결론 HPMC용창형성적응효층대탁랍새미적삼투구유조체작용，대HPMC응용도완석골가편적연구제공삼고。
Objective To study the effect of hydroxypropyl methyl cellulose (HPMC) hydrogel on penetrability of torasemide. Methods HPMC was prepared into hydrophilic gel, and torasemide was used as representative drug. A device with three compartments was used to determine penetration speed of drug through the middle chamber. Penetration of drug through hydrophilic gel was tested at 1, 3, 7, 10, and 24 h under 37℃. The influences of concentration and viscosity of HPMC on penetration speed were taken into consideration. Block rate was calculated by the penetration speed of drug itself.Results Semipermeable membrane had influence on the balance speed of the drug. Under 37℃, the penetrated drug molecules was about 50% at 10 h, and the system achieves balance at 24 h. In the presence of the gel, block rate reduced gradually with the time increasing, became flat after 7 h. The higher concentrations of HPMC, the larger block rates of the drug. And the lager viscosities, the larger block rates of the drug. The reasonable standardized condition was as following: 37℃ water bath, the concentrations of HPMC were 5, 10, and 20 mg/mL, the concentration of torasemide was 50μg/mL, and those were determined at 10 h. The same type (100 M) of domestic and imported HPMC was compared to find their difference. Their block rates were similar at 10 mg/mL and 5 mg/mL. But the block rate of domestic product was significantly greater than that of imported product at high concentration.Conclusion HPMC hydrogel has blocking effect on penetrability of torasemide which may provide references on sustained release matrix tablets prepared by HPMC.