Kim N S, Umejima H, Ito T, Uchida T, Goto S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Chem Pharm Bull (Tokyo). 1992 Oct;40(10):2800-4. doi: 10.1248/cpb.40.2800.
The release of lidocaine from hydrogel and xerogel preparations was remarkably suppressed compared with polyethylene glycol (PEG) 2000 suppository. The release rate of lidocaine from hydrogel and xerogel increased with the increase in the amount of sodium hydroxide incorporated within the range of 3 to 7 milliequivalent (meq). After an oral administration of lidocaine HCl solution, the plasma concentration of lidocaine was considerably lower than that after intravenous administration for all time periods. The absolute bioavailability (F(oral)) was 5.63%. For the Witepsol S-55 and PEG 2000 suppositories, the plasma levels of lidocaine were higher than those for the oral preparation, and Cmax and area under the concentration-time curve (AUC) values significantly improved (p < 0.01). The absolute bioavailabilities were 21.3 and 29.6%, respectively. On the other hand, Eudispert hv-hydrogel and xerogel preparations showed the characteristics of a sustained-release preparation, especially the xerogel preparation with 5 meq NaOH. Absolute bioavailability for hydrogel and xerogel preparations increased significantly (p < 0.05) by approximately 1.7-3.4 folds compared with those of Witepsol S-55 and PEG 2000 suppositories.
与聚乙二醇（PEG）2000栓相比，水凝胶和干凝胶制剂中利多卡因的释放明显受到抑制。在3至7毫当量（meq）范围内，随着氢氧化钠加入量的增加，利多卡因从水凝胶和干凝胶中的释放速率增加。口服盐酸利多卡因溶液后，在所有时间段内，利多卡因的血浆浓度均显著低于静脉给药后的浓度。绝对生物利用度（F(口服)）为5.63%。对于Witepsol S - 55栓和PEG 2000栓，利多卡因的血浆水平高于口服制剂，且Cmax和浓度 - 时间曲线下面积（AUC）值显著改善（p < 0.01）。绝对生物利用度分别为21.3%和29.6%。另一方面，Eudispert hv - 水凝胶和干凝胶制剂表现出缓释制剂的特性，尤其是含5 meq NaOH的干凝胶制剂。与Witepsol S - 55栓和PEG 2000栓相比，水凝胶和干凝胶制剂的绝对生物利用度显著提高（p < 0.05），提高了约1.7 - 3.4倍。
