Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, Piscataway, NJ 08854, United States.
Int J Pharm. 2011 Dec 12;421(1):53-62. doi: 10.1016/j.ijpharm.2011.09.025. Epub 2011 Sep 22.
We investigated the enhancement effect of chemical enhancers and iontophoresis on the in vitro transdermal and transbuccal delivery of lidocaine HCl (LHCl), nicotine hydrogen tartrate (NHT), and diltiazem HCl (DHCl) using porcine skin and buccal tissues. Dodecyl 2-(N,N-dimethylamino) propionate (DDAIP), dodecyl-2-(N,N-dimethylamino) propionate hydrochloride (DDAIP HCl), N-(4-bromobenzoyl)-S,S-dimethyliminosulfurane (Br-iminosulfurane), and azone (laurocapram) were used as chemical enhancers. The study results showed that the application of iontophoresis at either 0.1 mA or 0.3 mA significantly enhanced transdermal and transmucosal delivery of LHCl, NHT and DHCl. It was also demonstrated that iontophoresis had a more pronounced enhancement effect on transdermal delivery than on transbuccal delivery of LHCl, NHT and DHCl. In addition, DDAIP HCl was found to be the most effective enhancer for transbuccal delivery of LHCl and NHT.
我们研究了化学渗透促进剂和离子导入对盐酸利多卡因（LHCl）、酒石酸氢烟碱（NHT）和盐酸地尔硫卓（DHCl）经皮和经口腔给药的体外渗透增强作用，使用了猪皮和口腔组织。十二烷基 2-（N，N-二甲基氨基）丙酸盐（DDAIP）、十二烷基 2-（N，N-二甲基氨基）丙酸盐盐酸盐（DDAIP HCl）、N-（4-溴苯甲酰基）-S，S-二甲基亚氨基硫烷（Br-iminosulfurane）和氮酮（月桂氮酮）被用作化学渗透促进剂。研究结果表明，在 0.1 mA 或 0.3 mA 的电流强度下应用离子导入技术可显著增强 LHCl、NHT 和 DHCl 的经皮和经黏膜给药。还表明，离子导入对 LHCl、NHT 和 DHCl 的经皮给药的增强效果比经口腔给药更为明显。此外，发现 DDAIP HCl 是 LHCl 和 NHT 经口腔给药的最有效渗透促进剂。
