Park Jong Woo, Park Eun-Seok, Chi Sang-Cheol, Kil Ho Yeong, Lee Kyu-Hyun
*Department of Pharmaceutics, College of Pharmacy, Sungkyunkwan University, Suwon, South Korea; †FDL, Inc., Science & Technology Park, Sungkyunkwan University, Suwon, South Korea; and ‡Department of Anesthesiology, Hangang Sacred Heart Hospital, College of Medicine, Hallym University, Seoul, South Korea.
Anesth Analg. 2003 Sep;97(3):769-771. doi: 10.1213/01.ANE.0000074797.70349.CA.
In this study, we sought to determine the globule size distribution of a propofol/lidocaine mixture as a function of lidocaine concentration and time elapsed after mixing in a standard formulation of propofol emulsion (Diprivan) and in a new formulation containing L-lysine to improve stability. The globule size was measured with a laser diffraction technique. The median diameter of the globule size in 20 mL of Diprivan immediately after the addition of 0, 10, 20, 30, 40, and 50 mg of lidocaine was similar to that of chylomicrons, ranging from 0.28 +/- 0.01 micro m to 0.30 +/- 0.02 micro m, over the whole range of lidocaine concentration. However, the maximum diameter increased slightly (from 0.97 +/- 0.01 micro m to 2.90 +/- 0.07 micro m) as the concentration of lidocaine increased. At 6 h after adding lidocaine, the maximum globule size had increased slightly (to 2.98 +/- 0.04 micro m) with 20 mg of lidocaine and increased considerably (to 51.76 +/- 0.62 micro m) when 30 mg of lidocaine was added. At 2 h after the addition of 50 mg of lidocaine, the maximum globule diameter had increased to 52.2 +/- 1.92 micro m. The maximum globule diameter in the propofol emulsion to which L-lysine was added as a stabilizer did not exceed 3.0 micro m even when the largest amount of lidocaine was added. This study demonstrated that when 30 mg of lidocaine was added to 20 mL of Diprivan and the solution was left for a period of time, the globule size increased. Its increase was minimized by the addition of L-lysine to the propofol emulsion.
在本研究中,我们试图确定在丙泊酚乳剂(得普利麻)标准制剂以及含L-赖氨酸以提高稳定性的新制剂中,丙泊酚/利多卡因混合物的微球大小分布与利多卡因浓度及混合后经过时间的函数关系。微球大小采用激光衍射技术进行测量。在加入0、10、20、30、40和50 mg利多卡因后,20 mL得普利麻中微球大小的中位直径与乳糜微粒的中位直径相似,在利多卡因浓度的整个范围内,为0.28±0.01μm至0.30±0.02μm。然而,随着利多卡因浓度的增加,最大直径略有增加(从0.97±0.01μm增加到2.90±0.07μm)。加入利多卡因6小时后,加入20 mg利多卡因时最大微球大小略有增加(至2.98±0.04μm),加入30 mg利多卡因时则显著增加(至51.76±0.62μm)。加入50 mg利多卡因2小时后,最大微球直径增加到52.2±1.92μm。即使加入最大量的利多卡因,添加L-赖氨酸作为稳定剂的丙泊酚乳剂中的最大微球直径也不超过3.0μm。本研究表明,向20 mL得普利麻中加入30 mg利多卡因并放置一段时间后,微球大小会增加。在丙泊酚乳剂中添加L-赖氨酸可使这种增加最小化。