Formulation and evaluation of less-painful clarithromycin lipid microspheres

作者: Qin LingHao , Leng Wei

DOI: 10.1007/BF02980275

关键词:

摘要: Lipid microspheres (LMs) have recently been use as drug carriers for intravenous due to its low toxicity, good physiological tolerance and the reduction of related side-effect. In this study, clarithromycin was incorporated in LMs, an attempt reduce pain caused by use. The composition loaded LMs 0.5%, oil phase 10%, soybean phospholipid 2%, egg lecithin Sodium oleate 0.1%. Clarithromycin prepared high pressure homogenization method at 80 MPa 8-10 cycles. mean particle size surface charge were 208.7±7.8 nm -23.6±2.3 mv respectively. entrapment efficiency 66.4%. Drug stable during storage time 6±2°C 9 month, zeta-potential did not change significantly. concentration 5 mg/mL, there no degradation long term storage. Animal tests (rat paw lick test rabbit ear vein irritation test) used evaluate compared with that aqueous solution. These results suggest LM system is a promising option replace solutions treatment.

参考文章(30)
Torsten Zimmermann, Heinrich Laufen, Klaus-Dieter Riedel, Glenda Treadway, Alexander Wildfeuer, Comparative Tolerability of Intravenous Azithromycin, Clarithromycin and Erythromycin in Healthy Volunteers Results of a Double-Blind, Double-Dummy, Four-Way Crossover Study Clinical Drug Investigation. ,vol. 21, pp. 527- 536 ,(2001) , 10.2165/00044011-200121080-00001
Menashe Yoram Levy, Lev Langerman, Shoshanna Gottschalk‐Sabag, Simon Benita, Side-Effect Evaluation of a New Diazepam Formulation: Venous Sequela Reduction Following Intravenous (iv) Injection of a Diazepam Emulsion in Rabbits Pharmaceutical Research. ,vol. 6, pp. 510- 516 ,(1989) , 10.1023/A:1015928825882
Eugene H. Cox, Catherijne A. J. Knibbe, Victorine S. Koster, Mariska W. E. Langemeijer, Erica E. Tukker, Rogier Lange, Paul F. M. Kuks, Han J. M. Langemeijer, Loraine Lie‐A‐Huen, Meindert Danhof, Influence of different fat emulsion-based intravenous formulations on the pharmacokinetics and pharmacodynamics of propofol Pharmaceutical Research. ,vol. 15, pp. 442- 448 ,(1998) , 10.1023/A:1011980432646
A. Akkar, R.H. Müller, Formulation of intravenous Carbamazepine emulsions by SolEmuls® technology European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 55, pp. 305- 312 ,(2003) , 10.1016/S0939-6411(03)00028-6
Yasuo NAKAGAWA, Shigeru ITAI, Tsuguchika YOSHIDA, Tsuneji NAGAI, Physicochemical properties and stability in the acidic solution of a new macrolide antibiotic, clarithromycin, in comparison with erythromycin Chemical & Pharmaceutical Bulletin. ,vol. 40, pp. 725- 728 ,(1992) , 10.1248/CPB.40.725
C O Onyeji, C H Nightingale, D P Nicolau, R Quintiliani, Efficacies of liposome-encapsulated clarithromycin and ofloxacin against Mycobacterium avium-M. intracellulare complex in human macrophages. Antimicrobial Agents and Chemotherapy. ,vol. 38, pp. 523- 527 ,(1994) , 10.1128/AAC.38.3.523
Aslihan Akkar, Rainer H. Müller, Intravenous itraconazole emulsions produced by SolEmuls technology. European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 56, pp. 29- 36 ,(2003) , 10.1016/S0939-6411(03)00063-8
R.H Müller, S Schmidt, I Buttle, A Akkar, J Schmitt, S Brömer, SolEmuls-novel technology for the formulation of i.v. emulsions with poorly soluble drugs. International Journal of Pharmaceutics. ,vol. 269, pp. 293- 302 ,(2004) , 10.1016/J.IJPHARM.2003.09.019