OBJECTIVE To study the stabilization effect of the aqueous solutions of polyoxyethylated nonionic surfactants with different polymerization degree of ethylene oxide and different hydrophobic groups on chloramphenicol. METHODS The stability of chloramphenicol in aqueous solution of TX (polyoxyethylene alkylphenol ether),AEO (polyoxyethylene fatty alcohol ether),Tween (polyoxyethylene sorbitan fatty acid ester) and EL (polyoxyethylene castor oil ether) series were investigated by HPLC in accelerated experiments. The location of the chloramphenicol molecules in the micelles was determined by 1H-NMR spectroscopy. RESULTS The hydrolysis kinetics of chloramphenicol showed first order character in the aqueous solutions of surfactants. The hydrolysis rate constants differed with different structures of hydrophobic group,while kept nearly the same with different polymerization degree of ethylene oxide. The 1H-NMR chemical shift of methylene which composed of the palisade layer of the micelles significantly changed. CONCLUSION The chloramphenicol molecules should be trapped into the palisade layer of the micelles. The polymerization degree of ethylene oxide had slight effect on the stabilization of chloramphenicol while the structure of hydrophobic group had significant effect. Polyoxyethylated nonionic surfactant with double bond,such as tween80 and EL,showed better stabilization effect on chloramphenicol.
ZHNG Li-xi;CHEN Zhi-rong;YIN Hong;YUN Shen-feng.
Stability Study of Chloramphenicol in Polyoxyethylated Nonionic Surfactant Aqueous Solution[J]. Chinese Pharmaceutical Journal, 2011, 46(16): 1258-1261
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] Ch. P(2005) Vol 2(中国药典2005年版.二部)[S]. 2005:778. [2] LING P X. Manufactural method for runshu eye drops: China,1083360A[P]. 1994-3-9. [3] BOER Y,PIJNENBURG A. HPLC Determination of chloramphenicol degradation in eye drops [J]. Pharm Weekbl,1983,5:95-101. [4] HIGUCHI T,ARNOLD MARCUS D,CHARLES BIAS D. The kinetics of degradation of chloramphenicol in solutionⅡ. Over-all disappearance rate from buffered solutions [J]. J Am Pharm Assoc,1954,XLⅢ(3):129-134. [5] CHEN Y X,ZHU W X,MA J G,et al. Progress of micelle solubilizing technology [J]. Food Sci (食品科学),2004,25( z1):265-270. [6] HAMMAD M A,MLLER B W. Solubility and stability of clonazepam in mixed micelles [J]. Int J Pharm,1998,169: 55-64. [7] JIAO J. Polyoxyethylated nonionic surfactants and their application in topical ocular drug delivery[J]. Adv Drug Deliv Rev,2008,60(15):1663-1673. [8] MALCOLM BOGHOSIAN P,LONG BEACH,JOHN WILSON W. Stabilized chloramphenicol composition:America,3702364A [P]. 1972-09-07. [9] ZHANG Y Q,ZENG X C,CHENG S Q,et al. NMR Study of solubilization of dimethylphthalate into micelles [J]. Acta Phys Chim (物理化学学报),1997,13 (11):1024-1028. [10] LV F F,LI N,ZHENG L Q,et al. Studies on the stability of the chloramphenicol in the microemulsion free of alcohols [J]. Eur J Pharm Biopharm,2006,62(3):288-294. [11] XIE N,HE X Y,ZHANG X M,et al. Determination of chloramphenicol and glycols in chloramphenicol eye drops by HPLC[J]. West China J Pharm Sci(华西药学杂志),2006,21 (1):93-95. [12] YAMAGUCHI M,YASUEDA S,ISOWAKI A,et al. Formulation of an ophthalmic lipid emulsion containing an anti-inflammatory steroidal drug,difluprednate[J]. Int J Pharm,2005,301(1-2):121-128. [13] CARMIGNANI C,ROSSI S,SAETTONE M F,et al. Ophthalmic vehicles containing polymer-solubilized tropicamide: “in vitro/in vivo” evaluation[J]. Drug Dev Ind Pharm,2002,28(1): 101-105. [14] SABAT J,PUJOL M,CENTELLES E,et al. Determination of equilibrium distribution constants of phenol between surfactant micelles and water using ultrafiltering centrifuge tubes[J]. Colloids Surfaces A Physicochem Eng Aspects,1999,150(1-3): 229-245.