Preparation Of The Xun Huan Tong Luo Ointments And Functional Assessment

Objective:Preparing the XUN HU AN TONG LUO ointments,determining prescription and process conditions of the ointments,establishing quality standards confidant and functional evaluation.Method:1.By reviewing the literature and combining with the pre-experiment to determine the scope of substrate selection,using the comprehensive score method by the appearance,stability,emulsion particles and moisture retention of the ointments as the evaluation index to screen preliminarily of the prescription,2.taking the comprehensive score as indexes to screen the best prescription by orthogonal experiment,3.with the agitation speed,emulsifying temperature,time and method as indexes,optimize the process conditions through the single factor,4.the physical properties,irritation and security of the samples were examined,the content of total flavonoids was determined by UV spectrophotometry determination,the contents of Prim-O-glucosylcimifugin,Asarinin and 5-O-Methylvisammioside were determined by HPLC determination,the establishment of quality standards,establish the quality standard of the ointments,5.several models of inflammation and pain in mice were given low,medium and high dose groups of samples to examine their anti-inflammatory and analgesic effects,6.the rat model of rheumatoid arthritis were given low,medium and high dose groups were established,with the weight rate,Arthritis score,toes swelling rate and the content of TNF-α,IL-1β,IL-6,IL-10 in rats serum as indexes to study its role.Results:1.The optimum preparation prescription of XUN HUAN TONG LUO ointments:concentrated liquid 20g,petrolatum 9g,lanolin 1 g,liquid paraffin 8g,glyceryl monostearate 5g,stearic acid 6.5g,glycerol 18g,Tween-80 4g,liquid paraffin 8g,laurocapram 1g,ethylparaben 0.5 g,and water was added to 100g,2.the optimum preparation process:the stirring speed of 250 r·min-1,the emulsification temperature of 70℃,the emulsification time of 10 min,by adding oil and water emulsifier method respectively,3.the product was brown yellow semi-fluid ointment,shiny,uniform texture,delicate,o/w optimum,consistency,pH,emulsion particles were accorded with the Chinese Pharmacopoeia,good stability,safe and non-irritating,4.The average content of total flavonoids in the samples was 50.54mg/g by UV spectrophotometry determination,5.in the high performance liquid chromatography,the linear relationship between the injection concentration and the peak area of Prim-O-glucosylcimifugin,Asarinin and 5-O-Methylvisammioside in the range of 0.01-0.05mg/mL was well,the methodology study of each index in the RSD value was<2%,the average content of Prim-O-glucosylcimifugin was 0.2885mg/g,the average content of Asarinin was 0.3735mg/g,the average content of 5-O-Methylvisammioside was 0.4593mg/g,6.the anti-inflammatory and analgesic experiments showed that the samples could inhibit the acute inflammation of xylene and the proliferation of agar granulation tissue in mice,enhance the permeability of capillaries in mice induced by acetic acid,inhibit pain reaction produced by the thermal stimulation and acetic acid,high dose group effect was significant,7.the results of anti-rheumatoid arthritis showed that the samples could improve the weight and arthritis score of AA rats,inhibit the swelling of the joints,and could decrease the levels of TNF-α,IL-1β and IL-6 in the serum of rats,increase the levels of anti-inflammatory factor IL-10.Conclusion:The ointments was prepared in accordance with the optimum formulation prescription and the optimized process parameters,the ointments was brown and yellow semi-fluid,the samples was exquisite,shiny,no grainy,suitable for consistency and easy to be coated,the emulsion particles of the samples were spherical,uniform and the size was qualified,the stability and moisture retention were good and non-irritating to skin,the optimized preparation process was stable and feasible,the quality standard was good and can be used for preparation quality control.The samples prepared according to the above method had anti-inflammatory analgesic and anti-rheumatoid arthritis effects.