Study Of Nao-qing Nasal Emulsion

According to the World Health Organization (WHO)’s latest statistics, stroke mortality,only after ischemic heart disease, ranks as the second of the world’s top ten causes ofdeath, causing more than six million people die each year. The traditional Chinesemedicine treatments of ischemic stroke are implemented through multiple targets andmultiple pathways. Particularly, the traditional Chinese medicine preparation, underthe guidance of overall concept and differential treatment theory, has the effect ofmultidirectional regulation, and highlights its unique advantages in treatment ofstroke.Based on the traditional Chinese medicine theory and using modern improvements ofpreparation,"Nao-qing" was made according to several years clinical experience ofprofessor Zhu Weifeng, who came from Guangzhou Hospital of Chinese Medicine. Asthere are some liposoluble components and volatile ingredients in the formulation of"Nao-qing", it is not appropriate to extract it through traditional decoction method.In order to make the hydrosoluble and liposoluble ingredients to be efficientlytransferred into the preparation, six medicinal materials were made to be emulsionthrough appropriate extraction method. Simultaneously, compared to microemulsionpreparation, emulsion preparation has the advantage of greatly reducing dosage oforganic solvent, which is more suitable for the nasal spray.This study performed screening and optimization of the prescription throughdiscussing the composition and ratio of the oil phase of emulsion, the selection,proportion and dosage of emulsifier, the dosage of stabilizer, and the processparameters of emulsion preparation. The ultimate formulation and preparation method were as follow: the musk extracting solution which made using ethanol by ultrasound;the acorus gramineus oil which made by steam distillation; plus the borneol, mint oil,2%soybean oil,1.5%mixed emulsifier composed of soybean lecithin and CremophorRH40(1:4) and0.5%oleic acid as the stabilizer, formed the oil phase of emulsion. Thepanax notoginseng saponins and the extract of Chuanxiong Rhizome which dissolvedin water, plus2.6%glycerol, formed the water phase of emulsion. The primaryemulsion was prepared by phase inversion method that the water phase added to theoil phase in drops slowly in the high speed dispersing machine by the rate of10000r/min. It should be dispersed twice,5min per time. Then add water to formuladosage. After preparing the primary emulsion, it should be homogenized underpressure of1000bar, circulating5times in the high pressure homogenizer. Finally theemulsion should be filtrated through the0.22μm microporous membrane.This research continued to study the quality and stability of Nao-qing Emulsion, anddrew a physical and chemical properties conclusion as follows: the appearance ofNao-qing Emulsion was light yellow to brownish yellow homogeneous emulsion；pH value was6.50, within the normal range of human nasal fluid; particle size(intensity distribution) was119.9±22.9nm, polydispersity index was0.081, theparticle size was small and distribution was narrow. The results showed that thesystem of this product dispersed homogeneously, and with good physical stability.Then the TLC identification method was set up that panax notoginseng and ligusticumchuanxiong were index components. The GC determination method was establishedwith menthol, isoborneol and borneol as the index ingredients. According to therelevant provisions of the "Chinese pharmacopoeia", the study performed stability testfor Nao-qing Emulsion. Results showed that muscone has strong volatility and greatloss amount, and there existed significant variance in quality between different batchof medicinal materials. Therefore, it was not appropriate to be used as quality controlindex. However, when using borneol, isoborneol and borneol as quality controlindicators of content determination, the product showed good stability in these components within6months. This product was sensitive to temperature, whichshould be kept out of light, and at temperature of4~8°C.Finally, this study made preliminary analysis on the security of Nao-qing Emulsion.The nasal mucosa irritation test results showed that this product had certain stimuluson rats’ nasal mucosa, which would recover to certain degree after stopping using thedrug for48hours. When using toad palate to evaluate nasal cilium toxicity in vivo,results showed that the product had no significant effect on the shape and movementof the toad palate cilium (compared with normal saline group, P>0.05), and thusdemonstrated that the product had low toxicity on cilia.This study lay a foundation for further development and application of Nao-qingEmulsion, and provides reference and supporting for the pilot production, qualityevaluation and comprehensive safety evaluation in the future.