Study On Asarone Submicro-Emulsion And Submicro-Emulsion Nasal Spray System

α-asarone has prominent pharmacological activity and has been used clinically in the treatment of pneumonia, bronchial asthma, chronic obstructive pulmonary disease (COPD). Because of dominant lipophilicify and slight hydrophilicity, its bio-availability of the orally pharmaceutical product in the market only achieved 2-5%. The other pharmaceutical product on sale-α-asarone injection has low-compliance in clinical application and may have potential toxicity to people because of the adjuvant tween80 and ethanol in the formulation. Additionally, the amount of absorbed asarone after oral administration or injection distributed in liver reached 60%, thus hepatic lesion may occur for a long-term administration.Objective: A new emulsion system technique was studied to increase the solubility of asarone and drug loading, and to overcome the block that non-polar drugs are usually unfit for developing into solution pharmaceutical products for their low solubility. A safe, stable, efficacious, and convenient intranasal spray product will be prepared to improve the biological availability and decrease the side effect and adverse reaction.Method: ① Preformulation study "In situ hopeoad mandible mucosa method" was employed to investigate the toxicity of the model drug to nasal mucosa. Ultraviolet spectrphotometric method was utilized to study the solubility of the drug in water and vegetable oil. ②Asarone loaded submicro-emulsion study asarone was dissolved in oil, then mixed with purified water. The mixture was vigorous homogenized to form coarse emulsion, and the O/W dispersion was further homogenized to shape into a submicro-emulsion by high pressure homogenizer. Set emulsion diameter, demixing or not after centrifugalization, and zeta potential as criteria, to investigate the influence of the emulsifier, stabilizer, pH values, emulsification process and homogenization parameters on the stabilization of emulsion. The experiment of ex-vivo rabbit nasal mucosa partition was used to evaluate the influence of emulsion diameter and the amount of emulsifier on the affinity between the drug and the rabbit nasal mucosa. An orthogonal experiment was undertaken to optimize the formulation and production process. ③Evaluate the regulation...