Preparation And Inspection Of Nicotine Ion-Sensitive In Situ Nasal Gel

OBJECTIVE:To prepare and evaluate an ion-sensitive in situ nasal gel of nicotine.METHODS:(1) Using UV and HPLC method for the determination of nicotine content.(2) Nit-HP-β-CD was prepared by freeze-drying method.(3) The validation of inclusion was made by the method of infrared spectrum.(4) The central composite design and response surface methodology were chose to optimize the process of preparation to the inclusion rate of inclusion as examining index.(5) The stability of the inclusion complex was examine by comparing the volatile of inclusion complex and mixture.(6) The nicotine ion-sensitive in situ nasal gel was prepared employing gellan gum as the gel matrix and Menthol, Nipagin Esters and VE as the accessories.(7) The viscosity characteristics with the different concentrations of DGG were investigated by the rotary viscometer(8) By using diffusion pool, ionic membrane stripping inspection the in vitro release of nicotine nasal in situ gel.(9) By using SD rats repeatedly to the study on the drug nicotine nasal irritation to the nasal in situ gel.(10) By using the toad palate mucosa cilia as the experimental model to check the nicotine ionic cilia toxicity of nasal in situ gel.RESULTS:(1) Established a relatively perfect method for the determination of Nit content.(2)Freeze drying can preparing High inclusion rate of Nit-HP-beta-CD inclusion complex.(3) Verified by infrared spectrum found Nit working with HP-beta-CD to generate a new phase, rather than a mixture of simple.(4) The optimum technological parameters were as follows:ratio of HP-β-CD/nit 3.36:1, the reaction temperature was 45℃, ratio of water/ HP-β-CD 20:1 and the reaction time was 3.5h. The inclusion rate was 59.74%.(5)Nicotine that was included by HP-β-CD could promote the stability of the drug.(6)nicotine nasal in situ gel was prepared.(7) Select 0.5% DGG solution as gel matrix(8) The dissolution curves invitro showed that the drug release could be the bese described by the First order kinetic model, the release was not correlated with the erosion rate.(9) Nicotine ion-sensitive in situ nasal gel had no side effect to nasal mucosa.(10) Nicotine ion-sensitive in situ nasal gel had no side effect to Nasal cilia.CONCLUSIONS:The well-chosen preparation technology of nicotine nasal in situ gel is reasonable and reliable. With the characteristics of the sustainable drug release and the quality stable. It can be used as a new promotion of the smoking cessation drug.