The Studies On Xinzhi Ion-Activated Nasal In Situ Gel

OBJECTIVE: To preparate and evaluate Xinzhi ion-activated nasal in situ gel.METHOD : (1)The extraction conditions of volatile oil were optimized with the volatile oil content as the index .(2)The extraction conditions of medicinal materials were optimized with 95% alcohol as extracting solvent and with the Magnolin and Imperatorin content as the index using orthogonal test.(3)To optimize HP-β-cyclodextrinthe inclusion process in the inclusion of volatile oil ,Orthogonal experiment was performed,and HP-β-cyclodextrinthe inclusion process was evaluated with inclusion rate of volatile oil,recovery rate of inclusion compound as indexes.(4)With 95% alcohol used as solvent, 1,2-propylene glycol as solvent and penetration enhancer, Tween-80, polyglycol as solubilizing agent, the optimum formulation of Xinzhi ion-activated nasal in situ gel was selected with orthogonal test ,using the cumulative amount of Magnolin and Imperatorin in Xinzhi ion-activated nasal in situ gel permeating the scalper nose mucosa in vitro as the index.(5)Characteristic of the viscosity of Xinzhi ion-activated nasal in situ gel was studied.Regularity of the drug release was studied by using the Franz diffusion cell model and mechanism of the drug release was study by using the membrane-less dissolution model. (6)The preliminary stability of Xinzhi ion-activated nasal in situ gel were investigated.(7) Uses TLC to carry on the qualitative distinction of Magnolia sprengeri Pamp,Ligusticum chuanxiong Hort,Radix Angelicae dahurica and Xanthium sibiricum Patr . The Magnolin and Imperatorin content in Xinzhi ion-activated nasal in situ gel was determined by HPLC to establish the tentative quality standard of the preparation.(8)The mucosa irritation experiments and elementary pharmaco-dynamics tests of Xinzhi ion-activated nasal in situ gel.RESULTS:(1)The optimized extraction condition of volatile oil was as follows: Soaking 12h with 8 times water and extracting with 4h.(2)The optimized extraction and exaltatation conditions of residue were as follows: Soaking 12h with 5 times 95%alcohol and percolating with 10 times95% alcohol. The percolating rate was 2mL/min·Kg.(3)The optimized inclusion condition was as follows. The rate of volatile oil to HP-β-cyclodextrin was 1:8(mL/g), the inclusion temperature was at 80℃and inclusion time was 1h.(4)The optimum formulation of Xinzhi ion-activated nasal in situ gel consists of 2% alcohol,30%1,2-propylene glycol and 5% polyglycol.(5)The viscosity tests of the gellan gum show that the viscosity of Xinzhi ion-activated Nasal in situ gel employing 0.5%gellan gum as material was moderate. The process of endosmotic permeation of Xinzhi ion-activated Nasal in situ gel in vitro across the scalper nose mucosa followed one-order.The action of drug release of Xinzhi nasal in situ gel was diffusion and it was not erosion.(6)The results of preliminary stability experiments indicated that Xinzhi ion-activated nasal in situ gel were stable and the drug content of the spray was not obviously changed at ordinary temperature during six months.(7)The quality standard was simple, convenient and practical, which can be used for controlling the quality of Xinzhi ion-activated nasal in situ gel.(8)The results of nose mucosa irritation experiments and elementary pharmacodynamics tests showed that it is almost no irritation and it is effective in prevention and treatment for the chronic rhiniti of SD rats.CONCLUSIONS: The well-chosen preparation technology of Xinzhi ion-activated nasal in situ gel is reasonable and reliable,and the qualitiy control methods are practicable. It is effective to preventing and treating chronic coryza of SD rats with almost no irritation. The study results mentionged above show that it is a novel dosage form of drug for nose it is valuable for further research and development.