Preparation Technics And Quality Stangdards Of Compound Xiaozhi Nanoemulsion In Situ Gel Gystem

Objective: Hemorrhoids is a common multiple anorectal disease, long timewithout treatment can cause anemia, incarcerated, necrosis and infection, etc. Itwill be a serious threat to human health if there it can’t be treated timely andcorrectly. Compound prescription xiaozhi nanoemulsion in situ gel derived fromclinical prescriptions with curative effect, by salvia miltiorrhiza, sophoraeflavescentis, chrysanthemum indicum, borneol and menthol, with the effect ofheat-clearing and detoxifying, promoting blood circulation to remove blood stasis,swelling and pain, for the treatment of hemorrhoids, with the symptom of ulcerssore, bloody stool, blood, leading to anal fissure, anal pain, etc. This experimentadopts the modern new technology to study the prescription drug preparationsmade for the nanoemulsion in situ gel preparation with the action of transdermalrate, long duration, good curative effect, convenient.Methods:(1) The research of nano emulsion preparation process with themethod of pseudo ternary phase diagram, affecting the formation ofmicroemulsions, suitable the type and ratio of surface active agent, surfactant andoil phase; Star design-response surface method is used to optimize formulation ofnanometer, with the particle size and PDI as ultimate index determine the optimalpreparation technology of compound xiaozhi nanoemulsion.(2)The moldingprocess of compound xiaozhi nanoemulsion in situ gel forming technology wasstudied through without membrane stripping method of in situ gel dissolutionkinetics; Establish content determination method of salvianolic acid B, linarin;With the temperature gelling as the index, using single factor experiment choosethe range of the dosage of the gel matrix P407and P188scope; Gelling temperatureand the cumulative release percentage as indicators through the stardesign-response surface method optimize the prescription of the gel nano emulsion. (3) The research of quality standard set up the prescription of chrysanthemumindicum, borneol, salvia miltiorrhiza, identification method by with TLCrespectively, set up the prescription of chrysanthemum indicum, borneol, salviamiltiorrhiza identification method; Determine the content of matrine andoxymatrine, salvianolic acid B in prescription by HPLC.(4)The preliminarystability study of compound xiaozhi nanoemulsion, investigate the stability ofthe in situ gel of compound xiaozhi nanoemulsion in the high temperature, coldstorage, high humidity and light conditions; Sample observation, at zeroth month,January, February, March respectively sampling to conduct qualitativeidentification and content determination of inspection, examine of the finishedproduct.(5)Compound xiaozhi transdermal drug release mechanism of nanoemulsion in situ gel and stimulating study modified Franz transdermal diffusionpool, the in situ gel of compound xiaozhi nanoemulsion transdermal diffusionprocess, explore the compound xiaozhi nanoemulsion in situ gel permeationmechanism; Stimulating study using rabbits.Results:(1) Through the pseudo ternary phase diagram method and stardesign-response surface method to determine the preparation of nano emulsion: EL100.2g, anhydrous ethanol38.7g, IPM10.4g, borneol3.4g, menthol1.7g, adddistilled water to make up to1000g.(2) The study of gel dissolution kineticsshowed that the gel dissolution rate is proportional to the release area, showing thecharacteristics of the zero-order kinetics, and the change of release area does notaffect the corrosion kinetics characteristics of the gel. Through the single factorexperiment and star design-response surface method in situ gel compound xiaozhinanoemulsion preparation technology for: P18818g, P407105g~113g andcompound xiaozhi nanoemulsion made up to1000g.(3) The quality standardcompound xiaozhi nanoemulsion in situ gel is clear yellow brown, transparentsolution at room temperature with good fluidity, clear yellow brown, andtransparent flow of semi-solid gel within the scope of33℃~36℃; With TLCmethod to identify borneol, chrysanthemum indicum, salvia miltiorrhiza as anindex; Through the method of HPLC setting up the content measurement method ofmatrine and Oxymatrine, salvianolic acid B, linarin, in the finished product ofsalvia miltiorrhiza, sophorae flavescentis, chrysanthemum indicum.(4)The stability ofcompound xiaozhi nanoemulsion in situ gel under the condition of storage is good.(5) Compound xiaozhi nanoemulsion in situ gel in the bitter and total base, to release a quantity of flower glycosides pseudo-first-order model release;Compound xiaozhi nanoemulsion in situ gel in rabbit rectum mucosa withoutexcitant.Conclusion: Through the study of compound xiaozhi nanoemulsion in situ gelpreparation process, the preparation process is scientific, stable, easy to get.Quality standards established is property professional, can scientifically controlthe quality of compound xiaozhi nanoemulsion in situ gel.