Widespread Pain Subsides Content Of Effective Components And Health Human Pharmacokinetic Studies

Research background and objectiveDepartment of anorectal surgery usually treat diseases mainly include:anal fistula, hemorrhoids, rectum prolapse, rectum and anal canal abscess, rectal cancer, anal fissure, etc. These diseases usually need surgical treatment, But the pain, edema, hemorrhage, infection, delayed wound healing complications often appear after surgical treatments. The postoperative dressing changes become an important means to treat these postoperative complications and promote wound healing in addition to symptomatic treatments.At present, hemorrhoids ointment and hemorrhoids suppository are widely used to treat anorectal diseases, These drugs are supplied through the anus,They play an anti-inflammatory, analgesic, swelling by direct role in the surgical wound or the rectum mucosa. While there are small contact surface at the lesion site, uneven distribution, easy to melt and discharge, short duration of efficacy, low bioavailability. These are based on the above situation, Professor Zhao Baoming developed Guang TongXiao foam aerosol that based on the basic theory of TCM and combined with anorectal disease clinical characteristics,the foam aerosol can not only anti-inflammatory, swelling, relieve spasm and pain but also following advantages:the ejecta no flow, foam stable, long duration in the lesion site, coated with a wide range of uniformly dispersed in the lumen, effectively penetrate the mucosal folds, etc. It’s more effective than other formulations,and is a great development potential of dosage form.GuangTongXiao foam aerosols is a kind of traditional Chinese medicine foam aerosols. Professor Zhao Baoming developed this foam aerosols that is based on the basic theory of TCM and combined with characteristics of anorectal diseases. It is consisted of corydalis, white peony root, rubia cordifolia and othe Chinese medicines, it has spasmolysis analgesia, anti-inflammatory, hemostasis and promote wound healing. Treatment tips say"guang", means small and large intestines;"Tongxiao" means this foam aerosols have analgesia efficacy. Foam aerosol illustrate the formulations of the herbal compound."GuangTongXiao foam aerosols" summed the site of action of the herbal compound, efficacy and dosage forms.The foam aerosol has been finished these researches such as the extraction process、quality standards. efficacy, dosage form advantages and drug security researches by the department of Anorectal Surgery and laboratory of Guang An Men Hospital, the Department of Anorectal Surgery and the central laboratory of Dongzhimen Hospital、 Beijing University of Chinese Medicine the Academy of Military Sciences and Department of Pathology of Peking University Health Science. It has strong research bases because the animal experiments and clinical studies lasted more than20years, but these efficacy reasons unclear, Therefore,this subject will lay the foundation for the future study of the mechanism and guide clinical medication by determination of the active ingredient contents and pharmacokinetic study of healthy volunteers.Research methods and contents1.To determine five effective components in the water extract of GuangTongXiao.In this study, using LC-MS/MS method determine simultaneously tetrahydropalmatine, paeoniflorin, berberine, magnolol and honokiol, The results show that The method is rapid and sensitive, attribute strong, This method can determine simultaneously five kinds of effective components. LC-MS/MS method for determining contents of tetrahydropalmatine, paeoniflorin, berberine, magnolol and honokiol, the ibuprofen, raceanisodamine act internal standard. Chromatographic conditions:chromatographic column(Agilent Eclipse Plus C18,100mm×2.1mm,3.5μm), mobile phase A:0.1%of formic acid, B:acetonitrile, gradient elution, the column temperature30℃. Mass spectrometer conditions:ESI ion source, the positive ion mode drying gas temperature300℃, gas flow10L-min-1; Nebulizer pressure30Pa; the capillary voltage positive ions4000V, Paeoniflorin tetrahydropalmatine berberine, magnolol, honokiol, ibuprofen and raceanisodamine monitoring of ion-pair479.2/121,356.2/192.2,336.1/320.2,265.1/247.1,265.2/233.1,205.1/161.1,306.1/140,they are all analysised accurately.Linear ranges:0.8828125-113(r=0.9998);1.54375-49.4(r=0.9995);0.9046875-115.8(r=0.9997);0.88125-112.8(r=0.9994);0.165625-21.2(r=0.9999). spike recovery1.998%,1.14%,3.117%,1.828%and1.596%.The results show that the method high sensitivity, fast analysis,while qualitative ability and quantitative ability good, the method can determine simultaneously five main active ingredient contents in GuangTongXiao aqueous extracts.2. To study pharmacokinetics of Guangtongxiao foam aerosols that act on healthy human.The health human pharmacokinetics of GuangTongXiao foam aerosols that is administrated by anal.Determining the concentrations of tetrahydropalmatine and berberine in healthy male plasma by LC-MS/MS, raceanisodamine act internal mark, protein of plasma samples was precipitated by acetone,80%acetonitrile extraction, Chromatographic conditions:chromatographic column(Agilent Eclipse Plus C18,100mm×2.1mm,3.5μm), mobile phase A:0.1%of formic acid, B:acetonitrile, gradient elution0～1min(B15%、0.2mL/min);1～2min(B15%～40%,0.3mL/min);2～7min(B40%～80%,0.3mL);7～8min (B80%～15%,0.3mL/min);8～10min(B15%,0.3mL/min);10llmin(B15%,0.2mL/min);12min (B15%、0.2mL/min) Mass spectrometer conditions: ESI ion source, the positive ion mode drying gas temperature300℃, gas flow10L-min-1; Nebulizer pressure30Pa; the capillary voltage positive ions4000V, monitoring of ion-pair are479.2/121,356.2/192.2,306.1/140, the autosampler temperature15℃, the column temperature30℃. methodology evaluation show the tetrahydropalmatine and berberine hydrochloride that in biological samples show a good linear r>0.99, The linear range of the respective components are0.000594-1.188ng/mL,0.000536-1.072ng/mL, Lowest limit of quantification is0.000536ng/ml, intraday precision and day precision are both less than 15%,The extraction recovery are both more than85%. The method is simple, high efficiency, good selectivity, high sensitivity, and can be used successfully in the study of the dynamics of human plasma thay contain GuangTongXiao foam aerosols, On this basis, a high sensitivity, specificity, and accurate LC-MS/MS method has been establed, two kinds of active ingredients in the foam aerosols are determined simultaneously, and research the dynamic characteristics of foam aerosol in healthy male body,in order to provide a reference for the clinical and the late further researches.