AIM:To study pharmacokinetic of Pueraria Flavonid Nasal Drop in rabbits through nasal administration in comparison with oral administration. METHODS:Ten New Zealand rabbits were divided into two groups randomly and administrated nasally and orally (106.4 mg/kg of pueraria flavonid). HPLC was adopted to detect pueraria flavonoid content and DAS 2.0 was used to calculate bioavailability. RESULTS:The main pharmacokinetic parameters of nasal and oral administrations were AUC (0-∞)1 =(30.55?4.93)mg/(L?h),T max1 =(0.90?0.14)h,C max1 =(11.27?1.66)mg/L;AUC (0-∞)2 =(6.90?2.76)mg/(L?h),T max2 =(0.63?0.34)h,C max2 =(1.68?0.84)mg/L. Relative bioavailability of nasal delivery was 442.8%. CONCLUSION:Pueraria Flavonoid Nasal Drop is well absorbed in rabbits and has high bioavailability.

Recent metabolomics research revealed a new ginseng ginsenoside IH901 that is synthesized by intestinal microbial transformation in oral administration of ginseng. IH901 shows various biological activities, including anti-tumor, anti-inflammatory, anti-diabetic, and anti-aging. In recent years, great effort has been made to prepare IH901 by microbial and enzymatic transformation in a large scale. In this paper, we reviewed the biotransformation pathways both in vivo and in vitro and bioactive properties of rare ginsenoside IH901.
Biotransformation ; Ginsenosides ; metabolism ; pharmacokinetics ; Humans ; Intestines ; metabolism ; microbiology ; Panax ; chemistry ; Sapogenins ; metabolism

Objective HupA is one of the potential drugs which can be used to treat Alzheimer's disease(AD).The aim of this study was to explore the pharmacokinetics and biodistribution of HupA in vivo by using 11C-HupA.Methods A total of 25 SD rats were studied.They were divided into 5 groups (5 rats in each group).All had intravenous injection of 22 MBq(in0.2 ml)11C-HupA through tail vein.Dynamic im-aging Was acquired from 5 to 90 minutes after injection.Venous blood and organ activities were collected at 5,15,30,60.and 90 minutes after injection.Percentage activity of injected dose per gram of tissue(%ID/g)was calculated to characterize the biodistribution of tracer in different brain regions: frontal,apical, temporal,occipital,cerebellum,hippocampus,striatum,thalamencephalon, and brain stem, Variance analysis using SPSS 11.5 software was performed and compared among the study groups.Results 11C-HupA was character-istic for its quick clearance from blood,with half time T1/2 of (14.61±1.77) min,and clearance rate (CL)macokinetics of 11C-HupA in rats corresponded to a one-compartment model.with an activity curve(area 11C-HupA distribution in different brain regions,being greater in cerebral cortex,hippocampus,hypothala-mus and brain stem. Conclusions Pharmacokinetic study of 11C-HupA in brain was fast.convenient and showed high specificity and sensitivity.Its ability to quantitatively evaluate brain function and its character-istic distribution in mice provided some evidence for monitoring therapy in AD patients.

OBJECTIVETo investigate the influence of drug properties on the encapsulation effiency (EE) and drug release of transfersomes for a proper transfersome preparation.

METHODTo prepare the transfersomes of colchicines (CLC), vincristine sulfate (VCR) and mitoxantrone hydrochloride (DHAD) with the same materials and methods, and then measure their EE. To find out the relationship between drug properties like solubility, molecular weight and charges, and EE. To performe the drug release experiments of various types of transfersomes in vitro, and compare their differences.

RESULTVCR and DHAD are lipophilic or hydrophilic, owing positive charges and large molecular weight, as a result, their EE are high, while CLC is amphipathic, neutral, and of small molecular weight, its EE is very low. As DHAD can insert into the membrane of transfersome, the drug release of DHAD-T in vitro is much slower than that of VCR-T.

CONCLUSIONTo prepare transfersomes with high EE, drugs that are lipophilic or hydrophilic, high molecular weight and opposite charges to the membrane should be chosen. Interaction between drugs and membrane will influnce the rate of drug release.

Antineoplastic Agents ; administration & dosage ; chemistry ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; Colchicine ; administration & dosage ; chemistry ; Deoxycholic Acid ; Drug Carriers ; Gout Suppressants ; administration & dosage ; chemistry ; Mitoxantrone ; administration & dosage ; chemistry ; Particle Size ; Phosphatidylcholines ; Solubility ; Technology, Pharmaceutical ; methods ; Vincristine ; administration & dosage ; chemistry

Objective To investigate the effect of ketamine on the release of norepinephrine(NE)fromlocus coeruleus in the brain of rabbits,trying to elucidate the central mechanism of cardio-vascular responseinduced by ketamine.Methods Nine healthy male New Zealand rabbits weighing 2.0-2.5 kg were used in thisstudy.A trocar(0.8 mm in diameter)was inserted into locus coeruleus using the stereotactic technique and fixed.Four days later push-pull perfusion of the brain was performed.37℃ artificial cerebrospinal fluid(aCSF)wasinfused through the trocar at 0.1 ml?min~(-1).A loading dose of ketamine 2 mg?kg~(-1) was given i.v.followed byketamine infusion at 50 ?g?kg~(-1)?min~(-1) for 20 min.The perfusate from locus coeruleus was collected before duringand after ketamine infusion every 20 min.The NE concentration of the perfusate was measured by high performanceliquid chromatography(HPLC).Results The NE concentration of perfusate from locus coeruleus increasedsignificantly after ketamine infusion from(16?3) pg～?l~(-1) to(32?4)pg??l~(-1) and returned to baseline level 20min after termination of ketamine infusion.Conclusion Ketamine increases the concentration of NE in locuscoeruleus.The increased NE release from locus coeruleus may explain the central mechanism of circulatoryexcitement induced by ketamine.

Objective • To investigate the clinicopathological features, diagnosis and prognosis of rectal neuroendocrine neoplasms (R-NENs). Methods • The clinical data of 113 cases of R-NENs, from January 2008 to June 2017, were collected in Renji Hospital, Shanghai Jiao Tong University School of Medicine, and the clinicopathological features and prognostic factors were retrospectively analyzed. The expression of synapsin (Syn), neural cell adhesion molecule (CD56), and chromogranin A (CgA) were observed by immunohistochemistry in the R-NENs specimens. The specimens were also observed after hematoxylin-eosin staining. Results • In 113 cases of R-NENs, there were 59 males and 54 females, and their ages ranged from 25 to 83 with an average age of (52.3±13.3) years old. All the patients had no obvious clinical manifestations. The main symptoms included changes in bowel habits (21.3%), abdominal pain (8.9%) and anal symptoms (6.2 %), and 63.7% of cases were found in routine medical examinations. The R-NENs were diagnosed as G1 (79.6%), G2 (11.5%), and G3 (8.8%). Immunohistochemistry results demonstrated that 94.7% of tumors were positive for Syn, 80.9% for CD56, and 48.6% for CgA. Till November 2017, the median survival time was 33.10 months (0.40-114.67 months), with 1-year, 3-year, and 5-year survival rates of 93.8%, 90.0%, and 85.9%, respectively. The pathological grade, depth of tumor invasion, lymph node metastasis or distant metastasis, tumor size, and age were all associated with prognosis of patients with R-NENs. Conclusion • Most of R-NENs are low-grade malignant tumors with good overall prognosis and have a lack of specificity in clinical manifestations.

AIM: To address whether the analysis of CD45~+CD86~+ cells isolated from para-aortic lymph nodes (PLNs) is valuable in assessment of the status of local immunity at the feto-maternal interface. METHODS: CBA/J?DBA/2, virgin CBA/J, and CBA/J?BALB/c mice were used as an abortion-prone model (group A), non-pregnant controls (group N), and fertile controls (group F), respectively. The percentage of CD45~+CD86~+ cell in the CD45~+ cell group (CD45~+CD86~+ percentage for short) and the absolute number of these cells were determined with flow cytometry (FCM), using mononuclear cells isolated from PLNs collected on day 5.5, 9.5, and 13.5 of gestation, respectively, and mononuclear cells from placentas on day 13.5 of gestation. To clarify the identity of these CD86~+ cells, FCM was also performed with CD3, CD19 and DX5 as markers for T cells, B cells, and NK cells, respectively. RESULTS: Both resorption rate and absolute number of resorption were significantly higher in group A (29.3%, 1.8?1.0) than those in group F (4.8%, 0.3?0.5, P

AIM: To investigate the relationship between CD200~+CK7~+ trophoblasts and the resorption of embryos in a poly (I∶C)-induced abortion model. METHODS: The status of CD200 expression was investigated in Balb/c?C57BL/6 and Balb/c?Balb/c mice as induced model of embryo-resorption by an i.p. injection of poly (I∶C). CD200 expression on CK7~+ cells from placentas was detected with flow cytometry. CD200~+ cells in placenta were observed with immunocytochemical staining. RESULTS: Both the percentage and absolute number of CD200~+CK7~+ cells were dramatically decreased by injection of poly (I∶C) in Balb/c?C57BL/6 (6.3%?6.2% vs 36.1%?9.3%, P

Objective To explore the investigate of X-chromosome-linked inhibitor of apoptosis pro- tein(XIAP)and its effect on chemotherapeutic sensitivity in bladder carcinoma.Methods Using immu- nohistochemistry methods,the expression of XIAP was evaluated in 47 bladder carcinomas and 6 normal bladder tissues.The XIAP gene was transfected into bladder cancer cell line T24 by liposome and the positive clone was screened by G418.Cellular XIAP mRNA level was detected by RT-PCR.The apoptosis of T24 cells was induced by low-dose of mitocycin C(0.005 mg/ml and 0.05 mg/ml,respectively).The in vitro cellular growth activities were assayed by MTT color imetry;and the apoptosis rate was assayed by TUNEL methods. Results The expression rate of XIAP was 78.7%(37/47)in bladder carcinoma samples,with no corre- lation with carcinoma stages and grades(P＞0.05).XIAP mRNA level in transfected T24 ceils was signifi- cantly increased by 3.8 times.Treated with 0.005 mg/ml and 0.05 mg/ml of mitomycin C,the growth rates of XIAP transfected T24 cells were increased [(11.60?0.25)% and(16.51?0.87)% ,respectively,P＜0.05];and the apoptosis rates were decreased [(10.1?0.2)% and( 11.9?0.2)% ,respectively,P＜0.05]compared with those in control cells.Conclusions XIAP is highly expressed in humun bladder car- cinoma samples.Overexpression of XIAP in T24 cells results in decrease in bladder carcinoma cell apoptosis induced by MMC,which may decrease the chemotherapeutic sensitivity of T24 cells.

AIMTo report the experience with single stage dorsal inlay buccal mucosal grafts using the Snodgrass technique for complex redo cases.

METHODSFrom May 2004 to December 2005, a total of 53 patients aged from 3 to 34 years old (average 11.62 +/- 7.18 years) with failed previous hypospadias surgery were included in the present study. Indications included urethral strictures and repair breakdown. The unhealthy urethra was unroofed from the meatus in the ventral midline, a buccal mucosal graft was inlayed between the incised urethral plate and fixed to the corpora cavernosa. The neourethra was tubularized, and covered with subcutaneous (dartos) tissue and penile skin. Glanuloplasty was also performed in all cases. Outcome analysis included clinical follow-up, and endoscopy in 2 selected cases.

RESULTSThe buccal mucosal graft was 3.0-7.5 cm in length and 0.7-2.0 cm in width. All patients required glanuloplasty, with buccal mucosal grafts extended to the tip of the glans. After a follow-up of 14-30 months (mean 22.6 months), the total complication rate was 15.1%, with five cases of fistula and three cases of stricture.

CONCLUSIONInlaying dorsal buccal mucosal grafts applying the Snodgrass technique is a reliable method for creating a substitute urethral plate for tubularization. The recurrent rate of urethral stricture and fistula is at an acceptable level for redo cases. This approach represents an effective, simple and safe option for reoperations.

Adolescent ; Adult ; Child ; Child, Preschool ; Humans ; Hypospadias ; surgery ; Male ; Mouth Mucosa ; transplantation ; Secondary Prevention ; Transplants ; Treatment Outcome ; Urethra ; surgery ; Urethral Stricture ; prevention & control ; Urinary Fistula ; prevention & control ; Urologic Surgical Procedures, Male ; adverse effects ; methods