Objective: To prepare the solid dispersion of Pulsatilla saponin D (PSD-SD) and evalution its in vivo and in vitro drug release behavior. Methods: The PSD-SD was prepared by solvent method. Three carriers were used in the PSD-SD. Infrared spectroscopy (IR), differential thermal analysis (DSC), and X-ray diffraction (XRD) were used to determine the PSD-SD. Dissolution rates and pharmacokinetic parameters were evaluated in vitro and in vivo characteristics of the PSD-SD. Results: When the PEG 6000 was used as carrier, the solubility of PSD was increased from 2.39 to 7.06 mg/mL, and the cumulative release rate of PSD reached 90% in 60 min, and the bioavailability of PSD was increased to 2.24 times. Conclusion: The solid dispersion prepared PSD can increase the solubility, dissolution rate, and bioavailability.

Objective: To investigate the intestinal absorption characteristics of Pulsatilla saponin D in rats. Methods: In situ single-pass intestinal perfusion model was used to inspect the absorption of Pulsatilla saponin D in the intestinal tract of rats. HPLC was used to determine the concentration of Pulsatilla saponin D in intestinal perfusion fluid samples. Absorption rate constant (Ka) and apparent permeability coefficient (Papp) were used as indexes to investigate the effects of absorption sites, drug concentration, different pH values, and P-glycoprotein (P-gp) inhibitor on Pulsatilla saponin D absorption. Results: There was the significant difference (P<0.05) of intestinal perfusion fluid samples in each intestinal segment and the order of the Ka and Papp values of Pulsatilla saponin D in each intestinal segment was colon>ileum>jejunum>duodenum. With the pH value increasing, the Ka and Papp values also increased and both of them had significant differences (P<0.05). The colon absorption of perfusion fluid at different concentration (0.30, 0.15, and 0.08 mg/mL) had no significant difference (P>0.05); There was significant difference (P<0.05) in Ka and Papp values with and without P-gp inhibitor. Conclusion: Pulsatilla saponin D could be well absorbed in whole intestinal segments of rats, and the best intestinal absorption site is colon; The drug concentration in a certain range has no effect on Ka and Papp values, which preliminarily comfirms that the obsorption mechanism of Pulsatilla saponin D could be passive diffusion; Pulsatilla saponin D may be a substrate of P-gp and possess the saturation phenomenon of transporters.

In order to solve the adhesion and the softening problems of traditional Chinese medicine extract during spray drying, a new method of adding dehumidified air into spray drying process was proposed, and the storage stability conditions of extract powder could be predicted. Kouyanqing extract was taken as model drug to investigate on the wet air (RH = 70%) and dry air conditions of spray drying. Under the dry air condition, the influence of the spray drying result with different air compression ratio and the spray-dried powder properties (extract powder recovery rate, adhesion percentage, water content, angle of repose, compression ratio, particle size and distribution) with 100, 110, 120, 130, 140 °C inlet temperature were studied. The hygroscopic investigation and Tg value with different moisture content of ideal powder were determined. The water activity-equilibrium moisture content (aw-EMC) and the equilibrium moisture content-Tg (EMC-Tg) relationships were fitted by GAB equation and Gordon-Taylor model respectively, and the state diagram of kouyanqing powder was obtained to guide the rational storage conditions. The study found that in the condition of dry air, the extract powder water content decreased with the increase of air compression ratio and the spray drying effect with air compression ratio of 100% was the best performance; in the condition of wet air, the extract powder with high water content and low yield, and the value were 4.26% and 16.73 °C, while, in the dry air condition the values were 2.43% and 24.86 °C with the same other instru- ment parameters. From the analysis of kouyanqing powder state diagram, in order to keep the stability, the critical water content of 3.42% and the critical water content of 0.188. As the water decreased Tg value of extract powder is the major problem of causing adhesion and softening during spray drying, it is meaningful to aid dehumidified air during the process.
Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Humidity ; Medicine, Chinese Traditional ; Plant Extracts ; chemistry ; Powders ; Temperature

OBJECTIVETo determine the equilibrium solubility of pulchinenosiden D in different solvents and its n-octanol/water partition coefficients.

METHODCombining shaking flask method and high performance liquid chromatography (HPLC) to detect the n-octanol/water partition coefficients of pulchinenosiden D, the equilibrium solubility of pulchinenosiden D in six organic solvents and different pH buffer solution were determined by HPLC analysis.

RESULTn-Octanol/water partition coefficients of pulchinenosiden D in different pH were greater than zero, the equilibrium solubility of pulchinenosiden D was increased with increase the pH of the buffer solution. The maximum equilibrium solubility of pulchinenosiden D was 255.89 g x L(-1) in methanol, and minimum equilibrium solubility of pulchinenosiden D was 0.20 g x L(-1) in acetonitrile.

CONCLUSIONUnder gastrointestinal physiological conditions, pulchinenosiden D exists in molecular state and it has good absorption but poor water-solubility, so increasing the dissolution rate of pulchinenosiden D may enhance its bioavailability.

1-Octanol ; chemistry ; Acetonitriles ; chemistry ; Biological Availability ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Gastrointestinal Tract ; metabolism ; Humans ; Hydrogen-Ion Concentration ; Intestinal Absorption ; Kinetics ; Methanol ; chemistry ; Pulsatilla ; chemistry ; Solubility ; Solvents ; chemistry ; Water ; chemistry

Objective To analyze the efficacy of electric sacral neuromdulation and resiniferatoxin in patients with female overactive bladder.Methods 32 cases with IOAB female patients accepted percutaneous test sitmulation of the electric sacral nerves at S3 ,and treated by intravesical instillation with 100ml of 100nmol/L RTX.The effica- cy of voiding status were evaluated.The improvement of female patients life were evaluated comparing the rating of depression and anxiety.Results There were significant improvements in 32 cases in variables included the number of voiding,volume voided and signs every day and urgent uresis.In the rating of depression and anxiety,the patients improved a litter and still had stimulating symptom in urethra and bladder.Conclusion The treatment of IOAB with single administratoon of electric sacral neuromdulation and resiniferatoxin is effective,and can successfully im- prove the symptom with little side effects.

Objective To explore the clinical skills and curative efficacy of endovascular embolization on dural arteriovenous fistula (DAVF). Methods A total of 50 patients with DAVF,admitted to our hospital from 2000 to 2009, underwent endovascular embolization with different materials through a microcatheter under DSA. After embolization, imaging examination was applied and clinical manifestations were noted during the clinical follow-up to evaluate the clinical efficacies.Results Immediate postoperative angiography indicated that the fistulas were totally occluded in 43patients, occluded evidently in 6 and occluded partially in 1. The 6-84 months follow-up found that clinical symptoms of 34 patients disappeared, 6 alleviated evidently, 7 relapsed, and 3 worsened; no complications were noted. Conclusion The endovascular embolization for DAVF is effective; and choosing the right embolic approach and material and improving the technology are the keys of successful treatment.

OBJECTIVETo analyze the clinical effects of intramedullary fixation of Kirschner pin for the treatment of distal fibula fractures.

METHODSFrom April 2007 to June 2010, thirty patients with the distal fibula fractures were treated with intramedullary fixation of Kirschner pin. There were 22 males and 8 females with an average age of 35.6 years old (22 to 60 years), length of hospital stay was 10 to 30 days (means 15.8 days). There were 20 cases of Transverse fracture and 10 cases of oblique fracture. Evaluation of the function of the ankle joint is based on the American Orthopaedic Foot and Ankle Society (AOFAS) standard evaluation systems.

RESULTSAll the cases were followed up. The mean followed-up time was 15.5 months (3 to 30 months). All fractures were bone healed, no case suffered infection and nonunion, no case suffered nervus fibularis superficialis injury. According to the AOFAS (American Orthopaedic Foot and Ankle Society) evaluation systems, the total scores after operation was 96.1 +/- 4.3 (the pain was 39.0 +/- 4.0, the fracture force line was 10, the function was 47.1 +/- 2.1. Twenty-eight patients obtained excellent results, 2 good.

CONCLUSIONThis method can be easily operated with the advantages of less pain and safety. It can effectively attenuate the financial burden of the patients. Thus worth being popularized in clinicic and basic level hospital.

Adult ; Female ; Fibula ; injuries ; Fracture Fixation, Intramedullary ; methods ; Humans ; Male ; Middle Aged

BACKGROUNDNeurone atrophy and loss are major causes of chronic neurodegenerative disorders such as Alzheimer's disease. Despite many pharmacotherapies for neurodegeneration, there are no accepted treatments. We investigated the feasibility of human nerve growth factor beta (hNGFbeta) gene expression mediated by recombinant adeno-associated viruses type-2 (rAAV-2) vector in the central nervous system (CNS) after blood brain barrier (BBB) disruption.

METHODSrAAV-2 containing hNGFbeta gene was constructed. The ability of hNGFbeta gene mediated by rAAV-2 vector (rAAV-2/hNGFbeta) to transfect cells in vitro was confirmed by both ELISA and bioassay of hNGFbeta in the culture supernatant of BHK-21 cells infected by rAAV-2/hNGFbeta. rAAV-2/hNGFbeta and rAAV-2/green fluorescence protein (GFP) were administrated separately to rat brains through internal carotid intubation after BBB disruption with hypertonic mannitol. Brain hNGFbeta concentration was measured by ELISA and GFP in brain sections was examined by laser scan confocal microscope.

RESULTSAfter 48 hours, hNGFbeta content in supernatant was up to (188.0 +/- 28.6) pg/ml when BHK-21 cells were infected by rAAV-2/hNGFbeta at multiplicity of infection (MOI) 1.0 x 10(6) vector genome. Neurone fibre outgrowths were obvious in dorsal root ganglion neurone assays by adding serum free culture medium harvested from BHK-21 cells exposed to rAAV-2/hNGFbeta. Whole brain hNGFbeta content in rAAV-2/hNGFbeta transferred group was up to (636.2 +/- 140.6) pg/ml. hNGFbeta content of BBB disruption in rAAV-2/hNGFbeta infused group increased significantly compared to the control group (P <0.05). GFP expression was clearly observed in brain sections of rAAV-2/GFP transferred group.

CONCLUSIONrAAV-2/hNGFbeta successfully expresses in the CNS after BBB disruption induced by hypertonic mannitol.

Animals ; Blood-Brain Barrier ; Brain ; metabolism ; Cricetinae ; Dependovirus ; genetics ; Genetic Vectors ; genetics ; Humans ; Nerve Growth Factor ; genetics ; Recombination, Genetic

OBJECTIVETo compare the results of application of Qu single abdominal aorta clamping for bloodless hepatectomy and Pringle hepatectomy in 118 cases of liver tumors.

METHODSThe clinical data of 118 patients, including 59 patients undergoing Qu single abdominal aorta clamping for bloodless hepatectomy (Group QG) and 59 patients undergone Pringle first hepatic portal clamping hepatectomy (Group PG) since March 2009 in the Ningbo Tumor Hospital and Jiangxi Provincial Hospital were retrospectively reviewed. The changes of blood pressure, oxygen saturation, urine volume, intravenous fluid volume, amount of bleeding, time of abdominal aorta (or first hepatic portal) clamping, duration of operation and anesthesia, and other intraoperative indexes of the two groups were compared, and the changes of peritoneal drainage, blood tests, liver functions, etc. before operation and 1, 3, 7, 14 days after the hepatectomy in the two groups were also analyzed.

RESULTSAfter taking appropriate measures for intraoperative blood pressure control, only small fluctuations of blood pressure, which could be safely adjusted and controlled with stable vital signs, was observed in the group QG. The amount of intraoperative bleeding in the group QG was (96.25 ± 18.45) ml, significantly less than (536.25 ± 35.65) ml in the group PG (P < 0.05). In the group QG, both the duration of operation time [(227.58 ± 28.20) min] and duration of anesthesia [(249.48 ± 31.35) min] were significantly shorter than that [(261.46 ± 32.12) min and (286.58 ± 35.62) min, respectively] in the group PG (both P < 0.05). The postoperative liver dysfunction in the group QG was also milder than that in the group PG (P < 0.05).

CONCLUSIONSFor liver tumor patients, Qu single abdominal aorta clamping for bloodless hepatectomy can basically achieve the goal of bloodless hepatectomy. This surgical operation is simple and safe, worthy of recommendation to skillful liver surgeons in hospitals there are some difficulties of blood supply.

Adolescent ; Adult ; Alanine Transaminase ; blood ; Aorta, Abdominal ; Aspartate Aminotransferases ; blood ; Blood Loss, Surgical ; Blood Pressure ; Carcinoma, Hepatocellular ; blood ; surgery ; Constriction ; Female ; Hemangioma, Cavernous ; blood ; surgery ; Hepatectomy ; methods ; Humans ; Liver Neoplasms ; blood ; surgery ; Male ; Middle Aged ; Operative Time ; Portal Vein ; Retrospective Studies ; Serum Albumin ; metabolism ; Young Adult

OBJECTIVETo study the conditions and parameters of roller compaction of Banlangen effervsce tablet.

METHODThe experimentation adopts L9 (3(4)) orthogonal experiment to study the conditions and parameters of roller compaction of Banlangen effervsce tablet; studied factors that included roller pressure, roller speed and moisture content of power, which influence the result of granule yield and granule friability.

RESULTThe optimal technique is: roller pressure at 1.5 MPa; roller speed at 15 Hz; moisture content of power at 1.5%.

CONCLUSIONThe study of roller compaction technique of Banlangen effervsce tablets provides some technicial consults of its research and production.

Analysis of Variance ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Pressure ; Tablets ; Time Factors ; Water ; chemistry