AIM: To purify the water-extract of Sinisa recipe with macoroporous resigns. METHODS: Screening the purification condition by means of the content of active principle, fingerprint chromatography, the yield of dry extracts,et al. of the purified product. RESULTS: The purified product by type HP20 macoroporous resign is in good agreement with the active fraction of Sinisa in the composition of specific principles. CONCLUSION: HP20 type macoroporos resign is considered as optimum for active fraction of Sinisa recipe in purifying efficience.

OBJECTIVETo prepare coated tablets of glycyrrhetinic acid and hydroxypropyl-beta-cyclodextrin (GTA-HP-beta-CYD) inclusion complex tablets for colon-specific release.

METHODIn order to improve the solubility of GTA, the GTA-HP-beta-CYD inclusion complex was prepared by ultrasonic-lyophilization technique and its formation were characterized by X-ray powder diffraction profiles and infrared spectrometry. The effects of inclusion condition on the inclusion efficiency and stability coefficient of inclusion complex were investigated, respectively. After prepared GTA-HP-beta-CYD tablets by powder direct compression, the pH dependant polymer Eudragit III and/or mixed with Eudragit II were used for further coating materials in fluid-bed coater. The influences of coating weight on the GTA release in different pH conditions were evaluated to establish the method for prepering colon specific delivery tablets with pulsed release properties.

RESULTThe formation of inclusion complexes were proved by X-ray powder diffraction profile and phase solubility curve. The effect of pH value of solvent was played critical role on the preparation of GTA- HP-beta-CYD inclusion complex. And the inclusion efficiency of GTA was 9. 3% and the solubility was increased to 54. 6 times at optimized method. The Eudragit III coated GTA- HP-beta-CYD tablets with coating weight 10% and 16% were showed pH dependant colon specific release profiles with slow release rate. The release profile of tablets coated with the mixture of Eudragit II and Eudragit III (1:2) were indicated typical pH dependant colon specific and pulsed release properties while the coating weight was 17%.

CONCLUSIONThe preliminary method for preparation of colon specific release tablets containing glycyrrhetinic acid with improved solubility was established for further in vivo therapeutic experiment.

2-Hydroxypropyl-beta-cyclodextrin ; Animals ; Colon ; chemistry ; Drug Stability ; Glycyrrhetinic Acid ; chemistry ; pharmacokinetics ; Humans ; Hydrogen-Ion Concentration ; Spectrophotometry, Infrared ; Tablets ; chemistry ; X-Ray Diffraction ; beta-Cyclodextrins ; chemistry ; pharmacokinetics

Objective To investigate the characteristic sonographic and pathological features of breast ductal carcinoma in situ (DCIS) without microcalcifications on mammography (MG).Methods Forty cases of DCIS without microcalcifications on MG were retrospectively reviewed.The 40 lesions were classified into mass and non-mass groups according to their sonographic findings.The pathological subtypes and nuclear grades of these cases were also analyzed.Fisher exact test was used to compare the differences of the sonographic accuracy rate,sonographic microcalcification rate,pathological nuclear grade and subtype rate between mass and non-mass groups.Results No abnormal finding was found in sixteen cases (40.0％)on MG and only one case (2.5％) on ultrasonography (US),respectively.The most common sonographic feature of DCIS without microcalcifications on MG were masses (75.0％,30/40),and other sonographic findings were round/oval and irregular shape,microlobulated margin,heterogeneous hypoechogenicity and isoechogenicity,and posterior acoustic feature.Ductal dilatations and heterogeneous isoechogenicity were present in most non-mass lesions of DCIS without microcalcifications on MG (22.5％,9/40).The ultrasonographic microcalcifications were found in 5 cases of DCIS without microcalcifications on MG.The common pathological features of DCIS without microcalcifications on MG were medium-low nuclear grade (85.0％,34/40) and noncomedo (87.5％,35/40).The difference of US accuracy rate in mass and non-mass groups was statistically significant [73.3％ (22/30) vs 33.3％ (3/9),P=0.047].The differences of US microcalcification rate,pathological subtype and nuclear grade were not significant (P=1.000,0.070).Conclusions The mass appearance and medium-low nuclear grade were most common sonographic findings and pathological features of DCIS without microcalcifications on MG.Ultrasonography should be an helpful tool for improving the diagnostic sensitivity ofmammography in breast DCIS.

Piperazine drugs, N - benzyl piperazine (BZP), 1 - (3 - chlorobenzene) piperazine (mCPP), 1 - (3 - three lfuorinated methyl phenyl) piperazine (TFMPP) have excitation and hallucinogenic effects similar to MDMA. They have became the alternative LSDs, abuse of substitues in the world reported increased year by year. The paper reviewed three piperazines regulation, abuse, toxicology, detection methods, and hope to provide a reference for judicial departments to crack down on the crime of the drug uses.

OBJECTIVETo prepare a novel floating micropellets containing hydroxy propyl-beta-oyclodextrin(puerarin-HP-beta-CD) for gastroretentive dosage form and evaluate its pharmaceutical characteristics in vitro.

METHODThe puerarin HP-beta-cyclodextrin inclusion complex was prepared by freeze-drying method. Puerarin and its HP-beta-CD inclusion complex were incorporated into alginate beads, respectively. The effect of methyl cellulose (MC), Mg-Stearate and chitosan on buoyancy and cumulative release rate of puerarin were investigated in simulated gastric fluid.

RESULTThe spectrums of FTIR and profiles of X-ray powder diffraction of samples proved the formation of inclusion complex between puerarin and HP-beta-CD. Magnesium stearate had a significant effect on the buoyancy of micropellets, and satisfied results were gained by the content with 2%. The solubility of puerarin was increased 65.6-fold by the formation of inclusion complex, the dissolution rate and cumulative release percentage also improved significantly although with the burst release phenomena. The micropellets showed sustained release properties by using puerarin-HP-beta-CD inclusion complex mixed with puerarin (1:1) and treated thoroughly under homogenizer.

CONCLUSIONThe solubility and release rate of puerarin are increased by the formation of inclusion complex with HP-beta-CD and its gastroretentive dosage forms displayed satisfied floating and sustained release characteristics.

2-Hydroxypropyl-beta-cyclodextrin ; Dosage Forms ; Freeze Drying ; Isoflavones ; chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; X-Ray Diffraction ; beta-Cyclodextrins ; chemistry

Objective:To study the correlation between HBV Pre-S1 antigen,HBeAg levels and HBV DNA copies,so as to assess the clinical value of Pre-S1 in detection of HBV replication.Methods:A total of 363 HBsAg-positive samples were col- lected.The levels of Pre-S1 antigen,HBeAg and HBV DNA copies were determined by ELISA,time-resolved immuno-fluores- cent method and real-time fluorescent quantitative PCR(FQ-PCR),respectively.The correlation between the determination re- sults was analyzed.Results:Pre-S1 antigen level was correlated with the level of HBeAg(X~2=94.4,P

The aim of this study was to improve the stability and cover the unpleasant odor of valerian oil by preparation of beta-cyclodextrin inclusion complex. The preparation method was established based on the yield of inclusion complex and entrapment efficiency of valerian volatile oil. After that, the formulation and processing parameters were optimized by uniform design table. The formations of inclusion complex were validated by DSC and X-RD method. The stability of valerian oil beta-cyclodextrin inclusion was studied under stressed conditions. In conclusion, relatively high yield of inclusion complex and entrapment efficiency were obtained by saturated solution-ultrasonication method. Inclusion complex yield and entrapment efficiency of the valerian oil were (84.78 +/- 3.23)% and (86.23 +/- 2.48)%, which were prepared under the optimized conditions, respectively. The results of DSC and X-RD were indicated the formation of inclusion complex. The stability of test showed that the valerian oil-beta-cyclodextrin inclusion complex was improved significantly.
Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Odorants ; Oils, Volatile ; chemistry ; Valerian ; chemistry ; beta-Cyclodextrins ; chemistry

Objective To evaluate the efficacy and safety of fludarabine and pirarubicin (FT) regimen in the treatment of refractory or relapsed indolent non-Hodgkin lymphoma (NHL). Methods A total of 40 patients with relapsed or refractory indolent NHL were treated with FT regimen, one cycle for 28 days, total 6 cycles. The data of indolent NHL patients treated with fludarabine, noventrene and dexamethasone (FND) regimen were collected as control. Results 40 patients were given 228 cycles chemotherapy, overall response rate was 62.5 %, median progression-free survival was more than 20 months and 2 years overall survival rate was 70.0 %. The main toxicities was leucopenia (80.0 %), but the incidence of WHO Ⅲ-Ⅳ leucopenia and pneumonia was less than that of in the control group, the rate were 12.5 % vs 29.0 % and 2.5 % vs 23.0 % respectively (P <0.05). Conclusion The efficacy of FT regimen was as good as FND regimen, but the incidence of leucopenia and pneumonia by Ⅲ-Ⅳ was lower in FT group than in FND group. So the FT regimen was an effective and safe second-line salvage regimen for relapsed or refractory indolent non-Hodgkin lymphoma.

Background Femtosecond laser in situ keratomileusis (LASIK) inevitably injury keratocytes and corneal nerve fibers.The research report about postoperative morphological changes of corneal nerve regeneration and keratocytes in femtosecond LASIK is still rare.Objective The aim of this study was to observe the kinetic changes of keratocytes and corneal nerve in corneal flap after femtosecond LASIK.Method Femtosecond laser manufacture corneal flap of LASIK surgery was performed on 60 eyes of 30 patients with refractive error using both femtosecond laser system and excimer laser treatment system.The repair of corneal wound was examined by slit lamp microscope,and the morphology of keratocytes and corneal nerve were observed with confocal microscope 1 week,1month,3 months after surgery,respectively.Results No haze or flap folds were found under the slit lamp microscope from 1 week through 3 months after operation.One week after surgery,the corneal stromal cells at the interface of the corneal flap appeared to be a mild activation status in 42 eyes (70％),but the activated cells gradually reduced with lapse of time.Three months after surgery,mild activation state still was found in 7 eyes (12％).One week after surgery,independent,short (＜50 μm),curved subbasal nerve fibers were exhibited in 7 eyes (12％),and curved filamentous nerve fibers were discovered in 48 eyes (80％) one month after surgery.The nerve fiber length of subbasal nerve was ＞200 μm in 27 eyes (45％) and classes beaded structure appeared 3 months after operation but were still different with preoperative subbasal nerve fibers.One week after the operation,filaments or discontinuous nerve fibers could been seen in 46 eyes (77％) at theinterface,and long nerve fibers or filamentous nerves were visible around the terminal or periphery of nerve fibers in 49 eyes (82％) one month after surgery,and long nerve fibers or filaments of nerve fibers were visible in 57 eyes (95％) 3 months after the surgery.Conclusions Femtosecond LASIK cause wound reaction at cellular level.Corneal nerve fibers recover with the extension of time,but there are still some morphological differences 3 months after surgery from preoperation.

AIMTo investigate the effects of injectio Salvia Miltiorrhiza (SM) on gentamicin (GM)-induced free radical formation in guinea pig cochlea, and to explore possible mechanisms on GM-induced ototoxicity.

METHODSBiochemical assays of superoxide dismutase (SOD) activity and malondialdehyde (MDA) content in guinea pig cochlea, combined with auditory brainstem response (ABR) measurement and transmission electron microscopic observation were used in this investigation.

RESULTSSOD activity was significantly declined while MDA content was distinctly increased in cochlear tissues after GM injection (P < 0.01). Moreover, they were well correlated with auditory function damage (|r| > 0.7). Co-treatment with SM evidently enhanced SOD activity and decreased MDA content (P < 0.01, P < 0.05). Furthermore, auditory function was markedly ameliorated. Morphological changes of cochlea were consistent with those of hearing function.

CONCLUSIONLipid peroxidation elicited by free radical was involved in GM-induced cochleotoxicity. SM might enhance SOD activity and prevent lipid peroxidation. As the result it might alleviate GM ototoxicity, and improve auditory function.

Animals ; Cochlea ; drug effects ; metabolism ; Free Radicals ; metabolism ; Gentamicins ; toxicity ; Guinea Pigs ; Lipid Peroxidation ; Malondialdehyde ; analysis ; Salvia miltiorrhiza ; Superoxide Dismutase ; metabolism