For the minimized phase transtorming risk, the most stable polymorph is generally considered as the desirable solid form for pharmaceutical applications. However, occasionally, the stable form may have some shortcomings such as low solubility, dissolution rate and bioavailability, etc. In that case, the metastable form which is kinetically stable at room or lower temperature could be selected. Using metastable form may result in polymorph transformation in pharmaceutical manufacture and storage. Hence, the knowledge of the transformation between solid forms is essential to the development of the drug materials. In this paper, we will review the recent studies in the area of crystal conversion of polymorphs and hydrates, to illustrate some cases to introduce the types, conditions and mechanisms of the crystalline solid transformation.
Biological Availability ; Chemistry, Pharmaceutical ; methods ; Crystallization ; Drug Stability ; Kinetics ; Pharmaceutical Preparations ; chemistry ; Solubility

Objective To investigate the tissue distribution character of cinobufagin in in vivo in rats,in order to provide some references for rational drug use in the clinic.Methods Two kinds of solutions of cinobufagin were given to rats(0.5 and 1 mg/kg) by sublingual iv injection.The cinobufagin concentration in rat tissues corresponding to different time-point was determinated by HPLC.The biological samples of the different tissuses were performed by liquid-liquid extraction method.Results Cinobufagin distributed rapidly to tissue after sublingual iv injection.At 30 min cinobufagin in eight tissues except fat was detected.At 60 min the concentration in a majority of tissue achieved the peak value and liver′s was tiptop.When the concentration of cinobufagin increased by gemination,the time of reaching peak value had no change.Only the concentration of cinobufagin increased slightly corresponding to the time-point.Conclusion The distribution of cinobufagin in tissues of rats is extensive.Both the absorption and elimination of cinbufagin are quick and up to the top concentration in brain tissue.

Objective To study the effect of dexmedetomidine and midazolam on hemodynamics and sedation in patients with nasal intubation.Methods Forty patients whose ASA grade Ⅰ-Ⅱ and anticipated difficult airway were randomly divided into dexmedetomidine group(group D,20 cases)and midazolam group(group M,20 cases)according to the admission number.In group D,dexmedetomidine 1 μ g/kg were constant speed pumped in 10 minutes.In group M,midazolam 0.03 mg/kg were intravenous injected.Then nasal intubation were carried.Systolic blood pressure(SBP),diastolic blood pressure(DBP),mean arterial blood pressure(MAP),heart rate(HR),pulse oxygen saturation(SpO2),Ramsay sedation score,rate-pressure product(RPP),tip perfusion index(TPI)were recorded and compared before anesthesia (T0),fiberoptic bronchoscope pass by later nostril(T1),to spy on epiglottis(T2),intubation succeed(T3),after intubation 1 minute(T4)and after intubation 3 minutes(T5).Airway score and postoperative visit were evaluated.Results SBP,DBP,MAP,HR,RPP in group M were significantly higher at T1-T3 than those at T0 (P＜0.05),and were significantly higher than those in group D at the same time(P＜ 0.05).There was no significant difference in group D(P ＞ 0.05).Ramsay sedation score and TPI at T1-T3 in group M were significantly lower than those at To(P ＜0.05).Ramsay sedation score and TPI at T1-T5 in group D were significantly higher than those at T0(P ＜ 0.05),and were significantly higher than those in group M at the same time(P ＜ 0.05).The rate of airway score 1 score and intubation satisfaction in group D were significantly higher than those in group M[100％(20/20)vs.30％(6/20),90％(18/20)vs.50％(10/20)](P＜ 0.05).The rate of throat ache in group D was significantly lower than that in group M[5％(1/20)vs.35％(7/20)](P ＜0.05).Conclusions For difficult airway patients with nasal intubation during dexmedetomidine infusion,hemodynamics is stable and sedation is satisfied.

Objective:To compare the efficacy and safety between direct anterior approach (DAA) and posterior approach (PA) in total hip arthroplasty.Methods: This study evaluated postoperative results of 92 consecutive total hip arthroplasties performed by a single surgeon;44 from the DAA,and 48 from PA.The age,body mass index,operation time,blood loss,hospital stay,positioning of the artificial hip,postoperative Harris score and postoperative complications were recorded and analyzed.Results: Both the average age of the patients separately (58.0±11.9) years in DAA group and (61.0±10.4) years in PA group and the body mass index (25.1±3.7) in DAA group and (24.7±3.3) in PA group,showed no significant difference between the two groups.The DAA group had significantly reduced the hospital stay (3.8±1.7) days vs.(4.9±2.3) days for the PA group (P<0.05) and operation time was (76.0±17.4) min in DAA group,and (71.0±14.3) min in PA group (P>0.05).The amount of blood loss: in group DAA (238.0±55.3) mL,and in group PA (387.0±61.2) mL (P<0.05).There was no statistical difference in the positioning of the artificial hip: the cup anteversion in DAA group and PA group was 17.3°±5.3° vs.18.6°±5.1°,the cup inclination was 38.5°±5.7° vs.37.7°±5.2°.In DAA group,there was significantly less use of assistive devices [(24.6±7.8) d vs.(31.7±10.2) d,P<0.05],and the pain was significantly lower.Harris score at the end of 6 weeks of the follow-up: in DAA group 85.7±5.4,and in PA group 81.3±6.1 (P<0.05);at the end of the last follow-up: in DAA group 93.4±4.7,and in PA group 92.3±5.3 (P>0.05).Complications were encountered in the two groups.There were two intraoperative complications (4.4％),1 great trochanter fracture and 1 lateral cutaneous nerve injury in DAA group.No dislocation was observed in DAA group.One dislocations and 1 groin pain were recorded in PA group.No prosthesis loosening,deep vein thrombosis,sciatic nerve injury and other complications occurred in the two groups.Conclusion: Total hip arthroplasty using the anterior approach allows for superior recovery and better stability.

Adenoma ; Adult ; Ear Neoplasms ; Ear, Middle ; pathology ; Female ; Humans

OBJECTIVE To analyze the major reasons of wound infection after external fixator application and then introduce management measures to prevent following wound infections. METHODS Totally 542 patients adopting external fixators between May 2005 and May 2007 were retrospectively reviewed. All the external fixator-related infections were inspected and the excretions from these infected wounds were collected to perform bacterial culturing. RESULTS The total infection rate of these 542 patients after external fixator application was 2.77%. Among them, six were infected with the bacteria in distraction osteogenesis group and the infection rate was 8.82%; three were infected in bone un-union and bone defect group and the infection rate was 5.36%; whilest the common fracture-fixing group got the lowest infection rate of 0.39%. CONCLUSIONS Wire-crossing positions are the most frequently infected sites after external fixation and the drug-resisted bacteria are the most commonly detected pathogens. Thus, increasing the stability of fixators, enhancing the infection supervision of operation environment, draining the wound thoroughly and using antibiotics rationally are the most effective managing measures to prevent external fixator-related infections in orthopedics.

In order to show the development situation and trend in plaque research, Thomson Innovation Platform-covered application of patents associated with plaque researches was quantitatively analyzed using the Thomson Data Analyzer and Thomson Innovation or other tools, which revealed the overall development situation, the main accepted countries, the main application institutions and the technological direction layout of patents associated with plaque researches.

Objective To evaluate the characteristics of quantitative monitoring of brain function during the perioperative period in elderly patients and its relationship with postoperative cognitive dysfunction (POCD).Methods Seventy ASA physical status Ⅰ or Ⅱ patients,aged ≥ 60 yr,scheduled for elective lumbar spine decompression and fusion surgery under general anesthesia,having an expected postoperative length of hospital stay ≥ 7 days,were enrolled in the study.The cognitive function was assessed by using Mini-Mental State Examination before operation and the results were normal.Fifty healthy elderly volunteers were chosen and served as control group.Cognitive function was assessed at l day before operation (D0) and 3 (D3) and 7 days after operation (D7).Z score was used to identify POCD.All the patients were then divided into POCD group or control group (group C) according to the results of diagnosis.Quantitative monitoring of brain function was carried out using a traction system,and the wavelet index (WLI),i_22 and i_20 were recorded.Results A total of 67 patients completed the study and were enrolled in the analysis,there were 9 cases in group C,and 58 cases in group POCD.The WLI was significantly decreased at D7,and no significant change was found in WLI at D3 as compared with the value at D0.The WLI was significantly lower at D7 than at D3.There was no significant difference in i_22 and i_20 between the three time points.Compared with group C,i_22 was significantly decreased at D0,and no significant change was found in i_22 at the other time points and in WLI at each time point in POCD group.Conclusion During quantitative monitoring of brain function during the perioperative period in the elderly patients,WLI is significantly decreased on 7th day postoperatively,and no significant change is found in i_20 and i_22,however,the pre-operative low i_22 value can predict the development of POCD.

Altitude ; Altitude Sickness ; prevention & control ; Health Services Administration ; Humans

Objective To explore the diagnostic value of LUNX gene to marrow micrometastases of lung cancer.Methods To detect LUNX mRNA of marrow samples of 51 patients of lung cancer,4 patients of breast cancer,6 patients of lymphadenoma,3 patients of liver cancer and 22 patients of benign disease by real-time RT-PCR.Results The positive detection rate and meso-copies of lung cancer were 58.8% (30/51) and 35copies/ml respectively.The positive detection rate and meso-copies of other diseases were all 0,The positive detection rate and meso-copies of lung cancer was significantly higher than that of patients with other diseases (x~2=11.12,U_c=3.7329,P