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

Bone Density Conservation Agents ; therapeutic use ; Bone Neoplasms ; complications ; drug therapy ; secondary ; Breast Neoplasms ; pathology ; Diphosphonates ; therapeutic use ; Female ; Humans ; Male ; Pain ; drug therapy ; etiology ; Prostatic Neoplasms ; pathology ; Quality of Life

This paper aims to develop a method for the determination of aloe-emodin, rhein, chrysophanol and physcion and study the pharmacokinetic properties of four anthraquinones in rat plasma after oral administration of gardenia and rhubarb decoction. The plasma concentrations at different time points of four anthraquinones were determined by HPLC-FLD method. Plasma samples were extracted with liquid-liquid extraction procedure. Plasma samples were separated on a C18 column (4.6 mm x 150 mm, 5 μm), using 0.2% acetic acid and methanol as mobile phase at a flow rate of 1.0 mL min(-1) with gradient elution. The excitation and emission wavelengths were set at 430, 525 nm, respectively. DAS 2.0 software was applied to calculate the pharmacokinetic parameters. The results showed four anthraquinones can be absorbed. The main parameters of aloe-emodin, rhein, chrysophanol and physcion were as follows: C(max) for aloe-emodin was (0.085 ± 0.058), (3.772 ± 1.152), (0.464 ± 0.267), (0.028 ± 0.008) mg x L(-1) respectively; t(max) for rhein was (1.042 ± 0.510), (0.805 ± 0.307), (1.167 ± 0.283), (0.616 ± 0.162) h respectively; t½ for chrysophanol was (3.557 ± 1.250), (6.879 ± 1.126), (5.196 ± 2.032), (4.337 ± 1.816) h; AUC(0-t) for physcion was (0.504 ± 0.130), (9.558 ± 1.106), (2.545 ± 1.554), (0.052 ± 0.018) mg x h x L(-1). This paper developed a selective, accurate and sensitive HPLC-FLD method for the simultaneous determination of four anthraquiones in rat plasma.
Animals ; Anthraquinones ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; instrumentation ; methods ; Drugs, Chinese Herbal ; analysis ; pharmacokinetics ; Male ; Rats ; Rats, Sprague-Dawley

Adult ; Dimethylformamide ; poisoning ; Female ; Humans ; Occupational Exposure ; Young Adult

· Vascular endothelial growth factor is indispensable inducing factor in retinalangiogenesis. After the retinal neovascularization of proliferative diabetic retinopathy ( PDR ) patients, it can cause fibrovascular membrane formation, epiretinal membrane fibrosis increased, resulting in traction retinal detachment with further aggravate the condition. The recent research suggests that cytokines promote fibroblast proliferation, movement, adhesion, and secretion of extracellular matrix functions in the diabetic state of the environment changes to profibrogenic state, resulting in the accumulation and fibrosis of extracellular matrix. This paper reviewed the status quo of the correlation between vascular endothelial growth factor and fibrosis-related cytokine.

Objective To investigate the correlation between dose volume histogram(DVH)of tumor targets and organs at risk(OAR)at CT-image based 192Ir brachytherapy and effects and complications for patients with locally advanced cervical cancer. Methods Ten patients with FIGO stage ⅢB cervical cancer received CT image-based 192Ir intracavitary brachytherapy after 54 Gy of three-dimentional four-field pelvic external beam radiotherapy and concurrent weekly cisplatin chemotherapy. Before each brachytherapy,CT images were acquired with applicators in place. Gross tumor volume(GTV), clinical target volume (CTV)and OAR were contoured and inverse treatment planning was designed and optimized by using PLATO treatment planning system. Conventional two-dimensional plans were also designed for comparison.The total intracavitary brachytherapy dose was 30 -42 Gy in 5 -7 fractions. The patients were followed, and the local control and complications were analyzed. The biologically equivalent dose(BED)and biologically equivalent dose in 2 Gy fractions(BED2)for GTV, CTV and OAR were calculated. The minimum dose in the most irradiated tissue volume 2 cm3(D2 cm3)adjacent to the applicator of the sigmoid colon, rectum,bladder and small bowel was determined from the DVH. Results The 1-year local pelvic control rate was 90% and grade 1-2 late complication of sigmoid colon and rectum was 50%. No grade 3 or more complications developed. On CT-image based planning, the BED and BED2 to 90% of the CTV(D90)were 95.50 Gy ± 7. 81 Gy and 79. 73 Gy ± 6. 57 Gy. The BED and BED2 to 90% of the GTV(D90)were 101.86 Gy ± 7.27 Gy and 84. 95 Gy ± 6. 1 Gy. The volume enclosed by 90% of prescribed dose(V90)for GTV and CTV were 92% ±4% and 87% ±7% respectively. The D2cm3 for rectum and sigmoid colon were 74. 97 Gy ±1.64 Gy and 67. 93 Gy ± 4. 30 Gy(EQD2, α/β = 3). Comparing with 2D brachytherapy plans , CT - image based planning has improved D90 and V90 for GTV and CTV with similar dose at point A and rectum reference point. Conclusions Computer tomography-image based 192Ir brachytherapy has resulted in the better dose distribution to the tumor targets with excellent tumor control and acceptable toxicity.

In the basis of a large amount of literatures, this article sumed up the characteristics and application of eggshell membrane.

Objective To investigate the relation between the cellular immune function and unexplained recurrent spontaneous abortion(URSA) and the mechanism of active immunotherapy on URSA patients.Methods The flow cytometry(FCM) was used to detect CD3+ ,CD4+ ,CD8+ T lymphocyte and CD16+CD56+ natural killer(NK) cell subsets and the ratio of CD4+/CD8+ of peripheral blood(PBL).112 cases with URSA(76 cases treated with active immunotherapy) and 30 cases of normal fertiled(NF) women were studied.The percentages of T lymphocyte and NK cell subsets before and after therapy were compared among 76 cases wtih URSA treated by active immunotherapy.The rate of next successful pregnancy of URSA patients treated with and without active immunotherapy was compared.Results The percentages of CD3+ and CD16+CD56+ cell subsets as well as the ratio of CD4+/CD8+ of the URSA patients were significantly higher than those of NF cases(P <0.05).After active immunotherapy,the percentages of CD3+ and CD56+CD16+ cell subsets as well as the ratio of CD4+/CD8+ of URSA cases were significantly decreased(P <0.05 ).The rate of next successful pregnancy of URSA cases with and without active immunotherapy were 88.2% and 31.2% respectively,the difference was significant(P< 0.05).Conclusion The changes in the percentages of T lympyocyte and NK cell subsets have something to do with URSA.Active immunotherapy can effectively regulate the cellular immune function and increase the rate of next successful pregnancy of URSA patients.

ObjectiveTo explore the etiology, comolication a nd causes of death of hospitalized preterm infants. MethodsM aternal and neonatal medical records of 834 hospitalized preterm infants from Ja nuary 1991 to Decembre 2001 were reviewed.ResultsThe statist ics showed that there was an increased tendency of hospitalized preterm infants year by year. Most of them have a definite etiology of prematurity. There were m ore cases hospitalized in winter than in other seasons. 87.6% of preterm infants were associated with different complications. The morbidity of cold injury, pne umonia, recurrent apnea and intracranial hemorrhage declined in last 6 years. Si xty-four babies died, the mortality rate was 7.7%. The smaller the gestational age and birth weight was, the higher the mortality would be. The risk factors of death were birth weight, gestational age, Apgar score at 1 minute after birth, pulmonary hemorrhage and hyaline membrane disease.Conclusion It is important to enforce the perinatal health care and the co-operation of ob stetricians and pediatricians to reduce the complications of prematurity. We sho uld set up a well organized district perinatal transport system, raise the effic iency of rescue management, reduce the mortality and improve the prognosis of pr eterm infants.

Objective To explore the incidence and clinical characteristics of Han and Uygur pa- tients with ulcerative colitis(UC)in xinjiang.Methods Six hundred and ninty nine patients with UC from 2000 to 2006 were retrospectively reviewed.Patients were divided into 2 groups according to ethnic back- ground,including 522 Han patients and 177 Uygur patients.General data,age,clinical manifestation,le- sion range,lesion degree and complications were recorded in the 2 groups respectively.Results The detec- tion rate of UC by endoscopy in Urgur group was higher than that in Han group(P