1.Polymorph transformation of solid drugs.
Acta Pharmaceutica Sinica 2015;50(5):521-527
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
4.Simultaneous determination of four anthraquinones in rat plasma by HPLC-FLD method and its pharmacokinetic study.
Jin-Qiu HUANG ; Xue-Mei YAN ; Fang FENG
China Journal of Chinese Materia Medica 2014;39(19):3850-3854
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
5.Research the correIation of vascuIar endotheIiaI growth factor and fibrosis -reIated cytokines in proIiferative diabetic retinopathy
Mei-Qi, WEI ; Xiao-Long, CHEN ; Xue-Mei, FENG ; Hong-Wei, YANG ; Chun-Liu, GAI
International Eye Science 2015;(3):454-458
· 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.
6.Clinical effect of anterior vitrectomy for congenital cataract
Hua, HE ; Feng, ZHOU ; Qi, ZHU ; Qian, WANG ; Xue-Mei, WU ; Jian, MA ; Ya-Yun, WANG
International Eye Science 2015;(5):825-827
?AlM: To evaluate the clinical efficacy of posterior continuous curvilinear capsulorhexis ( PCCC ) combined with anterior vitrectomy in preventing posterior capsule opacification of congenital cataract surgery.
?METHODS:Postoperative clinical follow-up data of 82 cases ( 87 eyes ) with congenital cataract treated in Eye Center of our hospital from January 2011 to August 2014 were retrospectively analyzed. The patients were divided into the surgical control group ( 38 cases, 40 eyes, recieved phacoemulsification + PCCC ) and the study group ( 44 cases, 47 eyes, accepted phacoemulsification+ PCCC + anterior vitrectomy). The incidence of central optic axis opaque and postoperative visual acuity distribution were recorded at 1a follow - up. lntraoperative and postoperative complications were observed.
?RESULTS:The rate of central optic axis opaque grade 0 in control group was 37. 5%, compared to 76. 6% in study groups. The opacity distribution ratio of grade 1,2,3 and 4 in study group were lower than that of control group, and the central optic axis opacity distribution ratio in study group was significantly better than that of control group (P<0. 05). The 19 eyes(47. 5%) of visual acuity testing ≤0. 5 in control group , was higher than the 7 eyes(14. 89%) of that in the study group, The 21 eyes (52. 5%) of visual acuity testing >0. 5 in control group was lower than the 40 eyes ( 85. 11%) of that in study group. The visual acuity between two groups has statistical significance difference after 1a follow-up ( P<0. 05 ) , and the visual acuity in study group was significantly better than that in the control group. The postoperative intraocular pressure at 1mo and 1a follow-up was lower than before operation in two groups ( P<0. 05), but there was no significant difference between two groups in intraocular pressure (P<0. 05).
?CONCLUSlON: Combination of phacoemulsification, PCCC and anterior vitrectomy presents reliable clinical effects on postoperative central optic axis opacity distribution ratio and visual acuity, and it should be adopted to prevent the occurrence of posterior capsule opacification.
7.Clinical observation of endogenous endophthalmitis caused by liver abscess
Chun-Liu, GAI ; Xue-Mei, FENG ; Xiao-Long, CHEN ; Lei, SHI
International Eye Science 2011;11(6):951-953
AIM: To analyze the clinical feature and treatment of endogenous endophthalmitis caused by liver abscess. METHODS: A total of 9 eyes (7 cases) with endogenous endophthalmitis caused by liver abscess in our hospital from 2005 to 2010 were analyzed retrospectively. Microorganism was cultivated with blood or vitreous in all patients.4 eyes were performed vitrectomy. 2 eyes were injected antibiotics in vitreous cavity. 3 eyes were only treated with antibiotics.RESULTS: Two cases (2 eyes) were diagnosed with endophthalmitis firstly, then found liver abscess; 4 eyes were with diabetes mellitus, and 1 eye with abnormal glucose tolerance. Cultivation of microorganism was positive in 6 eyes (67%), including Pneumonia cray-research, Candida albicans and Escherichia coli. 5 eyes had useful vision after treatment, 1 eye had light perception,3 eyes became blindness. CONCLUSION: As an ocular emergency, endogenous endophthalmitis caused by liver abscess can severely damage visual function. Timely consultation, early diagnosis, proper systemic and topical anti-infective and anti-inflammatory treatment are the most effective methods for controlling infection. Vitrectomy with intravitreal antibiotics plays an important role in preserving useful vision function in patients.
8.Overview of Pharmacological Research on Eggshell Membrane
Jiang GONG ; Shi-feng NI ; Xue-mei ZHANG ; Jia QU ; Rong-fang LUO ; Zhi-xuan LI ;
International Journal of Traditional Chinese Medicine 2009;31(2):187-188
In the basis of a large amount of literatures, this article sumed up the characteristics and application of eggshell membrane.
9.The relation between cellular immune function and unexplained recurrent spontaneous abortion
Yong-feng ZHANG ; Lan XU ; Mei-ru YANG ; Xue-jiao YANG ;
Chinese Journal of Primary Medicine and Pharmacy 2008;15(11):1807-1809
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.
10.Influence of statins on antiplatelet effects of clopidogrel
Hongsong ZHANG ; Mingyuan LIU ; Mei HAN ; Feng CHEN ; Jincheng ZHAO ; Xue BAI ; Yu YANG ; Guangyuan YANG
Chinese Journal of cardiovascular Rehabilitation Medicine 2015;24(5):543-546
Objective:To observe influence of statins on antiplatelet activity of clopidogrel and provide basis for ra‐tionality of statins combined clopidogrel treatment .Methods :According to random number table ,a total of 90 pa‐tients diagnosed as acute coronary syndrome were equally divided into clopidogrel group ,clopidogrel + simvastatin group and clopidogrel + pravastatin group . Three groups received corresponding routine medication treatment . Plasma levels of platelet αgranule membrane protein (CD62P) ,lysosomal granule membrane glycoprotein (CD63) and maximum platelet aggregation rate (MPAR) were measured and compared among three groups before and 3d af‐ter treatment .Results:Compared with before treatment ,after treatment ,there were significant reductions in plas‐ma levels of CD62P and CD63 and MPAR in three groups , P<0.01 all .After treatment ,there were no significant difference in plasma levels of CD62P [ (14.63 ± 3.45) ng/ml vs .(14.14 ± 4.32) ng/ml vs .(14.59 ± 4.23) ng/ml] , CD63 [ (26.32 ± 10.43) ng/ml vs .(27.04 ± 10.75) ng/ml vs .(27.29 ± 9.27) ng/ml] and MPAR [ (28.62 ± 17.68)% vs .(28.38 ± 16.43)% vs .(29.13 ± 14.23)% ] among clopidogrel group ,clopidogrel + simvastatin group and clopidogrel + pravastatin group ,P>0.05 all .Conclusion:Short‐term and routine dose of statins combined clo‐pidogrel is feasible in treatment of acute coronary syndrome .The combined use of them will not affect antiplatelet function of clopidogrel .