2.Advances in nanocrystal technology and its application to improve the pharmacological efficacy for poorly-water soluble drugs
Xiao-xue LIU ; Jun-bo GONG ; Zhen-ping WEI
Acta Pharmaceutica Sinica 2021;56(12):3431-3440
In order to solve the problems of erratic drug absorption and low bioavailability after oral administration for poorly-water soluble drugs due to low solubility, a series of novel pharmaceutical dosage forms as solid dispersion, liposome, microemulsion, vesicle, cyclodextrin inclusion complexes and drug nanocrystal have been developed in recent years. Among which drug nanocrystal attracts more attentions for its simpler preparation method, higher drug loading and easier manufacturing technology in the design of dosage forms suitable for different administration routes. In this paper, the nanocrystals of the poorly-water soluble drugs prepared based on bottom-up and top-down technologies were introduced. The characteristics and applications of the nanocrystal-based dosage forms as suspension, tablet and capsule were also introduced and carefully evaluated with the focus on their pharmacokinetics, pharmacodynamics and tissue targeted drug distribution after delivery by oral administration, intravenous injection and pulmonary inhalation. The advantages of drug nanocrystals in their therapeutics effects over the bulk drugs were discussed together with the inherent mechanism. Finally, the problems existing in basic research and scaled-up manufacture of drug nanocrystal as well as the possible ways of solution were listed out so as to make the nanocrystal-based preparations exert their maximum therapeutic effect after clinical application.
3.Research on ultrafine grinding technology of improving dissolution rates of effective components in Sanjie Zhentong capsule.
Zhong-kun XU ; Jin GAO ; Jian-ping QIN ; Guang-bo CHEN ; Zhen-zhong WANG ; Wei XIAO
China Journal of Chinese Materia Medica 2015;40(10):1945-1947
The effects of ultrafine grinding on the dissolution rates of the effective components in Sanjie Zhentong capsule (SZC) were studied in this experiment. Fine and ultrafine powder of SZC intermediates were made by ordinary grinding and ultrafine grinding technology, and then granulated by wet granulation. SZC were prepared by fine powder, ultrafine powder and ultrafine granules, respectively. With resveratrol and loureirin B as investigated indexes, dissolution rates of the four intermediates in SZC were determined by cup method and HPLC. The dissolution rates of resveratrol in SZC prepared by fine powder, ultrafine powder and ultrafine granules were 26.11%, 63.27%, 67.49%, respectively; and the dissolution rates of loureirin B were 7.160%, 20.29%, 23.05%, respectively. The dissolution rate of resveratrol and loureirin B in SZC prepared by ultrafine granules was the best. D90 size of ultrafine grinding was 13.221 μm and could improve the dissolution rates of resveratrol and loureirin B in SZC.
Capsules
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chemistry
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Drugs, Chinese Herbal
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chemistry
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Particle Size
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Silicones
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chemistry
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Solubility
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Technology, Pharmaceutical
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methods
4.Effect of levetiracetam as an add-on to partial seizure on cognitive function and quality of life
Bo ZHOU ; Dong ZHOU ; Lin-Yu TIAN ; Zhen HONG ; Jun XIAO ;
Chinese Journal of Neurology 2001;0(03):-
Objective To explore the effect of levetiracetam(LEV)on cognitive function and quality of life of patients with partial seizure.Methods There were two phase for this study.Phase one was a randomized,double-blind,placebo-controlled study for 16 weeks.Phase two was an open label period for 24 weeks.Medicated patients underwent test on the cognitive function and Health Related Quality of Life (HRQOL)at the baseline respectively at the end of 16 weeks and at the end of 40 weeks.Results(1) Compared the result at the end of 16 weeks with the baseline,LEV group used less time to do Wisconsin card sorting test(WCST,reduce scores -110.3),delayed logical memory were improved(reduce scores 3.4,P
5.Percutaneous pinning internal fixation for the treatment of old distal radius fractures.
Xiao-bo WANG ; Bo LIU ; Zhen-guo DAI ; Wei-yuan LI
China Journal of Orthopaedics and Traumatology 2008;21(9):686-687
Adult
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Aged
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Bone Nails
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Female
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Follow-Up Studies
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Fracture Fixation, Internal
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instrumentation
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Humans
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Male
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Middle Aged
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Radiography
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Radius Fractures
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diagnostic imaging
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physiopathology
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surgery
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therapy
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Skin
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Treatment Outcome
6.Comparison of curative effect between two mesh suspensions in treating female stress urinary incontinence
Ling HONG ; Huai-fang LI ; Jing SUN ; Xiao-ming TENG ; Kun-ming LI ; Bo-zhen FAN ; Xiao-wen TONG ;
Journal of Chinese Physician 2010;12(4):433-436
ObjectiveTo evaluate the curative effect difference between Tong's anterior mesh suspension and modified tension-free vaginal tape-obturator (TVT-O). Methods75 SUI cases were random divided into two groups: Group A (35 cases) were accepted Tong's anterior mesh suspension and group B (40cases) were accepted modified tension-free vaginal tape- obturator. Curative effects, operation safety,and complications and so on, were recorded and compared. ResultsThere had no statistical differences between these two groups on operation time, bleeding lose, operation injury, immediate postoperative urinary retention andcure rates, but the operation expense of group A was cheaper than group B [ (980. 74 ±212.45)yuan vs (2879.06 ±467. 13)yuan , P <0.05). ConclusionThe curative effect between two methods were similar. It's a little complicated and fit to be popularized in large hospital to modified tensionfree vaginal tape-obturator. Tong's anterior mesh suspension was performed under completely direct vision,not through pelvic cavity, and it was an economic, convenient and easy way, which not only fit to be popularized in basic hospital, but also a surgical remedial measure to the failures who accepted these operations,such as TVT, SPARC, IVS, MONARC, TOT, TVT-O, etc.
7.Evaluation of an immunohistochemcal combination for diagnosis of prostate adenocarcinoma
Xiao-Hua LE ; Xiao-Jun ZHOU ; Min-Hong PAN ; Hang-Bo ZHOU ; Zhen-Feng LU ; Ji-Zhou GOU ;
Chinese Journal of Primary Medicine and Pharmacy 2006;0(10):-
0.05).Conclusion The immunohistoehemical combination of P504S,PSA,PAP,p63 and 341?E12 is a good adjuvant method to diagnose prostate adenocarcinoma.
8.Effect of small interfering RNA targeting Rac1 gene on colony formation of SW480 cells in vitro.
Qing-zhen NAN ; Lei GAO ; Bing XIAO ; Zhen-shu ZHANG ; Bo JIANG
Journal of Southern Medical University 2010;30(6):1339-1342
OBJECTIVETo construct a vector expressing small interfering RNA (siRNA) against Rac1 gene and observe its effect on soft agar colony formation of SW480 cells in vitro.
METHODSOligos of 64 base pairs for hairpin RNA targeting Rac1 were chemically synthesized and annealed. The siRNA constructs for Rac1, produced by inserting the annealed oligos into the downstream of H1 promoter of linearized pSUPER, were confirmed by restriction digestion and DNA sequencing. The constructed Rac1-siRNA was transfected into SW480 cells and Western blotting was performed to assess the expression and interference efficiency of siRNAs against Rac1.The soft agar colony formation assay was used to study the effect of Rac1 gene silencing on SW480 cells.
RESULTSRestriction digestion and DNA sequencing showed that the siRNA targeting Rac1 gene was successfully constructed. The siRNA could effectively down-regulate the expression of Rac1 in SW480 cells. Soft agar colony formation assay showed that the colony number and diameter of SW480 cells was reduced after siRNA transfection.
CONCLUSIONA vector expressing hairpin RNA against Rac1 gene are successfully produced, which significantly reduces the colony numbers and size of SW480 cells in vitro, suggesting that Rac1 plays an important role in the growth of colorectal cancer in vitro.
Base Sequence ; Cell Line, Tumor ; Cell Proliferation ; Colonic Neoplasms ; pathology ; Down-Regulation ; Humans ; Molecular Sequence Data ; RNA Interference ; RNA, Small Interfering ; genetics ; Transfection ; rac1 GTP-Binding Protein ; genetics
9.Inhibitory effects of cyclooxygenase-2 selective inhibitor Celecoxib on human nephroblastoma.
Xiao-li HU ; Lin-sheng ZHAO ; Wei LIU ; Jian-bo SHU ; Li XU ; Zhen-fang WANG
Chinese Journal of Pathology 2012;41(5):340-341
Celecoxib
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Cell Cycle
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drug effects
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Cell Line, Tumor
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Cell Proliferation
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drug effects
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Cyclin-Dependent Kinase Inhibitor p16
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genetics
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metabolism
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Cyclin-Dependent Kinase Inhibitor p21
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genetics
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metabolism
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Cyclooxygenase 2 Inhibitors
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administration & dosage
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pharmacology
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Dose-Response Relationship, Drug
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Humans
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Kidney Neoplasms
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metabolism
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pathology
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Pyrazoles
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administration & dosage
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pharmacology
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RNA, Messenger
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metabolism
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Sulfonamides
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administration & dosage
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pharmacology
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Wilms Tumor
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metabolism
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pathology
10.Granulocytic sarcoma: a clinical and pathologic analysis of ten cases.
Zhen-bo HOU ; Huai-yin SHI ; Xiao LIANG ; Xin-mei WANG
Chinese Journal of Pathology 2012;41(5):331-334
OBJECTIVETo investigate the clinical and pathological features, differential diagnosis of granulocytic sarcoma.
METHODSThe clinical manifestations, histopathological features, immunohistochemistry, treatment and prognosis were analyzed retrospectively in 10 cases of granulocytic sarcoma.
RESULTSThe age of patients ranged from 10 to 56 years (means = 35.8 years). The male-to-female ratio was 1.5:1. Histologically, the malignant cells of granulocytic sarcoma grew in a diffuse pattern. The cytoplasm was scanty, with eosinophilic fine granularity in some cells. The nuclei were round or focally irregular, and had finely dispersed chromatin. The mitotic figures were visible. Immunohistochemical stains for MPO, CD43, CD117, CD34 and CD99 were positive.
CONCLUSIONSGranulocytic sarcoma can occur in patients of all ages with a male predominance. The diagnosis of granulocytic sarcoma is assisted by the cytochemical stain for naphthol-ASD-chloroacetate esterase and/or immunophenotypic analyses for MPO, CD43, CD117, CD34, CD99. These stains aid in the distinction of granulocytic sarcoma from: lymphoblastic lymphoma, Burkitt lymphoma, diffuse large B-cell lymphoma, small round cell tumours, particularly in children, and blastic plasmacytoid dendritic cell neoplasm.
12E7 Antigen ; Adolescent ; Adult ; Antigens, CD ; metabolism ; Antigens, CD34 ; metabolism ; Burkitt Lymphoma ; metabolism ; pathology ; Cell Adhesion Molecules ; metabolism ; Child ; Dendritic Cells ; metabolism ; pathology ; Diagnosis, Differential ; Female ; Follow-Up Studies ; Humans ; Immunohistochemistry ; Leukosialin ; metabolism ; Lymphoma, Large B-Cell, Diffuse ; metabolism ; pathology ; Male ; Middle Aged ; Peroxidase ; metabolism ; Precursor Cell Lymphoblastic Leukemia-Lymphoma ; metabolism ; pathology ; Proto-Oncogene Proteins c-kit ; metabolism ; Retrospective Studies ; Sarcoma, Myeloid ; metabolism ; pathology ; Skin Neoplasms ; metabolism ; pathology ; Young Adult