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.Degradation of AZ31 magnesium alloysin vivo:micro-CT assessment
Yichi XU ; Heyong YIN ; Zhen SUN ; Haoye MENG ; Bo XIAO ; Aiyuan WANG ; Quanyi GUO ; Jiang PENG ; Shibi LU
Chinese Journal of Tissue Engineering Research 2016;20(16):2303-2309
BACKGROUND:Magnesium can be degraded voluntarily in vivo, so a second surgery is avoided. However, its aloys have not been widely used in the clinical orthopedics because there is a lack of accurate and reliable methods to assess its degradationin vivo.
OBJECTIVE:To explore the degradation of micro-arc-oxidized AZ31 magnesium aloy in the femoral condyle of rabbits based on micro-CT images and relative data.
METHODS:Forty micro-arc-oxidized AZ31 magnesium aloys were implanted into the right femoral condyle of 40 New Zealand rabbits. Then 10 right femoral condyles were removed at 5, 10, 15 and 20 weeks after surgery, respectively, to quantitatively analyze and evaluate the degradation of AZ31 magnesium aloys by micro-CT images and relative data.
RESULTS AND CONCLUSION:The surface of AZ31 aloys was corroded progressively with dark color and distorted appearance at 5-20 weeks post implantation. Micro-CT images showed that in the first 5 weeks, the degradation was inactive, and at the 10th week, it turned active; at the 15th week, the corrosion pits were obviously increased in number, and the corrosion area and corrosion speed were enlarged and fastened, respectively. Up to the 20th week, the aloy surfaces were ful of corrosion pits besides roughness and discontinuity. Relevant data analysis showed that the volume fraction of magnesium aloy was 98.6%, 97.1% and 86.4% at the 5th, 10th and 20th weeks after implantation, respectively, and it had a significant decrease from the 10th to 15th week and from the 15th to 20th week (P < 0.05). Within 15-20 weeks, the volume fraction of magnesium aloy was decreased by 6.5% that was the maximum volume reduction per unit cycle. With the progress of corrosion, the surface continuously became rough and vague, and its surface area was enlarged; the ratio of surface area to volume continuously increased, and there was a significant difference at 15 and 20 weeks (P < 0.05). Because of the increasing number of corrosion pits, the cross-sectional radius decreased, which was reflected by the trabecular thickness decreasing from 1.00 to 0.87 mm. From the view of the slope of curve, the trabecular thickness decreased most rapidly at 10-15 weeks. The mineral density of magnesium aloy continuously decreased from 649.302 to 356.445 mg/cm3 during the whole experiment period (P< 0.05). In addition, the micro-CT image density decreased from 679.710 to 644.947 mg/cm3, but there was no significant difference. To conclude, the degradation speed is peaked at 10-20 weeks after implantation, and the content of magnesium aloys decrease with degradation, but the magnesium density has no significant change.
10.Clinicopathological features and molecular genetic analysis of endolymphatic sac tumor: report of 2 cases.
Qiu RAO ; Xiao-jun ZHOU ; Xing-zao JIN ; Heng-hui MA ; Hang-bo ZHOU ; Zhen-feng LU
Chinese Journal of Pathology 2010;39(6):412-413
Adenoma
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metabolism
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pathology
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Adult
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Carcinoma, Renal Cell
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metabolism
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pathology
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Diagnosis, Differential
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Ear Neoplasms
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complications
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genetics
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metabolism
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pathology
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surgery
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Endolymphatic Sac
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Female
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Follow-Up Studies
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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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Middle Aged
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Paraganglioma
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metabolism
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pathology
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Point Mutation
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Von Hippel-Lindau Tumor Suppressor Protein
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genetics
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von Hippel-Lindau Disease
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complications
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genetics
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metabolism