1. Studies on transdermal delivery of sinomenine hydrochloride through mouse skin treated by microneedle arrays
Academic Journal of Second Military Medical University 2011;32(7):767-771
Objective: To study the characteristics and mechanism of transdermal delivery of sinomenine hydrochloride (SH) through mouse skin treated by solid silicon microneedle arrays. Methods: The amount of SH was determined by HPLC system. Hairless rat skin was pretreated with microneedle arrays. The side-by-side diffusion cell method was used to investigate the effects of needlepoint shape, different insertion forces, retention time, and number of microneedles on transdermal SH delivery. Skin samples treated by microneedles were made into paraffin sections for histological examination and were viewed by brightfield microscopy. Results: The skin pretreated with microneedle arrays had a remarkable enhancement of SH transport compared with passive diffusion group (P<0.01); the flat tipped microneedles were more effective than the sharp tipped microneedles in enhancing the skin permeability. The accumulation of SH increased with the enhancement of insertion force; however, when the insertion force exceeded 5.0 N, the accumulation of SH no longer increased. The skin permeability was enhanced with the increase of retention time; when the retention time exceeded 1.0 min, it no longer increased SH accumulation. Although skin permeability increased with the microneedle number, there was no linear correlation was found. Histological examination showed that microneedle piercing created micro-conduits in skin. Conclusion: Microneedles can create conduits in rat skin and greatly increase the skin permeability of SH; microneedle arrays provide an efficient and promising technology for transdermal drug delivery of SH.
2. Solution of camphor volatility in industrialized preparation of cataplasm based on inclusion technology of HP-β-CD
Chinese Traditional and Herbal Drugs 2020;51(4):965-970
Objective: To reduce or avoid the volatilization loss of camphor (CA) in the industrialized preparation of cataplasm, using the inclusion technology of HP-β-CD. Methods: The HP-β-CD inclusion compound of CA (CA-HP-β-CD) was prepared by the constant temperature stirring method. The preparation processing of CA-HP-β-CD was optimized with inclusion efficiency as an index, and the pharmaceutical properties of CA-HP-β-CD were characterized by DSC, UV and SEM. The CA and CA-HP-β-CD were prepared to cataplasm at the industrial-scale production respectively, then the content of CA was determined and the statistical analysis was carried out. Results: The inclusion efficiency of CA-HP-β-CD for CA was (68.57 ± 1.26)% when the CA-HP-β-CD was prepared with the mass ratio of CA to HP-β-CD 1:3, the working temperature at 35 ℃ and stirring at 300 r/min for 4.0 h. The DSC, UV and SEM scans showed that there was a good compatibility between CA and HP-β-CD, and CA could be fully encapsulated by HP-β-CD and formed a stable inclusion complex of CA-HP-β-CD. Results of industrial-scale production of cataplasm for CA and CA-HP-β-CD revealed that the retention rate (actual content/feeding quantity) were (80.13 ± 1.05)% and (39.45 ± 1.38)%, respectively. And there was a statistically significant difference between them (t-test, P < 0.01), indicating that the HP-β-CD inclusion complex effectively reduce the volatilization loss of camphor CA. Conclusion: The volatilization loss of CA at the industrial-scale production of cataplasm was effectively reduced by the CA-HP-β-CD, which improves the utilization rate of CA and reduces the cost, and provides ideas and reference for the research and development of cataplasm of volatile drugs.
3. Application of micellar solubilization technology in pilot production of Chinese materia medica cataplasma containing volatile oil
Chinese Traditional and Herbal Drugs 2013;44(19):2677-2682
Objective: Through the studies on pilot production of the cataplasma of Chinese materia medica (CMM) containing volatile oil, to provide a rational and feasible preparation technology for the pilot production of CMM cataplasma, so as to promote the development of CMM cataplasma. Methods: The CMM containing volatile oil was extracted by steam distillation method (SDM), ethanol reflux extraction (ERE), and CO2 supercritical fluid extraction (SFE), respectively. The extracts were prepared to cataplasma in order to investigate the effects of extracting methods on the preparation process and quality of CMM cataplasma. The effects of micellar solubilization in the distilled liquid of STM on the quality of cataplasma such as adhesiveness, flexibleness, and stability were also investigated. Results: There was the significant difference among the groups of STM, ERE, and SFE on the quality of cataplasma. The extract by STM was beneficial to the preparation process and enhancement of the quality of cataplasma obviously, while the distilled liquid by STM would cause some limitations such as oil-water separation and volatile oil volatilization losses, which could contribute to obvious difference among batches. These disadvantages by STM would be overcome by the adoption of micellar solubilization technology and the stability would be increased (P < 0.01); segregation happened for the extract by ERE at room temperature, thereby, the water bath heating was needed in the preparation; this characteristics would cause the homogeneous appearance of cataplasma due to some black spots, lower flexibleness of matrix, and the preparation was not easy to control; the extract by SFE contained a lot of impurity of grease and performed half solid. As a result, it was very difficult to blend the extract by SFE with other materials uniformly, the adhesive force of cataplasma was also reduced. In addition, the cost of higher energy consumption and production was another disadvantage for SFE. Conclusion: The STM followed by micellar solubilization would be a feasible preparation technology for the pilot production of CMM cataplasma containing volatile oil, so it is worth popularizing and applying widely.
4.Clinical research of ureteral replacement using the Yang-Monti principle
Wei SHI ; Ze QIN ; Junsheng BAO ; Ye LI ; Li DONG
Chinese Journal of Urology 2017;38(5):367-370
Objective We summarized the clinical experience of modified ileal ureter substitution for treating long segment ureteral defection.Methods We retrospectively analyze the clinical data of 2 patients with long segment ureteral defect who treated with Yang-Monti ileal ureter substitution between March 2015 and November 2015.One 75 years old male patient was diagnosed as upper ureteral malignance and solitary kidney.The length of defection from renal pelvis to bladder was 22 em.His serum creatinine was 100 μmol/L,blood urea nitrogen was 5.7 mmol/L,serum chloride was 98 mmol/L.Another one 41 years old female patient was diagnosed as middle and lower ureteral iatrogenic injury.The traumatic length was 15 cm.Her serum creatinine was 70 μmol/L,blood urea nitrogen was 5.1 mmol/L,serum chloride was 100 mmol/L.they were both treated by Yang-Monti ileal ureter substitution.The ileal intestinal segment was used for the ureteral replacement,which were more than 15 cm to the ilealcecum.The length of intestine was 10.0 cm and 7.5 cm,respectively.The ileal mesentery was preserved.After closing the mesangial hiatus,the ileal segment was pull into the retroperitoneal space and pulling out via descending colonic mesangial window.The ileal segment was divided into three parts,which was 2.5 to 3.0 cm in each part.Each part was opened via long axis and then rotated 90 degree.The 4-0 absorable suture was used to suture the edge of each intestinal part continuously.The sutured intestine was re-tubularized,using 4-0 absorable suture and the F16 catheter was used as the tube model.The length of reconstructed ureter was 22 cm and 18 cm,respectively.The neo-ureter was re-anastomosed with renal pelvis and bladder wall.Two F6 double J stents were placed in the neo-ureter.Results The operative time was 160 min and blood loss was 200 ml in the first case.In the second case,the operative time was 180 min and blood loss was 220 ml.No significant complications were noticed intra-operation and post-operation.Six months after operation,the male patient's serum creatinine was 112 pmol/L,blood urea nitrogen was 6.1 mmol/L,serum chloride was 106.0 mmol/L and electrolytes were normal.In another patient,serum creatinine was 79 μmol/L,blood urea nitrogen was 5.9 mmol/L and serum chloride was 103.0 mmol/L.The GFR was 24.9 ml/min and 22.1 m]/min 3 and 6 months after operation,respectively.Ureteral obstruction wasn't detected on IVU images 3 months after operation.Conclusions For patient with long ureteral defect,which cannot be replaced by other urinary tissue,YangMonti ileal ureter substitution is one of the optional modalities.As a new technique of ureteral substitution,Yang-Monti ileal ureter substitution is simple and fewer complications and can improve the quality of life in patient compared with traditional ureteral substitution.
5.Research progress of traditional Chinese medicine formulas and active compounds in the treatment of non-alcoholic fatty liver disease by regulating gut microbiota
Yan LI ; Wei-ze ZHU ; Hou-kai LI
Acta Pharmaceutica Sinica 2022;57(12):3451-3464
Non-alcoholic fatty liver disease (NAFLD) is one of the most common chronic liver diseases. However, due to its complex pathogenesis, there are no officially approved drugs for NAFLD treatment currently. Therefore, it is extremely urgent to find safe and effective anti-NAFLD drugs. Nowadays, lipid-lowering drugs are the main option for NAFLD therapy, but the clinical efficacy of chemical drugs is also very limited, as well as the frequent side effects or adverse reactions. Traditional Chinese medicine (TCM) has attracted more and more attention in the treatment of NAFLD due to its unique advantages through multiple targets and pathways with few side effects. In recent years, numerous studies have demonstrated that the imbalance of gut microbiota plays an important role in the occurrence and development of NAFLD. This review systematically summarizes the experimental and clinical evidences of TCM active compounds and TCM prescription involved in the regulation of intestinal flora in the treatment of NAFLD in recent years, so as to provide a reference for further exploring the pathogenesis of NAFLD and exploring TCM treatment methods.
6.Development of infusion remote-control system based on wireless data-transfer and ultrasonic acquisition
Duanyun PENG ; Zifeng CHENG ; Hongbo CHEN ; Zhanming LI ; Ze WEI
Chinese Medical Equipment Journal 2004;0(08):-
This paper introduces an infusion remote-control system based on wireless data-transfer.It can realize such functions as the accurate control of the infusion speed,humanized prompt,central monitoring,wardship and management.Ultrasonic adopted to detect the flux,the lower MCU can fulfill such functions as control,display and storage,which can also perform real-time wireless communication with the upper PC to facilitate remote control.
7.Observation of Differential Protein of Hypothalamus in the Hyperthyroidlsm Rats with Hyperactivity of Liver-Yang
Ling-Yan ZHOU ; Ze-Qi CHEN ; Wei LI ;
Chinese Journal of Information on Traditional Chinese Medicine 2006;0(05):-
Objective Utilization of proteome method,by observing differences on protein expression of hypothalamus in the hyperthyroidism rats with hyperactivity of liver-yang and normal rats,to search the differential protein.Methods Models of animal were prepared by ip L-T4 and Fuzi Decoction.Both the quantitative and qualitative changes of the protein expression were compared between model group and treated group by protein technique.Results Proteins were mainly displayed at range of pI 3~8,Mr(14.4~75)kD.18 protein increased and 24 protein decreased in model group compared with treated group, included Thioredoxin,Ubiquitin carboxyl-terminal hydrolase isozyme L1,Platelet-activating factor acetylhydrolase IB gamma subunit,glutamate dehydrogenase,dihydropyrimidinase-related protein 2, NSFL1 cofactor p47,Tubulin beta 5.Conc(?)sion There were 18 spots high expressed and 24 spots low expressed in the hyperthyroidism with hyperactivity of liver-yang,that maybe related with the develepment of the hyperthyroidism with hyperactivity of liver-yang.
8. Preparation of palmatine-loaded flexible nano-liposomes and their vaginal mucosa permeability in vitro
Chinese Pharmaceutical Journal 2015;50(24):2139-2145
OBJECTIVE: To prepare palmatine-loaded flexible nano-liposomes (PFNL) and study their pharmaceutical properties, in order to lay the foundation for the industral application. METHODS: The flexible nano-liposomes were prepared by thin-film homogenization method with propyleneglycol (PG) as softening agent. The entrapment rate of palmatine was evaluated by protamine aggregation method and HPLC. The effects of concentrations of phosphatidylcholine (PSC), cholesterol (CH), and PG on the entrapment efficiency of palmatine were also investigated. The pharmaceutical properties of PFNL were evaluated by TEM, PCS and CLSM. The deformation of PFNL was determined by its relative rate of permeating the microporous filter membrane. The coagulation rate constant (K) was measured by constant temperature conductivity method. The side-by-side diffusion cells and pig vaginal mucosa were used to investigate the characteristics of the release of palmatine from PFNL in vitro, and the effects of PFNL on the expression of cytokines (SLPI, LF and SP-D) were investigated and compared with classic liposomes and lotion of palmatine. RESULTS: The palmatine entrapment efficiency was (78 ±2.13)% when the PFNL were prepared with PSC (3%), CH (0.02%), and PG (20%). The prepared nano flexible liposomes had a closed spherical or elliptical shape and appeared as multi-lamellar vesicles under the TEM and CLSM. The calculated mean size was (185 ±19) nm, and the Zeta potential was (-53 ±2.27) mV. The deformation of PFNL was (79 ± 5.75)%. The coagulation rate constant (K) of PFNL was always lower than that of traditional palmatine- loaded liposomes. The accumulated permeation amount of palmatine from the PFNL at 6.0 h was 1.53 and 2.86 folds of those of classic liposomes and lotion, respectively. Moreover, the expressions of cytokines (SLPI, LF and SP-D) in female SD rats after being treated with PFNL, PCL and PL were similar to that of the control group. CONCLUSION: The prepared PFNL have high encapsulation efficiency, good stability and safety, and greatly increase the vaginal mucosa permeability of palmatine. Flexible nano-liposomes may be a useful drug delivery carrier for the gynecological application of palmatine.
9.Evaluation of eye injury degree of laser irradiation frequency and single duration
Yufei ZHANG ; Dongyu WEI ; Wei WANG ; Daming LIU ; Ze REN ; Xiangqian LI ; Tao CHEN ; Zuoming ZHANG
Chinese Journal of Experimental Ophthalmology 2021;39(3):184-190
Objective:To explore the effects of laser irradiation parameters (irradiation frequency and single duration) on tear secretion, lens and retina.Methods:Thirty-six healthy guinea pigs were randomly divided into 6 groups with random number table method according to different frequency and single exposure duration of laser to the eye, namely, high frequency short time (HFST) group, high frequency long time (HFLT) group, medium frequency short time (MFST) group, medium frequency long time (MFLT) group, low frequency short time (LFST) group and low frequency long time (LFLT) group, 6 for each group.The right eyes were irradiated with 500 lx laser as experimental eyes, and the left eyes of the guinea pigs served as the control eyes.The high, medium and low irradiation frequencies were defined as 15 times, 10 times and 5 times, respectively, and the short and long period was defined as 30 seconds and 60 seconds each time, respectively.The right eyes were irradiated based on the grouping at a 10-minute interval.The tear secretion was detected by SchirmerⅠtest; lens opacity was assessed under the slit-lamp microscope; fundus photography was performed to evaluate the general morphology of retina; retinal function was evaluated by electroretinogram (ERG) record and the thickness of retinal outer nuclear layer was measured by histopathology examination.This study protocol was approved by the Medical Ethics Committee of Air Force Military Medical University (No.20181203), and the use and care of the experimental animals complied with the ARVO statement.Results:The tear secretion was 8.00(7.37, 9.00), 8.75(8.25, 9.00), 8.50(7.75, 9.50), 9.00(8.50, 9.50), 8.00(7.37, 8.75) and 8.25(7.75, 8.75) mm/5 min in the HFST group, HFLT group, MFST group, MFLT group, LFST group and LFLT group, respectively, without significant difference among the groups(χ 2=5.502, P=0.240); after laser irradiation, there were no statistically significant differences in tear secretion between the control eyes and laser-irradiated eyes in all the groups (all at P>0.05). The lenses were clear and the fundus was normal through the experimental duration in all the groups.The amplitude of ERG a-wave was significantly reduced in the HFST group in comparison with the LFST group (P<0.05), and there was no significant difference in the b-wave amplitude among the six groups (F=1.358, P=0.268). The ERG a-, b-wave amplitudes were not significantly different between the control eyes and laser-irradiated eyes in various groups (both at P>0.05). There was no significant difference in the thickness of the outer nuclear layer of retina among the HFST group, HFLT group, MFST group, MFLT group, LFST group and LFLT group (F=0.952, P=0.463). Conclusions:The 500 lx laser irradiation is safe to ocular surface and lens, but there are some injuries to retinal function, and the injury degree is related to laser irradiation frequency.
10.Methylation status in the promoter region of Dickkopf-3 gene in patients with myelodysplastic syndromes
Yun FAN ; Xiaohong SHI ; Shangyong NING ; Jiangtao LI ; Wei CHENG ; Naibai CHANG ; Ze YANG
Journal of Leukemia & Lymphoma 2014;23(9):534-537
Objective To investigate the methylation status in the promoter region of Dickkopf-3 (Dkk3) gene in patients with myelodysplastic syndromes (MDS),and to initially explore the relationship between the methylation of this gene and survival time.Methods Methylation-specific PCR (MSP) was applied to measure the promoter methylation of Dkk3 gene in 43 bone marrow or peripheral blood samples of MDS patients.As controls,70 normal peripheral blood samples from general outpatients were examined.Results In 43 patients with MDS,7 patients (16.3 %) showed Dkk3 gene methylation.And 5 of them were semi-methylation status,2 of them were exhaustive methylation status.In 70 controls,1 showed Dkk3 gene semi-methylation.The frequency of methylation in MDS patients was significantly higher than that of controls (x2 =8.93,P =0.005).In the Dkk3 methylation group,2/7 were from bone marrow and 5/7 were from peripheral blood.Meanwhile,2 patients were RA,1 patient was RCMD,4 patients were RAEB.There was no significant difference between the different sample source (bone marrow or peripheral blood) for the results of the methylation status (x2 =0.051,P =0.821).Either between the different sex,age,type,chromosome and WPSS score (P > 0.05).The progress of disease didn't influence the methylation frequency (P > 0.05).The smvival analysis showed no relationship between the methylation of this gene and smvival time.Conclusions In this MDS group,there is high level of methyl-modification in Dkk3 gene.The methylation of Dkk3 might be one of the molecular mechanisms that contribute to the progress of patients with MDS.The peripheral blood sample maybe a better substitute in detective of Dkk3 with MDS.