1.Diagnostic value of ultrasonography and CT in the diagnosis of adrenal tumors
Chinese Journal of Primary Medicine and Pharmacy 2017;24(5):740-742,743
Objective To investigate the diagnostic value of ultrasonography and CT in the diagnosis of adrenal tumors,and to provide reference for clinical diagnosis of tumors in the future.Methods 86 cases of adrenal tumor in our hospital from July 2013 to February 2016 were retrospectively reviewed.All the patients were examined by ultrasonography and CT.The characteristics of different types of adrenal tumors were observed and analyzed,and the diagnostic accuracy was compared between the two methods.Results The coincidence rate of CT diagnosis (93.02%)was higher than that of ultrasonic imaging(84.88%),but the difference was not statistically significant (χ2 =2.899 2,P >0.05).Conclusion The coincidence rate of ultrasound imaging and CT are higher in adrenal tumors,and has significant value in clinical application,should be based on the imaging of a gradient,into the imaging system,the formation of a simple,practical and economical examination method to achieve the best diagnosis effect.
2.In vitro and in vivo Transdermal Penetration of Testosterone Undecanoate Binary Ethosomes Gel
China Pharmacist 2016;19(10):1840-1842
Objective:To study the in vitro and in vivo transdermal penetration of testosterone undecanoate ( TU) binary ethosomes gel. Methods:TU binary ethosomes were prepared by an ethanol injection method, and using carbopol 941 as the gel base, TU binary ethosomes gel was prepared. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes and the gel. Rats were used as the animals, and TU binary ethosomes and the gel was respectively administrated on the back skin. At the predetermined time points, plasma samples were withdrawn to detect the concentration of TU, and the main pharmacokinetics parameters were calculated. Results: The in vitro transdermal penetration of TU binary ethosomes and the gel was both fitted first-order equation:Q=8. 68t+6. 78(r=0. 998 2) and Q=6. 09t+3. 09(r=0. 999 3), and the stable penetration rate was 8. 68 μg·cm-2 ·h-1 and 6. 09μg·cm-2 ·h-1 , respectively. After the 24-hour penetration, the residual amount in skin of TU binary ethosomes and the gel was (208. 80 ± 55. 26)μg·g-1 and (225. 60 ± 38. 90)μg·g-1 , respectively. The main pharmacokinet-ics parameters of TU binary ethosomes and the gel were Cmax of(18.50 ±2.75)mg·L-1 and(20.80 ±2.42)mg·L-1, tmax of(6.20 ± 0. 14)h and(9. 54 ± 0. 52)h, and AUC0-48h of(336. 74 ± 2. 05)h and(486. 30 ± 1. 68)h. Conclusion:TU binary ethosomes and the gel both exhibit promising in vitro transdermal penetration, and the gel shows better sustained release property.
3.Study on the enhancement effect of N-trimethyl chitosan on transdermal absorption of 8-methoxypsoralenloaded liposomal gels in vitro
Shuhai YU ; Xianxi GUO ; Wen HE
Chinese Journal of Primary Medicine and Pharmacy 2013;20(17):2587-2589
Objective To explore the enhancement effect of N-trimethyl chitosan(TMC) on transdermal absorption of 8-methoxypsoralen-loaded liposomal(LMOP) gels in vitro.Methods TMC with quaternization degree of 60% (TMC60) as the enhancer,the LMOP gels were prepared with free TMC60 or TMC60-coating.The enhancement of free TMC60 or TMC60-coating was studied by using Franz diffusion,cells with LMOP gels as the negative control and LMOP gels including 1% Azone + propylene glycol as the positive control.Results Compared with the negative control,enhancement and drug amount in skin of LMOP gels with enhancer all showed significant difference (x2 =8.65,P < 0.05),and the free TMC.60 was the best.Conclusion TMC can enhance the transdermal penetration of LMOP gels in vitro and is valuable to be studied further.
4.Effect of Membrane-coating on Dissolution and Stability of Sirolimus Dropping Pills
Xianxi GUO ; Wen HE ; Shaoting LI
China Pharmacist 2014;(11):1846-1848,1849
Objective:To study the effect of membrane-coating on dissolution and stability of sirolimus ( SRL) dropping pills to prove the effect and rationality of the coating process. Methods:Opadry was used as the coating material for SRL dropping pills. Com-pared with those of uncoated SRL dropping pills, the dissolution and stability of membrane-coating SRL dropping pills were studied in vitro. Results:Compared with that of uncoated SRL dropping pills, the drug release amount of membrane-coating SRL dropping pills was lower (P<0. 05), however, the stable release rate showed no significant difference (P>0. 05). After the membrane-coating, the stability of SRL dropping pills was notable enhanced under high humidity (75% ± 5%) and strong light (4500lx ± 500lx) conditions, however, the stability showed no improved under high temperature(40℃ ± 2℃) condition. Conclusion: The membrane-coating can enhance the stability of SRL dropping pills without significant effect on drug release in vitro.
5.Preparation and Content Determination of Lidocaine Liposome Gel
Xianxi GUO ; Wen HE ; Yun LUO
China Pharmacy 2001;0(07):-
OBJECTIVE:To prepare lidocaine liposome gel and to establish its quality control method.METHODS:Li-docaine liposome was prepared using a film dispersion method and the liposome gels were prepared with carbomer-940as base.The concentration of lidocaine was determined by HPLC and the lipsome entrapment efficiency was determined by centrifuga-tion.RESULTS:The linear detection concentration range of lidocaine was2.5~25.0mg/ml(r=0.9996)with average re-covery at(99.83?0.53)%and entrapment efficiency at(82.7?1.83)%.CONCLUSION:This liposome gel is feasible in preparation techniques,stable in quality,convenient and reliable in quality control method.
6.Pharmacokinetics and Brain-targeting Ability of Gastrodin Nasal in Situ Gel in Rats
Wen HE ; Miao XIAO ; Xianxi GUO
China Pharmacist 2017;20(1):68-72
Objective:To study the pharmacokinetic parameters of gastrodin nasal in situ gel ( ISG) with the base of TMC-P407-P188-carbomer, and evaluate its brain-targeting ability preliminarily. Methods:Rats were used as the model animals. The experiment group was treated with gastrodin nasal in situ gel, and the control group was treated with gastrodin solution with intravenous administra-tion. The plasma sample and brain tissue ( cerebrum and cerebellum) were taken out at the predetermined time points, and the concen-tration of gastrodin in plasma and gastrodigenin in brain tissues were determined by HPLC to draw the curve of concentration vs time. The pharmacokinetic parameters such as MRT and AUC were calculated by 3P97 software. The bioavailability F (%) and the brain-targeting index BTI were compared between the groups. Results:The concentration of gastrodigenin in the brain tissues of grastrodin in situ gel was higher than that of gastrodin solution with intravenous administration (P<0. 05). AUC of cerebrum and cerebellum both increased significantly with BTI of 2. 38 and 1. 93, respectively. MRT increased by nearly two-fold in the gel group when compared with that in the control group, and F(%) increased significantly in cerebrum and cerebellum as well. Conclusion:Gastrodin nasal in situ gel with the base of TMC-P407-P188-carbomer has promising effectiveness. Meanwhile, it can improve the brain-targeting ability of gastrodin with sustained release.
7.Base Screening for Gastrodin Nasal in Situ Gel
Wen HE ; Miao XIAO ; Xianxi GUO
China Pharmacist 2016;19(7):1385-1386,1404
Objective:To screen the best base for gastrodin nasal in situ gel ( ISG) to lay foundation for the development of gastrodin new preparation .Methods:Two bases were chosen , one was the combination of N-trimethyl chitosan ( TMC) , polyethylene glycol 4000 (PEG4000) and glycerophosphate (GP), and another was the combination of TMC, poloxamer 407 (P407), poloxamer 188 (P188) and carbomer.With the nasal cavity temperature of 35℃as the test temperature, the gelling time of the two bases was determined to screen the optimal ratio.Furthermore, gastrodin was added into the two bases , and the gelling time was determined to choose the suitable base for the drug.Results:The base of TMC-PEG4000-GP couldn’t gel in the nasal cavity temperature when combined with gastrodin , while the base of TMC-P407-P188-carbomer could gel quickly when combined with gastrodin .Conclusion:TMC-P407-P188-carbomer can be used as the base for gastrodin nasal in situ gel .
8.Relative Bioavailability of Sirolimus Dropping Pills in Rats
Minghua ZOU ; Shaoting LI ; Xianxi GUO
China Pharmacist 2015;(6):919-921
Objective:To study the relative bioavailability of sirolimus ( SRL) dropping pills in rats. Methods:PEG6000 as the base, SRL dropping pills were prepared using solvent-melting method. The SRL marketed tablets as the reference preparation and rats as the animals, the relative bioavailability of SRL dropping pills was studied to obtain the pharmaceutical parameters and bioequiavail-ability. Results:Compared with that of the reference preparation, tmax of SRL dropping pills was the same (1 h). There was no signifi-cant difference in Cmax between the dropping pills and the tablets (P>0. 05). AUC0-24 of the dropping pills was notably higher than that of the marketed tablets (P<0. 05) with the bioequiavailability of 121. 98%. Conclusion:SRL dropping pills with promising bioavail-ability are valuable to be studied further.
9.Synthesis and Anti-HIV-1 Activity of One Schiff Base Derivative with Glucosamine of Gossypol
Jian YANG ; Wei ZHAO ; Jingxiang YANG ; Zhenhua JING ; Xianxi GUO
China Pharmacist 2017;20(5):787-790
Objective: To confirm the structure and preferential conformation of the Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine and explore its anti-HIV-1 activity.Methods: The Schiff base of gossypol with 11, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine was synthesized and identified by FT-IR, NMR spectroscopy and the PM6 semi-classical calculation.The inhibitory activity of the novel compound against the laboratory-adapted HIV-1IIIB strain was examined using the HIV-1IIIB/TZM-bl indicator cell culture system.Results: The 1H and 13C-NMR signals of the new Schiff base were assigned.The PM6 semi-classical calculation indicated that enamine-enamine tautomeric form of the new Schiff base was more stable,which was stabilized by the intramolecular hydrogen bonds.The anti-HIV-1 test showed that the compound could block the entry of HIV-1IIIB into the target cells.Conclusion: The Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine exhibits enamine-enamine tautomeric form in solution, which shows potential anti-HIV-1 activity.
10.Effect of Molecular Weight and Substitution Degree of Chitosan-poly-arginine on in vitro Transdermal Pene-tration Enhancement
Wen HE ; Bei LIU ; Xianxi GUO ; Yi TAN
China Pharmacist 2014;(12):1996-2000
Objective:To study the effect of molecular weight and degree of substitution (DS) of chitosan-poly-arginine (CS-R9) on transdermal penetration enhancement in vitro. Methods:Low molecular CS, medium molecular CS or high molecular CS was respectively used to synthesize CS-R9 with different molecular weight (LCS-R9-1, MCS-R9 and HCS-R9). Low molecular CS was used to synthesize CS-R9 with various degree of substitution by changing the mole ratio between R9 and CS (LCS-R9-1, LCS-R9-2 and LCS-R9-3). The in vitro transdermal penetration enhancement of the different CS-R9 on tinidazole ( TNZ) was studied using Franz diffusion cells. Results:According to the results of FTIR and 1 H-NMR, a series of target CS-R9 were synthesized including LCS-R9-1 with the DS of 2. 30, MCS-R9 with the DS of 2. 17, HCS-R9 with the DS of 2. 20, LCS-R9-2 with the DS of 8. 05 and LCS-R9-3 with the DS of 15. 87. Compared with the blank control group, Azone group, LCS group, R9 group and LCS+R9 group, LCS-R9-1 could enhance the in vitro transdermal penetration of TNZ significantly (P<0. 05). When the DS was unchanged, LCS-R9-1 and HCS-R9 showed similar enhancement in the first 12h, and the effects were both higher than that of MCS-R9 (P<0. 05). The enhancement of HCS-R9 was decreased during 12-24h, while compared with that of LCS-R9-1, the difference was not notable (P>0. 05). When the molecular weight of CS was unchanged, the effect was increased with the rise of DS in the first 21h, however, after that, the effect was decreased with the rise of DS. Conclusion:Molecular weight and DS both have significant effect on the in vitro transdermal penetration enhancement of CS-R9, and it is valuable to further study the in vivo transdermal penetration enhancement of CS-R9 and underlying mechanisms.