This study was to investigate the chemical constituents of the aerial part of Zygophyllumfabago, by phytochemical methods. The compounds were isolated by silica gel and Sephadex LH-20 column chromatographies from the EtOAc extract. Their structures were characterized by various spectroscopic data (1H-NMR, 13C-NMR, MS) and comparison with the literature. As a result, thirteen compounds were isolated and their structures were identified as 1-hydroxyhinesol(1), hinesol(2), atractylenolactam(3), beta-eudesmol (4), 5alpha-hydroperoxy-beta-eudesmol(5), 12-hydroxy-valenc-1(10)-en-2-one(6), pubinernoid A(7), (6S,7E)-6-hydroxy-4,7-megastigmadien-3,9-dione(8), 3-hydroxy-5alpha, 6alpha-epoxy-beta-ionone (9), (3S,5R, 6S, 7E)-3, 5, 6-trihydroxy-7-megastigmen-9-one(10), (6R,7E,9R)-9-hydroxy-4,7-megastigmadien-3-one(11), (S)-3-hydroxy-beta-ionone(12), and blumenol A(13). Compounds 1-7 were sesquiterpenoids and 8-13 were megastigmane type norsesquiterpenoids. All the compounds were obtained from Z. fabago for the first time, and compound 1 was a new natural product.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Terpenes ; chemistry ; isolation & purification ; Zygophyllum ; chemistry

AIMTo determine phenytoin sodium by a highly accurate nephelometric titration.

METHODSThe titration operating conditions were optimized and the solubility product constant of phenytoin silver precipitation was determined.

RESULTSThe result of the titration is comparable to those of control experiments.

CONCLUSIONThe proposed method has been found to be accurate, precise, specific, reproducible, and linear.

Nephelometry and Turbidimetry ; methods ; Phenytoin ; analysis ; Reproducibility of Results ; Solutions ; Titrimetry ; methods

Objective To evaluate the diagnostic value of conventional and dynamic contrast- enhanced MRI in lymphoma of the orbit.Methods Thirteen cases of lymphoma of the orbit,including B-C (10 cases),T-C (1 case),T-NK-C (1 case)lymphoma,and multiple myeloma (1 case),were studied using conventional MR and dynamic contrast-enhanced MR imaging with 3D fast spoiled gradient echo sequence.Calculated values included time to peak (Tpeak),washout ratio (WR),slope and enhancement ratio (ER),and time-intensity curves (TICs),and Tpeak,WR,slope and ER were calculated preoperatively.Results Eleven of the 13 lymphomas of the orbit was seen in the anterior portion of the orbit including eyelid and lacrimal gland.On conventional MRI,10 cases showed iso-intensity on T_1WI and T_2WI and all 13 cases showed moderate enhancement after contrast administration.TIC of all 13 cases showed rapid enhancing and wash-out,Tpeak was (58.7?8.5)s,and WR was (30.9?9.4)%.The accurate diagnosis with only conventional MRI was achieved in 6 out of 13 cases,while the accurate diagnosis was achieved in all 13 cases by using combined conventional MRI and dynamic enhanment MRI.Conclusion onventional MRI combined with dynamic contrast-enhanced MRI is useful for the diagnosis of lymphoma of the orbit.

Gastrectomy ; Humans ; Laparoscopy ; Stomach Neoplasms/surgery*

Accidents, Occupational ; statistics & numerical data ; China ; epidemiology ; Humans

AIMTo simplify the study on the effect of relative humidity and temperature on drug stability.

METHODSThe stability of penicillin potassium as a model was studied with programmed humidifying and heating.

RESULTSResults of our programmed humidifying and heating experiments are comparable to those of traditional experiment at constant humidity and temperature.

CONCLUSIONProgrammed humidifying and heating experiments are applicable to drug stability study.

Drug Stability ; Hot Temperature ; Humidity ; Penicillins ; chemistry

The release behavior of single pellet was investigated by LC/MS/MS method with tamsulosin hydrochloride (TSH) as the model drug of the research and then the pellets were divided into four groups according to the drug loading. Comparison of dissolution profiles of each group and capsule were performed using f1 and f2 factor methods to study the difference and similarity. The release profiles of single pellet, each group and capsule were analyzed using principle component analysis (PCA). The particle system was built through Matlab to get the target release profile. The result of this research demonstrated the release behavior of single pellet correlated well with the drug loading. While the dissolution profile of capsule as a reference, the similarity factor of dissolution profiles of the lower drug loading groups were 62.2, 67.1, 53.9, respectively and, 43.3 for highest drug loading group. The particle systems with different pellet distribution and same release profiles were built through release behavior of single pellet. It is of significance to investigate the release behavior of single pellets for studying the release regularity of multiple-unit drug delivery system.
Capsules ; Chemistry, Pharmaceutical ; Chromatography, Liquid ; Delayed-Action Preparations ; Drug Delivery Systems ; Drug Liberation ; Principal Component Analysis ; Sulfonamides ; administration & dosage ; chemistry ; Tandem Mass Spectrometry ; Technology, Pharmaceutical

A linear degradation humidifying model for drug stability experiment is introduced. This new humidifying model is presented as: H(r) = -M1-ln {exp(- MH(r,0)) - [exp(-MH(r,0)) -exp(-MH(r-m)) t(m)-t}. Where H(r) is the relative humidity; t is the time; H(r,m) and t(m) are the final relative humidity and time of the experiment, respectively. M is humidifying constant used in the humidifying program. In the new programmed humidifying model, a linear relationship between the content function of drugs and the relative humidity is obtained, the degradation of drugs can be more uniform within different humidity ranges and the experimental results are more accurate than those in the reported linear humidifying model. The stability of penicillin potassium, as a solid state model, was investigated by the linear degradation programmed humidifying and the exponential heating experiments. The results indicated that the kinetic parameters obtained by the linear degradation programmed humidifying and the exponential heating models were significantly more precise than those obtained by the linear programmed humidifying and the reciprocal heating models.
Drug Stability ; Humidity ; Kinetics ; Mathematics ; Models, Chemical ; Penicillins ; chemistry ; Technology, Pharmaceutical ; methods ; Temperature

AIMTo produce poly (lactic-co-glycolic acid) (PLGA) microspheres, containing a staphylokinase variant (K35R, DGR) with reduced immunogenecity and antiplatelet aggregation activities, which allowed the preservation of protein stability during both particle processing and drug release.

METHODSDGR-loaded microspheres were fabricated using a double emulsion-solvent evaporation technique. The effects of preparative parameters, such as stirring rate, polymer concentration, and the excipients of both internal and external aqueous phase (W2), on DGR encapsulation efficiency and microsphere characteristics were investigated. In vitro and in vivo release of DGR were conducted and the cause for instability of DGR during release was also investigated.

RESULTSModerate ultrasonic treatment of aqueous DGR/dichloromethane mixtures caused approximately. Eighty four per cent DGR denaturation. However, the activity recovery of DGR almost amounted to 100% when 2% polyvinyl alcohol (PVA) was addled into the aqueous phase. It was found that NaCl in the external water phase significantly increased DGR encapsulation efficiency. Furthermore, NaCl in the external water phase played a role in determining size and surface morphology of microsphere. In vitro release test showed a burst release of DGR from microspheres, followed by sustained release of 50% total activity over 15 days. In vivo experiments showed that DGR released from microspheres sustained 5 days. Denaturation of DGR within microspheres might be resulted from acidic microclimate.

CONCLUSIONThe stability of DGR was effectively protected during microencapsulation and a relatively high encapsulation efficiency of DGR was obtained. PLGA microspheres could be an effective carrier for DGR.

Animals ; Area Under Curve ; Drug Carriers ; Drug Compounding ; Drug Delivery Systems ; Escherichia coli Proteins ; administration & dosage ; genetics ; pharmacokinetics ; Genetic Variation ; Lactic Acid ; Male ; Metalloendopeptidases ; administration & dosage ; genetics ; pharmacokinetics ; Microspheres ; Particle Size ; Polyglycolic Acid ; Polymers ; Rabbits

Objective To evaluate MR imaging findings of uveal metastases.Methods MR imaging findings of 20 cases with uveal metastases comfirmed by pathology or follow-up were retrospectively analyzed.MR imaging was performed in 20 patients,of which postcontrast T1-weighted imaging was performed in 19 patients including dynamic contrast enhancement scanning in four cases.Results Metastatic tumor was found in the iris and ciliary body in two cases,and in choroid in 18 cases.The tumor demonstrated slightly hypointense signal on Tl-weighted imaging and isointense signal on T2-weighted imaging in two cases,isointense signal on T1-weighted imaging and isointense signal on T2-weighted imaging in nine cases,isointense signal on T_1-weighted imaging and slightly hyperintense signal on T_2-weighted imaging in three cases,isointense signal on T_1-weighted imaging and slightly hypointense signal on T_2- weighted imaging in three cases,slighdy hyperintense signal on T_1-weighted imaging and slightly hypointense signal on T_2-weighted imaging in two cases,and slightly hyperintense signal on T_1-weighted imaging and slightly hyperintense signal on T_2-weighted imaging in one case.The tumor appeared as mild thickness of the wall of the globe in eight cases,a crescent mass in three cases,a fusiform mass in seven cases,and a nodule in two cases.Nineteen patients showed moderate or marked enhancement on postcontrast T_1-weighted imaging.The time-intensity curve of dynamic contrast enhancement in four patients suggested a rapid enhancement and slow washout pattern.Retinal detachment was observed in 11 patients and abnormal signal intensity within the vitreous body was seen in two cases.Conclusion MRI can display the location,shape, signal characteristics,and enhancement pattern of uveal metastases,contributing to diagnosis and differential diagnosis.