OBJECTIVE:To study the pharmacokinetics and the bioavailability of naftopidil sustained-release capsules. METHODS:Naftopidil capsule and sustained-release capsules were given to five healthy male dogs respectively in an open randomized cross-over test.Naftopidil concentrations in plasma were determined by HPLC method.The pharmacokinetics parameters and the relative bioavailability were measured and compared between naftopidil capsules and sustained-release capsules.RESULTS:A one-compartment open model with first-order absorption kinetics best fitted the concentration-time data.The T 1/2 ,AUC 0～∞ ,C max and T max of naftopidil capsule were3.2?1.1h,3728.1?573.1ng?h/ml,697.5?94.2ng/ml and1.2?0.59h,these pharmacokinetics parameters of sustained-release capsules were5.9?0.8h,5518.3?391.1ng?h/ml and468.6?61.3ng/ml and4.0?0.7h respectively.The relative bioavailability of naftopidil sustained-release capsules was149.8?14.4%when compared with naftopidil capsules.CONCLUSION:Naftopidil sustained-release capsules have satisfactory property in slow release of drug and much higher bioavailability than naftopidil capsules.

0.05),and the costs were 441.28,436.63,543.55 and 437.89 yuan respectively,showing no significant difference compared among Group A,B and D,but the cost in Group C was 20% higher than in other groups.CONCLUSION: Scheme C is recommended only when scheme A,B and D are invalid(such as the patients are allergic to Amoxicillin or Furazolidone or resistant to Metronidazole).

OBJECTIVE:To explore the cleaning action of rhizoma pinelliae mi xture(RPM)on trachea secretions of the model animals.METHODS:The rats were divided randomly into high and low dose of RPM group and the control group;Then the secretion level of phenol red in each group was observed after the forming of models by tracheostomy and intraperitonal injection with phenol red;The respective time that spent on moving cork wood filings to a same distance by oral mucosa ep ?ithelium ciliary movement of toad both before and after medication were observed.RESULTS:The secretion level of phenol red in RPM group increased significantly compared with the control group(P

OBJECTIVE:To study the bioequiavailability of both the domestic and the imported azithromycin tablets in healthy human body.METHODS:The serum concentrations in 12 healthy volunteers was determined by HPLC-UV after administration of a single oral dose of 500mg azithromycin tablets by a cross-over design.The compartment model was discriminated by F-test and AIC method and the pharmacokinetic parameters were calculated by DAS program.RESULTS:The optimal compartment model fitted to two-compartment model.The main pharmacokinetics parameters of the domestic azithromycin tablets vs.the imported ones were the following:Cmax was(437.4 670? 51.5 670),(442.9 670? 61.5 030)? g/L;t1/2? was(44.7 450? 13.1 750),(49.2 670? 15.1 740)h;tmax was(2.5 830? 0.5 150),(2.5 830? 0.5 150)h;AUC0～ 144 was(13.2 799? 2.9 827),(12.1 953? 2.9 140)(mg? h)/L.The relative bioavailability of the domestic azithromycin tablets was(101.7? 0.1)%.CONCLUSION:The domestic azithromycin tablets and the imported ones were bioequivalent.

Objective: To investigate the clinical characteristics of extremely severe burn patients complicated with severe inhalation injury caused by dust explosion. Methods: The medical records of 13 extremely severe burn patients complicated with severe inhalation injury in August 2nd Kunshan factory aluminum dust explosion accident, who were admitted to the First Affiliated Hospital of Soochow University on August 2nd, 2014, were retrospectively analyzed. The following indicators were collected: (1) Acute Physiology and Chronic Health Evaluation Ⅱ (APACHE Ⅱ) score and Sequential Organ Failure Assessment (SOFA) score at post admission hour (PAH) 24. (2) Prognosis, death time, causes of death, and the mortality of patients with different sexes. (3) The number of times of airway electronic bronchoscopy, airway characteristics, and the corresponding onset time. (4) The number and result of microorganism culture of lesion tissue during the leukoplakia formation stage. Detection of Pseudomonas aeruginosa in patients with and without leukoplakia in airway mucosa. Fisher′s exact probability test was used to detect the mortality of patients with different sexes. Kappa test was used to detect the relevancy between leukoplakia and Pseudomonas aeruginosa. Results: (1) The APACHE Ⅱ score of patients of this group at PAH 24 was (19±3) points, and the SOFA score was (12±3) points. (2) Eight patients survived, while 5 patients died, and the time of death was 19-46 (34±10) d after injury. The main cause of death was multiple organ dysfunction syndrome, which was secondary to severe infection. One of the 7 male patients and 4 of the 6 female patients died, but there was no significantly statistical difference in mortality between patients of the two sexes (P>0.05). (3) Airway electronic bronchoscopy was performed 4-25 (10±5) times among patients of this group. Hyperemia and edema were found in the airway mucosa of all the 13 patients 2-3 weeks after injury; ulcer was found in the airway mucosa of 5 patients 2-4 weeks after injury; leukoplakia was found in the airway mucosa of 7 patients 4-14 weeks after injury; granulation formed in the airway mucosa of 7 patients 10-15 weeks after injury, and airway patency was affected, which was solved after local clamping or replacement of lengthened tracheal cannula. (4) During the leukoplakia formation stage, 19 cases of microorganism culture were performed basing on airway lesion tissue, and the results were 15 cases of Pseudomonas aeruginosa, 5 cases of Acinetobacter baumannii, 2 cases of Serratia marcescens, as well as 1 case of Stenotrophomonas maltophilia, Burkholderia cepacia, and Proteus mirabilis each. Among 7 patients with airway mucosa leukoplakia, 6 patients were detected with Pseudomonas aeruginosa. Among 6 patients without airway mucosa leukoplakia, 1 patient was detected with Pseudomonas aeruginosa. The appearance of leukoplakia was consistent with the detection of Pseudomonas aeruginosa (Kappa=0.69, P<0.05). Conclusions Most of these extremely severe burn patients complicated with severe inhalation injury caused by dust explosion survived, and there was no significant gender difference in mortality. Electronic bronchoscopy showed that the early manifestations of airway mucosa were hyperemia and edema, followed by varying degrees of erosion, ulcer, leukoplakia, and granulation formation, etc. Leukoplakia may be relevant to Pseudomonas aeruginosa infection.

In this study, a high performance thin-layer chromatography/single quadrupole mass spectrometry QDa (HPTLC-QDa) method for robust authentication of Ganoderma lucidum, a popular and valuable herbal medicine, has been developed. This method is simple and practical, which allows direct generation of characteristic mass spectra from the HPTLC plates automatically with the application of in situ solvent desorption interface. The HPTLC silica gel plates were developed with toluene-ethyl formate-formic acid (5 : 5 : 0.2, V/V) and all bands were transferred to QDa system directly in situ using 80% methanol with 0.1% formic acid as desorption solvent. The acquired HPTLC-QDa spectra showed that luminous yellow band b3, containing ganoderic acid B/G/H and ganodeneric acid B, the major active components of Ganoderma, could be found only in G. lucidum and G. lucidum (Antler-shaped), but not in G. sinense and G. applanatum. Moreover, bands b13 and b14 with m/z 475/477 and m/z 475/491/495, respectively, could be detected in G. lucidum (Antler-shaped), but not in G. lucidum, thus allowing simple and robust authentication of G. lucidum with confused species. This method is proved to be simple, practical and reproducible, which can be extended to analyze other herbal medicines.

Arisaema heterophyllum Blume is one of the three medicinal plants known as traditional Chinese medicine Rhizoma Arisaematis (RA). RA has been popularly used to treat patients with convulsions, inflammation, and cancer for a long time. However, the underlying mechanisms for RA effects are still unclear. The present study was designed to determine the cytotoxicity of agglutinin isolated from Arisema heterophyllum Blume (AHA) and explore the possible mechanisms in human non-small-cell lung cancer A549 cells. AHA with purity up to 95% was isolated and purified from Arisaema heterophyllum Blume using hydrophobic interaction chromatography. AHA dose-dependently inhibited the proliferation of A549 cells and induced G phase cell cycle arrest. AHA induced apoptosis by up-regulating pro-apoptotic Bax, decreasing anti-apoptotic Bcl-2, and activating caspase-9 and caspase-3. In A549 cells treated with AHA, the PI3K/Akt pathway was inhibited. Furthermore, AHA induced increase in the levels of ER stress markers such as phosphorylated eukaryotic initiation factor 2α (p-eIF2α), C/EBP-homologous protein (CHOP), inositol-requiring enzyme 1α (IRE1α), and phosphorylated c-Jun NH-terminal kinase (p-JNK). AHA also induced autophagy in A549 cells. Staining of acidic vesicular organelles (AVOs) and increase in the levels of LC3II and ATG7 were observed in AHA-treated cells. These findings suggested that AHA might be one of the active components with anti-cancer effects in Arisaema heterophyllum Blume. In conclusion, cytotoxicity of AHA on cancer cells might be related to its effects on apoptosis and autophagy through inhibition of PI3K/Akt pathway and induction of ER stress.
A549 Cells ; Agglutinins ; pharmacology ; Apoptosis ; drug effects ; Arisaema ; chemistry ; Autophagy ; drug effects ; Carcinoma, Non-Small-Cell Lung ; drug therapy ; enzymology ; metabolism ; physiopathology ; Cell Line, Tumor ; Drugs, Chinese Herbal ; pharmacology ; Endoplasmic Reticulum Stress ; drug effects ; Humans ; MAP Kinase Signaling System ; drug effects ; Phosphatidylinositol 3-Kinases ; genetics ; metabolism ; Phosphorylation ; drug effects ; Proto-Oncogene Proteins c-akt ; genetics ; metabolism

Achyranthes bidentata Blume is widely used as a traditional Chinese medicine with the effects of nourishing the liver and kidneys and strengthening muscles and bones. In this work, a rapid and simple strategy was developed for characterizing phytoecdysteroids by ultra-high-performance liquid chromatography coupled with liner ion trap-Orbitrap mass spectrometry using electrospray ionization in the negative mode. As a result, 47 phytoecdysteroids were unambiguously or tentatively characterized. Among them, seven known compounds were identified according to the reference standards along with molecular formula, retention time and fragmentation patterns, while others were mostly potential new compounds. Through targeted isolation, the structures of three new compounds were determined by NMR spectra, which were consistent with LC-MS characterization. The present study provides an efficient method to deeply characterize phytoecdysteroids.
Achyranthes/chemistry* ; Chromatography, High Pressure Liquid/methods* ; Gas Chromatography-Mass Spectrometry ; Mass Spectrometry ; Medicine, Chinese Traditional ; Spectrometry, Mass, Electrospray Ionization/methods*

Evaluating the consistency of herb injectable formulations could improve their product quality and clinical safety, particularly concerning the composition and content levels of trace ingredients. Panax notoginseng Saponins Injection (PNSI), widely used in China for treating acute cardiovascular diseases, contains low-abundance (10%-25%) and trace saponins in addition to its five main constituents (notoginsenoside R₁, ginsenoside Rg₁, ginsenoside Re, ginsenoside Rb₁, and ginsenoside Rd). This study aimed to establish a robust analytical method and assess the variability in trace saponin levels within PNSI from different vendors and formulation types. To achieve this, a liquid chromatography-triple quadrupole mass spectrometry (LC-MS/MS) method employing multiple ions monitoring (MIM) was developed. A "post-column valve switching" strategy was implemented to eliminate highly abundant peaks (NR₁, Rg₁, and Re) at 26 min. A total of 51 saponins in PNSI were quantified or relatively quantified using 18 saponin standards, with digoxin as the internal standard. This study evaluated 119 batches of PNSI from seven vendors, revealing significant variability in trace saponin levels among different vendors and formulation types. These findings highlight the importance of consistent content in low-abundance and trace saponins to ensure product control and clinical safety. Standardization of these ingredients is crucial for maintaining the quality and effectiveness of PNSI in treating acute cardiovascular diseases.
Ginsenosides ; Saponins ; Chemometrics ; Panax notoginseng ; Cardiovascular Diseases ; Chromatography, Liquid ; Tandem Mass Spectrometry