Acupuncture Points ; Adult ; Aged ; Anorexia ; therapy ; Child ; Constipation ; therapy ; Female ; Humans ; Inflammation ; therapy ; Male ; Medicine, Chinese Traditional ; methods ; Pruritus ; therapy

Objective To investigate the protective effect of pinacidil on the intestinal mucosa of scalded rats and the mechanism. Methods A total of 24 healthy SD rats were randomly divided into normal control group, burn group, and pinacidil treated group. Rats in burn group and pinacidil treated group were inflicted with 30% TBSA Ⅲ degree burn and resuscitated intraperitoneally with Ringer's solution immediately after burn. Pinacidil was injected intraperitoneally into rats in pinacidil treated group at the dose of 2 mg/kg. Mitochondrial respiratory function intestinal mucosa and levels of reactive oxygen species (ROS), maleic dialdehyde (MDA), and superoxide dismutase (SOD) in plasma were determined at 6 h after burn. Results Mitochondrial respiratory function control rate (RCR), ST3, and SOD levels in pinacidil treated group were evidently higher than those in the burn group. However, ST4, MDA, and ROS levels in pinacidil treated group were significantly lower than those in the burn group, but ST4 was not significantly different from that in the normal control. Conclusion Pinacidil can attenuate the damage of intestinal mucosa in scalded rats.

Idiosyncratic adverse drug reactions (IDR) induce severe medical complications or even death in patients. Alert structure in drugs can be metabolized as reactive metabolite (RM) in the bodies, which is one of the major factors to induce IDR. Structure modification and avoidance of alert structure in the drug candidates is an efficient method for reducing toxicity risks in drug design. This review briefly summarized the recent development of the methodologies for structure optimization strategy to reduce the toxicity risks of drug candidates. These methods include blocking metabolic site, altering metabolic pathway, reducing activity, bioisosterism, and prodrug.
Binding Sites ; Cytochrome P-450 Enzyme System ; metabolism ; Drug Design ; Drug Discovery ; methods ; Drug Recalls ; Drug-Related Side Effects and Adverse Reactions ; prevention & control ; Humans ; Structure-Activity Relationship

Objective To explore the feature of electrical physiology and the key aspect of diagnosis in early stage of spinal muscular atrophy in infants.Method The back clinical data of the musle change of electrical physiology within 25 cases were analyzed.Results The children were ill in 1 year old,with the symptom that four limbs present symmetry and paralysing slowly,low limbs being more serious than upper limbs,the close and the distant of the four limbs.The levels of creatine kinase(CK) and lactate dehydrogenase(LDH) in serum were normal and the case unconcentrated was not seen rarely.The show of electromyogram(EMG) was that three limbs presenting wide-range losing nerve electric potential in peace state,when straingently the deadline was long and the motor unit potential(MUP) was high,when strain highly the eletric potential was decreased;the speed of nerve conduction was common.Muscle inspection was typical nervine myatrophy.Conclusion The clinical feature,the changes of muscle electrical physiology and the muscle inspection are valuable for diagnosis so as to afford reliable evidence for further gene diagnosis.J Appl Clin Pediatr,2006,21(3):167

Objective To investigate the status of anxiety-depression and the relevant factors in puerpera be- fore delivery.Methods The emotion of anxiety and depression in puerpera before delivery was evaluated by self-rat- ing anxiety scale(SAS)and self-rating depression scale(SDS)which had satisfactory validity and reliability.Results The values of anxiety and depression in puerpera were higher than those of general crowd(P

Cinobufacino injection is a significant anti-tumor medicine for the treatment of various tumors in clinic, which was made from water extraction of the skin of Bufo bufo gargarizans. In present paper, HPLC-DAD-FT-ICR-MS method was used to identify the major bufadienolides in cinobufacino for the first time. Solid-phase extraction with dichloromethane and silica was used to enrich the total bufadienolides in cinobufacino. Based on the UV and high resolution MS/MS data, 33 bufadienolides were analyzed and characterized. Among them, eight compounds were identified by comparing with standard references unambiguously. This study elucidated the major bufadienolides in cinobufacino, which provided material foundation of cinobufacino and will be benefit for the further pharmacological research.
Amphibian Venoms ; chemistry ; Animals ; Bufanolides ; analysis ; chemistry ; Bufo bufo ; Chromatography, High Pressure Liquid ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

To obtain chemical constituent information of rat plasma after oral administration of Huang-Lian-Jie-Du Decoction (HLJDD), a LC-FT-ICR-MS method has been established, and both positive and negative ions scan modes were include in the analysis. By comparing their retention time, high resolution mass data of HLJDD extracts, blank plasma and dosed plasma, 38 constituents, including 22 prototype compounds and 16 metabolites, were detected in rat plasma after oral administration of HLJDD. In the 22 prototype compounds, 16 constituents were determined unambiguously by comparing with references. In the analysis of metabolites, phase II reactions like glucuronidation and sulfation were the major biotransformation pathways of HLJDD. M11 was observed as the only phase I metabolite in present experiment. The results will be beneficial for the further pharmacokinetics and pharmacological evaluations of HLJDD.
Administration, Oral ; Alkaloids ; blood ; Animals ; Biotransformation ; Chromatography, High Pressure Liquid ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; isolation & purification ; metabolism ; Flavonoids ; blood ; Iridoids ; blood ; Male ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry

OBJECTIVETo evaluate the applicability of immune-related response criteria (irRC) in treating non-small cell lung cancer (NSCLC) by Chinese medicine (CM).

METHODSTotally 97 stage III a-IV NSCLC patients were predominantly treated with comprehensive CM. Curative effects were evaluated by three methods such as Response Evaluation Criteria in Solid Tumors (RECIST), Oncologic Curative Effect Evaluation Criteria of Chinese Medicine in Solid Tumor (draft, abbreviated as CM criteria), and irRC. The correspondency and consistency between irRC, RECIST and CM criteria were analyzed and compared. The objectivity of irRC in evaluating curative effect of Chinese medical treatment for NSCLC was assessed.

RESULTSThe correspondency rate of irRC to RECIST was 59. 79% with Kappa value of 0. 379 (U test, P <0. 01). The two criteria had certain correspondence, but with an unsatisfactory consistency. The correspondency rate of irRC to CM criteria rate was 83. 51% with Kappa value of 0.751 (U test, P <0. 01). The two criteria had good correspondence and consistency.

CONCLUSIONSCM criteria had good consistency with CM criteria in evaluating curative effect for Chinese medical treatment of advanced NSCLC. Its results could objectively reflect features and advantages of CM for treating advanced NSCLC.

Asian Continental Ancestry Group ; Carcinoma, Non-Small-Cell Lung ; drug therapy ; immunology ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Lung Neoplasms ; drug therapy ; immunology ; Medicine, Chinese Traditional ; standards ; Treatment Outcome

In the present study, a risperidone loaded microsphere/sucrose acetate isobutyrate (SAIB) in situ forming complex depot was designed to reduce the burst release of SAIB in situ forming depot and to continuously release risperidone for a long-term period without lagime. The model drug risperidone (Ris) was first encapsulated into microspheres and then the Ris-microspheres were embedded into SAIB depot to reduce the amount of dissolved drug in the depot. The effects of different types of microsphere matrix, including chitosan and poly(lactide-coglycolide) (PLGA), matrix/Ris ratios in microspheres and morphology of microspheres on the drug release behavior of complex depot were investigated. In comparison with the Ris-loaded SAIB depot (Ris-SAIB), the complex depot containing chitosan microspheres (in which chitosan/Ris = 1 : 1, w/w) (Ris-Cm-SAIB) decreased the burst release from 12.16% to 5.80%. However, increased drug release rate after 4 days was observed in Ris-Cm-SAIB, which was caused by the high penetration of the medium to Ris-Cm-SAIB due to the hydrophilie of chitosan. By encapsulation of risperidone in PLGA microspheres, most drugs can be prevented from dissolving in the depot and meanwhile the hydrophobic PLGA can reduce the media penetration effect on the depot. The complex depot containing PLGA microspheres (in which PLGA/ drug=4 : 2, w/w) (Ris-Pm-SAIB) showed a significant effectiveness on reducing the burst release both in vitro and in vivo whereby only 0.64% drug was released on the first day in vitro and a low AUC0-4d value [(105.2± 24.4) ng.mL-1.d] was detected over the first 4 days in vivo. In addition, drug release from Ris-Pm-SAIB can be modified by varying the morphology of microspheres. The porous PLGA microspheres could be prepared by adding medium chain triglyceride (MCT) in the organic phase which served as pore agents during the preparation of PLGA microspheres. The complex depot containing porous PLGA microspheres (which were prepared by co-encapsulation of 20% MCT) (Ris-PPm-SAIB) exhibited a slightly increased AUC0-4d of (194.6±15.8) ng.mL-1d and high plasma concentration levels from 4 to 78 days [Cs(4-78d)=(7.8±1.2) ng.mL-1]. The plasma concentration on 78 day C78d was (9.0 2.5) ng.mL-1 which was higher than that of Ris-Pm-SAIB [C78d= (1.6 ± 0.6) ng.mL-1]. In comparison with Ris-Pm-SAIB, the AUC4-78d of Ris-PPm-SAIB increased from (379.0±114.3) ng.mL-1.d to (465.0 ±149.2) ng.mL-1.d, indicating sufficient drug release from the Ris-PPm-SAIB. These results demonstrate that the risperidone loaded porous PLGA microsphere/SAIB in situ forming complex depot could not only efficiently reduce the burst release of SAIB depot both in vitro and in vivo, but also release the drug sufficiently in vivo, and be capable to continuously release the drug for 78 days.
Chitosan ; Drug Carriers ; Lactic Acid ; Microspheres ; Polyglycolic Acid ; Risperidone ; chemistry ; Sucrose ; analogs & derivatives ; Technology, Pharmaceutical

AIMTo explore the causes of the difference in spermatogenic suppression between responders and non-responders in Chinese men treated with levonorgestrel (LNG) implants plus testosterone undecanoate (TU) injectable.

METHODSThe 16 Chinese volunteers treated were divided into two groups in regard to the sperm count during the treatment period, 7 men in the responder group (Group R), including 6 azoospermia and one severe oligozoospermia, and the remaining 9 in the non-responder group (Group N), including 4 oligozoospermia and 5 with sperm counts greater than 20 x 10(6)/mL. The differences in serum profiles of FSH, LH, T, LNG and T/LH ratio were compared between the two groups and the correlation between the seminal fluid parameters and serum reproductive hormones was analyzed.

RESULTSThe serum FSH level was lower in Group R than that in Group N (P<0.05), while the serum LH and LNG levels were higher in Group R than those in Group N (P<0.05). The sperm density (P<0.01, r=0.235), motility(P<0.01, r=0.326) and vitality (P<0.01, r=0.219) showed significantly positive correlation with the serum FSH level.

CONCLUSIONThe blood LNG and T levels, the degree of FSH inhibition and/or the sensitivity of the pituitary-testis axis to exogenous steroids, as well as the individual spermatogenetic potential and the functional status of the Leydig cells may be factors bringing about individual differences in spermatogenic suppression in Chinese men treated with LNG and TU.

Adult ; Contraceptive Agents, Male ; administration & dosage ; Drug Implants ; Follicle Stimulating Hormone ; blood ; Humans ; Injections ; Levonorgestrel ; administration & dosage ; pharmacokinetics ; Leydig Cells ; physiology ; Luteinizing Hormone ; blood ; Male ; Sperm Count ; Spermatogenesis ; drug effects ; Testosterone ; administration & dosage ; analogs & derivatives ; blood