Aim: To establish a linear additive model for the predication of in vitro sinomenine hydrochloride release from the combination of immediate release, enteric-coated and sustained-release pellets based on the release profiles of each pellet type. Methods: Immediate release pellets were manufactured by extrusion/spher-onization technology. The operation of bottom-spraying in the fluid-bed equipment was conducted to enteric-coating using Eudragit~(R) L-30D-55 and sustained-release coating using Surelease~(R) . In vitro sinomenine hydrochloride release profiles of both uncoated and coated pellets were fitted to the chosen mathematical equations offered by the curve fitting toolbox of Matlab~(R) before a linear additive model was created based upon the best-to-fitting equations. The proportion of each pellet type in the combined format to generate the desired 24 h sinomenine hydrochloride release profile was solved by Matlab~(R). The predicted and assayed sinomenine hydrochloride release from the polled pellets was compared. Results: It was shown that the actual sinomenine hydrochloride release profiles of each pellet type were approximate to those of predicted ones. A linear additive model of the appropriate mathematical equations of each pellet was proven to be capable of controlling in vitro release of sinomenine hydrochloride multiple-unit pellets. Conclusion: A multiple-unit combined system of the selected pellets, as a novel sustained-release system, was successfully prepared. In vitro release performance of the calculated combination of each pellet type could be guaranteed by this approach in designing sustained-release drug delivery system.

Adult ; Aged ; Anthracosis ; complications ; Humans ; Male ; Middle Aged ; Pulmonary Emphysema ; diagnosis ; etiology ; Respiratory Function Tests ; Tomography, X-Ray Computed

In order to identify the chemical constituents of Yushu tablets comprehensively, we studied the chemical constituents of CHCl3 extract from Yushu tablets by the ultra performance liquid chromatography-electrospray ionization-ion trap-time of flight mass spectrometry (UPLC-ESI-IT-TOF/MS). It showed that there were more than 100 compounds separated, and forty-nine peaks among these were identified on the basis of high resolution mass spectrometry data and literature data reported. Determination of twelve peaks was further confirmed by standard substances. These components assigned to the different plant sources mainly included phenylpropanoids, triterpenoids, quinones and m-trihydroxybenzene compounds. By analyzing the chemical components of CHCl3 extract from compound Chinese medicine Yushu tablets comprehensively, this study provided the foundation for studying chemical components, pharmacodynamic substance and quality control of Yushu tablets.
Chromatography, High Pressure Liquid ; Chromatography, Liquid ; Drugs, Chinese Herbal ; analysis ; Spectrometry, Mass, Electrospray Ionization ; Tablets ; Tandem Mass Spectrometry

Objective To observe the expression levels of matrix metalloproteinase-2 and 9 (MMP-2, MMP-9) in wound tissue and wound effusion in patients with chronic pressure ulcers treated with an alternating pres- sure relief mattress,and to correlate these observations with wound healing.Methods A total of 24 patients with chronic pressure ulcers were recruited and divided into two groups :one treated with an alternating pressure relief mat- tress and the other without,in addition to conventional treatment for pressure ulcers.The expression of MMP-2 and MMP-9 in the wound tissue and its exudate were amplified with a reverse transeriptase-polymerase chain reaction (RT-PCR) and analyzed using quantitative gelatin zymography.Wound healing was also observed and assessed using the pressure ulcer scale for healing (PUSH).Results The wounds were observed to heal well in both groups,as indicated by a significant decrease in the PUSH scores.Statistical analysis revealed a significant difference between the two groups with regard to the PUSH score on the 21st day after initiation of the study.With the healing of the pressure ulcers,the expression both MMP-2 and MMP-9 decreased.On the seventh and the 21st days,the expression of MMP-2 and MMP-9 in patients treated with an alternating pressure relief mattress was significantly less than in those without the mattress.Conclusion MMP-2 and MMP-9 can be biomarkers for the healing of pressure ulcers. An alternating pressure relief mattress is helpful for treating pressure ulcers.

OBJECTIVEThe purpose of this study was to investigate the relation between the Arg389Gly polymorphism of the beta(1)-AR gene and chronic heart failure (CHF) and to evaluate the effect of this polymorphism on clinical response to beta-adrenoceptor blockade (bisoprolol) in patients with CHF.

METHODSOne hundred and ten patients with stable CHF receiving basic therapy for heart failure were included. Before initiation and 3 months after the maximal tolerated dose of bisoprolol was reached, all indices (including BP, HR, LAD, LVEDD, LVESD, LVEF, BNP level, 6 min walk distance) were measured and compared with the Arg389Gly genotypes, which identified by PCR-restriction fragment length polymorphism analysis. We also determined the Arg389Gly genotypes in 100 healthy control subjects, and compared the distribution of Arg389Gly genotypes with that in CHF.

RESULTSNo difference was observed between the two groups in any of the three genotypes (CC, CG and GG). The prevalences of the three genotypes in normal subjects and patients with CHF were Arg389Arg 0.53 vs. 0.51, Arg389Gly 0.40 vs. 0.40, Gly38Gly 0.07 vs. 0.09, respectively. After 3 months of bisoprolol usage, a significant improvement in LVEF was observed in CC group, which increased from (36.7 +/- 8.63)% to (44.1 +/- 9.53)%, CG group, from (35.76 +/- 8.39)% to (42.90 +/- 9.41)%, but not GG group, from (36.00 +/- 5.66)% to (37.33 +/- 5.64)%. The improvement in BNP was also observed in CC [from (502.93 +/- 160.80) ng/L to (325.26 +/- 135.63) ng/L], CG [from (525.76 +/- 157.66) ng/L to (331.79 +/- 133.97) ng/L], but not GG [from (505.33 +/- 125.07) ng/L to (429.67 +/- 182.39) ng/L]. Arg389-homozygous patients showed a substantially greater improvement in LVEF and BNP, compared with Gly389-homozygous patients (all P < 0.01).

CONCLUSIONSThere was no difference in the prevalence of the three genotypes between healthy and CHF subjects. The Gly389 polymorphism of the beta(1)-AR gene was not associated with an increased risk of CHF. The Arg389 variant of the beta(1)-AR gene was associated with a greater response to bisoprolol than that of the Gly389 variant in patients with CHF.

Adrenergic beta-Antagonists ; therapeutic use ; Adult ; Aged ; Aged, 80 and over ; Bisoprolol ; therapeutic use ; Case-Control Studies ; Female ; Follow-Up Studies ; Heart Failure ; drug therapy ; genetics ; physiopathology ; Humans ; Male ; Middle Aged ; Natriuretic Peptide, Brain ; blood ; Polymorphism, Genetic ; Receptors, Adrenergic, beta-1 ; genetics

To explore novel ADP receptor inhibitors with anti-thrombotic activity, eighteen compounds were synthesized and their structures were confirmed by 1H NMR and MS. The results showed that the activity of compound C1 was superior to ticlopidine in platelet aggregation inhibition tests in vivo and worthy for further investigation. Compounds A4, B2, C4 and C7 possessed moderate platelet aggregation inhibitory activities.
Animals ; Male ; Molecular Structure ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Purinergic P2Y Receptor Antagonists ; chemical synthesis ; chemistry ; pharmacology ; Random Allocation ; Rats ; Rats, Wistar ; Thienopyridines ; chemical synthesis ; chemistry ; pharmacology

This study was purposed to investigated and analyze the allelic frequency of a common allele HLA-C*08:22 in the southern Chinese Han population. A total of 32 samples with the C*08:01:01/08:22 ambiguous results previously identified in 163 unrelated southern Chinese Han population by routine sequencing based typing (SBT) at exons 2 - 4 of HLA-C gene were subjected to HLA-C SBT at exons 5 and 6 using our in-house method. Forty C*08:01:01-positive unrelated donor/recipient pair identified before the C*08:22 allele were officially nomenclatured and released by the World Health Organization (WHO) Nomenclature Committee for Factors of HLA System, were re-sequenced at exons 2 - 6 of HLA-C gene by our in-house SBT method. The allele assignment was accomplished with the Assign 3.5 SBT software. The results showed that three samples were identified as C*08:22-positive in the 32 samples with C*08:01:01/08:22 ambiguous results, the allele frequency of C*08:22 was 0.92% in the southern Chinese Han population. Retrospective analysis indicated that 2 donor/recipient pairs previously identified as C*08:01:01-positive were actually C*08:22-positive in the 40 tested donor/recipient pairs. It is concluded that the novel C*08:22 allele is the common allele in southern Chinese Han population, it can't be considered as rare allele and is ruled out for the samples with C*08:01:01/08:22 ambiguous results.
Alleles ; Asian Continental Ancestry Group ; genetics ; China ; Gene Frequency ; Genetics, Population ; HLA-C Antigens ; genetics ; Humans ; Sequence Analysis, DNA ; Unrelated Donors

Objective To observe the effect of carvedilol on the expression of Cx43 in rabbits with myocardial infarction and its association with ventricular arrhythmia.Method Thirty-six rabbits were randomly divided into three groups in equal number(n=12),namely,myocardial infarction(MI)group,carvedilol group and sham MI group.Rabbits of carvedilol group were administered with carvedilol 5 mg kg~(-1)?d~(-1)after MI induced,while no carvedilol was administered to the MI group.The following observations were made:(1)Cx43 density of the epicardial border zone measured by quantitative immnuoconfocal laser scanning,and(2)cx43 protein expression analyzed by western blot.Results(1)Under immunoconfocal laser microscope,the relative density of Cx43 was(0.16?0.06)% in the infarction group and was(0.32?0.11)% in the sham MI group [(0.68?0.15)%,both P

BACKGROUND: Currently, there are few studies about prostaglandin E1 in the paracrine and migration of bone marrow mesenchymal stem cells. OBJECTIVE: To explore the effects of prostaglandin E1 in the paracrine and migration of bone marrow mesenchymal stem cells. METHODS: Bone marrow mesenchymal stem cells isolated from Sprague Dawley rats were cultured in vitro. Passage 3 cells were co-cultured with prostaglandin E1 at concentrations of 10 μg/L, and then culture supernatant was collected at 3, 6, 9, 12, 24, 48, and 72 hours after co-culture. The level of vascular endothelial growth factor was detected by enzyme-linked immunosorbent assay. Effects of prostaglandin E1 on the migration of bone marrow mesenchymal stem cells were detected by Transwell assay and cell scratch assay. RESULTS AND CONCLUSION: After treatment with prostaglandin E1 for 3 hours, bone marrow mesenchymal stem cells began to secrete vascular endothelial growth factors, and the secretion level was peaked at 24 hours and then gradually decreased. Results from the Transwell assay and cell scratch assay showed that the migration ability of bone marrow mesenchymal stem cells was significantly promoted by prostaglandin E1 (P < 0.05). Overall findings reveal that prostaglandin E1 promotes the secretion of vascular endothelial growth factor from bone marrow mesenchymal stem cells and enhances cell migration.

Objective To investigate the pathogens spectrum and epidemiological characteristics of rash and fever illness (RFIs) from January 2010 to December 2017 in Pudong New Area, in order to provide scientific evidence for the prevention and control ofRFIs.Methods Enzyme-linked immunosorbent assay and real-time fluorescence quantitative polymerase chain reaction were used to detect the pathogens of enterovirus, measles virus, rubella virus and others from 2 831 clinical samples, and statistical analysis was performed.Results Pathogens were found in 1 633 samples in total, accounting for 68.59%. The top 4 viruses in the pathogen spectrum were enterovirus (52.54%), measles virus (28.54%), rubella virus (13.04%), and varicella-zoster virus (3.37%). There was significnat difference in the detection rate of rubella pathogens among patients of different genders(P=0.026). In the pathogen spectrum of infections of different age groups, the detection rate of enteroviruses at the age of 3-6 years was higher than that of other age groups. The detection rate of varicella-zoster virus at the age of 6-18 years old was higher than that of other age groups. The detection rate of virus including measles virus, rubella virus, dengue virus and small DNA virus in age of 18 and older was higher than that of other age groups. There was significant difference in the detection rate of pathogens in different age groups (all P<0.05).The incidence of RFIs was the highest in spring (41.52%) and the lowest in winter (15.00%). There was a statistical difference in the detection rate of enterovirus, measles, rubella and dengue virus in different seasons (P<0.05).Conclusions Enteroviruses and measles viruses are the main pathogens leading to RFIs in Pudong New Area, and the activity level of RFIs pathogens should be monitored for a long time.