ABSTRACT
OBJECTIVE To evaluate the effects of pharmaceutical interventio n led by clinical pharmacists on medication appropriateness of elderly inpatients. METHODS A non-randomized concurrent controlled trial was carried out. Elderly patients admitted to two treatment groups in the geriatric department of Yancheng First People ’s Hospital since June 2021 were selected as the research objects. According to the inclusion and exclusion criteria ，the first 40 patients were selected from each of the two treatment groups （according to the order of admission time ）and set as the control group or the intervention group. The control group received routine treatment and nursing services ，and the intervention group additionally received pharmaceutical intervention led by clinical pharmacists on the basis control group. Clinical pharmacists found potential inappropriate medication （PIM）and put forward suggestions on optimization of medication regimen. American Geriatrics Society 2019 Updated AGS Beers Criteria ® for PIM Use in Older Adults （hereinafter referred to as “Beers criteria ”）and the Criteria of PIMs for Older Adults in China 2017 Edition （hereinafter referred to as “Chinese criteria ”）were used as reference tools for drug use review. The medication appropriateness index （MAI）total scores （main evaluation indicator ），the number of PIMs ，the number of drugs used ，the length of hospital stay ，the number of drug-related adverse events during hospital stay ，the number of drug regimen optimization suggestions by pharmacists ， and implementation rate of E-mail：zhihuadou@163.com optimization suggestions adopted by clinicians were compared between 2 groups at admission and at discharge. RESULTS At admission ，there were no statistically differences in MAI total scores，the number of PIMs based on Beers criteria ，the number of PIMs based on Chinese criteria or the number of drugs used between 2 groups（P＞0.05）. At discharge ，there were no statistically differences in the number of PIMs based on Chinese criteria and the length of hospital stay between 2 groups（P＞0.05），but the MAI total scores ，the number of PIMs based on Beers criteria and the number of drugs used in the intervention group were lower than those in the control group （P＜0.05）. In the intervention group，the proportion of drugs recorded as “inappropriate medication ”at admission （34.5％）was significantly higher than that at discharge（19.5％）（P＜0.05）. The difference between the number of drugs discharged from hospital and the number of drugs admitted to hospital in the control group [ 3（1-4.8)] was significantly higher than that in the intervention group [ 1（0-2.8)]（P＝ 0.012）. Compared with admission ，the proportion of drugs recorded as “inappropriate medication ”in the intervention group at discharge was significantly decreased on the basis of “effectiveness”dimension and “course”dimension （P＜0.05）. During hospitalization，clinical pharmacists put forward 70 optimization suggestions of drug regimen for the intervention group ，among which 39 suggestions were adopted and implemented by clinicians ，with an implementation rate of 55.7％. CONCLUSIONS The pharmaceutical intervention led by clinical pharmacists can improve overall appropriateness of drug use in the elderly inpatients using MAI as main evaluation indicator.
ABSTRACT
OBJECTIVE：To prepare supersaturated system of lip ophilic aci clovir（ACV）prodrug，and to increase the cutaneous bioavailability of ACV. METHODS ：Three prodrugs of ACV were synthesized by anhydride acylation ，i.e. aciclovir acetate （ACV-Ace），butyrate（ACV-But）and hexanoate （ACV-Hex）. The structures of ACV and three ACV prodrugs were confirmed by 1H-NMR and HRESI-MS ；the concentrations of ACV and three ACV prodrugs were determined by UPLC-triple quadrupole tandem mass spectrometry ，and saturated solubility of them in different volume fractions of propylene glycol-water solution was calculated. The compound with the greatest potential of form supersaturated system was screened out. The supersaturated system of that compound was prepared by co-solvent method. The effect of hydroxypropyl methylcellulose E 3 （HPMC E 3） on its physical stability was observed by light microscope. Vertical Franz diffusion cells were used to study the effects of degree of supersaturation （DS）and HPMC E 3 on the deposited amount of drug in the excised porcine skin after using the supersaturated system for 1 h. The distribution of ACV in the excised porcine skin was determined by frozen slicing stratified quantitative method after using the supersaturated system and marketed aciclovir cream for 1 h. RESULTS ：Three ACV prodrugs were successfully synthesized. The established quantification methods met the requirements of biological sample analysis. Among all of the three ACV prodrugs ， ACV-Hex showed the lowest saturated solubility in water [ （0.5±0.0）mmol/L] a nd the highest saturated solubility in propylene glycol [（53.4 ± 14.2）mmol/L]，which made it potentially feasible to form supersaturated system with high DS. In 10％propylene glycol-water system ，the addition of HPMC E 3 163.com enabled ACV-Hex supersaturated systems ，with DS no morethan 4，to maintain physical stability within 1 h. The total deposited amount （ACV + ACV-Hex ） in skin after the application of ACV-Hex supersaturated system with DS of 4 for 1 h was higher than that after the application of ACV-Hex supersaturated system with DS less than 4 or without HPMC E 3. In addition ，the concentration of ACV in the basal epidermis （skin thickness was 100-160 mm）by supersaturated system was significantly higher than that of the marketed aciclovir cream （P＜0.05）. CONCLUSIONS：ACV-Hex，the lipophilic prodrug of ACV ，can form stable supersaturated system with DS of 4 in 10％ propylene glycol-water system in the presence of HPMC E 3. High concentration of ACV could be accumulated in the basal epidermis after the skin was exposed to supersaturated system for 1 h，which may be valuable for local treatment skin infection of herpes simplex virus .
ABSTRACT
Objective:To optimize the extraction technology of compound Xiongdan capsules. Methods: The effects of water a-mount, decoction duration and decoction times on the water extraction technology were investigated by orthogonal design using the ex-tract derivation rate and the content of ginsenoside Rg1 , Re and Rb1 as the indices. Results:The optimal water extraction conditions for ginseng and Nidus vespa were as follows:decocting three times with 8-fold of water, and extracting for one hour each time. The extract was condensed until the relative density was 1.20(80-90℃), and then dried and crushed into fine powder. The other herbs were crushed into fine powder and screened by No. 5 meshes. The above powder was blended and well mixed with starch, and then packed into capsules. Conclusion:The optimized water extraction technology is stable, feasible and reproducible, which provide reference for industrial production.
ABSTRACT
Aim To study the effects of 2 ,3 ,4 ’ ,5-tet-rahydroxystilbene-2-O-β-D glucoside ( TSG ) on myo-cardial fibrosis ( MF) induced by isoproterenol ( ISO) in mice and its possible mechanism. Methods MF in mice was induced by subcutaneous injection of isoprot-erenol for 14 days. TSG (30,60,120 mg·kg-1 ) and captopril ( 40 mg · kg-1 ) were then administered by gavage to mice. The experiment was stopped 12 h after the last administration of the drugs. Hematoxylin-eosin ( HE) and Masson staining were used to estimate the extent of MF. Level of hydroxyproline in myocardial tissues was measured. Protein expressions of collagenⅠ, collagen Ⅲ and transforming growth factor-β1 (TGF-β1) in myocardial tissues were measured. Lev-els of superoxide dismutase ( SOD ) and glutathione peroxidase ( GSH-Px ) were determined. Results Compared with control mice, the level of hydroxypro-line in myocardial tissues was significantly increased in isoproterenol treated mice. Histological sections of iso-proterenol-treated hearts showed extensive myocardial fibrosis. And protein expressions of collagenⅠand col-lagen Ⅲwere markedly increased in isoproterenol trea-ted mice. However, therapy with TSG decreased the level of hydroxyproline in myocardial tissues, ameliora-ted the degree of myocardial fibrosis, and reduced the collagen expressions induced by isoproterenol adminis-tration. Moreover, treatment with TSG decreased TGF-β1 protein expression and elevated the myocardial SOD and GSH-Px activity. Conclusion TSG can inhibit MF formation induced by ISO in mice which might be due to regulating TGF-β1 protein expression and its an-tioxidant effect.
ABSTRACT
Aim: To study the effects of astragaloside IV on experimental ventricular remodeling in mice and its mechanism from matrix metalloproteinase aspect.Method: Ventricular remodeling in mice was induced by con-secutively subcutaneous injection of isoproterenol for 14 days.Astragaloside IV(40,80 mg/kg)and propranolol(40 mg/kg,positive control)were administered by gavage to mice.Echocardiography was used to observe the left ventricular end diastolic diameter(LVIDd),left ventricular end systolic diameter(LVIDs),fractional shortening(FS)and ejection fraction(EF).The myocardial pathological pattern was detected by HE staining.Expressions of matrix metalloproteinases(MMP2,MMP9)and tissue inhibitor of metalloproteinases(TIMP1,TIMP2)mRNA in myocardium were detected by RT-PCR.Activities of MMP2 and MMP9 were assayed by zymography.Results:Compared with those of control mice,LVIDd and LVIDs were increased,FS and EF were decreased in the model group.Myocardial injury and fibrosis existed in histop at hological slices of the model group.In addition,the mRNA expressions and activities of MMP2 and MMP9 were increased in the model group.However,there were no markable changes to TIMP1 and TIMP2.Treatment with astragaloside IV reduced LVIDd and LVIDs,increased FS and EF,attenuated myocardial injury,and down-regulated mRNA expressions and activities of MMP2 and MMP9 compared with the model group.Conclusion: Astragaloside IV can greatly improve ventricular remodeling and dysfunction via decreasing MMP2 and MMP9 mRNA expression and activities in cardiac ventricles.
ABSTRACT
Aim To study the effect of 2,3,4′,5-tetrahydroxystilbene-2-O-?-D glucoside(TSG) on vascular smooth muscle cells(VSMCs) proliferation induced by fetal bovine serum and explore the underlying mechanisms.Methods VSMCs were cultured from rat aorta using explant technique.VSMCs proliferation was analyzed by 5-bromo-2-deoxyuridine(Brdu) incorporation assay.Cell cycle phase distributions were determined by flow cytometry.The expression of proliferating cell nuclear antigen(PCNA) was evaluated by Western blot analysis.The level of intracellular reactive oxygen species(ROS) was estimated through fluorescence assay.The intracellular activities of superoxide dismutase(SOD),catalase(CAT),and glutathi one peroxidase(GSH-px) were measured using biochemical method.Results TSG in the experimental concentration 0.1～100 ?mol?L~-1 exhibited no apparent cytotoxocity.10 ?mol?L~-1 and 100 ?mol?L~-1 TSG significantly inhibited the proliferation of VSMCs induced by serum,cell cycle transition from G0/G1phase to S phase,PCNA expression in nucleus of VSMCs and level of intracellular ROS.100 ?mol?L~-1 TSG markedly increased the activities of SOD and GSH-px.Conclusions Certain concentration of TSG can prevent VSMCs proliferation effect mediated by serum;the mechanism about TSG effect may be associated with arresting G0/G1 to S progression,decreasing PCNA expression and improving the antioxidation of VSMCs.