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Objective To optimize the spray drying process of Banlangen(Isatidis Radix)formula granules based on quality by design(QbD)concept.Methods Using powder yield and the contents of uridine,adenosine,guanosine,and(R,S)-goitron as the critical quality attributes(CQAs),Plackett-Burman design was used to screen out critical process parameters(CPPs)for inlet temperature,spray pressure,liquid temperature,pump speed,and liquid relative density.The central-composite design(CCD)test was used to optimize the CPPs,which were screened.Based on the quadratic polynomial regression model,the design space of spray drying process of Banlangen(Isatidis Radix)formula granules was established,and further validated by experiments.Results Plackett-burman test results show that liquid relative density and inlet velocity are the key parameters for the study.The variance analysis results of CCD test showed that the constructed model in a good prediction ability,since the P-values of model was less than 0.01 and P-values of items lack of fit was more than 0.05.The optimized design space of CPPs was the liquid relative density 1.05-1.08,and pump speed 30%-40%.Conclusion Based on the QbD concept,the design space for the spray drying process of Banlangen(Isatidis Radix)formula granules can improve the stability of its process and help ensure the consistency of product quality.

BACKGROUND:As a routine method after lumbar spine surgery,a drainage tube is convenient for postoperative bleeding drainage and management,and there is still no consensus on the choice of postoperative removal time for short-segment lumbar spine surgery with less risk. OBJECTIVE:To explore the effect of different drainage times on early clinical efficacy after short-segment lumbar fusion. METHODS:A prospective randomized controlled study was performed on 220 patients in the Affiliated Hospital of Southwest Medical University who underwent posterior lumbar interbody fusion for lumbar degenerative diseases from March 2017 to April 2021.According to the different drainage times,the patients were randomly divided into removal on the second day after operation(group A),removal on the third day after operation(group B),and removal after the observation method 24-hour drainage volume<30 mL(group C).The perioperative indicators and follow-up results of the three groups of patients were observed and compared. RESULTS AND CONCLUSION:(1)Because 7 patients were lost to follow-up,2 patients were excluded,and 211 patients were finally included(72 patients in group A,71 patients in group B,and 68 patients in group C).(2)The average drainage time of group C was 2.91 days.The postoperative drainage volume in group A was significantly less than that in groups B and C,and the difference was statistically significant(P<0.05).On day 3 after operation,the hematocrit value of group C was lower than that of group A and group B,and the difference was statistically significant(P<0.05).Postoperative activity time and hospital stay in group A were shorter than those in groups B and C,and the difference was statistically significant(P<0.05).(3)Four patients in group A,two patients in group B and three patients in group C received an allogeneic blood transfusion.There was no significant difference among the groups(P>0.05).(4)In terms of postoperative complications,there were no statistical differences in postoperative wound leakage and surgical site infection in all three groups(P>0.05).(5)All patients were followed up for more than 12 months.Visual analog scale score and Oswestry dysfunction index of the three groups of patients before discharge and at the last follow-up were significantly improved compared with those before surgery(P<0.05).There was no statistical significance among the groups(P>0.05).(6)It is indicated that the removal of the drainage tube on the second day after a posterior lumbar fusion can effectively reduce the time to get out of bed and hospital stay,without increasing the postoperative blood loss and the risk of complications.

BACKGROUND:Some patients with cervical spondylosis have not been fully corrected sagittal position balance after cervical surgery,and this continuous sagittal position imbalance may be an important reason for the poor long-term clinical outcome of patients. OBJECTIVE:To analyze the correlation between the cervical sagittal position balance parameters and their changes and the clinical efficacy of patients in the unbalanced state after anterior cervical decompression and fusion and to explore the necessity of surgical correction of sagittal balance in order to improve the clinical effect in the later stage. METHODS:A retrospective analysis was performed on 125 patients with cervical spondylosis who underwent anterior cervical decompression and fusion in the Department of Spinal Surgery of Affiliated Hospital of Southwest Medical University from July 2019 to July 2022.Follow-up patients had good postoperative recovery(neck disability index score less than 10%one week after surgery)and had complete follow-up data.According to the axial vertical distance(C2-7 SVA)in sagittal position one week after surgery,patients were divided into type I imbalance group(C2-7 SVA loss≤5 mm,n=27),type Ⅱ imbalance group(C2-7 SVA loss>5 mm,and≤10 mm,n=19),and type Ⅲ imbalance group(C2-7 SVA loss>10 mm,n=12),and non-unbalanced group(C2-7 SVA in the normal range,n=67).The changes of visual analog scale score and neck disability index were compared among groups postoperatively and the last follow-up,as well as the changes of imaging sagittal balance parameters C2-7 cobb angle,C2-7 SVA value,neck inclination angle,T1 inclination angle,and thoracic entrance angle.The correlation between the late clinical effect and postoperative cervical sagittal disequilibrium was explored. RESULTS AND CONCLUSION:(1)There was no statistical difference in general data among the four groups(P>0.05).All patients underwent successful surgery without serious complications and postoperative wound infection.The follow-up time was more than 1 year.(2)There was no significant difference in preoperative symptom score and clinical efficacy one week after surgery(P>0.05).At the last follow-up,pain visual analog scale score,neck disability index and C2-7 SVA were lower than those before surgery but higher than those one week after surgery(P<0.05).C2-7 cobb angle was increased compared with those before operation(P<0.05).T1 inclination angle was decreased compared with those before operation(P<0.05).(3)Pearson correlation test showed that the change of neck disability index was positively correlated with the change of C2-7 SVA(P<0.05).(4)It is indicated that anterior cervical decompression and fusion is effective in the treatment of cervical spondylosis,and can effectively relieve the symptoms of patients.Patients with more severe cervical sagittal disequilibrium after surgery had worse curative effect in the later period.Continuous sagittal disequilibrium in patients with cervical spondylosis after surgery is an important cause of poor curative effect in the later stage.Clinicians should pay more attention to the correction of cervical sagittal balance before and during surgery,formulate surgical strategies and plans according to sagittal balance parameters before surgery,and correct C2-7 SVA intraoperatively to the normal range.

Objective: To analyze the clinical and imaging characteristics of stage Ⅰ occupational cement pneumoconiosis patients. Methods: In October 2021, the data of patients with occupational cement pneumoconiosis diagnosed by the Third Hospital of Peking University from 2014 to 2020 were collected, and the data of the patients' initial exposure age, dust exposure duration, diagnosis age, incubation period, chest X-ray findings, lung function and other data were analyzed retrospectively. Spearman grade correlation was used for correlation analysis of grade count data. The influencing factors of lung function were analyzed by binary logistic regression. Results: A total of 107 patients were enrolled in the study. There were 80 male patients and 27 female patients. The inital exposure age was (26.2±7.7) years, the diagnosis age was (59.4±7.9) years, the dust exposure duration was (17.9±8.0) years, and the incubation period was (33.1±10.3) years. The initial dust exposure age and the dust exposure duration in female patients were less than those in men, and the incubation period was longer than that in men (P<0.05). The imaging analysis showed the small opacities as"pp"accounted for 54.2%. 82 patients (76.6%) had small opacities distributed in two lung areas. The lung areas distribution of small opacities in female patients was less than that in male patients (2.04±0.19 vs 2.41±0.69, P<0.001). There were 57 cases of normal pulmonary function, 41 cases of mild abnormality and 9 cases of moderate abnormality. The number of lung regions with small opacities on X-ray was the risk factor for abnormal lung function in cement pneumoconiosis patients (OR=2.491, 95%CI=1.197-5.183, P=0.015) . Conclusion: The patients with occupational cement pneumoconiosis had long dust exposure duration and incubation period, light imaging changes and pulmonary function damage. The abnormal lung function was related to the range of pulmonary involvement.
Humans ; Female ; Male ; Adolescent ; Young Adult ; Adult ; Middle Aged ; Aged ; Retrospective Studies ; Pneumoconiosis ; Dust ; Hospitals ; Image Processing, Computer-Assisted

Humans ; Consensus ; Pancreatic Neoplasms/therapy* ; Neuroendocrine Tumors/therapy*

Scaffold hopping refers to computer-aided screening for active compounds with different structures against the same receptor to enrich privileged scaffolds, which is a topic of high interest in organic and medicinal chemistry. However, most approaches cannot efficiently predict the potency level of candidates after scaffold hopping. Herein, we identified potent PDE5 inhibitors with a novel scaffold via a free energy perturbation (FEP)-guided scaffold-hopping strategy, and FEP shows great advantages to precisely predict the theoretical binding potencies ΔG _FEP between ligands and their target, which were more consistent with the experimental binding potencies ΔG _EXP (the mean absolute deviations | Δ G FEP - Δ G EXP |  < 2 kcal/mol) than those ΔG _MM-PBSA or ΔG _MM-GBSA predicted by the MM-PBSA or MM-GBSA method. Lead L12 had an IC₅₀ of 8.7 nmol/L and exhibited a different binding pattern in its crystal structure with PDE5 from the famous starting drug tadalafil. Our work provides the first report via the FEP-guided scaffold hopping strategy for potent inhibitor discovery with a novel scaffold, implying that it will have a variety of future applications in rational molecular design and drug discovery.

Eight sesquiterpenoids were isolated from petroleum ether extract of Aquilariae Lignum Resinatum by various column chromatography techniques including silica gel, ODS, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, UV, IR, MS, and NMR spectroscopic data as(4S,5S,7R,10S)-5,7-dihydroxy-11-en-eudesmane(1),(7R,10S)-eudesma-4-en-11,15-diol(2),(2R,4S,5R,7R)-2-hydroxyeremophila-9,11-dien-8-one(3), 7α-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(4),(+)-9β,10β-epoxyeremophila-11(13)-en(5), 4(14)-eudesmene-8α,11-diol(6), 12,15-dioxo-selina-4,11-dien(7), and 2β,8 aα-dihydroxy-11-en-eremophilane(8). Compounds 1 and 2 are new compounds, and their absolute configurations were determined by calculating ECD. Compounds 1, 4, and 6-8 could significantly improve taurocholic acid(TCA)-induced gastric mucosal GES-1 cell injury at a concentration of 20 μmol·L~(-1), and the cell protection rates were 23.51%±2.79%, 16.10%±1.25%, 24.45%±4.89%, 17.48%±2.93%, and 21.44%±2.39%, respectively.
Chromatography, High Pressure Liquid ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Sesquiterpenes/chemistry*

The incidence of carbamate insecticide poisoning has increased gradually in recent years, and anticholinergic drugs are the specific antidotes. In 2020, the Peking University Third Hospital admitted a patient with carbamate insecticide poisoning, whose main clinical manifestations were dizziness, vomiting and blurred vision. During the treatment with penehyclidine hydrochloride, the patient developed delirium. This paper retrospectively analyzed the clinical data and treatment process of the patient to improve people's understanding of the side effects of penhyclidine hydrochloride in the treatment of insecticide poisoning.
Humans ; Insecticides ; Retrospective Studies ; Hydrochloric Acid ; Carbamates/therapeutic use* ; Delirium ; Poisoning/therapy* ; Organophosphate Poisoning/drug therapy*