The polymorphism and thermostability of nirmatrelvir, the main antiviral component of the oral COVID-19 treatment drug, were studied. Four polymorphs of nirmatrelvir were prepared by recrystallization methods. Among them, Form 1 and nirmatrelvir methyl tert-butyl ether solvate (Form 2) had been reported in the literature, while nirmatrelvir isobutyl acetate solvate (NMTW-IBAC) and nirmatrelvir ethyl acetate solvate (NMTW-EA) are two new solvates. The crystal structures were characterized by single-crystal X-ray diffraction, powder X-ray diffraction, thermogravimetric analysis and differential scanning calorimetry. The thermostability of polymorphism and crystalline transformation were also investigated by combining Hirshfeld surface analysis and interaction energy analysis. The results showed that nirmatrelvir Form 1 belongs orthorhombic crystal system with the space group P2₁2₁2₁ and one nirmatrelvir molecule included in the asymmetric unit, which has the same crystal structure as nirmatrelvir Form 4 reported in the literature. Owing to its larger thermal expansion, the differences in crystallographic parameters obtained at different temperatures were found between Form 1 and Form 4. Three solvates of nirmatrelvir belonged to the iso-structural with monoclinic crystal system and the space group P2₁, in which the asymmetric unit contains one nirmatrelvir molecule and one solvent molecule. The thermal analysis results showed that nirmatrelvir Form 1 was a solvent-free crystal form with the best thermal stability and the strongest intermolecular hydrogen bonding. Among the three solvates, NMTW-EA has the worst thermal stability and the weakest hydrogen bonding interaction between the nirmatrelvir molecule and the solvent molecule. The energy framework of nirmatrelvir solvates showed that the closer the arrangement between solvent and nirmatrelvir molecules, the greater the total interaction energy between solvent and nirmatrelvir molecules. The phase transition studies of the three solvates showed that NMTW-IBAC and NMTW-EA were transformed into amorphous after desolvation, respectively, while Form 2 undergoes oiling during desolvation. The research provides theoretical guidance for the analysis, identification and quality control of nirmatrelvir polymorphs.

Objective To discuss the effect of homemade oxygen gasbag on ICU patients with scrotal edema.Methods Seventy-two ICU patients with scrotal edema,in which 60 cases had erythema,peeling and seepage,were chosen and divided into the observation group and the control group,each with 36 cases.The observation group received treatment of air inflation by oxygen gasbag while the control group received treatment of infrared radiation and hydropathic compress of 33％ MgSO4.Both groups also received active treatment of primary disease,nutrition improvement,hypoalbuminemia rectifying,pain control and anxiety relief.Effects of two groups were compared.Results Effect on scrotal edema patients was better in the observation group than in the control group.There were 26 cases (72.7％) who had excellent effects,9 cases (25.0％) who had effects and 1 case (2.7％) who had no effect in the observation group,and there were 19 cases (52.7％) who had excellent effects,8 cases (22.2％) who had effects and 9 cases (25.0％) who had no effect in the control group.The difference was statistically significant (x2 =7548,P =0.023).The effect on patients with scrotal edema,erythema,peeling and seepage was also better in the observation group than in the control group,and the difference was statistically significant (x2 =9.977,P =0.007).Conclusions Homemade oxygen gasbag is a safe,effective,simple,economical and comfortable way to treat scrotal edema,which is worthy of clinical promotion.

To study the relationship between hematopoiesis and primordial germ cells, chick embryos at different developing stages were flatbed and located. After fixed by glutaral, the embryos were PAS and HE stained respectively, dehydrated serially, transparent, mounted, and were observed in situ or in cut sheet condition. The results showed: (1) the cellule amorphous and the disposition in chick embryo of PGCs were coincident no matter stained by PAS or HE staining, and HE staining could disclose the morphologic characteristics more clearly, exactly and completely; (2) genesis of blood island could be observed at the boundary of light and dark region of the extraembryonic blastoderm at about 26 hours; (3) both the blood vessel endothelium cells and free cells of the blood island were differentiated from PGCs. The generating of genuine yolk sac was at about 44 - 48 hours. It is concluded that the initial anatomic site of blood island genesis may be is mesoblast of extraembryonic blastoderm rather than the yolk sac; the blood vessel endothelium cells and the blood cells are generated parallel; the PGCs are the common ancestry of angioblast and HSC.
Animals ; Cell Differentiation ; Cell Movement ; Cells, Cultured ; Chick Embryo ; cytology ; Hematopoietic System ; cytology

Objective To explore the influencing factors on short -term efficacy of intravenous thrombolysis with rt -PA.Methods The clinical data of the 95 acute ischemic stroke(AIS)patients who received thrombolytic therapy were analyze.Multivariate logistic regression analysis was used to determine the possible influencing factors. Results Fifty -six(58.95%)patients had favourable outcomes after thrombolytic therapy for 24 hours.Multivariate logistic regression analysis indicated that diabetes(OR =3.933,95% CI 1.199 ~12.897)and TOAST classification (OR =1.448,95% CI 1.032 ~2.032 )were the independent predictors of short -term outcome.Conclusion Diabetes and TOAST classification are the major influencing factors of short -term efficacy after intravenous thrombolysis with rt -PA.It should pay attention screening patients for intravenous thrombolysis therapy and predicting the efficacy of thrombolysis.

Objective To discuss the application of post quantification inspection in nursing quality management in ICU of Siehuan cancer hospital. Methods According to the nursing quality criteria, work specification and different requirements in each post and weighted value of each post, quantification inspection regulations and score standardization were formulated and brought into effect in each post. Results After theapplication of post quantification inspection, the nursing service quality and patients' satisfaction to nursingservice were improved. This method could scientifically embody the quality of nursing work, and alsoconsummated the head nurses' administration, thereby improving the professional level of nurses to some extent.Conclusions The application of post quantification inspection enhances the science and operation of nursingmanagement, and helps to improve the level of nursing management.

Objective To evaluate the effectiveness of blood gas analysis in samples from two regions.Methods 112 patients with APACHE Ⅱ scores 27 ～ 43 were taken arterial blood from dorsalis pedis artery and femoral artery respectively. Compare the clinical effect of the samples. Results There is no statistically significant difference between results of two blood collection methods ( P ＞ 0. 05 ), While there is statistically significant difference in puncture success ( 110 vs 100, χ2 = 14.23, P ＜ 0. 05 ), vein mistaken injury, hematoma formation, thrombosis, and compression time ( 12 vs 1,7 vs 0,6 vs 0,5.5 ±0.7 vs 2.5 ±0.5 ;χ2 =9.32,5.99,4.85,t = 38. 06, P ＜ 0. 05 ). Conclusions Blood collection method should be determined by the different situation of critically ill patients. Femoral artery blood sample should be taken with caution in order to prevent complication and improve quality of nursing care.

Professor HUANG's clinical acupuncture and moxibustion characters are introduced from selection of acupoints, needles used, needling methods, etc. Based on the differentiation of symptoms and signs, he is good at using pair-points and syndrome differentiation, point-through-point acupuncture and combined many methods, and pays attention to adjusting mental activity, promoting flow of qi, treating both body and mental treatment. He also uses other therapies besides acupuncture and adopts good advance from others, so as to greatly increase clinical therapeutic effects.
Acupuncture Therapy ; Diagnosis, Differential ; Humans ; Medicine, Chinese Traditional

Endoplasmic reticulum stress (ERS) is an adaptive process in response to circumstantial changes, but excessive and/or prolonged ERS can induce cell apoptosis. C/EBP homologous protein (CHOP) is a very important marker participating in ERS-associated cell apoptosis, while the role of the myocyte apoptosis induced by CHOP remains unclear in the development of hypertrophy. The present study aimed to investigate the effect of CHOP-mediated ERS-associated apoptosis on myocardial hypertrophy induced by abdominal aortic constriction in rats. Healthy male Wistar rats were randomly divided into model group (n=45) and control group (n=40). The rats in model group received abdominal aortic constriction. Hemodynamic changes, whole heart weight/body weight (HW/BW) and left ventricular weight/body weight (LVW/BW) were measured on 1 d, 3 d, 7 d, 14 d and 28 d after surgery, respectively. The mRNA expression of glucose-regulated protein 78 (GRP78), calreticulin (CRT) and CHOP, which are important markers of ERS, were detected by RT-PCR, and Western blot was used to assess the protein level of GRP78, CRT, CHOP, and apoptosis-associated proteins, Bax and Bcl-2. The results obtained were as follows. Compared with control group, the blood pressure, LVW/BW, and HW/BW of rats in model group increased significantly and cardiac function enhanced compensatively on 7 d after surgery, and increased progressively during the experiment. As early as 1 d after surgery, the mRNA level of CRT in model group increased by 136% (P< 0.01) compared with control, while the protein expression increased by 69.2% on 7 d after surgery (P<0.01). Both mRNA and protein expression of GRP78 increased by 20% and 186% (P<0.01) respectively on 7 d after surgery, and the expression sustained high level during the experiment afterwards. Correlation analysis indicated a positive correlation between +dp/dt(max) and CRT protein expression (r=0.780, P<0.01) as well as GRP78 protein expression (r=0.694, P<0.01). Prolonged ERS triggered myocyte apoptosis, as both the mRNA and protein level of CHOP in model group increased by 22.2% (P<0.01) and 76.0% (P<0.01) respectively compared with control on 7 d after hypertrophy (14 d after surgery), and meanwhile, the protein expression of pro-apoptotic Bax increased by 41.1% (P<0.01) and anti-apoptotic Bcl-2 protein expression decreased by 25.5% (P<0.01). Correlation analysis indicated a positive correlation between CHOP and Bax expression (r=0.654, P<0.01), and a negative correlation between CHOP and Bcl-2 expression (r=-0.671, P<0.01). These results suggest that abdominal aortic constriction induces a significant up-regulation in ER molecular chaperones at early stage of post-surgery, indicating that ERS response is activated in the rat heart; while prolonged ERS could lead to myocyte apoptosis, and CHOP-mediated ERS-associated apoptosis may contribute to myocardial hypertrophy. We speculate that cell apoptosis may take part in the regulation of myocardial hypertrophy and heart failure, and determine the progression of decompensated hypertrophy.
Animals ; Aorta ; physiopathology ; Apoptosis ; Calreticulin ; metabolism ; Constriction ; Endoplasmic Reticulum Stress ; Heat-Shock Proteins ; metabolism ; Hypertrophy ; pathology ; Male ; Myocardium ; pathology ; Rats ; Rats, Wistar ; Transcription Factor CHOP ; metabolism ; Up-Regulation ; bcl-2-Associated X Protein ; metabolism

OBJECTIVETo investigate the effect of Rhizoma Curcumae (RC), arsenite trioxide (As2O3) on proliferation ana signal transduction molecule in lens epithelial cell (LEC), in order to provide experiment evidence for prevention and treatment of after cataract.

METHODProliferation of cultured bovine LEC were induced by induced by recombinant human basic fibroblast growth factor (rhbFGF); Inhibitory rates of LEC proliferation induced by RC, As2O3 were detected by methyl thiazolyl tetrazolium (MTT); Inhibitory effects of expression of proliferating cell nuclear antigen (PCNA) induced by RC, As2O3 in LEC were assayed via flow cytometer (FCM); Concentrations of LEC calcium ([Ca2+]i) were determined by spectrofluoremeter, intracellular concentrations of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) of LEC were measured by radioimmunoassay.

RESULTInhibitory rates of RC, As2O3 on LEC proliferation induced by rhbFGF increased significantly, showing dose-dependent (P < 0.01). PCNA expression of LEC proliferation induced by rhbFGF were down regulated obviously by RC, As2O3, showing dose-dependent (P < 0.01). Concentrations of [Ca2+]and cAMP increased and cGMP decreased significantly in LEC of proliferation inhibited by RC, As2O3 (P < 0.01).

CONCLUSIONRC, As2O3 can inhibit LEC proliferation obviously. Signal transductions of [Ca2+]i, cAMP, cGMP may be the important molecular mechanism. There are broad prospect for RC, As2O3 on prevention and treatment of after cataract.

Animals ; Arsenicals ; pharmacology ; Calcium ; metabolism ; Cattle ; Cell Proliferation ; drug effects ; Cells, Cultured ; Curcuma ; chemistry ; Cyclic AMP ; metabolism ; Cyclic GMP ; metabolism ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Epithelial Cells ; cytology ; drug effects ; metabolism ; Fibroblast Growth Factor 2 ; genetics ; pharmacology ; Flow Cytometry ; Growth Inhibitors ; pharmacology ; Lens, Crystalline ; cytology ; drug effects ; metabolism ; Oxides ; pharmacology ; Proliferating Cell Nuclear Antigen ; metabolism ; Radioimmunoassay ; Recombinant Proteins ; pharmacology ; Rhizome ; chemistry ; Signal Transduction ; drug effects

The purpose of this study is to investigate the applicability of a natural swelling matrix derived from boat-fruited sterculia seed (SMS) as the propellant of osmotic pump tablets. The sugar components, static swelling, water uptake and viscosity of SMS were determined and compared with that of polythylene oxide (WSR-N10 and WSR-303). Both ribavirin and glipizide were used as water-soluble and water-insoluble model drugs. Then, the monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide were prepared using SMS as the osmotically active substance and propellant. SMS was mainly composed of rhamnose, arabinose, xylose and galactose and exhibited relatively high swelling ability. The area of the disintegrated matrix tablet was 20.1 times as that at initial after swelling for 600 s. SMS swelled rapidly and was fully swelled (0.5%) in aqueous solution with relative low viscosity (3.66 +/- 0.03) mPa x s at 25 degrees C. The monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide using SMS as propellant exhibited typical drug release features of osmotic pumps. In conclusion, the swelling matrix derived from boat-fruited sterculia seed, with low viscosity and high swelling, is a potential propellant in the application of osmotic pump tablets.
Arabinose ; chemistry ; isolation & purification ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Drug Carriers ; Galactose ; chemistry ; isolation & purification ; Glipizide ; administration & dosage ; chemistry ; Osmosis ; Plants, Medicinal ; chemistry ; Rhamnose ; chemistry ; isolation & purification ; Ribavirin ; administration & dosage ; chemistry ; Seeds ; chemistry ; Solubility ; Sterculiaceae ; chemistry ; Tablets ; Technology, Pharmaceutical ; methods ; Viscosity ; Water ; Xylose ; chemistry ; isolation & purification