In this article, three types of metal ions with different oxidation state as mercury(Ⅱ), cerium(Ⅲ) thorium(Ⅳ) have been reacted with captopril drug(CAP). The isolated solid complexes were explained using elemental ...In this article, three types of metal ions with different oxidation state as mercury(Ⅱ), cerium(Ⅲ) thorium(Ⅳ) have been reacted with captopril drug(CAP). The isolated solid complexes were explained using elemental analysis, conductance measurements, infrared and 1H-NMR spectroscopy as well as the thermo gravimetric(TG/DTG) analysis. The micro analytical and spectroscopic results for all CAP complexes were agreement with the speculated structures. The stoichiometry for divalent Hg^2+, trivalent Ce^3+ and tetravalent Th(4+) metal ions with CAP ligand was established with 1∶2(M(n+):CAP) molar ratio. The qualitative analysis showed that in case of the mercury(Ⅱ) complex, the chloride ions didn't involved in the complexity, suggesting formula [Hg(CAP)2] in neutral form. However, regarding both Ce(Ⅲ) and Th(Ⅳ) complexes as [Ce(CAP)2(NO3)]·3 H2O and [Th(CAP)2(NO3)2(H2O)]·3 H2O formulas, the nitrate group is existed inside the coordination sphere. The infrared analysis data proved that CAP drug act as a bidentate ligand with the metal ions of Ce(Ⅲ) and Th(Ⅳ) through oxygen carbonyl group C=O and oxygen of the deprotonated carboxylic COOH group, while for the Hg(Ⅱ) complex, the CAP acts as a bidentate ligand through oxygen of C=O group and sulfur atom of the deprotonated -SH group. Thorium(Ⅵ) complex has a nine-coordinate geometry, while Hg(Ⅱ) and Ce(Ⅲ) have a four and six-coordination behaviors respectively. The 1H-NMR data of the CAP compound has a singlet sharp signal at 1.90 ppm due to the proton of -SH group, this peak absent in the spectrum of the Hg(Ⅱ) CAP complex upon the deprotonated of thiol group.展开更多
The captopril/Chitosan-gelatin net-polymer microspheres(CTP/CGNPMs) were prepared using Chitosan(CTS) and gelatin(GT) by the methods of emulsification,cross-linked reagent alone or in combination and microcrystalline ...The captopril/Chitosan-gelatin net-polymer microspheres(CTP/CGNPMs) were prepared using Chitosan(CTS) and gelatin(GT) by the methods of emulsification,cross-linked reagent alone or in combination and microcrystalline cellulose(MCC) added in the process of preparation of microspheres,which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril(CTP). The results indicated that CTP/CGNPMs had a spherical shape,smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio(EMR) and composition of cross linking reagents. Among these factors,the EMR(1/4),CLR(FA+SPP) and 0.75% microcrystalline cellulose(MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER,DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%,9.95±0.77% and 261±42%,respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.展开更多
The captopril/ Chitosan-gelatin net-polymer microspheres （ Gap/ CGNPMs ） were prepared using Chitosan （ CS ） and gelatin （ Gel ） by the methods of emulsification. A cross linked reagent alone or in combination ...The captopril/ Chitosan-gelatin net-polymer microspheres （ Gap/ CGNPMs ） were prepared using Chitosan （ CS ） and gelatin （ Gel ） by the methods of emulsification. A cross linked reagent alone or in combination with microcrystalline cellulose （ MCC ） was added in the process of preparation of microspheres to eliminate dose dumping and burst phenomenon of microspheres for the improvemeat of the therapeutic efficiency and the decrease of the side effects of captopril （ Cap ）. The results indicate that Cap/ CGNPMs have a spherical shape , smooth surface roorphology and integral inside structure and no adhesive phenomena and good roobility , and the size distribution is mairdy from 220 to 280 μm. Researches on the Cap release test in vitro demonstrate that Cap/ CGNPMs are of the role of retarding release of Cap compared with Cap ordinary tablets （COT）, embedding ratio （ER） , drug loading （ DL ）, and swelling ratio （ SR ）, and release behaviors of CGNPMS are influenced by process conditions of preparation such as experimental material ratio （EMR） , composition of cross linking reagents. Among these factors , the EMR（1/4）, CLR （ FOR ＋ TPP） and 0.75% microcrystulline cellulose （MCC） added to the microspheres are the optimal scheme to the preparation of Cap/CGNPMs. The Cap/CGNPMs have a good characteristic of sustained release of drug, and the process of emulsifieation and crossinking process is simple and stable. The CGNPMs is probable to be one of an ideal sustained release system for water-soluble drugs.展开更多
目的探讨硝苯地平缓释片联合卡托普利片治疗老年高血压的临床效果。方法选择2019年11月—2021年4月收治的50例老年高血压患者,按照用药的不同分为对照组(25例,服用卡托普利片)与观察组(25例,服用硝苯地平缓释片+卡托普利片),比较2组疗...目的探讨硝苯地平缓释片联合卡托普利片治疗老年高血压的临床效果。方法选择2019年11月—2021年4月收治的50例老年高血压患者,按照用药的不同分为对照组(25例,服用卡托普利片)与观察组(25例,服用硝苯地平缓释片+卡托普利片),比较2组疗效情况,治疗前后血压水平[24 h平均收缩压(24 h SBP)、24 h平均舒张压(24 h DBP)、日间平均SBP(d SBP)、日间平均DBP(d DBP)、夜间平均SBP(n SBP)、夜间平均DBP(n DBP)],根据监测结果计算患者SBP、DBP变异性(24 h SBPV、24 h DBPV),比较2组不良反应发生情况。结果观察组疗效总有效率高于对照组,差异有统计学意义(P<0.05);观察组治疗后24 h SBP、d SBP、n SBP水平均低于对照组,差异有统计学意义(P<0.05),2组治疗后24 h DBP、d DBP、n DBP水平比较差异无统计学意义(P>0.05);观察组治疗后24 h SBPV、24 h DBPV水平低于对照组(P<0.05);2组不良反应发生率比较差异无统计学意义(P>0.05)。结论硝苯地平缓释片联合卡托普利片治疗老年高血压效果显著,能够有效控制患者24 h血压变异性,安全性高。展开更多
To explore the possibility of hydrogen sulfide (H 2S) as a messenger molecule in cardiovascular system, the authors discovered that H 2S (5×10 -5 -5×10 -4 mol·L -1 )exerted an effect on inhibiting endot...To explore the possibility of hydrogen sulfide (H 2S) as a messenger molecule in cardiovascular system, the authors discovered that H 2S (5×10 -5 -5×10 -4 mol·L -1 )exerted an effect on inhibiting endothelin 1 induced proliferation of cultured vascular smooth muscle cells (VSMCs) of rats in vitro . The 3H TdR incorporation decreased by 16.8%～37.4% in H 2S treated VSMCs as compared with the controls ( P <0.01). The inhibitory effect was found to be associated with reduced activity of MAPK. The authors also observed that endogenous H 2S levels markedly increased in vessels of rats with either endotoxic shock or septic shock [H 2S level (pmol·min -1 ·mg -1 ):tail artery (16.18±2.06) vs (8.12±0.55);mesenteric artery (10.17±1.11) vs (6.19 ±0.55);pulmonary artery(11.38±1.24) vs (5.27±0.51); aorta(6.21±0.48) vs (4.10± 0.28), P < 0.01 ]. The above findings suggested that H 2S might play an important role in the regulation of cardiovascular pathophysiologic events.展开更多
目的:了解3个不同产地、2个不同批次的红藤饮片6种次生代谢产物含量、抑菌活性及两者的相关性。方法:利用分光光度法对红藤饮片提取物的6种次生代谢产物含量进行分析,以金黄色葡萄球菌和枯草芽孢杆菌为实验菌株,用纸片琼脂扩散法测定抑...目的:了解3个不同产地、2个不同批次的红藤饮片6种次生代谢产物含量、抑菌活性及两者的相关性。方法:利用分光光度法对红藤饮片提取物的6种次生代谢产物含量进行分析,以金黄色葡萄球菌和枯草芽孢杆菌为实验菌株,用纸片琼脂扩散法测定抑菌圈大小;以平板二倍稀释法统计最小抑菌浓度(M IC);以试管二倍稀释法统计最小杀菌浓度(M BC)。结果:红藤药液对金黄色葡萄球菌和枯草芽孢杆菌的抑菌活性以安徽产地第一批次最高,抑菌圈大小、M IC、M BC分别为(9.67±0.29)mm、12.5 m g/m l、31.25 m g/m l和(10.17±0.58)mm、12.5 m g/m l、31.25 m g/m l,江苏产地第二批次最低,抑菌圈大小、M IC、M BC分别为(7.67±0.29)mm、25 m g/m l、125 m g/m l和(8.17±0.29)mm、25 m g/m l、125 m g/m l。红藤饮片提取物对金黄色葡萄球菌的抑菌活性在不同产地和不同批次之间均有显著性差异(P<0.01);对枯草芽孢杆菌的抑菌活性在不同产地亦有显著性差异(P<0.01),但不同批次之间无显著性差异(P>0.05)。红藤药液的6种次生代谢产物总量以安徽产地第一批次最高(3.61%),江苏产地第二批次最低(1.90%)。红藤提取物的总生物碱和游离蒽醌在不同产地之间有显著性差异(P<0.01),而在不同批次之间无显著性差异(P>0.05);总绿原酸、黄酮类化合物、总鞣质和总皂苷在不同产地和不同批次之间均有显著性差异(P<0.01)。影响红藤饮片对2种细菌的抑菌活性的主要次生代谢产物可能为总皂甙、总鞣质、游离蒽醌及总绿原酸。结论:不同红藤饮片的次代谢产物的含量及抑菌活性以安徽和浙江产地较高,江苏产地较低;红藤的抑菌活性与饮片中总皂甙、总鞣质、游离蒽醌及总绿原酸的含量密切相关。展开更多
文摘In this article, three types of metal ions with different oxidation state as mercury(Ⅱ), cerium(Ⅲ) thorium(Ⅳ) have been reacted with captopril drug(CAP). The isolated solid complexes were explained using elemental analysis, conductance measurements, infrared and 1H-NMR spectroscopy as well as the thermo gravimetric(TG/DTG) analysis. The micro analytical and spectroscopic results for all CAP complexes were agreement with the speculated structures. The stoichiometry for divalent Hg^2+, trivalent Ce^3+ and tetravalent Th(4+) metal ions with CAP ligand was established with 1∶2(M(n+):CAP) molar ratio. The qualitative analysis showed that in case of the mercury(Ⅱ) complex, the chloride ions didn't involved in the complexity, suggesting formula [Hg(CAP)2] in neutral form. However, regarding both Ce(Ⅲ) and Th(Ⅳ) complexes as [Ce(CAP)2(NO3)]·3 H2O and [Th(CAP)2(NO3)2(H2O)]·3 H2O formulas, the nitrate group is existed inside the coordination sphere. The infrared analysis data proved that CAP drug act as a bidentate ligand with the metal ions of Ce(Ⅲ) and Th(Ⅳ) through oxygen carbonyl group C=O and oxygen of the deprotonated carboxylic COOH group, while for the Hg(Ⅱ) complex, the CAP acts as a bidentate ligand through oxygen of C=O group and sulfur atom of the deprotonated -SH group. Thorium(Ⅵ) complex has a nine-coordinate geometry, while Hg(Ⅱ) and Ce(Ⅲ) have a four and six-coordination behaviors respectively. The 1H-NMR data of the CAP compound has a singlet sharp signal at 1.90 ppm due to the proton of -SH group, this peak absent in the spectrum of the Hg(Ⅱ) CAP complex upon the deprotonated of thiol group.
文摘The captopril/Chitosan-gelatin net-polymer microspheres(CTP/CGNPMs) were prepared using Chitosan(CTS) and gelatin(GT) by the methods of emulsification,cross-linked reagent alone or in combination and microcrystalline cellulose(MCC) added in the process of preparation of microspheres,which aimed to eliminate dose dumping and burst phenomenon of microspheres for the improvement of the therapeutic efficiency and the decrease of the side effects of captopril(CTP). The results indicated that CTP/CGNPMs had a spherical shape,smooth surface and integral structure inside but no adhesive phenomena in the preparation. The size distribution ranged from 220 μm to 280 μm. The CTP release test in vitro demonstrated that CTP/CGNPMs played the role of retarding the release of CTP compared with ordinary CTP tablets. The release behaviors of CGNPMS were influenced by preparation conditions such as experimental material ratio(EMR) and composition of cross linking reagents. Among these factors,the EMR(1/4),CLR(FA+SPP) and 0.75% microcrystalline cellulose(MCC) added to the microspheres constituted the optimal scheme for the preparation of CTP/CGNPMs. The ER,DL and SR of CTP/CGNPMs prepared according to the optimal scheme were 46.23±4.51%,9.95±0.77% and 261±42%,respectively. The CTP/CGNPMs had the good characteristics of sustained release of drug and the process of emulsification and cross-linking were simple and stable. The CGNPMs are likely to be an ideal sustained release formulation for water-soluble drugs.
基金Funded by the National Natural Science Foundation of China(No.30370344)
文摘The captopril/ Chitosan-gelatin net-polymer microspheres （ Gap/ CGNPMs ） were prepared using Chitosan （ CS ） and gelatin （ Gel ） by the methods of emulsification. A cross linked reagent alone or in combination with microcrystalline cellulose （ MCC ） was added in the process of preparation of microspheres to eliminate dose dumping and burst phenomenon of microspheres for the improvemeat of the therapeutic efficiency and the decrease of the side effects of captopril （ Cap ）. The results indicate that Cap/ CGNPMs have a spherical shape , smooth surface roorphology and integral inside structure and no adhesive phenomena and good roobility , and the size distribution is mairdy from 220 to 280 μm. Researches on the Cap release test in vitro demonstrate that Cap/ CGNPMs are of the role of retarding release of Cap compared with Cap ordinary tablets （COT）, embedding ratio （ER） , drug loading （ DL ）, and swelling ratio （ SR ）, and release behaviors of CGNPMS are influenced by process conditions of preparation such as experimental material ratio （EMR） , composition of cross linking reagents. Among these factors , the EMR（1/4）, CLR （ FOR ＋ TPP） and 0.75% microcrystulline cellulose （MCC） added to the microspheres are the optimal scheme to the preparation of Cap/CGNPMs. The Cap/CGNPMs have a good characteristic of sustained release of drug, and the process of emulsifieation and crossinking process is simple and stable. The CGNPMs is probable to be one of an ideal sustained release system for water-soluble drugs.
文摘目的探讨硝苯地平缓释片联合卡托普利片治疗老年高血压的临床效果。方法选择2019年11月—2021年4月收治的50例老年高血压患者,按照用药的不同分为对照组(25例,服用卡托普利片)与观察组(25例,服用硝苯地平缓释片+卡托普利片),比较2组疗效情况,治疗前后血压水平[24 h平均收缩压(24 h SBP)、24 h平均舒张压(24 h DBP)、日间平均SBP(d SBP)、日间平均DBP(d DBP)、夜间平均SBP(n SBP)、夜间平均DBP(n DBP)],根据监测结果计算患者SBP、DBP变异性(24 h SBPV、24 h DBPV),比较2组不良反应发生情况。结果观察组疗效总有效率高于对照组,差异有统计学意义(P<0.05);观察组治疗后24 h SBP、d SBP、n SBP水平均低于对照组,差异有统计学意义(P<0.05),2组治疗后24 h DBP、d DBP、n DBP水平比较差异无统计学意义(P>0.05);观察组治疗后24 h SBPV、24 h DBPV水平低于对照组(P<0.05);2组不良反应发生率比较差异无统计学意义(P>0.05)。结论硝苯地平缓释片联合卡托普利片治疗老年高血压效果显著,能够有效控制患者24 h血压变异性,安全性高。
文摘To explore the possibility of hydrogen sulfide (H 2S) as a messenger molecule in cardiovascular system, the authors discovered that H 2S (5×10 -5 -5×10 -4 mol·L -1 )exerted an effect on inhibiting endothelin 1 induced proliferation of cultured vascular smooth muscle cells (VSMCs) of rats in vitro . The 3H TdR incorporation decreased by 16.8%～37.4% in H 2S treated VSMCs as compared with the controls ( P <0.01). The inhibitory effect was found to be associated with reduced activity of MAPK. The authors also observed that endogenous H 2S levels markedly increased in vessels of rats with either endotoxic shock or septic shock [H 2S level (pmol·min -1 ·mg -1 ):tail artery (16.18±2.06) vs (8.12±0.55);mesenteric artery (10.17±1.11) vs (6.19 ±0.55);pulmonary artery(11.38±1.24) vs (5.27±0.51); aorta(6.21±0.48) vs (4.10± 0.28), P < 0.01 ]. The above findings suggested that H 2S might play an important role in the regulation of cardiovascular pathophysiologic events.
文摘目的:了解3个不同产地、2个不同批次的红藤饮片6种次生代谢产物含量、抑菌活性及两者的相关性。方法:利用分光光度法对红藤饮片提取物的6种次生代谢产物含量进行分析,以金黄色葡萄球菌和枯草芽孢杆菌为实验菌株,用纸片琼脂扩散法测定抑菌圈大小;以平板二倍稀释法统计最小抑菌浓度(M IC);以试管二倍稀释法统计最小杀菌浓度(M BC)。结果:红藤药液对金黄色葡萄球菌和枯草芽孢杆菌的抑菌活性以安徽产地第一批次最高,抑菌圈大小、M IC、M BC分别为(9.67±0.29)mm、12.5 m g/m l、31.25 m g/m l和(10.17±0.58)mm、12.5 m g/m l、31.25 m g/m l,江苏产地第二批次最低,抑菌圈大小、M IC、M BC分别为(7.67±0.29)mm、25 m g/m l、125 m g/m l和(8.17±0.29)mm、25 m g/m l、125 m g/m l。红藤饮片提取物对金黄色葡萄球菌的抑菌活性在不同产地和不同批次之间均有显著性差异(P<0.01);对枯草芽孢杆菌的抑菌活性在不同产地亦有显著性差异(P<0.01),但不同批次之间无显著性差异(P>0.05)。红藤药液的6种次生代谢产物总量以安徽产地第一批次最高(3.61%),江苏产地第二批次最低(1.90%)。红藤提取物的总生物碱和游离蒽醌在不同产地之间有显著性差异(P<0.01),而在不同批次之间无显著性差异(P>0.05);总绿原酸、黄酮类化合物、总鞣质和总皂苷在不同产地和不同批次之间均有显著性差异(P<0.01)。影响红藤饮片对2种细菌的抑菌活性的主要次生代谢产物可能为总皂甙、总鞣质、游离蒽醌及总绿原酸。结论:不同红藤饮片的次代谢产物的含量及抑菌活性以安徽和浙江产地较高,江苏产地较低;红藤的抑菌活性与饮片中总皂甙、总鞣质、游离蒽醌及总绿原酸的含量密切相关。
