The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insi...The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid(SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. The three-dimensional(3 D) information of SA particles in tablets was detected by a quantitative and non-invasive 3 D structure elucidation technique, namely, synchrotron radiation X-ray micro-computed tomography(SR-μCT). SA particles in glipizide tablets prepared by using unmodified SA(GUT), reprocessed SA(GRT), as well as reference listed drug(RLD) of glipizide tablets were analyzed by SR-μCT. The results showed that the reprocessed SA with better flowability contributed to similarity of breaking forces between that of GRT and RLD. SA particles in GRT were very similar to those in RLD with uniform morphology and particle size, while SA particles in GUT were not evenly distributed. These findings not only demonstrated the feasibility of SR-μCT as a new method in revealing the morphology and spatial distribution of excipient in drug delivery system, but also deepened insights of solid dosage form design into a new scale by powder engineering.展开更多
Objective:To investigate the effects of tripterygium glycosides combined with compoundα-ketoacid tablets on inflammatory response, oxidative stress and urinary TGF-β1 and IV-C levels in patients with chronic renal f...Objective:To investigate the effects of tripterygium glycosides combined with compoundα-ketoacid tablets on inflammatory response, oxidative stress and urinary TGF-β1 and IV-C levels in patients with chronic renal failure.Methods: 102 patients with chronic renal failure admitted to Shuguang hospital from January 2017 to June 2018 were randomly divided into observation group (51 cases) and control group (51 cases). In the control group, the tripterygium glycosides tablets were orally administered, and the observation group was orally administered with tripterygium glycosides tablets and compoundα-keto acid tablets. The inflammatory response, oxidative stress index and urinary TGF-β1, IV-C levels were compared between the two groups.Results: There was no significant difference in CRP and TNF-α levels between the two groups before treatment (P>0.05). After treatment, the levels of CRP and TNF-α in the observation group were (9.32±1.10) mg/L and (3.14±0.36) ng/L, respectively, and the levels of CRP and TNF-α in the control group were (15.34±1.31) mg/ L, (5.01±0.53) ng / L. The CRP and TNF-α levels in the two groups were lower than those before treatment, and the CRP and TNF-α in the observation group were significantly lower than those in the control group (P<0.05). Before treatment, there was no significant difference in MDA, SOD and GSH-PX levels between the two groups (P>0.05). After treatment, the MDA level of the observation group was (3.01±0.32) μmol/L, and the MDA level of the control group was (5.17±0.61) μmol/L. The MDA of the two groups was lower than that before treatment, and the MDA of the observation group was significantly lower than that of the control group (P<0.05). After treatment, the levels of SOD and GSH-PX in the observation group were (101.45±13.16) U/L and (94.83±7.17) U/L, respectively. The levels of SOD and GSH-PX in the control group were (88.87±12.05) U/L, (87.38 ± 6.32) U/L. The SOD and GSH-PX of the two groups were higher than those before treatment, and the SOD and GSH-PX of the observation group were significantly higher than the control group (P<0.05). Before treatment, there was no significant difference in TGF-β1 and IV-C levels between the two groups (P>0.05). After treatment, the levels of TGF-β1 and IV-C in the observation group were (1.05±0.24) ng/L and (5.05±1.13) μg/L, respectively, and the levels of TGF-β1 and IV-C in the control group were (1.36±, respectively). 0.26) ng/L, (7.07±1.24) μg/L. The levels of TGF-β1 and IV-C in the two groups were lower than those before treatment, and the TGF-β1 and IV-C in the observation group were significantly lower than those in the control group (P<0.05).Conclusion: Tripterygium glycosides combined with compound -keto acid tablets can effectively reduce the inflammatory response, oxidative stress and renal interstitial fibrosis in patients with chronic renal failure.展开更多
The aim of this study was to prepare diphenhydramine hydrochloride (DPH)-loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either L-aspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressa...The aim of this study was to prepare diphenhydramine hydrochloride (DPH)-loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either L-aspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressant, to characterize the prepared tablets and to evaluate their bitterness under conditions mimicking those of the oral cavity. The preparation of five formulation batches of the OFDMTs involved mixing DPH, with or without two different concentrations of Asp or Glu, and a premix containing a disintegrating agent. When all ingredients were well mixed, the mixture was directly compacted to form small (4 mm diameter) DPH-loaded OFDMTs. There were only small differences between the tablets with respect to mass, diameter, width and hardness. The disintegration times of the five formulation batches of DPH-loaded OFDMTs were measured using the OD-mate, a disintegration test apparatus in which conditions resemble those of the oral cavity. The disintegration times were all within 10 s of exposure to a medium representing the inside of the oral cavity. Rapid release profiles were observed for DPH, Asp and Glu in these dissolution tests. The taste sensor outputs of samples taken at different times (5 - 30 s) from the dissolution test solutions of the four DPH-loaded OFDMTs containing Asp or Glu were significantly inhibited compared with those of control DPH-loaded OFDMT. These results suggest that the inclusion of Asp or Glu in DPH-loaded OFDMTs is sufficient to mask bitterness in the oral cavity for the first 30 s after the tablet is placed in the mouth. It is anticipated that swallowing will have taken place within 30 s.展开更多
目的探讨马来酸依那普利叶酸片与硝苯地平控释片联合应用于H型高血压患者中的效果。方法选取2020年6月至2021年6月滕州市中医医院收治的94例H型高血压患者作为研究对象,按照随机数字表法分为两组,各47例。对照组应用硝苯地平控释片治疗...目的探讨马来酸依那普利叶酸片与硝苯地平控释片联合应用于H型高血压患者中的效果。方法选取2020年6月至2021年6月滕州市中医医院收治的94例H型高血压患者作为研究对象,按照随机数字表法分为两组,各47例。对照组应用硝苯地平控释片治疗,观察组在对照组基础上加用马来酸依那普利叶酸片治疗,比较两组临床疗效、糖脂代谢水平、血压控制效果、血浆高同型半胱氨酸(HCY)水平及不良反应发生率。结果观察组治疗总有效率为95.74%,高于对照组的82.98%,差异有统计学意义(P<0.05)。治疗后,两组空腹血糖(FBG)、餐后2 h血糖(2 h PBG)、糖化血红蛋白A1c(HbAlc)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-C)及总胆固醇(TC)水平均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组收缩压、舒张压均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组血浆HCY水平均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05)。两组不良反应发生率比较差异无统计学意义。结论马来酸依那普利叶酸片联合硝苯地平控释片治疗H型高血压患者疗效显著,有利于改善患者糖脂代谢,降低血压与HCY水平,且不会增加不良反应的发生,安全性较高,值得临床推广应用。展开更多
基金The authors are grateful for the financial support from the National Science and Technology Major Project(2017ZX09101001-006)Thanks to the BL13W1 beamline of the SSRF for the precious beam time and help from the team.
文摘The shapes of particles and their distribution in tablets, controlled by pretreatment and tableting process, determine the pharmaceutical performance of excipient like lubricant. This study aims to provide deeper insights to the relationship of the morphology and spatial distribution of stearic acid(SA) with the lubrication efficiency, as well as the resulting tablet property. Unmodified SA particles as flat sheet-like particles were firstly reprocessed by emulsification in hot water to obtain the reprocessed SA particles with spherical morphology. The three-dimensional(3 D) information of SA particles in tablets was detected by a quantitative and non-invasive 3 D structure elucidation technique, namely, synchrotron radiation X-ray micro-computed tomography(SR-μCT). SA particles in glipizide tablets prepared by using unmodified SA(GUT), reprocessed SA(GRT), as well as reference listed drug(RLD) of glipizide tablets were analyzed by SR-μCT. The results showed that the reprocessed SA with better flowability contributed to similarity of breaking forces between that of GRT and RLD. SA particles in GRT were very similar to those in RLD with uniform morphology and particle size, while SA particles in GUT were not evenly distributed. These findings not only demonstrated the feasibility of SR-μCT as a new method in revealing the morphology and spatial distribution of excipient in drug delivery system, but also deepened insights of solid dosage form design into a new scale by powder engineering.
文摘Objective:To investigate the effects of tripterygium glycosides combined with compoundα-ketoacid tablets on inflammatory response, oxidative stress and urinary TGF-β1 and IV-C levels in patients with chronic renal failure.Methods: 102 patients with chronic renal failure admitted to Shuguang hospital from January 2017 to June 2018 were randomly divided into observation group (51 cases) and control group (51 cases). In the control group, the tripterygium glycosides tablets were orally administered, and the observation group was orally administered with tripterygium glycosides tablets and compoundα-keto acid tablets. The inflammatory response, oxidative stress index and urinary TGF-β1, IV-C levels were compared between the two groups.Results: There was no significant difference in CRP and TNF-α levels between the two groups before treatment (P>0.05). After treatment, the levels of CRP and TNF-α in the observation group were (9.32±1.10) mg/L and (3.14±0.36) ng/L, respectively, and the levels of CRP and TNF-α in the control group were (15.34±1.31) mg/ L, (5.01±0.53) ng / L. The CRP and TNF-α levels in the two groups were lower than those before treatment, and the CRP and TNF-α in the observation group were significantly lower than those in the control group (P<0.05). Before treatment, there was no significant difference in MDA, SOD and GSH-PX levels between the two groups (P>0.05). After treatment, the MDA level of the observation group was (3.01±0.32) μmol/L, and the MDA level of the control group was (5.17±0.61) μmol/L. The MDA of the two groups was lower than that before treatment, and the MDA of the observation group was significantly lower than that of the control group (P<0.05). After treatment, the levels of SOD and GSH-PX in the observation group were (101.45±13.16) U/L and (94.83±7.17) U/L, respectively. The levels of SOD and GSH-PX in the control group were (88.87±12.05) U/L, (87.38 ± 6.32) U/L. The SOD and GSH-PX of the two groups were higher than those before treatment, and the SOD and GSH-PX of the observation group were significantly higher than the control group (P<0.05). Before treatment, there was no significant difference in TGF-β1 and IV-C levels between the two groups (P>0.05). After treatment, the levels of TGF-β1 and IV-C in the observation group were (1.05±0.24) ng/L and (5.05±1.13) μg/L, respectively, and the levels of TGF-β1 and IV-C in the control group were (1.36±, respectively). 0.26) ng/L, (7.07±1.24) μg/L. The levels of TGF-β1 and IV-C in the two groups were lower than those before treatment, and the TGF-β1 and IV-C in the observation group were significantly lower than those in the control group (P<0.05).Conclusion: Tripterygium glycosides combined with compound -keto acid tablets can effectively reduce the inflammatory response, oxidative stress and renal interstitial fibrosis in patients with chronic renal failure.
文摘The aim of this study was to prepare diphenhydramine hydrochloride (DPH)-loaded orally fast-disintegrating mini-tablets (OFDMTs) containing either L-aspartic acid (Asp) or L-glutamic acid (Glu) as bitterness-suppressant, to characterize the prepared tablets and to evaluate their bitterness under conditions mimicking those of the oral cavity. The preparation of five formulation batches of the OFDMTs involved mixing DPH, with or without two different concentrations of Asp or Glu, and a premix containing a disintegrating agent. When all ingredients were well mixed, the mixture was directly compacted to form small (4 mm diameter) DPH-loaded OFDMTs. There were only small differences between the tablets with respect to mass, diameter, width and hardness. The disintegration times of the five formulation batches of DPH-loaded OFDMTs were measured using the OD-mate, a disintegration test apparatus in which conditions resemble those of the oral cavity. The disintegration times were all within 10 s of exposure to a medium representing the inside of the oral cavity. Rapid release profiles were observed for DPH, Asp and Glu in these dissolution tests. The taste sensor outputs of samples taken at different times (5 - 30 s) from the dissolution test solutions of the four DPH-loaded OFDMTs containing Asp or Glu were significantly inhibited compared with those of control DPH-loaded OFDMT. These results suggest that the inclusion of Asp or Glu in DPH-loaded OFDMTs is sufficient to mask bitterness in the oral cavity for the first 30 s after the tablet is placed in the mouth. It is anticipated that swallowing will have taken place within 30 s.
文摘目的探讨马来酸依那普利叶酸片与硝苯地平控释片联合应用于H型高血压患者中的效果。方法选取2020年6月至2021年6月滕州市中医医院收治的94例H型高血压患者作为研究对象,按照随机数字表法分为两组,各47例。对照组应用硝苯地平控释片治疗,观察组在对照组基础上加用马来酸依那普利叶酸片治疗,比较两组临床疗效、糖脂代谢水平、血压控制效果、血浆高同型半胱氨酸(HCY)水平及不良反应发生率。结果观察组治疗总有效率为95.74%,高于对照组的82.98%,差异有统计学意义(P<0.05)。治疗后,两组空腹血糖(FBG)、餐后2 h血糖(2 h PBG)、糖化血红蛋白A1c(HbAlc)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-C)及总胆固醇(TC)水平均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组收缩压、舒张压均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05);治疗后,两组血浆HCY水平均低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05)。两组不良反应发生率比较差异无统计学意义。结论马来酸依那普利叶酸片联合硝苯地平控释片治疗H型高血压患者疗效显著,有利于改善患者糖脂代谢,降低血压与HCY水平,且不会增加不良反应的发生,安全性较高,值得临床推广应用。