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
Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel d...Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.展开更多
[Objectives]To identify stained Schisandrae Chinensis Fructus in Lifei Tablets with carmine and acid red 73 as target substances.[Methods]High performance liquid chromatography(HPLC)and liquid chromatography tandem-ma...[Objectives]To identify stained Schisandrae Chinensis Fructus in Lifei Tablets with carmine and acid red 73 as target substances.[Methods]High performance liquid chromatography(HPLC)and liquid chromatography tandem-mass spectrometry(LC-MS/MS)was used to analyze the 70%methanol extract of the drug.The HPLC was equipped with an Inertstain-C_(18)(250 mm×4.6 mm,5μm)chromatographic column.The mobile phase was acetonitrile-5 mmol/L ammonium acetate solution,gradient elution:volume flow rate of 1.0 mL/min,column temperature of 30℃,detection wavelength of 509 nm.LC-MS/MS was equipped with a Waters-C_(18)(2.1 mm×150 mm,1.7μm)chromatographic column,the mobile phase was methanol-0.1%formic acid solution(containing 5 mmol/L ammonium acetate),gradient elution;the volume flow rate was 0.3 mL/min;ESI ion source,positive ion mode,full scan of primary and secondary mass spectrometry.[Results]Carmine and acid red 73 showed good linear relationship in HPLC and LC-MS/MS,with r greater than 0.995.The sample recovery and RSD values of HPLC and LC-MS/MS met the requirements.The RSD of the results determined by HPLC and LC-MS/MS was not greater than 5.0%.Both methods had good compatibility and could be used for the examination of carmine and acid red 73 in Lifei Tablets.[Conclusions]The method is reliable and reproducible and can be used to identify stained Schisandrae Chinensis Fructus in Lifei Tablets.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Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.
基金Supported by Chongqing Pharmaceutical Research Project of Chongqing Drug Administration and Chongqing Science and Technology Bureau(Yu Yao Jian[2021]30)。
文摘[Objectives]To identify stained Schisandrae Chinensis Fructus in Lifei Tablets with carmine and acid red 73 as target substances.[Methods]High performance liquid chromatography(HPLC)and liquid chromatography tandem-mass spectrometry(LC-MS/MS)was used to analyze the 70%methanol extract of the drug.The HPLC was equipped with an Inertstain-C_(18)(250 mm×4.6 mm,5μm)chromatographic column.The mobile phase was acetonitrile-5 mmol/L ammonium acetate solution,gradient elution:volume flow rate of 1.0 mL/min,column temperature of 30℃,detection wavelength of 509 nm.LC-MS/MS was equipped with a Waters-C_(18)(2.1 mm×150 mm,1.7μm)chromatographic column,the mobile phase was methanol-0.1%formic acid solution(containing 5 mmol/L ammonium acetate),gradient elution;the volume flow rate was 0.3 mL/min;ESI ion source,positive ion mode,full scan of primary and secondary mass spectrometry.[Results]Carmine and acid red 73 showed good linear relationship in HPLC and LC-MS/MS,with r greater than 0.995.The sample recovery and RSD values of HPLC and LC-MS/MS met the requirements.The RSD of the results determined by HPLC and LC-MS/MS was not greater than 5.0%.Both methods had good compatibility and could be used for the examination of carmine and acid red 73 in Lifei Tablets.[Conclusions]The method is reliable and reproducible and can be used to identify stained Schisandrae Chinensis Fructus in Lifei Tablets.