Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.I...Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.展开更多
Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug deli...Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.展开更多
Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu upt...Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.展开更多
Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities an...Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.展开更多
In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and mois...In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.展开更多
Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust d...Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.展开更多
While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effecti...While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effectiveness.In this study,we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs,enabling the fabrication of nanoparticles with fine and uniform particle size distribution.Regorafenib(1 g),as a model drug,copovidone(5 g),and sodium dodecyl sulfate(0.1 g)were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray dryer.The electrostatic spray-dried nanoparticles(ESDN)showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles(CSDN).ESDN demonstrated significantly enhanced solubility and rapid release in water.In vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent,exhibiting superior cytotoxicity compared to CSDN.Furthermore,ESDN substantially improved oral bioavailability and antitumor efficacy compared to CSDN.These findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs,effectively addressing the limitations associated with CSD methods.展开更多
Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active ingredient.It exhibits a wide range of ...Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active ingredient.It exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic properties.As a result,it has gained significant recognition among practitioners of traditional Chinese and Indian medicine.These biological effects may be associated with multiple molecular targets and signal transduction pathways.However,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its effectiveness.To address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery systems.This article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability.展开更多
In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary m...In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin<sup>®</sup> is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin<sup>®</sup> has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin<sup>®</sup> at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine<sup>®</sup> (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine<sup>®</sup> into CurCousin<sup>®</sup> (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin<sup>®</sup> (4.5 mg/kg) double the dose without BioPerine<sup>®</sup>. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage.展开更多
Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudra...Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35：65 ratio to made a modified-release （MR） capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release （IR） capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.展开更多
Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its ...Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its clinical applications.In the present study,phospholipid complex（PC） technology was employed to improve the solubility and bioavailability of HCPT.XRD data confirmed the formation of HCPT-PC.However,our previously prepared HCPT-PC is too sticky,which may result in the slow dissolution rate and negative effects on its absorption.Therefore,we prepared HCPT-PC-solid dispersion（HCPT-PC-SD）and lipid-based formulations of HCPT-PC through simple preparation process.The results showed that the dissolution rate of HCPT-PC was effectively improved by solid dispersion technology,which reached 91.73%in 45 min.Pharmacokinetic study revealed that the AUC_（0-t） of HCPT-PC-SD and HCPT-PC lipid-based formulations was effectively further increased compared with HCPT-PC.Moreover,we found that the combination of SD technology and lipid-base formulations could be a promising drug-delivery system to improve the oral bioavailability of HCPT-PC.In addition,we showed that the bioavailability of HCPT-PC lipid-base formulations was even greater than that of HCPT-PC-SD.In particular,lipid-base formulations could be prepared just by a simple method,suggesting its feasibility of industrialization.展开更多
A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined ...A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.展开更多
基金supported by the Science and Technology Programs of Department of Natural Resources of Zhejiang Province,China(No.2020006)the Zhejiang Provincial Natural Science Foundation of China(No.LGF22D030001)the Key R&D Program of Zhejiang Province,China(No.2021C04020)。
文摘Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil.
文摘Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine.
基金supported by the National Natural Science Foundation of China(No.22074058,S.Li).
文摘Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach.
基金supported by the National Natural Science Foundation of China(31972087)the earmarked fund for China Agriculture Research System-Bee(CARS-44-KXJ17)the Science and Technology Innovation Project of Chinese Academy of Agricultural Sciences(CAAS-ASTIP-2021-IAR)。
文摘Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry.
基金Supported by Open Fund of Engineering Research Center of Ministry of Education for Wetland Ecology and Agricultural Utilization(KF202015).
文摘In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity.
基金supported by National key research and development program of China(2022YFF1102500)。
文摘Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment.
基金This work was supported by the National Research Foundation of South Korea(NRF)grants funded by the South Korean government(MEST)(No.2022R1A2C2004197,RS-2024-00407053 and RS-2023-00208448).
文摘While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effectiveness.In this study,we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs,enabling the fabrication of nanoparticles with fine and uniform particle size distribution.Regorafenib(1 g),as a model drug,copovidone(5 g),and sodium dodecyl sulfate(0.1 g)were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray dryer.The electrostatic spray-dried nanoparticles(ESDN)showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles(CSDN).ESDN demonstrated significantly enhanced solubility and rapid release in water.In vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent,exhibiting superior cytotoxicity compared to CSDN.Furthermore,ESDN substantially improved oral bioavailability and antitumor efficacy compared to CSDN.These findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs,effectively addressing the limitations associated with CSD methods.
基金supported by the National Natural Science Foundation of China(82274313)Key R&D Program of Shaanxi Province(2023GHZD43).
文摘Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active ingredient.It exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic properties.As a result,it has gained significant recognition among practitioners of traditional Chinese and Indian medicine.These biological effects may be associated with multiple molecular targets and signal transduction pathways.However,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its effectiveness.To address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery systems.This article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability.
文摘In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin<sup>®</sup> is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin<sup>®</sup> has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin<sup>®</sup> at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine<sup>®</sup> (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine<sup>®</sup> into CurCousin<sup>®</sup> (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin<sup>®</sup> (4.5 mg/kg) double the dose without BioPerine<sup>®</sup>. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage.
文摘Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35：65 ratio to made a modified-release （MR） capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release （IR） capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.
基金Science and Technology Department of Henan province Fund Project(Grant No.144300510019)
文摘Previous study has shown that 10-hydroxycamptothecin（HCPT） has well-established pharmacological effects in vitro.However,its in vivo bioavailability is very poor due to various problems,which severely restricts its clinical applications.In the present study,phospholipid complex（PC） technology was employed to improve the solubility and bioavailability of HCPT.XRD data confirmed the formation of HCPT-PC.However,our previously prepared HCPT-PC is too sticky,which may result in the slow dissolution rate and negative effects on its absorption.Therefore,we prepared HCPT-PC-solid dispersion（HCPT-PC-SD）and lipid-based formulations of HCPT-PC through simple preparation process.The results showed that the dissolution rate of HCPT-PC was effectively improved by solid dispersion technology,which reached 91.73%in 45 min.Pharmacokinetic study revealed that the AUC_（0-t） of HCPT-PC-SD and HCPT-PC lipid-based formulations was effectively further increased compared with HCPT-PC.Moreover,we found that the combination of SD technology and lipid-base formulations could be a promising drug-delivery system to improve the oral bioavailability of HCPT-PC.In addition,we showed that the bioavailability of HCPT-PC lipid-base formulations was even greater than that of HCPT-PC-SD.In particular,lipid-base formulations could be prepared just by a simple method,suggesting its feasibility of industrialization.
文摘A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4～100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%～104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.
