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Purpose: The effect of African yam bean flour as an extender on the physicochemical and sensory properties of cooked beef sausage was studied. Methodology: Sausage samples were produced using beef and African yam bean flour (AYBF) as extender at 5%, 10%, 15% and 20% substitution levels while 100% beef sausage served as the control. The proximate composition and sensory properties of the formulated products were determined using standard methods. Findings: Proximate analysis revealed a significant (p<0.05) decrease in moisture content (71.45-65.50%), ash (2.45-0.30%), and fat (10.10-1.90%) with a corresponding increase in crude protein (23.06-28.00%), crude fibre (3.80-16.20%) and carbohydrate (5.74-7.91%) as beef was partially replaced with AYBF. Beef sausages containing AYBF showed a significantly lower pH and better water holding capacity and emulsion properties compared to the control sample. Sensory analysis also showed a significant (p<0.05) decrease in the mean sensory scores for taste, mouthfeel, aroma and overall acceptability. Colour and hardness of the products were improved at AYBF supplementation level of 5%. Generally, the control sample was not significantly (p>0.05) different from samples supplemented with 5% AYBF. Recommendations: It is concluded that the incorporation of AYBF could be an effective ingredient to improve the quality and sensory properties of beef sausage with reduced fat content. Thus, the use of full African yam bean flour as an extender at 5% substitution level for cooked beef sausages is feasible as this will reduce the amount of meat used, thereby reducing the cost of the cooked beef sausage and at same time producing nutritious sausages.
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Echinococcosis is a serious zoonosis parasitic disease caused by the parasitic larva of Echinococcus. Surgical treatment, as the preferred treatment of echinococcosis, has disadvantages such as small scope of application, difficulty in complete resection, high postoperative recurrence rate and heavy burden on patients. Drug therapy is not only a necessary supplement to the preoperative, intraoperative and postoperative treatment of echinococcosis patients, but also the first choice when surgical treatment is not applicable. This article reviews the physicochemical and pharmacokinetic properties of benzimidazole drugs, and summarizes the anti- Echinococcus activities of different benzimidazole formulations, it will provide a reference for future exploration of echinococcosis treatment drugs.
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The active ingredients in traditional Chinese medicine have been reported to possess significant pharmacological activity and played an important role in clinical treatments. However, lots of the active ingredients in traditional Chinese medicine suffer from disadvantages such as low solubility, high melting point and low stability that results in low bioavailability and limit its clinical application. Crystal structure plays an important role in improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine. This review concludes the research advances of several crystal forms used in the active ingredients in traditional Chinese medicine in terms of polymorph, cocrystal, amorphous/coamorphous and nanocrystal. And the effects of crystal forms on the physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine were reviewed. This research may be useful for the formulation preparation and development of the active ingredients in traditional Chinese medicine.
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Bioisosterism is one of the most common strategies in drug structure optimization. With the development of medicinal and organic chemistry, more and more classic and non-classical bioisosteres are used in the design of novel drugs. In recent years, fluorinated groups as a bioisostere have been paid more and more attention by pharmaceutical chemists. This paper briefly reviews the physicochemical properties, chemical preparation methods of difluoromethyl (CF2H) group, and its application in drug design to provide references for drug discovery researchers.
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The solubility/dissolution, hygroscopicity and mechanical properties of drug candidates have a profound effect on oral bioavailability, processability and stability. The physicochemical properties of crystalline drug are closely related to inner crystal structure. Crystal engineering technologies, as strategies of altering the crystal structure and tailoring physicochemical properties at molecular level, possess the potential of enhancing the pharmaceutical performance of product. The current article reviewed the modification of drug solubility/dissolution, hygroscopicity and mechanical properties by crystal engineering technologies through polymorphic selection, amorphization/co-amorphization, as well as co-crystallization, which provided a reference for the applications of pharmaceutical crystallography in improving physicochemical properties and druggability.
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Drug-drug complexes play important roles in improving the physicochemical properties of drugs including the solubility, dissolution rate and stability of the active pharmaceutical ingredients (APIs). In this paper, the design, synthesis, characterization, changes in physicochemical and pharmacologic properties, structural polymorphisms and the research and development pipelines of a variety of drug-drug cocrystals/salts synthesized based on the crystal engineering design are reviewed. This may provide theoretical support for the development of the new solid-state combinational drugs.
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OBJECTIVE: To investigate the physicochemical properties of hydroxypropyl methylcellulose(HPMC)produced by different manufacturers, and to establish a link between the physicochemical properties of HPMC and its sustained release effect, which can provides a theoretical basis for further rational application. METHODS: The physicochemical properties of HPMC collected from different manufacturers, such as particle size distribution, bulk density, physical form, crystallinity and degree of substitution were characterized by laser particle size analyzer, bulk density measuring device, scanning electron microscope, X-ray diffractometer and gas chromatography, respectively. Then, the HPMC from different manufacturers were pressed into sustained release tablets, and the sustained release effect was compared by the dissolution curve. RESULTS: The physicochemical properties of HPMC produced by different factories are different, which are manifested in different particle sizes,different bulk densities, different physical shapes, whether there are differences in crystallization peaks and the content of hydroxypropoxy groups, and the different physicochemical properties directly lead to the difference of sustained release effects. CONCLUSION: The study of physicochemical properties of HPMC can better control its quality and use it more widely.
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In this study, black phosphorus quantum dots (BPQDs)-loaded liposomes (liposome-BPQDs) were prepared to explore physicochemical properties and photothermal effects on cervical cancer cells. BPQDs were fabricated by ultrasonic method. Liposome-BPQDs were prepared by thin film dispersion. Surface morphology, particle size, zeta potential and Raman spectra of liposome-BPQDs were characterized. The cytotoxicity of the liposome-BPQDs against human cervical cancer cells (HeLa) was examined by CCK-8 assay. Confocal laser scanning microscope (CLSM) and fluorescence microscopy were used to observe the uptake and apoptosis of HeLa cells. The results indicated that liposome-BPQDs were ellipsoidal or spherical under scanning electron microscope, TEM observation showed liposome-BPQDs were about 90-110 nm in diameter. The particle size measurements showed liposome-BPQDs were (104.2±0.35) nm in diameter, and zeta potential were examined to be (-11.3±3.01) mV. The encapsulation efficiency was (84.40±2.13)%.Under natural conditions with outdoor ventilation, temperature range of 25 ℃-34 ℃ and relative humidity of 80%-82%, the photothermal effects of liposome-BPQDs was better and the degradation denaturation of liposome-BPQDs were slower than those of BPQDs. The results also reflected that liposome-BPQDs could be uptaken by HeLa cells easily. After near-infrared laser irradiation, the mortality of HeLa cells rise significantly when the amount of BPQDs reach 20 μg·mL-1. In summary, liposome-BPQDs with high stability exhibited good photothermal effects, which can be expected to be applied to photothermal therapy of cervical carcinoma.
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OBJECTIVE: To prepare paclitaxel / oleyl chitosan nanoparticles (PTX / OCS-NPs) and to examine its physicochemical properties and acute lung toxicity. METHODS: The morphology and size were determined by transmission electron microscope (TEM). The average diameters and polydispersity index were evaluated by dynamic light scattering (DLS). Encapsulation efficiency (EE) and in vitro release were determined by high performance liquid chromatography (HPLC). RESULTS: The RESULTS of PTX/OCS-NPs were spherical in shape, uniform particle size and dispersed uniformly. The diameters of NPs were(292.4±20)nm, PDI less than 0.246 and Zeta potential was about 25 mV. The drug loading of PTX was 15.06%. The encapsulation efficiency of PTX was 48.96%. In vitro release study showed that the cumulative release of PTX from NPs were 41.41% and 56.23% respectively, within 48 h in phosphate buffered saline (PBS) pH 7.4 and pH 4.5. Acute toxicity showed that there was no change in the number of white blood cells in the blood, and the content of LDH in the bronchoalveolar lavage fluid was not changed. The RESULTS indicated that the drug delivery system has a good biosafety and biocompatibility. CONCLUSION: PTX / OCS-NPs have excellent physicochemical properties, high drug loading, with sustained release, no acute lung toxicity, that is expected to be a good delivery of paclitaxel and other difficult anti-cancer drug delivery system.
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OBJECTIVE: To synthesize immunomagnetic nanoparticles with uniform particle size, strong superamagnetism as well as strong immune activity which can be specifically and sensitively combined with circulating tumor cells in peripheral blood of patients with breast cancer.METHODS: Superparamagnetic oxide iron nanoparticles containing active carboxyl groups (SMNP-COOH) were synthesized by polyol methods, thermogravimetric analysis was used to determine the amount of carboxyl groups on the surface of SMNP-COOH, while the content of iron was determined by o-phenanthroline. Mediated by 1-ethyl-3,3-dimethylaminopropyl carbodiimide(EDC) and N-hydroxysuccinimide (NHS), immunomagnetic nanoparticles(IMNP) against human breast carcinoma cell line were constructed by binding the monoclonal antibodies against hMAM with SMNP-COOH. X-Ray diffraction was used to confirm their synthesis,meanwhile,transmission electron microscope (TEM), dynamic light scattering (DLS), and vibrating sample magnetometry (VSM) were applied to characterize their physicochemical properties. The conjugation amount of the antibodies and the activity of IMNPs were evaluated by enzyme linked immunosorbent assay (ELISA).RESULTS: X-Ray diffraction showed that the chracteristic peaks of the crystalline powder of SMNP-COOH and IMNP agreed with the Fe3O4 standard. The concentration of iron in SMMP-COOH and IMNP were 0.205 and 0.164 mol•L-1, respectively.TEM showed that both synthesized SMNP-COOH and IMNP were almost spherical or ellipsoidal. The sizes of SMNP-COOH and IMNP were (13.7±3.6) and (15.4±4.5) nm, respectively. Dynamic light scattering(DLS) demonstrated the intensity particle size and polydispersity index (PDI) of SMNP-COOH and IMNP were 23.4 nm and 0.303, and 71.2 nm and 0.175,respectively. VSM results showed that both SMNP-COOH and IMNP had strong superamagnetism, and the saturation magnetization of SMNP-COOH and IMNP were 71.37 and 67.68 emu•g-1Fe, respectively, which confirmed antibody binding may reduce the magnetism of SMNP-COOH. The ELISA results showed the conjugation amount of antibody was about 93 μg on 1 mg SMNP-COOH by covalent bond. The obtained immunomagnetic nanoparticles (IMNP) which were bound with the hMAM monoclonal antibodies could specifically and sensitively combine with breast cancer cell line MDA-MB-415.CONCLUSION: IMNP with strong superparamagnetic property,excellent stability and perfect antibody activity were successfully synthesized, which demonstrate the potential to magnetically separate circulating tumor cells in peripheral blood from patients with breast cancer, thus providing a favorable weapon to accurately detect CTCs in breast tumor patients.
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Objective: To study the quality and stability of bromhexine hydrochloride dry powder inhalations (BH DPIs). Meth-ods: BH DPIs were prepared by freeze-drying with an air jetting method. The humidity and critical relative moisture of the inhalations were investigated. The aerodynamic particle size ( Dae) and water content were also analyzed. The powder morphology was observed under a scanning electronic microscope. The fine particle fraction (FPF) and delivered dose uniformity (DDU) of BH DPIs were de-termined. The stability of the inhalations was determined by accelerated testing and long-term testing. Results: The prepared BH DPIs exhibited the following properties: the critical relative humidity was 65% ; Dae was <5 μm; the water content was less than 2% ; FPF was >30% ,and DDU was good according to the requirement of Chinese Pharmacopoeia. The accelerated testing and long-term testing both indicated promising stability of BH DPIs. Conclusion: Bromhexine hydrochloride dry powder inhalations are stable, and suitable for the use in pulmonary delivery system.
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Aim To prepare hyaluronic acid nanoparti-cles(Ade/GA-HA) using glycyrrhetinic acid modified hyaluronic acid as the carrier and adenine as a model drug, and analyze their physicochemical property and proliferation effect on Bel-7402 cells. Methods Gly-cyrrhetinic acid and hyaluronic acid were combined by chemical cross-linking method, dialysis and freeze-dr-ying,based on which Ade/GA-HA was prepared using ultrasonic method, and the particle size and Zeta po-tential were determined by Malvern laser particle analy-zer,and the morphology was observed by transmission electron microscopy, and the absorbance was deter-mined by ultraviolet-visible spectrophotometer, high performance liquid chromatograph and microplate read-er to caculate drug load, encapsulation efficiency and in vitro release. MTT assays were utilized to determine the proliferation of nanoparticles treated Bel-7402 cells. Results GA-HA nanoparticles had spherical shape with a good dispersion, at diameters of 398.1 nm, of which Zeta potential was - 34.2 mV, and presented good short term stability. The drug load and encapsulation efficiency of Ade/GA-HA nanoparticles were (22.5 ± 5.8)% and (87.27 ± 0.33) %, re-spectively. Burst release was observed in Ade/GA-HA nanoparticles within 4 h, while controlled release 4 h later. Compared with free adenine,Ade/GA-HA nano-particles had a stronger inhibitory effect on cell prolif-eration with statistically significant difference. Conclu-sion GA-HA nanoparticles has excellent physico-chemical properties and meet the design requirement.
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The therapeutic application of artemisinin (ART) is restricted in application due to its poor water solubility and stability. In this study, the long-circulating liposomes (L-Lip) were constructed to improve the solubility and stability of ART. The preparation method, physicochemical properties, serum stability, in vitro release profile and cytotoxicity of the ART loaded long-circulating liposomes were investigated. Using the particle size and entrapment efficiency (EE) as the evaluation index, the preparation procedure was optimized by the Box-Behnken response surface design based on the single factor screening method. The ART loaded long-circulating liposomes were prepared by filming rehydration method, and evaluated with particle size and entrapment efficiency. The optimal formulation was as follows:lipid-cholesterol=5.22:1 (mass ratio), drug-lipid=1:23.15 (mass ratio), lipid concentration=14.35 mg·mL-1, and molar percentage of mPEG=2%. The morphology of L-Lip was uniformly spherical shape according to optimal formulation. The mean size and polydispersity index (PDI) were about (113.3 ±4.7) nm and 0.227 ±0.022 respectively, the zeta potential was (-12.9 ±2.6) mV, and the entrapment efficiency (EE) of ART was (95.88 ±4.8)%. The L-Lip had good stability at 4℃ for 15 days and the particle sizes did not exhibit significant variations in 50% rat plasma over 24 h at 37℃. The in vitro release study of formulation showed a sustained release. Moreover, the cytotoxicity exhibited that blank liposomes were of great safety. Compared with the free ART, the liposome formulation achieved lower cytotoxicity at the high concentration. The L-Lip successfully prepared by a simple filming-rehydration method exhibited ideal physicochemical properties and were enhanced safety, which may sever as a promising nanoplatform for clinical application.
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Objective • To construct a natural polymers-based hydrogels with enhanced mechanical property through double network (DN) strategy under the premise of retaining the good biocompatibility of natural polymers, and then evaluate the beneficial effect of hydrogels on the osteogenic differentiation of rat bone mesenchymal stem cells (rBMSCs). Methods • Methacrylated hyaluronic acid (HAMA) and methacrylated natural gelatin (GelMA) were synthesized through reaction of HA and Gel with methacrylic anhydride (MA), respectively. Thereafter, HA-Gel DN hydrogels were fabricated through two-step photo-crosslinking. The basic physicochemical properties of hydrogels were evaluated by scanning electron microscopy, swelling, compression and degradation analysis. Hydrogels were applied as substrate materials for rBMSCs culture in vitro. Cell viability, attachment, spreading and proliferation were assessed by CCK-8 analysis and fluorescent staining analysis. The osteogenic differentiation of rBMSCs was determined by quantitative PCR and Western blotting analysis. Results • In comparison to HA hydrogels and Gel hydrogels, HA-Gel DN hydrogels showed more suitable physicochemical properties, such as more suitable water absorption and water retention [(12.6± 0.7) fold, (10.3± 0.4) fold], stronger mechanical property [(43.7± 5.6) kPa] and slower degradation rate [(82.3±3.9)% for 12 weeks] for osteogenic differentiation of rBMSCs. Experiment in vitro revealed that HA-Gel DN hydrogels had good biocompatibility, quantitative PCR revealed that it could promote the expression of osteogenic genes including Runx2, BSP, OPN, OCN, OSX and ALP. Western blotting revealed that the HA-Gel DN hydrogels also increased the levels of osteogenic proteins (OPN, OSX and BSP). Conclusion • HAGel DN hydrogels have good biocompatibility and promote the osteogenic differentiation of rBMSCs, which provide a new experimental basis for DN hydrogels becoming the potential material for bone defects repair.
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Abstract Pterodon pubescens (Benth.) Benth., Fabaceae, fruits have been investigated for their anti-inflammatory and antinociceptive activities, and have demonstrated effectiveness in inflammatory conditions. A physiochemical and microbiological stability study was conducted to investigate two nanoemulsion-based delivery systems of two different hydrophilic surfactants (polyethylene glycol-40H castor oil or polyethylene glycol-40 castor oil). The nanoemulsions, containing P. pubescens oil, lecithin, hydrophilic surfactant and water, were analyzed for droplet size distribution, polydispersity index, pH, consistency index, stability against centrifugal force, and active content/vouacapan derivatives. The physicochemical characteristics were followed for 365 days. The nanoemulsion system was evaluated for anti-inflammatory activity by using with a peritonitis model, immediately after preparation and after 365 days of storage at 25 °C. The stability study demonstrated that proper storage (25 °C) preserved the characteristics of the nanoemulsion containing 7.5% polyethylene glycol-40H castor oil, 5% lecithin, and 5% P. pubescens oil. Further, it ensured a shelf life of 365 days as a phytotherapeutic formulation. In the peritonitis assay induced by carrageenan, nanoemulsion prepared with polyethylene glycol-40H castor oil (125 mg/kg) reduced leukocyte migration, even after 365 days of storage (25 °C), highlighting its potential for the treatment of inflammatory diseases. However, further studies are needed to confirm its clinical effectiveness.
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OBJECTIVE: To prepare oxcarbazepine nanostructured lipid carriers (OXC-NLC), and investigate their physicochemical properties. METHODS: OXC-NLC was prepared by emulsification solvent evaporation method, and the optimum prescription was screened by orthogonal design. Scanning electron microscope was used to observe the morphology of OXC-NLC. Granulometer was applied to determine the particle size and distribution. DSC was adopted for phase analysis. RESULTS: OXC-NLC prepared under the optimum conditions was mostly spherical grains, with an average particle size of (63.04 ± 2.05) nm, which were distributed evenly, and the Zeta potential was (-33.52 ± 0.34) mV. DSC results indicated that the drug was dispersed in nanoparticles in an amorphous state, with entrapment efficiency of (98.16 ± 1.59)% and drug-loading capacity of (4.27 ± 0.70)%. The in vitro drug release was 27.31% in 8 h, which was followed by a sustained release. CONCLUSION: The prepared OXC-NLC has uniform particle size distribution, high encapsulation efficiency, and sustained release effect. This processing technology is simple, reliable, and highly reproducible.
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Nanomedicine has shown huge potential in the treatment of cancer, which is not only due to the fact that it can overcome the drawbacks of some small molecular drugs such as insolubility, rapid metabolism, and bad targeting, but also realize the multi modality treatment by containing A minor of nanomedicine can be approved for clinical applications due to poor stability and rapid metabolism, resulting in the limited efficacy and bottlenecking the development of Nanomedicine, that is, “excellent performance in vitro -poor performance in vivo ”. We believe that the fundamental solution in nanomedicine depends on its basic physical and chemical properties, that is the research and innovation of physical pharmacy theoretical methods of nanopreparation. Herein, Focusing on the statistics of tumor microenvironment and targeting the practical clinical The rats were treated with aerobic chemotherapeutic drugs as an example, we systemically elaborated The relationship of the physicochemical properties including the carrier composition, self-assembly, drug loading and release, and stability with in vitro and in vivo properties, and explored the related mechanism in vivo.
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Objective:To predict the basic physicochemical properties ,structure and function ,and linear B-cell epitopes of the capsid protein VP1 of coxsackievirus A6(CVA6).Methods: The amino acid sequence of the CVA6 VP1 was analyzed using Bioedit software and various online tools including SubLoc ,TargetP and the others from ExPASy Bioinformatics Resource Portal.Results: The CVA6 VP1 protein was a hydrophilic protein with a relative molecular weight of 33.6 kD and an isoelectric point of 7.92.This protein containsed 24 phosphorylation sites , but no signal peptide , transmembrane domains and possible fatty acylation sites.Its secondary structure was characterized by the richest random coils , and 48.52 percent of its amino acid residues exposed at the solution inter-face.Epitope prediction by Bepipred showed a number of potential B cell epitopes in the protein ,the highest antigenicity index among them located in the region of amino acids residue 155-165.Conclusion:The basic physicochemical properties ,structure and function characteristics ,and potential linear B-cell epitopes of CVA 6 VP1 were successfully predicted , which laid foundations for the further study on the protein and the preparation of vaccines and immunological diagnostic reagents for CVA 6 infection.
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@#To construct nanostructured lipid carriers(NLCs)with different particle sizes but the same other physicochemical properties, central composite design was adopted. Coumarin-6(C-6)was selected as the model drug due to its high lipophilicity and high fluorescence intensity. Physicochemical properties of NLCs with 100 nm, 200 nm and 300 nm in particle size could remain stable during certain time in K-R solution and PBS. Release experiments in vitro showed that cumulative release of C-6 in NLCs was less than 7% after 24 h. The MTT assay indicated that both blank NLCs and C-6 loaded NLCs showed low toxicity. To confirm the integrity of NLCs in gastrointestinal tract, DiR-loaded NLCs were prepared and the distribution in vivo was monitored by fluorescence imaging. After 6 h oral administration, intact DiR-loaded NLCs could stiu be found, suggesting that NLCs could be used to characterize the uptake in gastrointestinal tract.
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Objective: To investigate the physicochemical properties of Epimedium polysaccharides (EP) from different producing areas in China to provide experimental support for selecting qualified herbal materials for specified product development. Methods: The leaves of Epimedium plants were extracted with water at 50°C,and the aqueous-extract was precipitated with ethanol. The precipitates were dissolved, dialyzed and lyophilized to obtain total polysaccharides, EP. Total sugar and uronic acid contents of the EP were determined by the phenol-sulfuric acid and the m-hydroxyl biphenyl methods, respectively. Molecular weights of the EP were determined by gel filtration chromatography, andmonosaccharide compositions of the EP were analyzed with the alditol acetates by gas chromatography. Results: Total polysaccharides in the Epimedium leaves were significantly different in the leaves from different area of China. Yields of the EP were higher in the leaves from Shannxi, Hunan and Jilin provinces, but the total sugar contents were higher in the EP from the leaves from Sichuan, Hunan and Jilin provinces, and the uronic acid contents in the EP higher in those from Hunan, Jilin and Henan provinces. Molecular weight distributions were similar in all of the EP, but the monosaccharide compositions of the EP were different mainly in the molar ratios of mannose, glucose and galactose. Conclusion: There were significant differences in the physicochemical properties of the EP from the Epimedium plants in different areas of China, which may originate from the different genes of varied species and/or the different habitats of the plants.