[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl ...[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.展开更多
[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Usin...[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Using particle size distribution and encapsulation rate as evaluation indicators, the effects of hydration time, ratio of organic phase to aqueous phase, granulation method, as well as thin film dispersion and reverse evaporation methods on liposomes preparation were investigated, and the optimal preparation method was selected. Single factor experiments were used to screen the drug phospholipid ratio, ultrasound time, and phospholipid cholesterol ratio, and the preparation process was optimized through orthogonal experiments. [Results] The optimal process of preparing hydroxypropyl tetrahydropyrantriol liposomes was as below: 1 : 10 of drug phospholipid ratio, 6 min of ultrasound time, 4 : 1 of phospholipid cholesterol ratio, (60.94%±7.24%) of entrapment efficiency, (86.44±6.08) nm of particle size, (0.195±0.077) of PDI. [Conclusions] The optimal preparation process of hydroxypropyl tetrahydropyrantriol liposomes selected by orthogonal experiment could effectively improve the encapsulation efficiency of hydroxypropyl tetrahydropyranotriol and reduce particle size. Moreover, the method was stable and reliable.展开更多
Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical ...Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan(FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 k Da. Moreover, our data indicated that there was an obvious degradation process occurred in liver(< 10 k Da at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.展开更多
Hydration heat effect of cement pastes and mechanism of hydroxypropyl methyl cellulose ether （HPMC） and expanded perlite in cement pastes were studied by means of hydration exothermic rate, hydration heat amount, FT...Hydration heat effect of cement pastes and mechanism of hydroxypropyl methyl cellulose ether （HPMC） and expanded perlite in cement pastes were studied by means of hydration exothermic rate, hydration heat amount, FTIR and TG-DTG. The results show that HPMC can significantly delay the hydration induction period and acceleration period of cement pastes. As mixing amount increased, hydration induction period of cement pastes enlarged and accelerated period gradually went back. At the same time, the amount of hydration heat gradually decreased. Expanded perlite had worse delay effects and less change of hydration heat amount of cement pastes than HPMC. HPMC changed the structure of C-S-H during cement hydration. The more amount of HPMC, the more obvious effect. However, EXP had little influence on the structure of C-S-H. At the same age, the content of Ca （OH）2 in cement pastes gradually decreased as the mixing amount increase of HPMC and expanded perlite, and had better delay effect than that single-doped with HPMC or expanded perlite when HPMC and expanded nerlite were both dooed in cement pastes.展开更多
The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-c...The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.展开更多
With potassium persulfate (KPS) as initiator, graft copolymerization of ethyl acrylate (EA) onto water-soluble hydroxypropyl methylcellulose (HPMC) was investigated in aqueous medium. Effects of monomer concentration,...With potassium persulfate (KPS) as initiator, graft copolymerization of ethyl acrylate (EA) onto water-soluble hydroxypropyl methylcellulose (HPMC) was investigated in aqueous medium. Effects of monomer concentration, initiator concentration, matrix concentration, and reaction temperature on the percentage of grafting (G) and grafting efficiency (G_E) were studied. The results show that G and G_E values both increase with the the increase of EA concentration and KPS concentration; when raising HPMC concentration from 0.12 mmol/L to 0.47 mmol/L, G decreases, while G_E increases;and when raising reaction temperature from 50 ℃ to 65 ℃,G increases, but G_E decreases. In addition, the graft copolymers were characterized by Fourier transform infrared (FTIR) spectra and transmission electron microscopy (TEM) methods.展开更多
Hydroxypropyl xanthan gum(HXG) was prepared from xanthan gum(XG) and propylene oxide under alkaline condition. Rheological and drag reduction properties of different concentrations of aqueous HXG and XG solution were ...Hydroxypropyl xanthan gum(HXG) was prepared from xanthan gum(XG) and propylene oxide under alkaline condition. Rheological and drag reduction properties of different concentrations of aqueous HXG and XG solution were studied. The micro-structure network of HXG and XG solutions was investigated by Cryo-FESEM. The results showed that HXG and XG solutions could exhibit shear thinning property. The apparent viscosity of6 g·L-1HXG solution was 1.25 times more than that of 6 g·L-1XG solution. The storage modulus G′ and the loss modulus G″ of HXG solutions were greater than those of XG solutions, and thixotropic and viscoelastic properties were more significant in HXG solutions. The HXG and XG solutions reduced the pressure drop of straight pipe, and the maximum drag reduction of 1 g·L-1HXG and XG in smooth tube reached 72.8% and 68.1%, respectively. Drag reduction rate was increased as the concentration increased. The HXG solution may become a new polymeric drag reducer.展开更多
Polymers and polymeric composites have steadily reflected their importance in our daily life. Blending poly(vinyl alcohol) (PVA) with a potentially useful natural biopolymers such as hydroxypropyl cellulose (HPC) seem...Polymers and polymeric composites have steadily reflected their importance in our daily life. Blending poly(vinyl alcohol) (PVA) with a potentially useful natural biopolymers such as hydroxypropyl cellulose (HPC) seems to be an interesting way of preparing a polymeric blends. In the present work, blends of PVA/HPC of compositions (100/0, 90/10, 75/25, 50/50, 25/75, and 0/100 wt/wt%) were prepared to be used as bioequivalent materials. Thermal analyses [differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA)], and X-ray diffraction (XRD) were employed to characterize and reveal the miscibility map and the structural properties of such blend system. The obtained results of the thermal analyses showed variations in the glass transition temperature (Tg) indicating the miscibility of the blend systems. Moreover, the changes in the melting temperature (Tm), shape and area were attributed to the different degrees of crystallinity and the existence of polymer-polymer interactions between PVA and HPC molecules. The X-ray diffraction (XRD) analysis showed broadening and sharpening of peaks at different HPC concentrations with PVA. This indicated changes in the crystallinity/amorphosity ratio, and also suggested that the miscibility between the amorphous components of homo-polymers PVA and HPC is possible. The results showed that HPC doped in PVA film can improve the thermal stability of the film under investigation, leading to interesting technological applications.展开更多
HGG (Hydroxypropyl guar gum) was synthesized by phase transfer catalysis for the first time. The effects of alkalinity, phase transfer catalyst, etherification, pH value, temperature, reaction time and stirring spee...HGG (Hydroxypropyl guar gum) was synthesized by phase transfer catalysis for the first time. The effects of alkalinity, phase transfer catalyst, etherification, pH value, temperature, reaction time and stirring speed were investigated. An optimal synthetic reaction technology was established, namely, dose of guar gum is 100 g, propylene oxide 40-50 g, HTAC (hexadecyl trimethyl ammonium chloride ) 1.3-1.7 g, pH value 10-10.5, temperature 45-50℃, and reaction time 3-4 hours. The result shows that the improved HGG has high viscosity. Its dissolution speed, content of insoluble residue, colloid light transparency and stability are apparently superior to guar flour.展开更多
Hydroxypropyl methyl cellulose(HPMC)-based hybrid nanocomposites reinforced with bacterial cellulose nanocrystals(BCNC) were prepared and characterized.The HPMC nanocomposites exhibited good thermal stability,with a t...Hydroxypropyl methyl cellulose(HPMC)-based hybrid nanocomposites reinforced with bacterial cellulose nanocrystals(BCNC) were prepared and characterized.The HPMC nanocomposites exhibited good thermal stability,with a thermogravimetric peak temperature of around 346℃.The addition of BCNC did not significantly affect the thermal degradation temperature or improve the transparency of HPMC nanocomposites.However,the addition of BCNC favorably affected the light scattering properties of the nanocomposites and enhanced mechanical properties such as tensile stress and Young's modulus from 65 MPa and 1.5 GPa up to 139 MPa and 3.2 GPa,respectively.The oxygen permeability of the HPMC nanocomposites also increased with increase in the amount of BCNC added.展开更多
In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolu...In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol （50：50, v/v）. Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.展开更多
Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan（CMC-HP-β-CD） were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterize...Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan（CMC-HP-β-CD） were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy（TEM） and dynamic light scattering（DLS）. Cumulative release in vitro study was performed respectively in simulated gastric medium fluid（SGF, p H=1.2）, simulated intestinal fluid（SIF, p H=6.8） and simulated colonic fluid（SCF, p H=7.4）. The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography（HPLC）. Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.展开更多
Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes h...Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes have been determined. Strong inclusion complexation by hydroxypropyl-β-cyclodextrin has been verified展开更多
The effect of application of cellulose-based edible coating, hydroxypropyl methylcellulose (HPMC) to mature-green tomatoes on the firmness and color was investigated. Tomatoes were stored at 20℃ for up to 18 days. Fi...The effect of application of cellulose-based edible coating, hydroxypropyl methylcellulose (HPMC) to mature-green tomatoes on the firmness and color was investigated. Tomatoes were stored at 20℃ for up to 18 days. Firmness decreased as storage time increased in all treatments. However, application of HPMC edible coating delayed softening of tomatoes during 18 days of storage at 20℃ . At days 7, 13 and 18,the firmness of tomatoes coated with HPMC was significantly ( P ≤ 0.05) greater than the firmness of uncoated tomatoes. The study also confirmed that HPMC coatings could significantly (P≤0.05) delay the changes in color of tomatoes stored at 20℃ . The ripening of tomatoes from the pink stage to the red stage was successfully retarded. HPMC coating could extend the shelf life of fresh tomatoes. The retardation of the rate of loss of firmness could reduce the economic loss that would result from spoilage by mechanical injury during transportation of tomatoes.展开更多
3-(3-hydroxypropyl)-phthalide 1, a phthalide isolated from the flowers of G. pedicellata Wall. has been synthesized in high yield from 2-carboxybenzaldehyde 3 in 2 steps. Reaction of 1 with 2,3-dihydroxybenzoic acid a...3-(3-hydroxypropyl)-phthalide 1, a phthalide isolated from the flowers of G. pedicellata Wall. has been synthesized in high yield from 2-carboxybenzaldehyde 3 in 2 steps. Reaction of 1 with 2,3-dihydroxybenzoic acid afforded pedicellosine 2, another phthalide from the leaves of G. pedicellata Wall.展开更多
To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt...To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.展开更多
Hydroxypropyl celluloses(HPC) were homogenously synthesized by the reaction of cellulose with propylene oxide in NaOH/urea aqueous solution.Water-soluble HPC with molar degree of substitution(MSNMR) in the range of 0....Hydroxypropyl celluloses(HPC) were homogenously synthesized by the reaction of cellulose with propylene oxide in NaOH/urea aqueous solution.Water-soluble HPC with molar degree of substitution(MSNMR) in the range of 0.52~0.78 was prepared from microcrystalline cellulose,cotton linters,and spruce sulfite pulp.The structure of the HPC samples was characterized by means of FT-IR,NMR,gas chromatography(GC),and size exclusion chromatography(SEC) analyses.Three types of cellulose samples with different molecular weights were found to dissolve well in the NaOH/urea solvent with no obvious differences in reactivity and regioselectivity.The relative reactivity of hydroxyl groups in the glycosyl unit was in the following order:O-6>O-2>O-3.In addition,the results of the study indicated that the tandem reaction during hydroxypropylation could be ignored.展开更多
Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the ...Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.展开更多
基金Youth Science Foundation Project of Sichuan Provincial Department of Science and Technology(2022NSFSC1437)Special Project of Scientific and Technological Research of Sichuan Provincial Administration of Traditional Chinese Medicine(2021MS121)Fundamental Research Funds for the Central Universities of Southwest Minzu University(ZYN2022040).
文摘[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.
基金Supported by Innovation and Entrepreneurship Training Program Project of Southwest Minzu University(S202210656134)Project of Sichuan Department of Science and Technology(2022NSFSC1437)Project of Sichuan Administration of Traditional Chinese Medicine(2021MS121).
文摘[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Using particle size distribution and encapsulation rate as evaluation indicators, the effects of hydration time, ratio of organic phase to aqueous phase, granulation method, as well as thin film dispersion and reverse evaporation methods on liposomes preparation were investigated, and the optimal preparation method was selected. Single factor experiments were used to screen the drug phospholipid ratio, ultrasound time, and phospholipid cholesterol ratio, and the preparation process was optimized through orthogonal experiments. [Results] The optimal process of preparing hydroxypropyl tetrahydropyrantriol liposomes was as below: 1 : 10 of drug phospholipid ratio, 6 min of ultrasound time, 4 : 1 of phospholipid cholesterol ratio, (60.94%±7.24%) of entrapment efficiency, (86.44±6.08) nm of particle size, (0.195±0.077) of PDI. [Conclusions] The optimal preparation process of hydroxypropyl tetrahydropyrantriol liposomes selected by orthogonal experiment could effectively improve the encapsulation efficiency of hydroxypropyl tetrahydropyranotriol and reduce particle size. Moreover, the method was stable and reliable.
基金financially supported by National High Technology Research and Development Program of China(863 Program,Grant No.2007AA091603)
文摘Hydroxypropyl chitosan(HP-chitosan) has been shown to have promising applications in a wide range of areas due to its biocompatibility, biodegradability and various biological activities, especially in the biomedical and pharmaceutical fields. However, it is not yet known about its pharmacokinetics and biodegradation performance, which are crucial for its clinical applications. In order to lay a foundation for its further applications and exploitations, here we carried out fluorescence intensity and GPC analyses to determine the pharmacokinetics mode of fluorescein isothiocyanate-labeled HP-chitosan(FITC-HP-chitosan) and its biodegradability. The results showed that after intraperitoneal administration at a dose of 10 mg per rat, FITC-HP-chitosan could be absorbed rapidly and distributed to liver, kidney and spleen through blood. It was indicated that FITC-HP-chitosan could be utilized effectively, and 88.47% of the FITC-HP-chitosan could be excreted by urine within 11 days with a molecular weight less than 10 k Da. Moreover, our data indicated that there was an obvious degradation process occurred in liver(< 10 k Da at 24 h). In summary, HP-chitosan has excellent bioavailability and biodegradability, suggesting the potential applications of hydroxypropyl-modified chitosan as materials in drug delivery, tissue engineering and biomedical area.
基金Funded by the National Natural Science Foundation of China(No.50902107)National Science and Technology Supporting Program (No.2011BAJ04B02)the Fundamental Research Funds for the Central Universities (No.2011-YB-03)
文摘Hydration heat effect of cement pastes and mechanism of hydroxypropyl methyl cellulose ether （HPMC） and expanded perlite in cement pastes were studied by means of hydration exothermic rate, hydration heat amount, FTIR and TG-DTG. The results show that HPMC can significantly delay the hydration induction period and acceleration period of cement pastes. As mixing amount increased, hydration induction period of cement pastes enlarged and accelerated period gradually went back. At the same time, the amount of hydration heat gradually decreased. Expanded perlite had worse delay effects and less change of hydration heat amount of cement pastes than HPMC. HPMC changed the structure of C-S-H during cement hydration. The more amount of HPMC, the more obvious effect. However, EXP had little influence on the structure of C-S-H. At the same age, the content of Ca （OH）2 in cement pastes gradually decreased as the mixing amount increase of HPMC and expanded perlite, and had better delay effect than that single-doped with HPMC or expanded perlite when HPMC and expanded nerlite were both dooed in cement pastes.
文摘The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.
文摘With potassium persulfate (KPS) as initiator, graft copolymerization of ethyl acrylate (EA) onto water-soluble hydroxypropyl methylcellulose (HPMC) was investigated in aqueous medium. Effects of monomer concentration, initiator concentration, matrix concentration, and reaction temperature on the percentage of grafting (G) and grafting efficiency (G_E) were studied. The results show that G and G_E values both increase with the the increase of EA concentration and KPS concentration; when raising HPMC concentration from 0.12 mmol/L to 0.47 mmol/L, G decreases, while G_E increases;and when raising reaction temperature from 50 ℃ to 65 ℃,G increases, but G_E decreases. In addition, the graft copolymers were characterized by Fourier transform infrared (FTIR) spectra and transmission electron microscopy (TEM) methods.
基金Supported by the National High Technology Research and Development Program of China(2013AA064801)
文摘Hydroxypropyl xanthan gum(HXG) was prepared from xanthan gum(XG) and propylene oxide under alkaline condition. Rheological and drag reduction properties of different concentrations of aqueous HXG and XG solution were studied. The micro-structure network of HXG and XG solutions was investigated by Cryo-FESEM. The results showed that HXG and XG solutions could exhibit shear thinning property. The apparent viscosity of6 g·L-1HXG solution was 1.25 times more than that of 6 g·L-1XG solution. The storage modulus G′ and the loss modulus G″ of HXG solutions were greater than those of XG solutions, and thixotropic and viscoelastic properties were more significant in HXG solutions. The HXG and XG solutions reduced the pressure drop of straight pipe, and the maximum drag reduction of 1 g·L-1HXG and XG in smooth tube reached 72.8% and 68.1%, respectively. Drag reduction rate was increased as the concentration increased. The HXG solution may become a new polymeric drag reducer.
文摘Polymers and polymeric composites have steadily reflected their importance in our daily life. Blending poly(vinyl alcohol) (PVA) with a potentially useful natural biopolymers such as hydroxypropyl cellulose (HPC) seems to be an interesting way of preparing a polymeric blends. In the present work, blends of PVA/HPC of compositions (100/0, 90/10, 75/25, 50/50, 25/75, and 0/100 wt/wt%) were prepared to be used as bioequivalent materials. Thermal analyses [differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA)], and X-ray diffraction (XRD) were employed to characterize and reveal the miscibility map and the structural properties of such blend system. The obtained results of the thermal analyses showed variations in the glass transition temperature (Tg) indicating the miscibility of the blend systems. Moreover, the changes in the melting temperature (Tm), shape and area were attributed to the different degrees of crystallinity and the existence of polymer-polymer interactions between PVA and HPC molecules. The X-ray diffraction (XRD) analysis showed broadening and sharpening of peaks at different HPC concentrations with PVA. This indicated changes in the crystallinity/amorphosity ratio, and also suggested that the miscibility between the amorphous components of homo-polymers PVA and HPC is possible. The results showed that HPC doped in PVA film can improve the thermal stability of the film under investigation, leading to interesting technological applications.
文摘HGG (Hydroxypropyl guar gum) was synthesized by phase transfer catalysis for the first time. The effects of alkalinity, phase transfer catalyst, etherification, pH value, temperature, reaction time and stirring speed were investigated. An optimal synthetic reaction technology was established, namely, dose of guar gum is 100 g, propylene oxide 40-50 g, HTAC (hexadecyl trimethyl ammonium chloride ) 1.3-1.7 g, pH value 10-10.5, temperature 45-50℃, and reaction time 3-4 hours. The result shows that the improved HGG has high viscosity. Its dissolution speed, content of insoluble residue, colloid light transparency and stability are apparently superior to guar flour.
基金financially supported by the GuangdongHong Kong joint innovation program(2014B050505019)the National Natural Science Foundation of China(31570569)
文摘Hydroxypropyl methyl cellulose(HPMC)-based hybrid nanocomposites reinforced with bacterial cellulose nanocrystals(BCNC) were prepared and characterized.The HPMC nanocomposites exhibited good thermal stability,with a thermogravimetric peak temperature of around 346℃.The addition of BCNC did not significantly affect the thermal degradation temperature or improve the transparency of HPMC nanocomposites.However,the addition of BCNC favorably affected the light scattering properties of the nanocomposites and enhanced mechanical properties such as tensile stress and Young's modulus from 65 MPa and 1.5 GPa up to 139 MPa and 3.2 GPa,respectively.The oxygen permeability of the HPMC nanocomposites also increased with increase in the amount of BCNC added.
基金the National Natural Science Foundation of China(No.20376085,No.20576142)for its financial support.
文摘In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol （50：50, v/v）. Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.
基金Funded by the National Nature Science Foundation of China(No.51273156)the Open Foundation of Hubei key laboratory of Purification and Application of Plant Anti-cancer Active Ingredients(No.HLPAI2014005)
文摘Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan（CMC-HP-β-CD） were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy（TEM） and dynamic light scattering（DLS）. Cumulative release in vitro study was performed respectively in simulated gastric medium fluid（SGF, p H=1.2）, simulated intestinal fluid（SIF, p H=6.8） and simulated colonic fluid（SCF, p H=7.4）. The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography（HPLC）. Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.
文摘Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes have been determined. Strong inclusion complexation by hydroxypropyl-β-cyclodextrin has been verified
文摘The effect of application of cellulose-based edible coating, hydroxypropyl methylcellulose (HPMC) to mature-green tomatoes on the firmness and color was investigated. Tomatoes were stored at 20℃ for up to 18 days. Firmness decreased as storage time increased in all treatments. However, application of HPMC edible coating delayed softening of tomatoes during 18 days of storage at 20℃ . At days 7, 13 and 18,the firmness of tomatoes coated with HPMC was significantly ( P ≤ 0.05) greater than the firmness of uncoated tomatoes. The study also confirmed that HPMC coatings could significantly (P≤0.05) delay the changes in color of tomatoes stored at 20℃ . The ripening of tomatoes from the pink stage to the red stage was successfully retarded. HPMC coating could extend the shelf life of fresh tomatoes. The retardation of the rate of loss of firmness could reduce the economic loss that would result from spoilage by mechanical injury during transportation of tomatoes.
文摘3-(3-hydroxypropyl)-phthalide 1, a phthalide isolated from the flowers of G. pedicellata Wall. has been synthesized in high yield from 2-carboxybenzaldehyde 3 in 2 steps. Reaction of 1 with 2,3-dihydroxybenzoic acid afforded pedicellosine 2, another phthalide from the leaves of G. pedicellata Wall.
基金Supported by National Science&Technology Pillar Program during the TwelfthFive-year Plan Period(2011BAD34B01)National Natural Science Foundation of China(31372485,31172362)the opening fund from Beijing Key Laboratory of TCVM(BUA-TCVM-200904)
文摘To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.
文摘Hydroxypropyl celluloses(HPC) were homogenously synthesized by the reaction of cellulose with propylene oxide in NaOH/urea aqueous solution.Water-soluble HPC with molar degree of substitution(MSNMR) in the range of 0.52~0.78 was prepared from microcrystalline cellulose,cotton linters,and spruce sulfite pulp.The structure of the HPC samples was characterized by means of FT-IR,NMR,gas chromatography(GC),and size exclusion chromatography(SEC) analyses.Three types of cellulose samples with different molecular weights were found to dissolve well in the NaOH/urea solvent with no obvious differences in reactivity and regioselectivity.The relative reactivity of hydroxyl groups in the glycosyl unit was in the following order:O-6>O-2>O-3.In addition,the results of the study indicated that the tandem reaction during hydroxypropylation could be ignored.
文摘Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.
