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Objective:To prepare vorinostat encapsulated hydroxypropyl-β-cyclodextrin (SAHA-CD) eye drops and investigate its inhibitory effect on corneal neovascularization (CNV) induced by alkali burns in mouse.Methods:The SAHA-CD eye drops at concentrations of 0.1%, 0.2%and 0.4%were prepared by inclusion technology with hydroxypropyl-β-cyclodextrin, and the content was assayed by high performance liquid chromatography.Seventy-five SPF mice with alkali burn-induced CNV were randomized into 0.1%SAHA-CD group, 0.2%SAHA-CD group, 0.4%SAHA-CD group, dexamethasone group and normal control group according to a random number table, 15 for each group, among which the SAHA-CD groups and dexamethasone group were treated with corresponding drugs, and model control group was treated with normal saline immediately after modeling, four times a day and five microliters each time, lasting for six days.The healing of corneal epithelium was examined with a slit lamp microscope after fluorescein sodium staining, and the areas of cornea epithelial defects were calculated using Eyestudio software.The corneal flat mount was prepared, and the length and areas of CNV were calculated with ImageJ software.The histology of mouse corneas was observed through hematoxylin and eosin staining.The expression level of vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF) and matrix metalloproteinase-9 (MMP-9) in cornea were measured with enzyme linked immunosorbent assay (ELISA) kits.The use and care of animals complied with the ARVO statement and this study protocol was approved by the Experimental Animal Ethics Committee of Henan Eye Institute (No.HNEECA-2020-01).Results:The actual drug contents of the 0.1%, 0.2% and 0.4%SAHA-CD eye drops were 97.62%, 98.33%and 98.14%of the labeled amount.The cornea showed edema and opacification after modeling.On the sixth day after treatment, significant differences were found in the length and areas of CNV among various groups ( F=7.655, 8.802; both at P<0.01).The areas of CNV in 0.2%SAHA-CD, 0.4%SAHA-CD and dexamethasone groups were significantly smaller than model control group, and the length of CNV in 0.1%SAHA-CD, 0.2%SAHA-CD and dexamethasone groups were significantly smaller than model control group (all at P<0.05).On the third and sixth day following modeling, significant differences in the expression levels of VEGF, bFGF and MMP-9 were found among the five groups (third day: F=6.345, 7.149, 18.650; all at P<0.01; sixth day: F=6.749, 5.105, 5.023; all at P<0.01), and the expression levels of VEGF, bFGF and MMP-9 in 0.2%SAHA-CD group were significantly lower than those in 0.1%SAHA-CD group, 0.4%SAHA-CD group and model control group (all at P<0.05). Conclusions:SAHA-CD eye drops can inhibit alkali burn-induced CNV in mouse.
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OBJECTIVE: To compare the intradermal delivery effects of composite phospholipid liposomes composed of different proportions of soy phospholipids (SPC) and hydrogenated soy phospholipids (HSPC) on the fluorescent modified hydroxypropyl-β-cyclodextrin(HP-β-CD), and to optimize the phospholipid composition with the best skin retention. METHODS: The fluorescent probe, fluorescein isothiocyanate (FITC), was combined with HP-β-CD to prepare fluorescent modified cyclodextrin FITC-HP-β-CD. FITC-HP-β-CD was encapsulated in different composite phospholipid liposomes. The amount of the permeation in the receiving solution and skin retention of the cyclodextrin after 10 h were determined in the in vitro intradermal delivery experiment. RESULTS: The order of cyclodextrin permeation of liposomes in the receiving solution was SPC > S/H (3:1) > S/H (1:1) > S/H (1:3) > HSPC >FITC-HP-β-CD, while the order of cyclodextrin intradermal retention was S/H (1:1) > S/H (1:3) > HSPC > S/H (3:1) > SPC > FITC-HP-β-CD. CONCLUSION: Using SPC to prepare liposomes is more beneficial to promote the permeation of FITC-HP-β-CD into the skin than HSPC, but the addition of HSPC can increase the skin retention of FITC-HP-β-CD. The S/H(1:1) liposomes have the better intradermal delivery effect on the fluorescent modified cyclodextrin, of which the skin retention effect is the best.
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OBJECTIVE： To investigate in vitro release rate and in vivo pharmacokinetics of Resveratrol/hydroxypropyl-β- cyclodextrin/chitosan sustained-release pellets （RES/HP-β-CD/Chitosan） in rats. METHODS： In vitro release rate of RES raw materials， RES-HP-β-CD complexes （RES/HP-β-CD） and RES/HP-β-CD/Chitosan in water within 12 h were investigated by paddle method. The pharmacokinetic characteristics of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan were compared within 720 min after intragastric administration. RESULTS： Compared with RES raw materials， in vitro release rate of RES/HP-β-CD was increased significantly， and 120 min accumulative release rate reached 87％. Compared with RES/HP-β-CD， in vitro release rate of RES/HP-β-CD/Chitosan were relieved significantly； release time prolonged significantly； 12 h accumulative release rate was 72％. The pharmacokinetic parameters of RES raw materials， RES/HP-β-CD and RES/HP-β-CD/Chitosan included that cmax were 473.3， 2 492.2， 590.5 ng/mL； t1/2 were 2.6， 0.5， 4.6 h； AUC0-12 h were 514.7， 824.6， 2 778.5 ng·h/mL. Compared with RES raw materials， relative bioavailability of RES/HP-β-CD and RES/HP-β-CD/Chitosan were 172.5％ and 540.0％. CONCLUSIONS： RES/HP-β-CD/Chitosan shows good sustained-release effect， and its bioavailability is significantly higher than that of RES raw materials， RES/HP-β-CD.
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OBJECTIVE： To prepare Resveratrol-hydroxypropyl-β-cyclodextrin-chitosan sustained-release pellets （RES-HP-β- CD-Chitosan）， and to characterize it. METHODS： Resveratrol raw material， HP-β-cyclodextrin and chitosan were collected with ratio of 1 ∶ 7 ∶ 0.25. Resveratrol-HP-β-cyclodextrin inclusion compound were prepared by solvent method， and then added into chitosan， RES-HP-β-CD-Chitosan were prepared by spray drying method. Particle size of prepared sustained-released pellets were observed by optical microscope. X-ray， DSC， IR and SEM were used to characterize RES-HP-β-CD-Chitosan. The contents of resveratrol in prepared sustained-released pellets were determined by UV spectrum， and drug-loading amount and encapsulation efficiency were calculated. RESULTS： Particle size of prepared RES-HP-β-CD-Chitosan was （2.23±0.35） μm （n＝300）. Characterization results show that RES-HP-β-CD-Chitosan was spherical in shape； shrinkage was found on the surface of microspheres， and resveratrol was included in HP-β-cyclodextrin in molecule or amorphous state. Drug-loading amount of prepared RES-HP-β-CD-Chitosan was 11.67％ （n＝3）， encapsulation efficiency was 96.27％ （n＝3）. CONCLUSIONS： RES-HP-β-CD- Chitosan is prepared successfully.
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Objective The inclusion complex of vincamine (VIN) and hydroxypropyl-β-cyclodextrin (HP-β-CD) was prepared and characterized. Molecular simulation method was used to study the formation mechanism of inclusion complex. Methods The inclusion complex of VIN/HP-β-CD was prepared by saturated solution. The preparation technology of VIN/HP-β-CD inclusion complex was optimized by orthogonal design, and taking the drug-loading of the inclusion compound as the index. The stability constant of inclusion complex between VIN and HP-β-CD was studied by UV-Vis spectrometry titration, and the inclusion ratio was determined by Job plots method. The VIN/HP-β-CD inclusion complex was characterized by scanning electron microscope (SEM), X-ray powder diffractometry (XRD), infrared spectroscopy (IR), thermal analysis techniques (TG and DSC), and nuclear magnetic resonance (1H, 2D NMR). The water solubility of the VIN/HP-β-CD inclusion complex was measured and the stability test was conducted in the simulated human gastric juice and intestinal fluid environment. Molecular docking and molecular dynamics were used to study the forming mechanism of supramolecular system of VIN/HP-β-CD. Results Using saturated solution method, the optimum conditions of inclusion were: 1:1 for molar ratio of VIN and HP-β-CD, 40 ℃ for inclusion temperature, 7 h for inclusion time and volume ratio of methanol to water (1:6) as solvent; Job curve and UV-vis spectroscopy showed that inclusion ratio of host-guest inclusion complexes was 1:1; After VIN formed inclusion complexes with HP-β-CD, its solubility increased from 0.04 mg/mL to 16.5 mg/mL, and the thermal decomposition temperature of VIN increased from 240.5 ℃ to 306.1 ℃. 1H-NMR and NOESY spectra indicated that the inclusion complex was formed by the a-ring of VIN entering from the large end of HP-β-CD. Quantum chemical calculation and molecular docking indicated that the optimal inclusion mode was consistent with the results of NMR studies. Molecular dynamics studies showed that VIN can penetrate into the hydrophobic cavity of HP-β-CD in water environment, and the interaction between host and guest was strengthened. The space size of host-guest matched better. Conclusion The solubility and thermal stability were significantly improved after the formation of inclusion complex with VIN and HP-β-CD. Hydrophobicity, hydrogen bonding, and van der Waals forces were the main driving forces for inclusion complex formation.
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Objective To investigate the physicochemical properties and pharmacokinetics of L-asparaginase loaded hydroxypropyl-β-cyclodextrin liposome (AHL) in rats. Methods AHL was prepared by reverse evaporation method, and the entrapment rate, particle size, zeta potential and morphology of AHL were observed. Twelve SD rats were randomly divided into two groups. One group was injected with AHL, and the other group was injected with L-asparaginase (L-ASN). The blood samples were taken from infraorbital venous plexus, and the activity of L-ASN in the samples were determined and the activity-time curve was plotted. Main pharmacokinetic parameters were calculated by software DAS2.1.1. Results The average entrapment efficiency of AHL was (53.53±0.58)%, with an average particle size of (388.99±2.02) nm and an average zeta potential of (－8.56±0.75) mV. The pharmacokinetic parameters for AHL and L-ASN were: 0-48 h area under curve (198.79±9.15) U/(mL • h), (57.78±2.90) U/(mL • h); 0-48 h mean resident time (4.61±0.09) h, (2.09±0.05) h; peak concentration (32.32±1.33) U/mL, (26.82±1.38) U/mL; and time to peak (1.08±0.20) h, (0.10±0.04) h, respectively. The relative bioavailability of AHL was 344.05%. Conclusion AHL can improve the pharmacokinetics and enhance the bioavailability of L-ASN.
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OBJECTIVE: To study the effect of water-soluble materials on the inclusion complex of fenofibrate and hydroxypropyl-β-cyclodextrin. METHODS: The inclusion complex of fenofibrate/hydroxypropyl-β-cyclodextrin and the ternary system containing water-soluble materials were obtained by ball milling. The inclusion complex was characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (XRD), Fourier-transformed infrared spectrophotometry (FTIR), 1H-NMR spectroscopy, as well as in vitro dissolution and stability test. RESULTS: The stability tests and in vitro dissolution results showed that the addition of water-soluble materials could improve the stability constant and inclusion efficiency of the inclusion complex. Moreover, the addition of hydroxypropyl methylcellulose(HPMC) could result in a more stable complex and the in vitro dissolution rate of complex was also increased. CONCLUSION: The addition of appropriate water-soluble materials could enhance the inclusion efficiency of hydroxypropyl-β-cyclodextrin with drugs and form a more stable system.
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Objective: To prepare tetrahydropalmatine (THP) and β-cyclodextrin (β-CD) and its derivatives inclusion complexes (HP-β-CD, DM-β-CD, and TM-β-CD and explore their inclusion behavior and properties. Methods: The inclusion complexes of THP with β-CD, HP-β-CD, DM-β-CD, and TM-β-CD were prepared by saturated solution. The inclusion ratio and stability constant of inclusion complexes were determined with the Job plot and UV-vis spectroscopy. The THP/CDs complexes were characterized and determinated by means of XRD, TG, and SEM. The molecular simulation was processed to investigate the inclusion behavior of THP and different CDs. The water solubility of the inclusion complexes was measured and the stability test was conducted in the simulated human gastric juice and intestinal fluid environment. Results: Job plot and UV-vis spectroscopy showed that inclusion ratio of host-guest inclusion complexes was 1:1. Molecular docking showed that the entire THP entered the macrophage port and run through the cavities of β-CD and DM-β-CD, with the two aromatic rings located at the large and small mouth, respectively. For HP-β-CD and TM-β-CD, the two nitrogen heterocycle of THP were “V” shaped inlaid into the CD cavity, and both aromatic rings were located at the large end of the CDs. Conclusion: The solubility of tetrahydropalmatine was increased from 0.30 mg/mL to 1.60, 3.40, 9.13, and 4.02 mg/mL for β-CD, HP-β-CD, DM-β-CD, and TM-β-CD, respectively. The thermal stability and biological environment stability had been significantly improved.
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AIM To optimize the preparation of two inclusion compounds of erinacine A and to evaluate their stabilities.METHODS With feed ratio,milling time and milling speed as influencing factors,inclusion rate and yield as evaluation indices,the preparation was optimized by orthogonal test.The obtained inclusion compounds were characterized by infrared spectrophotometry and TLC,whose stabilities at high temperature (60 ℃),strong light (3 000 1x) and high humidity [(90 ±5)％] were investigated.RESULTS The optimal β-cyclodextrin inclusion conditions were determined to be 5 ∶ 1 for feed ratio,60 min for milling time,and 300 r/min for milling speed,the inclusion rate and yield were 20.66％ and 88.21％,respectively.The optimal hydroxypropyl-β-cyclodextrin inclusion conditions were determined to be 25 ∶ 1 for feed ratio,90 min for milling time,and 400 r/min for milling speed,the inclusion rate and yield were 69.25％ and 96.31％,respectively.The inclusion of Hericium erinaceus 80％ ethanol extract was physical process without composition change.At high temperature and strong light,two inclusion compounds' appearance showed no obvious change with little loss of erinacine A,which was just the contrary at high humidity.The inclusion effect of hydroxypropyl-β-cyclodextrin inclusion compound was better than that of β-cyclodextrin inclusion compound.CONCLUSION Both β-cyclodextrin and hydroxypropyl-β-cyclodextrin inclusion compounds of erinacine A exhibit good heat stability and light stability,but deliquescence can easily happen to them.
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Objective To prepare formononetin-2-hydroxypropyl-β-cyclodextrin (FMN-2-HP-β-CD) inclusion complex and to explore its inclusion behavior. Methods The preparation method of FMN-2-HP-β-CD inclusion complex was optimized by comparing kneading method, stirring method, and ultrasonic method. The content of FMN was assayed by HPLC. The preparation technology of FMN-2-HP-β-CD inclusion complex was optimized by orthogonal design taking drug loading capacity as index. The inclusion complex was characterized by scanning electronic microscopy (SEM) and X-ray diffractometry (XRD). Phase solubility method was used to calculate the molar ratio between host and guest molecules and the related thermodynamic parameter. The molecular simulation was processed to investigate the inclusion behavior of FMN and 2-HP-β-CD. Results Using acid-base neutralization agitation method, the optimum inclusion conditions were: the molar ratio of FMN with 2-HP-β-CD 1∶1, inclusion temperature 50 ℃, and 2-HP-β-CD concentration 5 g/L. The drug loading capacity was (9.42 ± 0.25)%. The phase solubility curve was AL type and the stability constants decrease with the increasing temperature. The thermodynamic parameters showed that the inclusion of FMN and 2-HP-β-CD is a process of exothermic and entropy decreasing with enthalpy change as the main driving force. Molecular simulation showed that the 7-OH of the FMN takes the lead from the wider rim of 2-HP-β-CD into the cavity, and forms a hydrogen bond with the oxygen atom on the 2-HP-β-CD. Conclusion The FMN-2-HP-β-CD inclusion complex prepared by the optimumprocess conditions has good repeatability, which can improve the solubility of FMN. Molecular simulation of FMN and 2-HP-β-CD inclusion behavior was consistent with the relevant thermodynamic parameters.
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Objective: To study the solubilization of sulfonated butyl ether-β-cyclodextrin (SBE-β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) for voriconazole (VCZ) to lay basis for the preparation of inclusion compounds of VCZ.Methods: The phase-solubility method was used, and the solubilization of SBE-β-CD and HP-β-CD at different concentrations for VCZ was studied at various temperatures and the inclusion constant (K) and such inclusion parameters as ΔG, ΔH and ΔS were calculated.Results: Both SBE-β-CD and HP-β-CD could improve the solubility of VCZ in water, while the solubilization of SBE-β-CD was more significant than that of HP-β-CD at the same concentration under the same temperature.The equilibrium phase-solubility diagram of SBE-β-CD vs VCZ was AN type, and that of HP-β-CD vs VCZ was AL type.With the increase of temperature, K of both β-CD decreased.ΔG, ΔH and ΔS were all negative for the inclusion process.Conclusion: Compared with that of HP-β-CD, the solubilization of SBE-β-CD for VCZ is better.The inclusion is spontaneously formed with exothermic process, and the main acting force is Van der Waals'' force.
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AIM To prepare the hydroxypropyl-β cyclodextrin inclusion compound of volatile oil from Houttuyniae Herba.METHODS In the content determination of volatile oil by GC,2-undecanone was taken as a reference substance,and inclusion rate and drug loading were calculated.After the determination of optimal method for preparing the inclusion compound among techniques of mixing,grinding and ultrasonic methods.the preparation process was optimized by orthogonal test with ratio of volatile oil to hydroxypropyl-β cyclodextrin,inclusion temperature,mixing speed and inclusion time as influencing factors,and inclusion rate and drug loading as evaluation indices.The characterization was performed by TLC,infrared spectroscopy and differential scanning calorimetry.Then high temperature,high humidity and strong light tests were applied to investigating the inclusion compound stability.RESULTS Mixing method brought forth the maximal yield,inclusion rate and drug loading for the inclusion compound.And under the optimal conditions of 1 ∶ 25 for ratio of volatile oil to hydroxypropyl-β cyclodextrin,50 ℃ for inclusion temperature,420 r/min for mixing speed,and 80 min for inclusion time,the inclusion rate and drug loading were identified to be 77.35％ and 4.48％,respectively.The obtained inclusion compound was found to be white powder with loose texture and significantly increased solubility,the in vitro accumulative release rate reached 80.85％.Deliquescence and agglomeration,as well as obviously decreased inclusion rate and drug loading,were observed at a relative humidity of more than 75％,despite the good stability at high temperature (60 ℃) and strong light (3 000 lx),and yet the rehydration character was good.CONCLUSION It is possible that the hydroxypropyl-β cyclodextrin inclusion compound of volatile oil from Houttuyniae Herba generates a new phase rather than a simple mixture,which should be kept dry and sealed at the time of storage.
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OBJECTIVE:To prepare the Carboprost methyl-hydroxypropyl-β-cyclodextrin (HP-β-CD) clathrate sublingual tab-lets,and conduct quality evaluation. METHODS:Wet granulation method was used to prepare Carboprost methyl-HP-β-CD clath-rate sublingual tablets. Using the appearance,calving time,wetting time and main drug content as investigation indexes,mass ratio of mannitol-lactose,povidone volume fraction and amount of low-substituted hydroxypropylcellulose(L-HPC)as factors,orthogo-nal test was used to screen the formulation. The calving time,wetting time,main drug content,content uniformity,dissolution de-gree of sublingual tablets with optimal formulation were evaluated. RESULTS:The optimal formulation was as follow as 78.82 mg of carboprost methyl-HP-β-CD clathrate (containing carboprost methyl 1 mg),100 mg of mannitol-lactose (mass ratio of 9:1) mixed powder,appropriate amount of 2% povidone solution,30 mg of L-HPC,and 1 mg of magnesium stearate. The calving time of prepared 3 batches of sublingual tablets was(25.30±3.21)-(26.53±2.69)s;wetting time was(64.65±8.07)-(65.54±7.21)s;main drug content was (96.13 ± 0.43)%-(97.06 ± 0.82)%;content uniformity was 5.95-7.68;the cumulative dissolution degree within 10 min was more than 50%,and it can completely dissolute within 30 min. CONCLUSIONS:Carboprost methyl- HP-β-CD clathrate sublingual tablets,which are up to requirements,are prepared successfully.
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OBJECTIVE:To study the effect of HP-β-CD on solubility of 1,8-oxido-p-menthane in volatile oil of magnoliae flos,and optimize the extraction technology of Xinzhi nasal drops. METHODS:Steam distillation method was adopted to extract the volatile oil in magnoliae flos. Using the content of 1,8-oxido-p-menthane in volatile oil of magnoliae flos as index,HPLC was adopted to determine the effects of HP-β-CD with different concentration on solubility of 1,8-oxido-p-menthane in volatile oil of magnoliae flos. Using the comprehensive scores of imperatorin and extract yield as indexes,orthogonal test was used to optimize the amount of ethanol,volume fraction and extraction time in extraction technology of Xinzhi nasal drops. Verification test was car-ried out. RESULTS:50% HP-β-CD aqueous solution can improve the solubility of 1,8-oxido-p-menthane to 7.6 times. The optimal extraction technology of Xinzhi nasal drops was as follow as 10-fold 80% ethanol,extracting twice,1 h every time. In verification test,the average content of imperatorin was 0.078%(RSD=2.01%,n=3),and extract yield was 10.80%(RSD=1.85%,n=3). CONCLUSIONS:HP-β-CD shows good solubilization effect on the 1,8-oxido-p-menthane in volatile oil of magnoliae flos,and the optimized extration technology for Xinzhi nasal drops is feasible.
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The inclusion complex of cordycepin ( COR ) with hydroxypropyl-β-cyclodextrin ( HPβCD ) was prepared by the method of saturated solution. The inclusion of HPβCD with COR in aqueous solution was studied by UV-vis spectroscopy, and the inclusion ratio of COR/HPβCD complex was determined with the Job plots. The COR/HPβCD complex was characterized and determined by means of 1 H NMR and 2D NMR, differential scanning calorimetry ( DSC ) , thermogravimetric analysis ( TG ) , X-ray diffraction ( XRD ) , Fourier transform infrared spectroscopy ( FTIR) and scanning electron microscope ( SEM) . The results showed that the COR/HPβCD complex ratio was 1:1 and the water solubility and stability of COR were obviously increased in the inclusion complex with HPβCD. The COR/HPβCD complex will be potentially useful for its medical application.
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The inclusion complex of cordycepin ( COR ) with hydroxypropyl-β-cyclodextrin ( HPβCD ) was prepared by the method of saturated solution. The inclusion of HPβCD with COR in aqueous solution was studied by UV-vis spectroscopy, and the inclusion ratio of COR/HPβCD complex was determined with the Job plots. The COR/HPβCD complex was characterized and determined by means of 1 H NMR and 2D NMR, differential scanning calorimetry ( DSC ) , thermogravimetric analysis ( TG ) , X-ray diffraction ( XRD ) , Fourier transform infrared spectroscopy ( FTIR) and scanning electron microscope ( SEM) . The results showed that the COR/HPβCD complex ratio was 1:1 and the water solubility and stability of COR were obviously increased in the inclusion complex with HPβCD. The COR/HPβCD complex will be potentially useful for its medical application.
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Diclofenac sodium was complexed with hydroxypropyl-β-cyclodextrin and physicochemical characterization was performed to evaluate the photo stability of diclofenac sodium. X-ray powder diffraction, UV-Vis analysis and Fourier Transform Infrared Spectroscopy were performed to examine the changes if any in the morphology and the configuration of the complex. The photo stability test followed by High Performance Liquid Chromatography analysis of the complex was determined. In vitro anti-inflammatory test using Human Red Blood Cell membrane stabilization method and in vivo analgesic activity studies in rat models to evaluate the therapeutic potential assessment of the complexed and norml diclofenac sodium. The test results have proved that the complexed diclofenac with hydroxypropyl-β-cyclodextrin enhance the photodegradation rate and resolute the optimal molar ratio of diclofenac to hydroxypropyl-β-cyclodextrin as 1:4. In vitro anti-inflammatory activity and in vivo analgesic activity results are indicates that the complexed form of diclofenac sodium with hydroxypropyl-β-cyclodextrin does not affects the therapeutic potentials of the drug.
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Objective To study the intestinal absorption characteristics of demethoxycurcumin hydroxypropyl/β cyclodcxtrin (DECD) and demethoxycurcumin (DE) in rats. Methods DECD was prepared by cyclodcxtrin inclusion technique and characterized by spectroscopic method. The morphology of DECD was observed by microphotograph and zeta potential was examined by Malvern laser particle sizer. In vivo single-pass intestinal perfusion rat model was adopted; the absorption rate constant (Ka), effective permeability (Papp) and percent absorption of DECD and DE were determined using the ultraviolet spectrophotometry. Results DECD was successfully prepared, with a solubility of 2. 30 g/L, which was 38. 33 times that of DE. Zeta potential of DECD was —32. 2 mV. The results of intestinal absorption experiment showed that the Ka and Papp values of DECD decreased in order in the ileum, duodenum, jejunum, and colon. In addition, the Ka, Papp values and percent absorption of DECD were higher than that of DE. Conclusion DECD can markedly improve the intestinal absorption of DE in rats.
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OBJECTIVE: To prepare the inclusion complex of Lignum dalbergia odorifera oil with hydroxyl-β-cyclodextrin (HP-β-CD), and to optimize the preparation process of it. METHODS: The inclusion complex was prepared by the stirring-freeze-dry meth od. The preparation process was optimized by central composite design-response surface method (CCD-RSM), with the colligation score which was calculated by the yield of inclusion, the utilization rate of volatile oil and the content of trans-nerolidol as index. The inclu sion complex was verified by phase-solubility method, DSC,UV and microscopical identification. RESULTS: The optimum inclusion technology was: inclusion solvent 5% ethanol, stirring rate 500 r·min-1, HP-β-CD to volatile oil 33:1, inclusion temperature 42℃, inclusion time 2.5 h. The formation of inclusion complex can change the solubility, optical and thermodynamic properties of volatile oil. CONCLUSION: The preparation process of inclusion complex of Lignum dalbergia odorifera oil with HP-β-CD optimized by CCD-RSM is reasonable and feasible, and provide a reliable experiment basis for its application.
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Objective:To prepare mesalazine hydroxypropyl-β-cyclodextrin ( MSZ-HP-β-CD) inclusion complexes and observe the properties. Methods:The inclusion complexes were prepared by a stirring method and the content of MSZ was determined by HPLC. The preparation technology was optimized by orthogonal test with the inclusion rate and the yield of inclusion complexes as the indices. The inclusion complexes were identified respectively by ultraviolet ( UV) spectrometry, X-ray diffraction ( XRD) and solubility. The dissolution rate was investigated. Results: Using the stirring method, the optimum preparation process was as follows: the inclusion temperature was 35 ℃, the ratio of MSZ to HP-β-CD was 1∶ 4 ( mg/g) , and the inclusion time was 3 h. The average inclusion rate of the complexes was 96. 28%, and the yield was 97. 87%. The identification results showed that the freeze-dried powder was inclusion complexes. Compared with that of MSZ, the dissolution of MSZ- HP-β-CD inclusion complexes was notably enhanced. Conclusion:The prepared MSZ-HP-β-CD with optimized technology has good reproducibility and stable technology, which can obviously improve the dissolution of MSZ.