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Objective:To screen the optimal process of ambi-extracting of Xinyi Powder and inclusion of volatile oil.Methods:Single factor experiment was used to optimize the extraction process of Xinyi Powder by taking crushing particle size, extraction times, the amount of water added and extraction time as the investigation factors. L 9(3 4) orthogonal test was used to optimize the inclusion process of volatile oil in Xinyi Powder. Results:The optimal extraction process of ambi-extracting of Xinyi Powder was as follows: the slices were not crushed, 10 times the amount of water was added, and extracted for 3 hours; the best inclusion process of volatile oil as follows: β-cyclodextrin:water=1:25, β-cyclodextrin:volatile oil=6:1, inclusion temperature 35 ℃, inclusion time 3 hours.Conclusion:The ambi-extracting process and volatile oil inclusion process are simple, stable and feasible.
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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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In this study, butaselen-2,6-dimethyl-β-cyclodextrin inclusion complexes were prepared by saturated aqueous solution method to improve the solubility of butaselen, so as to obtain its injection solutions. The content of butaselen in the inclusions was determined by high performance liquid chromatography (HPLC), and then the preparation process was optimized by orthogonal design using the inclusion ratio as an indicator. X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscope (SEM) were used to verify the structure of the inclusions. The effects of the inclusions on the solubility and stability of butaselen were also investigated. The results showed that the optimized preparation process with a mass ratio of 1∶340, an encapsulation time of 3 h and an encapsulation temperature of 70 ℃ resulted in an encapsulation ratio of (91.24 ± 0.42) %, and the results of XRD, FTIR and SEM demonstrated the formation of inclusion complexes. The developed HPLC method is rapid, simple, accurate, applicable, specific and reproducible for the determination of butaselen content in butaselen cyclodextrin inclusion complexes, which can lay the foundation for the development of new butaselen dosage forms and clinical applications and provide technical support.
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The freeze-drying technique, characterized by low-temperature processing, is especially suitable for sensitive volatile oils with thermal instability. However, there are few studies focusing on the retention of volatile oils in the processing of freeze-dried preparations. This study evaluated the effects of different addition methods(adsorption, emulsification, solid dispersion, and inclusion) on the retention rate of the main components in peppermint oil, aiming to explore the application feasibility of freeze-dried preparations of volatile oils. Firstly, the addition method was determined based on the retention rates of menthol in four freeze-dried preparations. Secondly, an orthogonal test was designed to optimize the preparation process based on the characteristics of the preferred addition method. The results showed that the most suitable preparation form of peppermint oil was inclusion with beta-cyclodextrin(β-CD), and the retention rate of menthol in freeze-drying was 86.36%. According to the two-step preparation process of inclusion and freeze-drying, we introduced the product of inclusion rate and retention rate, i.e., comprehensive retention rate, to determine the optimum processing parameters. The results showed that β-CD/oil ratio of 7∶1, inclusion temperature of 40 ℃, and inclusion time of 2 h were the optimum processing parameters. The product prepared with these parameter had the comprehensive retention rate of 68.41%, retention rate of 92.53%, and inclusion rate of 73.93%. The inclusion compound was white powder with significantly increased solubility. The pre-paration process based on cyclodextrin inclusion in this study is stable and reliable and provides a new idea for ensuring the efficacy and stability of volatile components in freeze-dried preparations.
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Cyclodextrins , Freeze Drying , Mentha piperita , Oils, Volatile , Plant Oils , Solubility , TechnologyABSTRACT
Abstract Ramipril being ACE inhibitor belongs to BCS class II drug with low solubility and undergoes first-pass metabolism that leads to reduced bioavailability of 28%. The current research is aimed at formulating and evaluating ramipril fast dissolving oral films (FDOF). Solubility enhancement of ramipril was done by formation of inclusion complex with β-cyclodextrin in 3 ratios (1:0.5, 1:1, 1:2). Based on higher drug content and dissolution values the physical mixture of ramipril with β-cyclodextrin in 1:1 ratio (IC2) was chosen for further studies. Total 12 formulations of ramipril FDOF containing IC2 prepared with various polymers and evaluated for physicochemical properties. The optimized formulation F9 shown better tensile strength (11.6 g/cm2), significant % elongation (9.8) and maximum % drug content of 99.98 %. The formulation F9 exhibited minimum disintegration time of 9 sec that is desirable for immediate onset of action and maximum drug release. The FTIR data of F9 assured the compatibility of drug and formulation excipients, found to be stable for 180 days at accelerated conditions. The study confirmed that ramipril FDOF lead to quicker onset of action and enhanced therapeutic efficiency in comparison to marketed product.
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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 optimize the inclusion process for the volatile oil in Huaweishu Granules. Methods: Taking the ratio of volatile oil to β-cyclodextrin, inclusion temperature, stirring speed and stirring time as the factors, the inclusion process conditions were optimized by orthogonal test, the weight coefficients of each index were determined by entropy weight method, and the inclusion complex was verified by thin layer chromatography. Results: The inclusion rate of volatile oil obtained by stirring method was the highest, with the ratio of β-cyclodextrin to volatile oil of 10:1, the inclusion temperature was 40 ℃, the stirring time was 1 h, and the stirring rate was 400 r/min. Conclusion: The optimized volatile oil inclusion process is stable and feasible, with high inclusion rate of volatile oil and yield of inclusion compound.
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Objective: To investigate the applicability of the spray-dried microspheres of vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus for inclusion of cinnamon oil (CO) and compare with traditional inclusion technology of β-cyclodextrin. Methods: HPLC was used to determine the encapsulation rate of inclusion complex. Transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) were used to characterize the inclusion complex; The dissolution and stability of the inclusion complex was investigated by in vitro release test and accelerated stability test; The pharmacokinetic and analgesic efficacy tests were used to examine the bioavailability and efficacy of the inclusion complex. Results: The encapsulation rate of microsphere inclusion complex and β-cyclodextrin inclusion complex was (98.38 ± 0.30)% and (86.51 ± 0.52)%, respectively. Observation of the inclusion complex under TEM showed a uniform spherical-like structure with uniform dispersion; Observation under SEM showed that the inclusion complex was spherical with a concave surface; The endothermic peak of volatile oil of cinnamon in DSC and the diffraction peak in XRD disappeared. The cinnamon volatile oil was dispersed in theinclusion complex in the form of non-aggregation; The cumulative release rates of cinnamon volatile oil, microsphere inclusion complex and β-cyclodextrin inclusion complex in in vitro dissolution experiments were 97.05%, 93.36% and 80.26%, respectively; Accelerated stability test at 60 ℃ showed that the loss rate of volatile oil of microsphere inclusion complex was significantly lower than that of cinnamon volatile oil and β-cyclodextrin inclusion complex; Pharmacokinetics showed that the AUC0-∞ of cinnamon essential oil, microsphere inclusion complex and β-cyclodextrin inclusion complex were basically the same; Pharmacodynamics showed that the analgesic rates of cinnamon volatile oil in the three groups were 53.0%, 47.5% and 21.1%, respectively. Conclusion: The stability of cinnamon volatile oil was enhanced by the combination of spray-dried microspheres of vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus. The in vitro release, bioavailability and analgesic efficacy of microsphere were basically consistent with the volatile oil of cinnamon volatile oil, and it was superior to the inclusion compound of β-cyclodextrin. The vinyl pyrrolidone/vinyl acetate copolymer VA64-Soluplus microsphere inclusion compound had better water solubility. This study provides a new method for the inclusion of volatile oil.
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Objective::To investigate the pharmacodynamics of volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba, to establish a method for simultaneous determination of three essential ingredients (thymol, carvacrol and patchouli alcohol) in volatile oil of the couplet medicines by gas chromatography (GC), to optimize the preparation process of β-cyclodextrin (β-CD) inclusion complex of volatile oil in the couplet medicines and to confirm the formation of the inclusion complex. Method::An in vitro inflammatory response model was established by hyaluronidase activity inhibition test in order to detect the anti-inflammatory activity of the volatile oil. Also, the antioxidant activity of the volatile oil was assessed by 1, 1-diphenyl-2-trinitrophenylhydrazine (DPPH) free radical scavenging method. The inclusion of volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba was prepared by scaturated aqueous solution method, colloid milling method and grinding method, respectively. GC was used to determine the contents of thymol, carvacrol and patchouli alcohol in volatile oil for optimizing extraction and inclusion processes of volatile oil. Scanning electron microscope, infrared spectroscopy, thermal differential analysis, and X-ray diffraction (XRD) were used to verify the formation of the inclusion complex. Result::The volatile oil not only inhibited hyaluronidase activity to a certain extent, but also eliminated DPPH and increased with the increase of concentration. There was a good linear relationship between the peak area and concentration of thymol, carvacrol and patchouli alcohol at 0.021 3-0.426, 0.020 04-0.400 8, 0.022 6-0.452 g·L-1 (R2>0.999), respectively. Their recoveries were 99.59%(RSD 1.6%), 100.15%(RSD 1.5%), 100.70%(RSD 1.4%), respectively. The colloid milling method was optimized, and the formation of the inclusion complex was verified by the aforementioned methods. Conclusion::The volatile oil in couplet medicines of Moslae Herba and Pogostemonis Herba has certain anti-inflammatory activity and anti-oxidation ability. The colloid milling method was the best inclusion process for the volatile oil. The established GC has the advantages of simple, sensitive, accurate, reliable and reproducible, which can meet the requirements of simultaneous determination of thymol, carvacrol and patchouli alcohol in the inclusion complex.
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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 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 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 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： To establish a method for content determination of indapamide （IDP）-β-cyclodextrin （β-CD） inclusion compound， optimize the preparation technology， carry out phase identification and in vivo release study of it. METHODS： UV spectrophotometry was used to determine the content of IDP in IDP-β-CD inclusion compound. IDP-β-CD inclusion compound was prepared by the solution-stirring method and the preparation technology was optimized by the orthogonal experiment using inclusion rate as index. The inclusion rate and drug-loading rate were compared between different drying methods. Phase identification of IDP-β-CD inclusion compound was verified by IR and DSC. The cumulative release rate of inclusion compound was tested by in vitro experiment. RESULTS： The linear range of concentration of IDP was 2.0-14.0 μg/mL （r＝0.999 7）. The quantitative limit and detection limit were 0.204， 0.067 μg/mL， respectively. RSDs of precision， stability and repeatability tests were all less than 2％. The recoveries range was 98.8％-101.8％（RSD＝1.10％，n＝6）. The optimum technology conditions were as follows the molar ratio of β-CD to IDP was 3 ∶ 1， the inclusion time was 3 h， and the stirring speed was 300 r/min. Average inclusion rate of IDP-β-CD inclusion compound was 72.81％. IR and DSC analysis showed that IDP and β-CD formed inclusion compound through physical interaction. After spray drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （60.96±0.25）％ and （4.18±0.12）％. After freeze-drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （77.31±0.51）％ and （5.31±0.27）％. Accumulative release rates of IDP， IDP-β-CD inclusion compound （by freeze-drying and spray drying） were 37.2％， 42.5％ and 81.9％ within 12 h， respectively. Compared with IDP raw material， accumulative release rate of IDP-β-CD inclusion compound increased significantly after spray drying. CONCLUSIONS： Established method is simple and accurate. The optimal preparation technology of inclusion compound is stable and feasible. IDP-β-CD inclusion compound is prepared successfully. The inclusion compound prepared by spray drying shows higher release rate.
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OBJECTIVE： To establish the method for content determination of ligustilide and to optimize the extraction technology of volatile oil and inclusion technology in Quhan zhufeng granules. METHODS： HPLC method was adopted. The determination was performed on Waters C18 column with mobile phase consisted of methanol-water （70 ∶ 30， V/V） at the flow rate of 1 mL/min. The detection wavelength was set at 327 nm， and the column temperature was 30 ℃. The sample size was 10 μL. Using yield of volatile oil and the content of ligustilide as index， with soaking time， the amount of adding water and extraction time as factors， the extraction technology was optimized by orthogonal test. Using inclusion rate， the yield of inclusion compound and yield of volatile oil as index， with ratio of volatile oil to β-cyclodextrin， inclusion temperature and inclusion time as factors， the inclusion technology of volatile oil was optimized by orthogonal test. RESULTS： The linear range of ligustilide was 0.4-4 μg（r＝0.999 9）； RSDs of precision， stability and reproducibility tests were all lower than 2％ （n＝6）. The recoveries were 96.75％-102.03％（RSD＝2.06％，n＝6）. The optimal extraction technology of volatile oil included 10-fold water （mL/g）， soaking for 15 min， extracting for 8 h. Average yield of volatile oil was 0.310 7％， and average content of ligustilide was 0.418 0 mg/g. The optimal inclusion technology of volatile oil included ratio of β-cyclodextrin and volatile oil was 1 ∶ 8 （mL/g）； inclusion temperature was 50 ℃； inclusion time was 3 h. Average inclusion rate was 69.43％， and the yield of inclusion compound was 58.89％； the yield of volatile oil was 14.15％. CONCLUSIONS： Established determination method is simple， accurate and stable. The optimal extraction technology of volatile oil and inclusion technology are stable and feasible.
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OBJECTIVE: To observe effects of β-cyclodextrin inclusion on tanshinone ⅡA in the degradation which in rat intestinal flora in vitro. METHODS: Culturing the tanshinone ⅡA and inclusion compound separately with incubation buffer of rat intestinal flora, sampling after 06121824 h. Extracting the sample then analyze content by HPLC. RESULTS: The tanshinone ⅡA is degraded obviously by rat intestinal flora in vitro and degradation speed became slower after forming the inclusion compound. After degrading 18 h, the declining proportion of tanshinone ⅡA concerntration which in tanshinone ⅡA group and mixture of tanshinone ⅡA with β-cyclodextrin group reached (74.23±2.32)% and (80.23±1.14)% while (47.45±4.01)% in β-cyclodextrin inclusion group. CONCLUSION: The tanshinone ⅡA is degraded almost completely by rat intestinal flora in vitro during 24 h, the degradation speed will be slower while forming the inclusion compound.
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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 investigate the effect of β-cyclodextrin-assisted extraction on Cassiae Semen.METHODS The chemical constituents in aqueous extract and β-cyclodextrin extract determined and analyzed by UPLC and principal component analysis had their antioxidant activities tested by six methods (protective effects on lipid peroxidation injuries induced by spontaneous liver,CCl4,H2 O2,FeSO4-vitamin C,and scavenging effects on DPPH,hydroxyl free radicals).RESULTS Compared with aqueous extract,the component content and antioxidant activity of β-cyclodextrin extract were increased by 10.476％ and 80.88％,respectively.CONCLUSION β-Cyclodextrin can effectively enhance the component extraction rate and antioxidant activity of Cassiae Semen.
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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.