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Objective To optimize the extraction of volatile oil from Qingjie Granules and process of inclusion compound of beta-cyclodextrin. Methods Water Distillation was used for extraction. Extraction time, grinding degree, and the amount of water were set as inspection factors, and volatile oil volume was set as the evaluation index to inspect extraction process of volatile oil from Qingjie Granules. With inclusion rate as the evaluation index, the single factor test and the Box-Behnken combined with the response surface method were used to choose the optimum inclusion process. Results The optimum extraction process for Schizonepetae Herba, Saposhnikoviae Radix and Forsythiae Fructus coarse powder should be with 10 times amount of water, extracting 3 h. Inclusion method should be saturated water solution method, and the inclusion process of volatile oil as feed and beta-cyclodextrin inclusion ratio was 1:12; the temperature was 40 ℃; inclusion time was 3.5 h. By means of TLC, UV and IR spectra, the formation of the inclusion compound of volatile oil in clear solution particles was preliminarily proved. Conclusion The optimum extraction and inclusion process of volatile oil from Qingjie Granules are stable and feasible, which can be used in industrial production.
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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 study the content of volatile oil from old leaves, tender leaves, fallen leaves and seeds of cinnamomum camphora tree in Hunan, China. To prepare and identify the volatile oil of its β-cycoldextrin inclusion compound. Methods The volatile oil was extracted by water-steam distillation. With inclusion rate as the index, trituration method, saturated water solution method and ultrasound method were compared. The optimum conditions were investigated by the orthogonal test. The inclusion compound was identified by thin-layer chromatography (TLC), ultraviolet visible spectrum (UV-Vis) and differential scanning calorimetry (DSC). Results From June to July, the average content of volatile oil extracted from old leaves, tender leaves, fallen leaves and seeds were 1.58%, 1.52%, 0.84% and 1.39%, respectively. The optimum preparation conditions were as follows:the ratio of β-cyclodextrin and volatile oil was 10∶1, the adding water was 4 times and inclusing time was 2 h. Before and after inclusion, the spectrum of TLC and UV-Vis of volatile oil showed no obvious change. The DSC of inclusion compound,β-cycoldextrin, volatile oil and the mixture had significant differences. Conclusion The amount of the volatile oil from old leaves is higher. The optimized condition of inclusion is stable and reasonable.
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OBJECTIVE:To optimize the formulation technology of paeonol-?-cyclodextrin inclusion compound. METHODS: The formulation technology of paeonol-?-cyclodextrin inclusion compound was optimized by performing orthogonal experiment with the amount of ?-cyclodextrin,the solid-liquid ratio (ratio of ?-cyclodextrin to paeonol alcohol solution),the concentration of the envelop liquid (alcohol) as factors and the ultrasonic time was studied by single factor test and with the utilization ratio and entrapment efficiency of paeonol as indexes for evaluation. Meanwhile,a verification test was performed. RESULTS: The optimal formulation technology was as follows: the amount of ?-cyclodextrin was 8 g;the solid-liquid ratio was 1∶3;the concentration of the alcohol was 40% and the ultrasounding time was 40 min. The verification test revealed that the labeled contents were about 90% for all samples (4 batches). CONCLUSION: The optimized formulation technology is simple and reasonable,and it is applicable for the preparation of paeonol-?-cyclodextrin inclusion compound.
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Objective To investigate antithrombotic and antiplatelet effects of Dragon's Blood,?-cyclodextrin inclusion of Dragon's Blood.Methods The methods of injection of adenosin diphosphate(ADP) into mouse tail vein,electrically stimulated arterial thrombosis in rats were used to evaluate the anti-thrombotic effects of Dragon's Blood and?-cyclodextrin inclusion of Dragon's Blood,respectively.Platelet aggregation(PRP or washed platelets) was tested according to Born's method.Results ?CYDB significantly protected against thrombosis caused by ADP on mice,and electrical stimulation on rats.In vitro?-cyclodextrin inclusion of Dragon's Blood inhibited AA,ADP,PAF-induced platelet aggregation.Conclusions The results suggest that compared with Dragon's Blood,?-cyclodextrin inclusion of Dragon's Blood has more potent anti-thrombotic effects on the thrombotic models,its mechanisms may be closely related to the inhibition of anti-platelet aggregation.?-cyclodextrin inclusion of Dragon's Blood can improve the bioavailability of Dragon's Blood.
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Objective To study conditions of?-cyclodextrin inclusion compound for oil from Zukamu granule.Methods The study was carried out with orthogonal design andsaturation water solution.The process conditions were studied by determining the utilizition ratio of oil Zukamu granule of inclusion compound.Results The optimum preparation conditions forinclusion were established as that oil to?-CD was 0.7∶4,inclusion temperature 20℃and supersonic time for 30 min.Conclusion This method is simple and utilizition ratio of oil is high,which is benefit to development of oil from Zukamu granule.
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OBJECTIVE:To establish a method for the content determination of naproxen in naproxen-?-cyclodextrin inclusion complex.METHODS:The drug concentration in naproxen-?-cyclodextrin inclusion complex was detected at the wavelength of330nm by using UV spectrophotometry.RESULTS:The linear range of naproxen was2.0～80.0mg/L(r=0.9995,n=5),the average recovery was99.22%(RSD=1.03%).CONCLUSIONS:The method is simple and reliable,which can be used for the content determination of naproxen in naproxen-?-cyclodextrin inclusion complex.
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OBJECTIVE:To study the preparation technic and determination of the content and dissolubility of the fluconazole-?-cyclodextrin inclusion complex(FCIC) METHODS:The FCIC was prepared by coprecipitation method and ultr_asonic method The content and percentage of the accumulated dissolubility of FCIC were determined by UV-spectrophotometry RESULTS:Fluconazole and ?-cyclodextrin could form inclusion complex through either preparation technology The contents of fluconazole in the complex were(11 34?0 77)% and(11 23?0 24)% respectively The dissolubility met the standard in CP CONCLUSION:Stable complex could be formed between fluconazole and ?-cyclodextrin
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OBJECTIVE:To establish the preparation process of inclusion complex of diclofenac sodium-?-cyclodextrin (DS-?-CD) eyedrops METHODS:The DS-?-CD was prepared by the stir method and identified with instrumental method The content of diclofenac sodium was detected by UV,HPLC RESULTS:The inclusion ratio of DS-?-CD was(67 48?2 96)% There was no difference between diclofenac sodium and DS-?-CD in UV absorption spectrum The crystal diffraction peak of DS inclosed in DS-?-CD disappeared in X-ray CONCLUSION:The DS-?-CD can be used as eyedrops in clinical practice
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OBJECTIVE: To prepare Indomethacin-hydroxypropy-cyclodextrin inclusion complex ointments and establish its assay method. METHODS: The preparation was prepared with O/W type emulsion ointment as base material, and the content of Indomethacin in which was determined by UV spectrophotometry. RESULTS: The calibration curve of Indomethacin was linear in the range of 16.76～41.91?g?mL-1(r=0.999 6),and its average recovery was 99.53%(RSD=1.50%). CONCLUSION: The ointments were convenient in preparation technique, and simple and accurate in determination.
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Objective To optimize the HP-?-cyclodextrin(HP-?-CD)inclusion process condition for volatile oils from Anti-virus Oral Solution. Methods The process conditions were screened by determining the inclusion rate of volatile oils and the yield of inclusion compound,and by comparing the inclusion effect of supersonic method,saturated water solution method and grinding method.The optimum condition was investigated by the orthogonal test. The inclusion compound was identified by TLC,differential scanning calorimetry(DSC) and ultraviolet spectrophotometry (UV). Results The optimum preparation conditions for inclusion were established as follows: the proportion of volatile oils and HP-?-cyclodextrin was 1 ∶12,the inclusion temperature was at 45 ℃and the inclusion time was 3 hours .The inclusion rate of volatile oils was 66.71 %,and the yield of inclusion compound was 90.07 %. Conclusion The complex prepared under the optimized condition is stable and has a highest inclusion rate.
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Objective To study the stability of ligustilide and the inclusion process in ?-cyclodextrin to avoid its isomerization.Methods The content of ligustilide dropped severely even if it was kept away from layer and air under room temperature.The inclusion process with ?-cyclodextrin was carried out on orthogonal design.The optimum conditions were determined and inclusion complex was made sure by many ways.Results The validated trials by DCS,IR,and GC could exhibit the obvious difference between mixture and inclusion complex which showed the form of a new phase,because of ?-cyclodextrin and drugs in the molecular capsules.Conclusion Inclusion process with ?-cyclodextrin can improve stability of ligustilide that is unstable in normal situation.
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Objective: To study optimum inclusion process conditions for Bencaosuansu. Methods: The study was carried out with orthogonal design. The process conditions were studied by determining the utilization ratio of Bencaosuansu, the oil-bearing rate and extract ratio of inclusion compound. Results: The optimum preparation conditions for inclusion were established as: Bencaosuansu: ?-CD was 1∶12, pH6, the inclusion time was for 5h. The utilization ratio of Bencaosuansu is 94.61 percent. Conclusion: The method can be used for production of ?-CD inclusion compound.
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Objective: To study optimum inclusion process conditions for volatile oil from Fructus Amomi Rotunds. Methods: The study was carried out with orthogonal design. The process conditions were studied by determining the utilazision ratio of volatile oil from Fructus Amomi Rotundus. Results: The optimum preparation conditions for inclusion were established as: volatile oil:? CD was 1∶8, The inclusion temperature was at 50 ?C and inclusion time for 2h, The ultilizasion ratio of volatile oil was 79.7%. Conclusion: The method can be used for mass production.
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Objective:To study optimum inclusion process conditions for volatile oil from Curcuma wenyujin. Methods: The study was carried out with orthogonal design. The process conditions were studied by determining the ultizision ratio of volatile oil from Curcuma wenyujin , the oil bearing rate and extract ratio of inclusion compound. Results: The optimum preparation conditions for inclusion were established as∶oil∶? CD was 1∶9, The inclusion temperature and time were at 40 ?C and for 1.5h , The ultizision ratio of oil was 86.5% . Conclusions: The rate is high and the method is applicable.
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Objective:To increase the solubility of the campher and oleum anisi stellati in the syrup of cough and reduce the precipitation of syrup.Methods: The technology of ? cyclodextrin inclusion was used in the experiment. Results: The experiment shows the method may meet the demand of production. Conclusions: The method is very good in the production of cough syrup.
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AIM:To investigate the effect of ?-cyclodextrin inclusion on transdermal absorption of volatile oil in lilac-cassiabark Gel. METHODS: The release test of two kinds of lilac-cassiabark Gel(gel A without ?-cyclodextrin inclusion and gel B with ?-cyclodextrin inclusion) was assayed with Franz diffusion cell with the help of the cumulative amount of eugenol in unit area in vitro. RESULTS: The percutaneous absorption process of eugenol in two kinds of gels were conformed to zero-order releasing model,and the transdermal rates were 16.212?4.128 and 11.344?1.929 ?g/(cm~2?h) respectively.Compared with gel A,the transdermal rate of eugenol was slower in gel B(P