A preliminary study of pharmacokinetics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex / 南方医科大学学报

<p><b>OBJECTIVE</b>To compare the pharmacokinetic parameters of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex and free evodiamine suspension in rats, and investigate the pharmacokinetic characteristics of evodiamine inclusion complex.</p><p><b>METHODS</b>Both water solubility and cumulative release percentage of EHD were tested with evodiamine as the control. Blood samples were collected from the venous plexus of SD rats after intravenous administration with evodiamine inclusion complex and free evodiamine at 100 mg/kg (equivalent evodiamine dose). Plasma concentrations of evodiamine were determined by high-performance liquid chromatography (HPLC), and the pharmacokinetic parameters were calculated using DAS 2.1.1.</p><p><b>RESULTS</b>The evodiamine inclusion complex showed a better water solubility (18.46±0.36 µg/mL) and a higher cumulative release percentage [(76.8±4.9)%] than free evodiamine. The pharmacokinetic parameters of evodiamine inclusion complex and free evodiamine in rats were as follows: Cmax, 252.5±12.43 vs 161.3±3.45 µg/L; T(max), 4.00±0 vs 4.07±0 h; MRT(0-∞), 8.46±0.91 vs 4.43±0.74 h; AUC(0-t), 2266.40±28.64 vs 911.92±8.53 µg·L(-1)·h(-1); AUC(0-∞), 2359.76±31.58 vs 919.16±9.73 µg·L(-1)·h(-1). The relative bioavailability of evodiamine inclusion complex was 256.73%.</p><p><b>CONCLUSION</b>Compared with free evodiamine, evodiamine inclusion complex has a higher bioavailability.</p>

Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex / 中国中药杂志

Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.

Impact of drug molecules on HP-β-CD compound inclusion / 中国中药杂志

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.

Preparation of colon target pellets of Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare colon target pellets of Pulsatilla total saponins.</p><p><b>METHOD</b>Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion was prepared by the water solution-mixing method. Then plain pills of inclusion were prepared by the granulation-spheronization method, and coated by Glatt fluid bed.</p><p><b>RESULT</b>The dissolution of plain pills of Pulsatilla total saponins at 2 h was 16.0%, while that of plain pills of inclusion at 0.5 h was 91.9%. With Eudragit S100 as the coating material, TEC as the plasticizer and talcum power as the anti-adherent, when the coating weight was 12%, the coating efficiency was high, with almost no bonding and drug release of coated pellets in artificial gastric juice for 2 h. The accumulated drug release in artificial intestinal fluid for 4 h was less than 15%, and that in artificial colon fluid for 4 h was more than 90%.</p><p><b>CONCLUSION</b>Coated pellets of Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion showed a good colon targeted drug release in vitro, thus could be further developed to be oral colon targeted preparations.</p>

Preparation of naringenin by enzymolysis of naringin-HP-beta-CD / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the major factors affecting the conversion efficiency of naringin-HP-beta-CD that was enzymed to prepare naringenin were determined and select the process condition with high conversion efficiency, stable and suitable for industrial production.</p><p><b>METHOD</b>The dropping method was used to prepare naringin-HP-beta-CD, which was hydrolyzed by snailase to obtain naringenin. With the bioconversion rate as the index, the effects of pH value, temperature, reaction time, dosage of enzyme and concentration of naringin-HP-beta-CD on conversion rate of naringenin were detected for the purpose of optimizing the preparation condition. the conversion efficiency of naringin-HP-beta-CD was verified by scanning calorimetry, and the Hydrolysis product was identified by H-NMR, and 13C-NMR.</p><p><b>RESULT</b>The optimum enzymolysis of naringin-HP-beta-CD with snailase was 98.4% under the conditions of 37 degrees C, a pH 5.0 acetic acid- sodium acetate buffer solution for 12 hours. The substrate concentration was 30 g x L(-1) and the weight ratio of enzyme and substrate was 3: 5. Under the optimum enzymolysis condition, the conversion rate of naringin-HP-beta-CD was higher than naringin that was not entrapped with HP-beta-CD, with 272.25 reaction product relative molecules. The structure of naringenin was confirmed by the analysis of 1H-NMR and 13C-NMR.</p><p><b>CONCLUSION</b>Naringin which is entrapped with HP-beta-CD to prepare naringenin can significantly improve the conversion efficiency by shortening the reaction time, increasing the concentration of the substrate and reducing the amount of enzyme. Therefore, the process is stable and it was suitable for industrialization.</p>

Synthesis of a supermolecular nanoparticle γ-hy-PC/Ada-Dox and its antitumor activity / 浙江大学学报·医学版

<p><b>OBJECTIVE</b>To synthesize a (2-Hydroxypropyl)-γ-cyclodextrin-polyethylenimine/adamantane-conjugated doxorubicin (γ-hy-PC/Ada-Dox) based supramolecular nanoparticle with host-guest interaction and to identify its physicochemical characterizations and antitumor effect.</p><p><b>METHODS</b>A novel non-viral gene delivery vector γ-hy-PC/Ada-Dox was synthesized based on host-guest interaction. 1H-NMR, NOESY, UV-Vis, XRD and TGA were used to confirm the structure of the vector. The DNA condensing ability of complexes was investigated by particle size, zeta potential and gel retardation assay. Cytotoxicity of complexes was determined by MTT assay in BEL-7402 and SMMC-7721 cells. Cell wound healing assay was performed in HEK293 and BEL-7404 cells. The transfection efficiency was investigated in HEK293 cells. H/E staining and cell uptake assay was performed in BEL-7402 cells.</p><p><b>RESULTS</b>The structure of γ-hy-PC/Ada-Dox was characterized by 1H-NMR, NOESY, UV-Vis, XRD, TGA. The drug loading was 0.5% and 5.5%. Gel retardation assay showed that γ-hy-PC was able to completely condense DNA at N/P ratio of 2; 0.5% and 5.5% γ-hy-PC/Ada-Dox was able to completely condense DNA at N/P ratio of 3 and 4,respectively. The cytotoxicity of polymers was lower than that of PEI25KDa. The transfection efficiency of γ-hy-PC was higher than that of γ-hy-PC/Ada-Dox at N/P ratio of 30 in HEK293 cells; and the transfection efficiency was decreasing when Ada-Dox loading was increasing. Cell uptake assay showed that γ-hy-PC/Ada-Dox was able to carry drug and FAM-siRNA into cells.</p><p><b>CONCLUSION</b>The novel vector γ-hy-PC/Ada-Dox has been developed successfully, which has certain transfection efficiency and antitumor activity.</p>

Preparation and characterization of dihydroartemisinin/ hydroxypropyl-beta-cyclodextrin inclusion complex / 药学学报

To optimize the preparation method of the complex of dihydroartemisinin (DHA) included by hydroxypropyl-beta-cyclodextrin (HP-beta-CD), the molar ratio of DHA and HP-beta-CD, inclusion temperature and inclusion time were optimized by the orthogonal design method with the inclusion drug yield and drug loading as the evaluation indexes. The IR spectrum, DSC and PXRD analyses were employed to characterize the complex and the molecular simulation was processed to investigate the tendency of complex formation. The optimized molar ratio of DHA and HP-beta-CD was 1 : 5, and the optimized preparation was performed under 50 degrees C for 1 h. The IR spectrum, DSC and PXRD analyses indicated the formation of the complex. The low binding free energy and the high solvent accessible surface obtained by molecular simulation showed that DHA could be included by HP-beta-CD and its solubility could be improved significantly. In conclusion, the optimized conditions for the preparation of DHA-HP-beta-CD complex provide a theoretical and experimental basis for further scale-up research.

Preparation, identification and thermodynamic stability of capsaicin-hydroxypropyl-beta-cyclodextrin inclusion compound / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare and identify the capsaicin-hydroxypropyl-beta-cyclodextrin (capsaicin-HP-beta-CD) inclusion compound the mol ratio between capsaicin and HP-beta-CD and the thermodynamic constants in inclusion were studied simultaneously.</p><p><b>METHOD</b>The capsaicin-HP-beta-CD inclusion compound was prepared with the method of saturation aqueous solution. Meanwhile, the inclusion compound was identified by differential scanning calorimetry methods (DSC), infrared spectrometry (IR), and X-ray diffraction (XRD), respectively. The mol ratio between host and guest molecular and the thermodynamic constants during the inclusion process were also researched by phase solubility method.</p><p><b>RESULT</b>An 1 : 1 molar ratio inclusion compound of capsaicin with HP-beta-CD could form at 25, 35 and 45 degrees C. The phase diagram was A(L) type.</p><p><b>CONCLUSION</b>The solubility of capsaicin-HP-beta-CD inclusion compound can be increased obviously.</p>

Preparation of coated tablets of glycyrrhetic acid-HP-beta-cyclodextrin tablets for colon-specific release / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare coated tablets of glycyrrhetinic acid and hydroxypropyl-beta-cyclodextrin (GTA-HP-beta-CYD) inclusion complex tablets for colon-specific release.</p><p><b>METHOD</b>In order to improve the solubility of GTA, the GTA-HP-beta-CYD inclusion complex was prepared by ultrasonic-lyophilization technique and its formation were characterized by X-ray powder diffraction profiles and infrared spectrometry. The effects of inclusion condition on the inclusion efficiency and stability coefficient of inclusion complex were investigated, respectively. After prepared GTA-HP-beta-CYD tablets by powder direct compression, the pH dependant polymer Eudragit III and/or mixed with Eudragit II were used for further coating materials in fluid-bed coater. The influences of coating weight on the GTA release in different pH conditions were evaluated to establish the method for prepering colon specific delivery tablets with pulsed release properties.</p><p><b>RESULT</b>The formation of inclusion complexes were proved by X-ray powder diffraction profile and phase solubility curve. The effect of pH value of solvent was played critical role on the preparation of GTA- HP-beta-CYD inclusion complex. And the inclusion efficiency of GTA was 9. 3% and the solubility was increased to 54. 6 times at optimized method. The Eudragit III coated GTA- HP-beta-CYD tablets with coating weight 10% and 16% were showed pH dependant colon specific release profiles with slow release rate. The release profile of tablets coated with the mixture of Eudragit II and Eudragit III (1:2) were indicated typical pH dependant colon specific and pulsed release properties while the coating weight was 17%.</p><p><b>CONCLUSION</b>The preliminary method for preparation of colon specific release tablets containing glycyrrhetinic acid with improved solubility was established for further in vivo therapeutic experiment.</p>

Studies on cyclodextrin inclusion complexes of Dragon's blood and its tablets preparation / 中国中药杂志

<p><b>OBJECTIVE</b>To study the cyclodextrin inclusion complexes of Dragon's blood for improving the drug solubility and the preparation.</p><p><b>METHOD</b>The inclusion complexes were prepared with beta-cyclodextrin, HP-beta-cyclodextrin, SBE-beta-cyclodextrin and confirmed by DTA. The activity of the inclusion complex was tested by animal experiments. Inclusion complexes tablets were prepared and the dissolution test was performed.</p><p><b>RESULT</b>The solubility of inclusion complexes was increased to 13. 75-168. 39 times. The activity of the inclusion complex was markedly improved, and dissolution rate was 78.69%.</p><p><b>CONCLUSION</b>The cyclodextrin inclusion complexes of Dragon's blood have a good solubility, dissolution rate and pharmacological activity.</p>

Preparation and in vitro evaluation of gastroretentive dosage form containing puerarin-HP-beta-CD inclusion complex / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare a novel floating micropellets containing hydroxy propyl-beta-oyclodextrin(puerarin-HP-beta-CD) for gastroretentive dosage form and evaluate its pharmaceutical characteristics in vitro.</p><p><b>METHOD</b>The puerarin HP-beta-cyclodextrin inclusion complex was prepared by freeze-drying method. Puerarin and its HP-beta-CD inclusion complex were incorporated into alginate beads, respectively. The effect of methyl cellulose (MC), Mg-Stearate and chitosan on buoyancy and cumulative release rate of puerarin were investigated in simulated gastric fluid.</p><p><b>RESULT</b>The spectrums of FTIR and profiles of X-ray powder diffraction of samples proved the formation of inclusion complex between puerarin and HP-beta-CD. Magnesium stearate had a significant effect on the buoyancy of micropellets, and satisfied results were gained by the content with 2%. The solubility of puerarin was increased 65.6-fold by the formation of inclusion complex, the dissolution rate and cumulative release percentage also improved significantly although with the burst release phenomena. The micropellets showed sustained release properties by using puerarin-HP-beta-CD inclusion complex mixed with puerarin (1:1) and treated thoroughly under homogenizer.</p><p><b>CONCLUSION</b>The solubility and release rate of puerarin are increased by the formation of inclusion complex with HP-beta-CD and its gastroretentive dosage forms displayed satisfied floating and sustained release characteristics.</p>

Characterization of microstructure of ibuprofen-hydroxypropyl-beta-cyclodextrin and ibuprofen-beta-cyclodextrin by atomic force microscope / 药学学报

The microstructures of ibuprofen-hydroxypropyl-bets-cyclodextrin (IBU-HP-beta-CyD) and ibuprofen-beta-cyclodextrin (IBU-beta-CyD) were observed by atomic force microscope (AFM). The high resolving capability of AFM has the tungsten filament probe with the spring constant of 0.06 N x m(-1). Samples were observed in a small scale scanning area of 10.5 nm x 10.5 nm and 800 x 800 pixels. The original scanning images were gained by tapping mode at room temperature. Their three-dimensional reconstruction of microstructure was performed by G3DR software. The outer diameters of HP-beta-CyD and beta-CyD are 1.53 nm. The benzene diameter of IBU is 0.62 nm, fitting to the inner diameters of HP-beta-CyD and beta-CyD. The benzene and hydrophobic chain of IBU enter into the hole of cyclodextrin at 1:1 ratio. The results were evidenced by IR, X-ray diffraction and the phase solubility.

Promoting mechanism of enhancers and transport pathway of large hydrophilic molecular across nasal epithelium studied by ESR and CLSM technologies / 药学学报

The aim of this study is to investigate absorption-promoting mechanism of enhancers and the transport pathway of large hydrophilous molecular across rat nasal epithelium by electron spin resonance (ESR) and confocal laser scanning microscopy (CLSM) technologies. In the experiment, recombinant hirudin-2 (rHV2) was chosen as a large hydrophilic molecular model drug. After nasal administration in rats the bioavailability of rHV2 with or without various enhancers was compared. The effects of enhancers on membrane lipid fluidity and protein conformation were measured with 5-deoxyl-stearic acid (5-DSA), 16-deoxyl-stearic acid (16-DSA) and 3-maleidoproxyl (MSL) labeling ESR. The effects of enhancers on cytoskeletal F-actin of rat nasal epithelium and FITC-rHV2 transport pathway across rat nasal epithelium were performed by CLSM combined with fluorescence labeling. 0.5% Chitosan (CS), 5% hydroxyl-propyl-beta-cyclodextrin ( HP-beta-CD) and 1% ammonium glycyrrhizinate (AMGZ) were all able to significantly increase the nasal absorption of rHV2. CS could result in the paracellular pathway transport of FITC-rHV2 which seemed related to a transient effect on tight junctions. HP-beta-CD could cause paracellular and transcellular route transport of FITC-rHV2 by influencing upon membrane protein as well as lipid fluidity. AMGZ seemed to enhance the transcellular route transport of FITC-rHV2, and could exert some influence on membrane protein but not on lipid fluidity. So how it brought out this result needs further research. Present experiment may become a useful reference for promoting mechanism of enhancers and the transport pathway of large hydrophilic molecular across nasal epithelium research.

Factors influencing the content of residual tert-butyl alcohol in cyclodextrin complex prepared by lyophilization cosolvent system / 药学学报

In order to minimize the residual tert-butyl alcohol (TBA) level in cyclodextrin complex prepared by freeze drying TBA/water cosolvent system, the formulation and lyophilization procedure that may influence the residual TBA was studied. Residual TBA in freeze dried cyclodextrin complex was determined by gas chromatography. The significant formulation and processing factors that influence residual TBA were identified by adjusting the initial TBA concentration in cosolvent, selecting cyclodextrin type (beta-cyclodextrin or hydroxypropyl beta-cyclodextrin), changing sample volume in flasket, altering freezing mode (fast freezing or slow freezing) and modifying the duration of secondary drying. The results show that the amorphous cyclodextrin material (hydroxypropyl beta-cyclodextrin), initial low TBA concentration in cosolvent and fast freezing would lead to high TBA residue in cyclodextrin complex, annealing was effective in reducing the residual TBA. The duration of secondary drying had no distinct effect on residual TBA. It is concluded that in order to reduce residual TBA in cyclodextrin complex prepared by lyophilization monophase solution, the initial TBA concentration in cosolvent should be higher than the crystal formation concentration, the appropriate cyclodextrin type and freeze drying processing should be choosen.

Combined effect of cosolvent and cyclodextrin on solubilization of insoluble drugs / 药学学报

<p><b>AIM</b>To investigate the combined effect of cosolvent and cyclodextrin (CD) on solubilization of insoluble drugs.</p><p><b>METHODS</b>Phase-solubility method was applied to determine solubilization of two diterpenoids in cosolvent / cyclodextrin combinations. The combined effect was evaluated and explained with an established mathematical model, and the model parameters were calculated by means of nonlinear regression analysis.</p><p><b>RESULTS</b>The strong agreement between the predicted and the observed solubility data supports the validity of the proposed model, with the determination coefficients of two regression models were 0.993 and 0.992, separately.</p><p><b>CONCLUSION</b>The validated mathematical model can be used to explain and predict the combined solubilization of the two insoluble drugs in different cosolvent systems.</p>

Electroanalytical method for TPPS4, the interaction of TPPS4 with BSA and the influence of CDs on it by fluorescence spectroscopy / 药学学报

<p><b>AIM</b>To establish a simple, rapid and accurate electroanalytical method for water soluble porphyrin meso-tetrakis-(4-sulfonatophenyl) porphyrin (TPPS4); to clarify the reaction between water soluble porphyrins and bovine serum albumin (BSA); and to determine the interaction of TPPS4 with BSA in the absence of presence of cyclodextrins (CDs), separately.</p><p><b>METHODS</b>Three methods including LSV, UV spectroscopy and fluorescence spectroscopy had been employed to the relevant experiments. The way of employing three methods at the same time could make the experiment results more reliable.</p><p><b>RESULTS</b>In the supporting electrolyte of NaH2 PO4-Na2 HPO4 (pH 7.18), a sensitive reduction peak of TPPS4 was found by linear sweep voltammetry (LSV), the peak potential (Ep) was -0.70 V (vs SCE). The relationship between the second derivative peak of LSV (ip") and the concentration of TPPS4 was linear from 1.0 x 10(-7) mol x L(-1) to 1.0 x 10(-5) mol x L(-1), the square of correlation coefficients (r2) were 0.998 3 and 0.999 3, respectively. The relative standard deviation (RSD) was 0.56% (n = 5). The mean recovery of TPPS4 was 99.59%. In NH4Cl-NH3 x H2O buffers (pH 9.05), it was proved that BSA and TPPS4 could interact with each other and form 1 : 1 TPPS4-BSA supramolecular system. Moreover, the interaction between TPPS4 and BSA had been investigated by adding cyclodextrins (CDs). The interaction of TPPS4 with BSA was facilitated both by hydroxypropyl-beta-CD (HP-beta-CD) and sulforbutylether-beta-CD (SBE-beta-CD).</p><p><b>CONCLUSION</b>An electroanalytical method for TPPS4 has been established by LSV. The porphyrin drugs included by CDs could react with protein existing inside the human body easier. The consequences of this article also show that CDs will play important role in controlling and releasing the porphyrin drugs.</p>

Studies on absorptive mechanism of lipophilic components of danshen from its hydroxypropyl-beta-cyclodextrin inclusion complex / 生物医学工程学杂志

Taking Tanshinon IIA as the target and using reversed phase high performance liquid chromatography,we have developed a rapid and sensitive assay for lipophilic components of Danshen (LCD) in perfusate. The model of intestinal absorption was used to determine the concentration of Tanshinon IIA in rats as an in situ model. The change of concentration of Tanshinon IIA was separately calculated according to Michaelis-Menten and the Fick's equation to investigate the absorptive limit step of the LCD. It was concluded that the limit step to absorption of LCD was at the dissolution, by assessing the fitting index or correlative index. On the basis of the conclusion, the experiment was designed to prepare the inclusive complex of the LCD with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and to study its absorptive mechanism. With the increase of dosage of complex, its absorption did not show saturated phenomenon in gastro-intestinal tract in rats and the constant Ka did not show significant difference, suggesting that the transport of mechanism in vivo is similar to passive transport.

Preparation of inclusion complex of daidzein and hydropropyl-beta-cyclodextrin / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare an inclusion complex of daidzein and hydropropyl-beta-cyclodextrin to enhance the solubility of daidzein.</p><p><b>METHOD</b>The inclusion complex of daidzein was prepared by the solution stirring method. The binary system of daidzein and HP-beta-CD was confirmed by differential thermal, thermogravimetry analysis, infrared spectroscopy and X-ray diffractometry.</p><p><b>RESULT</b>The drug content in the inclusion complex was 6. 76% and the solubility was 13.68 mg x mL(-1). The identification results showed that the inclusion complex was formed.</p><p><b>CONCLUSION</b>The preparation method of the inclusion complex of daidzein and hydropropyl-beta-cyclodextrin is simple and available, with a increased solubility of daidzein.</p>

Preparation, identification and inclusion actions of irisquinone hydroxypropyl-beta-cyclodextrin inclusion complex / 药学学报

<p><b>AIM</b>To perpare and identify irisquinone hydroxypropyl-beta-cyclodextrin inclusion complex (irisquinone-HP-beta-CD), as well as to study the inclusion mechanism and molecule stoichiometry between irisquinone and hydroxypropyl-beta-cyclodextrin.</p><p><b>METHODS</b>Irisquinone-HP-beta-CD was prepared by freeze-drying technique. The ratio of host and guest was also studied in inclusion process by mol gradient and continuing variational methods. At the same time, the inclusion complex was identified by X-ray diffraction (XRD) and differential scanning calorimetry (DSC).</p><p><b>RESULTS</b>It was demonstrated that the solubility of irisquinone was enhanced markedly by inclusion with HP-beta-CD when stoichiometry was 2:1 of host and guest at 25 degrees C, 35 degrees C and 45 degrees C.</p><p><b>CONCLUSION</b>The solubility and stability of irisquinone could be increased by preparing the inclusion complex with hydroxypropyl-beta-cyclodextrin.</p>

Study of diffusion of muscone in different inclusion complexes and liposome through mouse (correction of rat) skin in vitro / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the penetrating rate of muscone in different inclusion complexes and liposome.</p><p><b>METHOD</b>The transdermal effect of muscone in different inclusion complexes and liposome was studied comparatively on mouse [corrected] skin with 40% EtOH as the absorption solution and with an improved Franz diffuse cell.</p><p><b>RESULT</b>Among the different inclusion complexes and liposome, the penetrating rate of muscone in the HP-beta-cyclodextrin inclusion and the liposome were higher than muscone, and that of muscone in the beta-cyclodextrin inclusion is the lowest.</p><p><b>CONCLUSION</b>The HP-beta-cyclodextrin inclusion and the liposome can hence the muscone transdermal speed.</p>