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Efavirenz is a widely prescribed anti-retroviral drug that belongs to BCS class II and exhibit low and variable oral bioavailability due to its poor aqueous solubility and it requires enhancement in solubility and dissolution rate for increasing its oral bioavailability. The aim of this study was to increase the solubility of Efavirenz (EFA) by complexing it with Hydroxypropyl-β-cyclodextrin (HPβCD). Solid binary systems were prepared by co-grinding and microwave irradiation methods. The interaction of EFA with HPβCD was evaluated by Phase solubility studies, in vitro dissolution studies and different analytical techniques including Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). The apparent stability constant revealed EFA with HPβCD produces 1:1 M stoichiometric complex. The host guest interactions studied by FTIR and DSC confirmed true inclusion of EFA with HPβCD at 1:2 M. The Dissolution rates of EFA- HPβCD binary systems were faster when compared to physical mixture and pure drug. Overall the rank order of improvement in dissolution properties of Efavirenz with ratios is 1:2M > 1:1M and methods MW > CG > PM > Pure drug. One-way ANOVA suggest the DP60 and DE60 values were significantly higher (P<0.05) in solid binary systems prepared by microwave irradiation method when compared to co-grinding and its corresponding physical mixtures and pure drug.
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Objective To investigate effects of different solvent, different temperature and different concentration of hydroxypropyl cyclodextrin on solubility of asarone. Method Determination of asarone solubility in different solvent, at different temperature and different concentration of cyclodextrin were carried out by HPLC-UV method. Results The solubility of asarone in water, tea oil, ethanol, and methanol were 0. 1 mg·mL-1 13.44 mg·mL-1, 1.87 mg·mL-1 and 1.76 mg·mL-1, respectively. The concentration and temperature of cyclodextrin showed a positive correlation with solubility of asarone. At normal temperature, the solubility of asarone in water increased 10 times by 45 % hydroxypropyl cyclodextrin. Conclusion Asarone has poor solubility in water and it can be improved by high concentration of hydroxypropyl cyelodetrin.
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OBJECTIVE:To prepare tacrolimus-hydroxypropyl-?-cyclodextrin inclusion compound and to investigate the solubility of inclusion compound.METHODS:The inclusion compound was prepared by agitation method and identified by differential scanning calorimetry and X-ray diffraction analysis respectively.The solubility of inclusion compound was evaluated by phase-solubility method.RESULTS:The solubility of tacrolimus in water could be improved remarkably by hydroxypropyl-?-cyclodextrin and increased along with the increase of hydroxypropyl-?-cyclodextrin concentration and testing temperature.The solubility of tacrolimus was increased from 2.07 ?g?mL-1 to 167.74 ?g?mL-1 when the concentration of hydroxypropyl-?-cyclodextrin was 0.50 g?mL-1 at 25 ℃.Results of differential scanning calorimetry and X-ray diffraction analysis indicated inclusion compound was prepared successfully.CONCLUSION:Hydroxypropyl-?-cyclodextrin could increase the solubility of tacrolimus.
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Objective To study the preparation of volatile oils obtained from asarum and lily magnolia complexed with ?-cyclodextrin and hydroxypropyl-?-cyclodextrin in Xuetie Dingchuan plaster,and to study its impacts of transdermal absorption.Methods The volatile oil was complexed with ?-cyclodextrin and hydroxypropyl-?-cyclodextrin.GC method was used in the determination of volatile oils complexed with ?-cyclodextrin and hydroxypropyl-?-cyclodextrin to investigate the impacts of transdermal absorption.Results The accumulation transmission of the volatile oils complexed with ?-cyclodextrin was superior to that with hydroxypropyl-?-cyclodextrin.Conclusion The inclusion of volatile oils with ?-cyclodextrin can enhance drug penetration via skin.
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OBJECTIVE:To prepare the inclusion complex capsules of actarit-HP-?-CD and investigate their dissolution rate.METHODS:The inclusion complex was prepared by the stirring method with its dissolution rate investigated.The inclusion complex capsules were prepared with fillers consisted of starch,microcrystalline cellulose,lactose and calcium sulphate.The dissolution rate of the capsules was investigated by basket-stirring method and compared with those of the pure material and the physical mixture.RESULTS:Compared with pure material and physical mixture,the inclusion complex had significant lower value of Td(P
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OBJECTIVE:To investigate the complexation of clonazepam with hydroxypropyl-?-cyclodextrin(HP-?-CD)in aqueous solutions.METHODS:The complexation of clonazepam with(HP-?-CD),the inclusion molar ratio of host and guest molecules and thermodynamic parameters were detected using phase solubility method,equimolar series method,UV absorption spectroscopy etc.RESULTS:The solubility of clonazepam increased linearly with the increase of(HP-?-CD)level in aqueous solutions at different temperatures(25℃,35℃and45℃)and in buffers at different pH values(4.0,6.0and7.0),the phase solubility diagram was classified as type AL.CONCLUSIONS:Under the above research condition,the incl_ usion complexes of clonazepam with(HP-?-CD)can be formed spontaneously at a molar ratio of1∶1.
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Objective To prepare gliclazide (GZ) hydroxypropyl ? cyclodextrin (HP ? CD) inclusion complexes in order to enhance its aqueous solubility. Methods Inclusion complexes, prepared using 3 different methods of spray drying, freeze drying, and grinding, were identified by phase solubility analysis, infrared spectrophotometry, thermal analysis, and determination of the limited ammonium concentration. Results The HP ? CD inclusion complexes could be prepared by using the 3 different methods. The ratio of host/guest molecules was 1∶1. Ammonium residues were detected in inclusion complexes prepared by the freeze dried method. Conclusion The inclusion complexes can be prepared by the spray drying and grinding methods. The solubility of gliclazide can be significantly increased in the inclusion complexes.
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Objective To develop a candidate reference method for the measurement of progesterone in human serum.Methods The serum sample is mixed with the internal standard [3,4-~(13)C_2] progesterone.After extraction with n-hexane and purified by a aqueous solution of 2-Hydroxypropyl-?- cyclodextrin (HP-?-CD),the serum progesterone and labeled progesterone are converted to the 3-enol heptafluorobutyrate and analyzed by gas chromatography mass spectrometry (GC/MS) with selected ion monitoring.The concentration of serum progesterone is calculated by bracketing method.Results The results gave coefficients of variation (CVs) of 0.69% to 2.12%.The analytical recoveries ranged from 98.3% to 100.1%.The results of measuring certified reference materials of serum progesterone are agree with the target value.Conclusion The procedure for measuring progesterone in serum is a highly accurate and precise method and may be used as a candidate reference method for serum progesterone assays.
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Objective To improve the permeation of nasal mucosa by preparing the cholic acid-hydroxypropyl-?-cyclodextrin(HP-?-CD) and characterize the inclusion complex.Methods The inclusion complex was characterized by using phase solubility,scanning electron microscope(SEM),Fourier transform-infrared(FT-IR),differential scanning calorimetry(DSC),and superconducting NMR;In an effort to investigate the effect of HP?-CD on cholic acid,the studies of in vitro permeation of nasal mucosa was performed.Results Phase solubility curve was AL type,K=564.30 L/mol,and the characterization de-monstrates the formation of inclusion complex;The permeability coefficients and steady state fluxes through ovine and porcine nasal mucosa were enhanced by the formation of inclusion complex with HP-?-CD about 1.46 and 1.44 times of the uncomplexed cholic acid,respectively.Conclusion The inclusion complex is formed and it could increase the permeability of nasal mucosa by preparing the cholic acid-HP-?-CD.
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Objective To investigate the solubilitization effect of macromolecular paclitaxel with cyclodextrin and mechanism between inclusion complex and drugs. Methods The influence effects on paclitaxel solubility were studied with ?-cyclodextrin (?-CD) and hydroxypropyl-?-cyclodextrin (HP-?-CD) as inclusion carriers. The chemical shifts of hydrogen atom in host and guest molecules were also investigated with 1H-NMR. Results The form of inclusion complex was responsible by host molecules and the enhancement solubility of paclitaxel in HP-?-CD was larger than that in ?-CD and increased with the ratio increasing. The benzene ring in the molecular of HP-?-CD and paclitaxel showed the most significant effect. Conclusion The solubility of diossolved paclitaxel is improved by hydroxypropyl-?-cyclodextrin.
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Objective To investigate the inclusion of ginsenoside Rg_3 with hydroxylpropyl-?-cyclodextrin (HP-?-CD) in aqueous solutions, inclusion molar ratio of host and guest molecules, and change of thermodynamic parameters during the inclusion process. Methods The measurements of the inclusion mechanism, inclusion molar of the host and guest molecules, and change of thermodynamic parameters were carried out by the following methods: phase solubility, IR, NMR, and TLC methods, respectively. Results The results indicated that the inclusion compound of ginsenoside Rg_3-HP-?-CD was formed. The content analysis of the inclusion compound showed that the inclusion ratio of ginsenoside Rg_3-HP-?-CD was 1∶1. The change in the thermodynamic parameters suggested that the inclusion could proceed (△G
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AIM: To optimize the preparation of cholic acid-hydroxypropy-?-cyclodextrin inclusion complex,and its phase solubility analysis. METHODS: Orthogonal test,including molar ratio,inclusion temperature,mixing time and liquid dropping rate of cholic acid-HP-?-CD,was adopted to screen the optimal preparation,based on the inclusion efficiency by HPLC method.The solubilization effect was evaluated by using phase solubility.(RESULTS): The optimal preparation consisted of the molar ratio of cholic acid-HP-?-CD was 1∶3,60 ℃ inclusion temperature,60 min mixing time,1.6 mL/min liquid dropping rate;A_L type of phase solubility curve,K=564.30 L/mol,and 11.81 times solubilization. CONCLUSION: The optimal preparation is stable,reasonable and practicable with the encapsulation efficiency of 97.1%.Inclusing cholic acid with HP-?-CD is feasible,and the solubilization effect is significant.
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OBJECTIVE:To study the influence of both pH and complexation by hydroxypropyl-?-cyclodextrin(HPCD) on the overall solubility of hydroxycamptothecin(HCPT) with particular focus on the equilibrium between its lactone-and carboxylate-form.METHODS:Phase solubility studies at pH values and physiologically acceptable HPCD concentrations were performed,and the amounts of solubilized HCPT quantified by HPLC.The lactone-carboxylate-ratios from the equilibrium were studied.RESULTS:The solubility of HCPT increased with both increasing pH and HPCD concentration.The apparent complexation constant decreased with increasing pH.The lactone-carboxylate equivalence point shifted from a pH value of 6.5,7.0 and 7.3 with 0%,10% and 25% HPCD,respectively.Separate complexation constants for the carboxylate-HCPT and lactone-HCPT could thus be derived.CONCLUSION:The solubilizing and stabilizing effects of HPCD on HCPT in aqueous solution were good.