Inclusion complex of nateglinide with sulfobutyl ether β-cyclodextrin: Preparation, characterization and water solubility

2017 ◽  
Vol 1141 ◽  
pp. 328-334 ◽  
Author(s):  
Jingna Xu ◽  
Yimin Zhang ◽  
Xiayang Li ◽  
Yan Zheng
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Sulfobutyl Ether

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

Investigation of inclusion complex of honokiol with sulfobutyl ether-β-cyclodextrin

2014 ◽  
Vol 113 ◽  
pp. 9-15 ◽  
Author(s):  
Caibing Xu ◽  
Yalan Tang ◽  
Wenjing Hu ◽  
Rui Tian ◽  
Yuntao Jia ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
Sulfobutyl Ether

scholarly journals Preparation, Characterization, and Bioavailability of Host-Guest Inclusion Complex of Ginsenoside Re with Gamma-Cyclodextrin

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7227
Author(s):  
Hui Li ◽  
Guolei Zhang ◽  
Wei Wang ◽  
Changbao Chen ◽  
Lili Jiao ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Area Under The Curve ◽  
Relative Bioavailability ◽  
Docking Studies ◽  
Solubility Parameters ◽  
Phase Solubility ◽  
Scanning Calorimetry ◽  
Ginsenoside Re

This work aimed at improving the water solubility of Ginsenoside (G)-Re by forming an inclusion complex. The solubility parameters of G-Re in alpha (α), beta (β), and gamma (γ) cyclodextrin (CD) were investigated. The phase solubility profiles were all classified as AL-type that indicated the 1:1 stoichiometric relationship with the stability constants Ks which were 22 M−1 (α-CD), 612 M−1 (β-CD), and 14,410 M−1 (γ-CD), respectively. Molecular docking studies confirmed the results of phase solubility with the binding energy of −4.7 (α-CD), −5.10 (β-CD), and −6.70 (γ-CD) kcal/mol, respectively. The inclusion complex (IC) of G-Re was prepared with γ-CD via the water-stirring method followed by freeze-drying. The successful preparation of IC was confirmed by powder X-ray diffraction (XRD), Fourier transform-infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). In-vivo absorption studies were carried out by LC-MS/MS. Dissolution rate of G-Re was increased 9.27 times after inclusion, and the peak blood concentration was 2.7-fold higher than that of pure G-Re powder. The relative bioavailability calculated from the ratio of Area under the curve AUC0–∞ of the inclusion to pure G-Re powder was 171%. This study offers the first report that describes G-Re’s inclusion into γ-CD, and explored the inclusion complex’s mechanism at the molecular level. The results indicated that the solubility could be significantly improved as well as the bioavailability, implying γ-CD was a very suitable inclusion host for complex preparation of G-Re.

An Assessment of Olmesartan Medoxomil Tablet by Inclusion Complex Technique

2021 ◽  
pp. 193-197
Author(s):  
Deepak Sarangi ◽  
Subhashree Mallick ◽  
Anjum Ara ◽  
Sanjeeb Kumar Sahoo ◽  
Rabinarayan Rana
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Olmesartan Medoxomil ◽  
Complexing Agents ◽  
Complexing Agent ◽  
Angiotensin Ii Receptor ◽  
Current Effort ◽  
Ir Studies ◽  
Beta Cyclodextrin ◽  
Ft Ir

Olmesartan Medoxomil is an AT1 subtype selected angiotensin-II receptor antagonist approved for the treatment of hypertension. It has low water solubility, so the current effort is being made to enhance the solubility of the Olmesartan by inclusion complex and to incorporate them into tablets by direct compression. Complexing agent like Beta cyclodextrin and polyvinyalpyrrolidone has been used for complexation method. FT-IR studies have shown that there is no link between drugs and complexing agents. Among all methods, the inclusion complex (OLBCD 3) containing the drug: Beta cyclodextrin in a 1: 3 ratio showed rapid drug release (87.41% within 30 minutes) and post compression parameters are within limits. All the values obtained from pre compression and post compression parameters meets the legal requirements for tablets. Stability studies of batch no OLBCD 3 shows no significant change. Therefore, it can be concluded that the structure was stable.

scholarly journals Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

Polymers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1396 ◽  
Author(s):  
Shuang Gao ◽  
Jing-Yu Jiang ◽  
Yan-Yan Liu ◽  
Ying Fu ◽  
Li-Xia Zhao ◽  
...  
Keyword(s):  
Inclusion Complex ◽  
1H Nmr ◽  
Water Solubility ◽  
Herbicidal Activity ◽  
Environmental Damage ◽  
Phase Solubility ◽  
Scanning Calorimetry ◽  
Enhanced Solubility ◽  
Phase Solubility Study ◽  
Herbicide Diuron

The herbicide diuron is hardly soluble in water and most organic solvents and is usually made into a wettable powder or mixed with soil when used, which causes environmental risk and a reduction in herbicidal efficacy. In this study, the physicochemical properties were changed by using β-cyclodextrin (β-CD) to encapsulate diuron to form an inclusion complex. Some key technologies, including X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and nuclear magnetic resonance (1H NMR), were used to characterize the inclusion complex. The stoichiometry of the inclusion complex was determined by recording the 1H NMR spectrum or by using a diagram of inclusion ratios. A phase solubility study proved that the formed inclusion complex exhibited higher water solubility. Thermogravimetric analysis (TGA) demonstrated that the formed inclusion complex exhibited better thermal stability. Biological activity studies indicated that the herbicidal activity, in terms of herbicide removal, of the formed inclusion complex was higher than that of the original diuron. In general, the formation of the inclusion complex could reduce the environmental damage caused by diuron and enhance its herbicidal activity, providing an environmentally friendly method for using diuron.

scholarly journals Functional Supramolecular of Inclusion Complex of Herbicide Fluroxypyr with HPβCD

Polymers ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 1294 ◽  
Author(s):  
Shuang Gao ◽  
Chao Bie ◽  
Yanyan Liu ◽  
Tianyu Zhang ◽  
Ying Fu ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Inclusion Complex ◽  
Solution Method ◽  
Water Solubility ◽  
Herbicidal Activity ◽  
Saturated Solution ◽  
Phase Solubility ◽  
Bioactivity Assay ◽  
Ft Ir ◽  
Tga Analysis

In this study, hydroxypropyl-β-cyclodextrin (HPβCD) was used to form an inclusion complex with fluroxypyr to enhance water solubility and thermal stability. The inclusion complex was prepared by a saturated solution method and characterized by FT-IR, SEM, TGA, and XRD. All results indicated that fluroxypyr successfully entered the HPβCD cavity. In addition, the study of phase solubility identifies that the water solubility of fluroxypyr was greatly improved after the formation of the inclusion complex, and TGA analysis suggested that the formation of the inclusion complex improved the thermal stability. Bioactivity assay tests showed that the inclusion complex still had strong herbicidal activity. Our research showed that HPβCD was a promising carrier for improving the properties of fluroxypyr and, thus, expanding its use in agrochemical formulations.

scholarly journals Associated-Extraction Efficiency of Six Cyclodextrins on Various Flavonoids in Puerariae Lobatae Radix

Molecules ◽  
2018 ◽  
Vol 24 (1) ◽  
pp. 93 ◽  
Author(s):  
Tao Feng ◽  
Fan Liu ◽  
Lili Sun ◽  
Hongna Huo ◽  
Xiaoliang Ren ◽  
...  
Keyword(s):  
High Performance ◽  
Water Solubility ◽  
Extraction Efficiency ◽  
Cerebrovascular Diseases ◽  
Water Soluble ◽  
Cyclodextrin Derivatives ◽  
Treatment And Prevention ◽  
Promising Application ◽  
Sulfobutyl Ether ◽  
Processed Products

Puerariae Lobatae Radix (PLR), a well-known herbal medicine, is the root of Pueraria lobata (Willd.) Ohwi and has been employed for the treatment and prevention of cardiovascular and cerebrovascular diseases. The purpose of this study was to compare the associated-extraction efficiency of six cyclodextrins (CDs) on five flavonoids in PLR, namely puerarin, daidzein, daidzin, genistein and genistin, which are the major secondary metabolites, and exhibit low water solubility. The six CDs applied were β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD), hydroxypropyl-γ-cyclodextrin (HP-γ-CD), carboxymethyl-β-cyclodextrin (CM-β-CD), and sulfobutyl ether β-cyclodextrin (SBE-β-CD). They can be grouped into one of the following three categories: traditional cyclodextrins (β-CD and γ-CD), water-soluble cyclodextrin derivatives (HP-β-CD and HP-γ-CD) and ionic cyclodextrin derivatives (SBE-β-CD and CM-β-CD). High-performance liquid chromatography (HPLC) was used to analyze the five flavonoids in the original aqueous extracts (OAE) in the presence or absence of various CDs. The associated-extraction efficiency of the various CDs followed the ranking: SBE-β-CD > HP-β-CD > CM-β-CD > HP-γ-CD > γ-CD > β-CD. It was clear that SBE-β-CD presented the highest associated-extraction capability, and it was used to extract the four flavonoids from three PLR products, including raw product, stir- fried product, and product simmered with wheat bran. The results showed that SBE-β-CD could improve the extraction capability of flavonoids, both from the raw product and in processed products of PLR. In conclusion, CDs, especially SBE-β-CD, have a promising application for the associated-extraction of flavonoids from PLR.

Sign in / Sign up

Export Citation Format

Share Document