Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

scholarly journals Preparation and Characterization of a Novel Cocrystal of Atorvastatin Calcium with Succinic Acid Coformer

2019 ◽  
Vol 19 (3) ◽  
pp. 660
Author(s):  
Yudi Wicaksono ◽  
Dwi Setyawan ◽  
Siswandono Siswandono ◽  
Tri Agus Siswoyo
Keyword(s):  
Succinic Acid ◽  
Dissolution Rate ◽  
Intermolecular Hydrogen Bond ◽  
Acid Amide ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Atorvastatin Calcium ◽  
Hydrogen Bond Interactions

Preparation and characterization of a novel cocrystal of atorvastatin calcium with succinic acid coformer were successfully performed. This research aims to modify the crystalline form of atorvastatin calcium through cocrystallization with succinic acid coformer. The cocrystal was prepared by a solvent evaporation method and characterized by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The atorvastatin calcium-succinic acid cocrystal has new crystalline peaks at 2θ of 12.9, 18.2 and 26.7° indicating the formation of a new crystalline phase. The cocrystal showed the melting point at 205.7 °C with an enthalpy of fusion 30.2 J/g which is different from the initial components. The FTIR spectra of cocrystal showed the shifting of absorption peaks of groups of initial components indicating of formation of atorvastatin calcium-succinic acid cocrystal through acid–amide intermolecular hydrogen bond interactions. The solubility and dissolution test showed that the cocrystal has solubility and dissolution rate significantly higher than the solubility and dissolution rate of pure atorvastatin calcium.

scholarly journals ENHANCEMENT OF GLIBENCLAMIDE DISSOLUTION RATE BY SOLID DISPERSION METHOD USING HPMC AND PVP

2019 ◽  
pp. 19-24 ◽  
Author(s):  
ARIF BUDIMAN ◽  
IYAN SOPYAN ◽  
DENIA SEPTY RIYANDI
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Rate Test ◽  
Ft Ir

Objective: The aim of this study was to investigate the effects of changing in the proportions of the solid dispersion formula on the dissolution rate of glibenclamide. Methods: Solid dispersions were prepared by solvent evaporation method by using methanol as solvent, hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as polymers. The prepared product was evaluated by the saturated solubility test and the dissolution rate test. The prepared product was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) and Scanning Electron Microscopy (SEM). Results: The result showed solid dispersion with a ratio of glibenclamide: PVP: HPMC (1: 3: 6) has the highest increase in solubility (20 fold) compared to pure glibenclamide. This formula also showed an improvement in dissolution rate from 19.9±1.19% (pure glibenclamide) to 99±1.60% in 60 min. Characterization of FT-IR showed that no chemical reaction occurred in solid dispersion of glibenclamide. The results of X-ray diffraction analysis showed an amorphous form in all solid dispersion formulas. The results of DSC analysis showed that endothermic peak melting point of solid dispersion occurred, and the morphology of solid dispersion was more irregular than pure glibenclamide based on SEM characterization Conclusion: The solid dispersion of glibenclamide using PVP: HPMC as carriers can increase the solubility and dissolution rate compared to pure glibenclamide.

Preparation and Characterization of Tea Polyphenols/Starch Inclusion Complex

2013 ◽  
Vol 432 ◽  
pp. 413-417 ◽  
Author(s):  
Li Ming Zhang ◽  
Zhi Ying Hu ◽  
Li Hu Yan ◽  
Run Liu Li ◽  
Cheng Wei Cao ◽  
...  
Keyword(s):  
Differential Scanning Calorimetry ◽  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Tea Polyphenols ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
The Stability ◽  
Good Retention

In order to improving the stability and bioavailability of tea polyphenols (TP), the TP/starchinclusion complex(TPSIC) was prepared by adding TP to starch slurry during gelatinization, and its TPreleasing behaviorswas investigated. The formation of inclusion complex was confirmed by powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The TPSIC showed a characteristic of V-type crystallinity and a looser gel matrix. The encapsulation increased the stability of TP and generated a good releasing behavior after enzymatic erosion. The lower releasing rate indicated that the prepared inclusion complexes had good retention ability and effectively reduced the releasing rate of TP. The releasing rate of TPSIC increased with the increase of TP concentration.

scholarly journals Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

2019 ◽  
Vol 9 (4) ◽  
pp. 559-570 ◽  
Author(s):  
Reham Al-Kazemi ◽  
Yacoub Al-Basarah ◽  
Aly Nada
Keyword(s):  
Dissolution Rate ◽  
Dissolution Enhancement ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Atorvastatin Calcium ◽  
Molar Ratios ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
Physical Mixtures ◽  
Biopharmaceutical Classification System

Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) bycocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of thedrug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expectedto enhance the bioavailability.Methods: Two methods were used for preparing the cocrystals, solvent drop grinding (SDG) andsolvent evaporation (SE) method using 1:1, 1:3, and 1:10 drug-coformer molar ratios. Glucosaminehydrochloride (GluN) and nicotinamide (NIC) were investigated as coformers. The cocrystals,their physical mixtures, and the raw ATC were characterized by fourier transform infrared (FTIRspectroscopy), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), massspectroscopy (MS), scanning electron microscopy (SEM), solubility, and dissolution rate studies.Results: SDG and SE were effective in improving the dissolution rate of ATC with both coformers.Drug: coformer ratio 1:3 was optimum. The solubility values for ATC, GluN-, and NIC-cocrystals were26, to 35 and 50 μg/mL, respectively. The dissolution rate of ATC from cocrystals was > 90% after 5minutes, compared to 41% untreated ATC.Conclusion: Cocrystallization significantly improved the solubility and dissolution, in comparison tothe untreated ATC.<br />

scholarly journals Enhancement of solubility and dissolution rate of poorly water soluble raloxifene using microwave induced fusion method

2013 ◽  
Vol 49 (3) ◽  
pp. 571-578 ◽  
Author(s):  
Payal Hasmukhlal Patil ◽  
Veena Sailendra Belgamwar ◽  
Pratibha Ramratan Patil ◽  
Sanjay Javerilal Surana
Keyword(s):  
Dissolution Rate ◽  
Hydroxypropyl Methylcellulose ◽  
Microwave Treatment ◽  
Water Soluble ◽  
Fusion Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Wetting Properties ◽  
Poorly Soluble ◽  
Poorly Water Soluble

The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and efficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased significantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased significantly when an SD of the drug is prepared using the microwave-induced fusion method.

Characterization of New Nonstoichiometric Ferroelectric (Li0.95Cu0.15)Ta0.76Nb0.19O3 and Comparative Study With (Li0.95Cu0.15)Ta0.57Nb0.38O3 as Photocatalysts in Microbial Fuel Cells

2018 ◽  
Vol 16 (2) ◽  
Author(s):  
S. Louki ◽  
N. Touach ◽  
A. Benzaouak ◽  
V. M. Ortiz-Martínez ◽  
M. J. Salar-García ◽  
...  
Keyword(s):  
Power Density ◽  
Microbial Fuel Cells ◽  
Removal Rate ◽  
Oxygen Demand ◽  
Ferroelectric Material ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Uv Visible

This work investigates the photocatalytic activity of new ferroelectric material with formula (Li0.95Cu0.15)Ta0.76Nb0.19O3 (LT76) in a single chamber microbial fuel cell (MFC) and compares its performance with the similar photocatalyst (Li0.95Cu0.15)Ta0.57Nb0.38O3 (LT57). The photocatalysts LT76 and LT57 were synthesized by ceramic route under the same conditions, with the same starting materials. The ratio Ta/Nb was fixed at 4.0 and 1.5 for LT76 and LT57, respectively. These phases were characterized by different techniques including X-ray diffraction (XRD), transmission electronic microscopy (TEM), particle size distribution (PSD), differential scanning calorimetry (DSC), and ultraviolet (UV)–visible (Vis). The new photocatalyst LT76 presents specific surface area of 0.791 m2/g and Curie temperature of 1197 °C. The photocatalytic efficiency of this material is assessed in terms of wastewater treatment and electricity generation by power density and removal rate of chemical oxygen demand (COD) in the presence of a light source. The values of maximum power density and COD removal were 19.77 mW/m3 and 93%, respectively, for LT76.

scholarly journals Stacking Control by Molecular Symmetry of Sterically Protected Phthalocyanines

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5552
Author(s):  
Ryota Kudo ◽  
Masahiro Sonobe ◽  
Yoshiaki Chino ◽  
Yu Kitazawa ◽  
Mutsumi Kimura
Keyword(s):  
Lamellar Structure ◽  
Synthesis And Characterization ◽  
Molecular Symmetry ◽  
X Ray Diffraction ◽  
Melting Points ◽  
Scanning Calorimetry ◽  
Structural Isomers ◽  
X Ray ◽  
Temperature Controlled

The synthesis and characterization of two phthalocyanine (Pc) structural isomers, 1 and 2, in which four 2,6-di(hexyloxy)phenyl units were attached directly to the 1,8,15,22- or 1,4,15,18-positions of the Pc rings, are described. Both Pcs 1 and 2 exhibited low melting points, i.e., 120 and 130 °C respectively, due to the reduction in intermolecular π-π interaction among the Pc rings caused by the steric hindrance of 2,6-dihexyloxybenzene units. The thermal behaviors were investigated with temperature-controlled polarizing optical microscopy, differential scanning calorimetry, powder X-ray diffraction, and absorption spectral analyses. Pc 1, having C4h molecular symmetry, organized into a lamellar structure containing lateral assemblies of Pc rings. In contrast, the other Pc 2 revealed the formation of metastable crystalline phases, including disordered stacks of Pcs due to rapid cooling from a melted liquid.

scholarly journals Perbaikan Kelarutan Albendazol Melalui Pembentukan Kristal Multikomponen dengan Asam Malat

2020 ◽  
Vol 6 (1) ◽  
pp. 114-123
Author(s):  
Fikri Alatas ◽  
Fahmi Abdul Azizsidiq ◽  
Titta Hartyana Sutarna ◽  
Hestyari Ratih ◽  
Sundani Nurono Soewandhi
Keyword(s):  
Phase Solubility ◽  
Crystal Formation ◽  
Solubility Curve ◽  
X Ray Diffraction ◽  
Ethanol Mixture ◽  
X Ray ◽  
Grinding Method ◽  
Diffraction Patterns ◽  
Phase Solubility Curve

An effort to improve the solubility of albendazole (ABZ), an anthelmintic drug has been successfully carried out through the formation of multicomponent crystal with dl-malic acid (MAL). Construction of phase solubility curve of ABZ in MAL solution and crystal morphological observations after recrystallization in the acetone-ethanol (9:1) mixture were performed for initial prediction of multicomponent crystal formation. ABZ-MAL multicomponent crystal was prepared by wet grinding or also known as solvent-drop grinding (SDG) with acetone-ethanol (9:1) mixture as a solvent followed by characterization of the multicomponent crystal formation by powder X-ray diffraction and Fourier transform infrared (FTIR) methods. The solubility of ABZ-MAL multicomponent crystal was tested in water at ambient temperature and in pH 1.2, 4.5 and 6.8 of buffered solutions at 37°C. The phase solubility curve of the ABZ in the MAL solution showed type Bs. The ABZ-MAL mixture has a different crystalline morphology than pure ABZ and MAL after recrystallization in the acetone-ethanol mixture (9:1). The powder X-ray diffraction pattern and the FTIR spectrum of ABZ-MAL from SDG different from intact ABZ and MAL powder X-ray diffraction patterns and these results can indicate the ABZ-MAL multicomponent crystal formation. The ABZ-MAL multicomponent crystal has better solubility than pure ABZ in all media used. These results can be concluded that ABZ-MAL multicomponent crystal can be prepared by solvent-drop grinding method with acetone-ethanol (9:1) mixture as a solvent and can increase the solubility of albendazole.

scholarly journals Characterization of the Interface Between the Bulk Glass Forming Alloy Zr41Ti14Cu12Ni10Be23 with Pure Metals and Ceramics

2000 ◽  
Vol 15 (7) ◽  
pp. 1617-1621 ◽  
Author(s):  
Jan Schroers ◽  
Konrad Samwer ◽  
Frigyes Szuecs ◽  
William L. Johnson
Keyword(s):  
Sessile Drop ◽  
Bulk Glass ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Glass Forming ◽  
Processing Times ◽  
Thermal Stability Of

The reaction of the bulk glass forming alloy Zr41Ti14Cu12Ni10Be23 (Vit 1) with W, Ta, Mo, AlN, Al2O3, Si, graphite, and amorphous carbon was investigated. Vit 1 samples were melted and subsequently solidified after different processing times on discs of the different materials. Sessile drop examinations of the macroscopic wetting of Vit 1 on the discs as a function of temperature were carried out in situ with a digital optical camera. The reactions at the interfaces between the Vit 1 sample and the different disc materials were investigated with an electron microprobe. The structure and thermal stability of the processed Vit 1 samples were examined by x-ray diffraction and differential scanning calorimetry. The results are discussed in terms of possible applications for composite materials.

scholarly journals SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE WITH INCREASING THE SOLUBILITY AND DISSOLUTION RATE USING COCRYSTALLIZATION

2018 ◽  
Vol 10 (6) ◽  
pp. 181
Author(s):  
Arif Budiman ◽  
Sandra Megantara ◽  
Putri Raraswati ◽  
Tazyinul Qoriah
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Crystallization Process ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Infra Red ◽  
Form Development

Objective: The aim of this study was to develop a solid dosage form of glibenclamide with increasing the solubility properties of glibenclamide with cocrystallization method.Methods: Virtual screening was performed to investigate the interaction between glibenclamide and a co-former. Saccharin, the selected co-former, then co-crystallized with glibenclamide with equimolar ratios of 1:1 and 1:2 using the solvent evaporation method. Further characterization was performed using an infra-red (IR) spectrophotometer, differential scanning calorimetry (DSC), and powder x-ray diffraction (PXRD).Results: Co-crystals of 1:2 equimolar ratio were more highly soluble compared to pure glibenclamide (30-fold for 12 h and 24-fold for 24 h). The dissolution rate had also increased from 46.838% of pure glibenclamide to 77.655% of glibenclamide co-crystal in 60 min. There was no chemical reaction observed during the co-crystallization process based on the IR spectrum. However, there was a new peak in the X-Ray diffractogram and a reduction of melting point in the DSC curve, indicating the formation of co-crystals.Conclusion: The optimal co-crystal ratio of glibenclamide-saccharin was found to be 1:2, which was successful in improving the solubility of glibenclamide.

Sign in / Sign up

Export Citation Format

Share Document