scholarly journals Formation of Ketoprofen-Malonic Acid Cocrystal by Solvent Evaporation Method

2017 ◽  
Vol 17 (2) ◽  
pp. 161 ◽  
Author(s):  
Yudi Wicaksono ◽  
Dwi Setyawan ◽  
Siswandono Siswandono
Keyword(s):  
Phase Diagram ◽  
Liquid Phase ◽  
Malonic Acid ◽  
Solvent Evaporation ◽  
Stoichiometric Ratio ◽  
Solvent Evaporation Method ◽  
Sem Images ◽  
Pxrd Pattern ◽  
Evaporation Method ◽  
Solid Liquid

The purpose of this work was to explore the formation of ketoprofen-malonic acid cocrystal by solvent evaporation method. Early detection of cocrystal formation was conducted by hot stage microscopy and solid-liquid phase diagram. Cocrystal were prepared by solvent evaporation method by using isopropyl alcohol as solvent. Characterization of cocrystal was done by Powder X-Ray Diffractometry (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) Spectroscopy and Scanning Electron Microscopy (SEM). The results of hot stage microscopic and solid-liquid phase diagram indicated formation of ketoprofen-malonic acid cocrystal. PXRD and DSC measurements showed stoichiometric ratio of cocrystal ketoprofen-malonic acid (2:1). The ketoprofen-malonic acid cocrystal had melting point at 86.2 °C and unique peaks of PXRD pattern at 2θ of 6.1°, 17.8°, 23.2° and 28.6°. FTIR spectra indicated the formation of cocrystal due to interaction of C=O ketone group of ketoprofen with MA molecule. SEM images show that ketoprofen-malonic acid cocrystal have multi-shaped particles with rough surfaces.

Solid/Liquid Phase Diagram of the Ammonium Sulfate/Malonic Acid/Water System

2010 ◽  
Vol 114 (12) ◽  
pp. 4282-4288 ◽  
Author(s):  
Keith D. Beyer ◽  
Jason Schroeder ◽  
Benjamin Palet
Keyword(s):  
Phase Diagram ◽  
Liquid Phase ◽  
Ammonium Sulfate ◽  
Malonic Acid ◽  
Water System ◽  
Acid Water ◽  
Solid Liquid

scholarly journals Improvement in vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

2018 ◽  
Vol 18 (3) ◽  
pp. 531 ◽  
Author(s):  
Dwi Setyawan ◽  
Sukma Adhi Permata ◽  
Ahmad Zainul ◽  
Maria Lucia Ardhani Dwi Lestari
Keyword(s):  
Dissolution Rate ◽  
Malonic Acid ◽  
Fourier Transforms ◽  
Solvent Evaporation ◽  
Physical Mixture ◽  
Original Position ◽  
In Vitro Dissolution ◽  
Solvent Evaporation Method ◽  
Evaporation Method

The aim of the study was to improve the in-vitro dissolution rate of quercetin (Qu) using cocrystallization of quercetin. Cocrystals of quercetin (Co Qu) were produced with malonic acid (Ma) as coformer at ratio 1:2 using solvent evaporation method. Cocrystals quercetin-malonic acid (Co Qu-Ma) was characterized using Differential Thermal Analysis (DTA), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), and Fourier Transforms Infrared Spectrophotometer (FTIR) and in-vitro dissolution study. A new endothermic peak at 277.9 °C was shown from the thermogram. Diffractogram of Co Qu-Ma showed a new diffraction peak at 2θ 9.81, 12.99, and 19.80°. Microphotograph showed that Qu and Ma exhibited a columnar-shaped and a pebble-shaped crystal, respectively, and FTIR wavenumber of O-H functional group of quercetin was shifted from its original position at 3411 to 3428 cm-1 in the physical mixture (pm) of Qu-Ma and 3418 cm-1 in Co Qu-Ma, respectively. The physicochemical characterizations using DTA, PXRD, SEM and FTIR indicated that Co Qu-Ma were successfully obtained through solvent evaporation method. The in-vitro dissolution rate of Co Qu-Ma was 95.30% at 60 min. Cocrystals effectively increased dissolution rate and dissolution efficiency in comparison to the pure quercetin and physical mixture of quercetin-malonic acid.

scholarly journals Identification of Physical Interaction in Binary Systems of Acyclovir – Succinic Acid

2017 ◽  
Vol 3 (1) ◽  
pp. 27
Author(s):  
Agnes Nuniek Winanta ◽  
Dwi Setyawan ◽  
Siswandono
Keyword(s):  
Succinic Acid ◽  
Binary Systems ◽  
Antiviral Drug ◽  
Solvent Evaporation ◽  
Crystal Habit ◽  
Physical Interaction ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Pxrd Pattern ◽  
Evaporation Method

Background: Acyclovir, a guanosine analogue antiviral drug with low solubility of water. Due to its poor solubility and permeability, causes low oral bioavailability. Objective: The aim of this research is to investigate the physical interaction in binary systems acyclovir-succinic acid (AS). Methods: The msystem was prepared by solvent evaporation method. Results: Thermogram Differential Scanning Calorimetry showed endothermic peaks at 172.68oC (ethanol) and 171.84oC (methanol). The Powder X-Ray Diffraction (PXRD) pattern of AS was different from pure component and physical mixtures. Furthermore, physical characterization showed the binary system of AS have unique crystal habit by polarization microscope. Conclusion: New crystalline phase is formed from the interaction between acyclovir and succinic acid by solvent evaporation method using ethanol and methanol.  

scholarly journals Identification of Physical Interaction in Binary Systems of Acyclovir – Succinic Acid

2017 ◽  
Vol 3 (1) ◽  
pp. 27
Author(s):  
Agnes Nuniek Winanta ◽  
Dwi Setyawan ◽  
Siswandono
Keyword(s):  
Succinic Acid ◽  
Binary Systems ◽  
Antiviral Drug ◽  
Solvent Evaporation ◽  
Crystal Habit ◽  
Physical Interaction ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Pxrd Pattern ◽  
Evaporation Method

Background: Acyclovir, a guanosine analogue antiviral drug with low solubility of water. Due to its poor solubility and permeability, causes low oral bioavailability. Objective: The aim of this research is to investigate the physical interaction in binary systems acyclovir-succinic acid (AS). Methods: The msystem was prepared by solvent evaporation method. Results: Thermogram Differential Scanning Calorimetry showed endothermic peaks at 172.68oC (ethanol) and 171.84oC (methanol). The Powder X-Ray Diffraction (PXRD) pattern of AS was different from pure component and physical mixtures. Furthermore, physical characterization showed the binary system of AS have unique crystal habit by polarization microscope. Conclusion: New crystalline phase is formed from the interaction between acyclovir and succinic acid by solvent evaporation method using ethanol and methanol.  

Glibenclamide-Nicotinamide Cocrystals Synthesized by The Solvent Evaporation Method to Enhance Solubility and Dissolution Rate of Glibenclamide

2019 ◽  
Vol 9 (01) ◽  
pp. 21-26
Author(s):  
Arif Budiman ◽  
Ayu Apriliani ◽  
Tazyinul Qoriah ◽  
Sandra Megantara
Keyword(s):  
Solvent Evaporation ◽  
Physical Mixture ◽  
Dissolution Profile ◽  
Solvent Evaporation Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Dissolution Properties ◽  
Mixture Characterization

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture

Preparation and Evaluation of Glipizide Tablets Containing both Enhanced and Sustained Release Solid Dispersions

1970 ◽  
Vol 2 (4) ◽  
pp. 714-725
Author(s):  
Adel M. Aly ◽  
Ahmed S. Ali
Keyword(s):  
Blood Glucose ◽  
Blood Glucose Level ◽  
Glucose Level ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vivo Studies ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Tablet Formulations

: Glipizide (GZ) is an oral blood-glucose-lowering drug of the sulfonylurea class characterized by its poor aqueous solubility. Aiming for the production of GZ tablets with rapid onset of action followed by prolonged effect; GZ-Polyethylene glycol (PEG 4000 and 6000) solid dispersions with different ratios, (using melting and solvent evaporation method), as well as, coprecipitate containing GZ with polymethyl-methacrylate (PMMA) were prepared. Four tablet formulations were prepared containing; a) GZ alone, b) GZ: PEG6000, 1:10, c) GZ:PMMA 1:3, and, d)both GZ:PEG6000 1:10 and GZ:PMMA 1:3. The solvent evaporation method showed more enhancement of GZ solubility than the melting one, and this solubilizing effect increased with PEG increment. Generally, PEG6000 showed more enhancement of dissolution than PEG4000 especially at 1:10 drug: polymer ratio (the most enhancing formula). Also, the prepared tablet formulations showed acceptable physical properties according to USP/NF requirements. The dissolution results revealed that tablets containing PEG6000 (1:10) have the most rapid release rate, followed by the formula containing both PEG6000 and PMMA, while that including PMMA alone showed the slowest dissolution rate. Moreover, In-vivo studies for each of the above four formulations, were performed using four mice groups. The most effective formula in decreasing the blood glucose level, through the first 6 hours, was that containing GZ and PEG6000, 1:10. However, formula containing the combination of enhanced and sustained GZ was the most effective in decreasing the blood glucose level through 16 hours. Successful in-vitro in-vivo correlations could be detected between the percent released and the percent decreasing of blood glucose level after 0.5 hours.

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

Sign in / Sign up

Export Citation Format

Share Document