scholarly journals SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE-ASPARTAME COCRYSTAL USING THE SOLVENT EVAPORATION METHOD TO INCREASE THE SOLUBILITY OF GLIBENCLAMIDE

2019 ◽  
pp. 150-154
Author(s):  
ARIF BUDIMAN ◽  
SANDRA MEGANTARA ◽  
AYU APRILIANI
Keyword(s):  
Hydrogen Bonding ◽  
Dissolution Rate ◽  
In Silico ◽  
Active Pharmaceutical Ingredient ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Rate Test ◽  
Ft Ir

Objective: The solubility of a drug in water plays an important role in the absorption of the drug after oral administration. Cocrystal is one method that improves the solubility of the active pharmaceutical ingredient (API). The aim of this study was to investigate the formation of a glibenclamide (GCM)-aspartame (APM) cocrystal using the solvent evaporation method and to evaluate its solubility and dissolution rate. Methods: Molecular docking of the GCM-APM cocrystal was observed using an in silico method. The GCM-APM cocrystal (1:2) was prepared by using the solvent evaporation method. The cocrystal of GCM-APM was evaluated by the saturated solubility test and the dissolution rate test (USP type 2 apparatus). The solvent evaporation product of GCM-APM was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). Results: In silico study showed that the interaction of GCM-APM has hydrogen bonding and the potential to improve the solubility of GCM. Evaluation of the cocrystal of GCM-APM showed that the solubility and dissolution rate of the cocrystal are significantly increased. Characterization of FT-IR showed that no chemical reaction occurred in the GCM-APM cocrystal. The DSC analysis showed the changes in the melting point of GCM. Measurement of PXRD showed the formation of a new solid crystal phase that is different from GCM and APM. Conclusion: GCM-APM has hydrogen bonding can improve the solubility and dissolution rate of GCM.

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Dissolution Rate ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Solubility Study ◽  
Sodium Caprylate

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.

Characterization, Physical Stability, and Dissolution Behavior of Naringenin / Mannitol Solid Dispersions Prepared by Solvent Evaporation Method with Three Drying Methods

2011 ◽  
Vol 236-238 ◽  
pp. 2264-2272
Author(s):  
Guang Fa Wang ◽  
Chun Lan Dai ◽  
Zheng Gen Liao ◽  
Guo Wei Zhao ◽  
Xin Li Liang ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physical Stability ◽  
Solvent Evaporation ◽  
Vacuum Drying ◽  
Dissolution Behavior ◽  
Drying Methods ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Ft Ir

Solid dispersions (SD) were prepared with naringenin and mannitol by the solvent evaporation method with three drying methods (vacuum drying, VD; microwave-vacuum drying, MVD; and spray drying, SPD). The SD was characterized by Differential Scanning Calorimetry (DSC), Powder X-ray Diffractometry (PXRD), Scanning Electronic Microscope (SEM), and Fourier Transform Infrared Spectroscopy (FT-IR).In vitrodissolution of naringenin and physical stability was investigated, and the energy consumption of different processing methods was measured. The results showed that the vitro dissolution rate and extent of naringenin was significantly improved by SD prepared with different drying methods compared to that of the pure drug and physical mixture (PM), and the dissolution rate of SD-SPD and SD-MVD was much higher than the SD-VD. The results of FT-IR showed that naringenin is possibly interacted with mannitol via intermolecular hydrogen bond; The PXRD showed that the crystallinity of the SD prepared with three drying methods was reduced sharply as compared with pure naringenin and PM. There results showed that the physical state of SD-MVD was more stable than SD-SPD and SD-VD that stored in the 40 °C/75% RH chamber in three month. Compared with other drying methods, the MVD method can save time and energy. These results suggest that MVD is feasible to replace the traditional time-consuming and low efficiency drying procedure for preparation of solid dispersions.

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

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.

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 Co-crystallization of quercetin and isonicotinamide using solvent evaporation method

2021 ◽  
Vol 18 (4) ◽  
pp. 697-702
Author(s):  
Budipratiwi Wisudyaningsih ◽  
Dwi Setyawan ◽  
Siswandono
Keyword(s):  
Minimum Energy ◽  
Solvent Evaporation ◽  
Crystal Habit ◽  
In Vitro Dissolution ◽  
Molar Ratio ◽  
Dissolution Profile ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method

Purpose: To obtain quercetin-isonicotinamide co-crystal (CQINA) with improved physicochemical and in-vitro dissolution characteristics. Methods: Co-crystallization of quercetin (Q) and isonicotinamide (INA) in molar ratio of 1:1 was performed using solvent evaporation method with the addition of 50 mL of ethanol (99.9%, v/v). The resultant solution was thoroughly mixed and stirred at room temperature for 48 h to slowly evaporate the solvent until CQINA was obtained. The co-crystal phase was characterized using differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), scanning electron microscopy (SEM), and fourier transform infrared (FTIR) spectroscopy. In-vitro dissolution was performed by USP method II in 900 mL citrate buffer (pH 5.0 ± 0.05), with stirring at 100 rpm and at 37 ± 0.5 °C. Results: Computational approach predicted the formation of hydrogen bonds between Q and coformers used, and the interaction involved minimum energy. In CQINA thermogram, a new endothermic peak was formed with a melting point of 255.26 °C, while Q (314.85 °C) and INA (156.62 °C). Images from DSC, PXRD, SEM and FTIR showed that the crystal habits and morphologies of the CQINA differed from those of the original components. There was an improvement in the dissolution profile of CQINA, when compared with those of the original components. Conclusion: Q and INA subjected to solvent evaporation result in the formation of a CQINA with different crystal habit, which possess physicochemical characteristics different from those of its constituents. Modification of Q crystals in CQINA increases its in vitro dissolution, making it a potential pharmaceutical agent.

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 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.

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