scholarly journals PREPARATION OF ACYCLOVIR-ISONICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION METHOD WITH METHANOL AND ISOPROPANOL

2020 ◽  
Vol 21 (3) ◽  
pp. 109
Author(s):  
Agnes Nuniek Winantari ◽  
Roisah Nawatila ◽  
Cecilia Jocelyn
Keyword(s):  
Herpes Simplex ◽  
Water Solubility ◽  
Parent Drug ◽  
Solvent Evaporation ◽  
Synthetic Analog ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Varicella Zoster ◽  
Ft Ir ◽  
Simplex Virus

PREPARATION OF ACYCLOVIR-ISONICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION METHOD WITH METHANOL AND ISOPROPANOL. Acyclovir is a nucleoside synthetic analog antiviral group used in the treatment of Herpes simplex virus (HSV-1 & HSV-2) and Varicella zoster virus (VZV). Acyclovir has low water solubility, so it needs to be modified in the form of cocrystal with isonicotinamide. This study aims to obtain the physical characteristics produced by acyclovir-isonicotinamide cocrystal (1:1) made through the solvent evaporation method with methanol and isopropanol. The crystalline formed is characterized by DSC, PXRD, FT-IR and SEM. The characterization results showed the presence of new crystals that formed between acyclovir-isonicotinamide in methanol and isopropanol solvents. Thermograms showed sharp exothermic peaks at 183.31°C and 186.24°C. The diffractogram showed a new peak at 2θ = 5.19 and 5.82. The spectrum showed a shift in wavelength in the cocrystal formed. The cocrystal has a different morphology compared with parent drug and coformer on analysis using SEM. This research shows that acyclovir can form cocrystal with isonicotinamide by solvent evaporation method with methanol and isopropanol.

scholarly journals Water Solubility Enhancement of Atorvastatin by Solid Dispersion Method

1970 ◽  
Vol 3 (2) ◽  
pp. 43-46
Author(s):  
Riaz Uddin ◽  
Farzana Ali ◽  
Subrata Kumar Biswas
Keyword(s):  
Key Words ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Dispersion Method ◽  
Evaporation Method

Key Words: Solid dispersions; solvent evaporation method; atorvastatin; HPMCDOI: http://dx.doi.org/10.3329/sjps.v3i2.8036 S.J. Pharm. Sci 3(2): 43-46

scholarly journals Nanocrystallization of the Pharmaceutically Active Agent Genipin by an Emulsion Solvent Evaporation Method

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Yuangang Zu ◽  
Xinyang Yu ◽  
Xiuhua Zhao ◽  
Weiguo Wang ◽  
Kunlun Wang
Keyword(s):  
Water Solubility ◽  
Oral Absorption ◽  
Active Agent ◽  
Solvent Evaporation ◽  
Single Factor ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Experimental Parameters ◽  
Drug Purity ◽  
Solvent Residue

To improve the water solubility and dissolution rate, genipin was nanocrystallized by an emulsion solvent evaporation method, followed by freeze-drying. The optimization condition of nanocrystallization process was carried out by single-factor experiment. The effects of five experimental parameters, such as concentration of surfactants the proportion of water to organic phase, homogenate speed and time, homogenization pressure and times, and the proportion of genipin to lyoprotectants on the mean particle size (MPS) of genipin nanoparticles, were investigated. Under the optimum conditions by single-factor experiments, genipin nanoparticles with an MPS of 59.8 nm were obtained. The genipin nanoparticles were characterized by SEM, FTIR, XRD, DSC, solvent residue, drug purity test, dissolution testing, and bioavailability analysis. The analysis results indicated that the chemical structure of genipin nanoparticles was unchanged, but the crystallinity was reduced. The solubility of genipin nanoparticles was 9.05 times of the raw drug. In addition, the residual amounts of chloroform and ethanol were separately less than the ICH limit for class II, and the oral bioavailability of the genipin nanoparticles powder was 7.99 times of raw genipin. According to the results above, genipin nanoparticles show the potential application value of its oral absorption.

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.

BINARY COMPLEXES OF GLIMEPIRIDE WITH Β-CYCLODEXTRIN FOR IMPROVED SOLUBILITY AND DRUG DELIVERY

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 54-60
Author(s):  
L Adhikari ◽  
M. Semalty ◽  
P. S Naruka ◽  
V. K Aswal ◽  
A Semalty ◽  
...  
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Molar Ratio ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Kneading Method ◽  
Ft Ir

Cyclodextrin complexation is a one of the most investigated techniques of solubility and dissolution enhancement of drugs. In the present study, a poorly water soluble drug glimepiride, was complexed with β-cyclodextrin (βCD) with the aim of improving water solubility and drug dissolution. The complexes were prepared using two different methods (solvent evaporation and kneading) and then characterized by Fourier-transform infrared spectroscopy (FT-IR), powder x-ray diffractometry (X-RD), thermal analysis (DSC),scanning electron microscopy and in-vitro dissolution study. The phase solubility study revealed the most suitable ratio of drug to β CD (1:4 molar ratio). Analysis of various physical and pharmacokinetic parameters for the complex prepared by solvent evaporation method showed better drug content, solubility and drug release profile in comparison to the complex prepared by the kneading method. The complex prepared with solvent evaporation method showed better drug release as compared with that of kneading method and the pure drug. The FT-IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:βCD molar ratio) using solvent evaporation method showed the better improvement in solubility and drug dissolution.

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.

Facile Preparation of Polylactic Acid/Ketoconazole Composite Microspheres by Oil/Water Solvent Evaporation Method

2013 ◽  
Vol 652-654 ◽  
pp. 335-338 ◽  
Author(s):  
Yan Hong Zhang ◽  
Yan Wang ◽  
Xian Chao Kong ◽  
Qian Ke Cheng ◽  
Xi Yuan Yang ◽  
...  
Keyword(s):  
Polylactic Acid ◽  
Solvent Evaporation ◽  
Thermal Decomposition Mechanism ◽  
Solvent Evaporation Method ◽  
X Ray Diffraction ◽  
Evaporation Method ◽  
Composite Microspheres ◽  
Water Solvent ◽  
Ft Ir ◽  
Oil Water

In this study, polylactic acid(PLA)/ketoconazole(KCZ) composite microspheres were prepared by oil/water solvent evaporation method. Those drug-loaded microspheres were characterized in morphology using the scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FT-IR) was used to determine the chemical functional groups in the sample and to analysis whether a chemical reaction occured between PLA and KCZ. The thermogravimetric spectra of PLA and PLA/KCZ microspheres were used to analyse the influence of KCZ on the thermal decomposition mechanism of PLA. Crystallinities of the KCZ and PLA/KCZ were analyzed by X-ray diffraction analysis (XRD).

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.

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