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.

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 FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLET OF MELOXICAM USING NATURAL SUPERDISINTEGRANTS

2020 ◽  
pp. 197-203
Author(s):  
CHETAN V PAWAR ◽  
SWATI S MUTHA ◽  
SAGAR V BHISE ◽  
PAYAL D BORAWAKE
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Taste Masking ◽  
Lauryl Sulfate ◽  
Solvent Evaporation Method ◽  
Powder Preparation ◽  
Dispersion Method ◽  
Evaporation Method

Objective: The objective of the present work was the preparation and evaluation of mouth dissolving tablets (MDTs) of meloxicam using natural superdisintegrants. Methods: Meloxicam is BCS Class II (low soluble, and high permeable) drug increasing the dissolution properties of the poorly water-soluble drug meloxicam using a solid dispersion method (solvent evaporation method). Solvent evaporation method using drug and carrier as polyethylene glycol (PEG)-6000 and PEG-15,000 the ratio of 1:1, 1:2 (drug:carrier), and acetone as solvent. In house prepared banana powder were used as natural superdisintegrant. Manufacturing of MDT was done by the direct compression method. In this MDTs, various excipients were used such as mannitol used as the diluent, sodium saccharin used as a sweetening agent, Avicel pH-102 used as a binding agent, and talc and sodium lauryl sulfate (SLS) used as lubricant and glidant. The best formula of the tablet was selected according to the disintegration time (DT) and friability tests. Results: The results have shown that an increase in the meloxicam solubility was obtained using solid dispersion with the solvent evaporation method using PEG-15000 as a carrier in the ratio of 1:2 (drug:carrier). Taste masking was also done by a solid dispersion method. Tablet prepared with in house prepared banana powder gave less DT (70 s) as compared to tablet prepared with branded banana powder (80 s), but formulation F5 failed in friability testing. Improved strength of tablet obtained using SLS (<1%) also showed an increase in the dissolution performance of the tablet in formulation F6. This F6 formulation having 10% natural super disintegrating agent (in house prepared banana powder) has shown 99% cumulative drug release within 18 min. It also passed the friability test. Conclusion: Accordingly, the solubility of meloxicam was successfully enhanced through solid dispersion with carrier PEG-15,000 and formulated as a MDT to improve its oral absorption. PEG has also been used as a taste masking agent in these formulations. It was concluded that in house banana powder had excellent DT as compared to branded banana powder. Banana powder is “economical” and “easily available” than other commonly used synthetic superdisintegrants. The process of banana powder preparation is eco friendly. The meloxicam MDT formulated with natural superdisintegrant in house prepared banana powder found to pass all pharmacopeial tests.

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.

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.

A simple and high efficient composite based on g-C3N4 for super rapid removal multiple organic dyes in water under sunlight

2022 ◽  
Author(s):  
Siwei Yang ◽  
Qiang Sun ◽  
Weihang Han ◽  
Yuanfang Shen ◽  
Zhigang Ni ◽  
...  
Keyword(s):  
Organic Dyes ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
High Efficient ◽  
Rapid Removal ◽  
Porous Composites

A simple and high efficient porous composites via the solvent evaporation method using g-C3N4 and NiSO4 was developed. It can super rapidly remove multiple organic dyes in water including rhodamine...

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