Poorly soluble drugs: disbalance of thermodynamic characteristics of crystal lattice and solvation

RSC Advances ◽  
2016 ◽  
Vol 6 (81) ◽  
pp. 77870-77886 ◽  
Author(s):  
G. L. Perlovich
Keyword(s):  
Benzoic Acid ◽  
Crystal Lattice ◽  
Aqueous Media ◽  
Thermodynamic Characteristics ◽  
Poorly Soluble Drugs ◽  
Benzoic Acid Derivatives ◽  
Poorly Soluble

The dissolution processes in aqueous media of poorly soluble drugs belonging to the classes of spiro and benzoic acid derivatives, sulfonamides, fenamates, and thiadiazoles were analyzed based on the data recently published by the author.

Polymeric Nanomicelles of Soluplus® as a Strategy for Enhancing the Solubility, Bioavailability and Efficacy of Poorly Soluble Active Compounds

2019 ◽  
Vol 9 (3) ◽  
pp. 184-197 ◽  
Author(s):  
Rosario Pignatello ◽  
Roberta Corsaro
Keyword(s):  
Polyvinyl Acetate ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Physical Stability ◽  
Small Diameter ◽  
Amorphous Solid ◽  
Poorly Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Soluble

: Soluplus® is a commercially available graft amphipathic copolymer consisting of polyvinyl caprolactam, polyvinyl acetate, and polyethyleneglycol (13% PEG 6000/57% vinyl caprolactam/30% vinyl acetate). Among the various applications of this solubilizer excipient, produced by BASF, such as the production of amorphous solid dispersions of insoluble drugs, Soluplus® has shown to be able to form nano-sized micelles in water or other aqueous solutions, characterized by a very small diameter and an exceptionally narrow size distribution. These formulations allow to improve the solubility and physical stability in aqueous media of poorly soluble drugs. This review summarizes the recent data from literature on the methods of production and characterization of drugloaded nanomicelles based on Soluplus®, highlighting the potential fields of therapeutic application.

Photoassisted dehalogenation and mineralization of chloro/fluoro-benzoic acid derivatives in aqueous media

2008 ◽  
Vol 197 (1) ◽  
pp. 115-123 ◽  
Author(s):  
Hisao Hidaka ◽  
Haruo Honjou ◽  
Takayoshi Koike ◽  
Yoshihiro Mitsutsuka ◽  
Toshiyuki Oyama ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Aqueous Media ◽  
Benzoic Acid Derivatives

Nanosuspensions: Recent Patents and Pharmaceutical Aspects as Drug Delivery Systems

2017 ◽  
Vol 10 (2) ◽  
pp. 3631-3644
Author(s):  
Vikram S Gharge ◽  
Mukesh B Shinde ◽  
Bipin D Pustake ◽  
Krishna B Kinage ◽  
Anup A Kulkarni
Keyword(s):  
Drug Delivery ◽  
Pharmaceutical Preparation ◽  
Aqueous Media ◽  
Poorly Soluble Drugs ◽  
Wet Milling ◽  
Drug Effectiveness ◽  
Pharmaceutical Application ◽  
Poorly Soluble ◽  
Emulsification Solvent Evaporation ◽  
Biphasic Systems

Solubility is an essential factor for drug effectiveness, independent of the route of administration. Poorly soluble drugs are often a challenging task for formulators in the industry. Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Nanosuspension technology can be used to improve the stability as well as the bioavailability of poorly soluble drugs. Nanosuspensions are biphasic systems consisting of pure drug particles dispersed in an aqueous vehicle, stabilized by surfactants. These are simple to prepare and are more advantageous than other approaches. Techniques such as wet milling, high-pressure homogenization, emulsification–solvent evaporation and super critical fluid have been used in the preparation of nanosuspensions. It has the advantage of delivery by various routes, including oral, parenteral, pulmonary and ocular routes. The present article reviews the current methods used to prepare nanosuspensions and their application in drug delivery. More than 100 patents have been published on nanosuspensions in the recent days. This patent reviews covers different methods of pharmaceutical preparation and applications in drug delivery as well as the recent marketed published or granted patent surveys. This patent review is useful in enhanceing the knowledge of pharmaceutical application in drug delivery.

Bjerkandera adusta as a source of benzoic acid derivatives targeting 26S proteasome and cathepsins B&L

2019 ◽  
Author(s):  
K Georgousaki ◽  
N Tsafantakis ◽  
S Gumeni ◽  
V González-Menéndez ◽  
G Lambrinidis ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
26S Proteasome ◽  
Bjerkandera Adusta ◽  
Benzoic Acid Derivatives

Technological Advancements in Oral Films

2019 ◽  
Vol 9 (01) ◽  
pp. 15-20
Author(s):  
B Pandey ◽  
A B Khan
Keyword(s):  
3D Printing ◽  
Historical Background ◽  
Poorly Soluble Drugs ◽  
Modern Approach ◽  
Poorly Soluble ◽  
Critical Process Parameters ◽  
Biopharmaceutical Properties ◽  
Oral Films ◽  
Hot Melt ◽  
Modern Technologies

The aim of the review was to explore the necessity, advantages and different techniques of oral films for enhancing solubility of poorly soluble drugs with an emphasis on the newer, state-of the art technologies, such as 3D printing and hot-melt extrusion (HME). The historical background of oral films is presented along with the regularly used techniques. The modern approach of quality-by-design (QbD) is unravelled, identifying appropriate critical process parameters (CPP) and applied to oral films. A section is devoted modern technologies such as 3D printing and HME of oral films. Oral films are innovative formulations by which poorly soluble drugs have been founds to give positive results in enhancing their solubility and dissolution characteristics. With modern sophisticated techniques, precise mass production of oral films has been given a thrust. Oral films have better patient compliance, improved biopharmaceutical properties, improved efficacy, and better safety. By applying QbD and implementation of modern technologies the newer generation of oral films are yielding promising results

2,4-Dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic Acid Derivatives: In Vitro Antidiabetic Activity, Molecular Modeling and In silico ADMET Screening

2019 ◽  
Vol 15 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Samridhi Thakral ◽  
Vikramjeet Singh
Keyword(s):  
Molecular Docking ◽  
Benzoic Acid ◽  
Inhibitory Activity ◽  
In Silico ◽  
Computational Study ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Benzoic Acid Derivatives ◽  
In Silico Admet ◽  
Inhibitory Potential

Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl] benzoic acid derivatives and evaluate α-glucosidase and α-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential α-glucosidase and α-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-dichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against α-amylase and 5 times inhibitory activity against α-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against α-glucosidase and α-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.

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