scholarly journals Solubility EnhancementTechniques forPoorly Soluble Pharmaceuticals: A Review

2019 ◽  
Vol 7 (02) ◽  
pp. 09-16
Author(s):  
Jyoti Gupta ◽  
Anjana Devi
Keyword(s):  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Peptic Ulcers ◽  
Drug Solubility ◽  
Formulation Development ◽  
Drug Candidates ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
New Formulation ◽  
Rate Limiting

Among newly discovered chemical entities about 40% drugs are hydrophobic which are failed to reach market due to their low aqueous solubility. For orally administered drugs solubility is one of the rate limiting parameter to achieve their desired concentration in systemic circulation for pharmacological response.Drug efficacy can be limited due to poor aqueous solubility and some drugs also show side effects like gastric irritation, peptic ulcers,due to their poor solubility. Because of solubility problem of many drugs the bioavailability of them gets affected and hence solubility enhancement becomes challenging. The present review is devoted to various traditional and novel techniques for enhancing drug solubility to reduce the percentage of poorly soluble drug candidates eliminated from the new formulation development.

scholarly journals Cyclodextrin Inclusion Complexes: Novel Techniques to Improve Solubility of Poorly Soluble Drugs: A Review

2016 ◽  
Vol I (I) ◽  
pp. 29-34
Author(s):  
Sobia Noreen ◽  
Irsah Maqbool ◽  
Muhammad Ijaz ◽  
Sairah Tanveer
Keyword(s):  
Inclusion Complexes ◽  
Aqueous Solubility ◽  
Complexing Agents ◽  
Dissolution Profile ◽  
Drug Candidates ◽  
Insoluble Drugs ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
Technological Strategies ◽  
Crucial Test

For a formulation scientist, the dilemma of solubility is a crucial test during the product development phase that can be resolved by opting various technological strategies. Some of the strategies that are usually applied for enhancing solubility of drugs with low aqueous solubility include micronization, solvent deposition and solid dispersion. With these approaches, some advantages as well as drawbacks, are affiliated. The strategy of complexation amid all techniques, has been applied more accurately for the improvement of dissolution profile, aqueous solubility, and bioavailability of poorly soluble drug candidates. Cyclodextrin are unique cyclic carbohydrates that have been exploited as successful complexing agents having capability of forming inclusion complexes with insoluble drugs. Numerous strategies have been considered to analyze the methods for preparation of inclusion complexes. In this review, we have pursued the discussion on different complexation techniques and in a nutshell, emphasized the applications and economical/technical limitations related to these techniques.

scholarly journals Drug Solubility: Importance and Enhancement Techniques

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Ketan T. Savjani ◽  
Anuradha K. Gajjar ◽  
Jignasa K. Savjani
Keyword(s):  
Crystal Engineering ◽  
Water Solubility ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
New Chemical Entities ◽  
Poorly Soluble ◽  
Physical And Chemical ◽  
Site Of Absorption

Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.

Exploration on the Drug Solubility Enhancement in Aqueous Medium with the Help of Endo-Functionalized Molecular Tubes: A Computational Approach

2021 ◽  
Author(s):  
Rabindranath Paul ◽  
Sandip Paul
Keyword(s):  
Pharmaceutical Industry ◽  
Aqueous Medium ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Computational Approach ◽  
Drug Solubility ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Molecular Tubes

One major problem in the pharmaceutical industry is the aqueous solubility of newly developed orally administered drug candidates. More than 50 % of the newly developed drug molecules suffer from...

scholarly journals A Short Review on Application of Liquisolid Technology

2021 ◽  
Vol 4 (1) ◽  
pp. 276-279
Author(s):  
Shaveta Sharma ◽  
Divya Sharma ◽  
Jyoti Singh
Keyword(s):  
Dissolution Rate ◽  
Aqueous Solubility ◽  
Short Review ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Drug Involvement ◽  
Poorly Soluble ◽  
Flowing Powder ◽  
Soluble Liquid ◽  
New Formulation

In this paper we have surveyed about formulation and evaluation of Liquisolid formulations and its work in antidiabetics . Mostly poorly water soluble drugs are in research category despite of less dissolution rate and poor bioavailability. Solubility is a vital parameter to develop new formulation as industries faced serious issue regarding the poor aqueous solubility of the drugs. Various methods for solubility enhancement include modifications of the drug, involvement of co-solvents, complexation, salt formation, size reduction. A propitious technique to solve major challenges like solubility, dissolution rate and their bioavailability. This technique can be defined as the conversion of poorly soluble liquid medications into non-adherent, dry, compressible and free flowing powder mixtures with help of excipients. Many anti-diabetic drugs are belonging to BCS Class-II facing challenges like solubility and bioavailability.

scholarly journals Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

2020 ◽  
Vol 13 (2) ◽  
pp. 80-93 ◽  
Author(s):  
Abikesh P.K. Mahapatra ◽  
Vinod Patil ◽  
Ravindra Patil
Keyword(s):  
Dissolution Rate ◽  
Class Ii ◽  
Systemic Circulation ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Solid Dosage ◽  
Bcs Class Ii ◽  
Pharmacological Response ◽  
Poorly Soluble ◽  
Low Solubility

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.

Solubility-Permeability Interplay of Hydrotropic Solubilization Using Response Surface Methodology

2020 ◽  
Vol 10 (3) ◽  
pp. 209-218
Author(s):  
Nidhi Nainwal ◽  
Sunil Jawala ◽  
Ranjit Singh ◽  
Vikas A. Saharan
Keyword(s):  
Sodium Benzoate ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Limiting Factor ◽  
Apparent Permeability ◽  
Poorly Soluble ◽  
Full Factorial ◽  
Rate Limiting ◽  
Different Levels

Background:: The solubility/dissolution of a drug in the gastrointestinal (GI) region and the permeability of a drug through the GI membrane are the two key parameters governing drug absorption. Poor aqueous solubility is the rate-limiting factor for the absorption of poorly soluble drugs through the GI region. Objective: The purpose of this work is to investigate the influence of two different hydrotropes, namely sodium benzoate (SB), and nicotinamide (NA), at different levels (10-40%) and in combination on the solubility and permeability of poorly soluble drug glibenclamide (GLB). The work will find out, whether the solubility enhancement of glibenclamide using hydrotropes and hydrotropic blends also affects the GI permeability of glibenclamide. Methods: A 32 full factorial design was employed to study the influence of hydrotropic blends of sodium benzoate and nicotinamide on the solubility and permeability of GLB. The solubility and permeability of drugs at different levels (10-40%) of hydrotropes (SB, NA) and their blends are determined using a magnetic stirrer and in vitro Franz diffusion cell, respectively. Results: The results of preliminary studies revealed an increase in the solubility and reduction in the apparent permeability of GLB as a function of increasing levels of both hydrotropes. Conclusion: In this work, it was found that an increase in solubility with hydrotropes results in a decrease in permeability of GLB. The solubility enhancement and the permeability decrease were observed more in hydrotropic blends in comparison to individual hydrotropes. Therefore, it is concluded that both factors, solubility and permeability, must be optimized to achieve appreciable gains in bioavailability.

scholarly journals A PROMISING TECHNIQUE TO IMPROVE THE SOLUBILITY BY LIQUISOLID COMPACTION TECHNOLOGY

2018 ◽  
Vol 8 (5) ◽  
pp. 56-61
Author(s):  
Narender G Naik ◽  
Shaym R Sunder ◽  
Sateesh kumar Manchikanti
Keyword(s):  
Promising Technique ◽  
Bcs Class Ii ◽  
Molecular Dispersion ◽  
Rate Limiting Step ◽  
Poorly Soluble ◽  
Pharmaceutical Industries ◽  
Powder Properties ◽  
Poorly Soluble Drug ◽  
Challenging Situation ◽  
Rate Limiting

About 60-70% of the drugs synthesized are poorly soluble and comes under BCS Class-II&IV. Now it is a challenging situation during the development of different dosage forms for pharmaceutical industries because solubility of the drug is the rate limiting step. Based on the solubility, the dissolution, bioavailability & therapeutic effect is dependent. To overcome this consequence a novel technique -Liquisolid compact is used by dissolving the poorly soluble drug in a non-volatile solvent that improves wettability & decreases the surface tension and ensures drug molecular dispersion in the formulation to increase the solubility of the drug. This admixture of drug loaded solution is blended with carrier adsorption & coating material (adsorption) that has free flowing and compressible powder properties.

Prediction of blood–brain barrier penetration of poorly soluble drug candidates using surface activity profiling

2010 ◽  
Vol 75 (3) ◽  
pp. 405-410 ◽  
Author(s):  
Anna Christine Petereit ◽  
Kelly Swinney ◽  
Jurgen Mensch ◽  
Claire Mackie ◽  
Sigrid Stokbroekx ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Surface Activity ◽  
Brain Barrier ◽  
Drug Candidates ◽  
Activity Profiling ◽  
Blood Brain ◽  
Barrier Penetration ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

scholarly journals LIQUISOLID COMPACTS: AN INNOVATIVE APPROACH FOR DISSOLUTION ENHANCEMENT

2018 ◽  
Vol 10 (6) ◽  
pp. 11
Author(s):  
Anjana Anil ◽  
Litha Thomas ◽  
Preethi Sudheer
Keyword(s):  
Aqueous Solubility ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Drug Candidates ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Coating Agents

The challenge faced by the majority of the pharmaceutical products is the poor solubility of the drug candidates which leads to low bioavailability. Liquisolid compact is one of the emerging techniques that enhances the dissolution of poorly water soluble drugs. Liquisolid system mentions to the formulation made by the transforming the liquid drug, either in the form of suspension or solution in non volatile solvents into a dry, non-sticky, free-flowing and compactable powder mixtures. This is achieved by mixing the suspension or solution of the drug with appropriate carriers and coating agents. The technology has the ability to increase aqueous solubility, rate of dissolution and absorption of poorly soluble drug by keeping it in molecularly dispersed form leading to its improved bioavailability when compared to conventional tablets. Liquisolid technology is the impending approach for enhancing the solubility of poorly water-soluble drug by adopting simple manufacturing process and low production cost.

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