CRITICAL REVIEW IN PHARMACEUTICAL SCIENCES ASPECTS OF SOLUBILISATION: A REVIEW (original) (raw)
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ChemInform Abstract: Drug Solubility: Importance and Enhancement Techniques
ChemInform, 2013
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.
Drug Solubility: Importance and Enhancement Techniques
ISRN Pharmaceutics, 2012
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.
Enhancement of solubilization and bioavailability of poorly soluble drugs
The aim of this review was to improve the solubility and bioavailability of poorly soluble drugs by using various approaches like physical, chemical and others modifications or techniques. The solubility of a solute is the maximum quantity of solute that can dissolve in a certain quantity of solvent or quantity of solution at a specified temperature. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown.
Various techniques for the enhancement of solubility of drug molecules
There are many methods and procedures available to improve the solubility and enhance bioavailability. But Solid dispersion systems have been realized as extremely useful tool in improving the dissolution properties of poorly water-soluble drugs. In recent years, a great deal of knowledge has been accumulated about solid dispersion technology, but other methods like micronization, complexation, pro-drugs concepts also useful in pharmaceutical operations. The deep study is required to prevent the limitation of any method. A success of formulation depends on how efficiently it makes the drug available at the site of action .Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. There are many techniques which are used to enhance the aqueous solubility. The ability to increase aqueous solubility can thus be a valuable aid to increasing efficiency and/or reducing side effects for drugs. This is true for parenterally, topically and orally administered solutions .Hence various techniques are used for the improvement of the solubility of poorly water soluble drugs include hydrotrophy, use of salt form, use of precipitation inhibitors, alteration of pH of the drug micro-environment, solvent deposition, precipitation pH adjustment, co-solvency,micellar solubilization, super critical fluid techniques, solid dispersion, complexation, micro-emulsion, solid solution, eutectic mixture, selective adsorption on insoluble carriers, evaporative precipitation into aqueous solution, use of surfactants, use of amorphous, anhydrates, solvate , nanonisation and coating.
Bioavailability is the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. Traditionally, nearly 40% of the new chemical entities (NCEs) identified by pharmaceutical industry screening programs have failed to be developed due to of poor water solubility, which makes their formulation difficult or even impossible to come into the regular market. Solubility is one of the important ways to achieve the desired concentration of drug in to the systemic circulation for its pharmacological response and also most of the drugs are weakly acidic and weakly basic with poorly aqueous solubility. The oral route of administration is the most preferred and widely acceptable route of delivery due to ease of ingestion for many drugs, however these drugs with slow dissolution rate and low solubility in aqueous media shows the incomplete absorption leading to low bioavailability when orally administered. Poorly aqueous soluble drugs often require high doses in order to reach therapeutic plasma concentrations of oral concentration because of which increase in the side effects for certain drugs. Pharmaceuticals falling under the Biopharmaceutics Classification System (BCS) class II and IV are the main emphasis of this review as these drugs are of low solubility. Here we discussed about traditional techniques, novel drug delivery technologies, solid dispersion techniques and vascular approaches to enhance the solubility as well as the bioavailability of low soluble drugs.
A Study on Solubility Enhancement Methods for Poorly Water Soluble Drugs
American Journal of Pharmacological Sciences, 2013
It is generally recognized that poor solubility is one of the most frequently encountered difficulties in the field of pharmaceutics. Low solubility and subsequent unsatisfactory dissolution rate often compromise oral bioavailability. There are most therapeutic agents used to produce systemic effects by oral route that are the preferred way of administration owing to its several advantages and high patient compliance compared to other routes. However, poorly water-soluble drugs, when administered orally, have been shown to be slowly and unpredictably absorbed since their bioavailability is largely dependent on the dissolution process in gastrointestinal tract. This article demonstrates the various methods used to increase dissolution rates, preparation techniques of solid dispersion, and characterization methods of the solid dispersion.
Solubility of Drugs, Their Enhancement, Factors Affecting and Their Limitations: A Review
International Journal for Pharmaceutical Sciences Research and Review, 2023
The solubility of drugs is a crucial factor in determining their efficacy and bioavailability. This review article provides an overview of the concept of drug solubility, including enhancement methods and factors that affect solubility. The limitations of current methods are also discussed, along with why we need to continue the improvement in drug solubility. The article highlights the importance of solubility in drug development and delivery, and provides insights into the future of solubility research and its potential impact on patient outcomes along with the examples of each method mentioned with advantages and disadvantages.
Poorly Water Soluble Drugs: Change in Solubility for Improved Dissolution Characteristics a Review
The aim of this review is to study various parameters to improve the solubility and bioavilability of poorly water soluble drugs. The oral route of administration is the most preferred and widely acceptable route of delivery due to ease of ingestion for many drugs. Drugs with slow dissolution rate show the incomplete absorption leading to low bioavilability when orally administered. Various approaches such as micronization, solid dispersion, complexation, hydrotrophy, co-solvency, use of surfactant, sonocrystallization, particle size reduction, micro emulsion, nanosuspensions, cryogenic Techniques has been used to enhance the solubility of poorly water soluble drugs. In this review authors discussed about various Techniques used to enhance absorption and bio avilability of drugs and various patents available on solubility enhancement.