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.

Insight into Delivery Approaches for Biopharmaceutics Classification System Class II and IV Drugs

2020 ◽  
Vol 10 (4) ◽  
pp. 255-277
Author(s):  
Shashank Chaturvedi ◽  
Raghav Mishra
Keyword(s):  
Class Ii ◽  
Crystal Habit ◽  
Extensive Literature ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
Bioavailability Enhancement ◽  
Poor Solubility ◽  
Biopharmaceutics Classification System Class ◽  
Poorly Soluble ◽  
Physical And Chemical

: Formulation development of BCS Class II and IV drugs is a challenging task due to their poor solubility and permeability issue. : An extensive literature survey was conducted to explore the relevant pharmaceutical approaches that have been used for solving the issue of poor solubility and permeability in the recent past. : It has been found that a plethora of approaches have been investigated for addressing the issue of poor solubility and or permeability. These include physical modifications (modification of crystal habit, particle size reduction, complexation, polymorphism and drug dispersion in carriers), chemical modifications (salt formation), and formulation modifications (Nanotechnology-based approaches and hydrotropy). : The physical and chemical modification approaches can be effectively used to enhance the solubility and dissolution rate of poorly soluble drugs, but the additional problem of poor permeability has been better addressed by lipid-based drug delivery systems. As the latter presents the drug in the solubilized state, bypass first-pass effects, circumvent the effect of Para-glycoprotein mediated efflux of drugs, hence contributing to overall bioavailability enhancement.

scholarly journals Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability

2019 ◽  
Vol 9 (2) ◽  
pp. 583-590 ◽  
Author(s):  
Sandip R. Pawar ◽  
Shashikant D. Barhate
Keyword(s):  
Particle Size ◽  
Solid Dispersion ◽  
Water Solubility ◽  
New Technologies ◽  
Aqueous Media ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Formulation Development ◽  
Particle Size Reduction ◽  
Poorly Soluble

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. Solubility is essential for the therapeutic effectiveness of the drug, independent of the route of administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. 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. Drug with poor water solubility cause slow dissolution rates, generally show erratic and incomplete absorption leading to low bioavailability when administered orally. Solubilization may be affected by cosolvent water  interaction, micellar solubilization, reduction in  particle  size,  inclusion  complexes,  solid  dispersion,  and  change  in  polymorph.  Some  new technologies  are  also  available  to  increase  the  solubility  like  micro emulsion,  self-emulsifying drug  delivery  system  and  supercritical  fluid  technology. This present review details about the different approaches used for the enhancement of the solubility of poorly water-soluble drugs include particle size reduction, nanonization, pH adjustment, solid dispersion, complexation, co‐solvency, hydrotropy etc. The purpose of this article is to describe the techniques of solubilization for the attainment of effective absorption and improved bioavailability. Keywords: Solubility, Solubility Enhancement, bioavailability, solid dispersion, Solid Dispersion, Solubilization.

scholarly journals Chemical Modification: A unique solutions to Solubility problem

2019 ◽  
Vol 9 (2) ◽  
pp. 542-546 ◽  
Author(s):  
M. Siddik N. Patel ◽  
Mohd Hasib Ahmed ◽  
Mohammad Saqib ◽  
Siraj N Shaikh
Keyword(s):  
Chemical Modification ◽  
Systemic Circulation ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Salt Formation ◽  
Formulation Development ◽  
Dissolution Properties ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Physical And Chemical

Almost 40% of the new chemical entities at present self find out poorly water soluble drugs. Badly water soluble drugs have solubility and dissolution related bioavailability problems. Solubility is one of the most important parameter to give desired concentration of drug in systemic circulation to get its pharmacological response. Orally administered drugs obtained completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs perform an valuable role in the process of formulation development. Enhancement of solubility of drug is the most challenging job in drug development process. Solubilization may be affected by co solvent water interaction, micellar solubilization, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph. This review highlight various techniques of solubility enhancement with special emphasis on Chemical modification methods like Salt formation, Co-crystallization, Co-solvency, Hydrotropy, use of novel solubilizer etc along with physical modification techniques. Keywords: Salt formation, Co-crystallization, Solubility, particle technologies, Milling solubility enhancement, Cosolvent, physical and chemical methods.

scholarly journals An Overview on the Recent Technologies and Advances in Drug Delivery of Poorly Water-Soluble Drugs

2019 ◽  
pp. 180-195
Keyword(s):  
Crystal Engineering ◽  
General Circulation ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Phase System ◽  
Particle Size Reduction ◽  
Pharmaceutical Ingredients ◽  
Solubility Improvement ◽  
New Chemical Entities ◽  
Water Soluble Drugs

Solubility can be defined as the amount of solute dissolved in a solvent at certain conditions to yield a single-phase system. Solubility of active pharmaceutical ingredients is considered the main parameter to get the most desired drug concentration in general circulation in order to achieve the desired therapeutic effect. Poor aqueous solubility considered the main problem occurs in the formulation progress of new chemical entities; in addition to the standard improvement; solubility is the main dispute for formulation scientists. The drug must appear as solution at the site of absorption in order to be absorbed. Many physical or chemical modification techniques are used to improve the solubility of low aqueous soluble drugs, in addition to other techniques such as particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant and complexation. The selection of the solubility improvement methods depends on drug characteristics, location of absorption and the features of the administered dosage form.

Solubility Enhancement Techniques for Poorly Water-Soluble Drugs

2017 ◽  
Vol 10 (3) ◽  
pp. 3701-3708
Author(s):  
Amol S Deshmukh ◽  
Kundan J Tiwari ◽  
Vijay R Mahajan
Keyword(s):  
Plasma Concentrations ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Water Soluble ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Poor Solubility ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for optimum pharmacological response. Poorly water-soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Poor aqueous solubility is a major problem encountered with formulation development of new chemical entities. There are over 40% of new chemical entities that exhibit poor solubility and low bioavailability. As per BCS classification system, these drugs comes under BCS class II that show poor solubility and high permeability. The bioavailability of these drugs can be dramatically improved by increasing the solubility of these drugs. This review article highlights a number of techniques for enhanc

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.

Self-microemulsion Technology for Water-insoluble Drug Delivery

2019 ◽  
Vol 15 (6) ◽  
pp. 576-588 ◽  
Author(s):  
Beibei Yan ◽  
Yu Gu ◽  
Juan Zhao ◽  
Yangyang Liu ◽  
Lulu Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Poorly Soluble Drugs ◽  
New Chemical Entities ◽  
Poorly Soluble ◽  
Water Insoluble Drug ◽  
Semi Solid ◽  
Solidification Technology

: According to the drug discovery, approximately 40% of the new chemical entities show poor bioavailability due to their low aqueous solubility. In order to increase the solubility of the drugs, self-micro emulsifying drug delivery systems (SMEDDS) are considered as an ideal technology for enhancing the permeability of poorly soluble drugs in GI membranes. The SMEDDS are also generally used to enhance the oral bioavailability of the hydrophobic drugs. At present, most of the self-microemulsion drugs are liquid dosage forms, which could cause some disadvantages, such as the low bioavailability of the traditional liquid SMEDDS. Therefore, solid self-micro emulsifying drug delivery systems (S-SMEDDS) have emerged widely in recent years, which were prepared by solidifying a semi-solid or liquid self-emulsifying (SE) ingredient into a powder in order to improve stability, treatment and patient compliance. The article gives a comprehensive introduction of the study of SMEDDS which could effectively tackle the problem of the water-insoluble drug, especially the development of solidification technology of SMEDDS. Finally, the present challenges and the prospects in this field were also discussed.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals Basic Review: Solubility Enhancement by Using Various Approaches

2021 ◽  
Vol 68 (2) ◽  
Author(s):  
Baldha Krunal ◽  
Sanjay Savaliya ◽  
Payal N Vaja ◽  
Dr. Chetan H Borkhtaria
Keyword(s):  
Pharmaceutical Industry ◽  
Water Solubility ◽  
Development Stage ◽  
Solubility Enhancement ◽  
Therapeutic Action ◽  
Drug Solubility ◽  
Formulation Development ◽  
Bioavailability Enhancement ◽  
Screening Programs ◽  
New Chemical Entities

The solubility enhancement process of drugs plays a key role in the formulation development to achieve the bioavailability and therapeutic action of the drug at the target site. About 40% of the new chemical entities identified by pharmaceutical industry screening programs face numerous problems in the formulation and development stage because of poor water solubility and low bioavailability. Drug solubility and bioavailability enhancement are the important challenges in the field of formulation of pharmaceuticals.

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