SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG

SANKET UDDHAORAO BOBADE M .PHARM.FIRST YEAR(PHARMACEUTICS) GUIDED BY PAWAN RATHI SIR SHRI BHAGWAN COLLEGE OF PHARMACY,AURANGABAD.
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CONTENT
Problem selection-solubility enhancement of poorly water soluble drug Importance of solubility Solubility expression Factors affecting solubility BCS classification of drug Different methods of solubility enhancement Nead,Objective,Justification,Literature review References
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PROBLEM SELECTION-SOLUBILITY OF POORLY WATER SOLUBLE DRUG

Solubility- defined in both quantitative and qualitative mannar Saturated solution Unsaturated solution or sub-saturated solution

IMPORTANCE OF SOLUBILITY
Is an important phenomenon as pharmaceutical point of view. Important pre-formulation parameter. Important prequisite for the drug absorption. Essential in dissolution of solid dosage forms.

SOLUBILITY EXPRESSION
Expressed quantitatively like in terms of molarity,molality,or part per millions. Expressions for solubility
Terms Very soluble Freely soluble Soluble Sparingly soluble Slightly soluble Very slightly soluble Part of solvent required Less than 1 part 1 to10 parts 10 to30 parts 30 to100 parts 100 to 1000 parts 1000 to 10000
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FACTORS AFFECTING SOLUBILITY

Temperature Pressure Nature of solute and solvent Partical size Dielectric constant pH Polymorphism,Salts,Stearic factors Presence of multiple solute
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BCS CLASSIFICATION OF DRUG

Class I- eg.Metoprolol Class IIeg.Glibenclamide Class IIIeg.Cimetidine Class IVeg.Hydrochlorothiazide

DIFFERENT METHODS OF SOLUBILITY ENHANCEMENT

Solubilization by surfactant Solubilization by complexation Solubilization by salt formation Solubilization by prodrug formation Solubilization by cosolency Solubilization by hydrotropy Solubilization by solid dispertion
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SOLUBILIZATION BY SURFACTANT
Enhances the solubility by wetting and penetration of solvent medium in to a drug eg.polysorbates

SOLUBLIZATION BY COMPLEXATION
Having ability to forming soluble complexes with poorly water soluble drug Eg.cyclodextrin

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SOLUBILIZATION BY SALT FORMATION

Most drugs are either weak acid or weak base Salt formation is mode of changing the pharmacokinetic property of drug by modifying its physical and chemical properties

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SOLUBILIZATION BY PRODRUG FORMATION

Water soluble drugs are desired where solubility is rate limiting step Drugs with hydroxyl function can be converted into their hydrophilic forms by use of halfesters. Eg.hemisuccinates

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SOLUBILIZATION BY COSOLVENCY
Cosolvents or solvent blends are defined as water miscible organic solvents that are used in liquid drug formulation. They increase solubility of non-polar drugs by reducing the polarity of the aquese mixture

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SOLUBILIZATION BY HYDROTROPY
Is a molecular phenomenon whereby addition of a second solute results in an increase in the aqueous solubility of poorly soluble solutes.

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NEED AND OBJECTIVES

Need Pharmacologic and toxicologic screening Rate limiting factor of drug absorption True solution provides most promt and reliable release of drug to the body Objective Selection and collection of various co-solvents Determination of solubility of drug Analysis of data of solubility
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JUSTIFICATION
It provides an opportunity to a pharmacist to choose a suitable solvent. Growing importance of solubility in designing drugs and developing formulation has forced physical pharmacist to develop techniques for quantitative solubility prediction and their utilization. During the past two decades,cosolvency has been of considarable interest.
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LITERATURE REVIEW
Author name 2012 Martin A.,Paruta A.N. Title Extended hindebrand solubility approch Journal International journal of pharmaceutical science,1981,76(10),11151120. International journal of pharmaceutical science,1992,78(1-3),1724. International journal of pharmaceutical research and development,june2012,Vol. 4(04),(071-086)

CVS Subrahmanyam,M sreeniwasa

Irregular solution behaviour of paracetamol in binary solvent Solubility enhancement techniques for poorly soluble drug

M I Limbachiya

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REFERENCES
1)Brahmankar,D.;Jaiswal, S.In Biopharmaceutics-A Treaties, Vallabh Prakashan,2002;19,pp297-298.
2)Subrahmanyam,CVS. Solubility of solids in liquids.In Essentials of Physical Pharmacy;1st edition;Vallabh Prakashan,2003;pp380. 3)Martin,A.; Paruta,A.N.;Adjei.A. Extended Hildebrand Solubility Approch: Methyl xanthines in Mixed Solvents,J. of Pharm.sci.1981,70(10),1115-1120. 4)Subrahmanyam,CVS.;Sreenivasa, M.; Reddy,J.; Rao, P. G. Irregular solution behaviour of paracetamol in binary solvent.Int.J.P.ceutics.1992, 78(1-3), 17-24.
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