solubility enhancer for poorly water soluble drugs
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solubility enhancer for poorly water soluble drugsTRANSCRIPT
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SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUG
SANKET UDDHAORAO BOBADEM .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 solubilitySolubility expressionFactors affecting solubilityBCS classification of drugDifferent methods of solubility enhancementNead,Objective,Justification,Literature reviewReferences
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PROBLEM SELECTION-SOLUBILITY OF POORLY WATER SOLUBLE DRUG
Solubility- defined in both quantitative and qualitative mannar
Saturated solutionUnsaturated solution or sub-saturated
solution
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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.
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SOLUBILITY EXPRESSION
Expressed quantitatively like in terms of molarity,molality,or part per millions.
Expressions for solubilityTerms Part of solvent required
Very soluble Less than 1 part
Freely soluble 1 to10 parts
Soluble 10 to30 parts
Sparingly soluble 30 to100 parts
Slightly soluble 100 to 1000 parts
Very slightly soluble 1000 to 10000
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FACTORS AFFECTING SOLUBILITY
TemperaturePressureNature of solute and solventPartical sizeDielectric constantpHPolymorphism,Salts,Stearic factorsPresence of multiple solute
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BCS CLASSIFICATION OF DRUG
Class I- eg.Metoprolol Class II- eg.Glibenclamide Class III- eg.Cimetidine Class IV- eg.Hydrochlorothiazide
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DIFFERENT METHODS OF SOLUBILITY ENHANCEMENT
Solubilization by surfactantSolubilization by complexationSolubilization by salt formationSolubilization by prodrug formationSolubilization by cosolencySolubilization by hydrotropySolubilization 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
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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 baseSalt 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 half-esters.
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-• 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
NEED AND OBJECTIVES
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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 REVIEWAuthor name 2012 Title Journal
Martin A.,Paruta A.N. Extended hindebrand solubility approch
International journal of pharmaceutical science,1981,76(10),1115-1120.
CVS Subrahmanyam,M sreeniwasa
Irregular solution behaviour of paracetamol in binary solvent
International journal of pharmaceutical science,1992,78(1-3),17-24.
M I Limbachiya Solubility enhancement techniques for poorly soluble drug
International journal of pharmaceutical research and development,june2012,Vol.4(04),(071-086)
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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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