solubility enhancer for poorly water soluble drugs

1

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.

2

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

3

PROBLEM SELECTION-SOLUBILITY OF POORLY WATER SOLUBLE DRUG

Solubility- defined in both quantitative and qualitative mannar

Saturated solutionUnsaturated solution or sub-saturated

solution

4

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.

5

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

6

FACTORS AFFECTING SOLUBILITY

TemperaturePressureNature of solute and solventPartical sizeDielectric constantpHPolymorphism,Salts,Stearic factorsPresence of multiple solute

7

BCS CLASSIFICATION OF DRUG

Class I- eg.Metoprolol Class II- eg.Glibenclamide Class III- eg.Cimetidine Class IV- eg.Hydrochlorothiazide

8

DIFFERENT METHODS OF SOLUBILITY ENHANCEMENT

Solubilization by surfactantSolubilization by complexationSolubilization by salt formationSolubilization by prodrug formationSolubilization by cosolencySolubilization by hydrotropySolubilization by solid dispertion

9

SOLUBILIZATION BY SURFACTANT

Enhances the solubility by wetting and penetration of solvent medium in to a drug

eg.polysorbates

10

SOLUBLIZATION BY COMPLEXATION

Having ability to forming soluble complexes with poorly water soluble drug

Eg.cyclodextrin

11

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

12

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

13

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

14

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.

15

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

16

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.

17

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)

18

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.

19