School Of Pharmacy SRTMU Nanded
PRESENTED BY:
RAJESH LAXMAN RAUT
M.Pharm I (QA)
GUIDED BY:
Mr. G. CHATE SIR
Ast. PROFESSOR
CO-SOLVENCY
Content
 Introduction
 Solubility Definition
 Reasons For Solubility Enhancement
 Techniques for solubility enhancement
 Cosolvancy
 Mechanism of cosolvency
 Advantages and disadvantages
Introduction
 Solubility, the phenomenon of dissolution of solute
in solvent to give a homogeneous system, it is one of
the important parameter to achieve desired
concentration of drug in systemic circulation for
desired pharmacological response.
 Any drug to be absorbed must be present in the form
of solution at the site of absorption
 Therefore various technique are used for the
enhancement of the solubility of poorly soluble drugs
Solubility
 Definition:
The amount of substance that passes into the
solution in order to establish equilibrium at constant
temperature and pressure to produce a saturated
solution.
Need of solubility enhancement
 Oral administration of drug is the most commonly
used drug delivery route.
 The oral bioavailability is highly dependant on
solubility.
 Poorly water soluble drugs having slow drug
absorption leads to inadequate and variable
bioavailability.
 It will cause gastrointestinal mucosal toxicities.
 Therefore just to improve the bioavailability of a
drug one has to increase the solubility.
Solubility Enhancement Techniques
Techniques
Chemical
Modification
Change in pH
Physical
Modification
Miscellaneous
Modification
Cosolvent
Surfactant
Particle size
reduction
Cosolvancy
 The solubility of a poorly water soluble drug can be
increased by the addition of water miscible solvent in
which the drug has a good solubility
 This whole procedure is known as cosolvency and the
solvent is called cosolvant
 Cosolvents are mixture of water and one or more
water miscible solvent use to create a solution with
enhance solubility for a poorly water soluble drugs.
Characteristics of Cosolvents
• Non-toxic
• Non-Irritant
• Able to solubilise the Drug in Given Solvents
• Able to cross membrane
• Value of Dielectric Constant is In between 25-80
Widely used cosolvents
Glycerine
PEG
Diethyl Acetamide
Glycoferol
Ethyl Lactate
Ehyl Alcohol
Discussion
 Parenteral formulation may require addition of water or
a dilution step before administration.
 Dimethyl sulphoxide(DMSO) and Dimethyl
acetamide (DMA) have been widely used as cosolvents
b’coz of there large solubilisation capacity for poorly
soluble drug and there relatively low toxicities
 A blend of propylene glycol and water is use to improve
the solubility of clotrimoxazole in oral solution and
paracetamol is formulated as elixir by use of alcohol and
propylene glycol
17/02/2017
17/02/2017

Cosolvency

  • 1.
    School Of PharmacySRTMU Nanded PRESENTED BY: RAJESH LAXMAN RAUT M.Pharm I (QA) GUIDED BY: Mr. G. CHATE SIR Ast. PROFESSOR CO-SOLVENCY
  • 2.
    Content  Introduction  SolubilityDefinition  Reasons For Solubility Enhancement  Techniques for solubility enhancement  Cosolvancy  Mechanism of cosolvency  Advantages and disadvantages
  • 3.
    Introduction  Solubility, thephenomenon of dissolution of solute in solvent to give a homogeneous system, it is one of the important parameter to achieve desired concentration of drug in systemic circulation for desired pharmacological response.  Any drug to be absorbed must be present in the form of solution at the site of absorption  Therefore various technique are used for the enhancement of the solubility of poorly soluble drugs
  • 4.
    Solubility  Definition: The amountof substance that passes into the solution in order to establish equilibrium at constant temperature and pressure to produce a saturated solution.
  • 5.
    Need of solubilityenhancement  Oral administration of drug is the most commonly used drug delivery route.  The oral bioavailability is highly dependant on solubility.  Poorly water soluble drugs having slow drug absorption leads to inadequate and variable bioavailability.  It will cause gastrointestinal mucosal toxicities.  Therefore just to improve the bioavailability of a drug one has to increase the solubility.
  • 6.
    Solubility Enhancement Techniques Techniques Chemical Modification Changein pH Physical Modification Miscellaneous Modification Cosolvent Surfactant Particle size reduction
  • 7.
    Cosolvancy  The solubilityof a poorly water soluble drug can be increased by the addition of water miscible solvent in which the drug has a good solubility  This whole procedure is known as cosolvency and the solvent is called cosolvant  Cosolvents are mixture of water and one or more water miscible solvent use to create a solution with enhance solubility for a poorly water soluble drugs.
  • 8.
    Characteristics of Cosolvents •Non-toxic • Non-Irritant • Able to solubilise the Drug in Given Solvents • Able to cross membrane • Value of Dielectric Constant is In between 25-80
  • 9.
    Widely used cosolvents Glycerine PEG DiethylAcetamide Glycoferol Ethyl Lactate Ehyl Alcohol
  • 12.
    Discussion  Parenteral formulationmay require addition of water or a dilution step before administration.  Dimethyl sulphoxide(DMSO) and Dimethyl acetamide (DMA) have been widely used as cosolvents b’coz of there large solubilisation capacity for poorly soluble drug and there relatively low toxicities  A blend of propylene glycol and water is use to improve the solubility of clotrimoxazole in oral solution and paracetamol is formulated as elixir by use of alcohol and propylene glycol
  • 16.
  • 17.