06/28/22 06/28/22 SOLUBILIZATION OF NON-ELECTRO SOLUBILIZATION OF NON-ELECTRO LYTES LYTES 1 SOLUBILIZATION OF NON- ELECTROLYTES GUIDED BY: A.M.SUDHAKAR BABU SIR, PRINCIPAL& HOD DEPARTMENT OF PHARMACEUTICS A.M.REDDY MEMORIAL COLLEGE OF PHARMACY Presented by: RAGHAVENDRA KUMAR GUNDA
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SOLUBILIZATION OF NON-ELECTROLYTES
GUIDED BY:A.M.SUDHAKAR BABU SIR,
PRINCIPAL& HODDEPARTMENT OF PHARMACEUTICS
A.M.REDDY MEMORIAL COLLEGE OF PHARMACYPresented by:
RAGHAVENDRA KUMAR GUNDA
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DEFINITION:-The term ‘solubility’ is defined as maximum amount of solute that can be dissolved in a given amount of solvent. It can also be defined quantitatively as well as qualitatively. Quantitatively it is defined as the concentration of the solute in a saturated solution at a certain temperature. In qualitative terms, solubility may be defined as the spontaneous interaction of two or more substances to form a homogenous molecular dispersion. A saturated solution is one in which the solute is in equilibrium with the solvent.
Spontaneous passage of poorly water soluble solute molecules into an aqueous solution of surfactant is termed as SOLUBILISATION.
Solubilization can be defined as a the Solubilization can be defined as a the preparation of a thermodynamically preparation of a thermodynamically stable isotropic solution of a stable isotropic solution of a substance normally insoluble or very substance normally insoluble or very slightly soluble in a given solvent by slightly soluble in a given solvent by the introduction of an additional the introduction of an additional component or componentscomponent or components
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Se the Concentration of Co-Solvent se Dielectric constant of the solvent Due to hydrogen bonding
Se solubility of hydrophobic molecules The energy required to separate two oppositely charged bodies is inversely proportional to the dielectric constant of the medium.
Chemical modification of the drug:By addition of polar groups like carboxylic acids, ketones and amines can increase solubility by increasing hydrogen bonding and the
interaction with water. Complexation Methods (inclusion complex or clathrates)Betacyclodextrins solubilise water insoluble drugs. HYDROXYL PROPYL METHYL CELLULOSE(HPMC) relies on
relatively weak force such as London forces, hydrogen bonding and hydrophobic interactions N-Methyl Pyrrolidone(NMP) for drugs like Phenobarbital, Griseofulvin, Phenytoin, Ketoprofen, Estrone, Testosterone, Ibuprofen, Amiodarone ; Carbendazim, 2-Phenoxypropionic acid (PPA) and Benzoylphenyl urea derivative
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Application of ultrasonic wavesSolubility increases by use o ultrasonic vibrators. A n oscillator of high frequency(100-500KHz) is use and device is known as Pohlman whistle.
Solubility Enhancement of Hydrophobic Drugs using Synergistically interacting Cyclodextrins and Co-Solvent Loftsson et al. reported that addition of polyethylene glycol or ethanol in an aqueous solution of CD reduced
the solubility of ibuprofen. Pitha and Hishino reported that the solubility of testosterone with hydroxypropyl- cyclodextrin (Hp--CD) is 10,000-fold lower in 80% ethanol than in water. The reason behind this was that the cosolvent may act by competing with the drug for entry into the CD cavity or by reducing solvent polarity
Poloxamer-188 is one of the commercial grades of poloxamers, which are water-soluble, non-ionic, surface active copolymers. The polyoxyethylene segment of poloxamer- 188 is relatively hydrophilic, while the polyoxypropylene segment is relatively hydrophobic. It has been used in pharmaceutical formulations, primarily as emulsifying and solubilizing agents. It has the ability to form a clear solution or gel in aqueous media, thus solubilizing many water-insoluble compounds by the formation of micelles
SOLUBILIZATION OF PARTICULATE PROTEINS AND NONELECTROLYTES BY CHAOTROPIC AGENTS*
Chaotropic ions (those ions which favor the transfer of Apolar groups to water) provide a highly effective means for the resolution of membranes and multi-component enzymes and for increasing the water solubility of particulate proteins and nonelectrolytes. The action of chaotropic agents is related to their effect on the structure and lipophilicity of water.
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REFERENCES:1>Solubility enhancement of hydrophobic drugs using synergistically interacting cyclodextrins and cosolvent Praveen Chaudhari1,*, Pramodkumar Sharma2, Nilesh Barhate1, Parag Kulkarni1 and Chetan Mistry12> TECHNIQUES OF SOLUBILIZATION BY Samuel H. Yalkowsky3> Encyclopedia of Pharmaceutical technology Vol 3 4> Essentials of Physical Pharmacy – subramanyam5> Biopharmaceutics and pharmacokinetics -Brahmankar.6> Enhancement of solubility of valdecoxib by Solid Dispersion Techniques – research paper By Modi1, P Tayade2 7> Pharmaceutical white papers –solubilization8> Martin’s physical pharmacy fifth edition9>Solubility of Nonelectrolytes in Water: A Thermodynamic and Quantum Chemical Approach based on Dihydroxynaphthalene Derivatives By Christian Machon, Ingfried Zimmermann10>SOLUBILITY ENHANCEMENT TECHNIQUES WITH SPECIAL EMPHASIS ON HYDROTROPHYPURWA JAIN*, ACHHRISH GOEL, SHWETA SHARMA, MEGHAL PARMAR11>ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE: AN OVERVIEW P. S Mohanachandran1*, P. G Sindhumol1 and T. S Kiran 2 12>Determination of Aqueous Solubility by Heating and Equilibration: A Technical Note Thorsteinn Loftsson1 and Dagný Hreinsdóttir1
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13>Enhancement of Solubility: A Pharmaceutical OverviewBehera A. L.*1, Sahoo S. K.2 and Patil S. V.314>Solubility Improvement of Drugs using N-Methyl PyrrolidoneRitesh Sanghvi,1,4 Ryuichi Narazaki,2 Stephen G. Machatha,3 and Samuel H. Yalkowsky115>Hydrotropic Solubilization of Poorly Water-Soluble DrugsJI YOUNG KIM,1 SUNGWON KIM,1 MICHELLE PAPP,1 KINAM PARK,1,2 RODOLFO PINAL116>FACTORS DETERMINING SOL UBILITY AMONGNON-ELECTROL YTES*BY JOEL H. HILDEBRAND17>Determination of Aqueous Solubility by Heating and Equilibration:A Technical Note by Thorsteinn Loftsson1 and Dagný Hreinsdóttir118>Oral Delivery of Poorly Soluble DrugsBy Michael Hite, Lead Research Associate, Stephen Turner19>Solubilization of Poorly Soluble Drugs: A Review by Anil J Shinde
20>ABSORPTION AND DRUG DEVELOPMENT BY ALEX AVDEEF
21>ORAL DRUG ABSORPTION BY JENNIFER B. DRESSMAN
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