solubility enhancement techniques

1. Complexation
preparation of cyclodextrin
complexes and application
Suchandra Bagchi
M.S(Pharmaceutics)
NIPERA1517PE10

2. FLOW OF SEMINAR
• INTRODUCTION
• METHODS OF PREPRATION
• EXAMPLES
• ADVANTAGES
• APPLICATIONS

3. INTRODUCTION
• Cyclodextrin molecules are cyclic oligosaccharides made up of 6 to 12 α-D-
glucopyranose monomers, connected at 1 and 4 carbon atoms of pyranose
moieties.
• 6 carbon atoms- α-cyclodextrin
• 7 carbon atoms- β-cyclodextrin
• 8 carbon atoms- γ-cyclodextrin

4. Modes of interaction
They generally forms host and guest complexes by
1. Hydrogen bonding
2. Van der waals interaction
3. Hydrophobic interactions and
4. Electrostatic interactions
These bond alter the guests photochemical and photophysical properties.
and they do not form covalent bonds…. Hence the physical, chemical and
biochemical properties of guest molecule is modified.

5. Methods of preparation
Physical mixture
Kneading method
Co precipitate method

6. Physical mixture
DRUG+β-CYCLODEXTRIN
PLACED IN MORTAR MIXED AND
TRITURATED FOR ONE HOUR
PASSEDTHROUGH SEIVE NO 80
STORED IN DESSICATOR FUSED
WITH CALCIUM CHLORIDE

7. KNEADING METHOD
CYCLODEXTRIN ISTAKEN IN MORTAR
A SLURRYWAS PREPAREDWITH 50% ETHANOL BY
TRITURATION
THEN DRUGWAS ADDED SLOWLYTOTHE SLURRY AND
FURTHERTRITURATIONWAS CARRIED OUT FOR ONE HOUR
THE SLURRYWASTHEN AIR DRIEDAT 25ºC FOR 24 HOURS
PULVERISEDAND PASSEDTHROUGH SEIVE NO 80
THEN STORED

8. CO PRECIPITATE METHOD
DRUGWAS DISSOLVED IN
ETHANOLAT ROOM
TEMPARETURE
Β-CYCLODEXTRINAND
HYDROXYPROPYL β
CYCLODEXTRINWAS
DISSOLVED IN DISTILLED
WATER
THEN DRUG SOLUTIONWAS
ADDEDTOTHEAQOUS
PHASEAND STIRREDAT
ROOMTEMPARETUREAND
THE SOLVENTWAS
EVAPORATEDON BOILING
WATER BATH.
THENTHE INCLUSION
COMPLEXES PRECIPITATED
AND PULVERISEDAND
PASSEDTHROUGH SEIVE NO
80 AND STORED IN
DESSICATORAFTERTHE
POWDERGOT FREE OF
RESIDUALSOLVENT.

9. EXAMPLES
POORLY SOLUBLE DRUGS ARETAKENTO FORM COMPLEXES GENERALLY
40% OF NCE ARE POORLY SOLUBLE INWATER HENCETO OVERCOME
SOLUBILITY ISSUES ANDTO INCREASE BIOAVAILABILITY OF DRUGSTHIS
PROCESS IS USED AS SOLUBILITY ENHANCMENTTECHNIQUES.
LIPOPHILIC DRUGS ARE MADE LIPOPHOBIC BY FORMING COMPLEXES
AND BY INCORPORATING IT INTHE CAVITIES OF CYCLODEXTRIN COMPLES
BY ENCAPSULATION, INTERACTION, ENTRAPPMENT TECHNIQUES…

10. ADVANTAGES
1. INCREASE IN SOLUBILITY OF POORLY SOLUBLE DRUGS GENERALLY BCS CLASS 2 AND 4.
2. LARGE MOLECULES CAN BE INCORPORATED INTOTHE COMPLEX
3. NONPOLAR HEADS CAN BETURNEDTO POLAR HEADS
4. TASTE MASKING OF BITTER DRUGS
5. ENHANCES PERMEABILITY OF DRUGS
6. ENHANCEMENT OF BIOAVAILABILITY
7. PREPARATION OF COMPLEXES ARE GENERALLY EASY
8. STERILITY NEED NOTTO MAINTAIN

11. Drugs
these are generally complexed with cyclodextrin
• Carbamazepine
• Digoxin
• Glibenclamide
• Miconazole
• Phenytoin
• Spironolactone
• Tolbutamide
• Α-tocopherol nicotinate etc
• Cyclosporine A (BCS- 4)