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INTRODUCTION
40-50% of NCEs- sparingly soluble compounds that
require specialized formulations.
This is where the role of lipid excipients comes in play
- used as co-solvents or as carriers to protect the API
and improve its pcokinetic and pcodynamic activity.
Lipids are hydrocarbon based molecules. Thus they
are predominantly hydrophobic, but also have a
hydrophilic functional portion, such as hydroxyl,
amine, phosphate esters and carboxyl groups.
This makes lipids- a group of amphipathic molecules
that posses both hydrophobic and hydrophilic portions
to self assemble into various colloid structures in
physiological conditions.
Classification
Fatty acids
Natural oils and fats
Semi-synthetic mono-, di-, triglycerides
Semi-synthetic PEG derivatives of glycerides and
fatty acids
Polyglyceryl fatty acid esters
Phospholipids
Cholesterol
Glycolipids
Fatty Acids
A Fatty acid is a carboxylic acid with a long unbranched aliphatic chain,
which is either saturated or unsaturated. Most naturally occurring fatty
acids have a chain of an even number of carbon atoms, from 4 to 28.
Saturated Fatty acids
STEARIC ACID
It has also been suggested that stearic acid may be used in enteric tablet
coatings and as a sustained-release drug carrier
AVERAGE MOLECULAR
WEIGHT
PEG200
190-210
PEG300
285-315
PEG400
380-420
PEG600
570-613
PEG900
855-900
Parenterals
ophthalmic
Used in
biodegradable
polymeric
matrices used in
controlledrelease systems
Topical
Application
s
Aqueous
polyethylene glycol
solutions can be
used either as
suspending agents
or to adjust the
viscosity and
consistency of other
suspending
vehicles.
As Suppository Bases
Polyoxyethylene Stearates
MOLECULAR
WEIGHT
Polyoxyl 6 stearate
548.80
Polyoxyl 8 stearate
636.91
Polyoxyl 12 stearate
813.12
Polyoxyl 20 stearate
1165.55
Polyoxyl 40 stearate
2046.61
COMMERCIAL PRODUCT
COMPOUND
COMMERCIAL PRODUCT
PEG-4-distearate
Kessco200 DS (Stepan)
PEG-6-distearate
PEG-12-distearate
PEG-8 Stearate
Cithrol 4MS
PEG-8 Isostearate
Cithrol 4MIS
Chemical Description
CITHROL 10MO
PEG-20 Oleate
Cithrol 10MO
CITHROL 10MS
(VEG)
ESTOL 3751
PEG-20 Stearate
Cithrol 10MS
PEG-6 Beeswax
Cithrol 3BW
ARLACEL P135
LAN
PEG 30
Dipolyhydroxystearate
Cithrol DPHS
Functional Category
Emulsifying agent
Solubilizing agent
Description
Penetration enhancer
Wetting agent
Method of Manufacture
Polyoxyethylene alkyl ethers are prepared by the condensation of
linear fatty alcohols with ethylene oxide.
The reaction is controlled so that the required ether is formed with the
polyethylene glycol of the desired molecular weight.
Physical
HLB
form
Value
MICROBE 15-17
ADS
White
4.9
translucen
t
plastic wax
Application
Used as emulsifier for o/w emulsion,
creams.
Used in microemulsion gels, creams
and lotions, physical sunscreens,
lipsticks, aqueous/alcoholic
preparations, depilatories,
antiperspirants and deodorants and
shaving preparations.
New applications:
General structure :
PHOSPHOLIPIDS
Amphiphilic molecules
Formed by phosphate grp linkage to the terminal OH grp of glycerols
COMMON HEAD Grps: choline(Phosphatidylcholine), ethanolamine
(Phosphatidylethanolamine),serine(Phosphatidylserine), etc.
Because of their amphiphilic nature, phospholipids will associate at
hydrophobic/hydrophilic interfaces
Functional Category Anionic, cationic, nonionic surfactant
biodegradable material;
dispersing agent; emulsifying agent; emulsion stabilizer;
solubilizing agent;
Applications in Pharmaceutical Formulations stabilize emulsions and suspensions
In formulations administered as lung surfactants, in intravenous fat
emulsions, and in oral solutions (e.g. Rapamune)
To form various types of liposomes eg.
1. Unilamellar
2. Multilamellar
3. Multivescicular
Examples
Common name
Trade name
manufacturer
synonym
Dilauroyl
Coatsome MCphosphatidylchol 2020PhosphoLipidine
DLAPC
NOFNippon
DLPC
Dimyristoyl
Coatsome MCphosphatidylchol 4040Lipoid PC
ine
14:0/14:0 (DMPC)
PhosphoLipidDMPC
NOFLipoid Nippon
DMPC
CHOLESTEROL
Nonproprietary Names
BP: Cholesterol
JP: Cholesterol
PhEur: Cholesterol
USP-NF: Cholesterol
Synonyms
Cholesterin; cholesterolum.
Chemical Name and CAS Registry Number
Cholest-5-en-3b-ol [57-88-5]
Empirical Formula and Molecular Weight
C27H46O 386.67
Structural Formula
Functional Category
Emollient; emulsifying agent.
REFERENCES
Handbook
of pharmaceutical excipient
Oral lipid-based formulations
Avanti polar lipids(www.avantilipids.com)