seminar on oral lipoid formulation and instability of emulsion

1. Oral lipoid formulation and
instability of emulsion
Rahul Uttam Mane
M.Pharmacy(Pharmaeutics)
Rajarambapu college of pharmacy,Kasegaon
RAJARAMBAPU COLLEGE OF
PHARMACY,KASEGAON
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2. Content
Introduction
Lipid based Excipients
Classification of lipid based excipients
Techniques for formulation
Characterization of formulation
Introduction of emulsion
Instability of emulsion
Conclusion
References RAJARAMBAPU COLLEGE OF
PHARMACY,KASEGAON 2

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INTRODUCTION
Definition:
It is a solid, liquid and semisolid dispersion of poorly water soluble
drugs in lipid and surfactant based excipients for improve oral
bioavaibility.
These are generally formulated as self emulsifying, non-emulsifying,
micro emulsifying drug delivery systems.
Lipid excipients are generally obtained from natural sources also can
be synthesized chemically.
Depending on the choice of excipient(s) and formulation techniques, it
is possible to obtain a variety of systems including physical mixtures,
liquid/solid solutions, and Self-Micro or Self- Nano Emulsifying Drug
Delivery Systems(SMEDDS/SNEDDS).

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Lipid based Excipients
•Lipids are fatty acids and their derivatives,and substances related
biosynthetically or functionally to these compounds.
•The most frequently chosen excipients for preparing oral lipid-
based formulations were,
dietary oils-(e.g., coconut or palm seed oil)
long-chain triglycerides-(e.g., corn, oliveor soybean oils)
lipid soluble solvents (e.g.,polyethylene glycol 400, ethanol,
glycerin)
Pharmaceutically acceptable surfactants (e.g., Cremophor®
polysorbate 20 or 80; D-α-tocopherol polyethylene glycol 1000)

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Classification of lipid based excipients
Natural product oils
Semi-synthetic Lipid Excipients
Synthetic Lipid Excipients
Surfactants

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Techniques for formulation
1. Spray Cooling

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2.Spray Drying

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3.Adsorption on Solid Carrier
4.Melt granulation
5.Melt Extrusion
6.Solid dispersion

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Characterization of formulation
1.Simulated Lipolysis Release
Testing
2.In vitro Dissolution testing

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Introduction of emulsion
An emulsion is liquid preparation containing two immiscible liquids, one of which is
dispersed as globules (dispersed phase) in the other liquid (continuous phase).
dispersed phase
continuous phase
An emulsion is a thermodynamically unstable system consisting of
at least two immiscible liquid phases one of which is dispersed as
globules in the other liquid phase stabilized by a third substance
called emulsifying agent.
Emulsions are also called heterogeneous systems or biphasic
systems
Two Immiscible Liquids
Dispersed Phase
(Internal phase)
Continuous Phase
(External phase)

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Types of emulsions
Simple emulsions (Macro emulsions)
• Oil-in-water (O/W)
• Water-in-oil (W/O)
Multiple emulsions
Oil-in-water-in-oil (O/W/O)
Water-in-oil-in-water (W/O/W)
Micro emulsions
Microemulsions are thermodynamically stable optically
transparent , mixtures of a biphasic oil –water system stabilized
with surfactants.

12. (a) Flocculation and creaming
(b) Coalescence and breaking
(c) Phase inversion.
Flocculation
• Neighboring globules come closer to each other
and form colonies in the continuous phase. This
aggregation of globules is not clearly visible.
• This is the initial stage that leads to instability.
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13. • The extent of flocculation of globules depends on
(a) globule size distribution.
(b) charge on the globule surface.
(c) viscosity of the external medium.
• Flocs slowly move either upward or downward leading
to creaming.
• Flocculation is due to the interaction of attractive and
repulsive forces, whereas creaming is due to density
differences in the two phases.
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14. Creaming
• Creaming is the concentration of globules at the top
or bottom of the emulsion.
• Droplets larger than 1 mm may settle preferentially
to the top or the bottom under gravitational forces.
• Creaming may also be observed on account of the
difference of individual globules (movement rather
than flocs).
• It can be observed by a difference in color shade of
the layers.
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15. Coalescence
• If the sizes of globules are not uniform, globules of
smaller size occupy the spaces between the larger
globules. A few globules tend to fuse with each other
and form bigger globules.
• This type of closed packing induces greater cohesion
which leads to coalescence.
• In this process, the emulsifier film around the globules
is to a certain extent. This step can be
recognized by increased globule size and reduced
number of globules. 15RAJARAMBAPU COLLEGE OF PHARMACY,KASEGAON

16. Coalescence is observed due to:
Insufficient amount of the emulsifying agent.
Altered partitioning of the emulsifying agent.
Incompatibilities between emulsifying agents.
• Phase volume ratio of an emulsion has a secondary
influence on the stability of the product and
represents the relative volume of water to oil in
emulsion.
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17. Breaking
• Separation of the internal phase from the external
phase is called breaking of the emulsion.
• This is indicated by complete separation of oil and
aqueous phases, is an irreversible process, i.e., simple
mixing fails. It is to resuspend the globules into an
uniform emulsion.
• In breaking, the protective sheath around the globules
is completely destroyed and oil tends to coalesence.
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18. Phase inversion
• This involves the change of emulsion type from o/w to
w/o or vice versa.
• When we intend to prepare one type of emulsion say
o/w, and if the final emulsion turns out to be w/o, it
can be termed as a sign of instability.
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Conclusion
The oral lipoid formulations are the novel drug delivery system to
improve the oral bioavaibility of poorly water soluble drugs.
The most significant issue to consider when formulating poorly
water-soluble drugs is the threat of drug precipitation in the lumen
of the gastrointestinal tract.
The stability of emulsion is very important in pharmaceutical
formulation.

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References
ORAL LIPID BASED FORMULATION: A REVIEW
M. NAGARAJU PATRO*1, AJIT S. BANKAR, SACHIN UTTAM RAKESH, DR. A. V. YADAV
1.Govt. College of Pharmacy, Karad- 415 124, Tal. Karad. Dist. – Satara, M. S. India.
2College of Pharmacy, Medha, At Jawalwadi, Post- Medha, Tal- Jaoli, Dist. - Satara M.S, India.
A REVIEW: NOVEL ORAL LIPID BASED FORMULATION FOR POORLY WATER SOLUBLE DRUGS
MAULIK PATEL,SANJAY PATEL,NATVARLAL PATEL AND MADHABHAI PATEL
1.Shri.B.M.Shah,college of pharmaceutical education & Research,Madosa,India.
2.Kalol institute of pharmacy,Kalol,India.
Leon lachman, Herbert A Lieberman, Joseph L Kanig, The Theory and practice of Industrial
Pharmacy, Third edition, Varghese publishing house, page no: 457- 463.
Lipid-based formulations for oral delivery of lipophilic drugs
Martin Kuentz University of Applied Sciences and Arts Northwestern Switzerland, Institute of
Pharma Technology, Gru¨ndenstr. 40, CH-4132 Muttenz, Switzerland

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