A pharmaceutical oil-in-water nano-emulsion, comprising:
a pharmaceutically active substance, encased in monounsaturated fatty
acid droplets, said droplets having an average particle size in the range of
60 to 200 nm;
a non-ionic surfactant system comprising a mixture of polyethers,
macrogolglycerides and polysaccharides; and
pharmaceutically acceptable adjuvants.
The composition as claimed in claim 1, wherein said pharmaceutically
active substance is lipophilic or partially lipophilic and selected from a
group consisting of antipsychotics, anti-emetics, analgesics, antipyretics,
anti-inflammatory agents or any lipophilic based drugs.
The composition as claimed in claim 2, wherein said antipsychotics are
ziprasidone, fluphenazine, haloperidol, olanzapine, chlorpromazine,
risperidone, aripiprazole, molindone, loxapine, sulpiride, preferably
olanzapine or risperidone and pharmaceutically acceptable salts thereof.
The composition as claimed in claim 2, wherein said anti-emetics are
diphenhydrinate, diphenhydramine, doxylamine, meclizine, ondansetron,
promethazine, prochlorperazine, preferably ondansetron or a
pharmaceutically acceptable salts thereof.
The composition as claimed in claim 2, wherein said analgesics,
antipyretics, anti-inflammatory agents are selected from methadone,
diamorphine, fentanyl, buprenorphine, temazepam, piracetam, sufentanil,
mefenamic acid, naproxen, piroxicam, indomethacin, valdecoxib,
celecoxib, probenecid, nabumetone, ibuprofen, flurbiprofen, isoxicam,
meclofenamic acid, fenclozic acid, phenyl butazone, preferably
paracetamol.

The composition as claimed in claim 1, wherein said monounsaturated
fatty acid is an oleic acid, in the range of about 5 to 25 % w/w, preferably
in the range of 7.5% to 10% w/w.
The composition as claimed in claim 1, wherein said polyether surfactant
is a combination of polyethylene glycol in the range of 2 to 20 % w/w and
transcutol of 2.5 to 10% w/w.
The composition as claimed in claim 1, wherein said polyether surfactant
is polyethylene glycol in the range of 2 to 20 % w/w, preferably 15% w/w.
The composition as claimed in claim 1, wherein said macrogolglyceride
surfactant is caprylocaproyl macrogol-8 glyceride or acconon CC 6, in the
range of 12 to 25% w/w or a combination thereof.
The composition as claimed in claim 1, wherein said polysaccharide
surfactant is selected from polyoxyethylene sorbitan fatty acid esters,
preferably polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene
(80) sorbitan monooleate and sorbitan monooleate or a combination
thereof.
The composition as claimed in claim 10, wherein said polysaccharide
surfactant is in the range of 2 to 30 % w/w, preferably from 5 to 25 %
w/w.
The composition as claimed in claim 1, wherein alternately benzyl alcohol,
phenyl ethyl alcohol or chloro butanol is used as a co-solvent.
The composition as claimed in claim 1 wherein said adjuvants are
stabilizers, antioxidants, preservatives, mucoadhesive agents, buffering
agents, absorption enhancers and pH adjusting agents.
The composition according to claim 13, wherein said antioxidant, selected
from butylated hydroxytoluene, butylated hydroxyanisole, ascorbic acid
and tochopherol or a combination thereof in the range of 0.01% to 0.2%
w/w.
The composition according to claim 13, wherein said absorption enhancers
are selected from macrogol-15-hydroxystearate, sodium glychocolate and
sodium caprylate or a combination thereof.

The composition as claimed in claim 1, wherein said composition adapted
for nasal administration comprising: a pharmaceutically active substance
selected from olanzipine, ondansetron or respirodone; in the presence of
oleic acid, polyethylene glycol, caprylocaproyl macrogol-8 glyceride and
polyoxyethylene (20) sorbitan monolaurate.
The composition as claimed in claim 16, wherein said composition is for
use in the treatment or prevention of migraine, nausea, vomiting,
psychosis, sleep disorders, respectively.
The composition as claimed in claim 1, wherein said composition adapted
as an ocular solution comprising: a pharmaceutically active substance
paracetamol; in the presence of polyethylene glycol; caprylocaproyl
macrogol-8 glyceride and polyoxyethylene (20) sorbitan monolaurate.
The composition as claimed in claim 18, wherein said ocular solution is
for use in the treatment or reduction of intraocular pressure.
The use of composition as claimed in claim 16, in the manufacture of
medicament for the treatment or prevention of nausea, vomiting, psychosis
and sleep disorders.
The use of composition as claimed in claim 18, in the manufacture of
medicament for the treatment or reduction of intraocular pressure.
A process for the preparation of an oil-in-water emulsion composition as
claimed in claim 1, comprising the steps of
i) forming an oil phase in the presence of a monounsaturated fatty acid, a
polyether surfactant, a macrogolglyceride surfactant and a polysaccharide
surfactant, under stirring at an ambient temperature; and
ii) adding a therapeutically amount pharmaceutically active substance to said oil phase, under constant stirring and at an ambient temperature, to encase said active substance, in said monounsaturated fatty acid droplets, said droplets with particle size in the range of 60 to 200 nm, to obtain a homogenous oil phase; and

iii) adding an aqueous medium to said homogenous oil phase, under stirring to obtain the oil-in-water emulsion.