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PharmaSol's SolEmuls
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SolEmuls
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O/W emulsions produced with SolEmuls technology can be used for:
intravenous delivery of drugs that are poorly soluble in both water and oil
dermal application of such drugs to achieve topical formulations with increased drug
concentration (drug is dissolved, not suspended)
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Technology description:
Drugs that are poorly soluble in both water and oil can only be incorporated into o/w
emulsions by localising them in the interfacial stabiliser layer e.g. lecithin layer (a typical example
being amphothericin B). The drug cannot simply be dissolved in an emulsion due to the low solubility
and consequently extremely low dissolution velocity. The SolEmuls technology co-homogenises the emulsion
droplets and the drug powder. Homogenisation of this hybrid dispersion leads to fast dissolution of
the drug due to the extremely high streaming velocities in the homogenisation gap (up to 1000 m/s).
This leads to fast dissolution and fast distribution of dissolved drug molecules in the interfacial
lecithin layer.
The production lines used in industry for the production of parenteral emulsions can be used for the
SolEmuls technology. Homogenisation pressures applied are typical of production conditions (e.g. 600 bar).
In regard to regulatory aspects, the SolEmuls technology is particularly advantageous as no additional excipients
are required because the delivery system consists of only the parenteral emulsion plus added drug.
Advantages over competing technologies:
Drugs, such as amphothericin B, can also be incorporated in liposomes. Disadvantages include not only the known
problems with the physical stability (often lyophilisation is required and thus tedious reconstitution before administration
is required) but also the fact that liposomes are relatively costly (e.g. daily treatment
with Fungizone costs approx. 24 US$/day and with liposomes or similar products, it costs approx. 1000 US$/day).
In comparison, o/w emulsions are of low cost.
Amphothericin B emulsions can also be produced using organic solvents, however, this is a more tedious
and expensive sterile production process, and to our knowledge, no products based on solvent technology are
on the market. SolEmuls avoids solvents and the production process is basically identical to the production
of a normal parenteral emulsion (only slightly higher pressure and cycle number).
Large scale production/costs:
As mentioned earlier, existing production lines can be used. Excipient costs are relatively low i.e.
identical to the costs of the excipients for a parenteral emulsion.
IP position:
For an overview of patents and patent applications please click "Intellectual property".
Further Information regarding this topic can be obtained by reading:
Akkar, A., Müller, R. H., Formulation of i. v. Carbamazepin emulsions by SolEmuls technology,
Eur. J. Pharm. Biopharm. 55, 305-312, 2003
Akkar, A., Müller, R. H., Intravenous itraconazole emulsions produced by SolEmuls Technology,
Eur. J. Pharm. Biopharm. 56, 29-36, 2003
Müller, R. H., Schmidt, S., Buttle, S., Akkar, A., Schmitt, J., Brömer, S., SolEmuls -
Novel technology for the formulation of i.v. emulsions with poorly soluble drugs, Int. J. Pharm. 269, 293-302, 2004
Buttle, I., Schmidt, S., Müller, R. H., Production of amphotericin B emulsions based on SolEmuls
technology, 4th World Meeting ADRITELF/APV/APGI, Florence, 1535-1536, 2002
Müller, R. H., Schmidt, S., SolEmuls technology for i. v. emulsions of poorly soluble drugs:
amphotericin B, 4th World Meeting ADRITELF/APV/APGI, Florence, 1451-1452, 2002
Akkar, A., Müller, R. H., Production of sub-micron sized carbamazepine emulsions with SolEmuls
technology, Intern. Symp. Control. Rel. Bioact. Mater. 30, #201, 2003
Müller, R. H., Akkar, A., Physical principles of SolEmuls process technology for i. v. emulsions
of poorly soluble drugs, Intern. Symp. Control. Rel. Bioact. Mater. 30, #294, 2003
To obtain access to further information regarding this topic:
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Thank You.
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