Issue 23: July 2011
Greetings!
The oral bio-availability of hydrophobic drugs has baffled formulation scientists for years and hence
many pharmaceutical approaches have been tried to improve the drug release. The most common
technique used to achieve these results have been the self-emulsifying drug delivery system (SEDDS)
in the form of viscous liquids and marketed mostly in the form of soft gelatine capsules. Production of
soft gelatine capsules have major drawbacks in the manufacturing process such as difficulty in
process control, leakage of the encapsulated components, high production cost and lower stability.
In this newsletter we present a study, carried out by College of Pharmacy, Korea, published in Drug
development and industrial Pharmacy, 2011. Kang et al reported the immediate release self
emulsifying tablet (IR-SET) of ibuprofen (IBU) with Fujicalin, which can replace the viscous and liquid
SEDDS by free flowing powder. Ibuprofen was selected as a model drug because it is a poorly watersoluble analgesic agent and requires a fast onset of action for the relief of acute pain.
The IR-SETs were prepared in three steps. (i) powderization of liquid SMEDDS by adsorbing it to
porous solid carriers, (ii) blending of powdered SEDDS with pharmaceutical excipients, and (iii)
compression of the tablet mixture. The liquid SEDDS containing 100mg of IBU was mixed with the solid
carriers (Fujicalin®, Neusilin® or Neosyl®). The powder was then mixed with disintegrants and sodium
carbonate in certain cases (Table 1). The microscopic structures of the SEDDS retaining solid carriers
are shown in figure 1.
Table1. Percent compositions of immediate release self emulsifying tablets
(IR-SETs)
Codes
SEDDS
Neusilin
®
F1
F2
F3
F4
F5
F6
F7
F8
F9
F10
F11
F12
52.0
52.0
36.1
36.1
36.1
36.1
34.2
30.4
36.1
36.1
34.2
32.3
58.4
58.4
58.4
58.4
55.3
49.1
58.4
58.4
55.3
52.2
10.0
20.0
5.0
5.0
5.0
5.0
5.0
10.0
0.5
0.5
0.5
0.5
3.6±0.6
3.4±0.5
42.5
Neosyl®
Fujicalin
42.5
®
®
Polyplasdone
Amberlite
Primellose
5.0
5.0
5.0
5.0
®
5.0
®
5.0
Vivastar
NaHCO3
Mg-St
0.5
0.5
0.5
0.5
0.5
0.5
Na-SF
0.5
SLS
Hardness (kp)
0.5
5.1±1.6
5.8±0.8
3.2±0.4
3.4±0.3
3.0±0.5
3.3±0.6
3.7±0.3
3.6±0.2
3.0±0.5
3.4±0.4
Abbreviations: Mg-st, Magnesium stearate; Na-SF, sodium steary fumarate; SLS, sodium lauryl sulfate; SEDDS, self-emulsifying
drug delivery system. Hardness data are expressed as the mean±SD(n=3).
Figure1. Scanning electron micrographs (300x) of Fujicalin and Neusilin before and after
self-emulsifying drug delivery system (SEDDS) adsorption
The release profiles of IBU from Neusilin, Neosyl and Fujicalin based SETs (F1, F2 and F3) were
compared with that obtained with the liquid SEDDS as shown in figure2. Various other combinations
were analysed such as influence of disintegrants, influence of lubricants, and influence of sodium
bicarbonate. (For details, please refer to original paper.)
Figure2. Release profiles of ibuprofen (IBU) from liquid self emulsifying drug
delivery system (SEDDS), Neusilin-based self- emulsifying tablet (SET),
Neosyl-based SET, and Fujicalin-based SET in simulated gastric juice. Data
are expressed as mean± SD (n=3).
Sodium carbonate was additionally included to F3 formulation to facilitate tablet
disintegration and the formulation F11 was optimised and tested with different
paddle speeds against the liquid SEDDS, shown in Figure 3.
Figure3. Effect of stirring rate on the release characteristis of ibuprofen (IBU)
from self-emulsifying tablet (SET) formulation of F11 in simulated gastric
juice. Data are expressed as mean ± SD (n=3).
Conclusion
The novel IR-SET of IBU was successfully prepared based on the powderisation of liquid SEDDS with
Fujicalin, The optimised IR-SET with Fujicalin showed exactly the similar release rate as that of the
liquid SEDDS.
Reference
Joo Kang, Soo Young Jung, Woo Heon Song, Jun Sang park, Sung-up Choi, Kyung Taek Oh, Hyung-Kyoon
CHoi, Young Wook Choi, Jaehwi Lee, Beom-Jin lee, and Sang-Cheol Chi (2011) Immediate release of Ibuprofen
from Fujicalin - based fast-dissolving self-emulsifying tablets. Drug Development and Industrial Pharmacy, 1-8,
Early online
Fujicalin® and Neusilin® and are trademarks or registered trademarks of Fuji Chemical Industry Co., Ltd in
Japan, United States of America, Europe and/or other countries.
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