Issue 23: July 2011 
Pharma header_Fujicalin

Immediate release of Ibuprofen from Fujicalin� based fast dissolving self emulsifying tablets

 

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 water-soluble 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

F1

F2

F3

F4

F5

F6

F7

F8

F9

F10

F11

F12

SEDDS

52.0

52.0

36.1

36.1

36.1

36.1

34.2

30.4

36.1

36.1

34.2

32.3

Neusilin

42.5

 

 

 

 

 

 

 

 

 

 

 

Neosyl

 

42.5

 

 

 

 

 

 

 

 

 

 

Fujicalin

 

 

58.4

58.4

58.4

58.4

55.3

49.1

58.4

58.4

55.3

52.2

Polyplasdone

5.0

5.0

5.0

 

 

 

10.0

20.0

5.0

5.0

5.0

5.0

Amberlite

 

 

 

5.0

 

 

 

 

 

 

 

 

Primellose

 

 

 

 

5.0

 

 

 

 

 

 

 

Vivastar

 

 

 

 

 

5.0

 

 

 

 

 

 

NaHCO3

 

 

 

 

 

 

 

 

 

 

5.0

10.0

Mg-St

0.5

0.5

0.5

0.5

0.5

0.5

0.5

0.5

 

 

0.5

0.5

Na-SF

 

 

 

 

 

 

 

 

0.5

 

 

 

SLS

 

 

 

 

 

 

 

 

 

0.5

 

 

Hardness (kp)

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

3.6�0.6

3.4�0.5

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
fig1

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).

 fig2

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).

 

 fig3

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

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