Study the physicochemical characteristics of ibuprofen and evaluate the solid dispersion formulation of ibuprofen by using different molecular weight of PEG

1. Study the physicochemical characteristics of ibuprofen and
evaluate the solid dispersion formulation of ibuprofen by
using different molecular weight of PEG
Presented by:- Hadeia Mashaqbeh

2.  Is a nonsteroidal anti-inflammatory drug that
is widely used as an analgesic
 It is a non-selective inhibitor of cyclo-
oxygenase-1 (COX-1) and Cyclooxygenase-2
(COX-2)
 Used to reduce fever and treat pain or
inflammation caused by many conditions
such as headache, back pain, arthritis,
chronic laryngitis and bronchiolitis

3. 2-(4-isobutylphenyl)-propionic acid
Ibuprofen is Crystalline stable solid with characteristic odor.
It melts at about 75-78 °C

4.  its application in the pharmaceutical field is
limited by its:
 low aqueous solubility
 bad taste
 bad manufacturing behavior; the flow
properties are poor and it has a high
tendency to stick to the punches
 increasing risk of serious effects on the
stomach and intestines.

5.  class II drug according to the BCS
classification
 Ibuprofen is readily soluble in most organic
solvents, very soluble in alcohol and is
almost insoluble in water (21 mg/L at 25 °C).

6. Solubility enhancement includes :
 both conventional techniques as inclusion
complexation, solid dispersions, salt
formation etc.
 As well as relatively newer techniques such
as selfemulsifying systems, micro emulsion,
nanosizing and supercritical fluid processing.

7.  Solid dispersion is one of the most promising
approaches for solubility enhancement .
Solid dispersion of Ibuprofen was prepared
with Poloxamer 407, PVP K12, PEG 4000 and
PEG 6000
 solid dispersions using PEG 8000
 Solid dispersions of ibuprofen were prepared
using polyethylene glycol 20000 by physical
mixing and solvent evaporation method.

8. two phases form a monotropic set:
 Phase I is the more stable phase at all
temperatures lower than its melting at Tm I
= 348 K.
 Metastable phase II may exist up to its
melting point at Tm II= 0 290 K.

9.  Preparation of Ibuprofen Solid Dispersion.
Ibuprofen and PEG (4000, 6000 and 20000) in
1:10 proportions were prepared by melt method.
Each carrier, PEG 4000, 6000 and 20000 was first
melted separately at a temperature of 65 °C in a
water bath. The Ibuprofen was incorporated to
each melt of PEG 4000, 6000, 20000 and kept in
room temperature for cooling. The solidified
mass was scrapped and then crushed
 Preparation of Ibuprofen Physical Mixtures
Physical mixtures of ibuprofen were prepared
by mixing ibuprofen with PEG 4000, 6000 and
20000 each at once in combination and
individually in a glass mortar by trituration. The
ratio of Ibuprofen and PEG was 1:10.

10.  Solid dispersions were characterized by
differential scanning calorimetry (DSC),
Thermal Gravimetric Analysis (TGA) ,fourier
transform infrared spectroscopy (FTIR) and
x-ray diffraction
 Also evaluated for equilibrium solubility

11. The endothermic peak at 79.4 °C and the absence of
loss of mass in the TGA indicate that it is the melting
point of ibuprofen which is the charcteristics of racemic
ibuprofen.

12. The decomposition at 255 °C results in a loss of
mass with the release of CO2 and hydrogen from
the carboxylic acid chain

13. Carboxylic
group
3000-3400 cm-1
Methyl group
stretching
2955 cm-1
Stretching of
carbonyl group 1720
cm-1
C-C
stretching
1231cm-1
CH2 rocking
vibration
779 cm−1

14. 0
5000
10000
15000
20000
25000
30000
35000
40000
4.00
6.02
8.04
10.06
12.08
14.1
16.12
18.14
20.16
22.18
24.2
26.22
28.24
30.26
32.28
34.3
36.32
38.34
40.36
42.38
44.4
46.42
48.44
50.46
52.48
54.5
56.52
58.54
60.56
62.58
64.6

15.  The UV spectra of ibuprofen were presented.
The absorption maxima was observed at 222
nm.
R² = 0.9979
y = 0.0019x + 0.0088
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7
0.8
0.9
050100150200250300350400450
absorbance
concentration (µg/ml)
caliration curve

18.  the increase in the solubility of the drug
when it is physically mixed with PEG is
probably due to a wettability improvement
and a local solubilization effect by the
carrier.
 In the case of the solid dispersion it can be
concluded that higher drug saturated
solubility may only related to the presence of
polymeric carrier in the medium, but not
associated to the drug status in the solid
dispersion system (neither polymorphic
change nor reduction in particle size ).

19. Najib, N.M. and Sheikh Salem, M.A., 1987. Release of Ibuprofen from Polyethylene
glycol solid dispersions:-Equilibrium solubility approach.Drug Development and
Industrial Pharmacy,13(12), pp.2263-2275.

22. The new endothermic peaks appeared at nearly 60 c related to the melting point of PEG .

24.  Decreased by increasing both the polymer
molecular weight and concentrations.
 At a very high polymer concentration, a
prevailing viscosity delaying effect was
observed, solubilization effect will decrease
due to the decrease of the affinity of
polymer toward the drug

25. As the molecular weight of PEG and concentration increase
solubilization effect will decrease due to the decrease of
the affinity of polymer toward the drug

26.  Solubility studies showed enhancement in
solubility in the presence of PEG in solid
dispersions but physical mixture gives higher
ranges of solubility
 This study indicating compatibility between PEGs
and Ibuprofen
 As the molecular weight of PEG and
concentration increase solubilization effect will
decrease due to the decrease of the affinity of
polymer toward the drug .
 According to these result solid dispersion of
ibuprofen should prepared with higher drug
:polymer ratio or with lower molecular weight
PEG