Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
Microencapsulation has been employed to sustain the drug release, reduce or eliminate drug related adverse effects, dose intake and improve the bioavailability inspite drug undergo extensive first pass metabolism ultimately improve the compliance in pharmacotherapy of inflammation and pain.
Microencapsulation by ionotropic gelation technique is one of the widely used method for preparation of calcium alginate beads which has ability to form gels reaction with calcium salts .
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formulation and evaluation of microbeads
1. FORMULATION AND EVALUATION OF
MICROBEADS
PROJECT SUBMITTED TO UTTRAKHAND TECHNICAL UNIVERSITY
In partial fulfillment of the requirement for the award of the degree of
BACHELOR IN PHARMACY
2012-2016
Submitted By
Gurleen kaur
Roll No. 120260300018
B.Pharm 8th Semester
Under the guidance of
DR.Ashutosh Badola
Department of Pharmaceutical Sciences
Shri Guru Ram Rai Institute of Technology & Science
Patel Nagar, Dehradun (Uttarakhand)
3. INTRODUCTION
In recent years a wide variety of newer
drug delivery systems like oral
sustained/controlled release dosage forms
are designed and evaluated in order to
overcome the limitations of conventional
therapy. The non steroidal anti
inflammatory drug Ibuprofen is a good
candidate for the development of oral
controlled release formulation. It is used
for long term treatment of inflammation &
pain, with dosage 400-600mg (5-
10mg/kg)TDS as conventional
4. Adverse gastric discomfort have been observed, and its short biological half
life 2hr. Microencapsulation has been employed to sustain the drug release,
reduce or eliminate drug related adverse effects, dose intake and improve
the bioavailability inspite drug undergo extensive first pass metabolism
ultimately improve the compliance in pharmacotherapy of inflammation and
pain.
Microencapsulation by ionotropic gelation technique is one of the widely
used method for preparation of calcium alginate beads which has ability to
form gels reaction with calcium salts .
Recently the use calcium alginate gel beads as a vehicle for controlled drug
delivery system . However major disadvantage of alginate beads are their
fast disintegration in simulated intestinal fluid and high porosity, which
results in rapid drug release.
5. These consideration led to the objective of this
study, which was to prepare and evaluate oral
sustained release product namely microbeads for
ibuprofen by ionotropic gelation method using
sodium alginate alone to overcome the fast
disintegration of alginate beads in simulated
intestine.
Advantages:
Decreasing dosing frequency
Improve patient compliance
Reducing side effects
They are also attractive because it can be
fabricated into various shapes.
Disadvantages:
Some synthetic polymers are not biocompatible
6. Literature review
Thulasi v. menon , CI Sajeeth(2103), The main aim of the study is to formulate
Carvedilol loaded microbeads of sodium alginate using gelatine and pectin as
release modifiers by ionotropic gelation method. The microbeads were prepared by
varying the concentration of sodium alginate, gelatin and pectin. The drug-polymer
compatibility was studied by FTIR studies. The prepared microbeads were
evaluated for swelling ratio, particle size, drug entrapment, Scanning electron
microscopy (SEM), bio adhesion study and invitro release study. Particle size
distribution of both placebo and drug loaded formulations were measured by an
optical microscope and particle size of optimized beads was determined by SEM. No
significant drug-polymer interactions were observed in FT-IR studies. In-vitro drug
release profile of Carvedilol micro beads was examined in pH 1.2 N Hydrochloric
acid for first 2 hours followed by phosphate buffer pH 7.4 for remaining time. The in
vitro wash-off test indicated that the sodium alginate micro beads had good
mucoadhesive properties. The formulated beads had shown higher entrapment
efficiency, drug loading, low particle size and moisture content. The formulation F3
released Carvedilol for longer duration (24 hours) and showed better mucoadhesion.
Nayak A,K, Khatuas (2011), researched on Diclofenac sodium is a non-steroidal
anti-inflammatory agent with a short biological half-life (1-2 hr) and requires multiple
dosing. This research was carried out to develop and optimize diclofenac sodium
loaded alginate-PVP K 30 microbeads to eliminate the need for multiple dosing and
adverse effects. Methods: Diclofenac sodium loaded alginate-PVP K 30 microbeads
7. AIM & OBJECTIVE
To prepare microbeads of ibuprofen by using sodiun
alginate.
Preformulation studies
o Melting point
o Solubility
o U.V specroscopy
Evaluation studies
o Drug interaction studies
o Particle size distribution
o Surface and drug entrapment
o Bulk and tapped density
9. USES:
Used primarily for fever, pain,
inflammatory diseases such as
rheumatoid arthritis
Ibuprofen is a NSAID
It is used in the treatment of other
painful conditions such as toothache,
pain after operations, period pain and
headache.
ADVERSE EFFECTS:
Gastric discomfort
Nausea and vomiting
Dizziness and blurring of vision
10. POLYMER PROFILE:
SODIUM ALGINATE
Definition – Sodium salt of alginic acid
Chemical name - Sodium alginate: D-Galacturonic
acid sodium salt
Chemical formula - C6H9NaO7
Description – White to yellowish brown, filamentous,
grainy, granular or powdered forms.
Functional uses – Stabilizer, thickner, gelling agent,
emulsifier.
Solubility – Dissolves slowly in water, forming a
viscous solution, insoluble in ethanol and ether.
13. DISCUSSION - The standard curve plot between
conc. and absorbance. The value of R2 was found to
be 0.997 . So, the equation can be used for the further
calculations.
2. PERCENTAGE YIELD:FORM
ULATI
ON
THEORETIC
AL
YIELD
PRACTICLE
YIELD
PERCENTAG
E
YIELD
F1 1.5gm 1.06gm 70.6%
F2 2gm 1.14gm 57%
F3 2.5gm 1.81gm 72.4%
F4 3gm 2.42gm 80.6%
0.00%
10.00%
20.00%
30.00%
40.00%
50.00%
60.00%
70.00%
80.00%
90.00%
F1 F2 F3 F4
percentageyield
formulations
14. DISCUSSION – The formulation F4 was found to be the
best among all the other formulation.
3. DRUG CONTENT:
DISCUSSION – As the percentage of ibuprofen drug
increases the percentage of drug content also increases.
Formulation Drug content%
F1 78
F2 81
F3 85
F4 87
15. 4. SURFACE AND DRUG ENTRAPMENT:
DISCUSSION - From the result we can
conclude that as the amount of polymer in
the formulation increases, the surface
entrapment decreases as a result of increase
in drug entrapment.
Formulati
on
%surface entrapment %drug entrapment
F1 4.43 78.21
F2 4.21 80
F3 3.98 84.04
F4 3.86 88.72
16. 5. BULK & TAPPED DENSITY:
DISCUSSION – From the formulations we
observed that BD and TD for all the
formulations were found in the range
between 0.13 to 0.41 g/cm3 and o.20 to 0.34
3
Formulatio
n
Bulk density(gm/ml) Tapped
density(gm/ml)
F1 0.13 0.20
F2 0.25 0.29
F3 0.30 0.33
F4 0.41 0.34
18. 7. PARTICLE SIZE:
F1 F2 F3
DISCUSSION: The particle size varies from
125 to 165µm
Formulation Particle size (µm)
F1 125
F2 132
F3 140
F4 165
19. CONCLUSION
It could be concluded that the sustained release alginate
beads of Ibuprofen evaluated by qualitative method gave
effective data’s. Microbeads are one of the microparticulate
systems and are prepared to obtain prolonged or controlled
drug delivery, to improve bioavailability or stability and to
target drug to specific sites. Microbeads can also offer
advantages like limiting fluctuation within therapeutic range,
reducing side effects, decreasing dosing frequency and
improving patient compliance. Microbeads of ibuprofen were
prepared according to the using modified ion gelation method
by selecting concentration of sodium alginate and calcium
chloride as independent variables. Increasing polymer
concentration led to more sustained release effect whereas
presence of sodium alginate improves the encapsulation
efficiency. Calcium chloride can be increased up to certain
limit above which encapsulation was decreased. Moreover,
the effect of each variable on release characteristic was found
to be significant as confirmed by data analysis. Respectively,
the mathematical model developed in the present study can
be used to design microbeads of desired release
characteristic.