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FORMULATION ANDEVALUATION OFIBUPROFEN
MICROSPHERE
Submitted by-
SHOUVIK MONDAL
ROLL NO. - 1740113045, 7th SEMESTER
Under the Gidence of
Dr. Sudipta Das
Netaji Subhas Chandra Bose Institute of Pharmacy
Tatla, Chakdaha, Nadia
Introduction
 Microspheres can be defined as solid, spherical in shape and particles size from 1 to
1000 µm. Natural polymer can also be used to form microspheres preparation like
albumin, gelatin etc. Microspheres are essentially spherical in shape, where as,
microcapsules may be spherical or non-spherical in shape.
 Controlled release is a term referring to delivery of compounds in response to time.
Drug profile Exipients profile
• Gellan gum
• Sodium alginate
• Malic anhydride
• Aluminium chloride
• Chloroform
• Name- Ibuprofen
• IUPAC Name- (RS)-2-(4-(2-
methylpropyl)phenyl)propanoic acid
• Melting Point- 76⁰ C
• Use- Analgesic , Antipyretic ,
Osteoarthritis
Materials
For preparation of standard curve of ibuprofen
Sl. No. Chemicals
1 Ibuprofen
2 Hydrochloric Acid
3 Potassium dihydrogen phosphate
4 Sodium Hydroxide
5 Water
For preparation of ibuprofen microsphere
Sl. No. Chemicals
1 Gellan gum
2 Sodium alginate
3 Malic anhydride
4 Aluminium chloride
5 Chloroform
6 Water
7 Ibuprofen
Aim and objective of the study
 AIM:
The aim of the present work is formulation and evaluation of ibuprofen
microsphere.
OBJECTIVE:
1. Formulation of ibuprofen microsphere using different cross linking agent like
Malic anhydride , Aluminium chloride.
2. To reduce toxicity of ibuprofen.
3. Evaluation of drug entrapment efficiency , swelling behaviour , in vitro
release studies , particle size determination.
Method
Sodium Alginate (0.5 gm) + Water
(40 ml)
Gellan Gum (0.5 gm) + Water
(40 ml)
Mixed 2 polymer Ibuprofen (0.5 gm) + Chloroform (10 ml)
Drug polymer solutionWater (70 ml) + Malic Anhydride (1
gm) OR Aluminium Chloride (1 gm) OR
Malic Anhydride (1 gm) & Aluminium
Chloride (1 gm)
Ibuprofen Microsphere
Formulatio
n code
Sodium
alginate
[%w/v]
Gellan
gum
(gm)
Ibuprofen
(gm)
Malic
anhydride
(gm)
Aluminium
chloride
(gm)
F1 0.5 0.5 0.5 1
F2 0.5 0.5 0.5 1
F3 0.5 0.5 0.5 1 1
Evaluation study
 Drug entrapment efficiency:
 Swelling behaviour:
 In vitro release studies:
 Particle size determination:
Results and discussion
Standard curve of ibuprofen
Concentration (µg/ml) Absorbance
2 0.1047
4 0.1491
6 0.2169
8 0.2675
10 0.3245
y = 36.785x - 1.844
R² = 0.9934
0
2
4
6
8
10
12
0 0.05 0.1 0.15 0.2 0.25 0.3 0.35
Concinmg/ml
Abs at nm
In vitro release studies
Time F1 % release F2 % release F3 % release
0 0 0 0
15 5.59 0.00 0.0
30 14.23 5.15 5.5
45 19.13 13.74 9.7
60 31.27 14.42 12.9
75 44.80 19.90 20.9
90 56.44 26.44 27.9
105 65.40 31.99 32.7
120 72.41 35.43 42.7
135 77.04 36.66 46.2
150 79.89 40.35 56.9
165 83.82 46.92 61.5
180 93.68 51.42 68.4
0
10
20
30
40
50
60
70
80
90
100
110
0 60 120 180 240 300 360
%release
Time in minutes
F1
F2
F3
Swelling indices
Code Dry Weight (gm) Swelling Index (%)
F1
0.12 200.0
F2
0.13 115.4
F3
0.12 166.7
0
50
100
150
200
250
F1 F2 F3
SwellingIndex(%)
Code
Swelling…
Microscopic analysis
Code Size
F1
160 µm to 190 µm
F2
150 µm to 160 µm
F3
150 µm to 170 µm
Entrapment efficiency
Code % Entrapped
F1 82.7
F2 97.6
F3 88.4
Conclusion
From this experiment, we have come to know that the formulation with aluminium chloride as a cross
linker (F2) is the better formulation than the other formulation. Swelling of F2 was least while the
entrapment was the maximum 97.6% recorded by the formulation F2 and the In-vitro release of F2
batch is approximately 50% over 3 hours.
Reference
1. D. Brahmankar and BS jaiswal, controlled release medication, biopharmaceutics and pharmacokinetics - A treatise, vallabh prakashan, 2010;
397–511.
2. KD tripathi essentials of medicinal pharmacology, jaypee brother edicinal publishers (P) ltd, 2014; 199-200.
3. P. K. Vinodbhai, M.C. Gohel, R.K. Parikh, S. Bariya and R. N. Suthar. Sustained release floating microspheres of acyclovir: formulation,
optimization, characterization and in vitro evaluation. Into J of drug development & research, 2011; 2(1): 242-251.
4. P. K. Vinodbhai, M.C. Gohel, R.K. Parikh, S. Bariya and R. N. Suthar. Sustained release floating microspheres of acyclovir: formulation,
optimization, characterization and in vitro evaluation. Into J of drug development & research, 2011; 2(1): 242-251.
5. H. B. Samal, S. Dey, D. Kumar, D. Sandeep kumar, S.A. Srinivas and V. Rahul,. Formulation, charcterization and in-vitro evaluation of
floating microspheres of nateglinide. Int J of pharma and bio sciences, 2011; 2(1): 147-156.
6. B. Chinna gangadhar, R. Shyam sunder, V. Vimal kumar, M. Sleeva raju and M. Sai kiran. Formulation and evaluation of indomethacin
microspheres using natural and synthetic polymers as controlled release dosage forms. Int J of drug discovery, 2010; 2(1): 8-16.
7. J. Hamdani, J. Goole, A.J. Mo¨es, K. Amighi. In vitro and in vivo evaluation of floating riboflavin pelletsdeveloped using the melt pelletization
process. Int J of pharmaceutics, 2006; 323: 86-92.
Formulation and evaluation of Ibuprofen Microsphere

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Formulation and evaluation of Ibuprofen Microsphere

  • 1. FORMULATION ANDEVALUATION OFIBUPROFEN MICROSPHERE Submitted by- SHOUVIK MONDAL ROLL NO. - 1740113045, 7th SEMESTER Under the Gidence of Dr. Sudipta Das Netaji Subhas Chandra Bose Institute of Pharmacy Tatla, Chakdaha, Nadia
  • 2. Introduction  Microspheres can be defined as solid, spherical in shape and particles size from 1 to 1000 µm. Natural polymer can also be used to form microspheres preparation like albumin, gelatin etc. Microspheres are essentially spherical in shape, where as, microcapsules may be spherical or non-spherical in shape.  Controlled release is a term referring to delivery of compounds in response to time.
  • 3. Drug profile Exipients profile • Gellan gum • Sodium alginate • Malic anhydride • Aluminium chloride • Chloroform • Name- Ibuprofen • IUPAC Name- (RS)-2-(4-(2- methylpropyl)phenyl)propanoic acid • Melting Point- 76⁰ C • Use- Analgesic , Antipyretic , Osteoarthritis
  • 4. Materials For preparation of standard curve of ibuprofen Sl. No. Chemicals 1 Ibuprofen 2 Hydrochloric Acid 3 Potassium dihydrogen phosphate 4 Sodium Hydroxide 5 Water For preparation of ibuprofen microsphere Sl. No. Chemicals 1 Gellan gum 2 Sodium alginate 3 Malic anhydride 4 Aluminium chloride 5 Chloroform 6 Water 7 Ibuprofen
  • 5. Aim and objective of the study  AIM: The aim of the present work is formulation and evaluation of ibuprofen microsphere. OBJECTIVE: 1. Formulation of ibuprofen microsphere using different cross linking agent like Malic anhydride , Aluminium chloride. 2. To reduce toxicity of ibuprofen. 3. Evaluation of drug entrapment efficiency , swelling behaviour , in vitro release studies , particle size determination.
  • 6. Method Sodium Alginate (0.5 gm) + Water (40 ml) Gellan Gum (0.5 gm) + Water (40 ml) Mixed 2 polymer Ibuprofen (0.5 gm) + Chloroform (10 ml) Drug polymer solutionWater (70 ml) + Malic Anhydride (1 gm) OR Aluminium Chloride (1 gm) OR Malic Anhydride (1 gm) & Aluminium Chloride (1 gm) Ibuprofen Microsphere Formulatio n code Sodium alginate [%w/v] Gellan gum (gm) Ibuprofen (gm) Malic anhydride (gm) Aluminium chloride (gm) F1 0.5 0.5 0.5 1 F2 0.5 0.5 0.5 1 F3 0.5 0.5 0.5 1 1
  • 7. Evaluation study  Drug entrapment efficiency:  Swelling behaviour:  In vitro release studies:  Particle size determination:
  • 8. Results and discussion Standard curve of ibuprofen Concentration (µg/ml) Absorbance 2 0.1047 4 0.1491 6 0.2169 8 0.2675 10 0.3245 y = 36.785x - 1.844 R² = 0.9934 0 2 4 6 8 10 12 0 0.05 0.1 0.15 0.2 0.25 0.3 0.35 Concinmg/ml Abs at nm
  • 9. In vitro release studies Time F1 % release F2 % release F3 % release 0 0 0 0 15 5.59 0.00 0.0 30 14.23 5.15 5.5 45 19.13 13.74 9.7 60 31.27 14.42 12.9 75 44.80 19.90 20.9 90 56.44 26.44 27.9 105 65.40 31.99 32.7 120 72.41 35.43 42.7 135 77.04 36.66 46.2 150 79.89 40.35 56.9 165 83.82 46.92 61.5 180 93.68 51.42 68.4 0 10 20 30 40 50 60 70 80 90 100 110 0 60 120 180 240 300 360 %release Time in minutes F1 F2 F3
  • 10. Swelling indices Code Dry Weight (gm) Swelling Index (%) F1 0.12 200.0 F2 0.13 115.4 F3 0.12 166.7 0 50 100 150 200 250 F1 F2 F3 SwellingIndex(%) Code Swelling…
  • 11. Microscopic analysis Code Size F1 160 µm to 190 µm F2 150 µm to 160 µm F3 150 µm to 170 µm Entrapment efficiency Code % Entrapped F1 82.7 F2 97.6 F3 88.4
  • 12. Conclusion From this experiment, we have come to know that the formulation with aluminium chloride as a cross linker (F2) is the better formulation than the other formulation. Swelling of F2 was least while the entrapment was the maximum 97.6% recorded by the formulation F2 and the In-vitro release of F2 batch is approximately 50% over 3 hours.
  • 13. Reference 1. D. Brahmankar and BS jaiswal, controlled release medication, biopharmaceutics and pharmacokinetics - A treatise, vallabh prakashan, 2010; 397–511. 2. KD tripathi essentials of medicinal pharmacology, jaypee brother edicinal publishers (P) ltd, 2014; 199-200. 3. P. K. Vinodbhai, M.C. Gohel, R.K. Parikh, S. Bariya and R. N. Suthar. Sustained release floating microspheres of acyclovir: formulation, optimization, characterization and in vitro evaluation. Into J of drug development & research, 2011; 2(1): 242-251. 4. P. K. Vinodbhai, M.C. Gohel, R.K. Parikh, S. Bariya and R. N. Suthar. Sustained release floating microspheres of acyclovir: formulation, optimization, characterization and in vitro evaluation. Into J of drug development & research, 2011; 2(1): 242-251. 5. H. B. Samal, S. Dey, D. Kumar, D. Sandeep kumar, S.A. Srinivas and V. Rahul,. Formulation, charcterization and in-vitro evaluation of floating microspheres of nateglinide. Int J of pharma and bio sciences, 2011; 2(1): 147-156. 6. B. Chinna gangadhar, R. Shyam sunder, V. Vimal kumar, M. Sleeva raju and M. Sai kiran. Formulation and evaluation of indomethacin microspheres using natural and synthetic polymers as controlled release dosage forms. Int J of drug discovery, 2010; 2(1): 8-16. 7. J. Hamdani, J. Goole, A.J. Mo¨es, K. Amighi. In vitro and in vivo evaluation of floating riboflavin pelletsdeveloped using the melt pelletization process. Int J of pharmaceutics, 2006; 323: 86-92.