OPTIMIZATION AND EVALUATION OF IBUPROFEN TABLETS BY MADG METHOD
ABOUT AUHTORS
Devender Sharma1*, Ameya Lanjewar2
1Department of Pharmaceutics, Hi-Tech College of Pharmacy, Chandrapur India
2Department of Pharmaceutics, Kamala Nehru College of Pharmacy, Butibori Nagpur India
*sdevender350@gmail.com
ABSTRACT
Ibuprofen largely used in various disorders treatment likely to be rheumatoid arthritis, osteoarthritis and other musculoskeletal disorders, especially where pain is more prominent than inflammation. Ibuprofen is used as a simple analgesic, antipyretic and it is particularly effective in dysmenorrheal. By the process of Moisture activated dry granulation, Ibuprofen tablets prepared but these method prepared tablets do not give better drug content, drug release. So formulation optimize by full factorial i.e. change in various polymer concentration like SSG and Povidone at three different levels. Ibuprofen tablets manufactured by moisture activated dry granulation method with optimization show better drug release, drug stability in comparison of marketed preparation. Due to optimization, Ibuprofen tablets which manufactured by moisture activated dry granulation method have very low cost in comparison of marketed preparation. The main objective of this research work water poorly soluble drug like ibuprofen tablet manufactured by moisture activated dry granulation by optimize process gives better drug release, manufacture cost also less other than marketed tablets.
Reference Id: PHARMATUTOR-ART-2556
INTRODUCTION
Tablet are widely used other than dosage form of medicaments. Tablets are unit the solid dosage form of medicament or medicaments, usually circular in shape and may be biconvex or flat. Tablet have various advantages other than the dosage form, advantages like easy to administered, east to be dispensed, more stable and maintain the accuracy of dosage form. Manufacturing of tablets various step involved given below. (Devender et al., 2017)
Manufacturing of tablets |
Preparation of granules |
Compression of granules into tablets |
If required or necessary then coating |
Quality control of tablets |
In the main step preparation of granules for compression, mainly weighing the ingredients, mixing the powdered ingredients and excipients and converting the mixed ingredients into granules. Generally granules can be prepared by different method like moist granulation method, dry granulation method and granules by preliminary compression or other different method. But here now, we prepare granules by moisture activated granulation method. (Ankit et al., 2011) Moisture activated dry granulation method not largely used but effective in case of poorly water soluble drug or water insoluble drug like ibuprofen and other drug. Granulation is the process in which primary powder particles are made to adhere to form larger, multi particle aggregates called granules. (Lachman et al., 1990) Granulation is used mainly to improve flow and compressibility of powders so as to prevent segregation of the blend components to improve content uniformity, and eliminate excessive amounts of fines. Particle size of granules is mainly affected by the quantity and feeding rate. (Devender et al., 2017) Ibuprofen tablets are manufactured by moisture activated dry granulation method (following step carried out given below). (Devender et al., 2017)
Moisture Activated Dry Granulation |
Dispensing and Shifting |
Dry mixing |
Granulation |
Pre-mixing (unlubrication) |
Lubrication |
Compression |
Material and Method
Ibuprofen BP was procured as a gift sample from ZIM Laboratories Ltd, Nagpur, Maharashtra. Colloidal anhydrous silicon (Aerosil) was procured as a gift sample from ZIM Laboratories Ltd, Nagpur, Maharashtra. Maize starch was procured from ZIM Laboratories Ltd, Nagpur, Maharashtra. Lactose DC was procured from ZIM Laboratories Ltd, Nagpur. PVP K30 (Povidone) was procured from ZIM Laboratories Ltd, Nagpur, Maharashtra. Microcrystalline cellulose was procured from ZIM Laboratories Ltd, Nagpur, Maharashtra. Talcum was procured from ZIM Laboratories Ltd, Nagpur, Maharashtra. All other chemicals used were of analytical grade.
Formulation and Optimization
Optimization is the process of finding or determining the best way of using the existing or available resources while taking into accounts all of the factors that influence decisions in any experiment. It is a means of determining or finding the best possible value of a dependent variable by changing certain independent variables (those are depend upon dependent variables). This approach is time-consuming and reliable. Optimization by means of an experimental design may helpful in shortening the experimenting time. (Devender et al., 2017)
Design of experiments Factorial design was applied to design the experiments. On the basis of Preliminary trials concentration of SSG, Povidone and RPM were used as independent variables. Whereas disintegration time and %drug release, were kept as dependent variables. Formulations F1 to F9 were prepared using SSG and Povidone concentration at three different levels. The summary of the formulations is shown in table. (Ankit et al., 2011)
Independent variables |
Dependent variables |
X1= Sodium starch glycolate |
Y1= Disintegration time |
X2=Povidone |
Y2= % Drug release |
Factors and levels with their real values (Devender et al., 2017)
Factors |
Low level (-1) |
Middle level (0) |
High level (1) |
Sodium starch glycolate (mg) |
5mg |
12.5mg |
20mg |
Povidone (mg) |
1.25mg |
6.87mg |
12.5mg |
Formulations of optimized batches Ibuprofen 650mg
Batch No. |
|
Lactose DC (mg) |
Aerosile (mg) |
MCC (mg) |
Starch (mg) |
PVP K30 (mg) |
SSG (mg) |
Talc (mg) |
Magnesium stearate (mg) |
Moisture (%) |
Time (min.) |
RPM
|
F1 |
400 |
|
4 |
20 |
50 |
12.5 |
20 |
5 |
2 |
2.0 |
30 |
150 |
F2 |
400 |
|
4 |
20 |
50 |
1.25 |
20 |
5 |
2 |
2.0 |
30 |
150 |
F3 |
400 |
|
4 |
20 |
50 |
6.87 |
12.5 |
5 |
2 |
2.0 |
30 |
150 |
F4 |
400 |
|
4 |
20 |
50 |
12.5 |
5 |
5 |
2 |
2.0 |
30 |
150 |
F5 |
400 |
|
4 |
20 |
50 |
1.25 |
5 |
5 |
2 |
2.0 |
30 |
150 |
F6 |
400 |
|
4 |
20 |
50 |
6.87 |
5 |
5 |
2 |
2.0 |
30 |
150 |
F7 |
400 |
|
4 |
20 |
50 |
1.25 |
12.5 |
5 |
2 |
2.0 |
30 |
150 |
F8 |
400 |
|
4 |
20 |
50 |
6.87 |
20 |
5 |
2 |
2.0 |
30 |
150 |
F9 |
400 |
|
4 |
20 |
50 |
12.5 |
12.5 |
5 |
2 |
2.0 |
30 |
150 |
Preformulation study (Devender et al., 2017)
Flow characterization
A. Bulk density
Bulk density or apparent density is defined as the ratio of mass of a powder to the bulk volume. The bulk density of a powder depends primarily on particle size distribution, particle shape and the tendency of the particles to adhere to one another. (Lachman et al., 1990)
Procedure: A quantity of 15.0 g of drug powder or granules was passed through 20 # sieve to break any agglomerates formed during the drug storage. This quantity was introduced into a 50 ml measuring cylinder. The powder was level without compacting it and the apparent volume was measured.
Bulk density = weight of sample in gram / volume occupied by the sample |
B. Tapped density
A quantity of 15.0 g of powder or granules was passed through 20# sieve to break any agglomerates formed during storage. This quantity was introduced into a 50 ml measuring cylinder. The graduated cylinder containing a known mass of blend was tapped for a fix time. Cylinder was tapped for 500 times initially and the tapped volume (V1) was measured to the nearest graduated units repeated the tapping was repeated for additional 750 times and tapped volume (V2) was measured to the nearest graduated units. If the difference between the two volumes is less than 2 percent then volume (V2) is taken rather again tapping for additional 1250 times.
Tapped density = Wt. of sample in g / Tapped volume |
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