Formulation and Evaluation of Fast Dissolving Tablet of Clopidogrel
Mahesh PG1*, Raman S. G.2
1Department of Pharmaceutics, School of Pharmaceutical Sciences, Vels Institute of Science Technology and Advanced Studies, Pallavaram, Chennai 600117.
2Department of Chemistry, School of Pharmacy, Sri Balaji Vidyapeeth Deemed to be University,
Puducherry, India.
*Corresponding Author E-mail: pgmahesh83@gmail.com
ABSTRACT:
Aim: Clopidogrel is used to treat heart attack and strokes in persons with heart disease (recent heart attack). It helps keep blood flowing smoothly in your body. Objective: Difficulty in swallowing (dysphasia) is a common problem of all age groups, especially the elderly and pediatrics, because of physiological changes associated with these groups. Conculsion: In the present work it has been observed from all formulations of Precompression and post compression studies were given within the limit of values. The in vitro dissolution data, F1 (combination of different superdisintegrants) formulation was found that the drug release is best and the cumulative % of drug release was 90.88 % respectively, when compared to other formulation.
KEYWORDS: Clopidogrel, dysphasia, superdisintegrants, cumulative.
INTRODUCTION:
Recent developments in technology have presented viable alternatives for the patients who may have difficulty in swallowing tablets or liquids.
EXPERIMENTAL METHODS:
PRE-FORMULATION STUDIES:
Pharmaceutical method substances.
STANDARD CURVE OFCLOPIDOGREL:
Sodium hydroxide solution, 0.2M
8gm of sodium hydroxide was dissolved in 1000ml distilled water and it gives 0.2M solution.
STANDARD CURVE OF CLOPIDOGREL:
Table No.1: Standard curve of Clopidogrel in Phosphate buffer (pH 6.8)
|
S. No |
Concentration(μg /ml) |
Absorbance (290nm) |
|
1 |
0 |
0.00 |
|
2 |
2 |
0.264 |
|
3 |
4 |
0.416 |
|
4 |
6 |
0.636 |
|
5 |
8 |
0.864 |
|
6 |
10 |
1.248 |
Fig 1: Standard curve of Clopidogrel in Phosphate buffer (pH 6.8)
METHOD OF PREPARATION:
Preparation of Clopidogrel tablets:
Direct Compression Technique:
Each Tablet wt. – 200mg.
PRECOMPRESSION STUDIES OF POWDER BLENDS:
Angle of Repose θ = Tan-1 (h/r)
Where,
θ = Angle of repose,
h = Height of the powder cone,
r = Radius of the powder cone.
Table No 2: Different formulation of clopidogrel fast dissolving tablets
Table no2:Different formulation of clopidogrel fast dissolving tablets
|
S. No |
Formulation Code |
Drug |
SSG |
CCS |
Mannitol |
Sodium Saccharin |
Magnesium Stearate |
Mint flavor |
|
1 |
F1 |
150 |
10 |
- |
30 |
5 |
5 |
q. s |
|
2 |
F2 |
150 |
- |
10 |
30 |
5 |
5 |
q. s |
|
3 |
F3 |
150 |
5 |
10 |
25 |
5 |
5 |
q. s |
|
4 |
F4 |
150 |
- |
5 |
35 |
5 |
5 |
q. s |
|
5 |
F5 |
150 |
5 |
- |
35 |
5 |
5 |
q. s |
Table no: 3 Precompression studies of powder blending
|
S. No |
Formulations |
Hardness Test (kg/cm) |
Thickness Test (cm) |
Friability Test (%) |
% of Weight variation test |
Estimation of Drug Content |
|
1 |
F1 |
2.64 |
0.35 |
0.126 |
99.5 |
96.22 |
|
2 |
F2 |
2.15 |
0.35 |
0.312 |
99.7 |
95.99 |
|
3 |
F3 |
2.52 |
0.35 |
0.285 |
99.8 |
97.64 |
|
4 |
F4 |
3.82 |
0.35 |
0.198 |
99.7 |
96.47 |
|
5 |
F5 |
2.25 |
0.35 |
0.234 |
99.7 |
95.48 |
Table No.4: Post compression studies of Clopidogrel fast dissolving Tablets
|
S. No |
Formulations |
Bulk Density (gm/cm3) |
Tapped Density (gm/cm3) |
Angle of Repose (θ) |
Carr's Index (%) |
Hausner's Ratio |
|
1 |
F1 |
0.414 |
0.398 |
32.56 |
9.53 |
1.315 |
|
2 |
F2 |
0.335 |
0.465 |
35.55 |
7.52 |
1.159 |
|
3 |
F3 |
0.355 |
0.412 |
32.82 |
9.29 |
1.256 |
|
4 |
F4 |
0.382 |
0.397 |
31.38 |
6.68 |
1.357 |
|
5 |
F5 |
0.343 |
0.385 |
33.27 |
8.21 |
1.005 |
FigNo2: FTIR spectrum of SSG
Figure No.3: FTIR spectrum of SSG
Table No.5:Formulations-1(F1)
|
Time (MINS) |
Absorbance (290nm) |
Concentration (µg/ml) |
Amount of drug release (in 900 ml) |
% of drug release |
|
|
1 |
0 |
0.000 |
0.000 |
0.000 |
0.000 |
|
2 |
1 |
0.128 |
1.068 |
9.810 |
6.49 |
|
3 |
3 |
0.498 |
4.354 |
39.85 |
26.67 |
|
4 |
6 |
0.687 |
6.010 |
54.20 |
36.55 |
|
5 |
9 |
0.922 |
8.056 |
72.66 |
48.77 |
|
6 |
12 |
1.243 |
10.976 |
98.68 |
68.68 |
|
7 |
15 |
1.724 |
14.184 |
136.01 |
90.58 |
Figure No.4: Formulations-5 (F5)
PRE-FORMULATION STUDIES:
The present study was undertaken to formulate Clopidogrel oral dispersible tablets with three polymers namely., CCS and SSG and in combination of three Super disintegrants and by dry granulation technique.
INVITRO DRUG RELEASE STUDY:
Tablets of all the formulations were subjected for invitro release studies. The results are presented. in Table no. (5).
DISCUSSION:
Fast dissolving tablets of Clopidogrel were prepared by direct compression method. Microscopic examination of tablets from each formulation batch showed circular result.
CONCLUSION:
In the present work it has been observed from all formulations of Precompression and post compression studies were given within the limit of values.
REFERENCES:
1. Sudarsan S. Fast Dissolving Drug Delivery System, JAMA India. 2001; 4(10): 27-31.
2. Habib W, Khankari R, Hontz J. Fast dissolving drug delivery system: Critical Review In Therapeutics, Drug Carrier Systems. 2000; 17(1): 61-72.
3. Lorenzp-Lamosa ML, Cuna M, Vila-Jato JL, Torres D. Fast dissolving drug delivery system: An Update, J Microencapsul. 1997; 14: 607.
4. Chaudhary P D, Chaudhary S P, Lanke S D and Patel Nakul T K. Formulation and in vitro evaluation of taste masked Orodispersible dosage forms of Levocetrizine dihydrochloride, Indian J. Ph arm. Educ. Res. 2007; 41: 319-327.
5. Avani J and Amin F. Emerging Trends in the development of orally disintegrating tablet technology- A Review, Pharma.Tech. 2006; 4: 26-32.
6. Shailesh Sharma R and Gupta G D. Formulation and characterization of fast dissolving tablets of Promethazine theoclate, Asian Journal of Pharmaceutics. 2008; 16: 70-72.
7. SandipanKundu P K and Sahoo K. Recent trends in the developments of orally disintegrating tablet technology, Pharma Times. 2008; 40: 11-15.
8. Panigrahi D, Baghel S and Mishra B. Mouth dissolving tablets: A over view of preparation techniques, evaluation and patented technologies, Journal of Pharmaceutical Research,2005; 49: 33-38
Received on 21.09.2019 Modified on 19.12.2019
Accepted on 01.02.2020 © RJPT All right reserved
Research J. Pharm. and Tech 2020; 13(9):4084-4086.
DOI: 10.5958/0974-360X.2020.00721.0