1. FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS FOR INSOMNIA TREATMENT
J.Preethi*, P. Madhu, K. Arshad Ahmed Khan.
Department of Pharmaceutics, Center for Pharmaceutical Research (CPR),
Raghavendra Institute of Pharmaceutical Education and Research, Anantapur, A.P, India.
Abstract:
The present work is an attempt to prepare fast dissolving tablet of Zolpidem tartarte with a view to enhance the patient compliance, provide a quick onset of action for effective treatment of insomnia. Tablets were prepared by direct compression using different super disintegrants like Lycoat, Crospovidone (Polyplasdone XL-10) and Sodium starch glycolate in different concentrations such as 5, 7.5 and 10%. Aspartame and microcrystalline cellulose were used as sweetener and lubricant respectively. FTIR and DSC studies showed that the drug and carriers were compatible. The Pre-compression studies indicated the excellent flow properties of bulk powder and results are within an acceptable range of pharmacopoeia specifications. The prepared tablets were evaluated for hardness, friability, content uniformity, water absorption ratio, in-vitro dispersion time, in-vitro disintegration time and in-vitro dissolution studies. The results of post compression evaluations were found to be satisfactory. The drug release from FDT increased with increasing the concentration of super disintegrants. The best formulation F3 containing 10% crospovidone disintegrated with in 14 sec and released up to 99.64% of drug in 10 min. Thus results conclusively demonstrated rapid disintegration of the formulated tablet in oral cavity with good mouth feel.
INTRODUCTION:
Zolpidem tartrate is a sedative hypnotic and belongs to the class of Selective Benzodiazepines GABA-A receptor agonist. This is to encourage calmness or to produce sleep for people who are subject to states of emotional tension and uneasiness hence, there raises a need to provide fast action. This drug is suitable candidate as it has rapid absorption from the gastroinestinal tract and a short elimination half-life (2-2.6 hrs).
METHODOLOGY:
Preparation of fast dissolving Tablets:
Fast dissolving tablets, each conatianing 10 mg zolpidem tartarte were prepared by direct compression using different super disintegrants like Crospovidone (F1, F2, F3), Sodium starch glycolate (F4, F5, F6) and Lycoat (F7, F8, F9).
Evaluation of FDT tablets:
Precompressional characterization of powder blend: Angle of repose, loose bulk density, tapped bulk density, % compressibility index and Hausner’s ratio.
Post compressional evaluations: Weight variation, Hardness, thickness, friability, drug content, in-vitro dispersion time, in-vitro disintegration time and in vitro dissolution studies.
In vitro dissolution study:
The drug release rate from fast dissolving tablets was studied using the USP (II) dissolution test apparatus. The assembly is kept in a jacketed vessel of water maintained at 37±0.50C. The beaker is filled with 900ml of phosphate buffer pH 6.8. The paddle was maintained at 75rpm, at various time intervals 5 ml samples were withdrawn and analysed by U.V spectrophotometer at 239 nm.
RESULTS AND FINDINGS:
COMPOSITION OF ZOLPIDEM TARTARTE FAST DISSOLVING TABLETS
Ingredients
(mg/tablet)
Formulation Codes F1 F2 F3 F4 F5 F6 F7 F8 F9
Zolpidem tartarte 10
Crospovidone 5
7.5 --
Sodium starch glycolate
Lycoat
Microcrystalline cellulose 83
80.5 78
Mg. Stearate
1.5
Aspartame
0.5
Formulation code
Micromeritic properties of powder blend
Post compressional evaluation of fast dissolving tablets.
Angle of repose ()
Compressibility (%)
Hausner’s ratio
Hardness (kg/cm2)
Friability (%)
Thickness (mm)
Drug content (mg)
%Weight variation
in-vitro dispersion time (sec)
in-vitro disintegration time (sec) F1
24.71°±0.33
16.41±0.026
1.196±0.011
4.46±0.14
0.3493
2.49±0.03
8.855±0.146
5.76±1.712
20.63±1.148
20.43±0.65 F2
26.12°±0.89
17.99±0.025
1.218±0.03
4.66±0.20
0.2451
2.55±0.01
8.988±0.022
6.29±0.671
18.63±1.51
17.64±1.15 F3
24.21°±0.28
13.23±1.023
1.152±0.014
4.40±0.13
0.3291
2.62±0.03
8.933±0.023
6.29±1.183
16.33±1.24
14.38±2.19 F4
28.16°±1.025
15.49±0.015
1.183±0.011
4.30±0.23
0.2647
2.47±0.01
8.965±0.136
6.31±1.121
30.67±1.23
29.63±2.13 F5
29.17°±1.89
16.17±0.011
1.192±0.015
4.41±0.21
0.2834
2.53±0.04
9.215±0.061
5.41±2.531
22.64±1.43
25.30±1.69 F6
28.91°±1.535
15.94±0.021
1.189±0.02
4.70±0.21
0.3261
2.51±0.05
8.977±0.023
5.64±1.663
26.34±0.86
20.63±1.48 F7
29.68°±1.99
19.71±0.033
1.245±0.015
4.72±0.23
0.2888
2.65±0.03
9.585±0.125
6.01±1.225
28.54±0.66
25.50±1.16 F8
26.51°±0.995
16.666±0.015
1.200±0.011
4.21±0.12
0.2537
8.945±0.067
5.43±2.133
20.50±1.12
20.53±0.61 F9
24.26°±0.22
14.149±0.020
1.169±0.01
4.45±0.16
0.3123
8.953±0.021
5.62±1.60
17.44±1.24
17.53±1.12
Zolpidem tarterate
Zolpidem tarterate
Formulation F-3
Formulation F-3
CONCLUSION:
From the study it can be concluded that zolpidem tartarte fast dissolving tablets of desired release were obtained by using crospovidone as polymer at a concentration of 10% in formulation F-3. The relative efficiency of these superdisintegrants to improve disintegration and dissolution rates of tablets was in order Crosspovidone> Sodium starch glycolate >Lycoat.
ACKNOWLEDGMENTS:
The authors greatly acknowledge Spectrum pharmaceuticals, India for providing the gift samples of Zolpidem tartarte. We are greatly thankful to our collage management for providing suitable facilities for carrying out the work.