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Carvedilol FDT
Carvedilol FDT
BY
PADMA,
IV B.PHARMACY
OBJECTIVES
To obviate the demerit of pill swallowing difficulty in case of geriatrics, fast dissolving tablets are preferred. Present study aimed at developing the fast dissolving tablets for a poorly soluble drug with low bioavailability due to its first pass effect. Development of FDT based on a effective drug-cyclodextrin complex system. Concept of fast dissolving tablets may overcome the first pass metabolism. Solubility enhancement obtained by complexation with cyclodextrins. Increasing solubility may substantially contribute the enhancement of absorption consequently bioavailability.
PLAN OF WORK
Literature review Selection of drug and polymers Procurement of materials Preformulation studies Preparation and characterization of drug-cyclodextrin complexes using different concentrations of F-CD and HP-F-CD.
y y y
Optimization of type and ratio of cyclodextrin Formulation and evaluation of carvedilol FDT
y y y y y
MATERIALS
Carvedilol F-cyclodextrin (F-CD) Hydroxypropyl- F-cyclodextrin (HP-F-CD) Dichloromethane Methanol Mannitol Sodium starch glycolate Crosspovidone Crosscarmellose sodium Magnessium stearate Talc
EXPERIMENTAL METHODOLOGY
A UV spectrophotometric method based on the measurement of absorbance at 242 nm in 0.1N HCl, was used in the present study for the estimation of carvedilol.
1.0000 y = 0.0993x + 0.0087 R = 0.9992 0.6167
Absorbance
0.9887 0.8097
0.8000
0.0000 0 2
Concentration (g/ml)
10
% Drug Released
80
60
40
20
Procedure:
y
Required quantities of drug and excients were weighed accurately and passed through sieve #40 and were compressed in to tablet by direct compression technique. Formulae given below
Ingredients C-HP CD(1:1) Sodium starch glycolate Crospovidone Croscarmellose sodium Mannitol Magnessium stearate Talc
Parameter
CFDT 1
CFDT 2
CFDT 3
CFDT 4
CFDT 5
CFDT 6
CFDT 7
CFDT 8
CFDT 9
Hardness (kg/cm
3.5
3.5
Friability (%)
0.2
0.2
0.2
0.2
0.2
0.2
0.2
0.2
0.2
Disintegration (min)
6.4
5.7
5.4
2.7
2.9
5.1
4.4
3.4
4.5
4.7
5.9
2.3
5.6
Solid state of inclusion complexes were characterized by phase solubility studies and were confirmed by FTIR analysis.
The drug content is uniform and dissolution enhancement efficacy is in the order of HP-F-CD> F-CD.
Inclusion complexes of carvedilol with HP-F-CD (1:1) were found by dissolution studies to be superior due to its greater hydrophilicity and higher wetting ability.
Fast dissolving tablets prepared employing optimized concentration of cyclodextrin complexes of carvedilol with HP-F-CD (1:1) with different ratios of superdisintegrants.
In-vitro dissolution study shows the tablet formulation CFDT 5 containing drug: HPF-CD in the ratio of 1:1 binary system with 8% cross povidone as super disintegrent showed excellent dissolution profile 99.81% in 45 minutes when compared to other formulations as well as marketed formulation.
The wetting time and disintegration time of these tablets is 2.3 and 2.7 minutes respectively, the DE (30%) value is 3.17 and T50 (min) value is only 22minutes.
CONCLUSIONS
Carvedilol fast dissolving tablet was developed and optimized, CFDT 5 containing C-HP CD (1:1) employing 8% of crospovidone showed better dissolution rate i.e 99.81% in 45 min when compared to other formulations.
Wetting
and
disintegration
times
are
in
the
order
of
Results of in vitro dissolution study are in agreement with the disintegration values observed.
FDT containing co-precipitated drug with HP CD satisfied with all the requirements for rapid dissolving , allowing more than 85% drug dissolved within 30 min.
Enhancement of dissolution rate may result in the increase of its bioavailability with the possibility of reducing drug dose and side effects.
REFERENCES
1.
Dong-han won et al. Improved physicochemical characteristics of carvedilol solid dispersion particles by super critical anti-solvent precipitation process international journal of pharmaceutics 2005; 30(1): 199-208. Dario leonardi et al. Development of predisolone: poly ethylene glycol 6000 fast release tablets from solid dispersions: solid-state characterization, dissolution behaviour, and formulation parameters Aaps pharm sci tech. 2007; 8(4): 108. Omaima A. sammour et al. Formulation and optimization of mouth dissolve tablets containing carvedilol solid dispersion Aaps pharm sci tech 2006; 7(2): 55.
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