FORMULATION DEVELOPMENT AND EVALUATION OF FAST …

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Saupure et al. World Journal of Pharmacy and Pharmaceutical Sciences

FORMULATION DEVELOPMENT AND EVALUATION OF FAST

DISSOLING TABLET OF LABETALOL HCL

Gaurav C. Saupure*, Nilesh P. Salunkhe, Sandip A. Tadavi, Sunil P. Pawar

Department of Pharmaceutic’s, P.S.G.V.P. Mandal’s, College of Pharmacy, Shahada-

425409, Dist:- Nandurbar, Maharashtra, India.

ABSTRACT

Delivery of drug is always been a challenge and is the most important

aspect in formulation. Drug are usually delivered via different delivery

systems and selection of the system depends on drug solubility, bio

available half life, site of action etc. Oral delivery is usually the

preferred route of drug administration, and there have been many

advances in controlling the release rate of a drug and its bioavailability.

Increased patient compliance is important for any Drug delivery

system. Many patients do not adhere to a regime of prescribed drugs

because of difficulty in administration or the taste of a drug. So it is

vital to ensure the convenient administration of a drug. In the present

work, fast dissolving tablet of Labetalol Hcl prepared using novel co-

proceed superdisntegrants and physical mixtures consisting of avicel

pH 102 and Ac-Di-sol in the different ratio and in vice versa. Labetalol Hcl is a drug of

choice which is used in treatment of Hypertension and Angina. Drug compatibility with

excipients was checked by FRIR studies. After examining the flow properties of the powder

blends the results are found to be with in prescribed limits and indicated good flow

properties. It was then subjected to tablet compression. All the formulation were subjected to

post compression parameters like hardness and friability and they showed good mechanical

strength and resistance. From this study, it can be concluded that dissolution rate of Labetalol

Hcl FDTs can be enhanced by the use of coprocessed superdisintegrants.

KEYWORDS: Formulation, Development, Labetalol Hcl, FAST Dissolving.

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 7.421

Volume 8, Issue 8, 1287-1306 Research Article ISSN 2278 – 4357

*Corresponding Author

Gaurav C. Saupure

Department of

Pharmaceutic’s, P.S.G.V.P.

Mandal’s, College of

Pharmacy, Shahada-425409,

Dist:- Nandurbar,

Maharashtra, India.

Article Received on

16 June 2019,

Revised on 06 July 2019,

Accepted on 27 July 2019

DOI: 10.20959/wjpps20198-14474


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INTRODUCTION

The fast dissolving tablets usually dissolve in the oral cavity within 15 seconds to 3 minutes.

In another words a fast-dissolving drug delivery system, in most cases, is a tablet that

dissolves or disintigrants in the oral cavity without the need of water or chewing.Fast

dissolving tablet also called as mouth dissolving tablet, melt-in mouth tablet, orodispersible

tablet, rapimelts, porous tablet, quick dissolving etc. Fast dissolving tablet are those when put

on tongue disintegrate instantaneously releasing the drug which dissolve or disperse in the

saliva. Faster the release of drug into solution, quicker absorption and onset of clinical effect.

Some drugs are absorbed from the mouth, pharynx and esophagus an the saliva passes down

into the stomach. In such cases, bioavailability of drug is significantly greater than those

observed dosage forms conventional tablet dosage form. The advantages of mouth dissolving

dosage form are increasingly being recognized in both industry and academics. Their

growing importance was underlined recently when European pharmacopeia adopted term

orodispersible tablet as a tablet that to be placed in the mouth where it disperses rapidly

before swallowing.[1,2]

Labetalol Hcl combines both selective, competitive, alpha-1-adrenergic blocking and

nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the

ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7

following oral and intravenous (IV) administration, respectively. The principal physiologic

action of labetalol is to competitively block adrenergic stimulation of β-receptors within the

myocardium (β1-receptors) and within bronchial and vascular smooth muscle (β2-receptors),

and α1-receptors within vascular smooth muscle. This causes a decrease in systemic arterial

blood pressure and systemic vascular resistance without a substantial reduction in resting

heart rate, cardiac output, or stroke volume, apparently because of its combined α- and β-

adrenergic blocking activity.


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MATERIALS AND METHODS

Materials: Labetalol Hcl was obtained as gift sample from Zydex Pharma limited,

Ahmedabad. All other polymers and chemicals were of either pharmaceutical or analytical

grade.

Methods

Preformulation Studies

Preformulation can be defined as investigation of physical and chemical properties of drug

substance alone and when combined with excipients. Preformulation studies are designed to

identify those physicochemical properties of drug and excipients that may influence the

formulation design, method of manufacture, pharmacokinetic and biopharmaceutical

properties of the resulting product.

1. Determination of melting point

The melting point of Labetalol Hcl was determined by melting point apparatus. The

substance under test was reduced to a very fine powder. Capillary was sealed at one end and

filled with tapping with sufficient drug (RB) powder. The thermometer was put in silver

pocket and capillary was put in capillary holder/pocket. The light button was switched ON.

The temperature was set at 0oC. The heating was continued until the drug was completely

melted and the thermometer reading was noted down. This study was performed in triplicate

(Indian Pharmacopoeia, 2014).

2. Colour

A small quantity of Labetalol Hcl powder was taken in butter paper and viewed in well

illuminated place.

3. Taste and odor

Very less quantity of Labetalol Hcl was used to taste with the help of tongue as well as

smelled to get the odor.

4. Drug Excipient Compatibility Study

FT-IR Spectroscopy

The interaction between the Labetalol Hcl and polymers were determined by using the FT-IR

spectroscopy where in infrared spectra of Labetalol Hcl, Avicel pH102, Ac-di-


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sol,Crossprovidone K 30, Lactose, Mannitol were carried out using the KBr disk method. The

scanning range was 450 to 4000 cm -1 and the resolution was 1/cm.

Preparation of calibration curve in 0.1N HCL[11]

The standard solution of pure drug was prepared in phosphate buffer (pH 6.8). The prepared

solution was scanned between 400-200 nm by UV- visible spectrophotometer (Jasco V-630).

Preparation of Phosphate buffer Solution pH 6.8

To 50 ml of 0.2 M Potassium dihydrogen phosphate in 200 ml volumetric flask, 22.4ml of 0.2

M sodium hydroxide was added and made up to the volume with water to 200ml.

Preparation of Standard Solution of Labetalol Hcl[11]

50mg drug dissolve it in 50ml methanol and from that 10ml was taken in a 100ml volumetric

flask and make up the volume up to 100ml with phosphate buffer ph 6.8.This is stock

solution of concentration 100μg/ml.

Preparation of Working Solution

From Standard solution 1, 2, 3, 4,ml and 5ml was withdrawn in 10ml volumetric flask and

diluted up to 10 ml with phosphate buffer ph 6.8. (1o-50μg/ml).Respectively solutions of

concentrations 10, 20, 30, 40, 50μg/ml was prepared. The solution was analyzed by UV

Spectrophotometer at 302 nm and results were recorded. The calibration graph was plotted as

concentration an x-axis and absorbance on y-axis.

Fig. no. 1 Calibration curve of Labetalol Hcl in 0.1N HCL.


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Preparation of Fast Dissolving Tablets

Direct Compression

It is the easiest way to manufacture tablets. Conventional equipments, commonly available

excipients and limited number of processing steps are involved in direct compression. Also

high doses can be accommodated and final weight of tablet can easily exceed that of other

production method. This technique can now be applied to fast dissolving tablets because of

the availability of improved tablet excipients, especially tablet disintegrants and sugar based

excipients. Addition of disintegrants in fast dissolving tablets, leads to quick disintegration of

tablets and hence improves dissolution. In many fast dissolving tablet technologies based on

direct compression, the disintegrants principally affect the rate of disintegration and hence the

dissolution. The introduction superdisintegrants and a better understanding of their properties

have increased the popularity of this technology.[1,3-5]

Table no. 1: Composition of different batches Fast dissolving Labetalol Hcl tablets.

Formulation code F1 F2 F3 F4 F5 F6

Labetalol Hcl 50 50 50 50 50 50

Avicel pH102 33 35 38 - - -

Ac-Di-sol - - - 1.5 2 3

Crossprovidone K30 6 9 12 6 9 12

Magneshium

stearate 4 3 5 4 3 5

Mannitol 50 50 50 50.5 50 50

Lactose 57 53 45 88 86 80

Evaluation of powder mixed blend[6,7,8]

The powder blend was evaluated for properties as follow:

1. Angle of repose

Angle of repose is defined as the maximum angle possible between the surface of pile of

powder and horizontal plane. The angle of repose was determined by the fixed funnel

method. A glass funnel was secured with its tip at a given height (H) above a piece of graph

paper placed on a horizontal surface. Powder was poured through the funnel until the apex of


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the conical pile touched the tip of the funnel. The angle of repose was calculated with the

formula,

Or

Where, is the angle of repose, h is the height of heap, and r is the radius of the heap circle .

Table 2: Flow properties and corresponding angle of repose.

Flow ability Angle of repose

degree

Excellent 25-30

Good 31-35

Fair-aid not needed 36-40

passable- must agitate 41-45

Poor-must agitate,

vibrate 46-55

Very Poor 56-65

Very, very poor > 66

2. Bulk Density

Bulk density of powder was determined by pouring gently know quantity of powder sample

through a glass funnel into graduated measuring cylinder. The volume occupied by the

sample were recorded. Bulk density was calculated using following formula.

Db = M / Vb

Where,Db = Bulk density.

M= Mass of the powder.

Vb= Bulk volume of the powder.

3 Tapped density

The powder sample was poured gently through glass funnel into graduated measuring

cylinder. Initial volume of powder was noted and the sample subjected to tapping until no

further reduction in volume was noted or the percentages of difference in volume was not

more than 2 %. Volume occupied by the samples after tapping was recorded and tapped

density was calculated using following formula.

Dt= M / Vt

Where,Dt = Tapped density.

M = Mass of the powder.


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Vt = Tapped volume of the powder

4. Compressibility index and Hausner ratio

In recent year, compressibility index and the closely related hausner ratio have become the

simple, fast and popular method of predicting powder flow characteristics. Compressibility

index has been proposed as an indirect measure of bulk density, size, shape, surface area,

moisture content and cohesiveness of materials because all of these can influence the

observed compressibility index. The compressibility index and hausner ratio are determined

by measuring both bulk and the tapped density of powder.

Dt - Db

I = × 100

tD

I = Compressibility index.

Dt = Tapped density of the powder.

Db = Bulk density of the powder.

Hausner ratio = Dt / Db

Where, Dt = tapped density.

Db = bulk density

Table 3: Scale flow ability.

Evaluation of fast dissolving tablet of Labetalol Hcl[2,9,10]

1. Weight variation test

To find out weight variation, 20 tablets of each type of formulation were weighed

individually using an electronic balance, average weight was calculated and individual tablet

weight was then compared with average value to find the deviation in weight (Indian

Pharmacopoeia 2014).

Compressibility

Index (%)1

Flow

character

Haunser

Ratio

<10 Excellent 1.00-1.11

11-15 Good 1.12-1.18

16-20 Fair 1.19-1.25

21-25 Passable 1.26-1.34

26-31 poor 1.35-1.45

32-37 Very poor 1.46-1.59

< 38 Very, very poor >1.60


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Table 4: Specifications for tablets as per Indian Pharmacopoeia – 2014.

Sr.

No. Average weight of tablet % Deviation allowed

1. 130 mg or less 10 %

2. More than 130 mg but less that mg 7.5%

3. 324 mg or more 5%

2. Friability test

Friability is the measure of tablet strength. Roche Friabilator (Meta Lab, Mumbai) was used

for testing the friability using the following procedure. This test subjects a number of tablets

to the combined effect of shock abrasion by utilizing a plastic chamber which revolves at a

speed of 25 rpm, dropping the tablets to a distance of 6 inches in each revolution. A sample

of preweighed 6 tablets was placed in Roche Friabilator which was then operated for 100

revolutions i.e. 4 minutes. The tablets were then dusted and reweighed. A loss of less than 1

% in weight in generally considered acceptable. Percent friability (% F) was calculated as

follows (Indian Pharmacopoeia 2014).

3. Hardness test

The resistance of tablets to shipping, breakage, under conditions of storage, transportation

and handling before usage depends on its hardness. For each formulation, the hardness of 6

tablets was determined using the hardness tester (Monsanto, Mumbai). The tablet was held

along its diametrical axis in between the two jaws of the tester. At this point, reading should

be zero kg/cm2. Then constant force was applied by rotating the knob until the tablet

fractured. The value at this point was noted.

4. Thickness test

Control of physical dimension of the tablets such as size and thickness is essential for

consumer acceptance and to maintain tablet to tablet uniformity. The dimension

specifications were measured using screw gauge. Twenty tablets were randomly selected

from formulations and thickness was measured individually. It was expressed in millimeter

and average was calculated.


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5. Wetting time

Wetting time corresponds to the time taken for the tablet to disintegrate when kept motionless

on the tongue. Wetting time is closely related to the inner structure of the tablets and to the

hydrophilicity of the excipient. A piece of tissue paper folded double was placed in a petri

plate (internal diameter is 10 cm) containing 10 mL of water. The tablet was placed on the

paper and the time for complete wetting of the tablet was measured in seconds. The method

was slightly modified by maintaining water at 37 ˚C.

6. Disintegration test

The standard procedure of performing disintegration test for these dosage forms has several

limitation and they do not support the measurement of very short disintegration times. The

disintegration time for FDT needs to be modified as disintegration is required without water

thus the test should mimic disintegration in salivery contents. For these purpose a petridish

(10 cm diameter) was filled with 10 ml of water. The tablet was carefully put in the petridish

and for tablet to completely disintegrate into fine particle was noted.

7. In-vitro dissolution study

In-vitro dissolution studies for all the fabricated of Labetalol Hcl were out using USP

apparatus type II at 50 rpm. The dissolution medium used was 6.8 phosphate buffer (900ml)

maintained at 37 ± 0.5 ˚C.

Aliquots of dissolution media were withdrawn (5 ml) at different interval and content of

Labetalol Hcl was measured by determine absorbance at 303 nm. 5 ml aliquot was withdrawn

at the 1 min, 2 min …. To be continued at the 5 min. intervals and filtered by whatman filter

paper, suitably diluted and analyzed at 302 nm using UV cisible spectrophotometer.

An equal volume of fresh medium, which was pre- warmed at 37˚C, was replaced in to the

dissolution medium after each sampling to maintain the constant volume throughout the test.

RESULT AND DISCUSSION

Preformulation Study

Determination of Melting Point

The observed melting point of API was found to be 181-182°C by using Thiele’s tube

method.


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Determination of colour, odour,taste

These test was performed as per procedure given in material and method. The result are

illustrated in following.

Table 5: Organoleptic properties of Labetalol Hcl.

Drug –Polymer Compatibility Studies by FTIR

From the observations of FTIR peaks it was concluded that all the polymers used in the

formulation were compatible with drug and also with each other.

Formulation development

The IR spectrum show the peaks at following value, which are characterstic for the drug. The

FTIR spectra of Labetalol Hcl are show in below Fig. respectively.

Fig no. 2: IR Spectra Of Labetalol Hcl.

Test Observation

Color White

Taste Bitter

Odor Odorless


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Fig no. 3: IR Spectra of Avicel pH 102.

Fig no. 4: IR Spectra of Ac-di-sol.

Fig no. 5: IR Specta of Labetalol Hcl + Avicel pH 102.


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Fig no. 6: IR Spectra of Labetalol Hcl + Ac-di-sol.

Evaluation of prepared blend

All the formulations wre evaluated for pre-compression such as Angle of repose, Bulk

density, Tapped density, Compressibility index and Hausner’s Ratio. Result obtained is

shown in the Table. 6

1. Bulk density and tapped density

The loose bulk density and tapped bulk density for all the formulation varied in range of

0.510gm/cm3

and 0.616 gm/cm3

to 0.650 gm/cm3

recpectively . The value obtained lies within

the accepable range and with not much difference found between loose bulk density and

tapped bulk density. These result may further influence property such as compressibility and

tablet dissolution. Both loose bulk density and Tapped bulk density results are shown in

Table 6.

2. Compressibility index and Hausner’s ratio

The percent compressibility and hausner’s ratio for all formulation lies within the range of

13.33 to 19.38 and 1.154 to 1.240 respectively. All the formulation shows acceptable

compressibility and flow property. The percent compressibility of powder mix was

determined by Carr’s compressibility index are shown in Table 6.


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3. Angle of repose

The value of angle of repose of all the formulation were found to be in range of 260

28, to 320

02’ indicating acceptable flow property and this was further supported by lower

compressibility index value. The Angle of repose results are shown in Table 6.

Table 6: Evaluation of physical properties.

Formulation

Batches

Physical properties*

Loosebulk

density Tapped bulk

density Compressibility

Index (%) Hunser’s

ratio Angle of

repose

F1 0.523±0.005 0.630±0.08 16.98±0.260 1.204±0.004 32002’±0.20

F2 0.529± 0.006 0.644±0.06 17.86±0.165 1.217±0.002 31008’±0.24

F3 0.514± 0.004 0.632±0.07 18.67±0.265 1.229±0.004 30650’

±0.106

F4 0.534± 0.006 0.623±0.08 19.38±0.070 1.240±0.001 29048’±0.15

F5 0.510± 0.005 0.623±0.08 18.14±0.245 1.221±0.003 28068’±0.103

F6 0.514± 0.005 0.615±0.07 13.33±0.70 1.154±0.002 26028’±0.12

*All the value represent mean ± Standard deviation (n=3)]

Evaluation of prepared tablet

All Tablet formulations (F1 to F6) were evaluated for different parameter such as thickness,

hardness, weight variation, drug content and friability. Physical evaluation of tablets from all

batches showed flat circular shape with no cracks with yellowish color. The thickness of

tablets ranged from. The evaluation parameters such as weight variation, hardness, friability

and thickness were carried out for the tablets. The results revealed that there was no

variations in weight of the tablets as all tablets were found to be within the range limit for

weight variation. The thickness was found to be 3.72 to 3.95 mm. and the hardness of tablets

was found to 3.27 to 4.37 k g/cm2 which is the required hardness for fast disintegrating

tablets. Thus, uniformity in thickness and hardness was observed. All the tablets showed %

friability in the range of 0.291 to 0.678 % which was within the limit. All the batches

complied with.

Table 7: Standard Physical tests for FDT.

Formulation

Batches

Physical properties*

Hardness(kg/cm2)

Percent

friability Thickness(mm)

Content

uniformity (%) Wt.

variation

F1 4.25 ±0.264 0.440 ±0.007 3.82 ± 0.11 100.52±0.2 Passes

F2 4.27 ±0.153 0.288 ± 0.35 3.95 ± 0.09 99.86±1.4 Passes

F3 4.37 ±0.128 0.660 ±0.015 3.85 ± 0.05 98.98±0.6 Passes

F4 4.11±0.220 0.541 ±0.026 3.82 ± 0.11 98.82±0.7 Passes

F5 3.27±0.18 0.497 ±0.008 3.85 ± 0.09 100.44±12 Passes

F6 3.91± 0.296 0.625 ±0.010 3.86 ± 0.05 99.96±0.5 Passes


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*All the value represent mean ± Standard deviation (n=3)

1. In-vitro drug release studies

The In-vitro drug release characteristics were studied in phosphate buffer 6.8 pH for 25 min

using IP type 1 dissolution apparatus.

In-vitro dissolution data of formulation showed that, formulation F1, F2 and F3 released

98.578%, 98.283% and 98.434% drug respectively within20-25 min. Formulation F4, F5 and

F6 released 98.769%, 98.454% and 99.273% respectively within 20-25 min.

Table 8: in vitro dissolution data of formulation F1, F2, and F3.

Figure 7: in vitro dissolution studies of formulation F1, F2 and F3.

Time

in

min

Percentage cumulative drug release*

F1 F2 F3

0 0 0 0

5 24.620 26.724 28.181

10 55.674 52.125 60.712

15 77.375 73.470 75.298

20 84.778 89.937 88.004

25 98.578 98.283 98.434


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Table 9: in -vitro dissolution data of formulation F4, F5, and F6.

Time

in

min

Percentage cumulative drug release*

F4 F5 F6

0 0 0 0

5 28.505 27.696 27.048

10 58.933 57.957 58.925

15 77.069 75.930 75.288

20 90.118 91.569 93.346

25 98.769 98.454 99.273

Figure 8: in- vitro dissolution studies of formulation F4, F5, and F6.

Comparative dissolution profile of fast dissolving Labetalol Hcl in pH 6.8 buffer

solution

Table 10: Comparative percent cumulative drug release of F1-F6.

Time

minutes

Percent cumulative drug release

F1 F2 F3 F4 F5 F6

0 0 0 0 0 0 0

5 24.620 26.724 28.181 28.505 27.696 27.048

10 55.674 52.125 60.712 58.933 57.957 58.925

15 77.375 73.470 75.298 77.069 75.930 75.288

30 84.778 89.937 88.004 90.118 91.569 93.346

25 98.578 98.283 98.434 98.769 98.454 99.273


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Figure 9: in- vitro dissolution profile of all formulation F1-F6 in pH 6.8 phosphate

buffer.

2. In-vitro disintegration time, wetting time, dispersion time and mouth feel of

formulated tablet

The disintegration time for formulation F1-F6 was found to be in the range of 21.02 to 42 .38

sec. The wetting time for formulation F1-F6 was found to be in the range of 28.38 sec. to

48.44 sec the water absorption ratio for formulation F1-F6 was found to be in the range of

85.16 to 90.01%, this reflects that the optimum concentration of superdisintegrant, rapidly

disintegration, wetting and more water absorption ratio.

Table 11. In-vitro disintegration time, wetting time water absorption ratio and mouth

feel of formulated tablet.


Formulation

batches

Parametrs*

Disintegration

time (sec) Wetting time

Water

absorption

ratio (%)

Mouth Feel

F1 42.38±1.90 48.44±3.055 85.16±3.15 Good

F2 36.05±1.55 41.52±2.825 87.16±3.08 Good

F3 34.10±2.60 40.96±2.115 88.10±2.67 Good

F4 31.15±1.40 37.15±2.180 87.14±285 Good

F5 29.58±1.55 35.08±1.935 87.09±1.74 Good

F6 21.02±0.90 28.23±1.840 90.01±1.49 Good


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Figure 10: Disintegration time of F1-F6.

Figure 11: Wetting time of F1-F6.


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Figure 12: Water absorption ratio(%) of F1-F6.

3. Accelerated Stability study

In which, effect of temperature and humidity was determined at 40 ºC ± 2 ºC/75% ± 5% RH

maintained in environmental stability chamber for three month. Evaluation was done after 0,

30, 60 and 90 days. The results were tabulated in table 12.

Table 12: Effect of temperature and humidity on optimized batch (F3).

Parameters Days

0 30 60 90

Appearance smooth smooth smooth smooth

Hardness (kg/cm2)

(mean ± SD)* 4.37 ±0.128 4.33 ± 0.01 4.34 ± 0.09 4.25 ± 0.11

DT (sec) (mean ±

SD)* 34.10±2.60 34.20± 0.26 34.24 ± 0.49 34.30± 0.25

Uniformity of

content (%) (mean

± SD)*

98.98±0.46 97.97 ± 0.89 97.62 ± 0.67 97.04 ± 0.73


Table 13: Dissolution study of formulation F6 before and after stability.

Time (hrs) Percentage cumulative release

Before S.S After S.S

0 0 0

5 27.048 26.488

10 58.925 57.898

15 75.288 74.224

20 93.346 92.255

25 99.273 98.887


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Stability studies of optimized batch F6 was carried out by placing the sample at 40 ±20C/75 ±

5% RH for the period of one month. There is no significant change in release characteristics

and physicochemical properties of the tablets used in the release study. Based on the results it

can be concluded that the formulated fast dissolving tablets was stable at high temperature

and relative humidity over a period of 1 month. Even though its stability is assured for one

month, further studies at different temperatures and humidity condition are needed to

establish its shelf- life.

CONCLUSION

The demand for fast dissolving tablets has enormously increased during the last decade,

particularly for geriatric and pediatric patient who have difficulty in swallowing conventional

tablets and capsules. Oral administration of the drugs is difficult in patients having

concomitant vomiting or diarrhea. Fast dissolving or fast disintegrating dosage form is

advantages for such patient. Fast dissolving or fast disintegrating dosage from are meant to

disintegrate immediately upon contact with the saliva leading to faster release of the dugs in

the oral cavity. Labetalol HCl combines both selective, competitive, alpha-1-adrenergic

blocking and nonselective, competitive, beta-adrenergic blocking activity in a single

substance. In man, the ratios of alpha- to beta- blockade have been estimated to be

approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively.

Using Labetalol Hcl, Avicel pH-102 directly compressible Ac-Di-sol was selected as

diluents. Crosprovidone k-30 were selected as superdisintegrants. Magneshium stearate and

lactose were selected as lubricant and glidant respectively. Mannitol was added as a a

sweetening agent.

ACKNOWLEDGEMENT

The Author and Co-author are thankful to P.S.G.V.P.M’s College of pharmacy, Department

of Pharmaceutics, Shahada, Dist.Nandurbar for continuous support and encouragement

throughout this project work and wish to thank friends.

REFERENCE

1. P.M. Dandagi V.S. Mastiholimath ; S.A. Srinivas, “Oro-dispersdible tablets; new-fangled

drug delivery system –A review” Inian j. pharm. Educ. Res., 2005; 39(4): oct-dec, 177-

181.

2. Leon lachman, Herbert A. Liberman, Joseph I. Kanig, “The Theory And Practice of

Industrial Pharmac”, 3rd ed, 293-295.


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3. Kuchekar B.S, Badhan A.C., Mahajan H.S. “Mouth dissolving tablet: A novel drug

delivery system” pharma times: 2003; 6(35): 7-9.

4. Panigrahi D, Baghel S, Mishra B, “Mouth dissolving tablet: An Overview of preparation

techniques, evaluation and patented technologies” journal of pharmaceutical research:

2006; 4(7): 33-38.

5. “Fast dissolving drug delivery system” a Litature from pharmpedia.

6. Sukulj, Vensa; Sirca, Judia; Jenko Osel, “Fast disintegrating a tablet” United states

application no. 20060115528, june 2006.

7. Moen Md, “Sumatriptan fast-disintegrating/rapid-release tablet” Keating gm drugs 2006;

66(6): 2-891.

8. Dandagi P.M L Sreenivas S A: Manvi F V, “Taste masked ofloxacin mouth disintegrating

tablet” Indian drugs: 2005; 42(1): 53-55.

9. Sathses Kumar E, Senthil Kumar B, Gopalakrishna B : Formulation and evaluation of fast

dissolving tablet of aceclofenac. International journal of pharmaceutical sciences. May-

august 2010; 2(3): 810-821.

10. Tejash serasiya, Shailesh koradia, subhash vaghani, n.p.jivanil : Design, optimizization

and in vitro evaluation of orodispersible tablet of pheniramine malate. International

journal of pharmaceutical research and development-online. Vol-1/ issue-10 / des / 004.

1-18.

11. Mohd Mirasuddin Hilal, Md. Mumtaz Hussain,Sara Shreen, Formulation and Evaluation

of Labetalol Hcl Fast dissolving talet. AJPT: 2013; 3(5): (410-412).

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