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Preparation and Evaluation of Fast Dissolving Tablets for an Selected Drug


METHODOLOGY-
1. SELECTION OF DRUG-

Diclofenac sodium is used to treat severe pain.It is also given in angina pectoris.It gives quick onset of action so,it is an important drug in present drug market.so, we selected diclofenac sodium for preparation and evaluation.

2. SELECTION OF EXCIPIENTS-
We used various excipients which are used in the preparation of drug.some lubricants such as Magnesium stearate and Talc are used in all four formulations.The other excipients such as MCC,Citric Acid,Menthol,SLS,Sodium CMC are used in different preparations to achieve desired properties of the preparation.

3. DRUG AUTHENTICATION-
A. Determination of melting point
B. Determination of IR Spectra

Determination of IR Spectra: ( by press pellet technique )
In this method a small amount of finely ground solid sample is intimately mixed with about 100 times its weight of powdered potassium bromide. The finely ground mixture is then passed very high pressure in a press (at 25,000 p sig) to form a small pellet (about 1-2 m thick and cm in diameter). The resulting pellet is transparent to IR radiation. Now this pellet is use to IR spectra with help of  INFRA  ABSORPTION  SPECROSCOPY

Determination of melting point:-
Melting point is determine by theil’s tube method. In this method a small theil’s tube is tied with thermometer. Now put the sample, whose melting point is determine,  in the theil’s  tube .Dip the thermometer in liquid sample which have the high melting point. On the heating  liquid sample, the temperature at which sample  melt , taken as melting point.

4. INCOMPATIBILITY STUDIES-
Incompatibility study has been done by taking drug and excipient  in ratio 1:1,and keep in oven. Change physically appearance of matrix tablet of mebendazole by keeping at 400 c for one month. There is no change physically appearance of matrix tablet

PREPARATION OF TABLET-
FORMULATION  FOR  ONE  TABLET-

INGREDIENTS

FORMOLA-1

 FORMULA-2                                         

FORMULA-3

FORMULA-4


DRUG(DICLOFENAC SODIUM)

100mg.

100mg.

100mg.

100mg.

MCC

100mg.

100mg.

100mg.

20mg.

 CITRIC ACID

50mg.

30mg.

30mg.

30mg.

MENTHOL

-

-

20mg.

-

SLS

-

20mg.

-


SODIUM CMC

-

-

-

100mg.

MAGNESIUM STEARATE

1mg.

1mg.

1mg.

1mg.

TALC

1mg

1mg.

1mg.

1mg.

BY DIRECT COMPRESSION METHOD-

PROCEDURE-
Direct compression method involves following steps

  • Blending
  • Compression

Blending Procedure For Preparation Of Mixed Blend Of Drug And Excipients
All ingredients were mixed as per the formulations.Super disintegrates were incorporated in the powder mix. And finally magnesium stearate and talc were added as lubricant. Control tablet was prepared without any super disintegrant.

Compression
MixedBlends were compressed by direct compression method using  hand operated single punch machine.

Evaluation Test For Fast Dissolving Tablet-
Tablets from all the formulation were subjected to following
quality control test.

1. General Appearance
The general appearance of a tablet, its visual identity and over all “elegance” is essential for consumer acceptance. Include in are tablet’s size, shape, colour, presence or absence of an odour, taste, surface texture, physical flaws and consistency and legibility of any identifying marking.

2. Size and Shape
The size and shape of the tablet can be dimensionally described, monitored and controlled

3. Uniformity of weight
I.P. procedure for uniformity of weight was followed, twenty tablets were taken and their weight was determined individually and collectively on a digital weighing balance. The average weight of one tablet was determined from the collective weight. The weight variation test would be a satisfactory method of determining the drug content uniformity.

Sr. No. Average weight of Tablets(mg) Maximum percentage different allowed
1 130 or less 10
2 130-324 7.5
3 More than 324 5

Table: I.P. Specification for uniformity of weight

4.Tablet hardness
Hardness of tablet is defined as the force applied across the diameter of the tablet in the order to break the tablet. The resistance of the tablet to chipping, abrasion or breakage under condition of storage transformation and handling before usage depends on its hardness. Hardness of the tablet of each formulation was determined using Monsato Hardness tester.

5. Friability
It is measured of mechanical strength of tablets. Roche fribaiator was used to determine the friability by following procedure. A preweighed tablet was placed in the fribaiator. Fribaiator consist of a plastic-chamber that revolves at 25 rpm, dropping those tablets at a distance of 6 inches with each revolution. The tablets were rotated in the friabalator for at least 4 minutes. At the end of test tablets were dusied and reweighed, the loss in the weight of tablet is the measure of friability and is expressed in percentage as %Friability = loss in weight / Initial weight x 100

6. In Vivo Dsintegration test
The test was carried out on 6 tablets using the apparatus specified in I.P.-1996 distilled water at 37ºC ± 2ºC was used as a disintegration media and the time in second taken for complete disintegration of the tablet with no palable mass remaining in the apparatus was measured in seconds.

7. Wetting time
The wetting time of the tablets was measured using a simple procedure. Five circular tissue papers of 10cm diameter were placed in a Petri dish containing water (6ml). A tablet was carefully placed on the surface of tissue paper. The time required for water to reach the upper surface of the tablet was noted as the wetting time.

8. Dissolution Studies
Dissolution was carried out by using Electro lab dissolution apparatus (USP XXI) by paddle method using 900ml of 1%w/v SLS as the medium and rotating the paddle at 50 rpm for 10 minutes. The temperature of dissolution medium was maintained at 37±20C. Aliquots were withdrawn at different time intervals of 0, 2, 4, 6, 8 and 10 minutes. And it was replaced by adding equal volumes of fresh dissolution medium. The samples were suitably diluted and absorbance of the solution was determined at 368nm by using  UV-visible spectrophotometer.

Drug release study was carried out by using specification given:-

1.    Apparatus                                      : Dissolution apparatus

2.    Dissolution                                    : 0.1 N Hcl

3.    Temperature                                 : 370 c

4.    RPM                                               : 50

5.    Vol. withdraw & replace             : 10 ml for every 30  min & later 1 hour for two sample                                                          6.    λ max                                            : 368 nm

                  7.    Blank solution                               :   0.1N Hcl

RESULT-
Data for Standard curve of Diclofenac sodium-

S.N.

Concentration (µg/ml)

Absorbance (nm)

1

10

0.310

2

20

0.728

3

30

1.1

4

40

1.42

5

50

1.75

STANDARD CURVE OF DICLOFENAC SODIUM
IR Spectra-

I.R. spectra was obtained using KBr pellet method and compared with spectra as given in Indian Pharmacopoeia.

Melting point

Parameters

Literature value

Observed value

Melting point

283 – 285

280 – 287

Incompatibility studies
EVALUATION-

PARAMETERS

FORMULA-1

FORMULA-2

FORMULA-3

FORMULA-4

HARDNESS

4.4

1.4

2.2

1.1

WEIGHT  VARIATION

1.28%

3.5%

4.55%

2.62%

FRIABILITY

.95%

0.90%

0.82%

0.75%

WETTING TIME

12.57 min.

07.35 min.

7.55 min

6.42 min.

DISINTEGRATION TEST

8.57min.

7.04 min.

6.50 min.

4.30 min.

Data for Drug release study of formulations-

TIME INTERVAL(MINUTE)

FORMULA-1

FORMULA-2

FORMULA-3

FORMULA-4

5

35

38

42

51

10

48

46

49

57

15

62

58

59

59

20

68

69

64

74

25

79

78

74

79

30

87

83

89

94

DISCUSSION
In formulation -1 we used MCC in the formulation of  Diclofenac sodium.MCC is a surfactant which is used in the preparation of Diclofenac sodium tablets due to its surface enhancing property.But we could not get the desired tablet.

So, in formula -2 we used sodium lauryl sulphate with citric acid to enhance the dissolution of the tablet.In this formulation we get the less disintegration time than formula-1.In formula-3 we used menthol which is a volatile substance.after keeping tablet in oven at 50’ c for 1 hour.after drying the menthol evaporated and left small pores on the surface of the tablet which enhance the dissolution and disintegration.In formula-4 CMC is used in the formulation because of its highly hydrophilic nature which enhance dissolution and disintegration and we get the desired formulation.

References
1. Lieberman H. A., Lachman L. & Kanig L. J. Theory & Practice of Industrial Pharmacy, 3rd Edition, Varghese Publishing House, Mumbai, 2008; 412-428.
2. Tripathi K.D. Essentials of Medical Pharmacology, 6th Edition, Jay Pee Publishers, New Delhi, 2008; 193.
3. Indian Pharmacopoeia, Vol.-I, The Controller of Publication, Delhi, 1996; 135.
4. Jain N.K. Advance in Controlled & Novel Drug Delivery System, 4th Edition, Vallabh Prakashan, New Delhi, pg. No. 3-4 & 107
5. Vyas SP, Khar RK. Controlled drug delivery: Concepts an advances:drug delivery; p.411-476.

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