MOUTH DISSOLVING TABLET

Dhanaji . K . Chavan

(M-Pharm, Sem-III)

Under the guidance of

Prof. Mr. Nandgude T. D.

Padm.Dr D.Y.Patil I.P.S.R. Pimpri, Pune.

content

a. Introduction

b. Aim

c. Objective

d. Need of work

e. Plan of work

f. Experiental: Material and method

g. Evaluation

h. References

Introduction

The oral route of drug administration is the most and convenient

for patient use. Novel oral drug delivery systems that dissolve or disperse

quickly in a few seconds after placement in the mouth without water can

alleviate the problem of swallowing tablets, and active medicament easily

get absorbed into the blood circulation

Ideal Properties of MDT

(i) should be dissolve or disintegrate in the mouth (in saliva) within seconds.

(ii) not require any liquid or water to show its action,

(iii) Be compatible with taste masking and Have a pleasing mouth feel.

(v) The excipients should have high wettability, and the tablet structure should

also have a highly porous network.

(vi) It should not leave Leave minimal or no residue in the mouth

(vii) less effective by environmental conditions like humidity, temperature etc.

(viii) More rapid drug absorption from the pre-gastric area i.e. mouth, pharynx

and oesophagus which may produce rapid onset of action.

(ix) Be adaptable and amenable to existing processing and packaging

machinery.

( x) Allow high drug loading

(xi) Have sufficient strength to withstand the rigors of the manufacturing

process and post manufacturing handling.

Limitations of mouth dissolving tablets

The tablets usually have insufficient mechanical strength

The tablets may leave unpleasant taste and/or grittiness in mouth if

not formulated properly.

Drugs with relatively larger doses are difficult to formulate into

MDT

e.g. antibiotics like amoxicillin with adult dose tablet

containing about 500 mg of the drug.

Patients who concurrently take anticholinergic medications may not be

the best candidates for MDT.

Similarly patients with dryness of the mouth due to decreased saliva

production may not be good candidates for these tablet formulations

Difficulties with existing oral dosage form

(i) Patient may suffer from tremors therefore they have difficulty to

take powder and liquids. In dysphasia physical obstacles and

adherence to an esophagus may cause gastrointestinal ulceration.

(ii) Swallowing of solid dosage forms like tablet and capsules and

produce difficulty for young adult of incomplete development of

muscular and nervous system and elderly patients suffer from

dysphasia.

(iii) Liquid medicaments (suspension and emulsion) are packed in multi-dose

container; therefore achievement of uniformity in the content of each dose

may be difficult.

(iv) Buccal and sublingual formation may cause irritation to oral mucosa, so

patients refused to use such medications.

(v) Cost of products is main factor as parenteral formulations are most costly

and discomfort.

Criteria for drug selection

(i) It should not have bitter taste.

(ii) The dose should be less than 20 mg.

(iii) Molecular weight should be small to Moderate.

(iv) Should be of good solubility in water and saliva.

(v) It should have Partially non ionized at the oral cavities pH.

(vi) Should have extensive First pass metabolism.

(vii) Should have oral tissue permeability.

Aim and objective

Aim

The aim of this study was to prepare mouth dissolving tablets of

meloxicam after its increasing solubility by solid dispersion method and to

evaluate the tablet for hardness, Disintegration, Wetting time, Friability,

Content Uniformity and invitro dissolution study,

Objective

The major problem of Meloxicam is its very low solubility in

biological fluids. The results revealed that it is possible to enhance the

dissolution rate of Meloxicam by increasing the surface area of the drug by

solid dispersion method.

Literature review

Need of work

The major problem of Meloxicam is its very low solubility in

biological fluids. The results revealed that it is possible to enhance the

dissolution rate of Meloxicam by increasing the surface area of the drug or

by solid dispersion method.

Plan of work

Literature review

Procurement of drug and excipients

Characterization of drug and excipients.

Preparation of calibration curve for drug.

Prepration of solid dispersion of using by kneading method.

Evaluation of solid dispersion .

i. SEM .

ii. DSC.

iii. Appearance

iv. Percent transmittance.

v. Drug content determination.

vi. Percent drug entrapment.

vii. In vitro drug release.

Preparation of tablets containing solid dispersions of drug.

Evaluation of tablet for

I. Weight variation

II. Hardness and friability

III. Thickness

IV. Wetting time

V. Drug content

VI. In vitro Disintegration

VII. In vitro Dissolution

Experimental: Material and method

Analysis of Drug

1. Organoleptic properties:

The drug powder was analyzed for colour and odour..

2. Description:

The drug sample was analyzed for physical appearance and

powder nature.

3. Melting point:

The melting point of was found out by capillary method using

programmable melting point apparatus.

4. Solubility:

The solubility ofwas checked in distilled water and other

organic solvent at room temperature for 24 hours using rotary shaker.

5. Infra -red Spectrum:

IR absorption spectrum of was recorded by potassium bromide

dispersion technique. Drug and potassium bromide was mixed uniformly

and filled into the die cavity of sample holder and an IR spectrum was

recorded using FTIR spectrophotometer (FTIR-8400 S)

6. U.V. Spectroscopy:

a) 10 mg of drug 100 ml

volumetric

flask

. Drug was

dissolved in

methanol (25ml)

and diluted to

100 ml with

water

a stock

solution of

meloxicam of

100 μg/ml

was prepared

in distilled

water

solution was

diluted with

water to

produce a

solution of

concentration

8 μg/ml.

UV

spectrum

was

recorded

in the

range

200-400

nm.

calibration

(standard)

curve was

carried out at

the

wavelength of

maximum

absorption (λ

max).

Same procedure is to be followed for dilution with 0.1N HCL and

phospate buffer solution

Material

Name

Method

Enhancing the solubility of drug by kneading method

Active drug with suitable polymer in different ratios is added to the

mortar and triturated with small quantity of ethanol to prepare a slurry.

Slowly the drug is incorporated into the slurry with constant trituration.

The prepared slurry is then air dried at 25oC for 24hrs. The resultant

product is pulverised and passed through sieve no. 80 and stored in

dessicator over fused calcium chloride

Preparation of tablets containing solid dispersions of drug

by sublimation

Evaluation

All prepared tablets were evaluated for

Hardness,

Thickness

Friability,

Disintegration time,

Invitro dissolution

Wetting time,

drug content and stability studies.

a) Hardness

Pfizer hardness tester was used for the determination of the hardness of the tablets.

The tablet was placedmin contact between the plungers and the handle was pressed,the

force of the fracture was recorded

b) thickness of tablets

were recorded during the process of compression

usingCalipers(Mitotoyo;Japan)

c) Frability

The friability of the tablets was determined using a Roche Friabilator

by taking two tablets from each batch and accurately weighed and placed

in the Friabilator then operated for 100 revolutions .Then the tablets were

dedusted and reweighed .Percentage friability was calculated using the

formula,

F= (1‐wo/w )*100.

d) Disintegration

In the disintegration time study, the tablets were taken and introduced

in each tube of disintegration apparatus, and the tablet rack of the

disintegration apparatus was positioned into a 1 litre beaker containing

900ml of distilled water and time of disintegration was recorded at 37±2º

C.

e) Wetting time

In the wetting time study, a piece of tissue paper folded twice was

placed in a petridish (with internal diameter 6.5cm) containing 5ml of

distilled water. A tablet was placed on the paper and the time for complete

wetting of the tablet was measured in seconds.

f) Drug content

For drug content analysis a total 10 tablets were weighed and powdered

.The powder equivalent to 7.5mg of Meloxicam was taken and dissolvedin

phosphate buffer pH 7.4 .After that an aliquot of the filtrate was diluted

and analysed spectrophotometrically (UV 1700 Shimadzu

Corporation.Japan) at 360 nm .

g) Stability study

The stability study of the tablets was carried out according to ICH

guidelines .

h) Invitro release studies

The invitro dissolution study was carried out in the USP dissolution test

apparatus USP type 2(paddle). 900 ml of the dissolution medium was

taken in vessel and the temperature was maintained at 37 ± 0.5oC. The

speed of the paddle was set at 50 rpm. 5ml of the dissolution medium was

withdrawn and the same amount of freshmedium was replenished to the

dissolution medium.

The sample withdrawn was filtered and diluted prior to analysis in the

UV Spectrophotometer .

References