Asthma

1. Asthma
 Most common chronic illness of childhood, affecting approximately
10% children.
 Available preventive therapies for persistent asthma include inhaled
delivery system containing corticosteroids and long acting beta
agonists.
 Adherence with inhaled therapies is poor in pediatrics.
 Orally active leukotriene receptor antagonists are shown to be
effective in pediatric patients.

2. Montelukast sodium
 Indications: Prophylaxis and treatment of asthma, exercise induced
asthma, in Aspirin sensitive asthamatics.
 Potent, selective and orally acting leukotriene receptor antagonist.
 Acts by inhibiting physiological actions of LTC4, LTD4 and LTE4 at the
Cystiene Leukotriene levels (Cys LT1 receptor).
 Dose: Adults :- 10 mg OD Child 6-14 yrs:- 5 mg OD
2-5 yrs :- 4 mg OD
 Rapid oral absorption with mean oral bioavailability of 64 %.

3. Objective of incevtigation
 Formulation palatable mouth dissolve tablets of Montelukast Sodium.
 Evaluate the efficacy of Ion exchange resin (Indion 414) as
superdisintegrant over the extsting ones in mouth dissolve tablets.

4. Melt in Mouth Tablets
These are solid dosage forms that dissolve or disintegrate within a
Minute in the oral cavity without the need of water or chewing and
have a pleasant taste.
Advantages offered
 Ease of swallowing
 Ease of handling
 Improved patient compliance
 Line extension and lifecycle management.

5. Ion Exchange Resins
 Safe for oral consumption.
 Indion 414 is a water insoluble, chemically crosslinked acrylic
copolymer matrix with carboxylic acid as functional group (Potassium
form).
 Swelling property of ion exchange resins makes them ideal candidate
as superdisintegrants.

6. Analytical Method Development
UV Spectrophotometric method for analysis of Montelukast Sodium
Detection λmax 342 nm
Linearity range 10-50 µg/ml
Slope ± SD 0.0194 ± 0.0014
Regression coefficient 0.999

7. Formulation Development
 Montelukast Sodium was mixed in geometric proportions with
superdisintegrants, sweetners, diluent, flavors and lubricants. Various
concentrations of superdisintegrants were employed to arrive at an
optimum disintegration time.
 Blend was screened through 40 #.
 Compressed on Cadmach single station tablet press machine equipped
with 9 mm flat beveled punches.

8. Formulation details of melt in mouth
tablets of Montelukast Sodium
The tablet weight was fixed to 150 mg.
Montelukast Sodium Active
Aspartame Sweetner
Avicel PH102 Diluent
Indion 414 Superdisintegrant
Menthol Coolant
Instacoat Strawberry flavor Flavor
Supplied by Ideal Cures Pvt Ltd.
Talc Lubricant
Magnesium stearate Anti adherent
Aerosil Glidant

9. Comparison of Indion 414 with
existing superdisintegrants
Superdisintegrants
Appearance of
tablet
In-vitro disintegration
time (sec)
Indion 414 Smooth 20
Sodium Starch Glycolate Smooth 15
Croscarmellose sodium Smooth 15
Crospovidone Pitted 10

10. Evaluation of the Optimized
Formulation
Parameter Observation
Appearance Flat beveled tablets off white in color
Texture Smooth
Taste Palatable
Dimensions 9 mm in diameter
Weight variation (mg) ± SD 150 ± 2.87
Hardness (kg/cm2
) 3-4
In-vitro disintegration time (sec) 20
Drug content (%) 101.2% ± 1.34
Drug release (%)
Apparatus – USP Type II
Medium – 500 ml Water 95%
rpm – 100, Time – 30 min

11. Conclusion
 Patient compliant and palatable melt in mouth tablets of Montelukast
Sodium having optimum physicochemical properties were formulated.
 Ion exchange resin (Indion 414) could be successfully used as
superdisintegrant, thus making the formulation cost effective.
 The tablets exhibited an in-vitro disintegration time of 20 seconds.
 The technology can also be easily employed for large-scale
manufacturing.

12. Acknowledgements
The authors thank
 Ideal Cures Pvt. Ltd. for providing financial assistance towards this
presentation and also for gift samples of Instacoat flavors.
 Cipla Ltd, Mumbai for gift sample of Montelukast Sodium.
 Ion Exchange India Ltd for gift sample of Ion Exchange resin.