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 lmax 342 nm
• Linearity range 10-50 mg/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
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.