Transcript IRON SUPPLEMENTATION - Ideal Cures Pvt. Ltd.

IRON SUPPLEMENTATION
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Iron is an essential constituent of the body; necessary for hemoglobin
formation and oxidative processes of living tissues.
Iron deficiency is the most common nutritional disorder in the world.
Approximately 25% of the world’s population is iron deficient.
Studies have indicated that iron supplementation may increase
cognitive skills in children and adolescents with iron deficiency.
The major activity of supplemental iron is in the prevention and
treatment of iron deficiency anemia. A number of ferrous and ferric
salts are available for the same. However, the compliance with iron
salts is poor, mainly because of the associated metallic taste.
Iron in ferrous state is more readily absorbed by the body than in
ferric state.
COMPLIANCE OF MEDICINES IN
PEDIATRICS
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Taste is a major consideration when designing a pediatric compliant
dosage form.
‘Melt in Mouth’ solid dosage forms encompass the advantages of solid
and liquid dosage forms.
‘Melt in Mouth’ pellets or ‘Meltlets’ are :
A novel and an innovative extension of ‘Melt in mouth’ solid dosage
forms
Fast dissolving; when placed in mouth
Pleasant tasting, flavored
Unit dosage form, packed in sachets and can be directly emptied in
the child’s mouth
Can be used for administering high dose drugs
‘MELT IN MOUTH’ DOSAGE FORMS ARE A NOVEL AND AN INNOVATIVE
DOSAGE FORM AND ARE EXPECTED TO IMPROVE THE ACCEPTANCE OF
MEDICINES BY PEDIATRIC POPULATION
OBJECTIVES OF THE INVESTIGATION
 Formulation of palatable ‘Melt in Mouth’ pellets of Ferrous fumarate
that would improve the compliance of the same in pediatrics.
 Development of analytical technique for Ferrous fumarate
 Exploiting ‘Extrusion – Spheronization’, as a technique for formulating
the Melt in mouth pellets. This technique has been explored only for
the formulation of immediate and controlled release pellets.
MATERIALS USED IN THE STUDY
Ferrous fumarate
Sweetener
Novel channelizing agent
Instacoat Flavor *
Lemon Lime Flavor
Novel Disintegrant
Diluents
Spheronization aid
Flow enhancer
* Instacoat Flavor is a blend of color, flavor and a cellulosic polymer.
This is added as an excipient to mask the metallic taste of iron salt and
to increase the palatibility and aesthetic appeal of the formulation.
EQUIPMENTS USED IN THE STUDY :
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Extruder E – 65 (R. R. Enterprises)
Spheronizer S – 120 (R. R. Enterprises)
Drying Oven (Expo, EIC – IA)
IN – VITRO DISSOLUTION STUDIES:
USP Type II, 75 rpm, 900 ml Dissolution Medium
Dissolution Medium : USP pH 1.2 Hydrochloride Acid Buffer containing
0.5% w/v Sodium Lauryl Sulfate
OPTIMIZATION OF EXTRUSION - SPHERONIZATION
 Extrusion was optimized for :
 Extruder speed
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Extruder screen size
 Spheronization was optimised for :
 Spheronization speed
 Spheronization dwell time
 Formulation optimization :
 Ratio of Diluents
 Quantity of granulating medium
 Drying Time
 Quantity of Instacoat Flavor, Lemon flavor and disintegrant
FORMULATION OF THE ‘MELT IN MOUTH’ PELLETS
Drug
Sweetener
Disintegrant
Channelizing Agent
Flavour (I) Instacoat Flavour (II)
Cellulose Derivative
POWDER BLEND
Diluent
Granulation
Extrude (Extrude E – 65)
Spheronize (Spheronizer S – 160)
Dry in oven for 4 hours at 60C and fractionate (16/20 #), Add Talc
Fill in sachets
The formulated pellets were evaluated by a panel of 10 human volunteers
and the results are as indicated :
MELT IN MOUTH PELLETS (I)
Volunteers
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VIII
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Mouthfeel
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Sweetness
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Flavor
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Disintegration
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Slight
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Slight
Parameter
Taste
Aftertaste
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None
Good
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Ok
Excellent
The formulated pellets were evaluated by a panel of 10 human volunteers
and the results are as indicated :
MELT IN MOUTH PELLETS (II)
Volunteers
I
II
III
IV
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VI
VII
VIII
IX
X
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Mouthfeel
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Sweetness
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Flavor
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Disintegration
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Parameter
Taste
Aftertaste
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None
Good
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Ok
Excellent
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ANALYTICAL METHOD DEVELOPMENT
TITRIMETRY : (As per Indian Pharmacopoeia 1996)
For drug content as well as stability indicating assay.
Analysis of Ferrous Iron :
Analysis of Ferric iron:
Titrant : Ceric Ammonium Sulfate VS
Indicator : Ferroin
End Point : Red to pale blue
Standardized against : Sodium
Thiosulphate
Titrant : Sodium Thiosulphate VS
Indicator : Starch solution
End Point : Blue to colourless
Standardized against :
Potassium bromate
COLORIMETRY:
For drug content and analysis of drug in an in vitro release study.
Principle : Iron forms a red colored complex with
Thioglycollic acid in the presence of citric acid and at an
alkaline pH.