primaquin taste msking- c.d

8/3/2019 Primaquin Taste Msking- C.D.

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LOGO

FORMATION AND EVALUATION OF TASTE MASKED ORAL

RECONSTITUTABLE SUSPENSION OF PRIMAQUINE PHOSPHATE

Presented by

Vineeth Kumar Ekbote

(PTF/2011-XIV/1379/MP)M.Pharm. (2 nd semester)

Department of Pharmaceutical Technology (Formulations)

NIPER, S.A.S. Nagar, Punjab.


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FLOW OF PRESENTATION

1. Basis of Selection of Article

2. Introduction

3. Materials and Methods

4. Results and Discussion

5. Conclusion

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1. BASIS OF SELECTION OF ARTICLE

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Contd

API- Primaquine phosphate

Taste masking

Method- industrially applicable

Dosage form related parameters

Patient compliance

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2. INTRODUCTION

Objective of taste masking of drug substance is for the patient compliance,especially important in case of pediatrics.

There are several approaches for taste masking of drug substances

i. Addition of sweetening agents and flavors

ii. Coating with polymeric solutionsiii. Molecular inclusion complexes

iv. Adsorption on ion-exchange resins

v. Chemical modification to API

In above methods, taste masking by the formation of molecular inclusioncomplex with cyclodextrins is represented in this article..

The first such observation was already described in 1953 in the very first

drug/CD patent by Freudenberg et al. The bad taste of bromoisovaleryl urea

was masked by CD complexation.

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The cavity of CD is occupied by water molecules (about 1314% w/w) both

in crystalline state as well as in aqueous solution. Roughly half of this water

is so-called crystal water and the other half is inclusion water.

CD is the host molecule and an important component of the driving force

for the inclusion complex formation is the substitution of high enthalpy water

molecules by the guest molecules.

As the guest molecule is included into the CD molecule, which is

enwrapped into a hydrate shell, the interaction of the guest molecule with

cell membranes and receptors is considerably inhibited, resulting in reducedcytotoxicity or reduced taste.

Formation of inclusion complex with APIFormation of inclusion complex with API

Contd

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Primaquin phosphate

-Cyclodextrin(CD)

Methanol

Hydrochloric acid

Potassium chloride Potassium di hydrogen phosphate

Sodium hydroxide

Primaquine phosphate (PRM), an antimalarial drug that was active against

exo-erythrocyte forms of Plasmodium that is P. vivax, P. ovale and the early

pre-erythrocytic form ofPlasmodium falciparum, was used to induce radical

cures of relapsing malarias. PRM has an extremely unpleasant bitter taste.

It has been reported that PRM depolarize taste cells by closing K+ channels

and produce bitterness.

3. MATERIALS AND METHODS

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. Prepare the binary systems of API and CD in in

1:1, 1:5, 1:10, 1:15, 1:20 and 1:25 molar ratios.

Kneaded system(pass through the sieve 44)

Physical mixture(pass through the sieve 44)

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Scanning range 500-4000 cm-1

KBr pellet.

39C to 390C

Rate of 5C/min.

Cu- K source, Ni-filter,

2= 10- 30

DSC

DissolutionTemp. 37+/- 2C

50 rpm

pH6.8 & 1.2

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Contd

1 g equivalent of PRM was

dispersed in 100 ml of water

for 15 s.

About 1 ml of the dispersionin the mouth for 30 s.

Record the bitterness level

0 = tasteless

0.5 = very slightly bitter1 = slightly bitter

1.5 = slight to moderate

bitter

2 = moderately bitter

2.5 = moderate to strong

bitter

3 = strongly bitter

3+ = very strong

Twenty healthy human volunteers

23 27 years

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4. RESULTS AND DISCUSSION

a. Primaquin

b. CD

c. Physical mixture

d. Kneaded system

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Contd

a. Primaquin

b. CD

c. Physical mixture

d. Kneaded system

HeatChange

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Contd

a. Primaquin

b. CD

c. Physical mixture

d. Kneaded system

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Contd

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Contd

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5. CONCLUSION

The study conclusively demonstrated the complete masking of bitter taste of

PRM with CD in physical mixture.

The FTIR, DSC and XRPD studies indicated inclusion complexation in

physical mixture and kneaded system.

This may be of value for the pharmaceutical industries dealing with bitter

drugs to improve patient compliance and thus effective pharmacotherapy.

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primaquin taste msking- c.d

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