Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride

Prabhakara Prabhu, Ravi Malli, Marina Koland, K Vijaynarayana, Ullas D'Souza, Nm Harish, Cs Shastry, Rn Charyulu

Research output: Contribution to journalArticle

Abstract

INTRODUCTION: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water.

MATERIALS AND METHODS: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats.

RESULTS: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets.

CONCLUSIONS: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.

Original languageEnglish
Pages (from-to)99-104
Number of pages6
JournalInternational Journal of Pharmaceutical Investigation
Volume1
Issue number2
DOIs
Publication statusPublished - 04-2011

Fingerprint

Polymers
Dosage Forms
Tablets
Hypersensitivity
Catalepsy
Polyvinyl Alcohol
Seasonal Allergic Rhinitis
Tensile Strength
Histamine Antagonists
Leukocytosis
Haloperidol
Deglutition
Nose
Biological Availability
levocetirizine
Milk
Weights and Measures
Water
Pharmaceutical Preparations
Hypromellose Derivatives

Cite this

Prabhu, Prabhakara ; Malli, Ravi ; Koland, Marina ; Vijaynarayana, K ; D'Souza, Ullas ; Harish, Nm ; Shastry, Cs ; Charyulu, Rn. / Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride. In: International Journal of Pharmaceutical Investigation. 2011 ; Vol. 1, No. 2. pp. 99-104.
@article{7bd0e987aa52452092c4edff484b39f4,
title = "Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride",
abstract = "INTRODUCTION: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water.MATERIALS AND METHODS: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats.RESULTS: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets.CONCLUSIONS: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.",
author = "Prabhakara Prabhu and Ravi Malli and Marina Koland and K Vijaynarayana and Ullas D'Souza and Nm Harish and Cs Shastry and Rn Charyulu",
year = "2011",
month = "4",
doi = "10.4103/2230-973X.82417",
language = "English",
volume = "1",
pages = "99--104",
journal = "International Journal of Pharmaceutical Investigation",
issn = "2230-973X",
publisher = "Wolters Kluwer Medknow Publications",
number = "2",

}

Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride. / Prabhu, Prabhakara; Malli, Ravi; Koland, Marina; Vijaynarayana, K; D'Souza, Ullas; Harish, Nm; Shastry, Cs; Charyulu, Rn.

In: International Journal of Pharmaceutical Investigation, Vol. 1, No. 2, 04.2011, p. 99-104.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride

AU - Prabhu, Prabhakara

AU - Malli, Ravi

AU - Koland, Marina

AU - Vijaynarayana, K

AU - D'Souza, Ullas

AU - Harish, Nm

AU - Shastry, Cs

AU - Charyulu, Rn

PY - 2011/4

Y1 - 2011/4

N2 - INTRODUCTION: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water.MATERIALS AND METHODS: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats.RESULTS: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets.CONCLUSIONS: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.

AB - INTRODUCTION: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water.MATERIALS AND METHODS: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats.RESULTS: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets.CONCLUSIONS: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.

U2 - 10.4103/2230-973X.82417

DO - 10.4103/2230-973X.82417

M3 - Article

VL - 1

SP - 99

EP - 104

JO - International Journal of Pharmaceutical Investigation

JF - International Journal of Pharmaceutical Investigation

SN - 2230-973X

IS - 2

ER -