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Journal of Thai Traditional & Alternative Medicine Vol. 8 No. 2 May-August (Supplement) 2010 ˆ˘

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Preparation and Evaluation of Compressed Lozenges Containing

Vernonia cineria (L.) Less. Extract as Smoking Cessation Aid

Jatuporn Deengam, Somsin Suchittanonratana, Somchai Luangsanam, Ornlaksana Paeratakul

Faculty of Pharmacy, Srinakharinwirot University, Nakhon Nayok 26120, Thailand

Rationale: Tobacco smoking is recognized as a major health problem worldwide. For smokers, it is
essential to overcome the withdrawal symptoms for a successful smoking cessation. In Thailand, Vernonia
cinerea (L.) Less. (VC) has been used in traditional and complementary medicine as an aid in smoking cessation
treatment. With regard to the method of delivery, VC has generally been administered in the dosage form of
herbal tea (herbal infusion) or a decoction. In this study, compressed tablet lozenges were evaluated as an
alternative dosage form for the delivery of VC.
Objective: To prepare and evaluate compressed tablet lozenges containing water-soluble extract of Ver-
nonia cinerea (L.) Less. (VC) as smoking cessation aids.
Methods: Crude extract of VC was prepared by freeze drying an aqueous macerate of powdered herb.
Medicated lozenges containing VC extract were prepared by direct compression or wet granulation. The
lozenge formulations consisted of VC extract (active ingredient); lactose, mannitol, sucrose, xylitol (fillers and
sweeteners), aspartame (intense sweetener); peppermint oil (flavoring agent) and magnesium stearate (lubri-
cant). The prepared lozenges were evaluated for their hardness, friability, weight variation, and in vitro drug
release using USP 30 paddle apparatus. Selected formulations were assessed for their organoleptic properties
(taste, color, odor, texture/mouthfeel) by healthy volunteer smokers.
Results: With direct compression technique, the VC lozenges containing lactose as filler/sweetener had
good physical appearance but unacceptable taste and mouthfeel. Sucrose resulted in sticking problem during
compression as a result of melting whereas directly compressed mannitol lozenges had insufficient hardnesses.
In the wet granulation method, VC extract was incorporated by either intragranular or extragranular addition
whereby the extract was mixed with dried mannitol granules or dissolved in the binder solution prior to
granulation, respectively. The method of addition was found to significantly affect the physical appearance of
resultant lozenges. A more uniform distribution of VC extract was obtained when using an intragranular
addition as the active ingredient was molecularly dispersed in the binder solution prior to granulation. The drug
release from lozenges prepared by extragranular addition was slightly slower due to the larger particle size of
original VC extract. All lozenge formulations slowly dissolved/eroded and did not disintegrate during dissolu-
tion; giving a complete drug release within 30 minutes. The VC extract-containing lozenges were well accepted
by most of the volunteer smokers when compared to herbal tea as a result of their pleasant organoleptic
properties (taste, odor, mouthfeel), ease of administration and carrying convenience.
Conclusion: Compressed lozenges containing VC extract were prepared and evaluated for their physical
properties and in vitro drug release. The VC extract-containing compressed tablet lozenges could offer an
attractive alternative to currently available preparations as an aid in relieving withdrawal symptoms in smoking
cessation treatment.
Acknowledgments: This research work was supported by a grant entitled çFormulation development of
pharmaceutical preparations containing Thai herbs for smoking cessationé from Srinakharinwirot University
under the research plan çThe Development of Herbal Products for Smoking Cessation Aidsé (Grant #020/2550).