FIELD OF THE INVENTION

This present invention relates to a troche composition which imparts a favorable oral
sensation.

Further the invention relates to novel the torche formulation which contains Dichlorobenzyl
alcohol and Amylmetacresol.

BACKGROUND OF THE INVENTION

Lozenges are tablets that dissolve or disintegrate slowly in the mouth to release drug into the saliva. They are easy to administer to paediatric and geriatric patients and are useful for extending drug form retention within the oral cavity. They usually contain one or more ingredient in a sweetened flavoured base.

Drug delivery can be either for local administration in the mouth, such as anaesthetics, antiseptics, and antimicrobials or for systemic effects if the drug is well absorbed through the buccal lining or is swallowed. More traditional drugs used in this dosage form include phenol, sodium phenolate, benzocaine, and cetylpyridinium chloride. Decongestants and antitussives are in many over - the - counter (OTC) lozenge formulations, and there are also lozenges that contain nicotine (as bitartrate salt or as nicotine polacrilex resin), flurbiprofen (Strefen), or mucin for treatment of dry mouth.

Lozenges can be made by molding (Pastilles) or by compression (Troches) at high pressures, often following wet granulation, resulting in a mechanically strong tablet that can dissolve in the mouth. Compressed lozenges (or troches) differ from conventional tablets in that they are nonporous and do not contain disintegrant. As the formulation is designed to release drug slowly in the mouth, it must have a pleasant taste, smoothness, and mouth feel. The choice of binder, filler, color, and flavour is therefore most important. Most hard - candy - type lozenges (Pastilles) contain sugar, corn syrup, acidulant, colorant, and flavors.

The administration of disinfectant substances (such as Cetylpyridinium chloride, Dequalinium chloride, Dichlorobenzyl alcohol, Amyl metacresol etc) or antibiotic substances with topical action (such as Tyrothricin or Fusafungine) has been used for a long time in the treatment of some conditions of infective origin (bacterial or fungi) typical of the oropharyngeal cavity and of the periodontal areas.

The topical administration of the various active ingredients is performed by means of the pharmaceutical forms conventionally employed for the topical use in the oropharynx, such as tablets, Mouthwashes, tinctures, sugar or no-sugar lozenges.

The present invention relates to lozenges based on sugar or no-sugar excipients, obtained with the technology described herein, containing active ingredients with topical action for use in the pharyngo-oral cavity.

The conventional troches impart coarse and powdery feelings, and thus are not favorably accepted by patients.

In view of this situation, extensive studies were undertaken to develop troches which are not coarse or powdery, but give a favorable feeling when administered.

DETAILED DESCRIPTION OF THE INVENTION

Dichlorobenzyl alcohol is chemically known as 2, 4- dichlorobenzenemethanol. Its molecular formula is CvHeCbO and the molecular weight is 177.03.
It has the following chemical structure:

It's a white or almost white, crystalline powder and very slightly soluble in water, very soluble in ethanol (96 per cent).

Dichlorobenzyl alcohol is an antiseptic used in the treatment of minor infections of the mouth and throat. It destroys or inhibits microorganisms on living tissue, having the effect of limiting or preventing the harmful results of infection. However, the presence of the antibacterial agent in this product has not been shown to have a beneficial effect on the severity or duration of a sore throat.

Amylmetacresol (53043-14-4) is an antiseptic used to treat infections of the mouth and throat. Amylmetacresol is 5-methyl-2-pentylphenol.
LI

It is a clear or almost clear liquid or a solid crystalline mass, colourless or slightly yellow when freshly prepared, which darkens on storage. The pure substance melts at 24°C, and boils between 137 to 139°C. It is soluble in water, ethanol, acetone, ether, and oil. AMC exhibits low toxicity.

The present invention relates to a taste masked Dichlorobenzyl alcohol and Amylmetacresol formulation in the form of compressed lozenges (troche composition) which imparts a favorable oral sensation. An attempt was made to formulate and evaluate lozenges of Dichlorobenzyl alcohol and Amylmetacresol using different sugars, flavours & colours for optimization.

The pharmaceutical compositions according to the present invention are in the form of compressed lozenges containing sugar (Saccharose, Fructose, or other crystallizable sugars) or without sugar, based on polyalcohols (Sorbitol, Xylitol, Mannitol, Isomalt, Maltitol and the like) in combination with artificial sweeteners(Aspartame, Sucralose, Saccharin, Neotame, Acesulfame K, Cyclamate).

According to the present invention, the process for preparation of said lozenges comprises the following steps:


a) Granulating Dichlorobenzyl alcohol and Amylmetacresol, Mannitol/Glucose and microcrystalline cellulose with binder solution.
b) Dry the wet mass till required LoD is achieved.
c) Mill the dried granules using suitable mesh.
d) Lubricate the dried sifted granules with remaining materials.
e) Compress the lubricated granules at high hardness using suitable punch set.

CLAIMS:

1. A Novel Solid oral lozenges pharmaceutical compositions comprises Dichlorobenzyl alcohol and Amylmetacresol.

2. A novel solid oral lozenges of claim 1, comprises of Sweetner, Binding agent, Colours and Flavours.

3. A novel solid oral lozenges of claim 2, wherein sugar is selected from Sugar
(Sucrose, Glucose, Dextrose, Fructose), Sugar Alcohols
(Sorbitol, Xylitol, Mannitol, Maltitol, Erythritol, Isomalt, Lactitol, Glycerol) or Artificial

Sweeteners (Aspartame, Sucralose, Saccharin, Neotame, Acesulfame K, Cyclamate).

4. A novel solid oral lozenges of claim 3, wherein binding agent is Ethyl cellulose/Polyvinyl pyrrolidone/ Methacrylic Acid Copolymers/ Hypromellose.

5. A novel solid oral lozenges of claim 4, wherein contain suitable Colours and Flavours.

6. A novel solid oral lozenges of claim 5, is in the form of compressed tablet.