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

Dextromethorphan Hydrobromide.

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, Dextromethorphan Hydrobromide. 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 Dextromethorphan, 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

Dextromethorphan Hydrobromide (CAS 125-69-9) is a white or almost white crystalline powder, soluble in alcohol and chloroform, sparingly soluble in water, and practically insoluble in ether.

The structural formula for dextromethorphan hydrobromide is as follows:

Dextromethorphan is an opioid antitussive substance that exerts a depressant action on the medullary cough centre, thereby elevating the cough threshold. It does not possess analgesic, respiratory-suppressant or psychomimetic properties in therapeutic doses.

The present invention relates to a taste masked Dextromethorphan 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 Dextromethorphan 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) Taste masking Dextromethorphan by coating with polymer.
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.

Example 1:
Table 1: Dextromethorphan sugar lozenges
SI. No. Ingredients Qty/tab (mg)
1 Dextromethorphan HBr 5.0
~ Ethyl cellulose/PoIyvinyl pyrrolidone/Methacrylie Acid ~ <_
Copolymers (Binder)
3 Fructose 600-800
4 Sodium citrate 3-5 - Aspartame/Sucralose/Sodium saccharin/Acesulfame « ,
potassium
6 Flavour 2-4
7 Magnesium stearate 10-20
8 Colour 3-5

Example 2:
Table 2: Dextromethorphan sugar-free lozenges
SI. No. Ingredients Qty/tab (mg)
1 Dextromethorphan HBr 5.0
~ Ethyl cellulose/Polyvinyl pyrrolidone/ Methacrylic Acid 9 <.
Copolymers (Binder)
3 Mannitol/ Sorbitol Powder/Isomalt/Dextrose monohydrate 600-800
4 Sodium citrate 3-5 <. Aspartame/Sucralose/Sodium saccharin/Acesulfame » -
potassium
6 Flavour 2-4
7 Magnesium stearate 10-20
8 Colour 3-5

The prepared lozenges were evaluated for various parameters like thickness, Hardness, & friability. The disintegration time was determined by in-house method.. The time taken by the lozenge to dissolve completely was determined by placing each lozenge in separate beaker containing 100 ml phosphate buffer pH 6.8 in tablet disintegration apparatus and time was noted at 37°C. Time taken to dissolve lozenges was found be around 18 min.

The prepared tablets were packed in amber glass bottles & stored at 50°C for 1 month to check any changes in the physical observations. It was found that there was no change in the appearance, colour of the product.

CLAIMS:

LA Novel Solid oral lozenges pharmaceutical compositions comprises Dextromethorphan Hydrobromide.

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.