FORM 2
THE PATENT ACT 1970
(39 of 1970)
&
The Patents Rules, 2003
PROVISIONAL SPECIFICATION
(See section 10 and rule13)
1. TITLE OF THE INVENTION:
"Rimonabant mouth dissolving tablets"
2. APPLICANT
(a) NAME: Lyka Labs Limited.
(b) NATIONALITY : Indian Company incorporated under the
Indian Companies ACT, 1956
(c) ADDRESS: 101, Shivshakti Industrial Estate, Andheri-Kurla Road,
Andheri (East), Mumbai - 400059, Maharashtra, India.
3. PREAMBLE TO THE DESCRIPTION
The following specification particularly describes the invention:

Technical field of the invention
The present invention relates to a pharmaceutical composition comprising a CB1 cannabinoid receptor antagonist, Rimonabant, and a process for preparing the same. In particular it relates to a pharmaceutical composition comprising Rimonabant in the form of mouth dissolving tablet as an adjunct to diet and exercise for the treatment of obese patients
Background of the Invention
Obesity is a serious and growing public health problem as excessive body weight has been shown to predispose to various diseases such as cardiovascular diseases, diabetes mellitus type 2, sleep apnea, gal bladder disease, depression, certain types of cancers (e.g. endometrial, breast, prostate, and colon) or osteoarthritis. Obesity and overweight is typically defined by body mass index (BMI), which is correlated with total body fat and estimates the relative risk of disease. BMI is calculated by weight in kilograms divided by height in meters squared (kg/m ). Overweight is typically defined as a BMI of 25 - 29.9 kg/m and obesity is typically defined as a BMI of 30 kg/m2.
It has been recognized that it is necessary to treat obesity so as to reduce the health problems associated with it. Rimonabant a well known CB1 cannabinoid receptor antagonist, has been used in the treatment of diabetes and obesity and the Rimonabant tablets are sold under the name Acomplia or Zimulti.
Still there is a need for mouth dissolving tablets comprising an anti-obesity agent, particularly for patients that require oral medication but have difficulty in swallowing tablets/capsule. Very often convalescent, aged people have difficulty in swallowing tablets/ capsule. Also it can be ideal for unfavorable conditions such as when water is not available.
The present invention provides a mouth dissolving solid dosage forms comprising Rimonabant with many added benefits over conventional tablet dosage form. Also the tablets are sweetened and flavoured to make them palatable.

Object of the Invention
The object of the invention is to provide a pharmaceutical composition comprising a CB1 cannabinoid receptor antagonist, Rimonabant in the form of palatable mouth dissolving tablet, as an adjunct to diet and exercise for the treatment of obese patients, which has the advantages of ease of administration for patients who have difficulty in swallowing.
Another object of the present invention is to provide a process for the preparation of mouth dissolving Rimonabant tablet composition.
Detailed description of the invention
The present invention provides mouth dissolving pharmaceutical composition of Rimonabant and the process of preparation thereof.
The present composition comprises Rimonabant and pharmaceutically accepted excipients selected from fillers, disintegrants, flavors, sweeteners, colors lubricants, and/or glidants.
Fillers of the present invention can be selected from any such pharmaceutically acceptable excipient, which gives bulk to the rimonabant composition and which is physically and chemically compatible with rimonabant, preferably those fillers may be selected from carbohydrates such as directly compressible maltose, sorbitol, mannitol, lactose, fructose; cellulose such as directly compressible microcrystalline cellulose, calcium carboxy methyl cellulose; starches such as pregelatinized starch, potato starch, maize starch or mixtures thereof. However the diluent chosen for present invention is microcrystalline cellulose, Mannitol and Lactose monohydrate. These diluents alone or in combination may be used in the range from 20-90% weight of the total formulation.
The direct compression excipients are chosen such that they have good flow and compressible characteristics and prevent segregation of powder in the hopper and thereby help in direct compression.

Disintegrants preferred for present invention may be selected from starches or modified starches such as sodium starch glycolate, corn starch, pregelatinized starch; celluloses such as microcrystalline cellulose, hydroxy propyl cellulose; cross-linked cellulose such as Croscarmellose sodium; cross-linked polymers such as Crospovidone; or mixtures thereof.
The Croscarmellose sodium provides superior disintegration characteristics, thus improving dispersion time of the formulation. It may be used in the range from 1.5% - 5.0% weight of total formulation.
The microcrystalline cellulose (Avicel PH 101/Avicel PH 102) is used in the range of 10 % to 50 % weight of total formulation.
The Sodium starch glycollate is used in the range of 2 - 15 % weight of total formulation.
The Lubricants of present invention may be selected from talc, magnesium stearate, calcium stearate, and hydrogenated vegetable oil. Preferably selected lubricants are Magnesium Stearate, and talc.
The Magnesium Stearate is used in the range of 0.25 - 2 % weight of total formulation.
The talc is used in the Range of 0.25 - 2.0% weight of total formulation.
The glidants of the present invention may be selected from colloidal silicon dioxide and talc.
The sweeteners for present invention may be chosen from both natural and artificial sweeteners. The sweetener may includes glucose, sucrose, sorbitol, mannitol; water soluble artificial sweeteners such as soluble saccharin salt, aspartame; sweetener from natural origin like sodium glycyrrhizinate. The preferable sweetener is Aspartame in the range of 1 - 5 %.

The flavoring agent for present invention include both natural and artificial flavors such as strawberry, pineapple, mango, lemon, orange, peppermint, American Ice-cream and Rasberry flavor. The flavor used in the range of 1.0 - 5.0%.
The coloring agent of present invention may be selected from any colorant used in pharmaceuticals which is indicated in D&C Act.
In another embodiment the present invention provides a process for the preparation of Rimonabant mouth dissolving tablet composition, wherein the process comprises the steps of sieving of the drug, fillers, disintegrants, binders, glidants, coloring agents, flavoring agents, and sweeteners, through a suitable sieve; admixing them to make a uniform blend; passing the lubricant through the suitable sieve; mixing the lubricant with the blend; and then directly compressing the blend using the suitable tooling.
The tablets made by the present inventive process disintegrate/dissolves quickly in mouth, preferably not more than 3 minutes, especially within 1 minute.
The tablet composition according present invention can be administered orally at the optimal daily dosage of 20 mg once a day.
The following examples, which include preferred embodiments, will serve to illustrate the practice of this invention, it being understood that the particulars shown are by way of example and for purpose of illustrative discussion of preferred embodiments of the invention.
Examples

Ingredient Qty/tablet (mg)
Exp. I Exp. II Exp. Ill Exp. IV Exp. V Exp. VI
Rimonabant 20.4 20.4 20.4 20.4 20.4 20.4

Microcrystalline cellulose 52.0 52.2 42.2 55.6 70.0 70.6
Lactose monohydrate 45.0 39.8 33.8 43.0 31.0 30.6
Mannitol 135.0 135.0 160.0 135.0 135.0 135.0
Croscarmellose sodium 5.0 10.0 5.0 5.0 5.0 5.0
Aspartame 4.6 4.6 4.6 4.6 4.6 4.6
Sodium starch Glycollate 10.0 10.0 10.0 12.0 10.0 10.0
Mix fruit flavour 8.0 8.0 4.0 4.4 4.0 4.0
Colloidal silicon dioxide 3.0 3.0 3.0 3.0 3.0 3.0
Talc 4.0 4.0 4.0 4.0 4.0 4.0
Magnesium stearate 3.0 3.0 3.0 3.0 3.0 3.0
Total Weight 290.0 290.0 290.0 290.0 290.0 290.0
Average Wt./tablet : 290 mg+/-2%
Hardness : 2.5 - 5.0 kg/cm2
Friability : Not more than 1% w/w
The standard process followed for the manufacture of Rimonabant mouth dissolving tablet composition comprises the steps of:
i) Sifting Rimonabant through 100 mesh sieve;
ii) Sifting color through 100 mesh sieve;
iii) Sifting Avicel PH 102, lactose monohydrate, Mannitol and through 40 mesh
sieve;
iv) Mixing the sifted ingredients of step i), step ii) and step iii) geometrically for sufficient time to get uniform blend;

v) Sifting croscarmellose sodium, aspartame, sodium starch glycollate, flavor, color
through 40 mesh sieve and mixing with the blend of step iv) for sufficient time to
get uniform blend.
vi) Sifting the material of step v) through 40 mesh sieve and the mixing the blend to
get uniform blend;
vii) Sifting colloidal silicon dioxide, talc and magnesium stearate through 40 mesh
sieve;
viii) Mixing the sifted blend of step vi) and sifted lubricants of step vii) for sufficient
time to get uniform blend;
xi) Compressing the lubricated blend on Rotary Machine using 9.5 mm, circular,
standard concave punches to obtain white colored circular, standard concave
tablets.