Title of Invention

MOUTH DISSOLVING VINPOCETINE COMPOSITIONS

Abstract The present invention relates mouth dissolving Vinpocetine tablet composition which disintegrates rapidly within 30 to 300 seconds, when ingested in mouth and process for preparation thereof. Further, this composition is formulated to have good organoleptic acceptance such as are suitably sweetened and flavored to mask the unpleasant taste of the active substance. 2 8 FEB 2008
Full Text FORM 2
THE PATENTS ACT, 1970
(39 of 1970)
COMPLETE SPECIFICATION
[See section 10; rule 13]
MOUTH DISSOLVING VINPOCETINE COMPOSITIONS'


(a) M/s LYKA LABS LIMITED.
(b) 77, Nehru Road, Vile Parle (East), Mumbai - 400 099, Maharashtra, India
(c) Indian Company incorporated under the Companies Act 1956
The following specification particularly describes the nature of this invention and the manner in which it is to be performed.



Technical field:
This invention relates to rapidly disintegrating, fast dissolving oral solid dosage form composition of vinpocetine that dissolves in mouth. This invention further relates to mouth dissolving tablets of vinpocetine.
Background and prior art:
Vinpocetine chemically known as ethyl apovincaminate is prepared by slightly and suitably modifying the vincamine alkaloid obtained from vinca minor, the periwinkle plant. The active agent, apovincaminic acid ethyl ester is disclosed in US patent No. 4035370. Thereinafter, this active agent is designated by its generic name, Vinpocetine. Vinpocetine has been in use for more than 25 years. Vinpocetine is a cerebral metabolic enhancer. It is used in the treatment of cerebrovascular disorders.lt is useful for a wide range of diseases like cerebral arterio-sclerosis, senile dementia and is a selective cerebral vasodilator.
Other suitable ester forms of apovincaminic acid are described in U.S. Pat. No. 4,035,370 and include the butyl ester, the allyl ester, the benzyl ester, and the ethyl ester methoiodide forms. The preferred ester form is the ethyl ester, i.e. apovincaminic acid ethyl ester, vinpocetine.
Vinpocetine is administered to humans either orally or parenterally. For many reasons oral administration is preferred.
Vinpocetine being effective when taken orally, tablets of vinpocetine (5mg) are commercially marketed for over 25 years.

Mouth dissolving tablets and granules offer many added benefits and advantages over conventional tablet dosage forms. These solid dosage forms of present invention dissolves in mouth and are particularly useful for subjects that require or desire oral medication but have difficulty in swallowing oral dosage form such as tablets, capsules. Very ofteji, infants, children, convalescent, aged people and subjects suffering from emesis have difficulty in swallowing tablets, capsules.
Secondly, conventional tablets or capsules require water or other liquids or drinks to swallow the tablet that becomes inconvenient to be administered during travel and other times. Mouth dissolving tablets of vinpocetine are suitably formulated to spontaneously disintegrate/ dissolve in the oral cavity as in contact with saliva in 30 seconds to 60 seconds after introducing into the mouth, without having to consume water or any other drink along with it. Hence it is very convenient to take these tablets any where any time.
These tablets of present invention are also sweetened and flavored to make them palatable. Taste- masking of active ingredient is also done in mouth dissolving tablets thereby increasing patient compliance.
Absorption of conventional tablets are often slower as dissolution of drug takes place after swallowing and disintegrating. Mouth dissolving tablets are also useful for rapid drug delivery for sublingual or buccal administration of the drug.
U.S. Pat. No. 4,035,370 describes various dosage forms for oral or parenteral administration of vinpocetine.
US patent 6663883 describes matrix adhering to nasal mucosa involving drugs exerting their effects in the brain, comprising a polyglycerol fatty acid ester.
An effervescent composition involving at least one physiologically active substance comprising a core-shell powder is reported in US patent 5824339.

Methods for making quick-dissolving oral mucosal delivery devices offering measured and controlled release of an active agent or a combination of active agents are described in US patent application 2003118653.
Russian patent RU 2155039 describes pharmaceutical compositions of vinpocetine in the form of conventional tablets and its method of preparation.
Even though, there are various patents available on vinpocetine, there are no prior art patent available on vinpocetine mouth dissolving tablets or granules.
Objective of this Invention:
The objective of present invention is to provide an oral solid dosage form composition of Vinpocetine which rapidly disintegrating, fast dissolving as in contact with saliva in mouth. An easily administrable mouth dissolving tablet composition of vinpocetine, which helps a faster onset of the therapeutic effect on the brain.
Summary of the Invention:
Mouth dissolving tablet dosage forms of vinpovetine are described. Mouth dissolving tablets are prepared by using ingredients that are having good compressibility, gives good sufficient strength when compressed. They can be directly mixed and compressed without granulation or alternatively, after granulation process. When ingested in mouth, it rapidly disintegrates within 30 to 300 seconds. These tablets are formulated to get good organoleptic acceptance. They are suitably sweetened and flavored to mask the unacceptable taste of the therapeutically active substance.
Detailed Description of the Invention:
Tablet Composition of the present invention are suitably formulated to dissolve in mouth as soon as it comes in contact with saliva in buccal cavity within 30 seconds to 60

seconds. Various embodiments of the Invention are formulated with suitable excipients. One or more of excipients in the present invention may be selected from diluent, binder, disintegrant, flow promoters, anti adherent, flavours and sweetening agents in different embodiments.
The present invention utilizes one or more of the diluents used either alone or in combination with other diluents, may be selected from water soluble diluents well known in the art such as mannitol, sorbitol,xylitol, lactose monohydrate, sucrose, Glucose, Fructose, Calcium carbonate and Maltodextrin. Diluents such as maize starch, potato starch, cellulose material such as microcrystalline cellulose are less preferred than more preffered such as mannitol, sorbitol, and lactose as they form low density matrix which disintegrates rapidly in mouth. However the most preferred diluent for present invention is mannitol as it gives very good mouth feel when mouth dissolving tablet disintegrates / dissolves in mouth. This diluent either alone or in combination may be used in the range from 20% weight up to 90% weight of total formulation.
The tablet composition of present invention consists of binder selected from synthetic gums such as methylcellulose, carboxy methylcellulose and its sodium salt, hydroxy propyl cellulose low substitution (LHPC), hydroxy propyl methyl cellulose (HPMC), povidone (PVPK.30). They may be used in the range from 1% weight up to 6% weight of total formulation, preferably in 3%-5% weight.
Flow property enhancer / antiadherents may be selected from Talc, colloidal silicon dioxide (Aerosil), magnesium stearate, sodium steryl fumarate. They may be used in the range from 0.5% weight up to 5% weight of total formulation, preferably used in 3%-4% weight.
Disintegrants may be selected from celluloses such as microcrystalline cellulose, crosslinked carboxymethyl cellulose sodium salt, maize starch, sodium starch glycollate, polymers like hydroxyproylmethyl cellulose. They may be used in the range from 1%

weight up to 5% weight of total formulation, preferably used concentration in present invention in 3%-4% weight.
One or more sweetening agents to make the solid dosage form of present invention palatable may be chosen from artificial sweeteners such as aspartame, sodium saccharin, sodium cyclamate, acesulfame potassium or sweetner from natural origin like Sodium glycerrhizinate,mono ammonium glycyrrhizinate (magnasweet) are used in different embodiments. They may be used in the range from 1% weight up to 3% weight of total formulation, preferably used concentration in present invention in 1.5%-2.5% weight. Different artificial flavours are used to provide palatability.
i
To mask the taste of active ingredient, methacrylic acid co-polymer (eudragit) is used and also beta-cyclodextrin is used. Various embodiments of the invention are described in examples 1 to 11.
Wherein the said mouth dissolving tablets are prepared by Direct compression method comprising of, sifting active ingredient and excipients through sieve of suitable mesh size from 40 to 100 mesh, mixing ingredients together in geometric proportion, mixing with sweeteners, flavours, disintegrants and lubricants and compressing the said blend to obtain the tablets.
Alternatively granulation method is also implied, the process comprising of, sifting active ingredient and excipients through sieve of suitable mesh size from 40 to 100 mesh, mixing ingredients together in geometric proportion, preparing binder solution / paste, granulating the blend with binder solution, drying the granules, further mixing with presifted sweeteners, flavours, disintegrants and lubricants and compressing the said blend to obtain the tablets. Experimental Example 1
Mouth dissolving vinpocetine tablets are prepared by the following manner.

STEP 1: Vinpocetine is passed through 100 mesh sieve.
STEP 2 :Mannitol passed through 40 mesh sieve and mixed with Vinpocetine.
STEP 3 .-Aspartame, flavour Pepermint DC 117 ,Menthol, Croscarmellose Sodium,
colloidal silicon dioxide (Aerosil) and Talc are passed through 40 mesh sieve.
STEP 4 Mixed the above sifted ingredients with blend of step 2 in geometric proportion.
STEP 5 : Finally Magnesium Stearate is passed through 40 mesh sieve and mixed with
blend of step 4 to the lubricated blend.
STEP 6 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia = 8.0mm
Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 10 seconds - 180 seconds after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.


Example 2
Mouth dissolving vinpocetine tablets are prepared by the following manner
i
STEP 1: Vinpocetine is passed through 100 mesh sieve.
STEP 2 :Lactose(Tablettose 80), Lowsubstituted hydroxypropylcellulose (LHPC LH 11)
and Croscarmellose Sodium are passed through 40 mesh sieve.
STEP 3 -.Mixed the ingredients of step 1 and step 2 in geometric proportion.
STEP 4 :Sodium Saccharin,Mix fruit flavour, Talc and colloidal silicon dioxide
(Aerosil)are passed through 40 mesh sieve and mixed with blend of step 3 .
STEP 5 :Magnesium Stearate passed through 40 mesh sieve mixed with blend of step 4.
STEP6 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 1^0 mg, Dia = 8.0mm
Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet
thus obtained completely disintegrates/dissolves in oral cavity in saliva within
10 seconds - 180 seconds after its administration without taking water to gulp the tablet.
The composition of the above said ingredients are given in the following table.


Example 3:
Mouth dissolving vinpocetine tablets are prepared by the following manner.
f
STEP 1: Vinpocetine is passed through 100 mesh sieve.
STEP 2 :Mannitol, Lactose (Tablettose - 80), Lowsubstituted hydroxypropyl cellulose
(LHPC LH-11), Croscarmellose Sodium are passed through 40 mesh sieve.
STEP 3 :Mixed the ingredients of step 1 with step 2 in G.P and mixed again.
STEP 4 •Aspartame, flavour Peppermint DC117, menthol, Talc and colloidal silicon
dioxide (Aerosil) are passed through 40 mesh sieve.
STEP 5 :Mixed the above ingredients with the mixture of step 3
STEP 6 :Finally Magnesium Stearate is passed through 40 mesh and mixed with step 5
STEP 7 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 nig, Dia = 8.0mm
Hardness = 2-6 kg/cm2
9
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 10 seconds -180seconds after its administration without taking water to gulp the tablet.Thus this type of tablets are commonly known as Mouth Dissolving tablets. The composition of the above said ingredients are given in the following table.



Example 4
Mouth dissolving vinpocetine tablets are prepared by the following manner.
STEP 1 :Vinpocetine is passed through 100 mesh sieve.
STEP 2 : Microcrystalline cellulose (Avicel ph 102), lactose (Tablettose 80),
Croscarmellose Sodium are passed through 40 mesh sieve..
STEP 3 :Mixed the ingredients of step 1 with step 2 well in geometric proportion.
STEP 4 .-Sodium saccharin, flavour Mix fruit, Talc and Aerosil are passed through 40
mesh sieve.
STEP 5 -.Mixed the above ingredients with mixture of step 3
STEP 6 : Finally Magnesium Stearate is passed through 40 mesh sieve and mixed with
step 5 to obtain the lubricated blend.
STEP 7 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia = 8.0mm
Hardness = 2-6 kg/cm2
ji r
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 10 seconds -180 seconds after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.

t


Example 5
Mouth dissolving vinpocetine tablets are prepared by the following manner

STEP 1: Vinpocetine is passed through 100 mesh sieve.
STEP 2 : Mannitol, Microcrystalline cellulose (Avicel pH 102), Lactose (Tablettose),
Low Substituted hydroxypropyl cellulose (LHPC), and Croscarmellose Sodium are
passed through 40 mesh sieve.
STEP 3 :Mixed the ingredients of step 1 with step 2 well in geometric proportion.
STEP 4 :Monoammonium Glycyrrhizinate (Magnasweet), flavour mango trusil, Talc,
Colloidal silicon dioxide (Aerosil) and Sodium Starch GlycoUate are passed through 40
mesh sieve.
STEP 5 :Mixed the above ingredients with mixture of step 3
STEP 6:
Finally Magnesium Stearate is passed through 40 mesh sieve and mixed with step 5
STEP 7 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia = 8.0mm


Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet
thus obtained completely disintegrates/dissolves in oral cavity in saliva within
10 seconds -180 seconds after its administration without taking water to gulp the tablet.
The composition of the above said ingredients are given in the following table.
«

Example 6
Mouth dissolving vinpocetine tablets are prepared by the following manner uses beta cyclodextrin for improving jtaste and making tablets more palatable.
STEP 1: Vinpocetine and P-cyclodextrin are passed separately through 100 mesh sieve. STEP 2 : Vinpocetine is triturated with (3-cyclodextrin for 10 mins. and mixed well

STEP 3 : Mannitol (Perlitol DC 400), Low Substituted Hydroxy Propyl Cellulose [LHPC
(LH-11)], Sodium Starch Glycolate, Croscarmellose Sodium are passed through 40 mesh
sieve and mixed together with blend of step 2.
STEP 4 : Aspartame, flavour Orange trusil, Talc and Colloidal Silicon Dioxide
(Aerosil)are passed through 40 mesh sieve and mixed with blend of step 3.
STEP 5 : Magnesium Stearate is passed through 40 mesh and mixed with blend of step 4
to obtain the lubricated blend.
STEP 6 : The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia = 8.0mm
Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet
thus obtained completely disintegrates/dissolves in oral cavity in saliva within
10 seconds - 180 seconds after its administration without taking water to gulp the tablet.
The composition of the above said ingredients are given in the following table.


Example 7
Alternatively Mouth dissolving tablets are prepared by granulation process using different binders in different embodiments. Following are the few examples of Vinpocetine mouth dissolving tablets prepared by utilizing granulation process.
Mouth dissolving vinpocetipe tablets are prepared by the following manner.
STEP 1: Vinpocetine is passed through 100 mesh sieve.
STEP 2 : Mannitol and Lactose are passed through 40 mesh sieve and mixed with
Vinpocetine in geometric proportion.
STEP 3 : Solution of povidone (PVP K-30) in Isopropyl alcohol is prepared for
granulation.
STEP 4 : Granulated the blend of step 2 with binder solution of Step 3. Wet granules are
passed through 12# and dried in air then in tray dryer at 35-40°c for suitable period of
time. Dried granules are passed through 20 mesh sieve.
STEP 5 :Aspartame, flavour mango trusil, Croscarmellose Sodium, colloidal silicon
dioxide (Aerosil) and Talc are passed through 40 mesh sieve.
STEP 6 Mixed the above ingredients with mixture of step 4.
STEP 7 :Finally Magnesium Stearate is passed through 40 mesh and mixed with blend of
step 6
STEP 8 :The lubricated blend is compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia= 8.0mm
Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within

10 seconds - 180 seconds after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.

Example 8
Mouth dissolving vinpocetine tablets are prepared by the following manner.
STEP 1: Lactose, Mannitol, Microcrystalline Cellulose are sifted through 40# sieve.
STEP 2: Vinpocetine is passed through 100 mesh sieve and mixed together with
ingredients of step 1 in geometric proportion.
STEP 3 : Binder paste of Maize Starch & Povidone (PVP K-30) is prepared using
purified water.
STEP 4 : Granulated the blend of step 2 in mixer by adding solution of Step 3 till wet
mass of suitable consistancy is obtained.
STEP 5 : The wet mass is passed through 12# Sieve.
STEP 6 : The granules arejdried in tray dryer at 40-50°c for suitable period of time and
the dried granules are passed through 20# sieve.

STEP 7 : Talc, Magnesium Stearate, Crospovidone, Croscarmellose Sodium, Colloidal Silicon Dioxide (Aerosil), Sodium Saccharin and flavour pineapple trusil are sifted through 40 mesh sieve and mixed with dried granules of step 6 to obtain the lubricated granules.
STEP 8 : The lubricated granules are compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet = 180 mg
Dia = 8.0mm
Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet
thus obtained completely disintegrates/dissolves in oral cavity in saliva within
10 seconds - 180 seconds after its administration without taking water to gulp the tablet.
The composition of the above said ingredients are given in the following table.


Example 9
Mouth dissolving vinpocetine tablets are prepared by the following manner.
STEP 1: sifted Lactose, Mannitol and Microcrystalline Cellulose through 40# sieve and
mix. STEP 2: Vinpocetine is passed through 100 mesh sieve and mixed with blend of step 1. STEP 3 Solution of Povidone (PVP K-30) is prepared using purified water. STEP 4 .-Granulated the material in mixer by adding solution of Step 3 till wet mass of suitable consistancy is obtained. STEP 5 :The wet mass is passed through 12 mesh Sieve.
STEP 6 :The granules are dried in tray dryer at 40-50°c for suitable period of time and passed the dried granules through 20# sieve.
STEP 7 :Talc, Magnesium Stearate, Sodium Starch Glycollate, Croscarmellose Sodium, Colloidal Silicon Dioxide (Aerosil), Sodium Saccharin, Menthol and flavour peppermint DC117 are sifted through 40 mesh sieve and mixed with dried granules of step 6 to obtain the lubricated granules.
STEP 8 :The lubricated granules are compressed to obtain circular flat, bevelled scored tablets.
Average Wt. per tablet = 180 mg Dia= 8.0mm Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 10 seconds - 180 seconds after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.



Example 10
Mouth dissolving vinpocetine tablets are prepared by the following manner.
STEP 1 : Lactose, Mannitol, Microcrystalline Cellulose and Hydroxy Propyl Methyl
Cellulose (HPMC) are sifted through 40 mesh sieve.
STEP 2 Vinpocetine is passed through 100 mesh sieve and mixed with material of
step lin geometric proportion.
STEP 3 :Granulated the material in mixer using Purified water for binding till wet mass
of suitable consistancy is obtained.
STEP 4 :The wet mass is passed through 12 mesh Sieve.
STEP 5 •. The granules arej dried for suitable period of time and the dried granules are
passed through 20 mesh sieve.
STEP 6 : Talc, Magnesium Stearate, Sodium Starch Glycollate, Croscarmellose Sodium,
Colloidal Silicon Dioxide (Aerosil), Sodium Saccharin and flavour are sifted through 40
mesh sieve and mixed with dried granules of step 5 to obtain the lubricated granules.
STEP 7 : The lubricated granules are compressed to obtain circular flat, bevelled scored
tablets.
Average Wt. per tablet =180 mg
Dia = 8.0mm

Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 10 seconds - 180 seconds after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.

Example 11
Mouth dissolving vinpocetine tablets are prepared by the following manner STEP 1: Vinpocetine is passed through 100 mesh sieve.

STEP 2 :Microcrystalline cellulose (Avicel pH 101) and Croscarmellose Sodium (only
part - 7.0 gm) are passed through 40 mesh sieve and mixed with vinpocetine well in
geometric proportion.
STEP 3 : Solution of Sodium Lauryl Sulphate is prepared using Purified water.
Methacrylic acid co-polymer (Eudragit EPO) is added to this with stirring.
STEP 4 : Granulated the blend of step 2 with dispersion of step 3.
STEP 5 : Wet granules are passed through 12 mesh sieve and dried in tray dryer at
30 - 35°C for suitable period. Dried granules are passed through 20 mesh sieve.
STEP 6 : Mannitol is passed through 40 mesh sieve.
STEP7 : Binding solution of Povidone (PVP K-30) is prepared in purified water.
STEP 8 : Granulated the sifted Mannitol of step 6 with binding solution of step 7. Wet
mass is passed through 12 mesh and dried in tray dryer at 45 - 50°C for suitable time.
Dried granules passed through 20 mesh.
STEP 9 :Aspartame, flavours Peppermint DC 117 and Flavour Vanilla trusil, Magnesium
Stearate, Stearic acid and 'iCroscarmellose Sodium (remaining part - 6mg) are passed
through 40 mesh sieve.
STEP 10 Mixed the lubricants of step 9 with blend of step 5 and step 8 together to get
uniform blend.
STEP11 :The lubricated blend is compressed to obtain circularflat,bevelled scoredtablets.
Average Wt. per tablet = 180 mg Dia = 8.0mm Hardness = 2-6 kg/cm2
This tablet is suitably sweetened and flavoured to obtain a palatable tablet. The tablet thus obtained completely disintegrates/dissolves in oral cavity in saliva within 30 seconds - 2 min after its administration without taking water to gulp the tablet. The composition of the above said ingredients are given in the following table.


While the present invention is described above in connection with preferred or illustrative embodiments, these embodiments are not intended to be exhaustive or limiting of the invention. Rather, the invention is intended to cover all alternatives, modifications and equivalents included within its scope, as defined by the appended claims.

claim

1. Mouth dissolving tablet compositions of vinpocetine formulated to dissolve in mouth in contact with saliva in buccal cavity within 10 to 180 seconds comprising of
a) vinpocetine 5 mg;
b) one or more diluents selected from water soluble diluents such as mannitol, sorbitol, xylitol, lactose monohydrate, sucrose, glucose, fructose, calcium carbonate and maltodextrin and diluents such as maize starch, potato starch, cellulose material such as microcrystalline cellulose;
c) one or more binders selected from synthetic gums such as methylcellulose, carboxy methylcellulose and its sodium salt, hydroxy propyl cellulose low substitution (LHPC), hydroxy propyl methyl cellulose (HPMC), povidone (PVPK.30);
d) one or more flow property enhancer/ antiadherents selected from Talc,
colloidal silicon dioxide (Aerosil), magnesium stearate, sodium steryl fumarate;
e) one or more disintegrants selected from microcrystalline cellulose, crosslinked
carboxymethyl cellulose sodium salt, maize starch, sodium starch glycollate,
polymers like hydroxyproylmethyl cellulose;
f) one or more sweetening agents are selected from artificial sweeteners aspartame, sodium saccharin sodium cyclamate, acesulfame potassium or sweetener from natural origin like sodium glycerrhizinate, and mono ammonium glycerrhizinate (Magnasweet);
g) one or more flavours are selected from peppermint DC 117, mix fruit, mango trusil, vanilla trusil, orange trusil and pineapple trusil;
h) one or more taste masking agents such as methacrylic acid co-polymer (eudragit) and beta-cyclodextrin;


wherein the said mouth dissolving tablets are prepared by the process comprising
of,
passing active ingredient through 100 mesh sieve and excipients through suitable
mesh size of 40 to 100;
mixing ingredients together in geometric proportion;
mixing pre sieved sweeteners and flavours with the main mass to prepare a blend;
mixing magnesium stearate with the said blend;
compressing the lubricated blend to obtain the tablets.

2. Mouth dissolving tablets of vinpocetine as claimed in claim 1, wherein the said mouth dissolving tablets are prepared by wet granulation process comprising of, passing the active ingredients through lOOmesh sieve and excipients through suitable mesh size of 40 to 100; mixing ingredients together; preparing the binder solution; granulating the blend with binder solution; mixing presieved sweeteners and flavours with the dried granules; mixing magnesium stearate with the above blend; compressing the lubricated blend to obtain the tablets.
3. Mouth dissolving tablets of vinpocetine as claimed in claim land 2, wherein the said diluents are mannitol, sorbitol, and lactose.
4. Mouth dissolving tablets of vinpocetine as claimed in claim 1 and 2, wherein the said diluent is mannitol.
5. Mouth dissolving tablets of vinpocetine as claimed in claiml and 2, where in the weight of the said diluents are in the range from 20% to 90% weight of the
composition.


6. Mouth dissolving tablets of vinpocetine as claimed in claim 1 and 2, where in the weight of the said flow property enhancer/anti-adherents is in the range of 0.5% to 5% weight of the composition.
7. Mouth dissolving tablets of vinpocetine as claimed in claim 6, wherein the weight of the said flow property enhancer/anti- adherents is preferable in the range of 3% to 4% weight of the composition.
8. Mouth dissolving tablets of vinpocetine as claimed in claim 1 and 2,wherein the
ij weight of the said binders are in the range of 1% to 6% weight of the
composition.
9. Mouth dissolving tablets of vinpocetine as claimed in claim 8, where in the Weight of the said binders are preferably in the range of 3% to 5% weight of the composition.
10. Mouth dissolving tablets of vinpocetine as claimed in claim 1 and 2,wherein the weight of the said disintegrants are in the range of 1% to 5% weight of the composition.

11. Mouth dissolving tablets of vinpocetine as claimed in claim 10, wherein the weight of the said disintegrants are preferably in the range of 3% to 4% weight of the composition
12. Mouth dissolving tablets of vinpocetine as claimed in claim 1 and 2,wherein the weight of the said sweetening agents are in the range of l%to 3% weight of the composition.
13. Mouth dissolving tablets of vinpocetine as claimed in claim 12, wherein the weight of the said sweetening agents are preferable in the range of 1.5%to 2.5%

weight of the composition

14. Mouth dissolving tablets of vinpocetine as substantially described herein with reference to the foregoing examples 1-11.
Dated this 13tn day of Feb, 2004

Dr. Gopakumar G. Nair
Agent for the Applicant
35

Documents:

223-mum-2004-abstract(28-2-2008).doc

223-mum-2004-abstract(28-2-2008).pdf

223-mum-2004-cancelled pages(28-2-2008).pdf

223-mum-2004-claims(granted)-(28-2-2008).doc

223-mum-2004-claims(granted)-(28-2-2008).pdf

223-mum-2004-correspondence(28-2-2008).pdf

223-mum-2004-correspondence(ipo)-(3-6-2008).pdf

223-mum-2004-form 1(24-2-2004).pdf

223-mum-2004-form 18(26-5-2006).pdf

223-mum-2004-form 2(granted)-(28-2-2008).doc

223-mum-2004-form 2(granted)-(28-2-2008).pdf

223-mum-2004-form 26(4-3-2004).pdf

223-mum-2004-form 3(24-2-2004).pdf

223-mum-2004-form 3(28-2-2008).pdf


Patent Number 220741
Indian Patent Application Number 223/MUM/2004
PG Journal Number 42/2008
Publication Date 17-Oct-2008
Grant Date 03-Jun-2008
Date of Filing 24-Feb-2004
Name of Patentee M/S. LYKA LABS LIMITED
Applicant Address 77, NEHRU ROAD, VILE PARLE (EAST), MUMBAI 400 099, MAHARASHTRA, INDIA.
Inventors:
# Inventor's Name Inventor's Address
1 SAMANT RAJAN SHANTARAM M/S. LYKA LABS LIMITED, 77, NEHRU ROAD, VILE PARLE (EAST), MUMBAI-400 099. MAHARASHTRA, INDIA.
2 SHAH HARAKHCHAND KESHAVJI M/S LYKA LABS LIMITED, 77, NEHRU ROAD, VILE PARLE (EAST), MUMBAI-400 099. MAHARASHTRA, INDIA.
3 SANGODKAR SONAL RAJENDRA M/S LYKA LABS LIMITED, 77, NEHRU ROAD, VILE PARLE (EAST), MUMBAI-400 099. MAHARASHTRA, INDIA
4 SANGODKAR RAJENDRA PANDURANG M/S LYKA LABS LIMITED, 77, NEHRU ROAD, VILE PARLE (EAST), MUMBAI-400 099. MAHARASHTRA, INDIA.
PCT International Classification Number C07D459/00
PCT International Application Number N/A
PCT International Filing date
PCT Conventions:
# PCT Application Number Date of Convention Priority Country
1 NA