DESC:
Field of the invention
The present invention relates to oral formulations. More specifically the present invention relates to oral pouch composition with no added water.

Background and the prior art
Nicotine oral delivery products are generally known as replacements for smoking articles including cigarettes. And, tobacco may be enjoyed in a so-called "smokeless" form. Nicotine oral delivery products may be provided in loose form, commonly known as snus, or comprise a composition enclosed within a convenient format called pouch / sachet. They are typically placed between the upper or lower gum and lip or cheek of a user, and are retained in this position for a period of time during which, for the pouched nicotine oral delivery products, saliva passes into the interior of the pouch and dissolved components including flavour and nicotine-containing components disseminate therefrom for the user.

Many attempts have been made in this context which includes, WO2021116862 which discloses a pouch product with less water content, however, it lacks the combination of enhanced and consistent flavor delivery through encapsulated flavors. WO’862 employs the use of liquid flavor in the formulation, which are highly volatile, concentrated and the release is not long-lasting.

US11344057 discloses the nicotine delivery format through pouches, however, it does not deal with the reduced water content instead it discloses the use of at least one capsule contained within the cavity of the water-permeable fabric pouch.

Despite the desire for certain properties to be present in an oral composition or product, materials with a relatively high-water content do suffer from product stability and may also be prone to more microbial contaminations. Further, with regard to powdered compositions, flowability is used as a measure of the processability, which is also a challenging aspect to have a desired flowability. However, most of the oral-pouch compositions do contain higher amounts of water. Additionally, it would also contain sugar alcohols, which eventually tends to agglomerate and the flowability is drastically reduced.

Object of the invention
It is an object of the present invention to provide an oral pouch composition with no water added.

It is another object of the present invention to provide an oral pouch composition containing sugar alcohols but a superior flowability with an angle of repose, not more than 40°.

It is a further object of the present invention to provide an oral pouch composition which is highly flowable and can be transported using gravitational force or a little energy.

Summary of the Invention
Accordingly, there is provided an oral, non-aqueous composition comprising; 0.4-5% by weight of atleast one active compound; 20-60% by weight of atleast one filler element; 5-40% by weight atleast one polyol element, atleast one encapsulated flavors; said composition forming a particulate blend having a size of 10-700 micron.

According to another aspect of the present invention there is provided an oral delivery product comprising the oral, non-aqueous composition of the present invention and a pouch; wherein said composition is formulated in the pouch and said pouch is made of a water permeable fabric.

According to a further embodiment of the present invention there is provided a method for delivering active, said method comprises providing an oral, non-aqueous composition of the present invention in the pouch format; such that said method results in delivery of a long-lasting flavor for a time period of about 60 mins, preferably for 45 mins when said composition comes in contact with water.

Detailed Description of the invention
Accordingly, the present invention provides an oral pouch composition, comprising atleast one active compound; atleast one filler element; atleast one polyol element, atleast one sweetener, encapsulated flavors and/or encapsulated blend of atleast one sweetener and atleast one flavor component combined, along with other excipients, forming a particulate blend with a size of 10-700 microns delivering a long-lasting flavor.

The present inventors have unexpectedly found that the present oral pouch composition with no water added, still containing sugar alcohols offers a superior flowability with an angle of repose, not more than 40°. Angle of repose is an important physical property used for characterization of the bulk of particulate foods such as seeds, grains, flours, grits, fruits, including very fine powdered materials. The angle of repose is important for the design of processing, storage, and conveying systems of particulate materials. Materials with low angle of repose are highly flowable and can be transported using gravitational force or a little energy.

Moreover, to offer long lasting flavor delivery, encapsulated flavors are incorporated in the formulation. The encapsulated flavours are present in powdered form with good flow properties, have very low volatile property, are easy to disperse, and release flavours up on contacting with moisture. This helps in achieving the long-lasting flavour. When encapsulated flavors are added, with uniform distribution, consistent flavor delivery for about 45 to 60 mins, preferably for 45 mins occurs when the composition comes in contact with water.

The oral composition of the present invention is contained within a pouch, which is made up of a water permeable fabric selected from viscose and vinyl acetate co-polymer, vinyl acyclic and acrylic co-polymer and the like.

The active compound according to the present invention is selected from the group consisting of a nicotine or nicotine salts, nicotine component, botanicals, stimulants, amino acids, vitamins, terpenes, nutraceuticals, nicotine or nicotine salts, nicotine component, tobacco alkaloid, and combinations thereof. The active compound can be one selected from the group consisting of a nicotine salt, nicotine free base, nicotine bound to an ion exchanger, such as an ion exchange resin, such as nicotine polacrilex resin, a nicotine inclusion complex or nicotine in any non-covalent binding; nicotine bound to cellulose, such as microcrystalline cellulose and a combination thereof. The active may be present in amounts of 0.4-5% by weight.

Filler according to the present invention is preferably microcrystalline cellulose/MCC. Filler may be present in an amount 20-60% by weight.

The composition of the present invention may further contain one or more other excipients selected from the group consisting of sweeteners, gums, binding agents, pH regulator or a combination thereof. Other excipients may be present in amounts 1 to 20 % by weight.

The oral composition of the present invention comprises flavors selected from paan, anise, vanilla, coffee, chocolate, cream, mint, spearmint, menthol, peppermint, wintergreen, lavender, cardamom, nutmeg, cinnamon, clove/eugenol, cascarilla, sandalwood, honey, jasmine, sage, licorice, lemon, orange, apple, peach, lime, cherry, eucalyptus, strawberry, berry flavors such as pomegranate, raspberry, blueberry, , boysenberry, and/or cranberry, , , spearmint, , citrus, olive oil, sesame oil, sunflower oil, bergamot oil, geranium oil, lemon oil, , thymol, and/or tea tree and combinations thereof. The flavour may be present in amounts 1-60 % by weight; preferably 1-25% by weight.

The oral composition of the present invention comprises polyol or sugar alcohol selected from xylitol, maltitol, mannitol, erythritol, isomalt, sorbitol, lactitol and mixtures thereof. According to a preferred embodiment the sugar alcohol is mannitol, erythritol or mixtures thereof. The sugar alcohol may be present in 5-40% by weight. Preferably the polyols are spray dried polyols.

The pH regulator used herein is selected from the group comprising sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, magnesium carbonate or any combination thereof. The pH regulator may be present in 1-8% by weight. The pH of the composition is about 7.

The artificial sweeteners used herein is selected from the group comprising saccharine, aspartame, sucralose, neotame, acesulfame-K, stevia or any combination thereof.

Humectant used herein is selected from the group comprising glycerol, glycerine, propylene glycol, hexyleneglycol, butylene glycol, polydextrose, sorbitol, maltitol, xylitol, glyceryl triacetate, triethylene glycol or any combination thereof.

In one or more embodiments, the present invention provides the methods of forming an oral composition with no water added. In one of the non-limiting examples, the invention offers a formulation with no added water or a non-aqueous based formulation for a long-lasting flavor delivery, with a very attractive soft, moldable texture, mouthfeel along with consumer acceptable taste profile.

It has known that water activity is defined as the ratio of the vapor pressure of water in a product (p) to the vapor pressure of pure water (po) at the same temperature. As per USP 1112 standard pharmaceutical drug products with water activities well below 0.75 aw are considered excellent candidates for reduced microbial testing for product release and stability evaluation.

It has been found that the water activity of the present composition is less than 0.85 aw, preferably less than 0.75 aw, more preferably less than 0.72 aw.

According to one embodiment of the present invention there is provided an active delivery formulation in the pouch format comprising encapsulated flavors with no added water, said formulation having a consistent flavor delivery and uniform particle size distribution. The wettability of the product is not compromised and also microbial contaminations during storage is prevented. Hence the product’s shelf life is also enhanced significantly.

According to another embodiment of the present invention there is provided an active delivery formulation, with relatively less or no water content, substituted with sugar alcohols. It has enhanced flavor delivery and consistency which is achieved through uniform particle size distribution. The formulation is offered in a pouch format for the convenient of the user, which is essentially a water permeable fabric forming a cavity. The ingredients including, actives that are made through synthetic routes, along with other releasable components are filled therein the said cavity.

The encapsulated flavors are made through spray dried process which is well known in the art. Since the present formulation does not contain water, there is no need for preservatives.

The present composition can be formulated in the form of a pouch and sachet. However, the present composition can be used to produce various other compositions such as snus, snuff, lozenges, film, gum, chewing gum, tablets, strips, capsules, caplet, spray, food and combinations thereof.

According to another embodiment of the present invention there is provided an oral delivery product comprising the above mentioned oral, non-aqueous composition of the present invention and a pouch; wherein said composition is formulated in the pouch and said pouch is made of a water permeable fabric.

According to a further embodiment of the present invention there is provided a method for delivering active, said method comprises providing an oral, non-aqueous composition in the pouch format comprising encapsulated flavors with no added water, such that said method results in delivery of a long-lasting flavor for a time period of about 60 mins, preferably for 45 mins when the composition comes in contact with water.

The present invention is now being illustrated by way of non-limiting examples.

Example 1
Table 1 shows the range of components that can be present in the formulation of the present invention as well as an example of the composition in accordance with the present invention.
Table 1
S. No Ingredients/Functionality wt% wt%
1 Filler 20-60% 40
2 Encapsulated Flavor 1-25% 10
3 Spray dried Polyols 5-40% 30
4 Spray dried Pre-Gelatinized Starch 1-8% 5
5` Active pharmaceutical ingredient (API) 0.4-5% 4
6 pH Regulator 1-8% 3
7 Artificial Sweetener 1-8% 2.5
8 Humectant 1-15% 5.5

for preparing the above formulation:
Pre-mix-1 was prepared by spraying humectant on to the filler followed by mixing for uniform distribution. Pre-mix-1, API and excipients (encapsulated flavor, spray dried polyol, spray dried pre-gelatinized starch, pH Regulator, artificial sweetener) were further mixed and sifted to obtain a blend. Geometric dilution of API mixing with excipients was maintained. The blend obtained was collected and stored in an air tight container in a dry and dark place. The required amount of blend was transferred to hopper of pouching machine to attain pouch formulation.

Table 2: Testing parameters (Flow property, Hausner ratio and Angle of repose)
Flow property Hausner ratio Angle of Repose
Excellent 1 – 1.11 25-30
Good 1.12 – 1.18 31-35
Fair-aid not needed 1.19 – 1.25 36-40
Passable – may hang up 1.26 – 1.34 41-45
Poor – must agitate / vibrate 1.35 – 1.45 46-55
Very poor 1.46 – 1.59 56-65
Extremely poor > 1.60 >66

The above oral delivery compositions in spite of being a non-aqueous based formulation when provided through pouch formats, offers enhanced and consistent flavor delivery for about 45 min to 60 min upon use. Table 2 provides the testing parameters that are commonly used. It has been found that the angle of repose for the composition in Table 1 is not more than 40.

The criticality of the present invention resides in the judicious choice of the ingredients and its weight %. Either the ingredient or its weight % when chosen beyond its suggested levels (as mentioned in Table 1), it drastically affects the formulation, flow properties, angle of repose (preferred is <30), and overall flavor delivery.

Example 2
Effect of various components in the oral composition of the present invention
Various samples were prepared, where Example 1 is a working example and Examples 2 and 3 are non-working examples.

Table 3
S. No Ingredients Example 1 (working example) %w/w Example 2 (Non-working example) %w/w Example 3 (Non-working example) %w/w
1 Filler e.g. Micro crystalline cellulose 40.00 38.00 41.00
2 Flavor e.g. Encapsulated Mint Flavour 10.00 10.00 12.00
3 Polyol e.g. Standard Grade Mannitol 0.00 30.00 30.00
4 Spray dried polyol, Spray dried Mannitol 30.00 0.00 0.00
5 Spray dried Pre-Gelatinized Starch 5.00 5.00 5.20
6 Active Pharmaceutical ingredients 4.00 4.00 4.00
7 pH regulator, e.g. Carbonate Salts 3.00 5.00 3.80
8 Artificial Sweetener e.g. acesulfame-K 2.50 1.20 1.00
9 Humectant e.g. propylene glycol 5.50 6.80 3.00
Hausner ratio 1.1 1.45 1.33
Angle of Repose 29.0 49.00 43.00

From the above comparative data in Table 3 it is evident that angle of repose of the composition in non-working Examples 2 and 3 are very high compared to that of working example 1. The criticality of the present invention resides in the use of encapsulated flavorants, which forms a part of the whole formulation and further the judicious choice of the ingredients used and its wt.% which in turn impacts the angle of repose (<40 is always preferred) is also critical. The above table demonstrates, criticality of the wt.% of these ingredients used vis-à-vis the present invention, example 1.

Example 3: Sensory evaluation
The compositions in Example 1 and 2 were further evaluated for sensory evaluation.
Table 4
SENSORY EVALUATION
Sl. No. Parameter Example 1 –(working example) Example 2 (Non-working example) Rating Scale Definition
(ratings allowed: 1 - 1.5 - 2 - 2.5 - 3 - 3.5 - 4 - 4.5 - 5)
1 Aroma upon sniffing 3.3 4.0 1 2 3 4 5
Very Low Low Medium High Vey High
2 Taste & Flavour Onset 3.8 4.0 1 2 3 4 5
Very Late
(> 5 mins) Late
(3-5 mins) Medium
(2-3 mins) Early
(1-2 mins) Very Early
(< 1 min)
3 Taste & Flavour Quantity 3.7 3.8 1 2 3 4 5
Very Low Low Medium High Very High
4 Taste & Flavour Longevity 4.0 2.5 1 2 3 4 5
Very low Low Medium
(10-15 mins) High Very high
(till end of use)
5 Taste & Flavour Likeability 4.0 3.0 1 2 3 4 5
Not Liked at all Somewhat disliked Somewhat Liked Liked Liked Very Much
6 After taste quality 4.5 2.0 1 2 3 4 5
Disliked Somewhat disliked Somewhat Liked Liked Liked Very Much
7 Overall Likeability 4.0 2.0 1 2 3 4 5
Disliked Somewhat disliked Somewhat Liked Liked Liked Very Much

Table 4 shows that Example 1 provides a “long-lasting flavor” which is the crux of the present invention. Some parameters of example 2, especially 1-3 seems to be working however, the rest of the parameters and the overall likeability is seen, this always favors the example 1.
,CLAIMS:
1) An oral, non-aqueous composition comprising; 0.4-5% by weight of atleast one active compound; 20-60% by weight of atleast one filler element; 5-40% by weight atleast one polyol element, atleast one encapsulated flavors; said composition forming a particulate blend having a size of 10-700 micron.

2) The oral composition as claimed in claim 1, wherein said polyol is spray dried polyol.

3) The oral composition as claimed in claim 1, wherein said encapsulated flavors is present in an amount 1 to 25% by weight.

4) The oral composition as claimed in claim 1, wherein said active compound is selected from the group consisting of botanicals, stimulants, amino acids, vitamins, terpenes, nutraceuticals, nicotine or nicotine salts, nicotine component, tobacco alkaloid, and combinations thereof.

5) The oral composition as claimed in claim 1, wherein the active compound, is preferably selected from a nicotine salt, nicotine free base, nicotine bound to an ion exchanger, a nicotine inclusion complex or nicotine in any non-covalent binding; nicotine bound to cellulose, and a combination thereof.

6) The oral composition as claimed in claim 1, wherein said filler is microcrystalline cellulose.

7) The oral composition as claimed in claim 1, wherein said polyol is selected from xylitol, maltitol, mannitol, erythritol, isomalt, sorbitol, lactitol and mixtures thereof.

8) The oral composition as claimed in claim 7, wherein said polyol is preferably mannitol, erythritol or mixtures thereof.

9) The oral composition as claimed in claim 1, wherein said composition further comprises other excipients selected from the group consisting of sweeteners, gums, binding agents, pH regulator or a combination thereof.

10) The oral composition as claimed in any of the preceding claims, wherein said oral composition is contained within a pouch, which is made up of a water permeable fabric.

11) The oral composition as claimed in claim 1, wherein said flavors is selected from paan, anise, vanilla, coffee, chocolate, cream, mint, spearmint, menthol, peppermint, wintergreen, lavender, cardamom, nutmeg, cinnamon, clove/eugenol, cascarilla, sandalwood, honey, jasmine, sage, licorice, lemon, orange, apple, peach, lime, cherry, eucalyptus, strawberry, berry flavors such as pomegranate, raspberry, blueberry, , boysenberry, and/or cranberry, , , , citrus, olive oil, sesame oil, sunflower oil, bergamot oil, geranium oil, lemon oil, , thymol, and/or tea tree and combinations thereof.

12) The oral composition as claimed in any of the preceding claims, wherein said composition delivers a long-lasting flavor for a time period of about 60 mins, preferably for 45 mins when the composition comes in contact with water.

13) The oral composition according to any of the preceding claims, wherein said composition has an angle of repose of not more than 40.

14) The oral composition according to any of the preceding claims, wherein said composition has a water activity of less than 0.72 aw.

15) The oral composition as claimed in claim 9, wherein the pH regulator is selected from the group comprising sodium carbonate, sodium bicarbonate, potassium carbonate, potassium bicarbonate, magnesium carbonate or combination thereof.

16) The oral composition as claimed in any of the preceding claims, wherein said composition has a pH of about 7.

17) An oral delivery product comprising the oral, non-aqueous composition as claimed in any claims 1 to 16 and a pouch; wherein said composition is formulated in the pouch and said pouch is made of a water permeable fabric.

18) A method for delivering active, said method comprises providing an oral, non-aqueous composition as claimed in any claims 1 to 16 in the pouch format; such that said method results in delivery of a long-lasting flavor for a time period of about 60 mins, preferably for 45 mins when the composition comes in contact with water.