DESC:
FORM 2
THE PATENTS ACTS, 1970
(39 OF 1970)

COMPLETE SPECIFICATION
(See Section 10; rule 13)

“QUICK DISINTEGRATING FILM COATING COMPOSITION”

IDEAL CURES PVT. LTD., an Indian Company incorporated under the Indian Companies Act, 1956, of A-223 to A-229, 2nd Floor, Virwani Industrial Estate, Off Western Express Highway, Goregaon (East), Mumbai-400 063, India.

The following specification particularly describes the invention and the manner in which it is to be performed.

Field of the Invention

The present invention relates to a quick disintegrating film coating compositions comprising very low viscosity at a very high solid content particularly, the novel quick disintegrating film coating compositions of the current invention are capable of being dispersed at the high solids level in solvents that help in significant reduction in the coating process time by providing sprayability at high spray rates. The present invention further relates to the novel quick disintegrating film coating compositions capable of performing disintegration within 25 seconds of contact with water.

Background of the invention

Coating is a process by which an essentially dry, outer layer of coating material is applied to the surface of a dosage form in order to confer specific benefits over uncoated variety. It covers application of a sugar or polymeric coat on the tablet. It may serve various purposes like protect the inner contents from moisture, provide strength to the dosage forms, serve to release the inner contents at specified locations in the body like intestine or colon, to mask the taste of the bitter ingredients for better palatability or also to provide a smooth, better and glossy appearance to the tablets. Usually tablets coating are classified as sugar coatings, film coatings and compression or press coatings.

Various quick disintegrating films coating are available for the delivery of active agents such as pharmaceuticals, nutritional supplements (e.g., vitamins and minerals), and cosmetic agents (e.g., tooth-whiteners, breath fresheners, etc.). Often, such films are adapted for oral administration and intended to quickly disintegrate within the oral cavity. The advantages of quick disintegrating film coating composition comprising a very low viscosity at high solid content include reduce coating process time, increase production capacity by reducing process time, provide superior product appearance, simple to use on all types of coating equipment, wide processing capability, easy application, greater aqueous film coating uniformity due to low viscosity and yields desired weight gains in less time.

The problem associated with known film coating composition is that the relatively low dosage of active ingredients that can be included in the film. In order to achieve the desired flexibility, strength, integrity, and ease of handling, film-forming polymers typically comprise the majority of the weight of a dried film, with other excipients (e.g., plasticizers, flavorings, colorants, etc.) also comprising a substantial proportion of the dried film. This leaves a relatively small proportion of the dried film available for the active agent(s). Thus, the administration of a high dosage of an active agent may require the use of an unacceptably large film or the administration of multiple smaller dosages of the active agent in a standard-sized film.

An additional shortcoming of known film preparations is the incompatibility of high dosages of many active agents and common film-forming polymers. In some cases, this is due, in part, to the shortcoming above, i.e., a relatively high proportion of film-forming polymer is needed to produce a film preparation having the desired integrity, strength, and flexibility. In other cases, the incompatibility of high dosages of active agents and film-forming polymers may be due to an actual chemical incompatibility. As a result of these shortcomings, film coating preparations have not been a viable form of administration of some active agents, particularly where a relatively high dosage of the active agent is required.

Various patents and patent applications have also been filed for film coating compositions.

U.S. Patent No. 6723342 discloses edible coating compositions comprising a combination of microcrystalline cellulose, carrageenan, at least one strengthening polymer or a plasticizer. The specification discloses that the coating compositions can be dispersed at a concentration preferably between 8% to 11% of dry ingredients in water.

U.S. Patent No. 6994872 discloses coating that was conducted using a sugar-coating liquid formulated by mixing 40 parts of sucrose, 0.4 part of polyvinylpyrrolidone, 4 parts of polyethylene glycol 6000, 16 parts of calcium carbonate, 8 parts of talc and 31.6 parts of purified water, the parts being by weight. The coating method is traditional sugar coating wherein 4-10 ml per application of above sugar-coating liquid was applied to the tablets 30 times in total, at about 10 minutes' intervals.

U.S. Patent No. 9278063 discloses press coated orally disintegrating tablets having a powder/granular material with poor formability and an outer layer surrounding an inner core wherein the inner core has a thickness in the range of 30 to 80% per that of the whole tablet, and the outer layer comprises (a) microcrystalline cellulose, (b) a sugar or a sugar alcohol, and (c) one or more particular ingredients selected from the group consisting of crospovidone, starches, low-substituted hydroxypropylcellulose and carmellose.

Quick disintegrating films are well known in the prior art which use super disintegrants for disintegration of the inner contents of the tablets. Mostly these are related to having the drugs to be a part of the film. Some of the prior art which discloses such technology is disclosed as under.

U.S. Patent Application No, 2011305768discloses a quick-dissolving thin film composition comprising: a) one or more water-soluble polymers; b) one or more mucoadhesive polymers; one or more pH-sensitive microparticles, or mixtures thereof; and c) one or more bioactive agents, wherein said bioactive agents are independently encapsulated within said microparticles when said microparticles are present.

E.P. Patent Application No. 2493454 discloses fast dissolving/disintegrating coating compositions. A pharmaceutical dosage form comprising a core and a film coating, wherein the film coating comprises hydroxypropylcellulose and a super-disintegrant.

E.P. Patent Application No. 2131824 discloses the invention provides a fast-dissolving or fast-disintegrating film preparation having a high proportion (i.e., at least about 40%) of active agent(s) and at least one water-soluble polymer, preferably pullulan, comprising from 10% and 40%.

A need therefore exists to have a quick disintegrating film preparation suitable of oral administration comprising very low viscosity at very high solid content.

Object of the invention

The object of the current invention is to provide a quick disintegrating film coating composition comprising a very low viscosity at high solids content, capable of being sprayed at high spray rates, reduces coating process time and reduces carbon footprint by using lesser organic solvents. Another object of the present invention is to provide novel quick disintegrating film coatings having good strength and adhesion, and which disintegrate within 25 secs of contact with water.

Summary of the Invention:

Accordingly, the present invention provides a quick disintegrating film coating composition comprising very low viscosity at a very high solid content. The film coating compositions of the current invention are capable of being dispersed at high solids in solvents that help in significant reduction in the coating process time by providing sprayability at high spray rates.

In particular, the invention provides novel quick disintegrating film coating composition comprising a very low viscosity at high solid content and process of preparation thereof. Additionally, the selective use of excipients in the present invention is capable of being sprayed at high spray rates, reduces coating process time, greater aqueous film coating uniformity due to low viscosity and yields desired weight gains in less time.

In particular, the present invention provides novel quick disintegrating film coating compositions, the main components of which include a film forming polymer, a sugar or a sugar alcohol, a cellulosic polymer and other optional pharmaceutically acceptable excipients.

In one embodiment the present invention provides novel quick disintegrating film coating compositions which are in dry powder form and capable of being reconstituted in water at up to 35 % w/w of solids content.

In another embodiment of the invention, the film forming polymer may be present in a range of 2 to 20 %w/w of the film coating composition.

In another embodiment of the invention, the sugar or the sugar alcohol may be present in a range of 10 to 50 %w/w of the film coating composition.

In another embodiment of the invention, the cellulosic polymer may be present in a range of 5 to 25 %w/w of the film coating composition.

In another embodiment of the invention, the film coating composition may additionally comprise at least one of: plasticizer(s), anti-tacking agent(s), and colorant(s)/pigment(s).

In another embodiment of the invention, the plasticizer(s), if present, may be present in a range of 2 to 20 %w/w of the film coating composition.

In another embodiment of the invention, the anti-tacking agent(s), if present, may be present in a range of 2 to 30 %w/w of the film coating composition.

In another embodiment of the invention, the colorant(s)/pigment(s), if present, may be present in a range of 0.5 to 30 %w/w of the film coating composition.

In another embodiment of the invention, the film coating compositions comprise 2 to 20% w/w film forming polymer, 10 to 50% w/w sugar alcohol, 5 to 25% w/w cellulosic polymer, optionally 2 to 20% w/w plasticizer, optionally, 2 to 30% w/w anti-tacking agents, optionally 0.5 to 30% w/w colorants/pigments.

In still another embodiment of the invention, the film coating compositions comprise polyvinylpyrrolidone in an amount of from 2 to 20% w/w, Maltodextrin in an amount of from 10 to 50% w/w, microcrystalline cellulose in an amount of from 5 to 25% w/w and optionally, plasticizer(s) in an amount of from 2 to 20% w/w, anti-tacking agent(s) in an amount of from 2 to 30% w/w, and colorant(s)/pigment(s) in an amount of from 0.5 to 30% w/w.

It may be noted that in addition to film forming composition comprising the aforesaid ingredients / components in the weight percentages as mentioned above.

The details of one or more embodiments of the inventions are set forth in description below. Other features, objects and advantages of the inventions will be apparent from the description and claims.

Detailed description of the invention:

For the purpose of promoting an understanding of the principles of the invention, reference will now be made to the embodiment and specific language will be used to describe the same. It will nevertheless be understood that no limitation of the scope of the invention is thereby intended, such alterations and further modifications to the composition and the process for preparation, and such further applications of the principles of the invention as illustrated therein being contemplated as would normally occur to one skilled in the art to which the invention relates.

It will be understood by those skilled in the art that the foregoing general description and the following detailed description are exemplary and explanatory of the invention and are not intended to be restrictive thereof.

Reference throughout this specification to “an aspect”, “another aspect” or similar language means that a particular feature, structure, or characteristic described in connection with the embodiment is included in at least one embodiment of the present invention. Thus, appearances of the phrase “in an embodiment”, “in another embodiment” and similar language throughout this specification may, but do not necessarily, all refer to the same embodiment.

The terms "comprises", "comprising", or any other variations thereof, are intended to cover a non-exclusive inclusion, such that a process or method that comprises a list of steps does not include only those steps but may include other steps not expressly listed or inherent to such process or method. Similarly, one or more compounds or group of compounds proceeded by "comprises... a" does not, without more constraints, preclude the existence of other compounds or groups of compounds.

Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The system, methods, and examples provided herein are illustrative only and not intended to be limiting.

Embodiments of the present invention will be described below in detail.

There have been several modifications in the coating methods used over a couple of decades. These changes are not only limited to the coating process and equipment but also to the kind of ingredients that are used in making the coating materials. With the increasing quest of finding quicker and easier methods for coating and evolution of robust technologies there has been a change in the way the tablets are coated.

Traditional methods of coating include sugar coatings, film coatings and more recently compression coatings. Sugar coatings have been widely used in the food industry for coating of various consumables and confectionary items. It involves the repetitive deposition of sugar onto the substrates, such that there is a thick layer of sugar on the substrate. There is no film formation, and hence these coatings are brittle and are prone to chipping ifsubjected to an inappropriate mechanical stress. Moreover, due to their susceptibility to moisture, these coatings are not suitable particularly for coating substrates that are moisture sensitive. The sugar coating process involves plurality of steps namely sealing (water proofing- to provide moisture protection), grossing (smoothening), coloring (for providing color to the end product) and polishing (giving the final product a glossy appearance). It also requires skilled labor and long hours for the final product to be manufactured. Usually, the weight gain in these coatings is around 100% to 200%. Therefore, another disadvantage is that the tablets tend to be bulky.

Compression coatings or press coatings use pressure to form a coating over the substrate. Usually, it is dry process and doesn’t involve use of any solvents.This method also doesn’t involve the formation of film. However, one major drawback of such coatings is that they require the core material and other excipients of the formulation to possess excellent flow properties. Not all the ingredients have such properties, therefore it becomes necessary for first prepare the ingredients so that they possess essential flow properties. In alternate cases, excess of lubricants and anti-tacking agents are needed to be added to provide flow properties.

Even though, all the techniques described herein are pertaining to having a covering on top of the inner core that comprises the tablet, the methods differ in the coating process requirements, equipment, ease of use and time.Each method has its inherent advantages and shortcomings and usually the method of choice is basically dependent on kind of active ingredients to be coated. Film coatings are most preferred and comprise almost 80% or all the coatings that are done on pharmaceutical tablets. Film coating is the deposition of a thin film polymeric film onto the substrates, mainly solid dosage forms, from dispersions that are reconstituted in either organic based solvents or purified water. Over the years the organic solvents have been replaced with aqueous solvents so that there is overall reduction in the carbon footprint of the process. Ideally the film coating compositions are reconstituted in purified water at a solid content of 15 -35 % w/w, and they have viscosities in the range from 40-400 cps at room temperature.

The instant invention relates to quick disintegrating film coating composition comprising a film forming polymer, a sugar or sugar alcohol, a cellulosic polymer and other optional pharmaceutical excipients. It is surprisingly seen by the inventors that the film forming composition of the present invention comprising 2 to 20% w/w film forming polymer, 10 to 50 % w/w sugar or sugar alcohol, 5 to 25 % w/w cellulosic polymer, optionally 2 to 20% w/w plasticizer, optionally 2 to 30 % w/w anti-tacking agents, optionally, 0.5 to 30% w/w colorants/pigments is capable of being dispersed at high solids content in purified water, is capable of being sprayed at high spray rates and yields desired weight gains in less process time. It is further seen surprisingly by the inventors that the films thus obtained have good adhesion and strength, are capable of disintegrating rapidly within 25 secs of contact with water.

In one embodiment the invention relates to a dry quick disintegrating film coating composition capable of being reconstituted in water at ambient temperature at up to 35% solids content.

In another embodiment the invention relates to quickdisintegrating tablets that are capable of releasing the inner content of the solid dosage forms within 25 secs ofcontact with water.

In one embodiment, the "film forming polymer" as used herein refers to the polymers capable of forming film having monomeric units of N-vinylpyrrolidone like polyvinylpyrrolidone (alternate names povidone or polyvidone or PVP).

Polyvinylpyrrolidone is water - soluble, physiologically inert synthetic polymer consisting essentially of linear 1-vinyl-2-pyrrolidinone groups, with varying degree of polymerization which results in polyvinylpyrrolidone of different molecular weights. Polyvinylpyrrolidone is a water-soluble and hygroscopic polymerwhich may increase the drug permeability through formation of pores resulting fromrapid diffusion of polyvinylpyrrolidone into the surrounding diffusion medium.

The "sugar" as used herein means compounds having single or plurality of saccharide units, preferably the sugar being monosaccharides like glucose, maltose and disaccharides like lactose, lactose monohydrate or derivatives thereof. “Sugar alcohols” refer to derivatives of sugar containing alcoholic groups; preferably the sugar alcohol covers erythritol, lactitol, maltitol, maltodextrin, polydextrose or derivatives thereof.

The term “cellulosic polymer” refers to microcrystalline cellulose. It is added as an additive.

In one embodiment of the invention, the film coating composition may additionally comprise at least one of other pharmaceutically acceptable excipients: plasticizer(s), anti-tacking agent(s), and colorant(s)/pigment(s), flavour(s) and cooling agent(s).

The term "plasticizer" as used herein refers to the group of compounds having plasticizing property and helps in forming film with polymers. The plasticizer may be used alone or in combination with other plasticizers. These include triethyl citrate, polyethylene glycol, triacetin, glycerine and glyceride based plasticizers and phthalate based plasticizers.

The term "colorants/pigments" used herein refers to natural and synthetic colorants/pigments including but not limited to red, yellow and black iron oxides, titanium dioxide, calcium carbonate, zinc oxide, FD& C colors, lake colors and mica based pearlescent pigments. The composition of the present invention concerns to reduce the inherent flaws of polymer, for example coagulation, tackiness, clump formation, high viscosity, and non-conformity of dispersion, film unevenness etc.

The term "anti-tacking agents" used herein refers to substances that are added to reduce the stickiness of the coating compositions talc, calcium carbonate, silicon dioxide, Kaolin, modifies starch etc.

The term “composition” or “formulation” or “dosage form” or “preparation” has been employed interchangeably for the purpose of the present invention and mean that it is a pharmaceutical formulation which is suitable for administration to a patient. For the purpose of the present invention, the terms “controlled release” or “sustained release” or “extended release” or “modified release” or “prolonged release” have been used interchangeably and mean broadly that active agent is released at a predetermined rate that is different or slower than immediate release.

The term “very low viscosity” used herein refers to liquid with very low viscosity flows easily because its molecular makeup results in very little friction when it is in motion. The term “viscosity” used herein refers to resistance of a fluid to a change in shape, or movement of neighbouring portions relative to one another.

The term “very high solid content” as used herein refers to solids coating with a solids volume percent greater than 30% and, a single or two component coating formulated to have higher concentrations of solid components than a conventional coating but still maintain satisfactory coating or application properties in spite of the lower percentage of volatile organic compounds (VOCs). A high solids coating can be solvent, or water based, the advantages of high-solids coatings are reduced solvent use; reduce number of applications to achieve desired film thickness; reduce environmental problems; and reduce odor problems.

The quick disintegrating film coating compositions of the current invention are then reconstituted in water at high solids content or in a ratio of 1:1 with the solvent like purified water and coating onto desired substrates with suitable coating parameters.

A non-limiting list of suitable substrates that can be coated with the inventive coating system include compressed tablets, caplets, capsules, cores including pharmaceuticals, nutraceuticals and dietary supplements as well as any other art-recognized orally ingestible core.

In one embodiment, the quick disintegrating film coating composition of the present invention is coated with the composition of the present invention.

In one embodiment, the quick disintegrating film coating composition of the present invention is dispersed in purified water at high solids content with low viscosity.

The novel quick disintegrating film coating composition of present invention further provides reconstitution at high solids content, which means it, utilizes less solvent for forming dispersion, thereby contributing actively to the reduction in carbon footprints, reduction in coating process time which result in increase in production capacity, and greater aqueous film coating uniformity.

In one embodiment, the low viscosity of present quick disintegrating film coating composition helps in the achieving easy manageable coating process with reduced gun choking and makes it ideal for use in high volume batch process and continuous coating operations.

In another embodiment, the quick disintegrating film coating compositions of the present invention have good film adhesion and strength, and still capable of disintegrating/disintegrating the inner contents of the solid dosage forms within 25 secs of contact with water.

In another embodiment, the film forming polymer may be polyvinylpyrrolidone or povidone or polyvidone or PVP or hydroxypropyl cellulose and the like or combinations thereof.

In one embodiment, the cellulosic polymer may be microcrystalline cellulose or hydroxypropyl cellulose and the like or combinations.

In one embodiment, the at least one pharmaceutically acceptable excipient, that may be incorporated in the formulation of the present invention depending on the final dosage form to be prepared include, such as, but not limited to plasticizer(s), anti-tacking agent(s), and colorant(s)/pigment(s), flavour(s) and cooling agent.

Suitable plasticizers can be selected from, but not limiting to triethyl citrate,polyethylene glycol, propylene glycol, triacetin, glycerin and glyceride-based plasticizers and phthalate-based plasticizers or combination thereof. Examples of anti-tacking agents include, but are not limited to talc, glyceryl monostearate, Kaolin, stearic acids, calcium carbonate, silicon dioxide, modifies starch etc. Suitable colorants/pigments can be selected from, but not limiting to red, yellow and black iron oxides, titanium dioxide, calcium carbonate, zinc oxide, FD& C colors, lake colors, natural colourants and mica based pearlescent pigments or combination thereof.

In one embodiment, the components of the present invention work together collectively to provide films having good adhesion and strength characteristics and are capable of disintegrating rapidly within 25 secs of contact with water.

In further one embodiment, the quick disintegrating film coating composition of present invention comprising at least one film forming polymer in an amount of from 2 to 20% w/w, at least one sugar or sugar alcohol in an amount of from 10 to 50% w/w, at least one cellulosic polymer in an amount of from 5 to 25% w/w and plasticizer(s) in an amount of from 2 to 20% w/w is capable of providing films having good adhesion and strength characteristics and are capable of disintegrating rapidly within 25 secs of contact with water.

The one embodiment, the present invention also relates to a process for preparing quick disintegrating film coating compositions. The process of preparation comprises a) Blending dry components in blender and slowly added the wet ingredients to obtain a homogeneous dispersion by maintaining appropriate process parameters. b) Filtering the dispersion before spraying c) Spraying the dispersion onto placebo tablets using schlick spray gun.

In another embodiment, the present invention also relates to quick disintegrating film coating compositions comprising at least one second pharmaceutically active agent in addition to at least one pharmaceutically active agent present in the compositions.

While the invention has been described with reference to exemplary embodiments, it will be understood by those skilled in the art that various changes may be made and equivalents may be substituted for elements thereof without departing from the scope of the invention. In addition, many modifications may be made to adapt a particular situation or material to the teachings without departing from the essential scope thereof. Therefore, it is intended that the invention not be limited to the embodiment disclosed, but that the invention will include all embodiments falling within the scope thereof. Details of the present invention, including its objects and advantages, are provided in the non-limiting exemplary illustrations below.

The invention is further described in detail with the help of the following examples which are merely listed for the purposes of illustration and should not be considered to restrict the scope of the invention in any way. Any further embodiments that may be apparent to the person skilled in the art are considered to be under the scope of this invention.

EXAMPLES
Example 1
Ingredients % w/w
Povidone (PVPK-30) 10
Microcrystalline Cellulose (PH 105) 15
Lactose Monohydrate 30
PEG 6000 8
PEG 400 12
Talc 5
Titanium Dioxide 18
Indigo Carmine (22%) 2
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 1-2 gm/min onto round biconvex placebo tablets in a conventional pan coater at pan speed 40-44 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 2
Ingredients % w/w
Povidone (PVPK-30) 5
Microcrystalline Cellulose (PH 105) 10
Lactose Monohydrate 20
PEG 6000 8
PEG 400 12
Talc 20
Titanium Dioxide 23
Indigo Carmine (22%) 2
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 1-2 gm/min onto round biconvex placebo tablets in a conventional pan coater at pan speed 40-44 rpm; temperature 42-450C using 1mm gun size of schlick spray gun.

Example 3
Ingredients % w/w
Povidone (PVPK-30) 15
Microcrystalline Cellulose (PH 105) 20
Lactose Monohydrate 40
PEG 6000 6
PEG 400 8
Talc 4
Titanium Dioxide 6
Indigo Carmine (22%) 1
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 1-2 gm/min onto round biconvex placebo tablets in a conventional pan coater at pan speed 40-44 rpm; temperature 42-450C using 1mm gun size of schlick spray gun.

Example 4
Ingredients % w/w
Povidone (PVPK-30) 10
Microcrystalline Cellulose (PH 105) 15
Maltodextrin 30
Triacetin 10
Talc 10
Titanium Dioxide 23
Indigo Carmine (22%) 2
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex placebo tablets in Autocoater at pan speed 20-30 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 5
Ingredients % w/w
Povidone (PVPK-30) 5
Microcrystalline Cellulose (PH 105) 10
Maltodextrin 20
PEG 400 12
PEG 6000 8
Talc 20
Titanium Dioxide 23
Indigo Carmine (22%) 2
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex placebo tablets in Autocoater at pan speed 20-30 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.
Example 6
Ingredients % w/w
Povidone (PVPK-30) 15
Microcrystalline Cellulose (PH 105) 20
Maltodextrin 40
PEG 400 8
PEG 6000 6
Talc 4
Titanium Dioxide 6
Indigo Carmine (22%) 1
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex placebo tablets in Autocoater at pan speed 20-30 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 7

Ingredients % w/w
Povidone (PVPK-30) 10
Microcrystalline Cellulose (PH 105) 15
Lactose Monohydrate 30
Triacetin 10
Talc 10
Calcium Carbonate 25
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 1-2 gm/min onto round biconvex placebo tablets in a conventional pan coater at pan speed 40-44 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 8

Ingredients % w/w
Povidone (PVPK-30) 10
Microcrystalline Cellulose (PH 105) 15
Lactose Monohydrate 30
Triacetin 10
Calcium Carbonate 15
Modified Starch 10
Lake Erythrosine 10
Total 100

Manufacturing Procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 1-2 gm/min onto round biconvex tablets in a conventional pan coater at pan speed 40-44 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 9
Ingredients % w/w
Povidone (PVPK-30) 10
Microcrystalline Cellulose (PH 105) 15
Polydextrose 30
Triacetin 10
Calcium Carbonate 25
Modified Starch 10
Total 100

Manufacturing procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex tablets in auto-coater at pan speed 20-30 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 10
Ingredients % w/w
Povidone (PVPK-30) 5
Microcrystalline Cellulose (PH 105) 10
Polydextrose 20
PEG 400 12
PEG 6000 8
Talc 20
Titanium Dioxide 23
Indigo Carmine 2
Total 100

Manufacturing procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex tablets in auto-coater at pan speed 20-30 rpm; temperature 40-440C using 1mm gun size of schlick spray gun.

Example 11
Ingredients % w/w
Povidone (PVPK-30) 15
Microcrystalline Cellulose (PH 105) 20
Polydextrose 40
PEG 400 8
PEG 6000 6
Talc 4
Titanium Dioxide 6
Indigo Carmine 1
Total 100

Manufacturing procedure: All the dry components were mixed in blender and slowly added the wet ingredients in order to obtain a homogenous dispersion. The homogenization can be achieved by maintaining appropriate heating, stirring, mixing and other process parameters. To make the film coating dispersion 50gms of the film coating powder was reconstituted in 50gms of purified water to obtain dispersion with high solids content. Finally, the dispersion was filtered before spraying. The filtered dispersion as obtained was sprayed at spray rate 4-6 gm/min onto round biconvex tablets in auto-coater at pan speed 20-30 rpm; temperature 42-450C using 1mm gun size of schlick spray gun.

Table 1: Film Disintegration time of novel quick disintegrating film coating compositions.

Examples Film Disintegration time (Seconds)
1 18
2 20
3 20
4 7
5 8
6 19
7 19
8 18
9 17
10 10
11 20

The conventional film coating composition is capable of performing disintegration within 1-3 minutes of contact with water, whereas, quick disintegrating film coating composition is capable of early exposure of the core to the dissolution medium and is capable of performing disintegration within 25 seconds of water result in reduction in the time duration between administration and onset of action of the active agents. The advantages of quick disintegrating film coating compositions having very low viscosity at a very high solid content include coating suspension can be reconstituted up to 35% solids thus providing reductions in energy consumption and production costs, coating formulation optimized for rapid disintegration.

While specific language has been used to describe the disclosure, any limitations arising on account of the same are not intended. As would be apparent to a person in the art, various working modifications may be made to the method in order to implement the inventive concept as taught herein. The scope of embodiments is by no means limited by these specific examples. Numerous variations, whether explicitly given in the specification or not, such as differences in structure, dimension, and use of material, are possible. The scope of embodiments is at least as broad as given by the following claims.

,CLAIMS:WE CLAIM:

1. A novel quick disintegrating film coating composition comprising at least one film forming polymer in an amount of from 2 to 20% w/w, at least one sugar or sugar alcohol in an amount of from 10 to 50% w/w, at least one cellulosic polymer in an amount of from 5 to 25% w/wand optionally, other pharmaceutically acceptable excipients wherein, the film disintegrates within 25 seconds of contact with moisture.

2. The novel quick disintegrating film coating composition as claimed in claim 1, wherein, the film forming polymer is polyvinylpyrrolidone, hydroxypropyl cellulose or combinations thereof.

3. The novel quick disintegrating film coating composition as claimed in claim 1, wherein, the sugar or sugar alcohol is selected from the group consisting of glucose, maltose, mannitol, sorbitol, xylitol, lactose, lactose monohydrate, maltodextrin, polydextrose or combinations thereof.

4. The novel quick disintegrating film coating composition as claimed in claim 1, wherein, the cellulosic polymer is microcrystalline cellulose, hydroxypropyl cellulose or combinations thereof.

5.The novel quick disintegrating film coating composition as claimed in claim 1, wherein, other optional pharmaceutical excipients comprise at least one of: plasticizer(s) in an amount of from 2 to 20% w/w, anti-tacking agent(s) in an amount of from 2 to 30% w/w, and colorant(s)/pigment(s)in an amount of from 0.5 to 30% w/w.

6. The novel quick disintegrating film coating composition as claimed in claim 5, wherein, the plasticizer(s) is selected from the group consisting of triacetin, triethyl citrate, propylene glycol, polyethylene glycol, triglycerin and glyceridebased plasticizers and phthalate based plasticizers or combinations.

7. The novel quick disintegrating film coating composition as claimed in claim 5, wherein, the anti-tacking agents is selected from the group consisting of talc, glyceryl monostearate, kaolin, stearic acids, calcium carbonate, silicon dioxide, modified starch or combinations.

8. The novel quick disintegrating film coating composition as claimed in claim 5, wherein, the colorants/pigments is selected from the group consisting of red, yellow and black iron oxides, titanium dioxide, calcium carbonate, zinc oxide, natural colourants, FD& C colors, lake colors and mica based pearlescent pigment or combination thereof.

9.A novel quick disintegrating film coating composition comprising polyvinylpyrrolidone in an amount of from 2 to 20% w/w, Maltodextrin in an amount of from 10 to 50% w/w, microcrystalline cellulose in an amount of from 5 to 25% w/w and optionally, other pharmaceutically acceptable excipients wherein, the film disintegrates within 25 seconds of contact with moisture.

10. The novel quick disintegrating film coating composition as claimed in claim 9, wherein, other optional pharmaceutical excipients comprise at least one of: plasticizer(s) in an amount of from 2 to 20% w/w, anti-tacking agent(s) in an amount of from 2 to 30% w/w, and colorant(s)/pigment(s) in an amount of from 0.5 to 30% w/w.

Dated, this 14th day of JUNE, 2019.

Rajeshwari H.
OF RAJESHWARI & ASSOCIATES
AGENT FOR THE APPLICANT