WO2006072879A1 - Preparation of sweetener tablets of stevia extract by dry granulation methods - Google Patents

Preparation of sweetener tablets of stevia extract by dry granulation methods Download PDF

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Publication number
WO2006072879A1
WO2006072879A1 PCT/IB2006/000016 IB2006000016W WO2006072879A1 WO 2006072879 A1 WO2006072879 A1 WO 2006072879A1 IB 2006000016 W IB2006000016 W IB 2006000016W WO 2006072879 A1 WO2006072879 A1 WO 2006072879A1
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Prior art keywords
tablet
stevia extract
dry granulated
granulated sweetener
sweetener
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Application number
PCT/IB2006/000016
Other languages
French (fr)
Inventor
Chandra Kant Katihyar
Arvind Padiyar
Avinash Narwaria
Rahul Singh
Roopak Kumar
Anil Kanaujia
Yogita Rani
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Ranbaxy Laboratories Limited
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Publication of WO2006072879A1 publication Critical patent/WO2006072879A1/en

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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L27/00Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
    • A23L27/30Artificial sweetening agents
    • A23L27/33Artificial sweetening agents containing sugars or derivatives
    • A23L27/36Terpene glycosides
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23PSHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
    • A23P10/00Shaping or working of foodstuffs characterised by the products
    • A23P10/20Agglomerating; Granulating; Tabletting
    • A23P10/25Agglomeration or granulation by extrusion or by pressing, e.g. through small holes, through sieves or between surfaces

Definitions

  • the technical field of the present invention relates to sweetener tablets of stevia extract prepared by dry granulation methods.
  • Stevia rebaudiana Bertoni is a perennial shrub of the Asteraceae (Compositae) family native to Paraguay and Brazil. Leaves of Stevia rebaudiana are well known for their sweetening properties.
  • the sweet compounds are mainly the diterpene glycosides based on the kaurene skeleton that represents about 14% constituent of dried leaves.
  • the sweet diterpene glycosides include stevioside, steviolbioside, rebaudioside A, B, C, D and E, and dulcoside A and B. Steviol is the aglycone moiety in all these glycosides.
  • the major sweet components are stevioside, which has a molecular weight of 804.9 and a melting point between 196-198 0 C, and rebaudioside A, which has a molecular weight of 967.0 and a melting point between 242-244 0 C.
  • Stevia rebaudiana extract is widely accepted worldwide as a food for use as a dietary supplement and also as a natural sweetener, particularly in foods and beverages.
  • the major component, stevioside is heat and pH stable. It is approximately three hundred times sweeter than sucrose, and has zero calorific value. It has been used for more than twenty years in Japan with no adverse effects reported so far.
  • the major component stevioside apart from its high level of sweetness, also has inherent properties of unpleasant and undesirable menthol-like bitter aftertaste. The unpleasant taste is also contributed to by volatile aromatic or essential oils, tannins, and flavanoids present in Stevia leaf extract (Stevia extract).
  • Sweetener compositions of stevia extract are disclosed in various publications.
  • Japanese patent 3046763 discloses irregular shaped cubes of stevioside that maybe readily mixed in beverages like coffee and tea.
  • Laid open Japanese patent application 4287659 discloses powder composition of stevioside mixed with polydextrose, maltitol, erythritol and thaumatin.
  • Japanese patent 53044666 discloses sweetener compositions of stevioside and maltitol for use in low-calorie gelatin jelly.
  • Stevia extract is fluffy in nature and therefore difficult to compress into tablets as such using conventional tabletting techniques involving aqueous or non-aqueous granulation.
  • the tablets develop problems of capping, sticking, and disintegrate slowly, which are undesirable problems when forming tablets. Further, direct compression of stevia extract particles leads to excessive sticking.
  • a dry granulated sweetener tablet comprising stevia extract.
  • Embodiments of the tablet may include one or more of the following features.
  • the stevia extract may make up from about 5% w/w to about 50% w/w of the tablet.
  • the stevia extract may make up from about 15% w/w to about 25% w/w of the tablet.
  • the stevia extract may be stevioside.
  • the stevia extract may be at least 30% w/w stevioside.
  • the stevia extract may further include rebaudioside A.
  • the stevia extract may include at least 10% w/w rebaudioside A.
  • the tablet may further include one or more inert excipients.
  • the one or more inert excipients may be flavors, disintegrants/superdisintegrants, binders, fillers, suspending agents, surfactants, colors, and lubricants/glidants.
  • the flavor may be any FEMA/GRAS approved flavor for oral use. In particular, the flavor may be maltol.
  • the tablet may disintegrate in water in less than about 180 seconds. In particular, the tablet may disintegrate in water in less than about 60 seconds.
  • the tablet may have a hardness of at least 1 kg.
  • the tablet may further include an active pharmaceutical ingredient.
  • a process for preparing a dry granulated sweetener tablet of stevia extract including (i) forming a compact mass of stevia extract or stevia extract and one or more inert excipients; (ii) milling and/or sieving the compact mass to form granules; (iii) optionally blending with one or more inert excipients; and (iv) compressing into tablets.
  • Embodiments of the process may include one or more of the following features or those described herein.
  • the compact mass may be prepared in a tablet press, a roller compactor or a chilsonator.
  • the process may further include an active pharmaceutical ingredient in either or any of the compact mass, granules, and blend.
  • a method of treating a medical condition includes administering a pharmaceutical composition comprising a dry granulated tablet that includes an active pharmaceutical ingredient indicated for the medical condition and stevia extract.
  • a pharmaceutical composition comprising a dry granulated tablet that includes an active pharmaceutical ingredient indicated for the medical condition and stevia extract.
  • Embodiments of the method and tablet may include any one or more of the features described herein or above.
  • sweetener tablets of stevia extract having acceptable disintegration properties may be prepared by processes involving dry granulation.
  • dry granulated sweetener tablets comprising stevia extract.
  • a process of preparing dry granulated sweetener tablets of stevia extract wherein the said process comprises the steps of;
  • the compact mass may be prepared in conventionally used compactors such as roller compactors and chilsonators, or by the process of slugging in a tablet press.
  • the present invention may provide a simple and cost effective method of preparing tablets of the poorly compressible stevia extract. Dry granulation methods of preparing stevia extract tablets involve a compaction process. During compaction the air entrapped in the stevia extract is released, facilitating compression into tablets of low friability and acceptable disintegration properties.
  • Stepvia extract refers to an aqueous extract obtained from leaves of Stevia rebaudiana. It is a white, free flowing, fluffy granular powder having an extremely sweet taste, and comprising at least 30% w/w stevioside and at least 10% w/w rebaudioside A, and in particular at least 50% w/w stevioside and at least 20% w/w rebaudioside A.
  • the amount of stevia extract in the tablet may vary from about 5% w/w to about 50% w/w of the sweetener tablets and, in particular, it may vary from about 15% w/w to about 25% w/w.
  • dry granulated sweetener tablet may comprise stevia extract and one or more inert excipients.
  • inert excipient includes all physiologically inert excipients used in the art for preparation sweetener compositions. Examples include flavors, disintegrants/superdisintegrants, binders, fillers, suspending agents, surfactants, lubricants/glidants, colors, and the like.
  • the bitter aftertaste of stevioside may be masked by inclusion of one or more flavors in the sweetener tablet composition.
  • flavors include any FEMA/GRAS approved flavor for oral use.
  • flavors comprising maltol may be used.
  • Maltol (Larixinic acid) is a white, crystalline compound obtained from larch bark, pine needles, chicory, and roasted malt. Maltol is soluble in water and glycerine, slightly soluble in alcohols and chloroform, and has a melting point of 161 0 C. Maltol and its derivatives have a caramel-like odor and are used as versatile flavor enhancers and modifiers (sweet, caramel, fruity, strawberry) in foods, wines, and perfumes. Commercially, maltol is available under various trade names such as Veltol and Pyromaltol. Maltol also is an important constituent of many flavors approved for oral use, for example, Contramarum Forte (Flavour 225023) obtained from Symrise.
  • Contramarum Forte Frazier 225023
  • Contramarum Forte Flavour comprises maltodextrin, gum arabic, and artificial and natural identical ingredients like menthyl esters and food esters.
  • maltol On combining maltol with stevia extract in sweetener tablet compositions, the bitter aftertaste is masked to acceptable levels. Further, maltol is required in very low quantity.
  • Specific examples of disintegrants/superdisintegrants include starch, cellulose derivatives, natural and synthetic gums, sodium starch glycolate, croscarmellose sodium, crospovidone, and low-substituted hydroxypropylcellulose. Extremely fast disintegration may be achieved by using superdisntegrants.
  • binders include starch; gelatin; sugars such as molasses, lactose, glucose, dextrose and sucrose; and natural and synthetic gums such as acacia, sodium alginate, carboxymethyl cellulose, methylcellulose, polyvinyl pyrrolidone and veegum.
  • fillers include calcium carbonate, calcium phosphate-dibasic, calcium phosphate-tribasic, calcium sulfate, microcrystalline cellulose, powdered cellulose, dextrates, dextrins, fructose, kaolin, lactitol, lactose, mannitol, sorbitol, starch, sucrose, sugar compressible, and sugar confectioners.
  • microcrystalline cellulose may be used.
  • suspending agents include microcrystalline cellulose, sodium carboxy methylcellulose, colloidal anhydrous silica, mannitol, povidone, sodium starch glycolate, and veegum.
  • surfactants include both non-ionic and ionic (cationic, anionic and zwitterionic) surfactants suitable for use in sweetener compositions. These include polyethoxylated fatty acids and their derivatives, for example, polyethylene glycol 400 distearate, polyethylene glycol - 20 dioleate, polyethylene glycol 4 -150 mono dilaurate, polyethylene glycol -20 glyceryl stearate; alcohol - oil transesterification products, for example, polyethylene glycol - 6 corn oil; polyglycerized fatty acids, for example, polyglyceryl - 6 pentaoleate; propylene glycol fatty acid esters, for example, propylene glycol monocaprylate; mono and diglycerides, for example, glyceryl ricinoleate; sterol and sterol derivatives; sorbitan fatty acid esters and their derivatives, for example, polyethylene glycol - 20 sorbitan monooleate and sorb
  • lubricants/glidants include colloidal anhydrous silica, stearic acid, magnesium stearate, calcium stearate, zinc stearate, sodium stearyl fumarate, talc, hydrogenated castor oil, sucrose esters of fatty acid, microcrystalline wax, yellow beeswax, and white beeswax.
  • colors include any approved color for oral use.
  • Sweetener tablets prepared according to any of the embodiments above showed a hardness of about 1.5-2.0 kg and a disintegration time of less than about 3 minutes, in particular less than about 1 minute.
  • dry granulated sweetener tablets of stevia extract may be prepared by a process comprising the steps of
  • step (iii) blending the granules of step (ii) with one or more of filler, superdisintegrants, and lubricant/glidant;
  • the sweetener tablets prepared above may comprise a flavoring agent, particularly maltol.
  • Stevia extract was dried in a hot air oven at 70 0 C for 3 hours and then blended with lactose (only compact mass 2).
  • Dried stevia extract or blend with lactose was fed into a roller compactor to form a compact mass.
  • the compactor parameters were as follows: screw feeder speed, 40 rpm; Roller speed, 4 rpm; and Hydraulic pressure, 20 bars (for compact mass 1) and 90 bars (for compact mass 2).
  • step 2 The compact masses of step 2 were passed through a # 30 sieve using an oscillating granulator.
  • Croscarmellose sodium, silicon dioxide and stearic acid were individually sieved through a # 60 sieve. 2. The sieved croscarmellose sodium, silicon dioxide and stearic acid of step 1 were blended in a suitable mixer followed by blending with a part of the lactose.
  • the stevia extract granules prepared above were then added to the blend of step 2 and mixed for about 5-10 minutes, followed by blending with the remaining part of lactose for about 10-15 minutes.
  • step 3 The blend of step 3 was compressed into 100 mg tablets using appropriate tooling.
  • the dry granulated stevia extract tablets can be a taste masking agent in a pharmaceutical dosage form with an active ingredient.
  • Such pharmaceutical dosage forms can be made using the processes described herein with slight modifications as needed.
  • Maltol can be used in the pharmaceutical compositions as desired.
  • the pharmaceutical composition can be administered to treat a medical condition for which the active pharmaceutical ingredient is indicated or recommended. Accordingly, it is not intended that the inventions be limited, except as by the appended claims.

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  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Health & Medical Sciences (AREA)
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  • Medicinal Preparation (AREA)

Abstract

The present invention relates to sweetener tablets of stevia extract prepared by dry granulation methods. It further relates to pharmaceutical compositions that include stevia extract prepared by dry granulation methods.

Description

PREPARATION OF SWEETENER TABLETS OF STEVIA EXTRACT BY DRY GRANULATION METHODS
Technical Field of the Invention
The technical field of the present invention relates to sweetener tablets of stevia extract prepared by dry granulation methods.
Background of the Invention
Stevia rebaudiana Bertoni is a perennial shrub of the Asteraceae (Compositae) family native to Paraguay and Brazil. Leaves of Stevia rebaudiana are well known for their sweetening properties. The sweet compounds are mainly the diterpene glycosides based on the kaurene skeleton that represents about 14% constituent of dried leaves. The sweet diterpene glycosides include stevioside, steviolbioside, rebaudioside A, B, C, D and E, and dulcoside A and B. Steviol is the aglycone moiety in all these glycosides. Among these, the major sweet components are stevioside, which has a molecular weight of 804.9 and a melting point between 196-1980C, and rebaudioside A, which has a molecular weight of 967.0 and a melting point between 242-2440C.
Stevia rebaudiana extract is widely accepted worldwide as a food for use as a dietary supplement and also as a natural sweetener, particularly in foods and beverages. The major component, stevioside, is heat and pH stable. It is approximately three hundred times sweeter than sucrose, and has zero calorific value. It has been used for more than twenty years in Japan with no adverse effects reported so far. However, the major component stevioside, apart from its high level of sweetness, also has inherent properties of unpleasant and undesirable menthol-like bitter aftertaste. The unpleasant taste is also contributed to by volatile aromatic or essential oils, tannins, and flavanoids present in Stevia leaf extract (Stevia extract). Sweetener compositions of stevia extract are disclosed in various publications. For example, Japanese patent 3046763 discloses irregular shaped cubes of stevioside that maybe readily mixed in beverages like coffee and tea. Laid open Japanese patent application 4287659 discloses powder composition of stevioside mixed with polydextrose, maltitol, erythritol and thaumatin. Japanese patent 53044666 discloses sweetener compositions of stevioside and maltitol for use in low-calorie gelatin jelly.
Stevia extract is fluffy in nature and therefore difficult to compress into tablets as such using conventional tabletting techniques involving aqueous or non-aqueous granulation. The tablets develop problems of capping, sticking, and disintegrate slowly, which are undesirable problems when forming tablets. Further, direct compression of stevia extract particles leads to excessive sticking.
Summary of the Invention
In one general aspect there is provided a dry granulated sweetener tablet comprising stevia extract.
Embodiments of the tablet may include one or more of the following features. For example, the stevia extract may make up from about 5% w/w to about 50% w/w of the tablet. The stevia extract may make up from about 15% w/w to about 25% w/w of the tablet.
The stevia extract may be stevioside. The stevia extract may be at least 30% w/w stevioside. The stevia extract may further include rebaudioside A. The stevia extract may include at least 10% w/w rebaudioside A.
The tablet may further include one or more inert excipients. The one or more inert excipients may be flavors, disintegrants/superdisintegrants, binders, fillers, suspending agents, surfactants, colors, and lubricants/glidants. The flavor may be any FEMA/GRAS approved flavor for oral use. In particular, the flavor may be maltol.
The tablet may disintegrate in water in less than about 180 seconds. In particular, the tablet may disintegrate in water in less than about 60 seconds. The tablet may have a hardness of at least 1 kg.
The tablet may further include an active pharmaceutical ingredient. In another general aspect there is provided a process for preparing a dry granulated sweetener tablet of stevia extract, the process including (i) forming a compact mass of stevia extract or stevia extract and one or more inert excipients; (ii) milling and/or sieving the compact mass to form granules; (iii) optionally blending with one or more inert excipients; and (iv) compressing into tablets.
Embodiments of the process may include one or more of the following features or those described herein. For example, the compact mass may be prepared in a tablet press, a roller compactor or a chilsonator. The process may further include an active pharmaceutical ingredient in either or any of the compact mass, granules, and blend.
In another general aspect there is provided a method of treating a medical condition. The method includes administering a pharmaceutical composition comprising a dry granulated tablet that includes an active pharmaceutical ingredient indicated for the medical condition and stevia extract. Embodiments of the method and tablet may include any one or more of the features described herein or above.
The details of one or more embodiments of the inventions are set forth in the description below. Other features, objects and advantages of the inventions will be apparent from the description and claims. Detailed Description of the Invention
We have now surprisingly discovered that sweetener tablets of stevia extract having acceptable disintegration properties may be prepared by processes involving dry granulation. Hence in one general aspect there is provided dry granulated sweetener tablets comprising stevia extract. In another general aspect there is provided a process of preparing dry granulated sweetener tablets of stevia extract wherein the said process comprises the steps of;
(i) forming a compact mass of stevia extract or stevia extract and inert excipient, (ii) milling and/or sieving the compact mass to form granules, (iii) optionally blending with inert excipient, and (iv) compressing into tablets.
The compact mass may be prepared in conventionally used compactors such as roller compactors and chilsonators, or by the process of slugging in a tablet press. The present invention may provide a simple and cost effective method of preparing tablets of the poorly compressible stevia extract. Dry granulation methods of preparing stevia extract tablets involve a compaction process. During compaction the air entrapped in the stevia extract is released, facilitating compression into tablets of low friability and acceptable disintegration properties.
The term "Stevia extract" as used herein refers to an aqueous extract obtained from leaves of Stevia rebaudiana. It is a white, free flowing, fluffy granular powder having an extremely sweet taste, and comprising at least 30% w/w stevioside and at least 10% w/w rebaudioside A, and in particular at least 50% w/w stevioside and at least 20% w/w rebaudioside A.
The amount of stevia extract in the tablet may vary from about 5% w/w to about 50% w/w of the sweetener tablets and, in particular, it may vary from about 15% w/w to about 25% w/w.
In one of the embodiments, dry granulated sweetener tablet may comprise stevia extract and one or more inert excipients. The term "inert excipient" as used herein includes all physiologically inert excipients used in the art for preparation sweetener compositions. Examples include flavors, disintegrants/superdisintegrants, binders, fillers, suspending agents, surfactants, lubricants/glidants, colors, and the like.
The bitter aftertaste of stevioside may be masked by inclusion of one or more flavors in the sweetener tablet composition. Examples of flavors include any FEMA/GRAS approved flavor for oral use. In particular, flavors comprising maltol may be used.
Maltol (Larixinic acid) is a white, crystalline compound obtained from larch bark, pine needles, chicory, and roasted malt. Maltol is soluble in water and glycerine, slightly soluble in alcohols and chloroform, and has a melting point of 1610C. Maltol and its derivatives have a caramel-like odor and are used as versatile flavor enhancers and modifiers (sweet, caramel, fruity, strawberry) in foods, wines, and perfumes. Commercially, maltol is available under various trade names such as Veltol and Pyromaltol. Maltol also is an important constituent of many flavors approved for oral use, for example, Contramarum Forte (Flavour 225023) obtained from Symrise. Besides maltol, Contramarum Forte Flavour comprises maltodextrin, gum arabic, and artificial and natural identical ingredients like menthyl esters and food esters. On combining maltol with stevia extract in sweetener tablet compositions, the bitter aftertaste is masked to acceptable levels. Further, maltol is required in very low quantity. Specific examples of disintegrants/superdisintegrants include starch, cellulose derivatives, natural and synthetic gums, sodium starch glycolate, croscarmellose sodium, crospovidone, and low-substituted hydroxypropylcellulose. Extremely fast disintegration may be achieved by using superdisntegrants.
Specific examples of binders include starch; gelatin; sugars such as molasses, lactose, glucose, dextrose and sucrose; and natural and synthetic gums such as acacia, sodium alginate, carboxymethyl cellulose, methylcellulose, polyvinyl pyrrolidone and veegum.
Specific examples of fillers include calcium carbonate, calcium phosphate-dibasic, calcium phosphate-tribasic, calcium sulfate, microcrystalline cellulose, powdered cellulose, dextrates, dextrins, fructose, kaolin, lactitol, lactose, mannitol, sorbitol, starch, sucrose, sugar compressible, and sugar confectioners. In particular, microcrystalline cellulose may be used.
Specific examples of suspending agents include microcrystalline cellulose, sodium carboxy methylcellulose, colloidal anhydrous silica, mannitol, povidone, sodium starch glycolate, and veegum.
Specific examples of surfactants include both non-ionic and ionic (cationic, anionic and zwitterionic) surfactants suitable for use in sweetener compositions. These include polyethoxylated fatty acids and their derivatives, for example, polyethylene glycol 400 distearate, polyethylene glycol - 20 dioleate, polyethylene glycol 4 -150 mono dilaurate, polyethylene glycol -20 glyceryl stearate; alcohol - oil transesterification products, for example, polyethylene glycol - 6 corn oil; polyglycerized fatty acids, for example, polyglyceryl - 6 pentaoleate; propylene glycol fatty acid esters, for example, propylene glycol monocaprylate; mono and diglycerides, for example, glyceryl ricinoleate; sterol and sterol derivatives; sorbitan fatty acid esters and their derivatives, for example, polyethylene glycol - 20 sorbitan monooleate and sorbitan monolaurate; polyethylene glycol alkyl ether or phenols, for example, polyethylene glycol - 20 cetyl ether, polyethylene glycol - 10 — 100 nonyl phenol; sugar esters, for example, sucrose monopalmitate; polyoxyethylene — polyoxypropylene block copolymers known as "poloxamer"; and ionic surfactants, for example, sodium caproate, sodium glycocholate, soy lecithin, sodium stearyl fumarate, propylene glycol alginate, octyl sulfosuccinate disodium, and palmitoyl carnitine.
Specific examples of lubricants/glidants include colloidal anhydrous silica, stearic acid, magnesium stearate, calcium stearate, zinc stearate, sodium stearyl fumarate, talc, hydrogenated castor oil, sucrose esters of fatty acid, microcrystalline wax, yellow beeswax, and white beeswax. Examples of colors include any approved color for oral use.
Sweetener tablets prepared according to any of the embodiments above showed a hardness of about 1.5-2.0 kg and a disintegration time of less than about 3 minutes, in particular less than about 1 minute.
In one of the embodiments, dry granulated sweetener tablets of stevia extract may be prepared by a process comprising the steps of
(i) preparing a compact mass of stevia extract in conventionally used compactors such as a roller compactor, a chilsonator, and a tablet press;
(ii) milling and sieving through suitable sieves to form granules;
(iii) blending the granules of step (ii) with one or more of filler, superdisintegrants, and lubricant/glidant; and
(iv) compressing into tablets using appropriate toolings.
In another embodiment, the sweetener tablets prepared above may comprise a flavoring agent, particularly maltol.
The invention is further illustrated by the following examples, which are provided for illustrative purposes only and should not be construed as limiting the scope of the invention in any way. Examples Com act mass com osition of stevia extract
Figure imgf000008_0001
*A11 stevia extract particles pass through a # 100 sieve
Procedure
1. Stevia extract was dried in a hot air oven at 700C for 3 hours and then blended with lactose (only compact mass 2).
2. Dried stevia extract or blend with lactose was fed into a roller compactor to form a compact mass. The compactor parameters were as follows: screw feeder speed, 40 rpm; Roller speed, 4 rpm; and Hydraulic pressure, 20 bars (for compact mass 1) and 90 bars (for compact mass 2).
3. The compact masses of step 2 were passed through a # 30 sieve using an oscillating granulator.
Stevia extract tablet com osition
Figure imgf000008_0002
Procedure
1. Croscarmellose sodium, silicon dioxide and stearic acid were individually sieved through a # 60 sieve. 2. The sieved croscarmellose sodium, silicon dioxide and stearic acid of step 1 were blended in a suitable mixer followed by blending with a part of the lactose.
3. The stevia extract granules prepared above were then added to the blend of step 2 and mixed for about 5-10 minutes, followed by blending with the remaining part of lactose for about 10-15 minutes.
4. The blend of step 3 was compressed into 100 mg tablets using appropriate tooling.
The tablets prepared as per Examples 1 and 2 were tested for hardness using a Monsanto hardness tester and for in vitro disintegration by using an Electrolab® instrument. The values of the various parameters are listed below.
Figure imgf000009_0001
While several particular forms of the inventions have been described, it will be apparent that various modifications and combinations of the inventions detailed in the text can be made without departing from the spirit and scope of the inventions. For example, the dry granulated stevia extract tablets can be a taste masking agent in a pharmaceutical dosage form with an active ingredient. Such pharmaceutical dosage forms can be made using the processes described herein with slight modifications as needed. Maltol can be used in the pharmaceutical compositions as desired. The pharmaceutical composition can be administered to treat a medical condition for which the active pharmaceutical ingredient is indicated or recommended. Accordingly, it is not intended that the inventions be limited, except as by the appended claims.

Claims

We Claim: 1. A dry granulated sweetener tablet comprising stevia extract. 2. The dry granulated sweetener tablet of claim 1 wherein the stevia extract comprises from about 5% w/w to about 50% w/w of the tablet. 3. The dry granulated sweetener tablet of claim 2 wherein the stevia extract comprises from about 15% w/w to about 25% w/w of the tablet. 4. The dry granulated sweetener tablet of claim 1 wherein the stevia extract comprises stevioside. 5. The dry granulated sweetener tablet of claim 4 wherein the stevia extract comprises at least 30% w/w stevioside. 6. The dry granulated sweetener tablet of claim 4 wherein the stevia extract further comprises rebaudioside A. 7. The dry granulated sweetener tablet of claim 6 wherein the stevia extract comprises at least 10% w/w rebaudioside A. 8. The dry granulated sweetener tablet of claim 1 wherein the tablet further comprises one or more inert excipients. 9. The dry granulated sweetener tablet of claim 8 wherein the one or more inert excipients are selected from flavors, disintegrants/superdisintegrants, binders, fillers, suspending agents, surfactants, colors, and lubricants/glidants. 10. The dry granulated sweetener tablet of claim 9 wherein the flavor comprises any FEMA/GRAS approved flavor for oral use. 11. The dry granulated sweetener tablet of claim 9 wherein the flavor comprises maltol. 12. The dry granulated sweetener tablet of claim 1 wherein the tablet disintegrates in water in less than about 180 seconds. 13. The dry granulated sweetener tablet of claim 1 wherein the tablet disintegrates in water in less than about 60 seconds. 14. The dry granulated sweetener tablet of claim 1 wherein the tablet has a hardness of at least 1 kg. 15. The dry granulated sweetener tablet of claim 1 wherein the tablet further comprises an active pharmaceutical ingredient. 16. A process for preparing a dry granulated sweetener tablet of stevia extract, the process comprising: (i) forming a compact mass of stevia extract or stevia extract and one or more inert excipients; (ii) milling and/or sieving the compact mass to form granules; (iii) optionally blending with one or more inert excipients; and (iv) compressing into tablets. 17. The process of claim 16 wherein the compact mass is prepared in a tablet press. 18. The process of claim 16 wherein compact mass is prepared in a roller compactor or chilsonator. 19. The process of claim 16, further comprising including an active pharmaceutical ingredient in either or any of the compact mass, granules, and blend. 20. A method of treating a medical condition, the method comprising administering a pharmaceutical composition comprising a dry granulated tablet that includes an active pharmaceutical ingredient indicated for the medical condition and stevia extract.
PCT/IB2006/000016 2005-01-07 2006-01-06 Preparation of sweetener tablets of stevia extract by dry granulation methods WO2006072879A1 (en)

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US10952458B2 (en) 2013-06-07 2021-03-23 Purecircle Usa Inc Stevia extract containing selected steviol glycosides as flavor, salty and sweetness profile modifier
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