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  Pharmaceutical Patents  

 

Title:  Effervescent composition and method of making an effervescent composition including a viscous component
United States Patent: 
7,507,396
Issued: 
March 24, 2009

Inventors:
 Aldritt; Mary (Excelsior, MN), Wehling; Fred (New Hope, MN), Lee; Robert E. (Maple Grove, MN)
Assignee:
  Amerilab Technologies, Inc. (Plymouth, MN)
Appl. No.:
 10/963,222
Filed:
 October 12, 2004


 

Outsourcing Guide


Abstract

Disclosed is an effervescent composition and a method of making an effervescent composition that includes a viscous component and is a free flowing granulation.

Description of the Invention

SUMMARY

In one aspect, the invention features a method of making an effervescent composition, the method including heating a viscous component to a temperature of at least 45.degree. C., the viscous component exhibiting a viscosity greater than 50,000 cps at 23.degree. C. and 1 sec.sup.-1 and a viscosity less than 5000 cps at a temperature of at least 38.degree. C. and 1 sec.sup.-1, heating a composition including an effervescent agent to a temperature of at least 45.degree. C., and combining the heated viscous component and the heated composition. In one embodiment, the viscous component is selected from the group consisting of honey, molasses, wax and combinations thereof. In other embodiments, the viscous component includes hop extract. In another embodiment, the viscous component includes kava.

In one embodiment, the effervescent composition includes from 5% by weight to 30% by weight of the viscous component. In another embodiment, the effervescent composition includes from about 5% by weight to about 25% by weight of the viscous component. In other embodiments, the effervescent composition includes from about 10% by weight to about 20% by weight the viscous component.

In some embodiments, the effervescent composition further includes a flow agent. In one embodiment, the flow agent is selected from the group consisting of silica, fumed silica, precipitated silica, magnesium oxide, calcium phosphate, magnesium carbonate, calcium silicate, sodium alumino silicate, and combinations thereof.

In other embodiments, the effervescent composition includes from 3% by weight to 20% by weight silica, or even from 5% by weight to 15% by weight silica.

In another aspect, the invention features a method of making a free flowing powder that includes an effervescent composition disclosed herein.

In other aspects, the invention features a method of making an effervescent tablet, the method including making an effervescent composition, and tableting the effervescent composition. In one embodiment, the tableting includes forming a tablet having a hardness of from 3 Kp to 15 Kp. In other embodiments, the tablet includes from 5% by weight to 30% by weight of the viscous component. In some embodiments, the tablet includes from about 10% by weight to about 20% by weight of the viscous component.

In another embodiment, the tablet further includes binder and lubricant.

In one embodiment, the method of making an effervescent composition, includes heating a viscous component having a viscosity greater than 50,000 cps at 23.degree. C. to a temperature sufficient to cause the component to exhibit a viscosity no greater than 5000 cps, heating a composition including an effervescent agent to a temperature of at least 45.degree. C., and combining the component and the heated effervescent agent to form an effervescent composition.

In another aspect, the invention features an effervescent composition that includes a viscous component exhibiting a viscosity greater than 50,000 cps at 23.degree. C. and 1 sec.sup.-1 and no greater than 5000 cps at a temperature of at least 38.degree. C. and 1 sec.sup.-1, effervescent agent, and silica, the effervescent composition being a uniform, free-flowing granulation. In some embodiments, the effervescent composition includes from 3% by weight to 20% by weight silica.

In another embodiment, the effervescent composition includes a viscous component exhibiting a viscosity greater than 50,000 cps at 1 sec.sup.-1 and 23.degree. C. and a viscosity less than 5000 cps at 10 sec.sup.-1 and a temperature of at least 55.degree. C., and effervescent agent. In one embodiment, the viscous component is solid at 23.degree. C. In another embodiment, the effervescent composition is a uniform, free-flowing granulation. In some embodiments, the effervescent composition includes from 5% by weight to 30% by weight the viscous component, from about 5% by weight to about 25% by weight of the viscous component, or even from about 10% by weight to about 20% by weight of the viscous component. In some embodiments, the effervescent composition includes a flow agent selected from the group consisting of silica, fumed silica, precipitated silica, magnesium oxide, calcium phosphate, magnesium carbonate, calcium silicate, sodium alumino silicate, and combinations thereof.

In some embodiments, an effervescent composition described herein is in the form of a tablet. In one embodiment, the composition of the tablet further includes binder, lubricant, or a combination thereof. In another embodiment, the effervescent composition described herein is in the form of a free flowing powder. In another embodiments, an effervescent composition described herein includes an effervescent agent that includes citric acid and sodium bicarbonate, and further includes silica, lactose, magnesium stearate, and sorbitol.

In another aspect, the invention features a method of using an effervescent composition described herein, the method including adding the effervescent composition to an aqueous liquid.

The invention features a method of incorporating a viscous component in an effervescent composition. The effervescent composition provides a viscous component in a predetermined amount and in a convenient form that is easy to handle.

The invention also features an effervescent composition that is capable of being tableted in an automated process and forming a tablet that exhibits good structural integrity.

The effervescent composition can be formulated to readily disperse in aqueous-based compositions. The effervescent composition can be formulated to disperse the viscous component in water at a rate that is faster relative to the rate of dispersion of the viscous component alone.

DETAILED DESCRIPTION

The effervescent composition includes a viscous component, and an effervescent agent. The viscous component is a solid, semisolid or has a viscosity of at least 50,000 centipoise (cps), at least 100,000 cps, or even at least 300,000 cps, at room temperature (i.e., from 68.degree. F. to 77.degree. F. (20.degree. C. to 25.degree. C.), and is a pourable liquid when heated to an elevated temperature. Preferably the viscous component exhibits a viscosity no greater than 5000 cps, or even no greater than 3000 cps at a temperature of at least 40.degree. C., at least 55.degree. C., or even at least 60.degree. C., when measured at 10 second.sup.-1 (reciprocal second), or even 1 sec.sup.-1.

Suitable viscous components include Newtonian and non-Newtonian compounds including, e.g., honey, molasses, wax, hop extract, kava, and mixtures thereof. A suitable hop extract is available under the trade designation YC Enhanced Oil hop extract from Yakima Chief, Inc. (Sunnyside, Wash.), one lot of which was found to have a viscosity of 54,000 cps at 23.degree. C. and 1 sec.sup.-1 and 8,400 cps at 23.degree. C. and 10 sec.sup.-1 and 2,900 at 40.degree. C. and 1 sec.sup.1 and 700 cps at 40.degree. C. and 10 sec.sup.-1. The viscous component is present in the effervescent composition in an amount suitable for its intended purpose. Useful formulations include a viscous component in an amount of at least 1% by weight, from about 5% by weight to about 30% by weight, from about 5% by weight to about 25% by weight, or even from about 10% by weight to about 20% by weight.

The effervescent agent preferably is at least one component of an effervescent couple that includes an acid and a base. The effervescent couple is activated when contacted with water, e.g., when the tablet is placed in a glass of water. The water liberates the acid and base and enables the acid and base to react with each other to produce carbon dioxide gas, which imparts carbonation to the aqueous composition. At least one component of the effervescent couple can also be an active agent. Examples of useful acids include citric acid, ascorbic acid, malic acid, adipic acid, tartaric acid, fumaric, succinic acid, sodium acid pyrophosphate, lactic acid, hexamic acid, and acid salts and acid anhydrides thereof, and mixtures thereof. Examples of useful acid anhydrides include citraconic anhydride, glucono-D-lactone, and succinic anhydride. Examples of useful acid salts include potassium bitartrate, acid citrate salts, sodium dihydrogen phosphate, disodium dihydrogen phosphate, sodium acid sulfite, and combinations thereof. Acid is present in the composition in an amount of from 5% by weight to about 60% by weight, from about 5% by weight to about 30% by weight, or even from about 10% by weight to about 20% by weight.

The base preferably is capable of generating carbon dioxide. Examples of suitable carbonate bases include sodium bicarbonate, sodium carbonate, sodium sesquicarbonate, potassium carbonate, potassium bicarbonate, calcium carbonate, magnesium carbonate, magnesium oxide, sodium glycine carbonate, L-lysine carbonate, arginine carbonate, zinc carbonate, zinc oxide and mixtures thereof. The base is present in the composition in an amount of from 10% by weight to about 60% by weight, from about 20% by weight to about 50% by weight, or even from about 30% by weight to about 45% by weight.

The effervescent composition preferably includes a flow agent. The flow agent preferably enhances the ability of the effervescent composition to flow through the components of a manufacturing operation including, e.g., the components of an automated tableting operation (e.g., a hopper and a tablet press). Suitable flow agents include, e.g., silica (e.g., fumed silica and precipitated silica), magnesium oxide, calcium phosphates (e.g., mono-, di- and tri-calcium phosphates), magnesium carbonate, calcium silicate, sodium alumino silicates, and combinations thereof. A useful fumed silica is commercially available under the trade designation CAB-O-SIL from Cabot Corp. (Boston, Mass.). The flow agent is preferably present in the composition in an amount of at least 0.5% by weight, from about 3% by weight to about 20% by weight, or even from about 5% by weight to about 15% by weight.

The effervescent composition can be in a variety of forms including, e.g., powder (e.g., a free flowing granulation), tablet, capsule, and pellet. The effervescent composition can be prepared to exhibit a desired dissolution rate. Useful effervescent tablets include effervescent tablets having a hardness of at least 3 kilopounds (Kp), at least 4 Kp, from about 5 Kp to about 15 Kp, or even from about 5 Kp to about 10 Kp, as measured on a standard hardness tester fitted with a strain gauge. In one embodiment, the tablets are formulated to weigh about 5000 mg and preferably dissolve in excess boiling water in less than 300 seconds, less than 100 second, or even less than 60 seconds.

When in the form of a tablet or capsule, the composition preferably includes binder, lubricant, and combinations thereof. Examples of suitable binders include, e.g., starches, natural gums, cellulose gums, microcrystalline cellulose, methylcellulose, cellulose ethers, sodium carboxymethylcellulose, ethylcellulose, gelatin, dextrose, lactose, sucrose, sorbitol, mannitol, polyethylene glycol, polyvinylpyrrolidone, pectins, alginates, polyacrylamides, polyvinyloxoazolidone, polyvinylalcohols and mixtures thereof.

The effervescent composition includes a sufficient amount of binder to assist in holding the components of the composition together in the form of a tablet. Preferably binder is present in the composition in an amount of from 10% by weight to about 60% by weight, from about 15% by weight to about 50% by weight, or even from about 25% by weight to about 40% by weight.

Various lubricants are suitable including water dispersible, water soluble, water insoluble lubricants and combinations thereof. Preferred lubricants are water soluble. Examples of useful water soluble lubricants include sodium benzoate, polyethylene glycol, L-leucine, adipic acid, and combinations thereof. The composition can also include water insoluble lubricants including, e.g., stearates (e.g., magnesium stearate, calcium stearate and zinc stearate), oils (e.g., mineral oil, hydrogenated and partially hydrogenated vegetable oils, and cotton seed oil) and combinations thereof. Other water insoluble lubricants include, e.g., animal fats, polyoxyethylene monostearate, talc, and combinations thereof.

The effervescent composition preferably includes a sufficient amount of lubricant to enable the composition to be formed into tablets and released from a high speed automated tableting press in the form of a tablet. The effervescent composition preferably includes water soluble lubricant in an amount of from 0.1% by weight to about 15% by weight, from about 0.1% by weight to about 10% by weight, from about 0.5% by weight to about 5% by weight, or even from about 0.5% by weight to about 3% by weight.

The effervescent composition can also include water insoluble lubricants. Preferably effervescent composition includes less than 3% by weight water insoluble lubricants.

The effervescent composition can also include other ingredients including, e.g., flavor agents, fillers, surfactants (e.g., polysorbate 80 and sodium lauryl sulfate), color agents including, e.g., dyes and pigments, sweetening agents, and combinations thereof.

In preparing the effervescent composition at least some of the components are preferably heated to a temperature of at least 40.degree. C., from 40.degree. C. to 70.degree. C., or even from 45.degree. C. to 65.degree. C., prior to being combined with one or more of the other components of the effervescent composition. In some embodiments, the viscous component is stirred (e.g., subjected to a shear stress) prior to combination with another component of the effervescent composition.

The effervescent composition is preferably stored in a moisture-proof package e.g., sealed foil containers (e.g., bags and pouches), sealed plastic bags, blister packs, desiccant capped tubes, and combinations thereof. A number of tablets or capsules can be placed in a single package.

The effervescent composition can be formulated for use in a variety of applications including, e.g., dispersing in an aqueous-based composition (e.g., water) at a variety of temperatures (e.g., refrigerated, room temperature, and boiling (e.g., boiling water)).
 

Claim 1 of 26 Claims

1. A method of making an effervescent composition, said method comprising heating a viscous component to a temperature of at least 45.degree. C., the viscous component exhibiting a viscosity greater than 50,000 cps at 23.degree. C. and a shear rate of 1 sec.sup.-1 and a viscosity less than 5000 cps at a temperature of at least 38.degree. C. and a shear rate of 1 sec.sup.-1; heating a composition comprising an effervescent agent to a temperature of at least 45.degree. C.; and combining said heated viscous component and said heated composition to form an effervescent composition.

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If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.

 

 

     
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