Classifications

• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
  • A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
  • A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
  • A23G3/346—Finished or semi-finished products in the form of powders, paste or liquids
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
  • A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
  • A23G3/02—Apparatus specially adapted for manufacture or treatment of sweetmeats or confectionery; Accessories therefor
  • A23G3/0236—Shaping of liquid, paste, powder; Manufacture of moulded articles, e.g. modelling, moulding, calendering
  • A23G3/0252—Apparatus in which the material is shaped at least partially in a mould, in the hollows of a surface, a drum, an endless band, or by a drop-by-drop casting or dispensing of the material on a surface, e.g. injection moulding, transfer moulding
  • A23G3/0289—Compression moulding of paste, e.g. in the form of a ball or rope or other preforms, or of a powder or granules
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
  • A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
  • A23G3/02—Apparatus specially adapted for manufacture or treatment of sweetmeats or confectionery; Accessories therefor
  • A23G3/0236—Shaping of liquid, paste, powder; Manufacture of moulded articles, e.g. modelling, moulding, calendering
  • A23G3/0294—Moulding or shaping of cellular or expanded articles
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
  • A23P10/00—Shaping or working of foodstuffs characterised by the products
  • A23P10/20—Agglomerating; Granulating; Tabletting
  • A23P10/28—Tabletting; Making food bars by compression of a dry powdered mixture
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/2004—Excipients; Inactive ingredients
  • A61K9/2013—Organic compounds, e.g. phospholipids, fats
  • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• • B—PERFORMING OPERATIONS; TRANSPORTING
  • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
  • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
  • B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
  • B01J2/22—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by pressing in moulds or between rollers
• • C—CHEMISTRY; METALLURGY
  • C13—SUGAR INDUSTRY
  • C13B—PRODUCTION OF SUCROSE; APPARATUS SPECIALLY ADAPTED THEREFOR
  • C13B50/00—Sugar products, e.g. powdered, lump or liquid sugar; Working-up of sugar
  • C13B50/02—Sugar products, e.g. powdered, lump or liquid sugar; Working-up of sugar formed by moulding sugar
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
  • A23G2200/00—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
  • A23G2200/00—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
  • A23G2200/06—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents containing beet sugar or cane sugar if specifically mentioned or containing other carbohydrates, e.g. starches, gums, alcohol sugar, polysaccharides, dextrin or containing high or low amount of carbohydrate

Definitions

• the mix ture may also contain additives such as colors, flavorants and the like.
• This invention relates to tablets comprising an active material and a direct compression vehicle. More particularly, this invention is concerned with tablets comprising an active material and a direct compression vehicle, which are formed from a mixture thereof without prior granulation or slugging.
• the compression technique may be further subdivided into three major categories, viz direct compression, wet granulation and dry granulation.
• the direct compression technique is the most desirable, in that it employs the fewest steps and, in the case of the production of tablets containing sensitive or unstable actives, such as certain pharmaceuticals, minimizes the exposure to water or other conditions tending to adversely affect stability of the active. Unfortunately, however, it has been found that the direct compression technique is of limited applicability.
• the active must be admixed with a direct compression vehicle, i.e., an inert composition which is compatible with the active and has good compressibility and binding action.
• a direct compression vehicle i.e., an inert composition which is compatible with the active and has good compressibility and binding action.
• the direct compression vehicle should have good flowability, good stability under normal ambient conditions, no adverse effect on tablet disintegration time, the ability to produce good tablet surfaces, and low cost.
• One of the principal objects of this invention is to provide a direct compression vehicle.
• Another object of the invention is to provide an improved tablet as the final product as a result of the more effective quality control made possible by eliminating variables in the manufacturing process.
• Another object of the invention is to permit the use of a wide variety of materials in the manufacture of tablets.
• sugar agglomerates are well suited for use as a direct compression vehicle for the production of tablets.
• This material comprises generally spherical, firm, porous agglomerates of sugar particles in a cementum or matrix.
• the agglomerates are dry (from about 0.1 to about 3 percent moisture), free-flowing particles having particle size within the range of from about 325 to about 12 mesh. Tablets formed using such sugar agglomerates as the direct compression vehicle are uniform, possess good physical properties, do not discolor on aging, and readily dissolve in aqueous media.
• the particulate sugar can be a mono-, dior tri-saccharide, such as arabinose, xylose, ribose, fructose, mannose, galactose, glucose, sucrose, maltose, lactose and the like, including mixtures of two or more of such sugars, with sucrose being preferred.
• the particulate sugar can be obtained synthetically, or it can be a refined natural product, such as corn syrup solids, molasses solids, honey solids, maple syrup solids and the like.
• the particle size of the sugar is not narrowly critical so long as it is small enough to permit formation of agglomerates of the desired size.
• the sugar should have substantially no particles, i.e., not more than 1 percent, having sizes greater than about 40 microns, and at least 50 percent of the particles should have sizes below about 25 microns. Preferred are sugars having an average particle size of about 15 microns.
• the second component which is employed to form the agglomerate is a noncrystallizing aqueous solution of a polyhydroxy compound as a binder.
• a polyhydroxy compound as a binder.
• Illustrative polyhydroxy compounds include propylene glycol, glycerol, erythritol, arabitol, xylitol, adonitol, mannitol, dulcitol, sorbitol, sugars, such as arabinose, xylose, ribose, glucose, mannose, fructose, sucrose, maltose and lactose, dextrin and the like, with polyols of the formula HOCH (CHOH),CH OH, wherein x is l to 4, and sugars being preferred.
• the aqueous binder composition can be a solution of a pure compound, or can comprise two or most polyhydroxy binders.
• the aqueous medium can be obtained synthetically, or it can be a refined natural product, such as corn syrup, molasses, honey, maple syrup and the like. lnvert syrup is preferred.
• the concentration of binder in the aqueous medium is not narrowly critical provided that it is not so high as to cause crystallization or provide solutions so viscous as to prevent spraying and intimate intermingling and uniform distribution of binder and solids.
• concentration will depend upon the solubility of the binder. For example, glucose ordinarily cannot be employed in amounts greater than about 48 percent, whereas propylene glycol, glycerol, mannitol and sorbitol can be present in amounts up to about 80 percent.
• concentrations of from about 50 to about 80 percent are employed, with concentrations of from about 70 to about 75 percent being preferred.
• the amount of water in the aqueous medium should be so correlated with the desired ratio of binder to sugar that agglomeration occurs.
• the amount of water should be insufficient to form a paste and yet sufficient to minimize the presence of powder, or unagglomerated sugar.
• the mixture of particulate sugar and aqueous binder medium should contain from about 2 to about 6 percent water, with amounts of about 4 percent water being preferred.
• the initial contact of the solids and liquids is effected by spraying the aqueous medium onto the dry solids at a rate such that there is employed from about 0.1 to about 30 parts of binding agent per 100 parts of solid.
• the mixing is ordinarily conducted at about room temperature (6575 F.). Higher and lower temperatures can be employed, if desired, provided the properties of the aqueous medium and the agglomerate product are not adversely affected.
• the temperature of the aqueous medium may be varied to achieve a desired viscosity for spraying. However, if the temperature is too low, e.g., below about 50 F., the aqueous medium is ordinarily too viscous to be easily sprayed; and if the temperature is too high, e.g., above about 200 F., water may evaporate too rapidly to permit adequate control of the characteristics of the binding solution.
• the use of elevated temperatures during processing tends to result in a discolored product, and also may cause dissolution of the dry ingredient and thus adversely affect particle size and quality.
• the mixture is agitated to thoroughly intermingle the solid sugar and the aqueous binder medium and to effect agglomeration.
• This requires high intensity mixing, such as is obtained with a Patterson-Kelley blender or a Lodige mixer.
• Agitation is continued until agglomerates of the desired size are formed, and ordinarily for a time sufficient to form agglomerates about about 325 mesh, but insufficient to form significant amounts of agglomerates larger than about l2 mesh.
• the size of the agglomerate is also affected by the ratio of aqueous binder to particulate sugar, with larger agglomerates being formed when a greater proportion of liquid medium is present.
• the agglomerates typically have a narrow size distribution. That is, high yields, normally 80 percent or more, of the agglomerates fall within a few screen sizes. For example, when operating to produce a 20- to 80-mesh agglomerate, at least 80 percent, and in some instances 90 percent or more, of the agglomerated product will fall within this range.
• the agglomerates are snowballed, i.e., subjected to a tumbling or rolling operation, to impart a general spherical shape thereto.
• the agglomerates are firmed or densified whereby the bulk density is increased by about 50-100 percent over that of the dry particulate sugar, and normally is in the range of from about 30 to about 50 pounds per cubic foot.
• the apparatus employed can be any suitable equipment which will achieve the desired results.
• a particularly preferred apparatus is the Patterson-Kelley blender, which performs all three operations of mixing, agglomerating and snowballing.
• the agglomerates are dried to a moisture content of less than about 3 percent, and preferably less than about 1.5 percent.
• the moisture content of the product need not be less than about 0.! to 0.2 percent.
• the temperature at which drying occurs is not narrowly critical in all cases, but ordinarily the temperature of the agglomerate should not exceed about 140 F.
• the product is preferably contacted with hot air at a temperature not exceeding 190 F.
• a preferred drying technique is the use of a fluid bed dryer. In this manner, very fine particles, i.e., dust, are separated from the product.
• the dried product may be screened. to remove oversized and undersized particles. Oversized particles are discarded or can be reduced to smaller size. Undersized particles can be recycled.
• the resulting agglomerate is admixed with the active material and the resulting mixture compressed without granulation or slugging to form a tablet.
• the amount of the agglomerate obviously will depend upon the properties of the active and any other additives which are to be incorporatedinto the finished tablet, for it is well known that the compactibility of tablet compounds and mixtures are subject to wide variation. in general, however, the agglomerate will comprise at least percent of the tabletting mixture and, therefore, at least 10 percent of the tablet. in most cases, however, the agglomerate will comprise from about 70 to about 95 percent of the tabletting mixture and the tablet.
• active material any material intended for ingestion and having a beneficial or desirable effect on the user.
• suitable active materials include therapeutic materials, such as anesthetics, antibiotics, antitussives, vitamins, aspirin, antacids, and the like; food stufis such as cocoa, dried oats, fruit flakes, and the like; edible dyes and other food additives; and so on.
• the vehicle is a free-flowing granular material and imparts improved flow characteristics to the active material and other components of the blend, thereby assuring ease of tabletting.
• the blend of direct compression vehicle, active material and other additives is mixed and directly compressed to form a tablet employing conventional techniques and apparatus.
• EXAMPLE I To parts of finely pulverized sucrose is rapidly added over a period of 5 minutes by spraying at room temperature and while agitating the pulverized sugar l4 parts of an aqueous invert sugar solution (72 percent total solids) in a PattersonKelley liquids-solids blender. After continuing agitation for an additional 10 minutes, the agglomerated material is screened through a vibrating l6-mesh screen and the screened material is dried to a moisture content of 1.5 percent or less. To 97 parts of dry agglomerated product is added, under agitation, 1 part of dry citric acid, 0.25 part of dry flavoring material and 1.75 part of magnesium stearate. The properly blended material is fed to a tabletting press and wafers are formed from it.
• EXAMPLE 2 Employing procedures similar to those described in example 1, 98 parts of finely pulverized sucrose is mixed with about 6.7 parts of an aqueous invert sugar solution (30 percent total solids). The agglomerated material is screened through a vibrating mesh screen and the screened material is dried to a moisture content of 1.5 percent or less.
• Equal parts of the agglomerate and vitamin C are blended. This blend can be further mixed with other dry ingredients such as minerals or other nutritionally active ingredients before being compressed into tablets.
• EXAMPLE 3 Employing procedures similar to those described in example l, a blend of lOO parts of finely pulverized dextrose monohydrate is sprayed with 14 parts of dextrose syrup (48 percent total solids). The agglomerated material is screened and dried to a moisture content of 1.5 percent or less.
• the agglomerated material can be directly compacted after adding and blending the proper release agent (magnesium stearate). Rapidly disintegrating ingredients can also be included in the formulation prior to tabletting.
• EXAMPLE 4 Employing procedures similar to those described in example l, a blend of 90 parts of finely pulverized sucrose and 10 parts of finely comminuted dextrose are sprayed with about 14 parts of invert syrup (72 percent total solids). The agglomerated materials is screened, and dried to a moisture content of 1.5 percent or less.
• Equal parts of the agglomcrate and aluminum hydroxide are blended together. This blend can be further mixed with small amounts of flavoring or other dry ingredients before being compressed into a commercial antacid tablet.
• EXAMPLE 5 Employing procedures similar to those described in example l, parts of finely pulverized dried molasses are sprayed with about 6.5 parts of afi'mation syrup (76 percent total solids). The agglomerated material is screened and dried to a moisture content of 1.5 percent or less.
• Equal parts of the agglomerate and dried ground oats are blended. This product can be further mixed with other dry ingredients such as minerals or other nutritives. After compacting, wafers for animal feeding are obtained.
• EXAMPLE 6 To 90 parts of pulverized sucrose having an average particle size of microns, less than 1 percent thereof exceeding 40 microns, and more than 50 percent thereof less than 25 microns in size, the said pulverized sugar being in a Patterson- Kelley liquids-solids blender, there is rapidly added by spraying at room temperature (65 F.), and while agitating the pulverized sucrose, about 14 parts of an aqueous invert sugar solution (72 Brix). A small amount of monocalcium phosphate is added to adjust the pH to 4.5-4.8 to prevent discoloration. After the addition of the invert syrup has been completed, the blender is run for about 2 minutes to complete the agglomeration. The total time of operation, i.e., spraying and agglomeration, is about 6 minutes.
• the resultant agglomerated material which contains about 3.8 percent water, is then screened through a vibrating mesh screen.
• the agglomerates coarser than 20 mesh are still relatively soft and can be rubbed through an auxiliary screen and added to the first product.
• the screened material is then placed in a rotary drier and warm air at about 180 F. is circulated through the drier to dry the agglomerates to a water content of 1 percent.
• the drier is operated so that the temperature of the agglomerates does not rise about 140 F.
• the dried product is then further screened on an 80-mesh screen.
• This agglomerate can be blended in accordance with the following recipes and compressed.
• agglomerate acetyl salicylic acid corn starch magnesium stearate Other active ingredients of use in blends with the agglomerate are: sodium bicarbonate, acetanilid, phenacetin, and magnesium trisilicate.
• the direct compression vehicle has been a spherical agglomerate. In some instances, in which a high degree of composition uniformity is desired, the use of the agglomerate per se has been found disadvantageous.
• the ratio of invert to particulate sugar increases with increasing agglomerate size.
• the invert content of the ZOO-mesh size particles is substantially less than the invert content of the 80-mesh particles.
• the agglomerates tend to segregate according to size upon handling. For example, when a 80-200 mesh fraction of the agglomerates is stored in a bag, the ZOO-mesh particles tend to settle out in the bottom of the bag during handling. As a result of the different composition and size segregation, the composition of tablets made from the agglomerates will vary depending upon whether the agglomerate is taken from the top or the bottom of the bag.
• the pulverize the agglomerate and then compact the pulverized agglomerate as for example by the use of a Fitzpatrick Chilsonator, and reduce the resulting compacted sheet to particles of a desired size.
• the granules of compacted agglomerate may be screened to provide a product of more restricted size variation.
• the resulting compacted agglomerate may be employed in a manner identical to the agglomerate itself. Thus, it may be substituted for the agglomerate in any of the foregoing examples to achieve a tablet of substantially identical characteristics.
• a method for preparing tablets containing as a direct compression vehicle a sugar composition comprising the steps of (a) forming a unifonn nongranulated mixture of an active material and a dry, free-flowing, generally spherical, porous agglomerate of parts of a solid pulverized sugar in 0.1 to about 30 parts of a matrix of a polyhydroxy compound, and (b) compressing said mixture into tablets, said agglomerate comprising at least 10 percent of said mixture, and having a particle size of from about 12 to about 325 mesh, a moisture content of from about 0.1 to about 3 percent, and having been prepared by a process including the steps of: (l) Spraying a particulate solid sugar with an aqueous solution of binder; (2) Providing the resulting mixture with sufficient high intensity agitation to uniformly intermingle the sugar and binder and to build up agglomerates of a desired size; and (3) Snowballing the agglomerates to impart a general spherical shape thereto and
• a method for preparing a direct compression vehicle comprising compacting a dry, free-flowing, generally spherical, porous agglomerate of I parts of a solid pulverized sugar in 0.] to 30 parts of a matrix of a polyhydroxy compound, said agglomerate having a particle size of from about 12 to about 325 mesh and a moisture content of from about 0.1 to about 3 percent, said agglomerate being prepared by a process including the steps of:
• a method for preparing a tablet comprising forming a uniform admixture of the product of claim 8 and active material, said product comprising at least 10 percent of said mixture, and compressing the mixture into tablets.

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• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Engineering & Computer Science (AREA)
• Food Science & Technology (AREA)
• Polymers & Plastics (AREA)
• Health & Medical Sciences (AREA)
• Organic Chemistry (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Molecular Biology (AREA)
• Veterinary Medicine (AREA)
• Biophysics (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Biochemistry (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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Cited By (53)

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Citations (2)

• 1969
  • 1969-04-29 US US820285A patent/US3627583A/en not_active Expired - Lifetime
• 1970
  • 1970-04-24 NL NL707006008A patent/NL148938B/xx unknown
  • 1970-04-27 CA CA081243A patent/CA937167A/en not_active Expired
  • 1970-04-28 FR FR7015515A patent/FR2042385B1/fr not_active Expired
  • 1970-04-28 JP JP45036221A patent/JPS5013332B1/ja active Pending
  • 1970-04-28 GB GB2039370A patent/GB1310925A/en not_active Expired
  • 1970-04-29 DE DE2020982A patent/DE2020982C3/de not_active Expired
  • 1970-04-29 IT IT24039/70A patent/IT968013B/it active

Patent Citations (2)

Non-Patent Citations (1)

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