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WO2002091852A1 - Systeme d'administration par voie orale et son procede de fabrication - Google Patents

Systeme d'administration par voie orale et son procede de fabrication Download PDF

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Publication number
WO2002091852A1
WO2002091852A1 PCT/US2001/040723 US0140723W WO02091852A1 WO 2002091852 A1 WO2002091852 A1 WO 2002091852A1 US 0140723 W US0140723 W US 0140723W WO 02091852 A1 WO02091852 A1 WO 02091852A1
Authority
WO
WIPO (PCT)
Prior art keywords
oral dosage
capsule
dosage form
filler
substance
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2001/040723
Other languages
English (en)
Inventor
John T. Cooker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Priority to PCT/US2001/040723 priority Critical patent/WO2002091852A1/fr
Publication of WO2002091852A1 publication Critical patent/WO2002091852A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23K—FODDER
    • A23K20/00—Accessory food factors for animal feeding-stuffs
    • A23K20/20—Inorganic substances, e.g. oligoelements
    • A23K20/30—Oligoelements
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23K—FODDER
    • A23K40/00—Shaping or working-up of animal feeding-stuffs
    • A23K40/30—Shaping or working-up of animal feeding-stuffs by encapsulating; by coating
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds

Definitions

  • the present invention generally relates to an oral delivery system.
  • oral dosages that can be taken orally and which are in the
  • dosage forms become buoyant on the liquid with which they are taken. This is
  • the buoyancy of the oral dosage forms on the liquid causes discomfort and
  • the buoyancy property creates the buoyancy property
  • Oral dosage forms that have a cylindrical, oval or rectangular shape (but not
  • cylindrical-shaped tablets which were to replace round shaped tablets, (i.e. a
  • the present invention is directed to improved oral dosage forms that are
  • dosage forms are configured to have relatively greater weight and/or density to
  • the present invention is directed to an oral dosage form for
  • liquid comprising, an active ingredient, an inactive ingredient, and
  • the substance is a filler that is added to the active and
  • a filler is added to the medium of the oral dosage form.
  • a filler is added to the exterior of the oral dosage
  • the substance is a binder that is used to increase
  • the weight and/or density of the oral dosage form are the weight and/or density of the oral dosage form.
  • oral dosages are configured to have a
  • Oral dosage forms have a variety of physical characteristics, such as the
  • the present invention teaches a variety of
  • oral dosage forms (1) capsules, (2) tablets and caplets, and
  • FIG. 1 is a perspective view of one embodiment of a capsule configured in
  • FIG. 2 is a perspective view of a capsule having thereon indicia to indicate the
  • FIG. 3 is a perspective view of a further embodiment of a capsule configured in
  • FIG. 4 is a perspective view of yet a further embodiment of a capsule
  • FIG. 5 is a perspective view of yet another embodiment of a capsule configured
  • FIG. 6 is a perspective view of yet a further embodiment of a capsule
  • FIG. 7 is top plan view, partially in cross-section, of one embodiment of a
  • FIG. 8 is a top plan view, partially in cross-section, of one embodiment of a
  • FIG. 9 is a perspective view of a conical-shaped tablet configured in
  • FIG. 10 is a top plan view of a generally trapezoidal-shaped tablet having filler
  • oral dosage form configured to have a relatively greater weight than that of a
  • oral dosage form configured to have a relatively greater density than that of a
  • the oral dosage form having the
  • an oral dosage form maintains the oral dosage form in a
  • the heavier end is positioned such that it points generally in the
  • oral dosage form being swallowed at an uncomfortable angle is significantly
  • a particular end or side of an oral dosage form is such as to cause the oral dosage form to sink entirely in the liquid which is taken with the oral dosage form while
  • an oral dosage form is such as to cause the oral dosage
  • oral dosage form as discussed above.
  • a filler is
  • the filler may be in solid, semi-
  • the filler may be inactive or may
  • the filler can be formulated out of
  • any commercially available soluble or insoluble filler including sucrose, dextrose,
  • lactose fructose
  • microcrystaline cellulose calcium carbonate
  • sorbitol xylitol
  • fillers can be used as well.
  • the filler can be added at any time
  • a solid sucrose portion is molded or
  • the filler is
  • the filler is at one end of the oral
  • the filler is concentrated at the opposite end
  • having the filler is relatively heavier than the other end thereby causing the weighted end to sink first in the liquid taken with the oral dosage form.
  • the oral dosage form having a weighted end includes
  • indicia to indicate which end of the oral dosage form is weighted.
  • the indicia enables consumers to align the heavier end first in their
  • the indicia on the weighted end decreases the chance of the oral
  • the indicia on the weighted end of the oral dosage form is a
  • the oral dosage form may be configured such that the
  • filler is part of the medium, e.g. capsule, or formed to the medium.
  • a coating comprising the filler is disposed on the exterior surface of
  • the filler coating is between about 20 and 200 mils, inclusive.
  • the filler coating may be adhered to the medium of the
  • oral dosage form in many ways, e.g. coating, dipping, etc.
  • a relatively heavier or denser diluent is used as an
  • rice flour in solid granule form is used.
  • Rice flour in solid granule form is used.
  • a binder is used to effect a relatively denser oral
  • binder is mixed with a portion of a capsule's ingredients in order to effect a
  • a starch In one embodiment, a starch
  • binder is mixed with a portion of ingredients to form solids or semi-solids which,
  • the characteristics of a capsule e.g. the capsules shiny, smooth surface.
  • a binder In another embodiment, a binder
  • the present invention may be used in any combination to increase the weight
  • oral dosage form is taken as being water. However, it is to be understood that
  • liquids e.g. soda, juice, coffee, etc. and that the weight and/or
  • density of the oral dosage form may have to be increased in accordance with the
  • present invention to eliminate buoyancy of the oral dosage form on those types of
  • dosage forms (1) capsules, (2) tablets and caplets, and (3) soft-gels.
  • the sealed powder and air have buoyant
  • a capsule is provided
  • capsules are configured to have a relatively greater weight
  • zinc contains excipients that weigh 462 mg. Its total weight is 512 mg in a size 0
  • the density D of the capsule is
  • the end product i.e. the modified capsule
  • the density-augmented capsule will significantly reduce the
  • augmentation is such that it does not increase the size of the capsule beyond what
  • capsules having a size greater than the size preferred by consumers.
  • Example 1 250 mg or 32% of the total weight of the end product is
  • the present invention also will vary.
  • weight of the end product that is due to the addition of the filler ranges between
  • the 200 mg of a rice flour power diluent is
  • sucrose solid granules were replaced by 400 mg of sucrose solid granules.
  • the sucrose solid granules require
  • the weight of the capsule is increased to 712 mg at the same volume with a density
  • a binder is used to produce a capsule having a
  • capsule as described above in Example 1 contains about 112 mg of powder zinc
  • the density D of the end product would be 0.512 g/0.5 ml or 1.024
  • the density of the capsule be increased to at a density that
  • Capsules typically are comprised of two portions or components that are
  • the capsule portions are
  • invention includes a particular step that pertains to the application of such force.
  • the method of the present invention includes the step of applying a
  • the capsule in another embodiment of the method of the present invention, the capsule
  • portion holding the ingredients is configured to have a deeper well to
  • Portion 14 holds the ingredients during
  • portion 14 is configured to have a
  • the length of portion 12 is increased to
  • portion 14 is increased to accommodate filler material or binders.
  • the diameter of portions 12 and 14 are increased to
  • the filler may be configured to have any suitable shape. However, it has been
  • the filler should be generally spherical or oval in order to facilitate compacting
  • the filler is covered
  • the capsule in a further embodiment of the method of the present invention, the capsule
  • components e.g. portions 12 and 14 are formulated to have a relatively greater
  • sealing process includes the step of applying an adhering agent around the seam of
  • a locking process is used to hold the joined capsule
  • capsule cap and body The indentations or moldings are used to lock the cap and
  • a plurality of indentations or moldings can be used to provide
  • weight of the capsule is increased to improve swallowability, as described above,
  • the weight is concentrated at one end of the capsule.
  • indicia is applied to the weighted portion of the capsule.
  • Capsule 20 comprises portions 22 and 24.
  • Portion 22 has indicia 26 to indicate that portion 22 is the weighted portion and
  • the indicia is pointing toward the opening of the esophagus. In one embodiment, the indicia
  • sucrose solid granules are added to the capsule to the capsule to the particular substance, e.g. sucrose solid granules, are added to the capsule to the particular substance, e.g. sucrose solid granules, are added to the capsule to the particular substance, e.g. sucrose solid granules, are added to the capsule to the particular substance, e.g. sucrose solid granules, are added to the capsule to
  • invention includes the steps of (a) providing capsule 30 that comprises capsule
  • ingredients 35 to portion 34 (d) depositing granules 36 into portion 34, and (e)
  • the method may also include the
  • the method of the present invention also provides particular
  • invention includes the steps of (a) providing capsule 40 that comprises capsule
  • ingredients 45 to portion 44 (d) depositing single filler substance 46 into portion
  • the method may also include the
  • the method of the present invention also provides particular
  • the method of the present invention includes the steps of (a)
  • capsule 60 that comprises capsule portions 62 and 64, (b) retaining
  • portion 64 so that it is stationary, (c) depositing ingredients 66 into portion 64, (d) adhering or attaching filler substance 68 to the exterior surface of portion 62, and
  • the method of the present invention also provides particular
  • the method of the present invention includes the steps of (a)
  • capsule 80 that comprises capsule portions 82 and 84, (b) retaining
  • portion 84 so that it is stationary, (c) depositing ingredients 86 into portion 84, (d)
  • the method of the present invention also provides particular steps for adding a
  • the solid filler described above can be standardized in order to facilitate
  • the solid filler can be adhered to the inside
  • the optimum size filler possible is adhered to the
  • tablets and caplets are produced with
  • the increase in weight and density is accomplished by adding a
  • the filler is added to the
  • a solid sucrose filler is molded in
  • the filler is embedded within the tablet
  • the filler is attached to the exterior of the tablet or
  • Tablet 90 comprises portions 92 and
  • Portion 92 is comprised only of filler. Portion 94 is embedded within the
  • the tablet is configured such that one side, end or
  • portion of the tablet has concentrated weight and has indicia to indicate which
  • caplet is accomplished by increasing a component of the tablet or caplet.
  • weight of the component is between about 25% and 15%, inclusive.
  • the original weight of the tablet has been
  • the increase in weight and/or density provides significantly improved
  • FIGS. 9 and 10 there are shown alternate embodiments of the
  • FIG. 9 shows a conical-shaped tablet or caplet 200
  • Figure 10 shows a generally-
  • trapezoidal shaped tablet or caplet 208 which has a swelled or enlarged end 210
  • filler 214 is dispersed throughout the
  • the weight of softgels is increased to
  • the filler is added to the ingredients, e.g. a solid sucrose portion.
  • Softgel 100 comprises portions 102 and 104. Portion
  • Portion 104 includes filler 106. In one
  • filler 106 is comprised of solid sucrose.
  • softgels is accomplished by increasing the amount of a component.
  • the component is a liquid excipient
  • the amount of the excipient is
  • the softgels can be configured that one side or portion
  • the softgel has concentrated weight and has indicia to indicate this end.
  • the percentage of total weight of the softgel is preferably 90%, inclusive. More preferably, the percentage of total weight of the softgel
  • the increase in weight and/or density provides significantly improved
  • filler is placed in the body
  • the size of the body portion is
  • a 0.500 ml size #1 capsule is typically used to fill 400 mg of ingredients.
  • volume is used for the filler.
  • a filler having a density of 1.5 g/ml is used,
  • a size #00 capsule is
  • Table III shows typical commercially available capsule sizes and corresponding
  • Table IV shows specific filler weights, filler volumes and corresponding
  • the additional filler increases the density of the finished capsule to a density
  • Lactose or micro-crystalline cellulose fillers have a density of 1.5 in solid form.
  • Table VI shows new capsule sizes, and the amount of additional filler that can
  • capsule sizes 4 and 5 are increased to size 2.
  • Table VIII provides a conversion table that shows initial capsule sizes
  • Table VIII provides a standardization system which provides seven (7)
  • capsule sizes that accommodate the standard capsule sizes at four or more powder
  • One such advantage is that the end of the capsule having the filler
  • Another advantage is the improved swallowability of the capsule.
  • the cap portion of the capsule is joined with the body portion.
  • cap portion of the capsule is configured so as to
  • the capsule is joined with the body portion. In one embodiment, this is achieved
  • cap portion that is adjacent to the end of the cap portion is filled in with the same
  • weight and/or density of the oral dosage forms of the present invention effect augmentation of the gravitational force that facilitates the downward passage of
  • the oral dosage forms are the oral dosage forms.
  • the swallowability of the oral dosage forms is the swallowability of the oral dosage forms.
  • the present invention provides new and improved oral dosage forms that:
  • b) can be provided in the form of capsules, tablets, gelcaps and softgels;

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Zoology (AREA)
  • Food Science & Technology (AREA)
  • Animal Husbandry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention sur des formes galéniques orales améliorées du fait qu'elles peuvent s'avaler beaucoup plus facilement. Selon cette invention, les formes galéniques orales sont configurées de façon à avoir un poids et/ou une densité relativement supérieur pour les immerger partiellement ou totalement dans un liquide avec lequel elles seront absorbées. Selon une réalisation, une charge est ajoutée aux ingrédients de la forme galénique orale. Selon une autre réalisation, une charge est ajoutée à l'extérieur de la forme galénique, et dans une autre réalisation, une quantité d'ingrédients relativement plus grande, plus dense ou plus lourde est utilisée pour formuler la forme galénique. Et dans une autre réalisation, un liant est utilisé pour augmenter le poids et/ou la densité de la forme galénique. Et enfin dans une autre réalisation, une combinaison comprenant un liant et une quantité d'ingrédients relativement plus lourde, plus dense ou plus importante et utilisée pour formuler la forme galénique. Selon cette invention, des formes galéniques orales sont configurées de façon à avoir un poids et/ou une densité prédéterminé, la grosseur leur permettant d'être avalés facilement étant respectée.
PCT/US2001/040723 2001-05-14 2001-05-14 Systeme d'administration par voie orale et son procede de fabrication Ceased WO2002091852A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/US2001/040723 WO2002091852A1 (fr) 2001-05-14 2001-05-14 Systeme d'administration par voie orale et son procede de fabrication

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2001/040723 WO2002091852A1 (fr) 2001-05-14 2001-05-14 Systeme d'administration par voie orale et son procede de fabrication

Publications (1)

Publication Number Publication Date
WO2002091852A1 true WO2002091852A1 (fr) 2002-11-21

Family

ID=21742937

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/040723 Ceased WO2002091852A1 (fr) 2001-05-14 2001-05-14 Systeme d'administration par voie orale et son procede de fabrication

Country Status (1)

Country Link
WO (1) WO2002091852A1 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4262378A (en) * 1979-06-08 1981-04-21 Goodyear Aerospace Corporation Buoyant capsule depth controller
US5198222A (en) * 1990-08-31 1993-03-30 Agribiotech, Inc. Time release bolus
US6210713B1 (en) * 1995-07-21 2001-04-03 Alza Corporation Oral delivery of discrete units

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4262378A (en) * 1979-06-08 1981-04-21 Goodyear Aerospace Corporation Buoyant capsule depth controller
US5198222A (en) * 1990-08-31 1993-03-30 Agribiotech, Inc. Time release bolus
US6210713B1 (en) * 1995-07-21 2001-04-03 Alza Corporation Oral delivery of discrete units

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