US1879762A - Protection of autoxidizable materials - Google Patents

Protection of autoxidizable materials Download PDF

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Publication number
US1879762A
US1879762A US515421A US51542131A US1879762A US 1879762 A US1879762 A US 1879762A US 515421 A US515421 A US 515421A US 51542131 A US51542131 A US 51542131A US 1879762 A US1879762 A US 1879762A
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Prior art keywords
concentrate
autoxidizable
materials
antioxidant
protection
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Expired - Lifetime
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US515421A
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Ferdinand W Nitardy
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ER Squibb and Sons LLC
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ER Squibb and Sons LLC
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Priority to US515421A priority Critical patent/US1879762A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids

Definitions

  • This invention relates to autoxidizable materials, particularly those used for therapeutic or alimentary purposes, and has for its object the provision of means whereby 5 such materials may be protected against the deteriorative effects of the atmosphere.
  • My invention consists in interposing both mechanical and chemical barriers to the access of oxygen, by applying to the autoxidizable material an antioxidant and an impervious envelope.
  • antioxidants especially aromatic hydroxyl derivatives and aliphatic and aromatic amines.
  • impervious I mean highly obstructive to the passage of oxygen; that is to say, relatively airtight.
  • the antioxidant may be directly admixed with the autoxidizable material; or superposed thereupon, in a suitable coat, above or belowthe impervious envelope; or distributed through the impervious envelope itself.
  • vitaminous substances among them concentrates of the fat-soluble vitamins, particularly those obtained from cod-liver oil. These, notably as regards their vitamin- A content, are readily vitiated by exposure to oxygen; but my invention secures them against oxidative deterioration during the prolonged transportation and storage that, under the conditions of modern large-scale distribution, often intervene between manufacture and consumption.
  • I may form such concentrates into tablets, and, successively, superpose upon them a coat in which hydroquinone is uniformly incorporated and enrobe them with a coherent film of gelatin.
  • a coat in which hydroquinone is uniformly incorporated and enrobe them with a coherent film of gelatin.
  • the coat and film are applied anaerically and comprise multiple layers.
  • the finished tablet may, as a further precaution, be enclosed in a container from which the air has been displaced by an inert gas. Little, if any, air will penetrate the gelatin film; and whatever does infiltrate through it will come into contact with, and be rendered oxidatively innocuous by reaction with, the hydroquinone. Access of oxygen to the concentrate is thus substantially prevented.
  • any other antioxidant e. g. one of those first above specified, may be employed; and the gelatin may be replaced by gelatinous starch, shellac, acacia, tragacanth, or some other gum or resinous varnish.
  • the coats and films should be disintegrable in the gastric or intestinal fluids.
  • the sugar or chocolate covering commonly used will do.
  • the order and number of the coats and films, and of their re spective layers, are by no means invariable; and the antioxidant may be mingled with the concentrate or dissolved in the gelatin solution producing the film.
  • fat-solublevitamin-concentrate tablets embodying my invention may be made as follows, air being preferably excluded, by evacuation or by substitution of carbon dioxide, from the vessels used in the process, and the ingredients having preferably been deaerated: A granulation is formed, in the customary manner, of an excipient comprising milk sugar 4.9 parts, cocoa powder 30 parts, powdered sugar 20 parts, and monohydrated sodium carbonate 1 part, and after the excessively fine and coarse particles have been removed by sifting, is impregnated with an ethereal solution of a fat-soluble-vitamin concentrate obtained from cod-liver oil.
  • the granules are compressed into tablets and coated nine times with an antioxidant solution composed of simple sirupto which has been added 5% (calculated on the sucrose content) of hydroquinone. Then an impervious envelope is provided by applying, alternately with dusting powder to prevent the tablets from sticking together, six coats of a solution whose proportions are: gelatin 1 pound, sugar 25 pounds, water to make five gallons.
  • a starch mixture is next applied, and last a finishing sirup; the respective volumes of which used for 135,000 tablets are 3% and 2 gallons; and the respective formulas of which are: granulated sugar 16 parts, water 7 parts, corn starch 4 parts, part, and erythrosin .0035 part; and simple sirup to every 4 gallons of which 3% grams of erythrosin has been added.
  • the tablets are placed in bottles, which are then exhausted, flooded with carbon dioxide, and sealed.
  • the granulation referred to may include .5 part of hydroquinone, in which event the antioxidant-containing coat is not required; and the tablets after compression, or suitably composed and rolled pill masses, may then be completed by twice dipping, to cover them by successive halves, into the gelatin solution.
  • a tablet comprising a vitamin concentrate, an antioxidant distributed around the concentrate, and an impervious envelope over the antioxidant, the antioxidant being a substance that reacts so rapidly with any oxygen penetrating the envelope as substantially to prevent oxidative deterioration of the concentrate.
  • a tablet comprising a fat-soluble-vitamin concentrate, an antioxidant distributed around the concentrate, and a elatin film over the antioxidant, the antioxi ant being a substance that reacts so rapidly with any oxygen penetrating thefilm as substantially to prevent oxidative deterioration of the concentrate.
  • a tablet comprising a fat-soluble-vitamin concentrate, hydroquinone distributed on the surface of the concentrate, and a gelatin film over the hydroquinone.
  • a tablet comprising a fat-soluble-vitamin concentrate, over the concentrate a coat in which hydroquinone is distributed, and

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)

Description

Patented Sept. 27, 1932 UNITED STATES PATENT OFFICE FERDINAND 'WQNITARDY, OF BROOKLYN, NEW YORK, ASSIGNOR T E. R. SQUIBB & SONS, OF NEW YORK, N. Y., A CORPORATION OF NEW YORK PROTECTION OF AUTOXIDIZABLE MATERIALS No Drawing.
This invention relates to autoxidizable materials, particularly those used for therapeutic or alimentary purposes, and has for its object the provision of means whereby 5 such materials may be protected against the deteriorative effects of the atmosphere.
My invention consists in interposing both mechanical and chemical barriers to the access of oxygen, by applying to the autoxidizable material an antioxidant and an impervious envelope. A great variety of substances may serve as antioxidants, especially aromatic hydroxyl derivatives and aliphatic and aromatic amines. By impervious I mean highly obstructive to the passage of oxygen; that is to say, relatively airtight. It will be understood that the antioxidant may be directly admixed with the autoxidizable material; or superposed thereupon, in a suitable coat, above or belowthe impervious envelope; or distributed through the impervious envelope itself. By virtue of the cooperation between these mechanical and chemical barriers, the one excluding or neutralizing such oxygen as may, by any chance, have passed the other, autoxidiziable materials can be preserved for an indefinite period from oxidative deterioration. .l'
Conspicuous among the numerous materials to the protection of which my invention is adapted, are vitaminous substances, among them concentrates of the fat-soluble vitamins, particularly those obtained from cod-liver oil. These, notably as regards their vitamin- A content, are readily vitiated by exposure to oxygen; but my invention secures them against oxidative deterioration during the prolonged transportation and storage that, under the conditions of modern large-scale distribution, often intervene between manufacture and consumption.
As an example, I may form such concentrates into tablets, and, successively, superpose upon them a coat in which hydroquinone is uniformly incorporated and enrobe them with a coherent film of gelatin. Preferably,
' the coat and film are applied anaerically and comprise multiple layers. An outer coat to give any desired flavor or color and to safe- 50 guard the gelatin film from physical dam- Application flied February 12, 1931. Serial No. 515,421.
age, may also be provided; and the finished tablet may, as a further precaution, be enclosed in a container from which the air has been displaced by an inert gas. Little, if any, air will penetrate the gelatin film; and whatever does infiltrate through it will come into contact with, and be rendered oxidatively innocuous by reaction with, the hydroquinone. Access of oxygen to the concentrate is thus substantially prevented.
Instead of hydroquinonc, any other antioxidant, e. g. one of those first above specified, may be employed; and the gelatin may be replaced by gelatinous starch, shellac, acacia, tragacanth, or some other gum or resinous varnish. Ordinarily, the coats and films should be disintegrable in the gastric or intestinal fluids. For the outer coat, the sugar or chocolate covering commonly used will do. As previusly suggested, the order and number of the coats and films, and of their re spective layers, are by no means invariable; and the antioxidant may be mingled with the concentrate or dissolved in the gelatin solution producing the film.
As a more specific example, fat-solublevitamin-concentrate tablets embodying my invention may be made as follows, air being preferably excluded, by evacuation or by substitution of carbon dioxide, from the vessels used in the process, and the ingredients having preferably been deaerated: A granulation is formed, in the customary manner, of an excipient comprising milk sugar 4.9 parts, cocoa powder 30 parts, powdered sugar 20 parts, and monohydrated sodium carbonate 1 part, and after the excessively fine and coarse particles have been removed by sifting, is impregnated with an ethereal solution of a fat-soluble-vitamin concentrate obtained from cod-liver oil. Upon volatilization of the solvent, the granules are compressed into tablets and coated nine times with an antioxidant solution composed of simple sirupto which has been added 5% (calculated on the sucrose content) of hydroquinone. Then an impervious envelope is provided by applying, alternately with dusting powder to prevent the tablets from sticking together, six coats of a solution whose proportions are: gelatin 1 pound, sugar 25 pounds, water to make five gallons. A starch mixture is next applied, and last a finishing sirup; the respective volumes of which used for 135,000 tablets are 3% and 2 gallons; and the respective formulas of which are: granulated sugar 16 parts, water 7 parts, corn starch 4 parts, part, and erythrosin .0035 part; and simple sirup to every 4 gallons of which 3% grams of erythrosin has been added. When completed, the tablets are placed in bottles, which are then exhausted, flooded with carbon dioxide, and sealed. Optionally, the granulation referred to may include .5 part of hydroquinone, in which event the antioxidant-containing coat is not required; and the tablets after compression, or suitably composed and rolled pill masses, may then be completed by twice dipping, to cover them by successive halves, into the gelatin solution.
It is to be understood that the foregoing embodiments are merely illustrative and not definitive of my invention, which may assume various other forms-for instance, as to the particular autoxidizable material, antioxidant, or impervious envelope, and the specific procedures followed-within the see e of the appended claims.
claim:
1. A tablet comprising a vitamin concentrate, an antioxidant distributed around the concentrate, and an impervious envelope over the antioxidant, the antioxidant being a substance that reacts so rapidly with any oxygen penetrating the envelope as substantially to prevent oxidative deterioration of the concentrate.
2. A tablet comprising a fat-soluble-vitamin concentrate, an antioxidant distributed around the concentrate, and a elatin film over the antioxidant, the antioxi ant being a substance that reacts so rapidly with any oxygen penetrating thefilm as substantially to prevent oxidative deterioration of the concentrate.
3. A tablet comprising a fat-soluble-vitamin concentrate, hydroquinone distributed on the surface of the concentrate, and a gelatin film over the hydroquinone.
4. A tablet comprising a fat-soluble-vitamin concentrate, over the concentrate a coat in which hydroquinone is distributed, and
over the coat a gelatin film. 7
In witness whereof I aflix my signature. FERDINAND W. NITARDY.
alcohol .24 part, oil of spearmint .06 i
US515421A 1931-02-12 1931-02-12 Protection of autoxidizable materials Expired - Lifetime US1879762A (en)

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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2426762A (en) * 1945-04-16 1947-09-02 Scient Nutrition Corp Composition of matter
US2912332A (en) * 1958-02-27 1959-11-10 Swift & Co Stabilized thiamine composition and method of enriching food products
US3100783A (en) * 1958-06-26 1963-08-13 Philips Corp Method of stabilizing crystalline compounds against oxidation
US3110598A (en) * 1959-09-08 1963-11-12 Hoffmann La Roche Process of making a carotenoid preparation
US3124510A (en) * 1964-03-10 Stable dry powdered fat-soluble
US4389419A (en) * 1980-11-10 1983-06-21 Damon Corporation Vitamin encapsulation
US5750145A (en) * 1995-07-28 1998-05-12 Bristol-Myers Squibb Company Stable gelatin coated aspirin tablets

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3124510A (en) * 1964-03-10 Stable dry powdered fat-soluble
US2426762A (en) * 1945-04-16 1947-09-02 Scient Nutrition Corp Composition of matter
US2912332A (en) * 1958-02-27 1959-11-10 Swift & Co Stabilized thiamine composition and method of enriching food products
US3100783A (en) * 1958-06-26 1963-08-13 Philips Corp Method of stabilizing crystalline compounds against oxidation
US3110598A (en) * 1959-09-08 1963-11-12 Hoffmann La Roche Process of making a carotenoid preparation
US4389419A (en) * 1980-11-10 1983-06-21 Damon Corporation Vitamin encapsulation
US5750145A (en) * 1995-07-28 1998-05-12 Bristol-Myers Squibb Company Stable gelatin coated aspirin tablets

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