US2149005A - Shaped medicinal preparation - Google Patents

Shaped medicinal preparation Download PDF

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Publication number
US2149005A
US2149005A US109022A US10902236A US2149005A US 2149005 A US2149005 A US 2149005A US 109022 A US109022 A US 109022A US 10902236 A US10902236 A US 10902236A US 2149005 A US2149005 A US 2149005A
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US
United States
Prior art keywords
shaped
polyethylene oxide
medicinal preparation
medicinal preparations
shaped medicinal
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.)
Expired - Lifetime
Application number
US109022A
Inventor
Bockmuhl Max
Middendorf Leonhard
Starck Werner
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.)
WINTHROP CHEM CO Inc
WINTHROP CHEMICAL COMPANY Inc
Original Assignee
WINTHROP CHEM CO Inc
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
Priority to DE484600X priority Critical
Application filed by WINTHROP CHEM CO Inc filed Critical WINTHROP CHEM CO Inc
Application granted granted Critical
Publication of US2149005A publication Critical patent/US2149005A/en
Anticipated expiration legal-status Critical
Application status is Expired - Lifetime legal-status Critical

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S424/00Drug, bio-affecting and body treating compositions
    • Y10S424/15Suppositories

Description

Patented Feb. 1939 NITED STATES SHAPED MEDICINAL PREPARATION Max Bockmiihl, Frankfort-on-the-Main-Hochst,

Leonhard Middendorf,Frankfort-on-the-Main- Sindlingen, and Werner Starck, Hofheim in Taunus. Germany,

assignors to Winthrop Chemical Company, Inc., New York, N. Y., a corporation of New York No Drawing. Application November 3, 1936, Serial No. 109,022. In Germany November 9, 1935 4 Claims.

The present invention relates to shaped methermore, the resorption of the vehicle occurs 1.5 very slowly there is the danger that part of the molten mass will flow from the cavities whereby an exact dosing ofthe medicine is made impossible. Finally most of the fats readily become rancid and havethen an irritating efiect 20 upon the mucous membranes. For a long time therefore, the function of basis material for shaped medicinal preparations has been shared by masses prepared from solutions of gelatin, agar-agar and the like in glycerine and water.

25 But also these vehicles show many defects. They dry readily when stored whereby their solubility in the cavities is diminished.

Furthermore, they constitute a nutrient medium for Hyphomycetes and bacteria. They are 30 liable to become mouldy and to form in the cavities an undesired and in certain cases even noxious nutrient medium for pathogenic bacteria.

Attempts which have been made to remove the drawbacks associated with these several vehicles 35 have not shownany practical results. Also swelling bodies which are often used for medicinal preparations to be introduced into the urethra or openings of wounds are not free from drawbacks. They also become hard when they are 40 stored up and then break down in the cavities only with difilculty.

Now we have found that polyalkylene oxides and the derivatives thereof are suitable vehicles for the manufacture of shaped medicinal preparations to be introduced into the cavities. In contradistinction to the fatty vehicles the melting point of the new vehicles is of no importance because their function does not depend on fusion but on dissolution in the secretion of the cavity.

The medicinal preparations which may be prepared according to our present invention have also the following favorable properties. When they are stored they are not decomposed and do not dry. They mix well and can 55 be shaped in a solid as well as in a molten state with most of the medicines. The preparations made with their aid have an unobjectionable solidity and persistence of form. As these new vehicles are soluble in water and in lipoids the medicinal preparation quickly dissolves in the-6 cavities so that the medicines contained in it can rapidly and completely be resorbed.

The new vehicles are physiologically indifferent, nonirritant and odorless and are resistant to the tropical climate. In consequence of the 10 surface activity of the new vehicles a very high degree of distribution of the incorporated medicines is obtained. J

Polyalkylene oxides and especially polyethylene oxide, which has been polymerized up to a waxlike consistency are, for instance, suitable; furthermore the derivatives of the polyalkylene oxides, especially the reaction products of ethylene oxide upon organic compounds which contain hydroxy-, carboxy-, aminoor amido-groups and among these especially those which have been obtained by the action of 10 to 20 molecular proportions of ethylene oxide upon 1 molecular proportion of the organic compound in question especially of a compound containing at least 10 5 carbon atoms. The compounds, for instance, which are obtained by the action of ethylene oxide upon castor oil, ricinole'ic acid or oleyl alcohol are especially suitable.-

For the preparation of the solid medicinal preparations there may, of course, also be used mixtures of the new vehicles. According to the desired purpose there may also be used suitable adjuvants and corrigents, such as glycerine, water, small proportions of fat, hydrocarbons having a high molecular weight and the like.

We have furthermore found that polyalkylene oxides and their derivatives may be used with the same result for the preparation of pills, tablets and the like. It is know that those medicinal preparations, made in known manner, often become hard when they are stored and then break down only very slowly or insufiiciently in the stomach or intestine. The same is true of tablets and dragees. Medicinal preparations to be administered per 0s and free from the disadvantages mentioned may be made by the invention. Also in this case widely differing derivatives of the polyalkyiene oxides may be used. Adjuvants of quite difierent kinds may also be used therewith.

The following examples illustrate the invention but they are not intended to limit it thereto; the

parts are by weight:

(1) Morphine suppositories (4) Papaverine tablets Parts Parts Morphine hydrochloride 0.5 Papaverine hydrochloride 4 Very pure, bleached polyethylene oxide 227 Very pure, bleached polyethylene oxide 33 Condensation product from ethylene oxide Glycerine 3 and ricinoleic acid 22. 3 Water 22. 2

(2) Suppositories prepared from dimethylaminophenyldimethylpyrazolone, sodium phenyldimethvlpurazolonemethylammomethane sulfanate and urethane Parts Dimethylaminophenyldimethylpyrazolone 40 Sodium phenyldimethylpyrazolonemethylaminomethane sulfonate 60 Urethane 45 Very pure, bleached polyethylene oxide 250 (3),Small rods containing the compound prepared from gelatose with silver nitrate Parts The compound prepared from gelatose with silver nitra 0. 25 Very pure, bleached polyethylene oxide-" 42 The condensation product from ethylene oxide and ricinoleic acid 4 45 Water 4 The mass which is prepared as described in Example l is poured into hollow moulds for rods.

The papaverine is made into a paste with the glycerine and the polyethylene oxide which has been liquefied by heating it on a steam bath is then stirred in. The mass is either poured into hollow moulds and allowed to cool or it is poured onto a glass plate or the like where it is allowed to harden and is then cut to form tablets.

(5) Pills prepared from cafl'eine-phenylethylmalonyl-urea Parts Cafl ln 2.5 Phenylethylmalonyl-urea 5 Very pure, bleached polyethylene oxide 15 Sugar syrup 5 The phenylethylmalonyl-urea and the cafieine are mixed with the polyethylene oxide which previously has been pulverized and the mixture is kneaded with the sugar syrup to a plastic mass. Pills are formed from this mass in the usual manner.

We claim: I

1. Shaped medicinal preparations comprising a pharmacologically active substance and a vehicle consisting of polyethylene oxide.

2. Shaped medicinal preparations comprising a pharmacologically active substance, a compound obtained by the interaction of ethylene oxide and ricinoleic acid and a vehicle consisting of polyethylene oxide.

3. Shaped medicinal preparations comprising a pharmacologically active substance, a compound obtained by the interaction of ethylene oxide and castor oil and a vehicle consisting of polyethylene oxide. a

4. Shaped medicinal preparations comprising a pharmacologically active substance, 8. compound obtained by the interaction of ethylene oxide and oleyl alcohol and a vehicle consisting of polyethylene oxide.

MAX BocKMiiHL. LEONHARD MIDDENDORF. WERNER STARCK.

US109022A 1935-11-09 1936-11-03 Shaped medicinal preparation Expired - Lifetime US2149005A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DE484600X 1935-11-09

Publications (1)

Publication Number Publication Date
US2149005A true US2149005A (en) 1939-02-28

Family

ID=6543150

Family Applications (1)

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US109022A Expired - Lifetime US2149005A (en) 1935-11-09 1936-11-03 Shaped medicinal preparation

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US (1) US2149005A (en)
GB (1) GB484600A (en)
NL (1) NL44885C (en)

Cited By (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2457188A (en) * 1945-05-24 1948-12-28 Americaine Inc Benzocaine solution
US2469618A (en) * 1945-09-21 1949-05-10 Eaton Lab Inc Vaginal suppository
US2498374A (en) * 1945-10-05 1950-02-21 Francis E Martin Method and article for treatment of mammary glands
US2538127A (en) * 1948-02-26 1951-01-16 Searle & Co Medicated suppositories and bases therefor
US2540253A (en) * 1949-02-08 1951-02-06 Merck & Co Inc Granulation process
US2584166A (en) * 1948-05-25 1952-02-05 Ayerst Mckenna & Harrison Suppository
US2605209A (en) * 1950-11-03 1952-07-29 Lilly Co Eli Solutions of barbituric compounds
US2681297A (en) * 1950-10-31 1954-06-15 Mattox And Moore Inc Veterinary estrogen composition and administration method
US2698822A (en) * 1951-04-28 1955-01-04 Fougera & Co Inc E Cardiac glycoside buccal composition
US2762746A (en) * 1952-11-14 1956-09-11 American Home Prod Composition for combating malaria and process of making same
US2791530A (en) * 1953-08-31 1957-05-07 Abbott Lab Stabilized fumagillin compositions
US2890983A (en) * 1956-07-31 1959-06-16 Monot Pierre Louis Victor Excipient
US2899361A (en) * 1959-08-11 Certificate of correction
US3087860A (en) * 1958-12-19 1963-04-30 Abbott Lab Method of prolonging release of drug from a precompressed solid carrier
US3149038A (en) * 1961-09-05 1964-09-15 Dow Chemical Co Thin film coating for tablets and the like and method of coating
US3163576A (en) * 1961-06-12 1964-12-29 Olin Mathieson Suppository base comprising glycerin and a diester of polyethylene glycol
US3432592A (en) * 1962-08-31 1969-03-11 Ciba Geigy Corp Injection-moulded oral medicament in solid form
US3511914A (en) * 1967-01-31 1970-05-12 Schering Corp Throat lozenge vehicle
FR2199998A1 (en) * 1972-09-21 1974-04-19 Takeda Chemical Industries Ltd Medicaments contg. sulpyrin suppositories - giving high blood sulpyrin concentrations
US3826232A (en) * 1970-09-18 1974-07-30 Pet Chem Inc Composition and method for the control of fleas on domesticated animals
US3862311A (en) * 1971-04-12 1975-01-21 Ciba Geigy Corp Novel method of enhancing progestational endometrial proliferation with progesterone
US3876757A (en) * 1972-03-21 1975-04-08 Merz & Co Contraception agent
USRE29102E (en) * 1972-03-21 1977-01-04 Merz & Co. Contraception agent
US4151273A (en) * 1974-10-31 1979-04-24 The Regents Of The University Of California Increasing the absorption rate of insoluble drugs
US4265875A (en) * 1976-07-23 1981-05-05 Inveresk Research International Controlled release suppositories
US4343789A (en) * 1979-07-05 1982-08-10 Yamanouchi Pharmaceutical Co., Ltd. Sustained release pharmaceutical composition of solid medical material
WO1982003747A1 (en) * 1981-04-29 1982-11-11 Int Spike Systemic pesticide product and processes for making and using it
US4690822A (en) * 1985-03-26 1987-09-01 Fujisawa Pharmaceutical Co., Ltd. Novel drug carrier and pharmaceutical preparation comprising the same

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2949402A (en) * 1958-04-16 1960-08-16 American Cyanamid Co Tablet coating
BE756975A (en) * 1970-06-09 1971-04-02 Merck & Co Inc suppositories
BE789726A (en) * 1971-10-06 1973-04-05 Merck & Co Inc Suppositories has indomethacin
GB2159052A (en) * 1984-05-18 1985-11-27 Bernard John Roberts Artificial mucus material

Cited By (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2899361A (en) * 1959-08-11 Certificate of correction
US2457188A (en) * 1945-05-24 1948-12-28 Americaine Inc Benzocaine solution
US2469618A (en) * 1945-09-21 1949-05-10 Eaton Lab Inc Vaginal suppository
US2498374A (en) * 1945-10-05 1950-02-21 Francis E Martin Method and article for treatment of mammary glands
US2538127A (en) * 1948-02-26 1951-01-16 Searle & Co Medicated suppositories and bases therefor
US2584166A (en) * 1948-05-25 1952-02-05 Ayerst Mckenna & Harrison Suppository
US2540253A (en) * 1949-02-08 1951-02-06 Merck & Co Inc Granulation process
US2681297A (en) * 1950-10-31 1954-06-15 Mattox And Moore Inc Veterinary estrogen composition and administration method
US2605209A (en) * 1950-11-03 1952-07-29 Lilly Co Eli Solutions of barbituric compounds
US2698822A (en) * 1951-04-28 1955-01-04 Fougera & Co Inc E Cardiac glycoside buccal composition
US2762746A (en) * 1952-11-14 1956-09-11 American Home Prod Composition for combating malaria and process of making same
US2791530A (en) * 1953-08-31 1957-05-07 Abbott Lab Stabilized fumagillin compositions
US2890983A (en) * 1956-07-31 1959-06-16 Monot Pierre Louis Victor Excipient
US3087860A (en) * 1958-12-19 1963-04-30 Abbott Lab Method of prolonging release of drug from a precompressed solid carrier
US3163576A (en) * 1961-06-12 1964-12-29 Olin Mathieson Suppository base comprising glycerin and a diester of polyethylene glycol
US3149038A (en) * 1961-09-05 1964-09-15 Dow Chemical Co Thin film coating for tablets and the like and method of coating
US3432592A (en) * 1962-08-31 1969-03-11 Ciba Geigy Corp Injection-moulded oral medicament in solid form
US3511914A (en) * 1967-01-31 1970-05-12 Schering Corp Throat lozenge vehicle
US3826232A (en) * 1970-09-18 1974-07-30 Pet Chem Inc Composition and method for the control of fleas on domesticated animals
US3862311A (en) * 1971-04-12 1975-01-21 Ciba Geigy Corp Novel method of enhancing progestational endometrial proliferation with progesterone
US3876757A (en) * 1972-03-21 1975-04-08 Merz & Co Contraception agent
USRE29102E (en) * 1972-03-21 1977-01-04 Merz & Co. Contraception agent
FR2199998A1 (en) * 1972-09-21 1974-04-19 Takeda Chemical Industries Ltd Medicaments contg. sulpyrin suppositories - giving high blood sulpyrin concentrations
US4151273A (en) * 1974-10-31 1979-04-24 The Regents Of The University Of California Increasing the absorption rate of insoluble drugs
US4265875A (en) * 1976-07-23 1981-05-05 Inveresk Research International Controlled release suppositories
US4292300A (en) * 1976-07-23 1981-09-29 Inveresk Research International Controlled release suppositories
US4343789A (en) * 1979-07-05 1982-08-10 Yamanouchi Pharmaceutical Co., Ltd. Sustained release pharmaceutical composition of solid medical material
US4404183A (en) * 1979-07-05 1983-09-13 Yamanouchi Pharmaceutical Co., Ltd. Sustained release pharmaceutical composition of solid medical material
WO1982003747A1 (en) * 1981-04-29 1982-11-11 Int Spike Systemic pesticide product and processes for making and using it
US4690822A (en) * 1985-03-26 1987-09-01 Fujisawa Pharmaceutical Co., Ltd. Novel drug carrier and pharmaceutical preparation comprising the same

Also Published As

Publication number Publication date
GB484600A (en) 1938-05-09
NL44885C (en)

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