US2149005A - Shaped medicinal preparation - Google Patents
Shaped medicinal preparation Download PDFInfo
- 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
- Authority
- US
- United States
- Prior art keywords
- polyethylene oxide
- shaped
- shaped medicinal
- medicinal preparations
- medicinal preparation
- 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
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
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- 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
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- Y—GENERAL 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
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S424/00—Drug, bio-affecting and body treating compositions
- Y10S424/15—Suppositories
Definitions
- 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.
- Hyphomycetes and bacteria 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.
- polyalkylene oxides and the derivatives thereof are suitable vehicles for the manufacture of shaped medicinal preparations to be introduced into the cavities.
- 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.
- 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.
- compositions of the new vehicles there may, of course, also be used mixtures of the new vehicles.
- suitable adjuvants and corrigents such as glycerine, water, small proportions of fat, hydrocarbons having a high molecular weight and the like.
- 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.
- 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
- 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.
- Shaped medicinal preparations comprising a pharmacologically active substance and a vehicle consisting of polyethylene oxide.
- 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.
- 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.
- 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.
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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.
Applications Claiming Priority (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)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US109022A Expired - Lifetime US2149005A (en) | 1935-11-09 | 1936-11-03 | Shaped medicinal preparation |
Country Status (3)
Country | Link |
---|---|
US (1) | US2149005A (en) |
GB (1) | GB484600A (en) |
NL (1) | NL44885C (en) |
Cited By (28)
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)
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 TO INDOMETHACIN |
GB2159052A (en) * | 1984-05-18 | 1985-11-27 | Bernard John Roberts | Artificial mucus material |
-
0
- NL NL44885D patent/NL44885C/xx active
-
1936
- 1936-11-03 US US109022A patent/US2149005A/en not_active Expired - Lifetime
- 1936-11-09 GB GB30489/36A patent/GB484600A/en not_active Expired
Cited By (30)
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 |
USRE29102E (en) * | 1972-03-21 | 1977-01-04 | Merz & Co. | Contraception agent |
US3876757A (en) * | 1972-03-21 | 1975-04-08 | 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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