GB967610A - Sustained release medicament formulations - Google Patents

Sustained release medicament formulations

Info

Publication number
GB967610A
GB967610A GB38360/62A GB3836062A GB967610A GB 967610 A GB967610 A GB 967610A GB 38360/62 A GB38360/62 A GB 38360/62A GB 3836062 A GB3836062 A GB 3836062A GB 967610 A GB967610 A GB 967610A
Authority
GB
United Kingdom
Prior art keywords
polyoxyethylene glycol
medicament
tablets
esters
acid
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
Application number
GB38360/62A
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of GB967610A publication Critical patent/GB967610A/en
Expired legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A sustained release medicament formulation, in tablet, capsule or pellet form, comprises from 0.5 to 30% of a non-vitamin medicament or a mixture of such medicaments, from 5 to 85% of a carboxylic acid ester having a melting point of 65 DEG C. or above or a mixture of such esters, and from 1 to 10% of a polyoxyethylene glycol monoester or diester, which esters have the formulae <FORM:0967610/A5-A6/1> and <FORM:0967610/A5-A6/2> respectively in which n is 43 to 137 and R is the hydrocarbyl residue of a C12 and C18 fatty acid, or a mixture thereof; the percentages being based on the total weight of the formulation. Starch (1 to 20%), lubricant (0.5 to 3%) and filler (1 to 50%) may optionally be present. The formulations are manufactured by intimately admixing the medicament, polyoxyethylene glycol ester and carboxylic acid ester components and, if desired, any of the above mentioned optional ingredients, and forming the mixture into tablets, capsules or pellets. In a preferred embodiment, the polyoxyethylene glycol ester and carboxylic acid ester components are melted together at 85 DEG C. to 120 DEG C. and the medicament and optional excipients are suspended in the melt which is then chilled by, for example, pan-chilling, drum-chilling or spray-chilling, and the solidified mass is comminuted into pellets which can be converted into tablets or capsules, if desired. The tablets and pellets provide a sustained release of the medicament by erosion, which gives rise to an initial release of large quantities of medicament and a sustained release of smaller quantities of medicament over relatively long periods of time (e.g. about 4 to 12 hours) so as to maintain the desired blood level. The tablets and pellets may be sugar or enteric coated if desired, although the taste of the tablets and pellets is not objectionable even when somewhat bitter medicaments are employed. Specified medicaments for use in the invention are dextromethorphan hydrobromide, clidinium bromide, acetylsalicylic acid, phenacetin, phenylephrine and its hydrochloride, phenindamine, amphetamine sulphate, ephedrine hydrochloride, chlordiazepine, chlordiazepoxide hydrochloride and mixtures thereof, and 1-[(41-chlorophenyl) - ethyl] - 2 - methyl - 6,7 - dimethoxy - 1,2,3,4 - tetrahydroisoquinoline. In one of the examples, tablets are illustrated containing, in admixture, acetyl salicylic acid, acetophenetidine, phenylephrine and phenindamine. The carboxylic acid esters melting above 65 DEG C. include saturated waxes, e.g. carnauba wax and beeswax; saturated fats, e.g. mixed glyceryl esters of fatty acids such as stearic acid and palmitic acid; glyceryl tristearate and glyceryl tripalmitate; saturated diglycerides of fatty acids, e.g. castorwax; and mixtures of saturated monoglycerides, diglycerides and triglycerides of fatty acids such as stearic acid. The polyoxyethylene glycol esters may be esters of stearic acid, oleic acid and lauric acid, those specified being polyoxyethylene glycol (6000) distearate, polyoxyethylene glycol (4000) distearate, polyoxyethylene glycol (6000) dioleate, polyoxyethylene glycol (6000) dilaurate, polyoxyethylene glycol (4000) dilaurate and the corresponding monoesters.
GB38360/62A 1961-10-20 1962-10-10 Sustained release medicament formulations Expired GB967610A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14642261A 1961-10-20 1961-10-20

Publications (1)

Publication Number Publication Date
GB967610A true GB967610A (en) 1964-08-26

Family

ID=22517286

Family Applications (1)

Application Number Title Priority Date Filing Date
GB38360/62A Expired GB967610A (en) 1961-10-20 1962-10-10 Sustained release medicament formulations

Country Status (6)

Country Link
BE (1) BE623704A (en)
DE (1) DE1219176B (en)
ES (1) ES281704A1 (en)
FR (1) FR2172M (en)
GB (1) GB967610A (en)
MY (1) MY6600083A (en)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2254109A1 (en) * 1971-11-17 1973-05-24 Colgate Palmolive Co GRAINY MATERIAL, IN PARTICULAR FOR USE IN DENTAL CLEANING AGENTS AND THE PROCESS FOR THE PRODUCTION THEREOF
US4289795A (en) * 1975-11-17 1981-09-15 Aktiebolaget Hassle Method for preparing preparations having controlled release of an active component
EP0177368A2 (en) * 1984-10-05 1986-04-09 Warner-Lambert Company A novel drug delivery system and method of preparation thereof
EP0190255A1 (en) * 1984-07-23 1986-08-13 Zetachron Inc Erodible matrix for sustained release bioactive composition.
US4804548A (en) * 1984-10-05 1989-02-14 Warner-Lambert Company Novel sweetener delivery systems
US4828857A (en) * 1984-10-05 1989-05-09 Warner-Lambert Company Novel sweetener delivery systems
US5082655A (en) * 1984-07-23 1992-01-21 Zetachron, Inc. Pharmaceutical composition for drugs subject to supercooling

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3217071A1 (en) * 1982-05-06 1983-11-10 Rüdiger Dr. 6365 Rosbach Gröning Pharmaceutical composition for oral administration with improved bioavailability of the active substances

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2918411A (en) * 1957-11-01 1959-12-22 Olin Mathieson Pharmaceutical preparations

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2254109A1 (en) * 1971-11-17 1973-05-24 Colgate Palmolive Co GRAINY MATERIAL, IN PARTICULAR FOR USE IN DENTAL CLEANING AGENTS AND THE PROCESS FOR THE PRODUCTION THEREOF
US4289795A (en) * 1975-11-17 1981-09-15 Aktiebolaget Hassle Method for preparing preparations having controlled release of an active component
US4341759A (en) * 1975-11-17 1982-07-27 Aktiebolaget Hassle Granule having controlled release properties
EP0190255A1 (en) * 1984-07-23 1986-08-13 Zetachron Inc Erodible matrix for sustained release bioactive composition.
EP0190255A4 (en) * 1984-07-23 1987-10-20 Zetachron Inc Erodible matrix for sustained release bioactive composition.
US5082655A (en) * 1984-07-23 1992-01-21 Zetachron, Inc. Pharmaceutical composition for drugs subject to supercooling
EP0177368A2 (en) * 1984-10-05 1986-04-09 Warner-Lambert Company A novel drug delivery system and method of preparation thereof
EP0177368A3 (en) * 1984-10-05 1987-12-02 Warner-Lambert Company A novel drug delivery system and method of preparation thereof
US4804548A (en) * 1984-10-05 1989-02-14 Warner-Lambert Company Novel sweetener delivery systems
US4828857A (en) * 1984-10-05 1989-05-09 Warner-Lambert Company Novel sweetener delivery systems

Also Published As

Publication number Publication date
ES281704A1 (en) 1963-04-16
DE1219176B (en) 1966-06-16
MY6600083A (en) 1966-12-31
FR2172M (en) 1963-11-25
BE623704A (en)

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