GB878126A - Coated medicaments - Google Patents

Coated medicaments

Info

Publication number
GB878126A
GB878126A GB11114/58A GB1111458A GB878126A GB 878126 A GB878126 A GB 878126A GB 11114/58 A GB11114/58 A GB 11114/58A GB 1111458 A GB1111458 A GB 1111458A GB 878126 A GB878126 A GB 878126A
Authority
GB
United Kingdom
Prior art keywords
glyceryl
hydroxy
stearate
dihydroxy
alcohol
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
GB11114/58A
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.)
Smith Kline and French Laboratories Ltd
Original Assignee
Smith Kline and French Laboratories Ltd
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 Smith Kline and French Laboratories Ltd filed Critical Smith Kline and French Laboratories Ltd
Publication of GB878126A publication Critical patent/GB878126A/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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose

Landscapes

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

Abstract

A medicament coating material comprises an intimate mixture of a non-toxic, solid fatty alcohol having from 12-31 carbon atoms or a non-toxic, solid hydroxylated fatty ester having from 12-62 carbon atoms, and a solid cellulose derivative containing no free carboxylic groups. Preferred fatty esters include hydrogenated castor oil (principally glyceryl tri-12-hydroxystearate), glyceryl di-12-hydroxy stearate, glyceryl mono-12-hydroxy stearate, and preferred fatty alcohols include behenyl alcohol, stearyl alcohol and 12-hydroxy stearyl alcohol. Also specified are glyceryl mono- and di-stearate, propylene glycol monolaurate, ethylene glycol monopalmitate, ethylene glycol mono-12-hydroxy stearate, glyceryl monobehenate, glyceryl monocaprate, glyceryl didecanoate, propylene glycol monomyristate, glyceryl mono-12-hydroxy stearate, glyceryl tri-12-hydroxy stearate, propylene glycol di-12-hydroxy stearate, ethylene glycol di-9, 10, -dihydroxy stearate, glyceryl tridihydroxy stearate, glyceryl mono- and di-12-hydroxy stearate, glyceryl mono-16-hydroxy stearate, glyceryl di-11-hydroxy palmitate, glyceryl tri-12-hydroxy laurate, glyceryl monostearate di-12-hydroxy stearate, propyl- and dodecyl-9, 10-dihydroxy stearates, 12-hydroxy stearyl-butyrate and palmitate, octadecyl-9, 10-dihydroxy stearate and -12-hydroxylaurate, propyl 13, 14-dihydroxy behenate, 10-hydroxy stearyl alcohol, 9, 10-dihydroxy stearyl alcohol, 14-hydroxy behenyl alcohol and lauryl, ceryl, carnaubyl, myricyl, cetyl, myristyl and arachyl alcohols. Preferred cellulose derivatives are ethyl cellulose and cellulose acetate butyrate. Others specified are methyl- and propylcellulose, cellulose acetate, propionate, caprate, acetate-propionate and acetate-stearate. The ratio by weight of fatty alcohol or ester to cellulosic material in the coating may be from 1 : 1-20 : 1, especially from 1 : 1 -9 : 1. A preferred composition comprises hydrogenated castor oil and ethyl cellulose in proportions of 4 : 1. The coated medicament may be made by liquefying and admixing the fatty alcohol or ester and the cellulose derivative, either by heat or by solution in an organic solvent, e.g. chloroform and then applying the resulting coating material to the medicament. The coating should be at least 2% by weight of the coated pellets, preferably 5%-15%. Coated medicaments so made prolong the release of the medicament in the gastro-intestinal tract.ALSO:A medicament coating material for prolonging the release of the medicament in the gastrointestinal tract comprises an intimate mixture of a non-toxic, solid fatty alcohol having from 12-31 carbon atoms or a non-toxic, solid hydroxylated fatty ester having from 12-62 carbon atoms, and a solid cellulose derivative containing no free carboxylic groups. Preferred fatty esters include hydrogenated castor oil (principally glyceryl tri-12-hydroxystearate), glyceryl di-12-hydroxy stearate, glyceryl mono-12-hydroxy stearate, and preferred fatty alcohols include behenyl alcohol, stearyl alcohol and 12-hydroxy stearyl alcohol. Also specified are glyceryl mono- and di-stearate, propylene glycol monolaurate, ethylene glycol monopalmitate, ethylene glycol mono-12-hydroxy stearate, glyceryl monobehenate, glyceryl monocaprate, glyceryl didecanoate, propylene glycol monomyristate, glyceryl mono - 12 - hydroxy stearate, glyceryl tri-12-hydroxy stearate, propylene glycol di-12-hydroxy stearate, ethylene glycol di-9,10-dihydroxy stearate, glyceryl tridihydroxy stearate, glyceryl mono- and di-12-hydroxy stearate, glyceryl mono-16-hydroxy stearate, glyceryl di-11-hydroxy palmitate, glyceryl tri-12-hydroxy laurate, glyceryl monostearate di-12-hydroxy stearate, propyl- and dodecyl-9,10-dihydroxy stearates, 12-hydroxy stearyl-butyrate and palmitate, octadecyl-9,10-dihydroxy stearate and 12-hydroxylaurate, propyl 13,14-dihydroxy benhenate, 10-hydroxy stearyl alcohol, 9,10-dihydroxy stearyl alcohol, 14-hydroxy behenyl alcohol and lauryl, ceryl, carnaubyl, myricyl, cetyl, myristyl and arachly alcohols. Preferred cellulose derivatives are ethyl cellulose and cellulose acetate butyrate. Others specified are methyl- and propyl-cellulose, cellulose acetate, acetatebutyrate, propionate, caprate, acetate-propionate and acetate-stearate. The ratio by weight of fatty alcohol or ester to cellulosic material in the coating may be from 1 : 1 to 20 : 1, especially from 1 : 1 to 9 : 1. A preferred composition comprises hydrogenated castor oil and ethyl cellulose in proportions of 4 : 1. The coated medicament may be made by liquefying and admixing the fatty alcohol or ester and the cellulose derivative, either by heat or by solution in an organic solvent, e.g. chloroform, and then applying the resulting coating material to the medicament. The coating should be at least 2% by weight of the coated pellets, preferably 5-15%.
GB11114/58A 1957-05-03 1958-04-08 Coated medicaments Expired GB878126A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US878126XA 1957-05-03 1957-05-03

Publications (1)

Publication Number Publication Date
GB878126A true GB878126A (en) 1961-09-27

Family

ID=22207405

Family Applications (1)

Application Number Title Priority Date Filing Date
GB11114/58A Expired GB878126A (en) 1957-05-03 1958-04-08 Coated medicaments

Country Status (1)

Country Link
GB (1) GB878126A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2160096A (en) * 1984-06-04 1985-12-18 Mitsui Toatsu Chemicals Granule containing physiologically-active substance, method for preparing same and use thereof
GB2203336B (en) * 1987-04-01 1990-12-19 Strathclyde Chemical Co Ltd Composition

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2160096A (en) * 1984-06-04 1985-12-18 Mitsui Toatsu Chemicals Granule containing physiologically-active substance, method for preparing same and use thereof
GB2203336B (en) * 1987-04-01 1990-12-19 Strathclyde Chemical Co Ltd Composition

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