GB834397A - Therapeutic compositions comprising erythromycin esters - Google Patents

Therapeutic compositions comprising erythromycin esters

Info

Publication number
GB834397A
GB834397A GB2445758A GB2445758A GB834397A GB 834397 A GB834397 A GB 834397A GB 2445758 A GB2445758 A GB 2445758A GB 2445758 A GB2445758 A GB 2445758A GB 834397 A GB834397 A GB 834397A
Authority
GB
United Kingdom
Prior art keywords
erythromycin
acid
ester
magnesium stearate
esters
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
GB2445758A
Inventor
Verlin Clark Stephens
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Priority to GB2445758A priority Critical patent/GB834397A/en
Publication of GB834397A publication Critical patent/GB834397A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

The invention relates to a mono ester of erythromycin and its acid addition salts, said ester being represented by the formula <FORM:0834397/IV (b)/1> in which R is acetyl, propionyl or acrylyl. The erythromycin is acylated with 1 mol. equivalent of the acid halide or anhydride of acetic propionic or acrylic acid in the presence of a solvent such as acetone and, if desired, in the presence of an alkali such as sodium or potassium bicarbonate or magnesium oxide to remove the acid produced in the reaction. Water may be added to precipitate the ester. The esters are generally solvated. The esters form salts with inorganic acids such as hydrochloric, sulphuric and phosphoric and with organic acids such as oxalic acid dichloroacetic acid and naphthalene sulphonic acid. They produce high blood levels of erythromycin when administered orally (see Group VI).ALSO:A therapeutic composition for oral administration comprises a pharmaceutical carrier and an acetyl, propionyl or acrylyl mono-ester of erythromycin (see Group IV (b)), or an acid addition salt thereof. Specified are the hydrochloride, sulphate, phosphate, oxalate, dichloroacetate and naphthalene sulphonate. The compositions may be in the form of tablets or capsules. Examples relate to a tablet containing (a) monopropionylerythromycin, magnesium stearate, starch and sodium lauryl sulphate; (b) monoacetylerythromycin, starch, polyvinylpyrrolidone and magnesium stearate, and to a capsule containing monopropionylerythromycin, mineral oil, magnesium stearate and lactose. The compositions provide high blood levels of erythromycin.
GB2445758A 1958-07-29 1958-07-29 Therapeutic compositions comprising erythromycin esters Expired GB834397A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
GB2445758A GB834397A (en) 1958-07-29 1958-07-29 Therapeutic compositions comprising erythromycin esters

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB2445758A GB834397A (en) 1958-07-29 1958-07-29 Therapeutic compositions comprising erythromycin esters

Publications (1)

Publication Number Publication Date
GB834397A true GB834397A (en) 1960-05-04

Family

ID=10212007

Family Applications (1)

Application Number Title Priority Date Filing Date
GB2445758A Expired GB834397A (en) 1958-07-29 1958-07-29 Therapeutic compositions comprising erythromycin esters

Country Status (1)

Country Link
GB (1) GB834397A (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2557878A1 (en) * 1984-01-06 1985-07-12 Orion Yhtymae Oy ANTIBIOTIC COMPOUND, PROCESS FOR PREPARING THE SAME, AND COMPOSITIONS CONTAINING THE SAME

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2557878A1 (en) * 1984-01-06 1985-07-12 Orion Yhtymae Oy ANTIBIOTIC COMPOUND, PROCESS FOR PREPARING THE SAME, AND COMPOSITIONS CONTAINING THE SAME
DE3500179A1 (en) * 1984-01-06 1985-07-18 Orion-yhtymä Oy, Espoo ACETYLERYTHROMYCINSTEARATE, METHOD FOR THE PRODUCTION THEREOF AND MEDICINAL PRODUCT CONTAINING THIS
AT386414B (en) * 1984-01-06 1988-08-25 Orion Yhtymae Oy METHOD FOR PRODUCING THE NEW 2'-ACETYLERY THROMYCINSTEARATE

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