WO1981001652A1 - Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenues - Google Patents

Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenues Download PDF

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Publication number
WO1981001652A1
WO1981001652A1 PCT/FR1980/000176 FR8000176W WO8101652A1 WO 1981001652 A1 WO1981001652 A1 WO 1981001652A1 FR 8000176 W FR8000176 W FR 8000176W WO 8101652 A1 WO8101652 A1 WO 8101652A1
Authority
WO
WIPO (PCT)
Prior art keywords
galenical
dissolution
delayed action
preparation
preparing
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.)
Ceased
Application number
PCT/FR1980/000176
Other languages
English (en)
French (fr)
Inventor
D Panoz
G Corneille
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to DE803050131T priority Critical patent/DE3050131T1/de
Priority to AT0912580A priority patent/AT382513B/de
Publication of WO1981001652A1 publication Critical patent/WO1981001652A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K9/48—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
    • A61K9/5073—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 having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—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 having two or more different coatings optionally including drug-containing subcoatings with drug-free core

Definitions

  • the present invention relates to improvements made to methods of preparing various dosage forms. delayed action and in particular to the processes for preparing tablets, granules and the like with delayed action and programmed release.
  • Great strides have been made in recent times in the preparation of oral drug delivery forms to better control the release kinetics of the drug.
  • Wrapping means have been developed, means of retention in inert matrices, means of diffusion or controlled dialysis of medicaments or else a combination of several of these means has been used to ensure, at the starting from the same pharmaceutical form, a modification of the absorption or elimination of drugs in order to prolong the duration of action, as is the case for example for the combination, in the same galenic form , viscosifying agents which slow down the dissolution with active constituents of well-defined particle size.
  • the improvements brought to the preparations of form of administration by oral route with prolonged action are mainly reflected:
  • the object of the present invention is to further improve the process for the preparation of forms of oral administration of drugs with prolonged action and with programmable kinetics, so as to be able to dispense with high compression and to be able to further reduce the price of returns from these extremely widespread dosage forms.
  • the subject of the present invention is a process for the preparation of dosage forms with a delayed action, characterized in that the solutions for applying the excipients, the coatings and the active constituents are adjusted to a desired pH.
  • the application solutions are adjusted to an alkaline pH using organic and / or mineral bases and / or basic salts.
  • the application solutions are adjusted to an acidic pH using organic acids and / or acid salts.
  • the present invention also relates to the new dosage forms obtained according to the process according to the present invention.
  • curves a, b and c are those of commercial indomethacin ("INDOCID" from Merck, Sharp and Dohme), curves d and f represent the dissolutions of the form galenical according to the present invention.
  • Curve a represents the dissolution as a function of time at pH 6
  • curve b represents the dissolution at pH 3
  • curve c represents the dissolution at pH 1.5 of commercial indomethacin.
  • This dissolution rate is heterogeneous and depends on the pH of the medium. He is leaving . quite differently with the dosage form according to the present invention.
  • the dissolution is uniform and independent of pH: the three curves d (pH 1.5), e (pH 3) and f (pH 6) practically merge.
  • Table I summarizes the blood levels measured on 4 volunteers who were administered 150 mg of product (the results are expressed in mcg / ml of blood plasma).
  • This new dosage form is suitable for all drugs whose solubility rate varies with the pH, such as for example diazepam, cephalexin, cimetidine, cephalotin, methyldopa, cefazolin, propanolol, indomethacin, l 'ibuprofen, doxycycline, amoxycillin, furosemide, dipyridamole, spironolactone, erythromycin, gentamicin, diclofenac, glibenclamide, althiaside, naproxen, propoxyphene, 1' allopurinol, sulfamethox ampicillin, prosultium, lincomycin, betamethasone, troleandomycin, vincamine, clonidine, glafenin, clometacin, disopyramide, sulpiride, oxyphen-butazone, clorazepate, cephalosporin, rifamp

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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Excavating Of Shafts Or Tunnels (AREA)
PCT/FR1980/000176 1979-12-07 1980-12-05 Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenues Ceased WO1981001652A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
DE803050131T DE3050131T1 (de) 1979-12-07 1980-12-05 Improvements to methods for preparing galenical preparation with delayed action and programmed release and galenical preparations for drugs obtained thereby
AT0912580A AT382513B (de) 1979-12-07 1980-12-05 Verfahren zur herstellung von galenischen formen mit verzoegerter wirkung

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR7930085 1979-12-07
FR7930085A FR2470599A1 (fr) 1979-12-07 1979-12-07 Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenus

Publications (1)

Publication Number Publication Date
WO1981001652A1 true WO1981001652A1 (fr) 1981-06-25

Family

ID=9232512

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR1980/000176 Ceased WO1981001652A1 (fr) 1979-12-07 1980-12-05 Perfectionnements apportes aux procedes de preparation de formes galeniques a action retard et a liberation programmee et formes galeniques de medicaments ainsi obtenues

Country Status (11)

Country Link
US (1) US5051262A (enExample)
JP (1) JPH0530804B2 (enExample)
AT (1) AT382513B (enExample)
BE (1) BE886510A (enExample)
CH (1) CH648207A5 (enExample)
DE (1) DE3050131T1 (enExample)
ES (1) ES497534A0 (enExample)
FR (1) FR2470599A1 (enExample)
GB (1) GB2075343B (enExample)
IT (1) IT1134638B (enExample)
WO (1) WO1981001652A1 (enExample)

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WO2006010640A1 (en) * 2004-07-29 2006-02-02 Sanofi-Aventis Pharmaceutical multilayer tablet for controlled release of active ingredients with highly ph-dependent solubility

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IT1148784B (it) * 1980-04-09 1986-12-03 Eurand Spa Procedimento per la preparazione di microcapsule in un veicolo liquido
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HU183408B (en) * 1981-04-28 1984-05-28 Chinoin Gyogyszer Es Vegyeszet Process for producing oral ratard pharmaceutical compositions
DE3124090A1 (de) * 1981-06-19 1983-01-05 Dr. Karl Thomae Gmbh, 7950 Biberach Neue orale dipyridamolformen
DK150008C (da) * 1981-11-20 1987-05-25 Benzon As Alfred Fremgangsmaade til fremstilling af et farmaceutisk oralt polydepotpraeparat
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DK151608C (da) * 1982-08-13 1988-06-20 Benzon As Alfred Fremgangsmaade til fremstilling af et farmaceutisk peroralt polydepotpraeparat med kontrolleret afgivelse
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US4525345A (en) * 1981-12-24 1985-06-25 Verex Laboratories, Inc. Constant order release, solid dosage indomethacin formulation and method of treating arthritis and other inflammatory conditions
GB2151920A (en) * 1983-12-23 1985-07-31 Ile De France Oral compositions containing sulpiride
US4752470A (en) * 1986-11-24 1988-06-21 Mehta Atul M Controlled release indomethacin
FR2635460A1 (fr) * 1988-08-16 1990-02-23 Ss Pharmaceutical Co Preparation de diclofenac sodique a action de longue duree
BE1002710A5 (fr) * 1988-08-16 1991-05-14 Ss Pharmaceutical Co Preparation au diclofenac sodique a effet prolonge.
EP0355247A3 (en) * 1988-08-22 1990-12-12 Ss Pharmaceutical Co., Ltd. Compressed-molded preparations
US5186943A (en) * 1988-08-22 1993-02-16 Ss Pharmaceutical Co., Ltd. Compressed-molded preparations
US5275825A (en) * 1988-08-22 1994-01-04 Ss Pharmaceutical Co., Ltd. Compressed-molded preparations
WO2006010640A1 (en) * 2004-07-29 2006-02-02 Sanofi-Aventis Pharmaceutical multilayer tablet for controlled release of active ingredients with highly ph-dependent solubility

Also Published As

Publication number Publication date
GB2075343A (en) 1981-11-18
ES8306322A1 (es) 1983-05-16
DE3050131C2 (enExample) 1992-01-09
US5051262A (en) 1991-09-24
FR2470599B1 (enExample) 1983-03-25
ES497534A0 (es) 1983-05-16
IT8026515A0 (it) 1980-12-09
ATA912580A (de) 1986-08-15
FR2470599A1 (fr) 1981-06-12
BE886510A (fr) 1981-06-05
JPS56501803A (enExample) 1981-12-10
AT382513B (de) 1987-03-10
CH648207A5 (fr) 1985-03-15
GB2075343B (en) 1984-10-10
IT1134638B (it) 1986-08-13
DE3050131T1 (de) 1982-03-25
JPH0530804B2 (enExample) 1993-05-11

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