EP0453001A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Pharmaceutical composition for the targeted controlled release of an active principle within the intestine, and particularly within the colon
Assignee: Giuliani SpA
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Filing: 1991-01-29
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Granted: —
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Expires: 2011-01-29
Abstract
Abstract The invention provides pharmaceutical compositions with the property of targeted controlled release of active principles which act pharmacologically within the intestine and in particular within the colon and the terminal portion of the ileum. To attain this object the active principle is prepared in multiparticle multidose form and is covered with at least two membranes, one of pH-dependent solubility and the other insoluble but permeable to the intestinal fluids. While the covered active principle remains in the stomach and in the initial intestinal portion, ie while the pH is less than 5.5, it is not released. Only when it reaches an environment of higher pH (small intestine or colon) does the pH-dependent membrane dissolve to commence release of the active principle. From this moment the second membrane, which is pH-independent but permeable to the intestinal fluids, acts to slow down and control the dissolution of the medicament within the small intestine-colon tract.
Inventors
- 👤 Massimo Calanchi
- 👤 Marco Zema
- 👤 Gabriele Brunetti
- 👤 Enzo Giorgetti
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 03:56
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/20; A61K9/2072; A61K9/2086; A61K9/209
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
125 words
A pharmaceutical composition for the targeted controlled release of an active principle within the intestine, and in particular within the terminal portion of the ileum and the colon, characterised in that said active principle is chosen from the following: antiinflammatory-antiphlogistic agents of local and general action, such as 5-aminosalicylic acid (or mesalazine) and analogous salicylic derivatives, peppermint oil, corticosteroids of the kind directed to the local treatment of chronic intestinal diseases of inflammatory and irritative type; said active principle being formulated in multiparticle multidose form, each particle thereof being covered with at least two membranes, one of which is soluble at a pH equal to or greater than 5.5, the other of said membranes being insoluble at said pH but permeable to the intestinal fluids.
Claim 2
Dependent Claim
44 words
A composition as claimed in claim 1, characterised in that said active principle is covered with a first membrane soluble at said pH values, this first membrane being covered with a second membrane insoluble at said pH values but permeable to the intestinal fluids.
Claim 3
Dependent Claim
43 words
A composition as claimed in claim 1, characterised in that the active principle is covered with a first membrane insoluble at said pH values but permeable, and being covered with a second membrane soluble at said pH values in natural or artificial fluids.
Claim 4
Dependent Claim
38 words
A composition as claimed in claim 1, characterised in that said active principle in multiparticle multidose form is in the form of crystals, granules, pellets or minitablets having a particle size distribution of between 0.1 and 3.5 mm.
Claim 5
Dependent Claim
63 words
A composition as claimed in claim 1, characterised in that said membrane soluble at a pH equal to or greater than 5.5 consists of one or more of the following polymers: copolymers of methacrylic acid (Eudragit L, Eudragit S), cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate, polyvinyl acetate phthalate, shellac, hydroxypropylmethylcellulose acetate succinate, carboxymethylcellulose, cellulose acetate trimellitate, copolymers of maleic acid and phthalic acid derivatives.
Claim 6
Dependent Claim
62 words
A composition as claimed in one or more of the preceding claims, characterised in that the membrane insoluble at said pH values but permeable to the intestinal fluids consists of copolymers of methacrylic esters (Eudragit RS/RL/NE), ethylcellulose, polyethylene and polysiloxanes, either alone or mixed with each other or with other pH-independent polymers soluble in water, such as hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, methylcellulose, polyvinylpyrrolidone.
Claim 7
Dependent Claim
17 words
A composition as claimed in claim 5, characterised in that said membrane (pH-dependent) consists of Eudragit S.
Claim 8
Dependent Claim
28 words
A composition as claimed in claim 6, characterised in that said membrane (pH-independent) is ethylcellulose, or ethylcellulose mixed with hydroxypropylmethylcellulose in a ratio varying from 1:3 to 3:1.
Claim 9
Dependent Claim
31 words
A composition as claimed in claim 1, characterised in that said membranes comprise further components such as plasticizers, preferably consisting of polyethylene glycol, dibutyl phthalate, diethyl phthalate, or citric acid esters.
Claim 10
Dependent Claim
26 words
A composition as claimed in claim 1, characterised in that said membranes also comprise adjuvants, preferably consisting of talc, silicon dioxide, titanium dioxide or magnesium stearate.
Claim 11
Dependent Claim
18 words
A composition as claimed in claim 1, characterised in that said active principle is 5-aminosalicylic acid (or mesalazine).
Claim 12
Dependent Claim
16 words
A composition as claimed in claim 1, characterised in that said active principle is peppermint oil.
References Cited (Backward Citations)
GB2066070A
Cited
GB2134785A
Cited
EP0148811A1
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WO1985003437A1
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EP0212745A2
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EP0239361A1
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