Easy to swallow oral medicament composition

Details Easy to swallow oral medicament composition Easy to swallow oral medicament composition

1999-02-10

2004-03-23

Travers, Russell (Department: 1617)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

C424S494000, C424S493000, C424S474000, C424S475000, C424S476000, C424S479000, C424S480000, C424S481000, C424S492000, C424S495000, C424S496000, C424S497000, C424S482000, C427S002140, C427S002150, C514S200000, C514S198000, C514S165000

Reexamination Certificate

active

06709678

ABSTRACT:

This is a 371 of PCT/CH97/00299 filed on Aug. 14, 1997 which claims priority to Swiss Application 2006/96.
The invention relates to an easy to swallow pharmaceutical composition for oral administration comprising at least one pharmaceutically active compound in an effective amount and comprising one or more coated particles, and to a process for the production thereof and a method for treating or preventing diseases.
Oral intake of solid medicament compositions, such as tablets or capsules, is associated with problems in particular as a function of their size, it frequently being possible for swallowing difficulties to occur, especially in children and elderly people. Although simultaneous administration of several tablets or capsules may improve swallowability, on the other hand it has an adverse effect on patient compliance. Alternative formulations have already been proposed to get around these problems, for example powders or granules, which are made into suspensions, tablets which disintegrate in the mouth, or chewable tablets. Tablets which disintegrate in the mouth and chewable tablets are, however, generally not very suitable for active ingredients with an unpleasant taste or for medicinal products with delayed release of active ingredient, because the coatings present for this purpose are unavoidably damaged by the tabletting process or the chewing action. On the other hand, in the case of suspensions, the particles rapidly settle out and can usually be taken only incompletely on drinking, which leads to unacceptable variations in the dose. This problem cannot be eliminated in a satisfactory manner by increasing the viscosity, because an appropriately viscous liquid is drunk only reluctantly.
EP-A 0 313 328 describes effervescent tablets or water-dispersible tables with delayed release of active ingredient, which are obtained by compressing release-slowed particles with an effervescent material or other water-dispersible ingredients and in which the release-slowed particles have a coating containing a water-swellable acrylic polymer and a water-soluble hydroxylated cellulose derivative. Both types of tablets disintegrate in water or in the mouth, and the released particles can be swallowed together with the ancillary substances. However, as a consequence of the disintegration of the tablet, individual particles may remain in the glass or in the mouth, whereby deviations from the required dose may occur, or there is the risk that active ingredients with an unpleasant taste may be released in the mouth. In addition, the release characteristics may be adversely affected, depending on the content of water-soluble hydroxylated cellulose derivative, and the active ingredient may be released too quickly.
In a similar way, EP-A 0 459 695 proposes that active ingredient particles be coated, to mask the taste and/or delay release, with a mixture comprising cellulose acetate and/or cellulose acetate butyrate and hydroxypropylcellulose, although the coated particles are preferably compressed to a chewable tablet. However, these have the disadvantage—as do the aforementioned effervescent tablets and water-dispersible tablets—that the release-slowing coatings or taste-masking masking coatings are partly damaged by the tabletting process, whereby the release characteristics are altered in an unwanted manner, or active ingredients with an unpleasant taste may be released in the mouth, which may lead to the patient refusing the product.
By contrast, WO-A 93/01800 recommends coating microgranules of a bioactive substance (in particular a protein) and a weak base only partly with a material which delays release in the mouth and in the stomach, and mixing the partly coated microgranules with a particle size of from 50 to 500 &mgr;m with an acidifier which yields a pH of from 1.5 to 6 in solution, and with a gel-forming agent. The only partial enteric coating is intended to ensure, together with the pH buffering, that inactivation of the bioactive substance is avoided and, on the other hand, gradual release in the small intestine is ensured.
Pellets or granule particles with a taste-masking coating are also reported in WO-A 91/16043. The coated particles can be packed into sachets together with a polymer (xanthan gum), sweeteners and flavourings. In a similar way, BR-A 9 403 617 further recommends that medicinal products with an unpleasant taste be produced in the form of micropellets with a natural or synthetic coating, and these be mixed with thickeners, sweeteners, flavourings and colours.
By contrast, EP-A 0 662 320 describes a mixture of up to 40% by weight of a medicinal product which can be administered orally, at least 3% by weight of a gelling agent such as pregelatinized starch and up to 5% by weight of a binder as dry gel composition, which is intended on mixing with twice to fifteen times the amount of water to yield a homogeneous gruel-like gel. In the case of bitter active ingredients, it is recommended additionally to use a masking agent such as propylene glycol, glycerol or polyethylene glycol or a taste improver such as potassium glutamate or sodium inosinate or—alternatively—to powder the active ingredient and coat with a masking agent.
U.S. Pat. No. 4,882,169 proposes coated pellets with a diameter of from 0.2 to 3.0 mm which form a completely homogeneous dispersion in water and which have a core containing microparticles of at least one pharmaceutically active substance, where appropriate one or more release-controlling or taste-masking coatings and a swellable outer layer. The latter contains a swellable polymer, preferably guar gum. Since the swellable materials rapidly swell and disintegrate in water, they must be sprayed with an adhesive solution so that they adhere to the pellets. The coated pellets are packed together with guar gum granules and flavourings into sachets from which they can be removed and dispersed in water.
U.S. Pat. No. 5,288,500 likewise proposes combining a multiplicity of active ingredient-containing particles, which can preferably be coated with a diffusion-controlling layer and have a diameter of from 0.05 to 7 mm, with a gelling or swelling agent. The latter can be mixed with the active ingredient-containing particles, be present in a coating, be added to the active ingredient-containing particles before mixing with an aqueous vehicle, or be dispersed in an aqueous vehicle to which the active ingredient-containing particles are added. The proposed formulation is dispersed in an aqueous vehicle and is intended to form a smooth surface around each dispersed particle, whereby irregularities on the surface of the particles are to be masked and adhesion of the particles to the vessel or to the oral mucosa is to be prevented.
Suitable gelling or swelling agents for the formulations proposed in U.S. Pat. No. 5,228,500 are substances, especially hydrophilic polymers, which form colloidal dispersions, sols or suspensions in an aqueous medium. They are employed in an amount which is sufficient to mask the irregularities on the surfaces of the dispersed particles, but is not so large that the dispersibility in an aqueous vehicle might be adversely affected. If required, the viscosity in the immediate vicinity of the dispersed particles can be influenced by salt formation, chelate formation, changing the polarity and the like. However, the intention is to avoid an almost solid gel being formed by the complete formulation. The components of the formulation can be kept separate until administered or be packed together in sachets or processed to tablets or capsules; for oral administration, they are dispersed together in an aqueous vehicle.
The formulations described in WO-A 91/16043, BR-A 9 403 617, EP-A 0 662 320, U.S. Pat. Nos. 4,882,169 and 5,288,500 are taken together with an aqueous vehicle in which they are dispersed before the administration. The formulations disintegrate into the individual particles therein, which means that quantitative intake is no longer ensured as a rule. This is true even if the dispersed particles—as in the case of the fo

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