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Spheroids, preparation method thereof and pharmaceutical compositionsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or Pills, Sustained Or Differential Release Type, Layered Unitary Dosage FormsSpheroids, preparation method thereof and pharmaceutical compositions description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060165794, Spheroids, preparation method thereof and pharmaceutical compositions. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] The present invention relates to gastroresistant spheroids coated with a flexible and deformable film, and to multiparticulate tablets comprising said spheroids. [0002] The present invention further extends to the method of preparing such enteric spheroids and to the multiparticulate tablets comprising these spheroids. [0003] The present invention concerns, finally, a new use of a mixture of mono-, di- and triglycerides and of polyethylene glycol monoester and diester. [0004] By spheroids are meant spherical units whose size can vary from 0.1 mm to 2 mm, preferably from 0.1 mm to 2 mm. [0005] The enteric coating allows the core comprising the active principle to remain intact during the residence time in the stomach, of approximately two hours, in a medium whose pH is approximately between 1 and 3. Once inside the small intestine, comprising the duodenum, jejunum and ileum, the enteric coating will dissolve rapidly in a medium whose pH is greater than 4.5 and increases steadily up to a pH of approximately 7.2 in its distal part. [0006] The prior art includes numerous examples of multi-particulate tablets comprising coated granules. [0007] However, it has been shown that the film formers commonly used to coat granules are unable to absorb, normally, the mechanical stresses which are applied in the course of tableting (International Journal of Pharmaceutics, No. 143, 13-23, 1996). [0008] The tableting of coated granules is a delicate operation, altering the structure of the coating film by the appearance of fissures or by rupture; it may cause complete or partial loss of the properties of the film. [0009] The fissuring of granules irreversibly alters the release profile of the active principle or principles they contain. [0010] Films composed solely of enteric polymers or copolymers such as Eudragit.RTM. L30D have very mediocre mechanical properties, such that they are not resistant to tableting. [0011] One alternative may consist of the addition to the enteric film of other polymers endowed with mechanical properties which render them suitable for tableting. [0012] The document Drugs made in Germany 37, No. 2 (1994), p. 53 teaches that it is possible to combine Eudragit.RTM. L30D and Eudragit.RTM. NE30D to give multi-particulate tablets comprising said coated particles. Example III, however, shows that this approach does not work for all active principles. [0013] So as to preserve the characteristics of the coating film of the granules after tableting, another solution consists in diluting the granules with auxiliary substances, whose role is to absorb the physical stresses of tableting (binders) and to allow the breakdown of the tablet (disintegrants) in a liquid medium, i.e., in aqueous solution or in the digestive fluid. [0014] International application WO 96/01624 (Astra Zeneca) relates to a multiparticulate tablet comprising gastroresistant microgranules, wherein the proportion of said granules within the tablets is less than 75% by weight, preferably less than 60% by weight, relative to the total weight of the tablet, the remainder being a diluent which protects the granules. In the examples of the application, the proportion of enteric granules does not exceed 33% of the total weight of the tablet. [0015] The addition of these auxiliary substances makes these forms not very suitable when the dosage is high, complicates the process by adding mixing steps, and also increases the unit cost of the formulation. [0016] International application WO 02/19991 (Rohm) relates to a multiparticulate tablet and gastroresistant micro-granules, said microgranules comprising an enteric coating of a copolymer of methacrylic acid and propylene glycol. The proportion of said granules within the tablets is between 35% and 90%, preferably 40% to 70% by weight, relative to the total weight of the tablet, the remainder being a binder. [0017] The Applicant's International application WO 99/26608 relates to spheroids which comprise one or more active principles and are tabletable directly without the addition of a substantial part of an auxiliary substance. [0018] These spheroids are composed of a core comprising the active principle, said core being covered with a first layer comprising at least one thermoplastic excipient whose consistency is pasty to semisolid at a temperature of the order of 20.degree. C. and whose melting temperature is between approximately 25.degree. C. and approximately 100.degree. C., the resulting spheroid being itself coated with a flexible and deformable film based on a polymeric material. [0019] Although particularly suited to the preparation of gastroresistant forms, these spheroids exhibit the disadvantage of being composed of a plurality of successive layer of different compositions, entailing a lengthy and constricting preparation process, and of using thermoplastic excipients whose pasty to semisolid consistency at 20.degree. C. makes them not very easy to handle. [0020] There is therefore particular interest in obtaining gastroresistant spheroids devoid of any protective layer composed of thermoplastic excipients but nevertheless resistant to the stresses of tableting, such that it is possible to preserve the property of gastroresistance, and to do so without any need to add substantial amounts of auxiliaries. [0021] The Applicant has realized that, in contrast to what is taught by the prior art, it is entirely possible to improve the mechanical properties of enteric films sufficiently to allow the production of spheroids coated with such a film, of sufficient flexibility and deformability for them to be tableted directly without the addition of more than approximately 5% by weight of auxiliary substances. [0022] The use of Gelucire.RTM. in enteric polymer-based coatings makes it possible to improve, surprisingly, their mechanical properties in such a way that the spheroids coated with this coating composition may subsequently be tableted directly without the addition of more than approximately 5% by weight of auxiliary substances. [0023] The present invention provides a directly tabletable gastroresistant spheroid, characterized in that it comprises: [0024] a core comprising one or more active principles and at least one binder, directly coated with [0025] a flexible and deformable film comprising an enteric polymer and a mixture of saturated and/or unsaturated polyglycosylated glycerides whose fatty acids contain at least 8 carbon atoms, [0026] a water-dispersible outer layer comprising at least one disintegrant. [0027] By "directly tabletable" is meant that the spheroids can be tableted in the form of multiparticulate tablets without any need to add more than approximately 5% of auxiliary substances at the time of tableting. Continue reading about Spheroids, preparation method thereof and pharmaceutical compositions... Full patent description for Spheroids, preparation method thereof and pharmaceutical compositions Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Spheroids, preparation method thereof and pharmaceutical compositions patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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