For the symptomatic therapy of any other form of colitis, both the oral and rectal applications can be chosen for the therapeutic modification of the intestinal
10 จุลินทรีย์ประจำถิ่น. The oral applicationis preferred for the prophylaxis of the คาร์ซิโนมาของโคลอน, in particular in the case of ลำไส้ใหญ่อักเสบเป็นแผลเรื้อรัง, and for the therapy and/or prophylaxisof other diseases which partially or substantially result from changes in the จุลินทรีย์ประจำถิ่นในลำไส้ and/or an ปฏิสัมพันธ์ที่บกพร่อง between จุลินทรีย์ประจำถิ่นในลำไส้ and the intestines.
For oral การให้, particular รูปแบบขนาดยา that control and/or delay the release of
15 the สารออกฤทธิ์due to special galenics (so-called การปลดปล่อยแบบมีการควบคุม,slow release or การปลดปล่อยแบบชะลอ forms) are particularly suitable. Such รูปแบบขนาดยา may be simple tablets and also coated tablets, e.g., film tabletsor dragees. The tablets are usually round or biconvex. Oblong tablet forms, which allow the tablet to be separated, are also possible. In addition, แกรนูล, spheroids, pellets or microcapsules are possible, which are
20 filled in sachets or capsules,where appropriate.
The term "การปลดปล่อยแบบชะลอ" relates ที่ควรใช้คือ to a สูตรผสมทางเภสัชกรรม that releases the ส่วนผสมออกฤทธิ์safter a period of delay. In certain embodiments, the delay is sufficient for at least a portion of the สารออกฤทธิ์ in a สูตรผสม to release in the ลำไส้เล็กส่วนล่าง(e.g., ไอเลียมส่วนปลาย) and/or โคลอน.
25 The term "controlledrelease" refers ที่ควรใช้คือto a สูตรผสมทางเภสัชกรรม or component thereof that releases, or delivers, one or more ส่วนผสมออกฤทธิ์s over a prolonged period of time (time-dependent release) and/or under certain physiological conditions (e.g., pH-dependent release). In certain embodiments,the period of time or the release according to physiologicalconditions (e.g., pH) is sufficient for at least a portion of the
30 สารออกฤทธิ์ in a สูตรผสม to release in the ลำไส้เล็กส่วนล่าง (e.g., in the ไอเลียมส่วนปลาย) and/or โคลอน
The retardation and/or delayed release and/or controlled release is advantageously achieved, e.g., by coatings which are resistant to gastric juice and dissolve depending on the pH, by means of microcellulose and/or multi matrix (MMX) technologies, by using different carrier matrices or a combination of these techniques. Examples include film
5 coatings which contain acrylic and/or methacrylate polymers in various ของผสมs for
controlled and/or การปลดปล่อยแบบชะลอ. For example, the สารออกฤทธิ์(s)can be contained in a conventional matrix of microcrystallinecellulose or gelatin or with MMX technology, which is coated with a material, which provides the การปลดปล่อยแบบชะลอ of the active sub• stance(s). An สารออกฤทธิ์ can be administered in large-volume capsules (e.g.,
10 gelatin capsules having a content of 0.68 ml), which are coated by means of known methods. Suitable coating agents are water-insoluble waxes, such as carnauba wax, and/or polymers,such as poly(meth)acrylates[e.g., the poly(meth)acrylateproduct portfolio with the trade name Eudragit®, in particular Eudragit® L 30 D-55 (an aqueous dispersion of anionic polymers with methacrylicacid as a functionalgroup), Eudragit® L 100-55
15 (which contains an anionic copolymer based on methacrylic acid and ethyl acrylate), Eudragit® L 100 or L 12,5 or S 100 or S 12,5 (anionic โคโพลิเมอร์based on methacrylic acid and methyl methacrylate), or Eudragit® FS 30 D (an aqueous dispersion of an anionic copolymer based on methyl acrylate, methyl methacrylate and methacrylic acid); Evonik Industries AG, Essen, Germany) and/or water-insoluble celluloses (e.g., methyl
20 cellulose, ethyl cellulose). Where appropriate, water soluble polymers (e.g., polyvinylpyrrolidone), water-soluble celluloses (e.g., hydroxypropylmethyl cellulose or hydroxypropylcellulose), สารก่ออิมัลชัน and stabilisers (e.g., polysorbate 80), polyethylene glycol (PEG), lactose or mannitolcan also be contained in the coating material.
For example, a combination of Eudragit® S and L compounds (e.g., Eudragit® LIS 100)
25 effects a การปลดปล่อยแบบมีการควบคุม of the สารออกฤทธิ์ according to the การประดิษฐ์ at pH >
6.4, which occurs in the ไอเลียมส่วนปลาย. Further uses of Eudragit® preparations and mixtures thereof (FS, L, S and R compounds) are also conceivable for the packaging of an สารออกฤทธิ์, and therefore a topical use in selected portions of the entire gastrointestinal tract can be achieved by การปลดปล่อยแบบมีการควบคุม at certain pH values. A systematic
30 study of enteric targeting with hydroxypropyl methylcellulose(HPMC) capsules and more
recently developed Eudragit® polymers was published by Cole et al. in 2002 (Int. J.
Pharm. 231 :83).
The องค์ประกอบทางเภสัชกรรม can also contain further pharmaceutical excipient substances, such as binders, fillers, glidants,