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(12) Patent Application Publication (10) Pub. No.: US 2004/0058896 A1 Dietrich Et Al

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US 200400.58896A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0058896 A1 Dietrich et al. (43) Pub. Date: Mar. 25, 2004 (54) PHARMACEUTICAL PREPARATION (30) Foreign Application Priority Data COMPRISING AN ACTIVE DISPERSED ON A MATRIX Dec. 7, 2000 (EP)........................................ OO126847.3 (76) Inventors: Rango Dietrich, Konstanz (DE); Publication Classification Rudolf Linder, Kontanz (DE); Hartmut Ney, Konstanz (DE) (51) Int. Cl." ...................... A61K 31156; A61K 31/4439 (52) U.S. Cl. ........................... 514/171; 514/179; 514/338 Correspondence Address: (57) ABSTRACT NATH & ASSOCATES PLLC 1030 FIFTEENTH STREET, N.W. The present invention relates to the field of pharmaceutical SIXTH FLOOR technology and describes a novel advantageous preparation WASHINGTON, DC 20005 (US) for an active ingredient. The novel preparation is Suitable for 9 producing a large number of pharmaceutical dosage forms. (21) Appl. No.: 10/433,398 In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix com (22) PCT Filed: Dec. 6, 2001 posed of one or more excipients Selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid (86) PCT No.: PCT/EPO1/14307 eSter. US 2004/0058896 A1 Mar. 25, 2004 PHARMACEUTICAL PREPARATION 0008 Further subject matters are evident from the claims. COMPRISING AN ACTIVE DISPERSED ON A MATRIX 0009. The preparations for the purpose of the invention preferably comprise numerous individual units in which at least one active ingredient particle, preferably a large num TECHNICAL FIELD ber of active ingredient particles, is present in an excipient 0001. The present invention relates to the field of phar matrix composed of the excipients of the invention (also maceutical technology and describes a novel advantageous referred to as active ingredient units hereinafter). The active preparation for an active ingredient. The novel preparation is ingredient is preferably essentially uniformly dispersed, in Suitable for the production of a large number of pharmaceu particular homogeneously dispersed or dissolved, in the tical dosage forms. excipient matrix. A preparation preferably comprises micro Spheres. BACKGROUND ART 0010. The preparations of the invention are distinguished 0002. In order to achieve particular properties of a dosage in particular by high Stability, a release of active ingredient form, Such as, for example, taste masking in the case of which can be controlled by the particle size and composition active ingredients with an unpleasant taste, resistance to of the matrix, good flow characteristics, good compressibil gastric juice in the case of acid-labile active ingredients or ity and by a uniform delivery of active ingredient. In the case controlled release of an active ingredient, normally active of acid-labile active ingredients it is moreover possible to ingredient pellets are provided with an appropriate func achieve, through choice of the matrix excipients, an acid tional coating. If Such coated pellets are then further pro resistance So that it is possible in the case of oral forms to cessed to dosage forms, for example shaped to tablets by dispense with an acid-resistant coating (enteric coating). In compression with excipients, there is a risk that the coating the case of active ingredients which have an unpleasant taste is damaged and thus the functionality is at least partly lost or, for example, Show a local anesthetic effect in the mouth again. after administration, it has been observed that an unpleasant taste of the active ingredient can be masked, and anesthetic DESCRIPTION OF THE INVENTION effects in the mouth can be avoided, by preparations of the invention. It is particularly worthy of mention that the 0003. It is an object of the present invention to provide a preparations of the invention can be further processed to a preparation for active ingredients which is able to retain a large number of pharmaceutical dosage forms without desired functionality and can be further processed to a large thereby losing a given functionality (Such as taste masking, number of pharmaceutical process forms with negligible resistance to gastric juice, slowing of release). Thus, for impairment of a given functionality. example, on compression of the active ingredient units of the invention no or negligible loSS of functionality is observed 0004. It has now been found, surprisingly, that this object even if deformation of the active ingredient units occurs. In is achieved by a preparation in which an active ingredient is contrast to this, with conventional pellets, which normally essentially uniformly dispersed in an excipient matrix com have a functional coating (Such as taste masking, resistance posed of one or more excipients Selected from the group of to gastric juice, slowing of release), a certain degree of fatty alcohol, triglyceride, partial glyceride and fatty acid damage to the coating and thus to the functionality is eSter. observed on further processing to dosage forms, for example 0005 The invention therefore relates to a preparation in on compression to tablets. This may also lead in Some cases which an active ingredient is essentially uniformly dispersed to active ingredient being released in an unwanted way. in an excipient matrix composed of one or more excipients 0011. The particle size of the individual units is advan Selected from the group of fatty alcohol, triglyceride, partial tageously less than or equal to 2 mm, preferably 50-800 uM, glyceride and fatty acid ester. particularly preferably 50-700 um and very particularly 0006. It has further been found that particularly advan preferably 50-600 um. Preference is given to microsphers of tageous preparations can be obtained by adding Solid par a particle size of 50-500 um, particularly preferably of affin to the excipient matrix. The invention therefore relates 50-400 lum. Particular preference is given to monomodal further to a preparation in which an active ingredient is microspheres with a particle size of 50-400 um, particularly essentially uniformly dispersed in an excipient matrix com of 50-200 um. posed of at least one Solid paraffin together with one or more 0012 Active ingredients of the invention are, in particu excipients Selected from the group of fatty alcohol, triglyc lar, active pharmaceutical ingredients. Examples of active eride, partial glyceride and fatty acid ester. ingredients which may form part of the preparations of the 0007. The invention further relates to preparations in invention are, in particular, the active pharmaceutical ingre which an active ingredient is essentially uniformly dispersed dients mentioned below: i) in an excipient matrix composed of a mixture comprising 0013 Adrenergics: at least one fatty alcohol and at least one Solid paraffin, ii) in an excipient matrix comprised of a mixture comprising at 0014 apraclonidine; brimonidine; dapiprazole; least one triglyceride and at least one Solid paraffin, iii) In an deterenol; diplivefrin, dopamine; ephedrine, espro excipient matrix composed of a mixture comprising at least quin; etafedrine, hydroxyamphetamine; levonorde one partial glyceride and at least one Solid paraffin or iv) in frin, metaraminol; norepinephrine; oxidopamine; an excipient matrix composed of a mixture comprising at phenylpropanolamine; prenalterol; propylhexedrine; least one fatty acid ester and at least one Solid paraffin. pseudoephedrine. US 2004/0058896 A1 Mar. 25, 2004 0015 Adrenocorticosteroids: levomethadyl acetate hydrochloride; levonantradol; levorphanol, lofemizole, lofentanil oxalate; lorcina 0016 ciprocinonide; desoxycorticosterone acetate; dol, lomoxicarn; magnesium Salicylate, mefenamic deSoxycorticosterone pivalate; dexamethasone add; menabitan; meperidine, meptaZinol, metha acetate; fludrocortisone acetate; flumoxonide, hydro done; methadyl acetate; methopholine; methotrime cortisone hemisuccinate, methylprednisolone prazine, metkephamid acetate, mimbane, mirfenta hemisuccinate, naflocort, procinonide; timobesone nil; molinaZone; morphine Sulfate; moxazocine; acetate; tipredane. nabitan; nalbuphine, nalmeXOne, namoxyrate; nant 0017 Agents to prevent alcohol abuse: radol, naproxen; naproxen; naproXol; nefopam; neX eridine, noracy methadol; ocfentanil; octaZamide, 0018 disulfiram, acamprosate, milnacipran, fome olvanil; OXetorone; oxycodone; oxycodone; oxyc pizole, lazabemide, nadide, nitrefazole, Sunepitron. odone terephthalate; oxymorphone, pemedolac, pen 0019 Aldosterone antagonists: tamorphone; pentazocine; pentazocine; phenaZopy ridine, phenyramidol; picenadol; pinadoline; 0020 canrenoate; can renone, dicirenone; meXrenoate, prorenoate, Spironolactone, epoStane, pirfenidone, piroXicam olamine, pravadoline; prodi meSpire none; OXprenoate, Spirorenone, SpiroXaSone, lidine, profadol; propiram; propoxyphene, pro prorenone, eplerenone. poxyphene napsilate; proxazole, proXorphan; pyrro liphene, remifentanil; Salcolex, Salethamide maleate; 0021 Amino acids: Salicylamide, Salicylate meglumine; Salsalate, Sali cylate; Spiradoline, Sufentanil; Sufentanil; talmeta 0022 alanine; aspartic acid; cysteine; histidine, iso cin; talniflumate; taloSalate; taZadolene; tebufelone; leucine; leucine; lysine; methionine; phenylalanine; tetrydamine; tifurac, tilidine, tiopinac, tonazocine; proline, Serine; threonine, tryptophan; tyrosine; tramadol; trefentanil; trolamine; Veradoline, Verilo Valine. pam; volazocine, Xorphanol, Xylazine, Zenazocine 0023 Active ingredients
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  • Attenuated 5-Hydroxytryptamine Receptor-Mediated Responses in Aortae from Streptozotocin-Induced Diabetic Rats G.M

    Attenuated 5-Hydroxytryptamine Receptor-Mediated Responses in Aortae from Streptozotocin-Induced Diabetic Rats G.M

    Br. J. Pharmacol. (1994), 111, 370-376 '." Macmillan Press Ltd, 1994 Attenuated 5-hydroxytryptamine receptor-mediated responses in aortae from streptozotocin-induced diabetic rats G.M. James, 1W.C. Hodgson, E.A. Davis & 2J.M. Haynes Department of Pharmacology, Monash University, Clayton, Victoria, Australia, 3168 1 This study was designed to examine further the attenuated contractile responses to 5-hydroxy- tryptamine (5-HT) previously observed in aortae from diabetic rats. 2 Cumulative concentration-response curves to 5-HT, and the 5-HT receptor agonists, at-methyl 5-HT (a-Me-5-HT, 5-HT21lc agonist), (± )-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 5-HT21IC agonist) and 5-carboxamidotryptamine (5-CT, 5-HTIA/1B/1D agonist), were examined in endothelium- intact and -denuded aortae from 2-week streptozotocin (STZ)-diabetic and control rats. 3 In endothelium-intact and -denuded aortae from diabetic rats, maximum responses to 5-HT and a-Me-5-HT were significantly reduced compared to those of aortae from control rats. Responses to these agonists were inhibited by the 5-HT21lc receptor antagonist, ketanserin (0.1 jAM). 4 The attenuated responses to 5-HT of aortae from diabetic rats were normalized by chronic insulin treatment of the rats (5 units day-', s.c.), but not by altering the glucose concentration of the bathing fluid. 5 The nitric oxide synthase inhibitor N-nitro-L-arginine (NOLA, 0.1 mM) significantly potentiated responses to both 5-HT and a-Me-5-HT in endothelium-intact aortae. However, the difference between maximum responses of aortae from diabetic and control rats was still evident in the presence of NOLA.