565454 A7 _ B7 五、發明説明（1 ) (讀先閱讀背面之注意事項再填寫本頁) 本發明係關於一種包括一或多種多元醇的組成物，其 具有增強的變形力而且可以經處理而得到具有改良性質的 錠劑、緻密錠劑或硬糖（boiled sweets)。 很多的公告案和專利申請案揭示用來製造錠劑的組成 物’緻密錠劑或硬糖（EP-A-0 240 773，EP-A-0 462 066 或DE-A 1 -43 1 6 537 )，其中所有種類之生理學地可容忍的 辱· 經濟部智慧財產局員工消費合作社印製 物質係當做製藥活性化合物或調味料的賦形劑使用。這些 包括，尤其是，纖維素衍生物及其鹽類，醣類，糖類，例 如N -乙烯基吡咯烷酮/醋酸乙酯共聚物，聚乙烯基吡咯 烷酮，聚乙烯醇，聚丙烯酸及其鹽類，聚異丁烯酸及其鹽 類等水溶性聚合物，例如聚氧化乙烯，聚氧化丙烯還有乙 烯和氧化丙烯的共聚物等聚氧化烴烯，例如藻酸，其鹼金 屬和銨鹽，角叉菜素（carrageenans)，半乳甘露聚糖，黃 蓍，瓊脂，阿拉伯膠，黃原膠等多醣，例如去乙醯殻多醣 等幾丁質衍生物，例如羧基甲基戊基果膠鈉等果膠和澱粉 類，還有這些水溶性聚合物的混合物。在此水溶性係指在 2 0 °C下至少〇 · 5克，較佳2克的聚合物可以視需要地 以膠體的形式溶解1 0 0克水或溶解於丨〇 〇克水而形成 凝膠。 在製備錠劑，經塗覆的錠劑，口含錠或硬糖時，賦形 劑基質的良好水溶解度對於生物有效性和迅速吸收而言是 特別地重要。 水溶解度對嘴裡愉快的味道和感覺而言也是不可否認 地重要，但是表面組成物和在吸的時候的味道感覺也扮演 本紙張尺度適用中國國家標準（CNS ) A4規格（210X 297公釐） -4 ~ 565454 A7 B7 五、發明説明（2 ) (請先閲讀背面之注意事項再填寫本頁) 相當重要的角色。在那些已知的賦形劑材料的情況裡，無 法沒有問題地提供這樣的功效。雖然一方面具有布好的味 道，但是另一方面因其物理性質而產生不規則顆粒表面， 或因其加工性差而產生不均勻且可能是尖銳邊緣的表面。 通常，製備預混物以使所加入之活性化合物均勻地分 佈在賦形劑基質裡，將各種不同的組份彼此一起融化，或 將活性化合物藉由在已存在的聚合物熔融液裡揉合而混合 。這些方法裡的問題是一致的劑量，均勻混合和連續的程 序。 爲了以錠劑，經塗覆的鍵劑或口含錠形式服用製藥活 性化合物以保証劑量不變，活性化合物必須均勻地分散在 賦形劑基質裡。當使用溶解性差的活性化合物時，這是一 個特別的問題。 經濟部智慧財產局員工消費合作社印製 因此，本發明之目的一方面係提供一種組成物，其可 以在某溫度的範圍裡小心地處理以得到所需的產物，也就 是得到錠劑，緻密錠劑或硬糖，其中所加入的活性化合物 不受損害。本發明之目的也提供一種製法，其可以連續地 進行，藉此可以製得具吸入期間也保有之光滑表面而且也 具有口中愉悅味道和感覺的錠劑，緻密錠劑或硬糖，及製 得活性化合物和包含在其中之調味料的均勻分散液。本發 明另一目的係提供一種組成物，其可以用於本發明之方法 而且’由於變形力持久，所以可以利用簡單的方式處理而 得到所需的產物。 該目的係藉由包括先前共噴覆之多元醇的組成物，特 本紙張尺度適用中國國家標準（CNS ) A4規格（2)0X 297公釐） -5 - 565454 A7 B7 經濟部智慧財產局員工消費合作社印製 五、發明説明（3 別XE藉由包括一或多種選自一群包括木糖醇，山梨糖醇或 ?L m ( lactitol )，麥芽醇（maititol ) ，丁四醇或甘露醇等 多元醇和視需要包含選自一群包括澱粉，纖維素等醣類， 而且依產物而定視需要地包含一或多種活性化合物，一或 多種著色劑，一或多種天然增甜劑，一或多種合成增甜劑 ’酸化劑’調味料’香料和一般助劑的組成物而達成。 該目的也藉由製造塑膠成型或未成型材料的方法而達 成，其中主要包括一或多種多元醇的組成物係在3 〇到 1 7 0 °C的溫度範圍內擠型並視需要地成型。尤其，該目 的係藉由先前共噴覆的組成物而達成，其中將該組成物擠 型，然後將依此方式所得之擠出物在接續的成型單元裡進 (請先閲讀背面之注意事項再填寫本頁) 一步地加工 爲了製 的混合物擠 可以藉由砑 表面之等體 加工而得到 性化合物和 實際均勻之 之產物方面 由實驗 糖的物質， 質，可以視 醣類之組成 造口含錠，緻 型並在低於2 光機壓光而分 積仍可成形的 錠劑。也已知 其他的添加劑 活性化合物混 ，仍然有問題< 顯示，以山梨 例如麥芽醇， 需要地另外包 物可以利用簡 密錠劑或硬糖，已知將個別組份 0 0的溫度下彼此融化。擠出物 離或使用旋轉刀而粉碎成具固體 塊體，其可以直接接著利用壓縮 在擠型期間經由適當裝備加入活 。然而，即使是目前在爲了獲得 合物及爲了獲得具實際平滑表面 糖醇，木糖醇，乳醇或其他類似 丁四醇，甘露醇或其他物質爲底 含選自一群包括澱粉和纖維素等 單的方式成型而獲得可以更容易 訂 # 本紙張尺度適用中國國家標準（CNS ) A4規格（2!0X297公釐） -6 - 565454 A7 B7 五、發明説明（4 ) 地加工而且加工時間長的擠出物。包含這些多元醇混合物 的組成物可以依相同的方式及容易地加工。 (請先閱讀背面之注意事項再填寫本頁) 傾發現木糖醇含量高的多元醇材料可以特別容易地加 工。那些材料特別具有非常良好的加工性質，該材料的組 份在依專利申請案DE 19617487.2描述的共噴覆方法擒型之 前已經預先處理，並且一起加工而得到細分的粉末。濟型 所用的該粉末不但是二種或二種以上不同粉末的混合物， 而且獲得其中各別顆粒由於共噴覆而構成各別組份之混合 物的粉末，即混合的結晶。與所用的粉末混合物比較，這 些粉末具有較低的熔點，而所得的塑膠材料也可以變形一 段長時間並在擠出之後迅速地變形。該變形力可以進一步 地藉由添加熟習此項技藝者所知之適當的結晶阻滯劑而增 強，該結晶阻滯劑可以在共噴覆期間加入。有利的是，在 以本發明共噴覆多元醇或多元醇混合物爲底質的組成物裡 ，可以省略在其它情況裡必需加入的塑化劑或流動調節劑 〇 經濟部智慧財產局員工消費合作社印製 由於個別組份的共噴覆乾燥，獲得當在共噴覆方法裡 形成及收集時可以連續擠型的粉末。共噴覆和擠型加工階 段之間或期間，活性化合物，添加劑和一般製藥助劑，例 如塡充劑，潤滑劑，脫模劑，流動調節劑，塑化劑，著色 劑，安定劑，酸化劑，調味料和香料可以加入粉末混合物 〇 通常可以加入的塡充劑係爲熟習此項技藝者所知，例 如鎂，鋁，矽和鈦的氧化物，但是還有其他的物質。 本紙張尺度適用中國國家標準（〇^)六4規格（2]0><297公|) -7- 565454 A7 B7 五、發明説明（5 ) (請先閲讀背面之注意事項再填寫本頁) 在某些情況裡必要時，可以加入流動調節劑，例如長 鏈脂肪酸的單-、二-和三甘油酯，蠟，巴西棕櫚蠟或卵 磷脂。然而，一般而言，這些添加劑不爲本發明的組成物 所需。 除了低分子量聚烯氧化物，例如聚乙二醇、聚丙二醇 和聚伸乙基丙二醇之外，多元醇，例如丙二醇、甘油和季 戊四醇，還有二乙基硫代丁二酸鈉，甘油的單一、二一和 三醋酸酯和聚乙二醇硬脂酸酯也適合當做塑化劑，其可以 在必要時加入。 至於潤滑劑，可以使用鋁或鈣的硬脂酸鹽，而且也可 以使用滑石或矽酮。 至於著色劑，可以同樣地使用天然著色劑，及所有允 許當做食品添加劑的著色劑和顏料。 可用的安定劑是抗氧化劑，自由基煉淸劑，抗微生物 化學浸蝕的安定劑和光安定劑。 經濟部智慧財產局員工消費合作社印製 因組成物而定，所有的添加劑可以依熟習此項技藝者 的所知的濃度精確地加入，以致於達成添加劑的各別所需 效應。 在擠出期間可以加入所有的添加劑。然而，在組成物 的共噴覆期間將可溶性添加劑加入產物裡，對均勻的分散 液而言是有利的。不能溶解的添加劑可以利用共噴覆方法 與所得的粉末混合，及適時地可以將另一個組份在擠型之 前機械地混合。 由於先前的共噴覆處理，獲得以高通過料量擠型的混 本紙張尺度適用中國國家標準（CNS ) A4規格（2l0x：297公楚) -8- 565454 A7 B7 五、發明説明（6 ) (請先閱讀背面之注意事項再填寫本頁) 合物，而得到可變形的材料。該情況裡的這些粉末混合物 因熔點較低和可塑性改良而需要較低的能量輸入，明顯地 由所用之粉末的改良結構而產生。 因所用的多元醇或多元醇混合物而定，擠型期間因此 需要某能量輸入。這因如視如上所述之獲得多元醇混合物 的方式，即簡單的混合或共噴覆方式而定。能量輸入可以 藉由擠型方法及在此施加的力量而機械地進行。然而，其 也可以藉由另外加熱而進行。在此有特定的差異，在共噴 覆之多元醇組成物的情況裡所需的能量最低。本發明的多 元醇混合物可以在3 0到1 7 0 °C，特別是4 0到1 1 0 °C的溫度範圍擠出。對於共噴覆獲得的混合物而言，已經 證明能量輸入導致產物ίέ度大約7 0到1 1 0 °C的條件是 特別地適合。 經濟部智慧財產局員工消費合作社印製 然而共噴覆之多元醇混合物可以利用簡單的方式擠出 ，但是不可能將機械混合的多元醇組合擠出而得到均勻的 產物，因爲各種多元醇具有不同的熔點。尤其，包含甘露 醇的非共噴覆混合物需要高能量輸入，不然的話則獲得甘 露醇結晶同樣出現之粗粒擠型產物。對於包含甘露醇的混 合物而言，因此建議先前進行共噴覆。經由後來的擠出， 導致出口位置處產物溫度高達1 1 〇 °C的能量輸入，在成 型之後獲得具有平滑表面和良好吸食行爲的產物。如果其 中含有至少二種數量高達1 〇重量％另外的多元醇，則由 本發明方法加工之含甘露糖醇的混合物具有特別良好的產 物性質。 本紙張尺度適用中國國家標準（CNS ) A4規格（210X 297公餐） - 9- 565454 A7 B7 五、發明説明（7 ) (請先閱讀背面之注意事項再填寫本頁) 經由比較實驗，傾發現先前共噴覆之多元醇組成物可 以加工，得到具有比用簡單混合組成物擠型的情況更平滑 表面之擠型產物。如果，例如將市售可得的噴乾山梨糖醇 (K a 1· i ο η I n s t a n t @ )直接在與組成物的其它組份簡單混合一 產物在溫度約1 0 0 t出現-和接著成型之後擠出，則獲 得具有比使用對應之共噴覆組成物的情況更粗糙表面的產 物。如果，然而，以相同方式處理另外其它類似之市售可 得的結晶山梨糖醇（Neosorb®)，獲得具有平滑表面，額外 具有良好吸食行爲的擠出物。然而，在該情況裡，必需非 常高的能量輸入，而且不能夠任意地選擇厚桿直徑。 因混合物的組成物及其過去情形而定，選擇某擠出方 法。藉由使用雙螺旋式擠壓機或塑化螺旋機-其中利用螺 旋輸入能量-並適時地另外加熱的方式進行擠型。然而， 另外可以使用壓縮或運輸螺旋加熱擠型。至於擠型期間的 可變參數，可以改變，尤其改變產物輸入量，螺旋的輸送 速率，出口噴嘴的大小和溫度。 經濟部智慧財產局員工消費合作社印製 因爲其加工性質良好，所以那些經由本發明方法先前 共噴覆所得的材料可以經由比爲應產物一般所用更大的中 空直徑而壓縮得到良好的結果。藉此獲得較高的產物通過 料量。 選自一群包括木糖醇，山梨糖醇，乳醇，麥芽醇，丁 四醇和甘露醇，其混合物或與其它多元醇的混官物的共噴 覆多元醇可以利用本發明之方法加工而得到良好結果，將 混合物裡的這些多元醇其中一或多種擠型處理，得到塑膠 本纸張尺度適用中國國家標準（CNS ) A4規格（2丨0X 297公釐） -10- 565454 A 7 B7 五、發明説明（8 ) (請先閲讀背面之注意事項再填寫本頁) 成型或未成型材料。包含多元醇數量比爲50:50到 99:1 ，特別是65:35到98:2之山梨糖醇和木 糖醇的組成物已經證明特別適合。如果包含山梨糖醇，木 糖醇和甘露醇的數量比爲9 〇 : 1 : 9到7 0 : 2 9 : 1 ’特別是8 2 : 9 : 9，則包含三種多元醇山梨糖醇，木 糖醇和甘露醇在混合物裡的組成物具有特別好的性質。添 加劑的所有種類可以在擠型前加入該組成物的多元醇混合 物中。如此的添加劑可以是，例如一或多種活性化合物， 一或多種食品添加劑，但可以是一或多種天然及/或一或 多種合成增甜劑。這些添加劑可以單獨加入或一起加入。 也可以另外加入製藥或食品工業裡的加工助劑和添加劑。 可以使用現代計量天平，如EP-B1-0 337 256所描述，將這 些添加劑等量地加入，以致於擠出總是均勻的組成物。 從本發明多元醇組成物擠出後獲得之塑膠成型或未成 型材料可以藉由食品或製藥工業一般所用的成型單元，例 如刻鑿滾筒或自動旋轉機器，進一步地加工。 經濟部智慧財產局員工消費合作社印製 在與由已知方式製備的產物比較之下，從本發明材料 製備的產物，例如錠劑，緻密錠劑，口含錠或硬糖，具有 在使用期間，尤其是吸食時可以保有之明顯更平滑的表面 。在口中溶解的更均勻得多，本來非常平滑的表面也仍留 存。銳利邊緣因這些改良的性質而大量地減少。這些有利 的性質特別地在各別組份在擠型前已經與彼此混合的產物 中更彰顯。當倂用之活性化合物，調味料等曝於較低的溫 度而擠型桿仍然可變形一段比一般更長的時間時；即所得 本紙張尺度適用中國國家標準（CNS)A4規格（2丨0X 297公釐） -11 - 565454 A7 B7 五、發明説明（9 ) 之產物在擠出之後額外地保有塑膠軟性及可變形大約1到 2分鐘，共噴覆多元醇組成物因其熔點低而也特別地極適 合用於本發明的擠型處理。此外，在與一般所得之擠出物 比較之下，桿直徑係視根據本發明擠出物的明顯及良好塑 膠行爲而定，選擇性最大。這些組成物在擠出和成型之後 也顯示比迄今已知更好的吸食行爲。 與傳統的方法比較之下，本發明的方法具有許多的優 點。這些優點包括，由其是連續製備各別組份均相等不變 之粉化組成物的可能性，其直接地在較溫和的條件下擠型 ，得到塑膠成型或未成型材料而且可以接著加工成型而得 到錠劑，緻密錠劑，口含錠或硬糖。本發明組成物的特別 優點是所得的產物更平滑得多的表面，該表面在吸食期間 也仍留存。此外，有利的改良係藉由先前共噴覆本發明的 多元醇，及適時地共噴覆甘露醇而達成。尤其已知的制酸 劑裡所產生之含白堊的味道，係被本發明的組成物隱蓋。 當所製得的錠劑由於所用的賦形劑物質而迅速地溶解時， 合倂的活性化合物的生物有效性和吸收性因此也增加，而 且因爲其味道愉快而可以沒有問題地吸食。如果像是在例 如包含止痛藥的情形裡需要迅速的活性，則這是很重要的 〇 必要時，根據本發明製得的錠劑也可以覆上一般的塗 層，以改良外表或達到遲延活性化合物釋放之目的b如果 錠劑係藉由一種已知的技術以封閉細胞孔形式製得，以漂 浮在胃裡及藉此停留較久的話，則對錠劑遲滯活性化合物 本紙張尺度適用中國國家標準（CNS ) A4規格（2]OX 297公楚) ' -12- (請先閱讀背面之注意事項再填寫本頁) 訂- 舞 經濟部智慧財產局員工消費合作社印製 565454 A7 B7 五、發明説明（1〇 ) 釋放而言是有利的。 (請先閱讀背面之注意事項再填寫本頁) 本發明裡的製藥活性化合物係指所有如果其不在加工 條件下分解，則具有醫藥作用及最低可能副作用的物質。 每劑量單位和濃度的活性化合物數量可以是因活性及釋放 速率而在大範圍裡改變。如此活性化合物的濃度可以是 〇· 1到9 5，較佳爲5到8 0。活性化合物也可以組合 使用。本發明的組成物較佳地適合於倂用需要其立即生物 有效性及與其它成分一起得到有利味道的活性化合物。如 此的活性化合物可以是制酸劑，止痛藥，鎭靜劑，放鬆劑 或其他的製藥活性化合物。本發明裡的活性化合物也是可 食的生理物質，例如維生素，礦物和微量元素。 下列實施例係用來說明本發明，但並非限制其範圍。 實施例 組成物 a 機械混合多元醇組成物 b 噴乾的山梨糖醇 經濟部智慧財產局員工消費合作社印製 c P3〇〇山梨糖醇 d 結晶性山梨糖醇 本纸張尺度適用中國國家標準（CNS ) A4規格（210X 297公楚） -13- 565454 五、發明説明（1 經濟部智慈財產局員工消費合作社印製 kl B7 實施例 1 2 3 4 5 6 7 8 組成物 a b C b b b d d 通過料量 17 15 14 14 14 17 17 17 [公斤/小時] 溫度Eft] 90 100 92.5 92.5 101 103 壓力1[巴] 7 16 2 3 3 2 0 9 a s/i [°c] K K K K K K K K t2 S/l [°C] 90 70 110/120 80 77 88 130 115 t3 S/l [°C] 90 50 110/120 80 77 90 130 115 多孔板 1x4.6 2x2 1x4.5 1x4.5 1x4.5 12x9 12x9 1x4.5 OV OV 鐵浮龍 鐵浮龍 註 以20巴 平滑 產物柔軟 相當平滑 溫度最佳 非常平滑 易碎，開 粗糙的 的水開 的表 ，擠出物 的擠出物 化的實驗 的擠出物 孔，沒有 表面， 始，用小 面 斷裂 ，輕微的 ，良好的 擠出物 粗糙度 噴嘴產 震動 表面情形 因溫度 生較大 而定 的壓力 (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準（CNS ) Λ4規格（2]0X 297公釐） -14 -565454 A7 _ B7 V. Description of the invention (1) (Read the precautions on the back before filling this page) The present invention relates to a composition comprising one or more polyols, which has enhanced deformability and can be treated by Obtained lozenges, dense lozenges or boiled sweets with improved properties. Numerous publications and patent applications disclose compositions used to make lozenges' compact lozenges or hard candies (EP-A-0 240 773, EP-A-0 462 066 or DE-A 1 -43 1 6 537 ), Of which all kinds of physiologically tolerable insults · The printed materials of the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs are used as excipients for pharmaceutical active compounds or seasonings. These include, in particular, cellulose derivatives and their salts, sugars, sugars such as N-vinylpyrrolidone / ethyl acetate copolymers, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid and its salts, polysaccharides Water-soluble polymers such as methacrylic acid and its salts, such as polyoxyethylene, polyoxypropylene, and copolymers of ethylene and propylene oxide, such as polyoxyalkylenes, such as alginic acid, its alkali metals and ammonium salts, and carrageenin (Carrageenans), galactomannans, scutellaria baicalensis, agar, acacia, xanthan gum and other polysaccharides, such as chitin derivatives such as deacetylated chitin, such as pectin such as sodium carboxymethylpentyl pectin and Starches, and mixtures of these water-soluble polymers. Water-soluble means that at least 0.5 g, preferably 2 g, of the polymer can dissolve 100 g of water in the form of a colloid or dissolve in 100 g of water to form a coagulation, if necessary. gum. When preparing lozenges, coated lozenges, lozenges or hard candies, the good water solubility of the excipient base is particularly important for bioavailability and rapid absorption. Water solubility is also undeniably important for the pleasant taste and feel in the mouth, but the surface composition and taste sensation when inhaled also play the paper standard applicable to China National Standard (CNS) A4 specifications (210X 297 mm) -4 ~ 565454 A7 B7 V. Description of Invention (2) (Please read the notes on the back before filling this page) A very important role. In the case of those known excipient materials, such efficacy cannot be provided without problems. Although it has a good taste on the one hand, it has an irregular particle surface due to its physical properties or an uneven and possibly sharp-edged surface due to its poor processability. Generally, a premix is prepared so that the active compound added is evenly distributed in the excipient matrix, the various components are melted together with each other, or the active compound is kneaded in an existing polymer melt While mixed. The problems in these methods are consistent dosing, uniform mixing and continuous procedures. In order to administer the pharmaceutical active compound in the form of a tablet, a coated bond, or a buccal tablet to ensure a constant dosage, the active compound must be uniformly dispersed in the excipient matrix. This is a particular problem when using poorly soluble active compounds. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. Therefore, one aspect of the present invention is to provide a composition that can be carefully processed in a certain temperature range to obtain the desired product, that is, to obtain tablets, compact tablets. Agent or hard candy in which the active compound is added without damage. It is also an object of the present invention to provide a manufacturing method, which can be performed continuously, whereby tablets, dense tablets or hard candies having a smooth surface that is retained during inhalation and also having a pleasant taste and feel in the mouth can be prepared, and A homogeneous dispersion of the active compound and the seasoning contained therein. Another object of the present invention is to provide a composition which can be used in the method of the present invention and because the deformation force is long, it can be processed in a simple manner to obtain a desired product. The purpose is to include a composition of previously co-coated polyols. Special paper sizes are applicable to Chinese National Standard (CNS) A4 specifications (2) 0X 297 mm) -5-565454 A7 B7 Employees of the Intellectual Property Bureau of the Ministry of Economic Affairs Printed by the Consumer Cooperative. 5. Description of the invention (3. Other XE by including one or more selected from a group including xylitol, sorbitol or? L m (lactitol), malititol, butaerythritol or mannitol Polyols and optionally include a group of sugars including starch, cellulose, etc., and optionally one or more active compounds, one or more coloring agents, one or more natural sweeteners, one or more depending on the product The composition of sweetener 'acidifier', seasoning 'fragrance and general auxiliary is achieved. This object is also achieved by the method of manufacturing plastic molding or unshaped material, which mainly includes one or more polyol composition It is extruded in the temperature range of 30 to 170 ° C and shaped as required. In particular, this object is achieved by a previously co-sprayed composition, wherein the composition is extruded and then this The extrudate obtained by the formula is entered in the continuous molding unit (please read the precautions on the back before filling in this page). One-step processing The extruded mixture can be processed by the isotopes on the surface to obtain sexual compounds and practical uniformity. The product is composed of the substance and quality of the experimental sugar, which can be based on the composition of the sugar. The stoma contains an ingot, which is shaped and can still be formed into a lozenge that is calendered at less than 2 calenders. Other additives are also known. Active compounds are mixed and still have problems < shows that with sorbus such as maltitol, if necessary, additional inclusions can use compact lozenges or hard candies, known to melt the individual components at a temperature of 0 to 0. Extrudate It can be crushed to a solid block by using or using a rotary knife, which can be directly followed by compression during the extrusion process through suitable equipment. However, even now, in order to obtain the composition and to obtain a practically smooth surface sugar alcohol, wood Sugar alcohol, lactitol or other similar materials such as tetramethylene glycol, mannitol or other substances can be more easily obtained by molding from a group of monomers including starch and cellulose ## This paper size applies to Chinese National Standard (CNS) A4 (2! 0X297 mm) -6-565454 A7 B7 V. Description of the invention (4) Extrudate processed and processed for a long time. Contains these polyol mixtures The composition can be processed in the same way and easily. (Please read the notes on the back before filling this page.) It is found that polyol materials with high xylitol content can be processed particularly easily. Those materials have very good Processing properties. The components of this material have been pre-treated before the co-spraying method described in the patent application DE 19617487.2, and processed together to obtain a finely divided powder. The powder used for economical types is not only two or two A mixture of the above different powders, and a powder in which the respective particles constitute a mixture of the respective components due to co-spraying, that is, mixed crystals. Compared to the powder mixtures used, these powders have a lower melting point, and the resulting plastic material can also be deformed for a long period of time and rapidly deformed after extrusion. This deformation force can be further enhanced by adding an appropriate crystallization retarder known to those skilled in the art, which can be added during co-spraying. Advantageously, in the composition using the co-sprayed polyol or polyol mixture of the present invention as a substrate, the plasticizer or flow regulator which must be added in other cases may be omitted. Due to the co-spray drying of individual components, a powder can be obtained that can be extruded continuously when formed and collected in a co-spray method. Between or during the co-spraying and extrusion processing stages, active compounds, additives and general pharmaceutical auxiliaries such as fillers, lubricants, release agents, flow regulators, plasticizers, colorants, stabilizers, acidifiers Agents, seasonings, and spices can be added to the powder mixture. The fillers that can usually be added are known to those skilled in the art, such as the oxides of magnesium, aluminum, silicon, and titanium, but there are other substances. This paper size applies to the Chinese national standard (〇 ^) 6 4 specifications (2) 0 > < 297 public |) -7- 565454 A7 B7 V. Description of the invention (5) (Please read the precautions on the back before filling this page ) In some cases, flow regulators can be added, such as mono-, di-, and triglycerides of long-chain fatty acids, waxes, carnauba wax, or lecithin. However, in general, these additives are not required for the composition of the present invention. In addition to low molecular weight polyene oxides, such as polyethylene glycol, polypropylene glycol, and polyethylene glycol, polyhydric alcohols, such as propylene glycol, glycerol, and pentaerythritol, and sodium diethylthiosuccinate, a single unit of glycerol , Dione and triacetate and polyethylene glycol stearate are also suitable as plasticizers, which can be added if necessary. As the lubricant, aluminum or calcium stearate can be used, and talc or silicone can also be used. As for the colorant, a natural colorant can be similarly used, and all colorants and pigments allowed as a food additive. Usable stabilizers are antioxidants, free radical scouring agents, stabilizers for antimicrobial chemical etching, and light stabilizers. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. Depending on the composition, all additives can be accurately added at concentrations known to those skilled in the art, so as to achieve the desired effects of the additives. All additives can be added during the extrusion. However, it is advantageous for a homogeneous dispersion to add a soluble additive to the product during co-spraying of the composition. The insoluble additive can be mixed with the resulting powder by a co-spray method, and another component can be mechanically mixed before extrusion in a timely manner. Due to the previous co-spray treatment, the size of the mixed paper that is extruded with a high throughput is applicable to the Chinese National Standard (CNS) A4 (2l0x: 297 Gongchu) -8- 565454 A7 B7 V. Description of the invention (6) (Please read the precautions on the back before filling out this page) and obtain deformable materials. These powder mixtures in this case require a lower energy input due to the lower melting point and improved plasticity, apparently resulting from the improved structure of the powders used. Depending on the polyol or polyol mixture used, some energy input is therefore required during extrusion. This depends on, for example, the manner in which the polyol mixture is obtained, i.e., simple mixing or co-spraying. The energy input can be performed mechanically by the extrusion method and the force applied here. However, it can also be performed by additional heating. There are certain differences here, in the case of co-sprayed polyol compositions, the minimum energy is required. The polyol mixture of the present invention can be extruded at a temperature range of 30 to 170 ° C, especially 40 to 110 ° C. For mixtures obtained by co-spraying, conditions where the energy input results in a product with a degree of droop of approximately 70 to 110 ° C have proven to be particularly suitable. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs, but the co-sprayed polyol mixture can be extruded in a simple way, but it is impossible to extrude the mechanically mixed polyol combination to obtain a uniform product, because various polyols have different Of melting point. In particular, non-co-sprayed mixtures containing mannitol require a high energy input, otherwise a coarse-grained extruded product that also exhibits mannitol crystals is obtained. For mixtures containing mannitol, co-coating is therefore recommended. Through subsequent extrusion, an energy input of the product temperature at the exit position as high as 110 ° C was obtained, and a product with a smooth surface and good sucking behavior was obtained after molding. The mannitol-containing mixture processed by the method of the invention has particularly good product properties if it contains at least two additional polyols in an amount of up to 10% by weight. This paper size applies Chinese National Standard (CNS) A4 specification (210X 297 meals)-9- 565454 A7 B7 V. Description of the invention (7) (Please read the precautions on the back before filling this page) Through comparative experiments, it is found The previously co-sprayed polyol composition can be processed to obtain an extruded product having a smoother surface than in the case of extrusion molding with a simple mixing composition. If, for example, a commercially available spray-dried sorbitol (K a 1 · i ο η Instant @) is simply mixed directly with the other components of the composition, a product appears at a temperature of about 100 t-and then Extrusion after molding yields a product with a rougher surface than when using the corresponding co-sprayed composition. If, however, another similar commercially available crystalline sorbitol (Neosorb®) is treated in the same manner to obtain an extrudate with a smooth surface and additionally good sucking behavior. However, in this case, a very high energy input is necessary, and a thick rod diameter cannot be arbitrarily selected. Depending on the composition of the mixture and its past, an extrusion method is selected. Extrusion is carried out by using a twin-screw extruder or a plasticizing screw, in which energy is input by means of a screw, and additionally heated in a timely manner. However, it is also possible to use compression or transport screw heating extrusions. As for the variable parameters during extrusion, it is possible to change, in particular, the amount of product input, the conveying rate of the screw, the size and temperature of the outlet nozzle. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs. Because of its good processing properties, those materials previously co-sprayed by the method of the present invention can be compressed with a larger hollow diameter than those generally used for application products to obtain good results. This results in a higher product throughput. Co-coated polyols selected from the group consisting of xylitol, sorbitol, lactitol, maltitol, butaerythritol and mannitol, mixtures thereof or blends with other polyols can be processed using the method of the present invention and Good results were obtained. One or more of these polyols in the mixture were extruded to obtain plastic. The paper size is applicable to China National Standard (CNS) A4 (2 丨 0X 297 mm) -10- 565454 A 7 B7 5 Description of the invention (8) (Please read the precautions on the back before filling out this page) Molded or unformed materials. Compositions containing sorbitol and xylitol having a polyhydric alcohol quantity ratio of 50:50 to 99: 1, especially 65:35 to 98: 2, have proven to be particularly suitable. If sorbitol is included, the ratio of xylitol to mannitol is 9 0: 1: 9 to 7 0: 2 9: 1 ′, especially 8 2: 9: 9, then three kinds of polyol sorbitol, xylose are included. The composition of the alcohol and mannitol in the mixture has particularly good properties. All types of additives can be added to the polyol mixture of the composition before extrusion. Such additives may be, for example, one or more active compounds, one or more food additives, but may be one or more natural and / or one or more synthetic sweeteners. These additives can be added individually or together. Processing aids and additives can also be added in the pharmaceutical or food industry. Modern metering balances can be used, as described in EP-B1-0 337 256, where these additives are added in equal amounts so that a composition which is always homogeneous is extruded. The plastic molded or unformed material obtained after extrusion from the polyol composition of the present invention can be further processed by a molding unit generally used in the food or pharmaceutical industry, such as a chisel drum or an automatic rotating machine. The Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs prints products made from the materials of the present invention, such as lozenges, compact lozenges, lozenges or hard candies, in comparison with products made by known methods, having a period of use , Especially when smoking can keep a significantly smoother surface. Dissolves much more uniformly in the mouth, and the otherwise very smooth surface remains. Sharp edges are greatly reduced by these improved properties. These advantageous properties are particularly evident in products where the individual components have been mixed with each other before extrusion. When the used active compounds, seasonings, etc. are exposed to a lower temperature and the extruded rod can still be deformed for a longer period of time than normal; that is, the paper size obtained is applicable to the Chinese National Standard (CNS) A4 specification (2 丨 0X 297 mm) -11-565454 A7 B7 V. Description of the invention (9) After extrusion, the product retains the softness and deformability of the plastic for about 1 to 2 minutes. The co-sprayed polyol composition also has a low melting point. Particularly suitable for use in the extrusion process of the present invention. In addition, in comparison with conventionally obtained extrudates, the rod diameter is determined by the apparent and good plastic behavior of the extrudates according to the present invention, with the greatest selectivity. These compositions also show better sucking behavior after extrusion and molding than hitherto known. Compared with the conventional method, the method of the present invention has many advantages. These advantages include the possibility of continuously preparing pulverized compositions in which the respective components are equal and unchanged, which are directly extruded under milder conditions to obtain plastic molded or unshaped materials and which can then be processed and formed To obtain lozenges, dense lozenges, lozenges or hard candies. A particular advantage of the composition of the present invention is that the resulting product has a much smoother surface, which surface remains during smoking. In addition, advantageous improvements are achieved by previously co-spraying the polyol of the present invention and co-spraying mannitol in a timely manner. The chalky taste produced in the known antacids is hidden by the composition of the present invention. When the prepared lozenge is rapidly dissolved due to the excipient substance used, the bioavailability and absorbability of the combined active compound are also increased, and it can be inhaled without problems because of its pleasant taste. This is important if rapid activity is required, for example in the case of containing analgesics. If necessary, the tablets prepared according to the invention can also be coated with a general coating to improve appearance or achieve delayed activity Purpose of Compound Release b If tablets are prepared by a known technique in the form of closed cell pores to float in the stomach and thereby stay for a longer period of time, then the active compounds will be delayed for tablets. This paper is applicable to China Standard (CNS) A4 Specifications (2) OX 297 Gongchu) '-12- (Please read the precautions on the back before filling out this page) Order-Printed by the Consumer Property Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs 565454 A7 B7 V. Invention It shows that (10) is advantageous in terms of release. (Please read the precautions on the reverse side before filling out this page) The pharmaceutically active compounds in the present invention are all substances that have medicinal effects and the lowest possible side effects if they are not decomposed under processing conditions. The amount of active compound per dosage unit and concentration may vary widely depending on the activity and release rate. The concentration of such an active compound may be from 0.1 to 95, preferably from 5 to 80. The active compounds can also be used in combination. The composition of the present invention is preferably suitable for applying an active compound which requires its immediate bioavailability and obtains a favorable taste with other ingredients. Such active compounds may be antacids, analgesics, tranquilizers, relaxants or other pharmaceutical active compounds. The active compounds in the present invention are also edible physiological substances such as vitamins, minerals and trace elements. The following examples are intended to illustrate the invention, but not to limit its scope. Example composition a Mechanically mixed polyol composition b Spray-dried sorbitol Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs c P300 sorbitol d Crystalline sorbitol This paper standard applies Chinese national standards ( CNS) A4 specification (210X 297 Gongchu) -13- 565454 V. Description of the invention (1 Printed by Kl B7, Employee Consumer Cooperative of Intellectual Property Bureau, Ministry of Economic Affairs, Example 1 2 3 4 5 6 7 8 Composition ab C bbbdd Passed material Volume 17 15 14 14 14 17 17 17 [kg / hour] Temperature Eft] 90 100 92.5 92.5 101 103 Pressure 1 [bar] 7 16 2 3 3 2 0 9 as / i [° c] KKKKKKKK t2 S / l [° C] 90 70 110/120 80 77 88 130 115 t3 S / l [° C] 90 50 110/120 80 77 90 130 115 Multiwell plate 1x4.6 2x2 1x4.5 1x4.5 1x4.5 12x9 12x9 1x4.5 OV OV Tiefulong Tiefulong injection 20 bar smooth product soft and quite smooth temperature best very smooth and fragile, open rough water to open the table, extrudate extrudate materialization experiment extrudate hole, no Surface, beginning, break with facet, slight, good extrusion The roughness of the surface produced by the roughness nozzle depends on the pressure due to the larger temperature (please read the precautions on the back before filling this page) This paper size applies to the Chinese National Standard (CNS) Λ4 specification (2) 0X 297 mm)- 14-