經濟部中央標準局員工消費合作杜印裝 4193 了了 A7 _____B7 五、發明説明（） 傳統之鍵劑在加入活性成份之步驟不外乎是在製粒時加入，或在整 粒時加入，或於直接混合時加入，最終混合均勻再壓錠，但錠劑之 藥效性通常較液劑來的差，但液劑有調劑不便，且投藥時口感不佳 之缺點，因此本發明將一不含活性成份之藥學組成打錠製一空白鉸, 再以此空白錠浸潰在活性成份中，控制空白錠吸收活性成份至固定 量，必要時以離心方法將多餘之活性成份除掉，以此方法製得之產 品較傳統錠劑有較佳之藥效性，其活性成份為聚二甲矽烷 (Dimethylpolysiloxane)或喜每賜康(Simethicon)或其混合物。 聚二甲矽烷（Dimethylpolysiloxane)或喜每賜康(Simethicon)具有 界面活性作用，能使表面張力降低，達到消泡之作用，適用於腹部 膨滿感及鼓腸之患者，亦適於作胃視鏡檢查前之消泡劑。 目前在醫療院所中做胃視鏡檢查前，必須先服用液劑之聚二甲矽烷 (Dimethyipolysiloxane)或喜每賜康(Simethicon)或其混合物，來消 除胃中枯膜之氣泡。聚二甲梦娱^Dimethylpolysiloxane)或喜每賜 康(Simethicon)本身為液態時口慼甚差，要製成高劑量之錠劑有其 困難性，故市面上所製成之錠劑產品其消泡性者不佳，故本發明利 用習知之吸收劑、結合劑或稀釋劑或其混合物、潤滑劑或崩散劑 予以混合打錠，製得空白錠，再將此空白錠浸潰在聚二甲矽燒 (Dimethylpolysiloxane)或喜每賜康(Simethicon)或其混合物，控制 空白錠吸收至固定量，必要時以離心除掉多餘之活性成份。 以下説明為本發明之實施例僅作為舉例説明用，並非用來侷限本發 明之範蜂。 本纸财關家縣（CNS)从聽_ (2丨攸所公董> 83. 3. !〇,〇〇〇 {請先閱讀背面之注意事項再填寫本頁) 装- « 1 1The consumer cooperation of the Central Bureau of Standards of the Ministry of Economic Affairs of the People's Republic of China Du printed 4193 A7 _____B7 V. Description of the invention () The traditional bonding agent is added to the active ingredient only during granulation, or during granulation, or It is added during direct mixing, and finally mixed uniformly, and then pressed into tablets. However, the efficacy of tablets is usually worse than that of liquid preparations, but liquid preparations have the disadvantages of inconvenient adjustment and poor taste when administered. Therefore, the present invention will not contain any activity. The pharmaceutical composition of the ingredients is made into a blank hinge, and the blank ingredient is immersed in the active ingredient. The blank ingredient is controlled to absorb the active ingredient to a fixed amount. If necessary, the excess active ingredient is removed by centrifugation. The obtained product has better pharmacodynamics than traditional lozenges, and its active ingredient is Dimethylpolysiloxane or Simethicon or a mixture thereof. Dimethylpolysiloxane or Simethicon has interfacial activity, which can reduce the surface tension and achieve the effect of defoaming. It is suitable for patients with abdominal fullness and tympanic intestines. It is also suitable for gastroscopy. Check the defoamer before. At present, before performing gastroscopy in medical institutions, you must first take liquid solution of Dimethyipolysiloxane or Simethicon or a mixture of them to eliminate air bubbles in the stomach. Dimethylpolysiloxane or Simethicon is very poor when it is liquid. It is difficult to make high-dose lozenges. Therefore, the lozenge products made on the market are not good. The foamability is not good, so the present invention uses conventional absorbents, binding agents or diluents or their mixtures, lubricants or disintegrating agents to mix the tablets to obtain a blank tablet, which is then immersed in polydimethylamine Dimethylpolysiloxane or Simethicon or its mixture, control the blank tablets to absorb to a fixed amount, and if necessary, remove excess active ingredients by centrifugation. The following description is an embodiment of the present invention for the purpose of illustration only, and is not intended to limit the fan of the present invention. This paper Caiguan County (CNS) from listening _ (2 丨 Yousuo public director> 83. 3.! 〇, 〇〇〇 {Please read the precautions on the back before filling this page) Pack-«1 1
— · I I -I - - -I A7 B7 五、發明説明（） 實施例一： 鍵劑之組成物： 活性成份： 聚二f矽烷 40 mg 空白妓： 二氧化矽 4 mg 微結晶性纖維素 304 mg 羧甲基澱粉鈉 8 mg 滑石粉 4 mg 合 計 360 mg 裝— (請先《讀背面之注意事項再填寫本頁) 經濟部令央橾準局貝工消費合作社印家 製備方法： 將微結晶性纖維素與羧甲基澱粉鈉和二氧化矽予以混合，過篩 (30 mesh)—次，最後加入滑石粉，置入混合機内混合5分鐘，於 打鍵機壓成键劑(空白键）。 將此錠劑（空白鍵）浸潰於活性成份聚二甲麥燒 (Dimethylpolysiloxane)内，吸收聚二甲妙燒(Dimethylpolysilo xane)至固定量，必要時再經離心處理，除去多餘的活性成分， 即完成本發明品製造。 本紙張尺度逍用t國國家橾準（CNS } A4洗格（2]0Χ297公釐} 83. 3.10,000 419377 A7 ____B7五、發明説明（） 實施例二： 鍵劑之組成物： 活性成份： 喜每賜康 50 mg 空白錠： 二氧化矽 4 mg 乳醣 294 mg 羧甲基澱粉鈉 8 mg 硬脂酸緩 4 mg 合 計 360 mg 製備方法： n I- I- - I I I In I - I I I 1 i 1 I 1 1---i 丁 (請先闖讀背面之注$項再填寫本頁) 經濟部中央橾準局負工消费合作社印装 將乳醣與羧甲基澱粉鈉和二氧化矽予以混合，過篩(3 0 m esh) — 次，最後加入硬脂酸鎂，置入混合機内混合5分鐘，於打錠機壓 成錠劑(空白錠）。 將此錠劑(空白鍵)浸潰於活性成份喜每賜康(Simethicon)内，吸 收喜每賜康(Simethicon)至固定量，必要時再經離心處理，除去 多餘的活性成分，即完成本發明品製造。 本紙张尺度適用中國國家橾率（CNS ) A4規格（21〇χ29?公釐） 83* Ϊ· 10,000 Λ19377 A7 B7 五、發明説明（） 實施例三： 鍵劑之組成物： 活性成份： 聚二甲矽烷 80 mg 空白錠： 二氧化矽 8 mg 微結晶性纖維素 244 mg 葡萄醣 244 mg 羧甲基纖維素鈣 16 mg 硬脂酸鎂 8 mg 合 計 600 mg .東— {請先《讀背面之注意事項再填寫本頁) 丁 -5 經濟部中央標準局貞工消费合作社印¾ 製備方法： 將微結晶性纖維素與葡萄醣、羧甲基纖維素鈣及二氧化矽予 以混合，過篩(30 mesh)—次，最後加入硬脂酸鎂，置入混合機内 混合5分鐘，於打錠機壓成錠劑(空白鏡）。 將此錠劑（空白錠）浸潰於活性成份聚二甲矽烷 (Dimethylpolysiloxane)内，吸收聚二甲梦燒(Dimethylpolysilo-xane)至固定量，必要時再經離心處理，除去多餘的活性成分， 即完成本發明品製造。 本紙張尺度適用中國國家揉準（CNS ) A4规格U10X297公釐j 81 3.10,000 419377 五、發明说明（） 實施案例四： 銳香丨之組成物： 活性成份： 聚二f矽烷 80 mg 空白键： 二氧化矽 8 mg 微結晶性纖維素 390.4 mg 葡萄醣 97.6 mg 羧甲基纖維素鈉 16 mg 硬脂酸鐵 8 mg 合 計 600 mg (請先W讀背面之注意事項再填寫本頁) —裝· 經濟部中央樣準扃貝工消費合作社印裝 製備方法: 將微結晶性纖維素與葡萄醣、羧甲基纖維素鈉·及二氧化梦予 以混合，過篩(30 mesh)—次，最後加入硬脂酸鎂，置入混合機内 混合5分鐘，於打錠機壓成錠劑(空白錠）。 將此錠劑（空白錠）浸潰於活性成份聚二甲矽烷 (Dimethylpolysiloxane)内，吸收聚二甲矽烷(Dimethylpolysilo-xane)至固定量，必要時再經離心處理，除去多餘的活性成分， 即冗成本發明品製造。 本紙乐认制til國家樓準（CNS) A4^ (21()><297公们 83.3.10,000 41937 五、發明説明（ A7 B7 實施案例五： 錠劑之組成物： 活性成份： 聚二甲矽烷 80 mg 空白錠： 二氧化矽 8 mg 微結晶性纖维素 97.6 mg 葡萄醣 390.4 mg 羧甲基纖維素鈣 16 mg 硬脂酸鎂 8 mg 合 計 600 mg I I - 1 - - 1 -I I -1 · dioi I I I I ' I I »^1 X» (請先《讀背面之注$項再填寫表頁) 經濟部中央榇^扃貝工消背合作社印策 製備方法: 將微結晶性纖維素與葡萄醣、羧甲基纖維素鈣及二氧化矽予 以混合，過篩(30 mesh)—次，最後加入硬脂酸鎂，置入混合機内 混合5分鐘，於打錠機壓成錠劑(空白鍵）。 將此錠劑（空白錠）浸潰於活性成份聚二甲矽烷 (Dimethylpolysiloxane)内，吸收聚二甲梦能(Dimethylpolysilo-xane)至固定量，必要時再經離心處理，除去多餘的活性成分， 即完成本發明品製造。 適用中國國家標準（CNS ) Μ規格ί 210X2打公釐） 83.110,000 m?7 五、發明説明（） 外觀硬度朋散性和a泡性比較，其中崩散性 係依美國藥典之方法實施，其結果如下。 匕『疋涮疋， 外觀，市面上A.B.C.三產品其外崎為自色不具 品為白色具光澤性。 贫月 硬度：取市面上A.B.C‘三產品和本發明品分卿試 再取其平均値，測試結果如下： 欠〜 Α 產品：4.03 kg/cm2 B 產品：7.43 kg/cm2 C 產品：4.03 kg/cm2 本發明品：6.43 kg/cm2 崩散性：取市面上A.B.C·三產品和本發明品，分別測試其崩散性 (崩散時間),測試結果如下： A產品：10分5秒 B產品：13分25秒 C產品：7分4秒 本發明品：1分32秒 經濟部中央樣準局男工消費合作社印袈 消泡性：取市面上A.B.C.三產品和本發明品，分別測試其消泡性 (消泡時間),測試結果如下： 市甸上入卫^：.三產品在超過2分鐘後都未完全消泡 而本發明品卻在15秒即達到消泡之作用。 本纸張尺度逍用十國國家標準（CNS ) A4規格（210X297公釐） 經濟部中央標準局貝工消費合作社印t— · II -I---I A7 B7 V. Description of the invention () Example 1: Bonding agent composition: Active ingredient: Polydisilane 40 mg Blank prostitute: Silicon dioxide 4 mg Microcrystalline cellulose 304 mg Sodium Carboxymethyl Starch 8 mg Talc 4 mg Total 360 mg Pack — (Please read the “Notes on the back side before filling out this page”) Order from the Ministry of Economic Affairs, Central Bureau of Quasi-Bureau Consumer Cooperative, India Printing method: Microcrystalline The cellulose is mixed with sodium carboxymethyl starch and silicon dioxide, and sieved (30 mesh) times. Finally, talc is added, mixed in the mixer for 5 minutes, and pressed into a keying agent (blank key) in a key press. Dip this lozenge (blank bond) in the active ingredient Dimethylpolysiloxane, absorb Dimethylpolysilo xane to a fixed amount, and then centrifuge if necessary to remove excess active ingredients. The production of the product of the present invention is completed. The standard of this paper is in accordance with national standards (CNS} A4 washing grid (2) 0 × 297 mm} 83. 3.10,000 419377 A7 ____B7 V. Description of the invention () Example 2: Composition of the bonding agent: Active ingredients: Ximei Cikang 50 mg blank tablets: silicon dioxide 4 mg lactose 294 mg sodium carboxymethyl starch 8 mg stearic acid 4 mg total 360 mg Preparation method: n I- I--III In I-III 1 i 1 I 1 1 --- i Ding (please read the note “$” on the back before filling out this page) The Central Consumers' Bureau of the Ministry of Economic Affairs, the Consumer Cooperatives, printed lactose, sodium carboxymethyl starch and silicon dioxide. Mix and sieve (30 m esh) — times, finally add magnesium stearate, mix in the mixer for 5 minutes, and press into a tableting machine to form a tablet (blank tablet). Dip this tablet (blank key) Crush into the active ingredient Simethicon, absorb Simethicon to a fixed amount, and if necessary, perform centrifugal treatment to remove excess active ingredients to complete the manufacture of the invention. This paper size is applicable to China National ratio (CNS) A4 specification (21 × 29? Mm) 83 * Ϊ · 10,000 Λ19377 A7 B7 V. Description of the invention ( Example 3: Composition of bonding agent: Active ingredient: Polydimethyl silane 80 mg Blank tablet: Silicon dioxide 8 mg Microcrystalline cellulose 244 mg Glucose 244 mg Carboxymethyl cellulose calcium 16 mg Magnesium stearate 8 mg Total 600 mg. Dong — {Please read the “Precautions on the reverse side before filling out this page”) D-5 Printed by Zhengong Consumer Cooperative, Central Standards Bureau, Ministry of Economic Affairs Preparation method: Microcrystalline cellulose with glucose, carboxymethyl Cellulose calcium and silicon dioxide are mixed, sieved (30 mesh)-times, and finally magnesium stearate is added, placed in a mixer and mixed for 5 minutes, and pressed into a tableting machine (blank mirror). The agent (blank tablet) is immersed in the active ingredient Dimethylpolysiloxane, and absorbs Dimethylpolysilo-xane to a fixed amount. If necessary, it is centrifuged to remove the excess active ingredient to complete the preparation. Manufacture of inventions. This paper size is applicable to China National Standards (CNS) A4 specification U10X297 mm j 81 3.10,000 419377 V. Description of the invention () Example 4: Composition of rue 丨: Active ingredients: Poly Dif silane 80 mg blank bond: silicon dioxide 8 mg microcrystalline cellulose 390.4 mg glucose 97.6 mg sodium carboxymethyl cellulose 16 mg iron stearate 8 mg total 600 mg (please read the precautions on the back first) (Fill in this page) —Packing · Central sample of the Ministry of Economic Affairs, Printing and Printing Co., Ltd. Preparation method: Mix microcrystalline cellulose with glucose, sodium carboxymethylcellulose, and dioxide dream, and sieve (30 mesh ) -Times, finally add magnesium stearate, mix in a mixer for 5 minutes, and press into a tableting machine (blank tablet). This tablet (blank tablet) is immersed in the active ingredient Dimethylpolysiloxane, and the Dimethylpolysilo-xane is absorbed to a fixed amount, and if necessary, it is centrifuged to remove the excess active ingredient, that is, Redundant manufacturing of inventions. National Paper Standard (CNS) A4 ^ (21 () > < 297 men 83.3.10,000 41937) V. Description of the invention (A7 B7 Implementation case 5: Composition of lozenges: Active ingredient: Poly 2 Silane 80 mg blank tablets: silicon dioxide 8 mg microcrystalline cellulose 97.6 mg glucose 390.4 mg carboxymethyl cellulose calcium 16 mg magnesium stearate 8 mg total 600 mg II-1--1 -II -1 · Dioi IIII 'II »^ 1 X» (please read the “$” on the back side and fill in the form page) The central government ’s Ministry of Economic Affairs ^^ Beigong Xiaobei Cooperative Co., Ltd. Preparation method: Microcrystalline cellulose and glucose, Carboxymethylcellulose calcium and silicon dioxide are mixed, sieved (30 mesh) -times, and finally magnesium stearate is added, mixed in a mixer for 5 minutes, and pressed into a tablet (blank key) in a tableting machine. This tablet (blank tablet) is immersed in the active ingredient Dimethylpolysiloxane to absorb Dimethylpolysilo-xane to a fixed amount. If necessary, it is centrifuged to remove excess active ingredients. This completes the manufacture of the invention. Applicable to Chinese national standards (C NS) Specification M 210X2 dymm) 83.110,000 m? 7 V. Description of the invention () Comparison of appearance hardness diffusivity and a foaming property, in which disintegration is implemented according to the method of the United States Pharmacopoeia, and the results are as follows "疋 涮 疋, Appearance, the three ABC products on the market, the outer qi is self-colored, and the product is white and shiny. Poor Moon Hardness: Take the ABC 'three products on the market and the product of the present invention, and then take the average 値, test The results are as follows: O Product: 4.03 kg / cm2 B Product: 7.43 kg / cm2 C Product: 4.03 kg / cm2 The product of the invention: 6.43 kg / cm2 Disintegrability: Take ABC · Three products on the market and the product of the invention, Test the disintegration (disintegration time) separately, the test results are as follows: Product A: 10 minutes and 5 seconds B Product: 13 minutes 25 seconds C Product: 7 minutes 4 seconds Invented products: 1 minute 32 seconds Central Ministry of Economics Neem defoaming properties of local male consumer cooperatives: take ABC three products on the market and the product of the present invention, and test their defoaming properties (defoaming time) respectively. The test results are as follows: After 2 minutes, the foam was not completely defoamed, but the product of the invention reached the defoaming effect in 15 seconds. The paper size is in accordance with the National Standards of Ten Countries (CNS) A4 (210X297 mm). Printed by the Bayer Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs.
4 19377 A7 ----^___B7五、發明説明（） 通常相同之藥學组成份壓錠時，其硬度愈大則所需之崩散時間就愈 長，而本發明品之硬度(6.43kg/cm2)較市面上A產品(4.〇3kg/cm2)和c 產品(4.〇3kg/cm2)大，但本發明品崩散時間(丨分32秒）卻較A產品(9分5 秒）、c產品(7分4秒)快許多，且本發明品之消泡效果較市面上AB.c· 三產品優越，如表1.故本發明品與市面上相似錠劑有較快速效藥 性。 表1·本發明品與市售傳統產品特徵比較 市售產品 比較項目 A废 B廠 C廠 本發明品 外觀，色澤 白色，無光澤 白色,無光澤 白色，無光澤 白色具光澤 鍵劑硬度 x=4.03kg/cm2 x=7.43kg/cm2 x=4.03kg/cm2 ^^^Skg/cm2 x=6 X=6 X=6 X=6 崩散時間 9分5秒 13分25秒 7分4秒 1分32秒 消泡時間 超過120秒 超過Π0秒 超過120秒 15秒 本發明所用之吸收劑可為二氧化矽，崩散劑可為羧甲基澱粉鈉、截 甲基纖維素鈉、羧甲基纖維素鈣，潤滑劑可為滑石粉、硬脂酸、硬 脂酸鎂，稀釋劑可為單醣或雙醣，如葡萄醣、甘露醇、半乳醣、山 梨醇、果醣、庶醣、乳醣，結合劑可為微結晶性纖維素或直接壓錠 之乳醣，其中稀釋劑和結合劑可單獨使用或兩者混合使用。 本紙張从適财CNS) A術^ (21()讀公幻 83.3. !〇,〇( C-- 1請先PST*.背面之注意事項存4寫本真) ,ΐτ i *4-----4 19377 A7 ---- ^ ___ B7 V. Description of the invention () Usually when the same pharmaceutical composition is pressed into tablets, the larger the hardness, the longer the disintegration time required, and the hardness of the product of this invention (6.43kg / cm2 ) Is larger than A product (4.03kg / cm2) and c product (4.03kg / cm2) on the market, but the disintegration time (丨 32 seconds) of the product of the present invention is longer than that of A product (9 minutes 5 seconds) , C product (7 minutes 4 seconds) is much faster, and the defoaming effect of the product of the present invention is superior to the AB.c. three products on the market, as shown in Table 1. Therefore, the product of the present invention and the similar tablets on the market have faster efficacy. . Table 1 · Comparison of the characteristics of this product with traditional products on the market Comparison of products on the market A Waste B Factory C Factory The appearance of this product is white, matte white, matte white, matte white glossy key agent hardness x = 4.03kg / cm2 x = 7.43kg / cm2 x = 4.03kg / cm2 ^^^ Skg / cm2 x = 6 X = 6 X = 6 X = 6 Disintegration time 9 minutes 5 seconds 13 minutes 25 seconds 7 minutes 4 seconds 1 The defoaming time is more than 120 seconds, more than 120 seconds, more than 120 seconds, and more than 120 seconds and 15 seconds. The absorbent used in the present invention may be silicon dioxide, and the dispersant may be sodium carboxymethyl starch, sodium truncated methyl cellulose, and carboxymethyl fiber. Calcium, the lubricant can be talc, stearic acid, magnesium stearate, and the diluent can be mono- or disaccharides, such as glucose, mannitol, galactose, sorbitol, fructose, galose, lactose, The binding agent can be microcrystalline cellulose or directly compressed lactose, wherein the diluent and the binding agent can be used alone or in combination. This paper is from Shuai Choi CNS) A technique ^ (21 () read the public fantasy 83.3.! 〇, 〇 (C-1 please PST *. Note on the back to save 4 photos), ΐτ i * 4 --- -