JPS6327423A - Coating method for solid pharmaceutical - Google Patents
Coating method for solid pharmaceuticalInfo
- Publication number
- JPS6327423A JPS6327423A JP16925686A JP16925686A JPS6327423A JP S6327423 A JPS6327423 A JP S6327423A JP 16925686 A JP16925686 A JP 16925686A JP 16925686 A JP16925686 A JP 16925686A JP S6327423 A JPS6327423 A JP S6327423A
- Authority
- JP
- Japan
- Prior art keywords
- coating
- wax
- solid
- melting point
- soluble
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 238000000576 coating method Methods 0.000 title claims abstract description 51
- 239000007787 solid Substances 0.000 title claims abstract description 38
- 239000011248 coating agent Substances 0.000 claims abstract description 39
- 239000001993 wax Substances 0.000 claims abstract description 34
- 238000002844 melting Methods 0.000 claims abstract description 18
- 230000008018 melting Effects 0.000 claims abstract description 18
- 238000000034 method Methods 0.000 claims abstract description 13
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 7
- 239000000194 fatty acid Substances 0.000 claims abstract description 7
- 229930195729 fatty acid Natural products 0.000 claims abstract description 7
- 239000007888 film coating Substances 0.000 claims abstract description 6
- 238000009501 film coating Methods 0.000 claims abstract description 6
- -1 fatty acid ester Chemical class 0.000 claims abstract description 5
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 5
- 239000003925 fat Substances 0.000 claims abstract description 3
- 150000004665 fatty acids Chemical class 0.000 claims abstract description 3
- 229930195733 hydrocarbon Natural products 0.000 claims abstract description 3
- 150000002430 hydrocarbons Chemical class 0.000 claims abstract description 3
- 239000003921 oil Substances 0.000 claims abstract description 3
- 238000002360 preparation method Methods 0.000 claims description 31
- 239000000203 mixture Substances 0.000 claims description 8
- 150000001298 alcohols Chemical class 0.000 claims description 2
- 239000002253 acid Substances 0.000 abstract description 9
- 235000019658 bitter taste Nutrition 0.000 abstract description 9
- 235000013871 bee wax Nutrition 0.000 abstract description 8
- 239000012166 beeswax Substances 0.000 abstract description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 7
- 235000014121 butter Nutrition 0.000 abstract description 7
- 244000299461 Theobroma cacao Species 0.000 abstract description 6
- 235000005764 Theobroma cacao ssp. cacao Nutrition 0.000 abstract description 6
- 235000005767 Theobroma cacao ssp. sphaerocarpum Nutrition 0.000 abstract description 6
- 235000001046 cacaotero Nutrition 0.000 abstract description 6
- 230000000873 masking effect Effects 0.000 abstract description 4
- 235000019197 fats Nutrition 0.000 abstract description 2
- 239000004215 Carbon black (E152) Substances 0.000 abstract 1
- 235000013869 carnauba wax Nutrition 0.000 abstract 1
- 239000004203 carnauba wax Substances 0.000 abstract 1
- 230000002349 favourable effect Effects 0.000 abstract 1
- 210000002784 stomach Anatomy 0.000 abstract 1
- 238000007664 blowing Methods 0.000 description 11
- 239000007921 spray Substances 0.000 description 11
- 239000008187 granular material Substances 0.000 description 10
- 239000007788 liquid Substances 0.000 description 9
- 239000000243 solution Substances 0.000 description 9
- 239000003960 organic solvent Substances 0.000 description 8
- 238000009505 enteric coating Methods 0.000 description 7
- 239000002702 enteric coating Substances 0.000 description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- 239000003814 drug Substances 0.000 description 6
- 239000010410 layer Substances 0.000 description 6
- 229940079593 drug Drugs 0.000 description 5
- 238000001035 drying Methods 0.000 description 5
- 239000000454 talc Substances 0.000 description 5
- 229910052623 talc Inorganic materials 0.000 description 5
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 4
- 238000010828 elution Methods 0.000 description 4
- 238000005507 spraying Methods 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 239000001069 triethyl citrate Substances 0.000 description 4
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 4
- 235000013769 triethyl citrate Nutrition 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- 229960001138 acetylsalicylic acid Drugs 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 3
- 235000012239 silicon dioxide Nutrition 0.000 description 3
- 238000009495 sugar coating Methods 0.000 description 3
- 235000019640 taste Nutrition 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 229930003270 Vitamin B Natural products 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000007853 buffer solution Substances 0.000 description 2
- ZAIPMKNFIOOWCQ-UEKVPHQBSA-N cephalexin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=CC=C1 ZAIPMKNFIOOWCQ-UEKVPHQBSA-N 0.000 description 2
- 229940106164 cephalexin Drugs 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 2
- 235000019156 vitamin B Nutrition 0.000 description 2
- 239000011720 vitamin B Substances 0.000 description 2
- 239000004382 Amylase Substances 0.000 description 1
- 102000013142 Amylases Human genes 0.000 description 1
- 108010065511 Amylases Proteins 0.000 description 1
- 241000972773 Aulopiformes Species 0.000 description 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 108010019160 Pancreatin Proteins 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 description 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 235000019418 amylase Nutrition 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 239000011247 coating layer Substances 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000001087 glyceryl triacetate Substances 0.000 description 1
- 235000013773 glyceryl triacetate Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 229960003511 macrogol Drugs 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- SQABAALQCGKFFO-UHFFFAOYSA-N octanoic acid;propane-1,2,3-triol Chemical compound OCC(O)CO.CCCCCCCC(O)=O SQABAALQCGKFFO-UHFFFAOYSA-N 0.000 description 1
- 229940055695 pancreatin Drugs 0.000 description 1
- 238000005498 polishing Methods 0.000 description 1
- 238000007517 polishing process Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 235000019515 salmon Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明は固形製剤のフーティング法、殊に医薬品の剤形
として汎用きれる水溶性（胃溶性）または腸溶性のフィ
ルムコーティングを施した固形製剤、すなわち錠剤、大
側、顆粒または細粒におけるコーティング法に関するも
のである。DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to a footing method for solid preparations, especially solid preparations coated with a water-soluble (gastric-soluble) or enteric-coated film that can be used widely as pharmaceutical dosage forms. , i.e. coating methods on tablets, bulk, granules or granules.
周知のとおり錠剤、大側、顆粒もしくは細粒なと医薬品
における固形製剤のコーティングとしては、主としてシ
ョ糖水溶液からなる糖衣用シロップを被コーテイング製
剤に被覆して糖衣贋を形成せしめる糖衣コーティングと
、例えば各種セルロース系またはアクリル系物質からな
るフィルム形成能を有する高分子物質溶液を同製剤に噴
霧し、当該高分子物質膜を被覆形成せしめるフィルムコ
ーティングとがある。このフィルムコーティングを実施
する場合、従来は所望のフィルム形成性物質を専ら有機
溶媒に溶解芒せ、この溶液を噴霧して行っていた。As is well known, coatings for solid preparations such as tablets, large granules, granules, and fine granules for pharmaceuticals include sugar coating, in which the drug to be coated is coated with a sugar coating syrup mainly consisting of an aqueous sucrose solution to form a sugar coating; There is film coating, in which a solution of a polymeric substance having a film-forming ability made of various cellulose-based or acrylic-based substances is sprayed onto the same preparation to form a film of the polymeric substance. Conventionally, film coating has been carried out by dissolving a desired film-forming substance in an organic solvent and then spraying the solution.
しかしながら、近年これら作業の安全性、環境保全およ
び／またはコストの低減といった面から水溶液もしくは
水懸濁性のいわゆる水系コーティングが一部採月されつ
つあり、そのためのコ−ティング基剤、特に腸溶基剤も
開発され、既に数種の基剤が市販きれている０例えばセ
ルロース系の腸溶基剤として１ヒドロキシプロピルメチ
ルセルロースアセテートサクシネート（以下ＨＰＭＣＡ
Ｓと略記する）１、ｒカルボキシメチルエチルセルロー
ス（以下ＣＭＥＣと略記する）」、またアクリル系の腸
溶基剤としてはメタアクリル酸−アクリル酸エチルエス
テルコポリマーの１オイドラギツトし一３０ＤＪ（商品
名）などが知られているが、これらの水系腸溶性基剤は
、その造膜の機構上従来の有機溶媒に溶解するコーティ
ング法に比較し、同等の耐酸性を示す皮膜を得るために
は、その皮膜厚みを１０〜２０％程度増や芒なければな
らない、また、上記の腸溶基剤、殊にセルロース系の１
ｌｆ１溶性基剤は、これを水系で用いる場合には比較的
多くの溶解剤、例えばクエン酸トリエチル、トリアセチ
ンおよび／またはグリセリンカプリル酸エステルなどを
必要とし、これらはいずれもかなり強い苦味を有するの
で、このような基剤をコーティングした腸溶固形製剤は
必然的に苦味を呈するといった欠点がある。However, in recent years, so-called aqueous coatings that are aqueous solutions or water suspensions have been gaining popularity in view of the safety of these operations, environmental protection, and/or cost reduction. Bases have also been developed, and several types of bases are already commercially available.For example, 1-hydroxypropyl methyl cellulose acetate succinate (hereinafter referred to as HPMCA) is a cellulose-based enteric base.
(abbreviated as S) 1, rcarboxymethylethylcellulose (hereinafter abbreviated as CMEC), and acrylic enteric bases include methacrylic acid-acrylic acid ethyl ester copolymer 1 Eudragit-30DJ (trade name), etc. However, due to the film-forming mechanism of these water-based enteric bases, compared to conventional coating methods that dissolve in organic solvents, it is necessary to The thickness must be increased by about 10 to 20%, and the above enteric base, especially cellulose type 1
If the lf1 soluble base is used in an aqueous system, it requires a relatively large amount of solubilizing agent, such as triethyl citrate, triacetin, and/or glycerin caprylate, all of which have a fairly strong bitter taste. Enteric-coated solid preparations coated with such bases have the disadvantage of inevitably having a bitter taste.
本発明は以上のような状況において鋭意研究の結果完成
されたものである。The present invention was completed as a result of intensive research under the above circumstances.
従って、本発明は、かかる固形製剤の水系および有機溶
媒系コーティングにおける腸溶皮膜の耐酸性向上と、水
系コーティング着の苦味のマスキングを図るために提案
されたものである。Therefore, the present invention was proposed in order to improve the acid resistance of enteric coatings in water-based and organic solvent-based coatings of such solid preparations and to mask the bitter taste of water-based coatings.
本発明は上記の目的を達成するために、水溶性（胃溶性
）または腸溶性のフィルムフーティングを施した固形製
剤に、融点３０〜９０℃の固形ワックスを熱溶融法によ
って被覆することを、その要旨とするものである。In order to achieve the above object, the present invention involves coating a solid preparation with a water-soluble (gastric-soluble) or enteric film footing with a solid wax having a melting point of 30 to 90°C by a hot melting method. This is the summary.
本発明は上述のとおり水溶性（胃溶性）または腸溶性の
フィルムフーティングを施した固形製剤にワックス層を
熱各融法により・被覆形成するので、−当該製剤に好ま
しい耐酸性を付与し、かつ味のマスキング作用を奏する
ものである。As described above, the present invention involves coating a solid preparation with a water-soluble (gastric-soluble) or enteric-coated film footing with a wax layer by a thermal melting method, thereby imparting preferable acid resistance to the preparation; It also has a taste masking effect.
なお、固形製剤に対するワックス類による処理は、従来
から固形製剤の艶出し工程として一応は公知であるが、
この艶出し作業は、所望のワックスをいったん有機溶媒
に溶解して固形製剤に被覆し実施されるので、有機溶媒
を使用する点、また該ワックス類の使用量において本発
明とはその手段を異にする。Note that the treatment of solid preparations with waxes has been known for some time as a polishing process for solid preparations, but
This polishing work is carried out by dissolving the desired wax in an organic solvent and coating it on the solid preparation, so it differs from the present invention in the use of an organic solvent and the amount of wax used. Make it.
本発明において固形ワックスをコーティングし得る固形
製剤としては、通常の水溶性（胃溶性）または腸溶性の
フィルムコーティングを施した固形製剤、すなわち錠剤
、大剣、顆粒または細粒から適宜任意のものを選択し得
る。特に好ましい腸溶性コーティング製剤の例としては
前記ＨＰＭＣＡＳ、ＣＭＥＣまたは１才イドラギットＬ
−３０Ｄ、を基剤とした水系腸溶性コーティング製剤を
挙げることができる。In the present invention, solid preparations that can be coated with solid wax include any one of ordinary water-soluble (gastric-soluble) or enteric film-coated solid preparations, that is, tablets, large pieces, granules, or fine granules. You can choose. Particularly preferred enteric coated preparations include the HPMCAS, CMEC or 1 year old Hydragit L.
-30D, an aqueous enteric coated formulation based on.
次に、本発明において使用し得る固形ワックスは、その
融点が３０〜９０℃の範囲のものが適当である。すなわ
ち、融点が３０℃未満のものでは室温下でも液状となる
ことがあり、その取り扱いが種々厄介となり、コーティ
ング操作において作業性が悪くなり好ましくない、また
、融点が９０℃を越えるとコーティング作業時における
当該ワックスの熱溶融が充分には行われず、目的とする
固形製剤の均一なワックスコーティングを実施すること
が困難となる。もちろん、この場合において該ワックス
（コーティング基剤）に９０ ’Ｃ（融点）以上の温度
をかければ、前記ワックスの熱溶融が起こり、コーティ
ングそのものは充分に実施きれるであろうが、コーティ
ングされるべき固形製剤中の生薬の安定性に悪影響を及
ぼすことが予想きれるので好ましくない。Next, the solid wax that can be used in the present invention preferably has a melting point in the range of 30 to 90°C. In other words, if the melting point is less than 30°C, it may become liquid even at room temperature, making it difficult to handle and reducing workability during coating operations, which is not preferable. The wax is not sufficiently thermally melted, making it difficult to uniformly coat the target solid preparation with wax. Of course, in this case, if the wax (coating base) is heated to a temperature of 90'C (melting point) or higher, the wax will thermally melt and the coating itself will be able to be carried out satisfactorily, but the This is not preferred because it can be expected to have an adverse effect on the stability of crude drugs in solid preparations.
使用可能なワックス類としては、油脂、ロウ、炭化水素
、高級アルコール、高級脂肪酸、多価アルコールもしく
は多価アルコールの脂肪酸エステルから選ばれる１種ま
たはこれらの２種以上の混合物であり、特に好ましいも
のとしては、各種製剤工程において汎用きれるカカオ脂
（融点３２〜３５℃）、ミツロウ（同６２〜６６℃）ま
たは力ルナラバロウ（同７８〜８４℃）を挙げることが
できる。これらのワックスは、好ましくはいったん加熱
溶融した後、適当な大きさ、形状に冷却固化して、固形
に成形したものを使用するのがよい、すなわち、上記の
とおり適当な形状に成形した固形ワックスを流動層装置
もしくはコーティングパンのような通常のコーティング
装置内で、温風により予め加熱された被コーテイング物
（錠剤、顆粒等）中に投入すれば、その被コーテイング
物の品温（および温風）により該固形ワックスが溶融、
展延し、当該コーテイング物の表面に前記ワックスの均
一な層を形成する。As waxes that can be used, one type selected from fats and oils, waxes, hydrocarbons, higher alcohols, higher fatty acids, polyhydric alcohols, and fatty acid esters of polyhydric alcohols, or a mixture of two or more of these types are particularly preferred. Examples include cacao butter (melting point: 32-35°C), beeswax (melting point: 62-66°C), and luna butter wax (melting point: 78-84°C), which are commonly used in various formulation processes. It is preferable to use these waxes that have been heated and melted, then cooled and solidified into an appropriate size and shape, and then molded into a solid form.In other words, solid waxes that have been molded into an appropriate shape as described above are used. If the material to be coated (tablets, granules, etc.) is preheated by hot air in a normal coating device such as a fluidized bed device or a coating pan, the temperature of the material to be coated (and the hot air ) melts the solid wax,
It spreads to form a uniform layer of the wax on the surface of the coating.
本発明の場合、前記固形ワックスの好ましい被覆量は、
被コーテイング物、すなわちフーティングを施すべき固
形製剤に対して０．２〜２．０重量％の範囲である。固
形ワックスの被覆量が０゜２重量％未満では目的とする
耐酸性の向上および／または苦味のマスキング等を充分
に達成することができず、また、その被覆量が２．０重
量％を越えるとコーティング製剤における生薬の溶出が
著しく遅延するので、共に好ましくない。In the case of the present invention, the preferred coating amount of the solid wax is as follows:
The amount is in the range of 0.2 to 2.0% by weight based on the object to be coated, that is, the solid preparation to which footing is to be applied. If the amount of solid wax coated is less than 0.2% by weight, the desired improvement in acid resistance and/or masking of bitterness cannot be achieved sufficiently, and if the amount of solid wax coated exceeds 2.0% by weight. Both are undesirable because the dissolution of crude drugs in coated preparations is significantly delayed.
ところで、このようなワックスコーティングをしたとき
、特にカカオ脂のような低融点の７ノクスで処理した場
合には、処理後のベトフキ感をなくすために所望により
該フーティング製剤に対して例えば軽質無水ケイ厳、タ
ルク、ステアリン酸マグネシウム等の微粉体を添加して
もよい。By the way, when such wax coating is applied, especially when treated with low melting point 7x such as cacao butter, if desired, the footing preparation may be coated with, for example, a light anhydrous coating in order to eliminate the sticky feeling after treatment. Fine powder of silica, talc, magnesium stearate, etc. may be added.
本発明方法の実施は、通常のコーティング作業に汎用さ
れる公知の流動層コーティング装置またはコーティング
パン装置を用いて容易に行われる。The method of the present invention can be easily carried out using known fluidized bed coating equipment or coating pan equipment commonly used in conventional coating operations.
以下実施例により本発明をさらに具体的に説明する。The present invention will be explained in more detail with reference to Examples below.
実施例１
直径０．８ａｎのパンクレアチンを含有する円柱状顆粒
１００ｋｇを流動層コーティング装置（ブラッド社製Ｗ
ＳＧ−６０型）に入れ、水分散系腸溶性基剤）ＩＰＭｃ
Ａｓ： １００ ｇ、クエン酸トリエチル：３０ｇおよ
び精製水１７０ ｇ組成の腸溶コーテイング液を下記の
条件でスプレーし、Ｍｆ１ｇ層１６重量％を被覆形成し
た後スプレーを停止し、次いで下記の条件により後乾燥
する。乾燥後、粒状のミツロウ８００ｇを投入し、１０
分間流動させ、流動停止直前に軽質無水ケイ酸２５０ｇ
を添加する。Example 1 100 kg of cylindrical granules containing pancreatin with a diameter of 0.8 ann were coated in a fluidized bed coating device (W manufactured by Blood Co., Ltd.).
SG-60 type) and water-dispersed enteric base) IPMc.
An enteric coating solution containing 100 g of As, 30 g of triethyl citrate, and 170 g of purified water was sprayed under the following conditions, and after forming a coating of 16% by weight of the Mf1g layer, the spraying was stopped. dry. After drying, add 800g of granular beeswax and
250 g of light anhydrous silicic acid immediately before stopping the flow.
Add.
このようにして製した腸溶性コーティング製剤は、前記
クエン酸トリエチルの苦味をほぼ完全に消失し得ると共
にその耐酸性も充分に向上したものであることが確認さ
れた。It was confirmed that the enteric coated preparation thus produced could almost completely eliminate the bitter taste of triethyl citrate and had sufficiently improved acid resistance.
腸溶コーティングの条件 ・送風温度二８０℃ 送風風量： ４０ ｍ”７分 スプレー液量ニア００ｇ／分 スプレー液温：１５℃ スプレー時間＝３時間１５分 後乾燥条件 。Enteric coating conditions ・Air blowing temperature 280℃ Blow air volume: 40 m”7 minutes Spray liquid volume near 00g/min Spray liquid temperature: 15℃ Spray time = 3 hours 15 minutes Post-drying conditions.
・送風温度：８０”Ｃ
・送ＪＡ′ｉＡ量： ４０ ｍ”７分
・送風時間：４０分
耐酸性試験結果
６％液ＰＨ７，０に溶Ｆして、１１１定したアミラーゼ
力価に対し、緩衝液Ｐ）１３．０で１時間揺動後、咲衝
液ＰＨ７，０に移して溶解させたときの力価を測定した
（力価の残存率）、結果は次の通りである。・Blowing temperature: 80"C ・Blowing JA'iA amount: 40 m" 7 minutes ・Blowing time: 40 minutes Acid resistance test result Dissolved in 6% solution pH 7.0 F, 111 For amylase titer determined, After rocking in buffer solution P) 13.0 for 1 hour, it was transferred to Sakicho solution pH 7.0 and dissolved, and the titer was measured (residual titer rate). The results are as follows.
ミツロウコーティング前：８５％
ミツロウコーティング後＝９４．７％
実施例２
直径０．７ｒｍのアスピリンを含有する円柱状顆粒５−
を流動層コーティング装置〔（株）大川原製作所製ＷＳ
Ｇ−５型〕に入れ、有機溶媒系の腸溶性基剤′オイドラ
ギ／トＬ１００ｐ（商品名）７０区、グリセリン脂肪酸
エステル２０ｇ１タルク４０ｇ１エタノール４００ｇお
よびジクロルメタン４７０ｇからなるコーテイング液を
下記の条件でスプレーし、腸溶性コーティング１を１５
重量％まで被覆する。その後スプレーを停止し、乾燥す
る０次いで、カカオ脂４０ｇをきらに投入し、５分間流
動させる。ｔＮ動停止前に軽質無水ケイ酸１５ｇを添加
する。このカカオ脂によるフーティングによってかかる
製剤の耐酸性は明らかに向上し、またアスピリンの経時
分Ｓにより発生する酢酸臭の発生時期も延長した。Before beeswax coating: 85% After beeswax coating = 94.7% Example 2 Cylindrical granules containing aspirin with a diameter of 0.7rm 5-
Fluidized bed coating equipment [WS made by Okawara Seisakusho Co., Ltd.]
Type G-5] and sprayed with a coating solution consisting of an organic solvent-based enteric base Eudragi/To L100p (trade name) 70 sections, 20 g of glycerin fatty acid ester, 40 g of talc, 400 g of ethanol, and 470 g of dichloromethane under the following conditions. , enteric coating 1 to 15
Cover up to % by weight. After that, stop spraying and let it dry.Next, 40g of cacao butter is put into the kira and allowed to flow for 5 minutes. 15 g of light anhydrous silicic acid is added before stopping the N operation. Footing with cocoa butter clearly improved the acid resistance of the preparation, and also extended the period of acetic acid odor produced by aspirin over time.
腸溶コーティングの条件
・送風温度：４０’Ｃ
・送風風量：５ｍ”７分
・スプレー液量：４０ｇ／分
・スプレー液温：室温
・スプレー時間：２時間４０分
喪炙燥逢詐
・送風温度ニア０℃
・送！ｊＬ風量：５ｍ’／分
・送風時間：１５分
１酸性星鳳亙り
緩衝液ＰＨ１，５で１時間揺動後のアスピリンの溶出率
。Conditions for enteric coating ・Blow temperature: 40'C ・Blow air volume: 5m" 7 minutes ・Spray liquid amount: 40 g/min ・Spray liquid temperature: Room temperature ・Spray time: 2 hours 40 minutes ・Blow temperature Near 0°C ・Blow!jL Air volume: 5 m'/min ・Blow time: 15 minutes 1 Elution rate of aspirin after rocking for 1 hour with acidic Seiho Kage buffer solution PH1.5.
カカオ脂コーティング前：９．７％
カカオ脂コーティング後：４．２％
実施例３
［径０．６ｍのセフ７レキシンを含有する円形状顯粒５
−を流動着コーティング装置ｆ（実施例２と同型＊＞に
入れ、実施例１の場合と同じ水分散系腸溶基剤）！ＰＭ
ＣＡ５１００ ｇ、クエン酸トリエチル３０ｇ、タルク
３０ｇおよび精製水８４０ｇ組成のコーテイング液を下
記の条件でスプレーし、腸溶性コーティング層を３５重
量％被覆した後、スプレーを停止し、後乾燥する。乾燥
後、ミツロウとステアリン酸の等置部合物を５４ｇ投入
して５分間流動する。流動停止前にタルク１５ｇを添加
する。この混合ワックスの被覆により該腸溶性製剤の耐
酸性は下記に示すとおり明らかに向上し、その生薬の溶
出性にも遅延は見られなかった。Before coating with cacao butter: 9.7% After coating with cacao butter: 4.2% Example 3 [Circular shaped grains 5 containing Cef7 Rexin with a diameter of 0.6 m
- is placed in a fluidized coating device f (same type as in Example 2 *>, with the same water-dispersed enteric base as in Example 1)! PM
A coating solution containing 5100 g of CA, 30 g of triethyl citrate, 30 g of talc, and 840 g of purified water was sprayed under the following conditions to cover 35% by weight of the enteric coating layer, and then the spraying was stopped and the sample was dried. After drying, 54 g of an equidistant mixture of beeswax and stearic acid was added and allowed to flow for 5 minutes. Add 15 g of talc before stopping the flow. By coating with this mixed wax, the acid resistance of the enteric-coated preparation was clearly improved as shown below, and no delay was observed in the dissolution of the crude drug.
コーティングの条 ・送風温度：６０℃ ・送風風量：５ｍ”７分 ・スプレー液量７９０ｇ／分 ・スプレー液温：１５℃ ・スプレー時間：２時間１５分 聚整盈圭作 ・送風温度二８５℃ ・送風風量：５ｍ”７分 ・送風時間：２５分。Coating strip ・Blow temperature: 60℃ ・Airflow volume: 5m” 7 minutes ・Spray liquid amount 790g/min ・Spray liquid temperature: 15℃ ・Spray time: 2 hours 15 minutes Keisaku Jusei ・Air blowing temperature 285℃ ・Airflow volume: 5m” 7 minutes ・Air blowing time: 25 minutes.
鮭１ｊＪす１区！
日局第２法による緩衝液Ｐ）１５．５で２時間後のセフ
ァレキシンの溶出率。Salmon 1j Jsu 1 ward! Elution rate of cephalexin after 2 hours with buffer P) 15.5 according to Method 2 of the Japanese Pharmacopoeia.
混合ワックスコーティング前＝４．３％混合ワックスコ
ーティング後：１．２％ｌ旦二二に思瀦１
日局第２法による緩衝液ＰＨ６，５でのセファレキシン
の溶出速度を測定したところ下表のような結果を得た。Before mixed wax coating = 4.3% After mixed wax coating: 1.2% l The elution rate of cephalexin in buffer pH 6.5 was measured according to the second method of the Japanese Pharmacopoeia, and the table below shows I got similar results.
実施例４
直径７．０ｍ、重量１２０ｍｇの活性ビタミンＢ＋を含
有する錠剤５万錠を、バッフル付きコーティングパン〔
（株）菊水製作所製〕に入れ、下記の組成のフィルムコ
ーテイング液を３０ｇ／分でスプレーして、水溶性フィ
ルム層４ｍｇ／錠を被覆し、後乾燥する。乾燥後、ミツ
ロウ３０ｇを投入し、１０分間パンを回転きせた後軽質
無水ケイ酸１’Ｏｇを添加して放冷する。Example 4 50,000 tablets containing active vitamin B+ with a diameter of 7.0 m and a weight of 120 mg were placed in a coating pan with a baffle.
(manufactured by Kikusui Seisakusho Co., Ltd.) and sprayed with a film coating solution having the following composition at a rate of 30 g/min to coat a water-soluble film layer of 4 mg/tablet, followed by drying. After drying, 30 g of beeswax was added, and after rotating the pan for 10 minutes, 1'Og of light anhydrous silicic acid was added and allowed to cool.
このミツロウでのコーティングによりビタミンＢ、の苦
味は充分にマスクきれ、かつ該錠剤の刻印も鮮明なもの
であった。The coating with beeswax sufficiently masked the bitter taste of vitamin B, and the markings on the tablets were also clear.
フィルム°の組成（１ｋｇ当りの組成）ヒドロキシプロ
ピルセルロース（ＲＰＣ−５Ｌ ）００ｇ
マクロゴール６０００ （商品名） １５ｇタルク
２０ｇエタノール
４５９．５ ｇ精製水
４０５．５ ｇ溶コーティングの条件
・送風温度＝５０℃
・送風風量：１．５ｍ”７分
・スプレー液量：３０ｇ／分
・スプレー液温：室温
・スプレー時間：５５分
東監盈逢丑
・送風温度＝８０℃
・送ｊＬ風量：１．５ｍ’／分
・送風時間＝２０分
〔発明の効果〕
以上詳述したとおり本発明方法によれば、水溶性（胃溶
性）または腸溶性のフィルムコーティングを施した固形
製剤に均一なワックス層を形成することができるので、
前記水系腸溶基剤の被覆厚みは、従来の有機溶媒系皮膜
の厚みと同等もしくはそれ以下でも満足する耐酸性を示
すと共に、前記腸溶性皮膜の苦味等をマスクすることが
できる。なお、このときの生薬の溶出の延長は殆ど見ら
れず、またワックス処理後の粘着性によるコーティング
製剤相互の凝集といった不都合も発生せず、かつ当然の
ことながら当該製剤の艶も良好なものとなる。Composition of film (composition per 1 kg) Hydroxypropylcellulose (RPC-5L) 00g Macrogol 6000 (product name) 15g talc 20g ethanol
459.5 g purified water
Conditions for 405.5 g melt coating - Air blowing temperature = 50℃ - Blowing air volume: 1.5 m" 7 minutes - Spray liquid amount: 30 g / minute - Spray liquid temperature: room temperature - Spray time: 55 minutes Air blowing temperature = 80°C ・Blowing jL air volume: 1.5 m'/min ・Blowing time = 20 minutes [Effects of the invention] As detailed above, according to the method of the present invention, water-soluble (gastric-soluble) or enteric-coated film A uniform wax layer can be formed on coated solid preparations, so
Even if the coating thickness of the water-based enteric base is equal to or less than the thickness of conventional organic solvent-based coatings, it exhibits satisfactory acid resistance and can mask the bitterness and the like of the enteric coating. At this time, there was almost no prolongation of the elution of the crude drug, and there was no inconvenience such as aggregation of the coating preparations due to their stickiness after wax treatment, and the gloss of the preparations was naturally good. Become.
従って、本発明によれば、従来より主として矯味、矯臭
を目的として実施される水溶性フィルムコーティング製
剤および有機溶媒系で被覆された腸溶性フィルムコーテ
ィング製剤停におけるそれぞれのフィルムフーティング
量を可及的に減少することができる。特に、苦味のマス
クを目的として水溶性フィルムコーティングきれた刻印
付錠剤”ｌ’７）る場合には、従来方式のコーティング
では、ややもするとその刻印部がコーティング層に埋没
して不鮮明になることがあったが、本発明方法によれば
前述したきおり比較的薄いコーティング皮膜で矯味が達
成されるので、かかる不都合は解消される。加えて、本
発明方法は特殊な溶媒を使用することなく、従来公知の
汎用型コーティング装置を用いて実施することができる
ので、その実用的効果は多大かつ顕著である。Therefore, according to the present invention, the amount of film footing in water-soluble film-coated preparations and enteric film-coated preparations coated with organic solvents, which have conventionally been mainly used for taste correction and odor correction, can be reduced as much as possible. can be reduced to In particular, when using stamped tablets that have been coated with a water-soluble film to mask bitterness, with conventional coating methods, the stamped area may become buried in the coating layer and become unclear. However, according to the method of the present invention, such inconveniences are eliminated because taste masking is achieved with the aforementioned comparatively thin coating film.In addition, the method of the present invention does not require the use of special solvents. Since it can be carried out using a conventionally known general-purpose coating device, its practical effects are great and remarkable.
Claims (3)
ィングを施した固形製剤に、融点３０〜９０℃の固形ワ
ックスを熱溶融法により被覆することを特徴とする固形
製剤のコーティング法。(1) A method for coating a solid preparation, which comprises coating a solid preparation coated with a water-soluble (gastric-soluble) or enteric film coating with a solid wax having a melting point of 30 to 90°C by a hot melting method.
コール、高級脂肪酸、多価アルコールもしくは多価アル
コールの脂肪酸エステルの群から選ばれた１種または２
種以上の混合物である特許請求の範囲第（１）項記載の
コーティング法。(2) The solid wax is one or two selected from the group of fats and oils, waxes, hydrocarbons, higher alcohols, higher fatty acids, polyhydric alcohols, and fatty acid esters of polyhydric alcohols.
The coating method according to claim (1), which is a mixture of more than one species.
０重量％被覆するものである特許請求の範囲第（１）項
記載のコーティング法。(3) Add 0.2 to 2.0% of solid wax to the solid preparation.
The coating method according to claim (1), wherein the coating method is 0% by weight.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP16925686A JPS6327423A (en) | 1986-07-17 | 1986-07-17 | Coating method for solid pharmaceutical |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP16925686A JPS6327423A (en) | 1986-07-17 | 1986-07-17 | Coating method for solid pharmaceutical |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS6327423A true JPS6327423A (en) | 1988-02-05 |
Family
ID=15883138
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP16925686A Pending JPS6327423A (en) | 1986-07-17 | 1986-07-17 | Coating method for solid pharmaceutical |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6327423A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01287021A (en) * | 1988-05-13 | 1989-11-17 | Shin Etsu Chem Co Ltd | Preparation of wax-coated drug preparation |
| JPH01287020A (en) * | 1988-05-13 | 1989-11-17 | Shin Etsu Chem Co Ltd | Wax-coated slowly releasing drug preparation |
| JPH0240263A (en) * | 1988-07-27 | 1990-02-09 | Kounoshima Kasei Kk | Coating method |
| WO2001070201A1 (en) * | 2000-03-23 | 2001-09-27 | Shionogi & Co., Ltd. | Enteric granular preparations of hardly water soluble drugs characterized by containing water-repellent component |
| JP2005334122A (en) * | 2004-05-25 | 2005-12-08 | Shionogi & Co Ltd | Method for coating tablet |
| JPWO2005039538A1 (en) * | 2003-10-29 | 2007-11-22 | 塩野義製薬株式会社 | Method for producing coated preparation with improved unpleasant taste |
-
1986
- 1986-07-17 JP JP16925686A patent/JPS6327423A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01287021A (en) * | 1988-05-13 | 1989-11-17 | Shin Etsu Chem Co Ltd | Preparation of wax-coated drug preparation |
| JPH01287020A (en) * | 1988-05-13 | 1989-11-17 | Shin Etsu Chem Co Ltd | Wax-coated slowly releasing drug preparation |
| JPH0240263A (en) * | 1988-07-27 | 1990-02-09 | Kounoshima Kasei Kk | Coating method |
| WO2001070201A1 (en) * | 2000-03-23 | 2001-09-27 | Shionogi & Co., Ltd. | Enteric granular preparations of hardly water soluble drugs characterized by containing water-repellent component |
| JPWO2005039538A1 (en) * | 2003-10-29 | 2007-11-22 | 塩野義製薬株式会社 | Method for producing coated preparation with improved unpleasant taste |
| JP2005334122A (en) * | 2004-05-25 | 2005-12-08 | Shionogi & Co Ltd | Method for coating tablet |
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