JPS6317821A - Flavoring oral pharmaceutical - Google Patents
Flavoring oral pharmaceuticalInfo
- Publication number
- JPS6317821A JPS6317821A JP61162988A JP16298886A JPS6317821A JP S6317821 A JPS6317821 A JP S6317821A JP 61162988 A JP61162988 A JP 61162988A JP 16298886 A JP16298886 A JP 16298886A JP S6317821 A JPS6317821 A JP S6317821A
- Authority
- JP
- Japan
- Prior art keywords
- drug
- unpleasant taste
- antibiotic substance
- bioavailability
- soft capsules
- 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
- 239000003814 drug Substances 0.000 claims abstract description 27
- 229940079593 drug Drugs 0.000 claims abstract description 26
- 239000007901 soft capsule Substances 0.000 claims abstract description 10
- 238000002360 preparation method Methods 0.000 claims description 9
- 235000019640 taste Nutrition 0.000 abstract description 15
- 239000000203 mixture Substances 0.000 abstract description 5
- 239000000126 substance Substances 0.000 abstract description 5
- 230000000873 masking effect Effects 0.000 abstract description 4
- 239000002202 Polyethylene glycol Substances 0.000 abstract description 2
- 238000010521 absorption reaction Methods 0.000 abstract description 2
- 229960005091 chloramphenicol Drugs 0.000 abstract description 2
- WIIZWVCIJKGZOK-RKDXNWHRSA-N chloramphenicol Chemical compound ClC(Cl)C(=O)N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 WIIZWVCIJKGZOK-RKDXNWHRSA-N 0.000 abstract description 2
- 239000003120 macrolide antibiotic agent Substances 0.000 abstract description 2
- -1 medium-chain fatty acid triglycerides Chemical class 0.000 abstract description 2
- 239000002245 particle Substances 0.000 abstract description 2
- 229920001223 polyethylene glycol Polymers 0.000 abstract description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 abstract description 2
- 239000008158 vegetable oil Substances 0.000 abstract description 2
- 230000003115 biocidal effect Effects 0.000 abstract 4
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 231100000252 nontoxic Toxicity 0.000 abstract 2
- 230000003000 nontoxic effect Effects 0.000 abstract 2
- 239000004098 Tetracycline Substances 0.000 abstract 1
- 229960004111 buformin Drugs 0.000 abstract 1
- XSEUMFJMFFMCIU-UHFFFAOYSA-N buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 abstract 1
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 abstract 1
- 229960001076 chlorpromazine Drugs 0.000 abstract 1
- OEGDFSLNGABBKJ-UHFFFAOYSA-N etafenone Chemical compound CCN(CC)CCOC1=CC=CC=C1C(=O)CCC1=CC=CC=C1 OEGDFSLNGABBKJ-UHFFFAOYSA-N 0.000 abstract 1
- 229960002180 tetracycline Drugs 0.000 abstract 1
- 229930101283 tetracycline Natural products 0.000 abstract 1
- 235000019364 tetracycline Nutrition 0.000 abstract 1
- 150000003522 tetracyclines Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 description 11
- 239000002775 capsule Substances 0.000 description 7
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 108010010803 Gelatin Proteins 0.000 description 4
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 229920000159 gelatin Polymers 0.000 description 4
- 239000008273 gelatin Substances 0.000 description 4
- 235000019322 gelatine Nutrition 0.000 description 4
- 235000011852 gelatine desserts Nutrition 0.000 description 4
- 235000019658 bitter taste Nutrition 0.000 description 3
- 229960003276 erythromycin Drugs 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 2
- 229920000858 Cyclodextrin Polymers 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 238000005354 coacervation Methods 0.000 description 2
- 239000003240 coconut oil Substances 0.000 description 2
- 235000019864 coconut oil Nutrition 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 235000012343 cottonseed oil Nutrition 0.000 description 2
- 239000002385 cottonseed oil Substances 0.000 description 2
- 239000003456 ion exchange resin Substances 0.000 description 2
- 229920003303 ion-exchange polymer Polymers 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 239000003094 microcapsule Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 2
- 230000001953 sensory effect Effects 0.000 description 2
- 229920001059 synthetic polymer Polymers 0.000 description 2
- AKUVRZKNLXYTJX-UHFFFAOYSA-N 3-benzylazetidine Chemical compound C=1C=CC=CC=1CC1CNC1 AKUVRZKNLXYTJX-UHFFFAOYSA-N 0.000 description 1
- 241000283084 Balaenoptera musculus Species 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000238366 Cephalopoda Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- DMUAPQTXSSNEDD-QALJCMCCSA-N Midecamycin Chemical compound C1[C@](O)(C)[C@@H](OC(=O)CC)[C@H](C)O[C@H]1O[C@H]1[C@H](N(C)C)[C@@H](O)[C@H](O[C@@H]2[C@H]([C@H](OC(=O)CC)CC(=O)O[C@H](C)C/C=C/C=C/[C@H](O)[C@H](C)C[C@@H]2CC=O)OC)O[C@@H]1C DMUAPQTXSSNEDD-QALJCMCCSA-N 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 244000046052 Phaseolus vulgaris Species 0.000 description 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 description 1
- 235000019484 Rapeseed oil Nutrition 0.000 description 1
- 235000019774 Rice Bran oil Nutrition 0.000 description 1
- 235000019485 Safflower oil Nutrition 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 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
- 235000019486 Sunflower oil Nutrition 0.000 description 1
- 239000010775 animal oil Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 238000004166 bioassay Methods 0.000 description 1
- 239000010495 camellia oil Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 229960001657 chlorpromazine hydrochloride Drugs 0.000 description 1
- 235000012716 cod liver oil Nutrition 0.000 description 1
- 239000003026 cod liver oil Substances 0.000 description 1
- 235000005687 corn oil Nutrition 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 239000008157 edible vegetable oil Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 229940013317 fish oils Drugs 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- XJSFLOJWULLJQS-NGVXBBESSA-N josamycin Chemical compound CO[C@H]1[C@H](OC(C)=O)CC(=O)O[C@H](C)C\C=C\C=C\[C@H](O)[C@H](C)C[C@H](CC=O)[C@@H]1O[C@H]1[C@H](O)[C@@H](N(C)C)[C@H](O[C@@H]2O[C@@H](C)[C@H](OC(=O)CC(C)C)[C@](C)(O)C2)[C@@H](C)O1 XJSFLOJWULLJQS-NGVXBBESSA-N 0.000 description 1
- 229960004144 josamycin Drugs 0.000 description 1
- 229950007634 kitasamycin Drugs 0.000 description 1
- 238000004898 kneading Methods 0.000 description 1
- XYJOGTQLTFNMQG-KJHBSLKPSA-N leucomycin V Chemical compound CO[C@H]1[C@H](O)CC(=O)O[C@H](C)C\C=C\C=C\[C@H](O)[C@H](C)C[C@H](CC=O)[C@@H]1O[C@H]1[C@H](O)[C@@H](N(C)C)[C@H](O[C@@H]2O[C@@H](C)[C@H](O)[C@](C)(O)C2)[C@@H](C)O1 XYJOGTQLTFNMQG-KJHBSLKPSA-N 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229960002757 midecamycin Drugs 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 238000000554 physical therapy Methods 0.000 description 1
- 239000008165 rice bran oil Substances 0.000 description 1
- 235000005713 safflower oil Nutrition 0.000 description 1
- 239000003813 safflower oil Substances 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000010686 shark liver oil Substances 0.000 description 1
- 229940069764 shark liver oil Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000002600 sunflower oil Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 229940072172 tetracycline antibiotic Drugs 0.000 description 1
- 239000010496 thistle oil Substances 0.000 description 1
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 239000010698 whale oil Substances 0.000 description 1
- 239000010497 wheat germ oil Substances 0.000 description 1
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野コ
本発明は矯味経口製剤に関し、さらに詳しくは、薬物の
不快な味を除去すると共に、小児においても服用しやす
く、かつバイオアベイラビリティ−の高い矯味経口製剤
に関する。DETAILED DESCRIPTION OF THE INVENTION [Field of Industrial Application] The present invention relates to a taste masking oral preparation, and more specifically, to a taste masking oral preparation that eliminates the unpleasant taste of drugs, is easy to take even for children, and has high bioavailability. Concerning oral preparations.
［従来の技術］
従来、不快な味を呈する薬物の矯味製剤技術としては、
この種の薬物をイオン交換樹脂に吸着させる方法（特開
昭６０−６７４１８号公報）、サイクロデキストリンに
吸着させる方法（特開昭５５−７１４５６号公報）、合
成高分子化合物や脂質に練り込む方法（特開昭５５−５
４８７号公報、米国特許第３２７９９９４号公報）、コ
アセルベーション法でマイクロカプセルに封入する方法
（米国特許第３９２２３７９号公報）等が知られている
。[Prior Art] Conventionally, taste-correcting formulation technology for drugs that exhibit an unpleasant taste includes:
A method of adsorbing this kind of drug to an ion exchange resin (Japanese Unexamined Patent Publication No. 60-67418), a method of adsorbing it to cyclodextrin (Japanese Unexamined Patent Publication No. 55-71456), and a method of incorporating it into synthetic polymer compounds or lipids. (Unexamined Japanese Patent Publication No. 55-5
487, US Pat. No. 3,279,994), and a method of encapsulating microcapsules by coacervation method (US Pat. No. 3,922,379).
［発明が解決しようとする問題点コ これら従来の方法には下記の問題点がある。[The problem that the invention aims to solve] These conventional methods have the following problems.
（１）不快な味を呈する薬物をイオン交換樹脂に吸着さ
せる方法は、用いる薬物が水に難溶性かまたは非イオン
性である場合には適用できない。(1) The method of adsorbing a drug with an unpleasant taste onto an ion exchange resin cannot be applied when the drug used is sparingly soluble in water or nonionic.
（２）サイクロデキストリンに包接させる方法は、包接
できる分子サイズに制限があり、用いる薬物が特殊であ
る場合にのみ適用される。(2) The method of inclusion in cyclodextrin has limitations on the molecular size that can be included, and is only applicable when the drug to be used is special.
（３）合成高分子化合物や脂質に練り込む方法は基剤の
表面にも薬物が露出しているので、不快な味の強い物質
には不適当である。(3) The method of kneading into synthetic polymer compounds or lipids exposes the drug to the surface of the base material, so it is not suitable for substances with a strong unpleasant taste.
（４）コアセルベーション法でマイクロカプセルに封入
する方法は、壁材としてゼラチン等の水溶性基剤を選択
すると、服用時間中でカプセルがとけて不快な味の薬物
が出てしまう。また、エチルセルロース等の水不溶性基
剤を選択すれば、不快な味を改良できるが、服用した場
合、薬物の吸収が抑制きれてしまう。(4) If a water-soluble base such as gelatin is selected as the wall material in the coacervation method of enclosing the drug in microcapsules, the capsule will melt during the administration period, releasing the drug with an unpleasant taste. Moreover, if a water-insoluble base such as ethylcellulose is selected, the unpleasant taste can be improved, but absorption of the drug will be suppressed when taken.
（５）一般的な手法により作られるソフトカプセルでは
、カプセルが大きくなるため、小児などには飲みにくく
不向きである。(5) Soft capsules made using conventional methods are large and difficult to swallow for children.
［問題点を解決するための手段］
本発明者らは、前記問題点を解決すべく、薬物を油性基
剤に溶解あるいは懸濁して微粒ソフトカプセルに充填し
、これを前記と同じかまたは異なる油性基剤に分散する
と、前記目的を達成することができることを見出し本発
明に到達した。[Means for Solving the Problems] In order to solve the above-mentioned problems, the present inventors dissolved or suspended a drug in an oily base and filled it into microscopic soft capsules. The present inventors have discovered that the above object can be achieved by dispersing it in a base material.
本発明は、薬物を封入した微粒ソフトカプセルを薬理学
上無害の油性基剤に分散した矯味経口製剤である。The present invention is a taste-corrected oral preparation in which microscopic soft capsules encapsulating a drug are dispersed in a pharmacologically harmless oily base.
本発明において、微粒ソフトカプセルは、例えばゼラチ
ンを主体としてこれにグリセリン、ソルビトール等の保
水剤を加えて、所定の含水率のカプセルとなるように調
製する。In the present invention, the microscopic soft capsules are prepared, for example, by adding a water retaining agent such as glycerin or sorbitol to gelatin as a main ingredient so as to have a predetermined water content.
また、その製造方法には、例えば気中落下方式あるいは
液中落下方式がある。Moreover, the manufacturing method includes, for example, an air drop method or a submerged drop method.
カプセル内部に充填する内容物については、薬物が油性
基剤に溶がしていても、懸濁していても良い。Regarding the contents filled inside the capsule, the drug may be dissolved or suspended in an oily base.
また、薬物としては、マクロライド系抗生物質（例えば
エリスロマイシン、ミデカマイシン、キタサマイシン、
ジョサマイシン等）、テトラサイクリン系抗生物質、ク
ロラムフェニコール等ノ抗生物質や塩酸クロルプロマジ
ン、塩酸エタフエノン、塩酸ブフオルミン等の合成医薬
品等不快な味を呈する薬物が挙げられる。In addition, as drugs, macrolide antibiotics (e.g. erythromycin, midecamycin, kitasamycin,
Drugs that have an unpleasant taste include antibiotics such as josamycin, tetracycline antibiotics, and chloramphenicol, and synthetic drugs such as chlorpromazine hydrochloride, ethaphenone hydrochloride, and bufolumin hydrochloride.
さらに、油性基剤についても、薬理学上無害なものであ
ればいずれを用いても良く、各種食用油（例えばオリー
ブ油、サフラワー油、とうもろこし油、ひまわり油、綿
実油、つばき油、米ぬか油、大豆油、ごま油、小麦胚芽
油、ヤシ油、落花生油、なたね油等の植物油；イカ油、
ヤシ油等の魚油、サメ肝油、タラ肝油等の肝油；アザヤ
シ油、シロナガス鯨油等の海獣油等）、中鎖脂肪酸トリ
グリセライド［例えばカプリル酸トリグリセライド、カ
プリン酸トリグリセライド等；市販品としてはバナセー
ト８１０（商品名、日本抽選（株）製）があるコ、ポリ
エチレングリコール等が挙げられる。これらは単独で用
いても良いし、数種を混合して用いても良い。Furthermore, any oily base may be used as long as it is pharmacologically harmless, and various edible oils (e.g., olive oil, safflower oil, corn oil, sunflower oil, cottonseed oil, camellia oil, rice bran oil, Vegetable oils such as bean oil, sesame oil, wheat germ oil, coconut oil, peanut oil, rapeseed oil; squid oil,
fish oils such as coconut oil; liver oils such as shark liver oil and cod liver oil; marine animal oils such as thistle oil and blue whale oil; etc.), medium chain fatty acid triglycerides [e.g. caprylic acid triglyceride, capric acid triglyceride, etc.; commercially available products include vanacetate 810 (commercial products) Polyethylene glycol, etc. (manufactured by Nippon Lottery Co., Ltd.) can be mentioned. These may be used alone or in combination.
また油性基剤に配合する前記微粒ソフトカプセルの粒径
は、通常１ｍｍ以下であり、好ましくは０．８１１１ｆ
ｆｌ以下である。Further, the particle size of the fine soft capsules blended into the oily base is usually 1 mm or less, preferably 0.8111f.
It is below fl.
小児の服用を容易にするため、この油性基剤にショ糖等
の甘味剤を配合することも可能である。In order to make it easier for children to take it, it is also possible to add a sweetener such as sucrose to this oily base.
［発明の効果］
本発明の製剤は、服用して不快な味を感じる被験者がほ
とんど無く、またピーグル大での試験の結果、そのバイ
オアベイラビリティ−は薬物の原末と同等であることが
確認きれた。[Effects of the Invention] Almost no subjects felt an unpleasant taste after taking the preparation of the present invention, and the results of the test at Peagle University confirmed that its bioavailability was equivalent to that of the drug bulk powder. Ta.
本発明により、不快な味を呈する薬物のマスキング効果
とバイオアベイラビリティ−の優れた製剤を提供するこ
とができる。According to the present invention, it is possible to provide a formulation with excellent masking effect and bioavailability for drugs that exhibit an unpleasant taste.
［実施例］
以下、実施例および試験例を示してこの発明をさらに具
体的に説明する。[Examples] The present invention will now be described in more detail with reference to Examples and Test Examples.
〈実施例１）
不快な味を呈する薬物として、６−０−メチルエリスロ
マイシンＡ（以下ＴＥ−０３１と称す）を用いた。<Example 1> 6-0-methylerythromycin A (hereinafter referred to as TE-031) was used as a drug exhibiting an unpleasant taste.
バナセート８１０にＴＥ−０３１を２０重量％懸濁し、
これを直径０．５ｍｍのゼラチンソフトカプセルに内封
した。このカプセル１ｇ中に１２０ｍｇのＩＥ−０３１
を含有する。このカプセル５０ｇを軽質無水ケイ酸およ
び粉糖をそれぞれ５％配合した１５０ｍ１ｌのバナセー
ト８１０に分散し、矯味経口製剤を得た。20% by weight of TE-031 is suspended in vanasate 810,
This was encapsulated in a gelatin soft capsule with a diameter of 0.5 mm. 120mg of IE-031 in 1g of this capsule
Contains. 50 g of these capsules were dispersed in 150 ml of Vanasate 810 containing 5% each of light silicic anhydride and powdered sugar to obtain a taste-corrected oral preparation.
（実施例２）
綿実油にエリスロマイシンを２０重量％懸濁し、これを
直径０．８ｍｍのゼラチンソフトカプセルに内封した。(Example 2) Erythromycin was suspended in cottonseed oil in an amount of 20% by weight, and this was encapsulated in a gelatin soft capsule having a diameter of 0.8 mm.
このカプセル１ｇ中に１００ｍｇのエリスロマイシンを
含有する。このカプセル５０ｇを１５０ｍＱのパナセー
ト８１０に分散し、矯味経口製剤を得た。1 g of this capsule contains 100 mg of erythromycin. 50 g of this capsule was dispersed in 150 mQ of Panacet 810 to obtain a taste-corrected oral preparation.
（試験例１）
苦味の官能試験
被験者１５名にそれぞれ実施例１に準じて調製したＩＥ
−０３１として５０ｍｇ相当量の製剤を服用させ、苦た
ＴＥ−０３１として５０ｍｇ相当量の製剤を服用させ、
苦味の官能試験を実施した。評価時期は服用直後、服用
５分後の２点で、また苦味の程度は我慢できない、我慢
できるが苦い、苦くないの３点で評価した。(Test Example 1) IE prepared according to Example 1 was given to 15 bitter taste sensory test subjects.
-031 was administered in an amount equivalent to 50 mg, and bitter TE-031 was administered in an amount equivalent to 50 mg.
A sensory test for bitterness was conducted. The evaluation time was 2 points immediately after taking the drug and 5 minutes after taking the drug, and the degree of bitterness was evaluated using 3 points: intolerable, tolerable but bitter, and not bitter.
この結果を第１表に示す。The results are shown in Table 1.
第１表
（試験例２）
バイオアベイラビリティ−試験
体重１０ｋｇの雄性ピーグル犬４頭に、それぞれ実施例
１に準じて調製したＩＥ−０３１として１００ｍｇ相当
量の製剤を、水と共に投与した。血中濃度はバイオアッ
セイ法で求めた。沙に１０日間の体薬期間を置き、対照
製剤としてＩＥ−０３１の原末１００ｍｇを詰めたカプ
セルを、水と共に投与し、同様にして血中濃度を求めた
。Table 1 (Test Example 2) Bioavailability - Test A formulation equivalent to 100 mg of IE-031 prepared according to Example 1 was administered together with water to four male peagle dogs weighing 10 kg. Blood concentration was determined by bioassay method. After a 10-day period of physical therapy, a capsule filled with 100 mg of bulk powder of IE-031 was administered together with water as a control preparation, and the blood concentration was determined in the same manner.
その結果を第１図に示す。The results are shown in FIG.
第１図は本発明の製剤のバイオアベイラビリティ−を示
す濃度−時間特性図である。FIG. 1 is a concentration-time characteristic diagram showing the bioavailability of the formulation of the present invention.
Claims (1)
害の油性基剤に分散した矯味経口製剤。(1) A taste-corrected oral preparation in which microscopic soft capsules encapsulating a drug are dispersed in a pharmacologically harmless oil base.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61162988A JPS6317821A (en) | 1986-07-11 | 1986-07-11 | Flavoring oral pharmaceutical |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61162988A JPS6317821A (en) | 1986-07-11 | 1986-07-11 | Flavoring oral pharmaceutical |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS6317821A true JPS6317821A (en) | 1988-01-25 |
Family
ID=15765078
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP61162988A Pending JPS6317821A (en) | 1986-07-11 | 1986-07-11 | Flavoring oral pharmaceutical |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6317821A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63166838A (en) * | 1986-12-22 | 1988-07-11 | アストラ・レーケメデル・アクチエボラーグ | Liquid preparation for oral administration |
| US7635675B2 (en) | 2003-08-13 | 2009-12-22 | Biocon Limited | Micro-particle fatty acid salt solid dosage formulations for therapeutic agents |
-
1986
- 1986-07-11 JP JP61162988A patent/JPS6317821A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63166838A (en) * | 1986-12-22 | 1988-07-11 | アストラ・レーケメデル・アクチエボラーグ | Liquid preparation for oral administration |
| US7635675B2 (en) | 2003-08-13 | 2009-12-22 | Biocon Limited | Micro-particle fatty acid salt solid dosage formulations for therapeutic agents |
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