JP2002128705A - Medicinal basic preparation having unpleasant taste - Google Patents
Medicinal basic preparation having unpleasant tasteInfo
- Publication number
- JP2002128705A JP2002128705A JP2000322548A JP2000322548A JP2002128705A JP 2002128705 A JP2002128705 A JP 2002128705A JP 2000322548 A JP2000322548 A JP 2000322548A JP 2000322548 A JP2000322548 A JP 2000322548A JP 2002128705 A JP2002128705 A JP 2002128705A
- Authority
- JP
- Japan
- Prior art keywords
- unpleasant taste
- basic drug
- oral preparation
- aspartame
- dissolved
- 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.)
- Granted
Links
- 235000019640 taste Nutrition 0.000 title claims abstract description 39
- 238000002360 preparation method Methods 0.000 title claims abstract description 27
- 239000003814 drug Substances 0.000 claims abstract description 33
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims abstract description 16
- 108010011485 Aspartame Proteins 0.000 claims abstract description 15
- 235000010357 aspartame Nutrition 0.000 claims abstract description 15
- 239000000605 aspartame Substances 0.000 claims abstract description 15
- 229960003438 aspartame Drugs 0.000 claims abstract description 15
- 239000000203 mixture Substances 0.000 claims abstract description 13
- 239000006188 syrup Substances 0.000 claims description 10
- 235000020357 syrup Nutrition 0.000 claims description 10
- 229960002626 clarithromycin Drugs 0.000 claims description 9
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical group 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 claims description 9
- 230000001747 exhibiting effect Effects 0.000 claims description 7
- 239000007788 liquid Substances 0.000 claims description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- 239000008203 oral pharmaceutical composition Substances 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 2
- 239000000243 solution Substances 0.000 abstract description 5
- 230000000873 masking effect Effects 0.000 abstract description 3
- 239000003929 acidic solution Substances 0.000 abstract description 2
- 239000004615 ingredient Substances 0.000 abstract 1
- 235000019658 bitter taste Nutrition 0.000 description 9
- 229940079593 drug Drugs 0.000 description 5
- 230000002378 acidificating effect Effects 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 230000006866 deterioration Effects 0.000 description 3
- 230000001953 sensory effect Effects 0.000 description 3
- 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 2
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 2
- 235000019606 astringent taste Nutrition 0.000 description 2
- 230000015271 coagulation Effects 0.000 description 2
- 238000005345 coagulation Methods 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- -1 fluidizers Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 2
- 229960005190 phenylalanine Drugs 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000012085 test solution Substances 0.000 description 2
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 108010016626 Dipeptides Proteins 0.000 description 1
- 229920003148 Eudragit® E polymer Polymers 0.000 description 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 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
- 229920002472 Starch Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 229960004099 azithromycin Drugs 0.000 description 1
- MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[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 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- NEDGUIRITORSKL-UHFFFAOYSA-N butyl 2-methylprop-2-enoate;2-(dimethylamino)ethyl 2-methylprop-2-enoate;methyl 2-methylprop-2-enoate Chemical compound COC(=O)C(C)=C.CCCCOC(=O)C(C)=C.CN(C)CCOC(=O)C(C)=C NEDGUIRITORSKL-UHFFFAOYSA-N 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 229960003276 erythromycin Drugs 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 229920003121 gastrosoluble polymer Polymers 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 229960004144 josamycin Drugs 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
- 229950007634 kitasamycin Drugs 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
- 239000003120 macrolide antibiotic agent Substances 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 150000004702 methyl esters Chemical class 0.000 description 1
- 229960002757 midecamycin Drugs 0.000 description 1
- 230000007935 neutral effect Effects 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
- 239000002245 particle Substances 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、不快な味を呈する
塩基性薬物を含有する経口製剤用組成物を水に溶解又は
懸濁させたときに、該塩基性薬物に起因する不快な味を
簡易にマスキングし、服用性の改善を図った経口製剤に
関する。[0001] The present invention relates to an oral preparation composition containing a basic drug having an unpleasant taste, which is dissolved or suspended in water to remove the unpleasant taste caused by the basic drug. The present invention relates to an oral preparation which is easily masked to improve its ingestibility.
【０００２】[0002]
【従来の技術】液剤では経時的に力価、効力が低減した
り、再分散性が劣化するような薬物について、小児等が
服用し易い剤型として、用時溶解又は懸濁して用いるド
ライシロップ剤が広く普及している。そして、クラリス
ロマイシン等の不快な味を呈する塩基性薬物について
も、これを噴霧凝固造粒等によりワックスマトリックス
とし、ドライシロップ剤として提供することが可能とな
っている（特開平６−１１６１３８号公報）。こうした
塩基性薬物を含有するドライシロップ剤を塩基性域から
中性域の溶液に溶解又は懸濁させて使用する場合には、
該塩基性薬物が液中に溶出して不快な呈味が拡散するこ
とはほとんどないといえる。2. Description of the Related Art Dry syrups which are dissolved or suspended in liquid form at the time of use for drugs whose potency and potency decrease over time or whose redispersibility deteriorates are formulated into a dosage form that can be easily taken by children and the like. Are widely spread. A basic drug exhibiting an unpleasant taste, such as clarithromycin, can be formed into a wax matrix by spray coagulation granulation or the like and provided as a dry syrup (Japanese Patent Application Laid-Open No. 6-116138). ). When a dry syrup containing such a basic drug is used by dissolving or suspending it in a solution from a basic range to a neutral range,
It can be said that the basic drug is hardly eluted in the liquid and the unpleasant taste is hardly diffused.
【０００３】しかしながら、塩基性薬物を含有するドラ
イシロップ剤をジュース等の酸性液に溶解若しくは懸濁
させたとき、又は、酸性薬物とともに水に溶解若しくは
懸濁させたとき、すなわち、ドライシロップ剤が酸性液
下に溶解又は懸濁されている状態では、塩基性薬物が液
中に溶出して該薬物の不快な呈味が拡散し、服用性の悪
化を招来することがあった。[0003] However, when a dry syrup containing a basic drug is dissolved or suspended in an acidic liquid such as juice, or when dissolved or suspended in water together with an acidic drug, that is, when the dry syrup is converted into an acidic liquid. In the state where the basic drug is dissolved or suspended below, the basic drug is eluted into the liquid, and the unpleasant taste of the drug is diffused, which may cause deterioration of the ingestibility.
【０００４】[0004]
【発明が解決しようとする課題】本発明は、不快な味を
呈する塩基性薬物を含有するドライシロップ剤等の経口
製剤用組成物を、酸性液中に溶解又は懸濁させたときに
生じる不快な呈味を簡易な方法でマスキングし、服用性
の悪化を防止した経口製剤を提供することを課題とす
る。DISCLOSURE OF THE INVENTION The present invention relates to an unpleasant unpleasant taste produced when an oral pharmaceutical composition such as a dry syrup containing a basic drug exhibiting an unpleasant taste is dissolved or suspended in an acidic solution. An object of the present invention is to provide an oral preparation in which taste is masked by a simple method and deterioration of the ingestibility is prevented.
【０００５】[0005]
【課題を解決するための手段】本発明者らは、かかる課
題を解決すべく鋭意検討した結果、不快な味を呈する塩
基性薬物を含有するドライシロップ剤とアスパルテーム
を混合し、これを酸性液中に懸濁させたところ、該塩基
性薬物が呈する不快な味を顕著にマスキングしうること
を見出し、本発明を完成するに至った。Means for Solving the Problems The present inventors have made intensive studies to solve the above problems, and as a result, mixed a dry syrup containing a basic drug exhibiting an unpleasant taste with aspartame, and then mixed this with an acid solution. , The inventors found that the unpleasant taste exhibited by the basic drug can be remarkably masked, and have completed the present invention.
【０００６】すなわち，本発明は、不快な味を呈する塩
基性薬物を含有する経口製剤用組成物及びアスパルテー
ムを配合したことを特徴とする経口製剤である。That is, the present invention is an oral preparation characterized by blending a composition for oral preparation containing a basic drug exhibiting an unpleasant taste and aspartame.
【０００７】本発明において不快な味とは、苦味、渋
味、収斂味等の服用性の悪化を招来する呈味であれば特
に限定はない。このような不快な味を呈する塩基性薬物
としては、エリスロマイシン、クラリスロマイシン、キ
タサマイシン、ジョサマイシン、ミデカマイシン、ロキ
シスタマイシンおよびアジスロマイシン等のマクロライ
ド系抗生物質が挙げられる。[0007] In the present invention, the unpleasant taste is not particularly limited as long as it is a taste that causes deterioration of ingestibility such as bitterness, astringency, and astringency. Basic drugs that exhibit such an unpleasant taste include macrolide antibiotics such as erythromycin, clarithromycin, kitasamycin, josamycin, midecamycin, roxistamycin and azithromycin.
【０００８】本発明における経口製剤用組成物とは、
（ａ）不快な味を呈する塩基性薬物と胃溶性高分子化合
物を分散あるいは溶解させた低融点物質からなる複合
体、（ｂ）１０質量％から７０質量％の糖アルコールお
よび（ｃ）０．１質量％から７質量％の塩基性酸化物か
らなることを特徴とする経口製剤用組成物であって、そ
の製造方法等は、特開平６−１１６１３８号公報に記載
されている。[0008] The composition for oral preparation in the present invention includes:
(A) a complex comprising a low melting substance in which a basic drug having an unpleasant taste is dispersed or dissolved in a gastrosoluble polymer compound; (b) 10 to 70% by mass of a sugar alcohol; An oral pharmaceutical composition comprising 1% by mass to 7% by mass of a basic oxide, and its production method and the like are described in JP-A-6-116138.
【０００９】本発明におけるアスパルテームとは、アス
パラギン酸とフェニルアラニンが結合したジペプチドで
フェニルアラニンのメチルエステルであるアスパルテー
ム（α−Ｌ−アスパルチル−Ｌ−フェニルアラニンメチ
ルエステル）であるが、その誘導体であってもよい。The aspartame in the present invention is aspartame (α-L-aspartyl-L-phenylalanine methyl ester) which is a dipeptide in which aspartic acid and phenylalanine are bonded and is a methyl ester of phenylalanine, but may be a derivative thereof. .
【００１０】アスパルテームの配合量は、塩基性薬物の
呈する不快な味の種類、液中への溶出量等により異なる
ので一概には言えないが、不快な味を呈する塩基性薬物
１質量部に対して通常０．１質量部以上であり、好まし
くは０．１〜２質量部である。ただし、２質量部以上を
配合しても塩基性薬物の呈する不快な味のマスキング作
用を奏していることに何ら変わりはない。The amount of aspartame varies depending on the type of unpleasant taste presented by the basic drug, the amount of elution into the liquid, and the like, and cannot be specified unconditionally. And usually 0.1 part by mass or more, preferably 0.1 to 2 parts by mass. However, the addition of 2 parts by mass or more does not change the unpleasant taste masking action exhibited by the basic drug.
【００１１】なお、不快な味を呈する塩基性薬物として
クラリスロマイシンを含有する場合のアスパルテームの
配合量は、クラリスロマイシン１質量部に対して通常
０．１質量部以上であり、好ましくは０．２〜２質量部
であり、さらに好ましくは０．６〜１質量部である。た
だし、２質量部以上を配合してもクラリスロマイシンの
呈する苦味をマスキングしていることに何ら変わりはな
い。When clarithromycin is contained as a basic drug having an unpleasant taste, the amount of aspartame is usually 0.1 part by mass or more, preferably 0 part by mass, per 1 part by mass of clarithromycin. 0.2 to 2 parts by mass, more preferably 0.6 to 1 part by mass. However, there is no change in masking the bitterness exhibited by clarithromycin even if 2 parts by mass or more are blended.
【００１２】本発明における経口製剤は、一般的には不
快な味を呈する塩基性薬物を含有する経口製剤用組成物
とアスパルテームを混合することにより調製することが
できるが、その他に該塩基性薬物以外の医薬有効成分や
種々の製剤原料（賦形剤、結合剤、崩壊剤、流動化剤、
香料等）を配合してもよい。The oral preparation of the present invention can be prepared by mixing an aspartame with a composition for oral preparation containing a basic drug which generally gives an unpleasant taste. Other active pharmaceutical ingredients and various drug substances (excipients, binders, disintegrants, fluidizers,
Perfume, etc.).
【００１３】本発明の経口製剤の剤型としては、散剤、
顆粒剤等が挙げられるが、用時溶解又は懸濁させて使用
するドライシロップ剤について特に有効である。[0013] The dosage form of the oral preparation of the present invention includes powder,
Granules and the like can be mentioned, but it is particularly effective for dry syrups to be used after being dissolved or suspended at the time of use.
【００１４】本発明における経口製剤を溶解又は懸濁さ
せたときの溶液のｐＨは通常４〜７であり、好ましくは
５〜７である。塩基性域では、塩基性薬物が溶出せず、
不快な味を呈することがないため苦味をマスキングする
必要性がなく、また、ｐＨ４未満の強酸性域では、塩基
性薬物の溶出が著しく、アスパルテームの配合によって
は不快な呈味を充分にマスキングすることができないか
らである。The pH of the solution when the oral preparation of the present invention is dissolved or suspended is usually 4 to 7, preferably 5 to 7. In the basic range, basic drugs do not elute,
There is no need to mask bitterness because it does not give an unpleasant taste, and in the strongly acidic region of less than pH 4, the basic drug is remarkably eluted, and depending on the aspartame formulation, the unpleasant taste is sufficiently masked. Because they cannot do it.
【００１５】さらに、不快な味を呈する塩基性薬物を配
合した経口製剤（例えば、ドライシロップ剤）を水に溶
解又は懸濁させるときに、所要のアスパルテームを溶解
させることによっても該塩基性薬物の呈する不快な味を
マスキングすることができる。このときのアスパルテー
ムの使用量は、上述の経口製剤における不快な味を呈す
る塩基性薬物に対するアスパルテームの配合量と同様で
ある。Further, when an oral preparation (eg, a dry syrup) containing a basic drug exhibiting an unpleasant taste is dissolved or suspended in water, the basic drug is also exhibited by dissolving the required aspartame. Unpleasant taste can be masked. The amount of aspartame used at this time is the same as the amount of aspartame to the basic drug exhibiting an unpleasant taste in the above-mentioned oral preparation.
【００１６】[0016]
【実施例】以下に、実施例、比較例および試験例を挙げ
て本発明をより詳細に説明するが、本発明はこれらの実
施例等により限定されるものではない。EXAMPLES The present invention will be described in more detail with reference to examples, comparative examples and test examples, but the present invention is not limited to these examples.
【００１７】（実施例１） 経口製剤用組成物の製造 グリセリン脂肪酸エステル（主脂肪酸はステアリン酸
で、モノグリセリド含量は９０％以上）２００ｇを約１
００℃で融解させ、その中にオイドラギットＥ（（株）
樋口商会）３０ｇを分散、溶解させた。さらにその混合
液にクラリスロマシン１００ｇを分散させた。この分散
液をスプレードライ装置（ＣＬ−１２型大河原工業
（株））を用いて、入口温度８０℃、回転ディスク２０
０００ｒｐｍの条件で噴霧凝固造粒し、平均粒子径８０
μｍの３０％クラリスロマイシンの複合体を約２５０ｇ
得た。この複合体１５０ｇにマンニトール２４０ｇ、酸
化マグネシウム３ｇ、デンプン１０７ｇを加え、１０％
クラリスロマイシン経口製剤用組成物を得た。(Example 1) Production of a composition for an oral preparation 200 g of glycerin fatty acid ester (main fatty acid is stearic acid and monoglyceride content is 90% or more) is about 1 g.
Melted at 00 ° C, and Eudragit E (Co., Ltd.)
(Higuchi Shokai) 30 g was dispersed and dissolved. Further, 100 g of a Clarithro machine was dispersed in the mixture. This dispersion was spray-dried (CL-12 Okawara Kogyo Co., Ltd.) using an inlet temperature of 80 ° C. and a rotating disk 20.
Spray coagulation granulation under the condition of 000 rpm, average particle size 80
Approximately 250 g of 30 μm clarithromycin complex
Obtained. To 150 g of this complex, 240 g of mannitol, 3 g of magnesium oxide and 107 g of starch were added, and 10%
A composition for oral formulation of clarithromycin was obtained.
【００１８】（試験例１）［官能評価試験］ 実施例１で調製した経口製剤用組成物１ｇと下表１記載
の各甘味剤０．０２〜０．１ｇを混合し、各ｐＨの精製
水２５ｍＬに懸濁させた。懸濁直後及び５分経過後に５
名のパネラーによる苦味の官能評価試験を実施した。各
パネラーが試験液を口中に含み、苦味を評価した。その
後、液を吐き出し、口中を水ですすいでから３０分以上
経過後に他の試験液の苦味を評価した。官能評価は、苦
味の強さを以下の基準により数値化して平均値を比較し
た。その結果を表１に示す。(Test Example 1) [Sensory evaluation test] 1 g of the composition for oral preparation prepared in Example 1 and 0.02 to 0.1 g of each sweetener shown in Table 1 below were mixed, and purified water of each pH was mixed. It was suspended in 25 mL. 5 immediately after suspension and after 5 minutes
A sensory evaluation test of bitterness was conducted by a panel of names. Each paneler contained the test solution in his mouth and evaluated the bitterness. Thereafter, the solution was spit out, and the bitterness of the other test solutions was evaluated 30 minutes or more after rinsing the mouth with water. In the sensory evaluation, the intensity of bitterness was quantified according to the following criteria, and the average values were compared. Table 1 shows the results.
【００１９】苦味の評価 全く不快な呈味を感じない ５点 ほとんど不快な呈味を感じない ４点 少し不快な呈味を感じる ３点 不快な呈味をかんじる ２点 非常に不快な呈味を感じる １点Evaluation of bitterness No unpleasant taste is felt 5 points Almost no unpleasant taste is felt 4 points Slightly unpleasant taste is felt 3 points Unpleasant taste is sensed 2 points Very unpleasant taste is felt Feel one point
【００２０】[0020]
【表１】 [Table 1]
【００２１】[0021]
【発明の効果】本発明により、クラリスロマイシン等の
塩基性薬物を含有する経口用製剤組成物が弱酸性下に呈
する苦味等の不快な味を簡易にマスキングし、服用性良
好な経口製剤を提供することが可能となった。Industrial Applicability According to the present invention, an oral preparation composition containing a basic drug such as clarithromycin can easily mask unpleasant tastes such as bitterness exhibited under weak acidity, and provide an oral preparation with good swallowability. It became possible to provide.
フロントページの続き (72)発明者 矢島 稔央 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 Ｆターム(参考） 4C076 AA31 BB01 CC32 DD29 DD46 DD67 EE12 EE38 EE41T FF06 FF52 GG09 GG12 4C086 AA01 AA02 EA13 MA02 MA05 NA09 ZB35 Continuation of the front page (72) Inventor Toshio Yajima 3-24-1, Takada, Toshima-ku, Tokyo F-term in Taisho Pharmaceutical Co., Ltd. 4C076 AA31 BB01 CC32 DD29 DD46 DD67 EE12 EE38 EE41T FF06 FF52 GG09 GG12 4C086 AA01 AA02 EA13 MA02 MA05 NA09 ZB35
Claims (6)
経口製剤用組成物及びアスパルテームを配合したことを
特徴とする経口製剤。1. An oral preparation comprising an oral preparation composition containing a basic drug exhibiting an unpleasant taste and aspartame.
に対してアスパルテームを０．１質量部以上配合した請
求項１記載の経口製剤。2. The oral preparation according to claim 1, wherein 0.1 part by mass or more of aspartame is mixed with 1 part by mass of the basic drug having an unpleasant taste.
経口製剤用組成物を水に溶解又は懸濁させたときのｐＨ
が４〜７である請求項１記載の経口製剤。3. The pH of an oral pharmaceutical composition containing a basic drug having an unpleasant taste when dissolved or suspended in water.
The oral preparation according to claim 1, wherein is 4 to 7.
ロマイシンである請求項１〜３のいずれか１項に記載の
経口製剤。4. The oral preparation according to claim 1, wherein the basic drug having an unpleasant taste is clarithromycin.
いずれか１項に記載の経口製剤。5. The oral preparation according to any one of claims 1 to 4, which is a dry syrup.
経口製剤用組成物を水に溶解又は懸濁させたときに生じ
る不快な呈味を、該液中に溶解させたアスパルテームに
よってマスキングする方法。6. An unpleasant taste produced when an oral pharmaceutical composition containing a basic drug having an unpleasant taste is dissolved or suspended in water is masked by aspartame dissolved in the liquid. Method.
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|---|---|---|---|---|
| JPH0256416A (en) * | 1988-08-19 | 1990-02-26 | Daikyo Yakuhin Kogyo Kk | Granule with suppressed bitterness |
| JPH06116138A (en) * | 1992-03-12 | 1994-04-26 | Taisho Pharmaceut Co Ltd | Composition for oral pharmaceutical preparation |
| JPH0776517A (en) * | 1993-09-07 | 1995-03-20 | Yamanouchi Pharmaceut Co Ltd | Composition for medicine |
| JPH0971529A (en) * | 1995-02-03 | 1997-03-18 | Jouveinal Lab | New medicine composition containing trimebutin and its preparation |
| WO1999016470A1 (en) * | 1997-09-30 | 1999-04-08 | Daiichi Pharmaceutical Co., Ltd. | Oral preparation |
| WO1999049842A1 (en) * | 1998-03-31 | 1999-10-07 | Asta Medica Aktiengesellschaft | Fizzy formulations |
| WO1999055320A1 (en) * | 1998-04-29 | 1999-11-04 | Sumitomo Pharmaceuticals Co., Ltd. | Oral formulation comprising biguanide and an organic acid |
| JP2000273051A (en) * | 1999-03-19 | 2000-10-03 | Kobayashi Pharmaceut Co Ltd | Liquid preparation whose bitter taste is masked |
| JP2001226293A (en) * | 2000-02-17 | 2001-08-21 | Kotaro Kanpo Seiyaku Kk | Taking assisting agent |
-
2000
- 2000-10-23 JP JP2000322548A patent/JP4706096B2/en not_active Expired - Lifetime
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0256416A (en) * | 1988-08-19 | 1990-02-26 | Daikyo Yakuhin Kogyo Kk | Granule with suppressed bitterness |
| JPH06116138A (en) * | 1992-03-12 | 1994-04-26 | Taisho Pharmaceut Co Ltd | Composition for oral pharmaceutical preparation |
| JPH0776517A (en) * | 1993-09-07 | 1995-03-20 | Yamanouchi Pharmaceut Co Ltd | Composition for medicine |
| JPH0971529A (en) * | 1995-02-03 | 1997-03-18 | Jouveinal Lab | New medicine composition containing trimebutin and its preparation |
| WO1999016470A1 (en) * | 1997-09-30 | 1999-04-08 | Daiichi Pharmaceutical Co., Ltd. | Oral preparation |
| WO1999049842A1 (en) * | 1998-03-31 | 1999-10-07 | Asta Medica Aktiengesellschaft | Fizzy formulations |
| WO1999055320A1 (en) * | 1998-04-29 | 1999-11-04 | Sumitomo Pharmaceuticals Co., Ltd. | Oral formulation comprising biguanide and an organic acid |
| JP2000273051A (en) * | 1999-03-19 | 2000-10-03 | Kobayashi Pharmaceut Co Ltd | Liquid preparation whose bitter taste is masked |
| JP2001226293A (en) * | 2000-02-17 | 2001-08-21 | Kotaro Kanpo Seiyaku Kk | Taking assisting agent |
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|---|---|
| JP4706096B2 (en) | 2011-06-22 |
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