JPH1129474A - Method for dissolving biotin, and liquid internal medicine - Google Patents
Method for dissolving biotin, and liquid internal medicineInfo
- Publication number
- JPH1129474A JPH1129474A JP9187904A JP18790497A JPH1129474A JP H1129474 A JPH1129474 A JP H1129474A JP 9187904 A JP9187904 A JP 9187904A JP 18790497 A JP18790497 A JP 18790497A JP H1129474 A JPH1129474 A JP H1129474A
- Authority
- JP
- Japan
- Prior art keywords
- biotin
- benzoate
- dissolving
- caffeine
- 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
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 title claims abstract description 147
- 229960002685 biotin Drugs 0.000 title claims abstract description 73
- 235000020958 biotin Nutrition 0.000 title claims abstract description 73
- 239000011616 biotin Substances 0.000 title claims abstract description 73
- 238000000034 method Methods 0.000 title claims abstract description 16
- 239000007788 liquid Substances 0.000 title claims abstract description 11
- 239000003814 drug Substances 0.000 title abstract description 6
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims abstract description 44
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims abstract description 35
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229960001948 caffeine Drugs 0.000 claims abstract description 22
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims abstract description 22
- 239000007864 aqueous solution Substances 0.000 claims abstract description 19
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims abstract description 13
- 229940009098 aspartate Drugs 0.000 claims abstract description 13
- 238000002360 preparation method Methods 0.000 claims abstract description 9
- 229940050390 benzoate Drugs 0.000 claims description 29
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical group [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 14
- 239000004299 sodium benzoate Substances 0.000 claims description 14
- 235000010234 sodium benzoate Nutrition 0.000 claims description 14
- 229940100688 oral solution Drugs 0.000 claims description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 21
- 238000004090 dissolution Methods 0.000 abstract description 11
- 239000000243 solution Substances 0.000 abstract description 11
- 239000004615 ingredient Substances 0.000 abstract description 6
- 230000002378 acidificating effect Effects 0.000 abstract description 3
- 230000009469 supplementation Effects 0.000 abstract 1
- 230000001502 supplementing effect Effects 0.000 abstract 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 21
- 239000008213 purified water Substances 0.000 description 14
- 238000003756 stirring Methods 0.000 description 8
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 8
- 241000544066 Stevia Species 0.000 description 6
- 229940068988 potassium aspartate Drugs 0.000 description 6
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 description 6
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 5
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 5
- 239000001630 malic acid Substances 0.000 description 5
- 235000011090 malic acid Nutrition 0.000 description 5
- 229940099690 malic acid Drugs 0.000 description 5
- YKZPPPNXRZHVGX-PXYKVGKMSA-L dipotassium;(2s)-2-aminobutanedioate;hydron;hydrate Chemical compound [H+].[H+].O.[K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O YKZPPPNXRZHVGX-PXYKVGKMSA-L 0.000 description 4
- 239000000845 maltitol Substances 0.000 description 4
- 235000010449 maltitol Nutrition 0.000 description 4
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 4
- 229940035436 maltitol Drugs 0.000 description 4
- 239000003002 pH adjusting agent Substances 0.000 description 4
- 229960003080 taurine Drugs 0.000 description 4
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 3
- 239000003205 fragrance Substances 0.000 description 3
- 239000011777 magnesium Substances 0.000 description 3
- 229910052749 magnesium Inorganic materials 0.000 description 3
- 229960001983 magnesium aspartate Drugs 0.000 description 3
- 229940088594 vitamin Drugs 0.000 description 3
- 229930003231 vitamin Natural products 0.000 description 3
- 235000013343 vitamin Nutrition 0.000 description 3
- 239000011782 vitamin Substances 0.000 description 3
- 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 2
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 description 2
- 239000004386 Erythritol Substances 0.000 description 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 2
- 229930003471 Vitamin B2 Natural products 0.000 description 2
- 229910001854 alkali hydroxide Inorganic materials 0.000 description 2
- 150000008044 alkali metal hydroxides Chemical class 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 229940026310 caffeine 50 mg Drugs 0.000 description 2
- 229940009714 erythritol Drugs 0.000 description 2
- 235000019414 erythritol Nutrition 0.000 description 2
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000019634 flavors Nutrition 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 230000007721 medicinal effect Effects 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 2
- 229960002477 riboflavin Drugs 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- 235000010356 sorbitol Nutrition 0.000 description 2
- 229940045613 taurine 1000 mg Drugs 0.000 description 2
- UIERGBJEBXXIGO-UHFFFAOYSA-N thiamine mononitrate Chemical compound [O-][N+]([O-])=O.CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N UIERGBJEBXXIGO-UHFFFAOYSA-N 0.000 description 2
- 235000019164 vitamin B2 Nutrition 0.000 description 2
- 239000011716 vitamin B2 Substances 0.000 description 2
- -1 For example Substances 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
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 229930003756 Vitamin B7 Natural products 0.000 description 1
- HFWPXARYYXLTQE-UHFFFAOYSA-N [Mg].[K].[K] Chemical compound [Mg].[K].[K] HFWPXARYYXLTQE-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 239000004301 calcium benzoate Substances 0.000 description 1
- 235000010237 calcium benzoate Nutrition 0.000 description 1
- HZQXCUSDXIKLGS-UHFFFAOYSA-L calcium;dibenzoate;trihydrate Chemical compound O.O.O.[Ca+2].[O-]C(=O)C1=CC=CC=C1.[O-]C(=O)C1=CC=CC=C1 HZQXCUSDXIKLGS-UHFFFAOYSA-L 0.000 description 1
- 239000000306 component Substances 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- SWHAQEYMVUEVNF-UHFFFAOYSA-N magnesium potassium Chemical compound [Mg].[K] SWHAQEYMVUEVNF-UHFFFAOYSA-N 0.000 description 1
- RXMQCXCANMAVIO-CEOVSRFSSA-L magnesium;(2s)-2-amino-4-hydroxy-4-oxobutanoate Chemical compound [H+].[H+].[Mg+2].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O RXMQCXCANMAVIO-CEOVSRFSSA-L 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 230000037311 normal skin Effects 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 239000004300 potassium benzoate Substances 0.000 description 1
- 235000010235 potassium benzoate Nutrition 0.000 description 1
- 229940103091 potassium benzoate Drugs 0.000 description 1
- 229940111263 potassium magnesium aspartate Drugs 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- 229940109850 royal jelly Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 235000019158 vitamin B6 Nutrition 0.000 description 1
- 239000011726 vitamin B6 Substances 0.000 description 1
- 235000011912 vitamin B7 Nutrition 0.000 description 1
- 239000011735 vitamin B7 Substances 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 229940089133 vitamin b6 5 mg Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【0001】[0001]
【発明の属する技術分野】本発明は、ビオチンの溶解方
法及びビオチンを含有する内服液剤に関する。[0001] The present invention relates to a method for dissolving biotin and an oral solution containing biotin.
【0002】[0002]
【従来の技術】ビオチンは、ビタミンHとも称され皮
膚、毛髪を正常に維持するために必要なビタミンであ
る。一般的なドリンク剤のpH域である酸性域(2〜
5)ではビオチンは水に難溶性であり、その溶解には工
夫が必要であった。ビオチンを溶解する手法としては、
従来、ポリビニルピロリドンを使用する方法(特開平7
−76520号)や水酸化アルカリなどを使用して中性
〜アルカリ性に調整した後にビオチンを溶解する方法な
どが知られている。しかし、ポリビニルピロリドンは共
存成分と反応して沈殿を生成する場合や、他のビタミン
やアミノ酸などの配合成分と反応して成分を低下させる
場合がある。また、水酸化アルカリなどを使用する方法
は、中性〜アルカリ性でビオチンを溶解しても、内服液
剤のpHである酸性域に戻した場合、ビオチンが経時的
に析出してしまうことがある(特開平7−76520
号)。析出しないまでも、薬効上不必要な成分を添加し
なければならないことや調製が煩雑になることなど、必
ずしも好ましい方法であるとは言えない。2. Description of the Related Art Biotin, also called vitamin H, is a vitamin necessary for maintaining normal skin and hair. Acidic range (2 to 2)
In 5), biotin is hardly soluble in water, and a solution was required for its dissolution. As a method of dissolving biotin,
Conventionally, a method using polyvinylpyrrolidone (Japanese Unexamined Patent Publication No.
No. -76520), a method of adjusting the pH to neutral to alkaline using an alkali hydroxide or the like, and then dissolving biotin. However, polyvinylpyrrolidone may react with coexisting components to form a precipitate or react with other components such as vitamins and amino acids to lower the components. Further, in the method using alkali hydroxide or the like, even if biotin is dissolved in a neutral to alkaline state, biotin may be precipitated with time when the pH is returned to an acidic range which is the pH of an oral solution ( JP-A-7-76520
issue). Even if it does not precipitate, it is not necessarily a preferred method, for example, it is necessary to add a component unnecessary for its medicinal effect and the preparation becomes complicated.
【0003】[0003]
【発明が解決しようとする課題】本発明の目的は、製剤
上不必要な成分を追加することなく迅速かつ容易に水へ
ビオチンを溶解させる方法及びビオチンを含有する内服
液剤を提供することにある。SUMMARY OF THE INVENTION An object of the present invention is to provide a method for rapidly and easily dissolving biotin in water without adding unnecessary components in a pharmaceutical preparation, and to provide an oral solution containing biotin. .
【0004】[0004]
【課題を解決するための手段】本発明者らは上記目的に
ついて鋭意研究した結果、ビオチンを安息香酸塩、カフ
ェイン、アスパラギン酸塩などの水溶液に溶解した場
合、所期の目的を達成することを見いだし、本発明を完
成した。かくして、本発明は、(1) 安息香酸塩の水溶液
にビオチンを溶解することを特徴とするビオチンの溶解
方法、(2) 安息香酸塩及びカフェインを溶解させた水溶
液にビオチンを溶解することを特徴とするビオチンの溶
解方法、(3) 安息香酸塩、カフェイン及びアスパラギン
酸塩を溶解させた水溶液にビオチンを溶解することを特
徴とするビオチンの溶解方法、(4) 安息香酸塩の水溶液
にビオチンが溶解され、pHが2〜5の範囲であること
を特徴とする内服液剤、(5) 安息香酸塩及びカフェイン
の水溶液にビオチンが溶解され、pHが2〜5の範囲で
あることを特徴とする内服液剤、(6) 安息香酸塩、カフ
ェイン及びアスパラギン酸塩の水溶液にビオチンが溶解
されpHが2〜5の範囲であることを特徴とする内服液
剤、(7) ビオチン及びビオチンを溶解するための安息香
酸塩を含有する内服液剤、(8) ビオチン並びにビオチン
を溶解するための安息香酸塩及びカフェインを含有する
内服液剤、(9) ビオチン並びにビオチンを溶解するため
の安息香酸塩、カフェイン及びアスパラギン酸塩を含有
する内服液剤である。Means for Solving the Problems The inventors of the present invention have made intensive studies on the above-mentioned objects, and as a result, have found that when biotin is dissolved in an aqueous solution of benzoate, caffeine, aspartate, etc., the intended object can be achieved. And completed the present invention. Thus, the present invention provides (1) a method for dissolving biotin, which comprises dissolving biotin in an aqueous solution of benzoate, and (2) dissolving biotin in an aqueous solution in which benzoate and caffeine are dissolved. A biotin dissolving method characterized by dissolving biotin in an aqueous solution in which benzoate, caffeine and aspartate are dissolved, and (4) an aqueous solution of benzoate. Biotin is dissolved and the pH is in the range of 2 to 5; (5) that the biotin is dissolved in an aqueous solution of benzoate and caffeine and the pH is in the range of 2 to 5; (6) Biotin is dissolved in an aqueous solution of benzoate, caffeine and aspartate, and the pH is in the range of 2 to 5; (7) Biotin and biotin Dissolution (8) Biotin and a benzoate for dissolving biotin and an oral solution containing caffeine, (9) Biotin and a benzoate for dissolving biotin, It is an oral solution containing caffeine and aspartate.
【0005】[0005]
【発明の実施の形態】本発明における安息香酸塩とは、
安息香酸ナトリウム、安息香酸カリウム、安息香酸カル
シウムなどを挙げることができるが、好ましくは安息香
酸ナトリウムである。アスパラギン酸塩とは、アスパラ
ギン酸マグネシウム・カリウム、アスパラギン酸マグネ
シウム、アスパラギン酸カリウムの1種又はこれらを組
み合わせであり、就中アスパラギン酸マグネシウム・カ
リウムが好ましい。BEST MODE FOR CARRYING OUT THE INVENTION The benzoate in the present invention is
Examples thereof include sodium benzoate, potassium benzoate, calcium benzoate, and the like, with preference given to sodium benzoate. The aspartate is one or a combination of magnesium potassium aspartate, magnesium aspartate, and potassium aspartate, and magnesium potassium potassium aspartate is particularly preferred.
【0006】本発明においてビオチンの溶解は、まず安
息香酸塩(及びカフェイン、アスパラギン酸塩)を水に
溶解し、次いでこの溶液にビオチンを溶解することによ
り達成される。また、本発明のビオチン含有内服液剤
は、まず前記の如く安息香酸塩(及びカフェイン、アス
パラギン酸塩)の水溶液にビオチンを溶解し、別途各種
配合成分を溶解した液を調製して、両液を混合後、必要
に応じてpHを調整することによって製造される。In the present invention, the dissolution of biotin is achieved by first dissolving benzoate (and caffeine and aspartate) in water, and then dissolving biotin in this solution. In addition, the biotin-containing oral solution of the present invention is prepared by first dissolving biotin in an aqueous solution of benzoate (and caffeine and aspartate) as described above, and separately preparing solutions in which various components are dissolved. Is manufactured by adjusting pH as needed after mixing.
【0007】ビオチンを溶解するための安息香酸塩の水
溶液は、例えばビオチン0.2mgを溶解するためには
通常安息香酸塩5〜200mg、好ましくは10〜80
mgを水100mlに溶解した水溶液50〜100ml
が用いられる。以下、溶解するビオチン量によって安息
香酸塩の水溶液の量が決定される。The aqueous solution of benzoate for dissolving biotin is usually, for example, 5 to 200 mg, preferably 10 to 80 mg of benzoate for dissolving 0.2 mg of biotin.
50 to 100 ml of an aqueous solution prepared by dissolving mg in 100 ml of water
Is used. Hereinafter, the amount of the aqueous solution of benzoate is determined by the amount of biotin to be dissolved.
【0008】カフェインの添加量は、安息香酸塩1重量
部に対して0.1〜10重量部、好ましくは0.5〜5
重量部である。アスパラギン酸塩の添加量は、安息香酸
塩1重量部に対して0.1〜10重量部、好ましくは
0.5〜5重量部である。The amount of caffeine added is 0.1 to 10 parts by weight, preferably 0.5 to 5 parts by weight per 1 part by weight of benzoate.
Parts by weight. The amount of aspartate added is 0.1 to 10 parts by weight, preferably 0.5 to 5 parts by weight, per 1 part by weight of benzoate.
【0009】本発明において、pHの調整剤としては、
例えば、乳酸、クエン酸、リンゴ酸、コハク酸、フマル
酸、酒石酸、リン酸及びそれらの塩などを用いることが
できる。In the present invention, as the pH adjuster,
For example, lactic acid, citric acid, malic acid, succinic acid, fumaric acid, tartaric acid, phosphoric acid, and salts thereof can be used.
【0010】さらに、本発明の内服液剤には、上記成分
の他、通常内服液剤に用いることの可能な配合成分、例
えば各種ビタミン、アミノ酸、生薬、ローヤルゼリー、
多価アルコール、有機酸、ミネラル成分、香料、保存剤
などを本発明の効果を損なわない範囲で配合することが
できる。[0010] In addition to the above components, the oral liquid preparation of the present invention may contain other components which can be used in the oral liquid preparation, such as various vitamins, amino acids, crude drugs, royal jelly, etc.
Polyhydric alcohols, organic acids, mineral components, fragrances, preservatives, and the like can be blended within a range that does not impair the effects of the present invention.
【0011】[0011]
【発明の効果】本発明により、ビオチンの溶解のために
薬効上不要な成分を追加することなく迅速かつ容易な溶
解方法が提供されるとともに、酸性域でも経時的に安定
でかつ各種配合成分も補給できるビオチン含有内服液剤
が提供された。According to the present invention, a quick and easy dissolving method can be provided without adding unnecessary components for the medicinal effect for dissolving biotin. A replenishable biotin-containing oral solution was provided.
【0012】[0012]
【実施例】以下、実施例及び試験例を挙げて本発明を更
に詳細に説明する。 実施例1 タウリン 2000mg ビオチン 200μg マルチトール 1500mg ビタミンB6 5mg クエン酸(pH調整剤) 適量 安息香酸ナトリウム 70mg ステビア抽出物 30mg 香料 微量 精製水 全量100ml(pH3.5) 精製水60mlに安息香酸ナトリウムを加え溶解後、撹
拌しながらビオチンを添加し溶解した。その後、タウリ
ン、マルチトール、ビタミンB6、ステビア抽出物、香
料の順に添加し溶解確認後、クエン酸を加えpH3.5
にし精製水を加え全量を100mlにして、内服液剤を
得た。The present invention will be described below in more detail with reference to examples and test examples. Example 1 Taurine 2000 mg Biotin 200 μg Maltitol 1500 mg Vitamin B6 5 mg Citric acid (pH adjuster) Appropriate amount Sodium benzoate 70 mg Stevia extract 30 mg Fragrance Trace amount Purified water 100 ml (pH 3.5) Sodium benzoate is added to purified water 60 ml and dissolved. Thereafter, biotin was added and dissolved while stirring. Thereafter, taurine, maltitol, vitamin B6, stevia extract, and flavor are added in this order, and after confirming dissolution, citric acid is added and pH 3.5.
Then, purified water was added to make the total amount 100 ml to obtain an oral liquid preparation.
【0013】 実施例2 タウリン 1000mg ビオチン 200μg ビタミンB2 5mg カフェイン 50mg ソルビトール 2000mg マルチトール 9000mg クエン酸(pH調整剤) 適量 リンゴ酸 100mg 安息香酸ナトリウム 60mg ステビア抽出物 25mg 香料 微量 精製水 全量100ml(pH2.8) 精製水60mlに安息香酸ナトリウムとカフェインを溶
解後、撹拌しながらビオチンを添加し溶解した。その
後、タウリン、ビタミンB2、ソルビトール、マルチト
ール、リンゴ酸、ステビア抽出物、香料を加え溶解確認
後、クエン酸を加えpH2.8に調整し、精製水を加え
全量を100mlにして、内服液剤を得た。Example 2 Taurine 1000 mg Biotin 200 μg Vitamin B2 5 mg Caffeine 50 mg Sorbitol 2000 mg Maltitol 9000 mg Citric acid (pH adjuster) Suitable amount Malic acid 100 mg Sodium benzoate 60 mg Stevia extract 25 mg Fragrance Trace amount Purified water Total 100 ml (pH 2.8) After dissolving sodium benzoate and caffeine in 60 ml of purified water, biotin was added and dissolved while stirring. Then, after adding taurine, vitamin B2, sorbitol, maltitol, malic acid, stevia extract, and flavor, confirming dissolution, adjusting the pH to 2.8 by adding citric acid, adding purified water to make the total volume 100 ml, Obtained.
【0014】 実施例3 タウリン 1000mg ビオチン 300μg アスパラギン酸マグネシウム・カリウム 200mg ビタミンB1硝酸塩 2mg カフェイン 50mg エリスリトール 5000mg クエン酸(pH調整剤) 適量 リンゴ酸 100mg ニパブチ 4mg 安息香酸ナトリウム 60mg ステビア抽出物 15mg 精製水 全量100ml(pH4.0) 精製水60mlに安息香酸ナトリウム、カフェイン、ア
スパラギン酸マグネシウム・カリウムを溶解後、撹拌し
ながらビオチンを添加し溶解した。その後、タウリン、
ビタミンB1硝酸塩、エリスリトール、リンゴ酸、ニパ
ブチ、ステビア抽出物を添加し溶解確認後、クエン酸を
加えpH4.0に調整し、精製水を加え全量を100m
lとして、内服液剤を得た。Example 3 Taurine 1000 mg Biotin 300 μg Magnesium / potassium aspartate 200 mg Vitamin B1 nitrate 2 mg Caffeine 50 mg Erythritol 5000 mg Citric acid (pH adjuster) Appropriate amount Malic acid 100 mg Nipapuchi 4 mg Sodium benzoate 60 mg Stevia extract Total water 15 mg Purified water (PH 4.0) Sodium benzoate, caffeine, and magnesium / potassium aspartate were dissolved in 60 ml of purified water, and then biotin was added with stirring to dissolve. Then taurine,
After adding vitamin B1 nitrate, erythritol, malic acid, nipabuti and stevia extract and confirming dissolution, adjust the pH to 4.0 by adding citric acid, and add purified water to a total volume of 100 m.
As l, an oral solution was obtained.
【0015】試験例[溶解性試験] 実施例1について、精製水60mlに安息香酸ナトリ
ウムを加え溶解後、室温下撹拌しながらビオチンを20
0μg添加したところ、ビオチン添加後9分後にその溶
解を確認した。この溶液に他の処方成分を入れるととも
にpHを調整し、全量を100mlとした。これを5℃
と40℃で保管したが、6ヶ月経ってもビオチンの析出
は見られなかった。Test Example [Solubility test] In Example 1, sodium benzoate was added and dissolved in 60 ml of purified water, and then biotin was added at room temperature with stirring.
When 0 μg was added, the dissolution was confirmed 9 minutes after the addition of biotin. The other ingredients were added to the solution and the pH was adjusted to make the total volume 100 ml. 5 ℃
And at 40 ° C., but no biotin was deposited even after 6 months.
【0016】実施例2について、精製水60mlに安
息香酸ナトリウム60mg及びカフェイン50mgを加
え溶解後、室温下撹拌しながらビオチンを200μg添
加したところ、ビオチン添加後7分後にその溶解を確認
した。この溶液に他の処方成分を入れるとともにpHを
調整し、全量を100mlとした。これを5℃と40℃
で保管したが、6ヶ月経ってもビオチンの析出は見られ
なかった。In Example 2, 60 mg of sodium benzoate and 50 mg of caffeine were added to and dissolved in 60 ml of purified water, and 200 μg of biotin was added with stirring at room temperature. The dissolution was confirmed 7 minutes after the addition of biotin. The other ingredients were added to the solution and the pH was adjusted to make the total volume 100 ml. This is 5 ℃ and 40 ℃
However, no biotin was deposited even after 6 months.
【0017】実施例3について、精製水60mlに安
息香酸ナトリウム60mg及びカフェイン50mg及び
アスパラギン酸マグネシウム・カリウム200mgを加
え溶解後、室温下撹拌しながらビオチン300μg添加
したところ、ビオチン添加後6分後にその溶解を確認し
た。この溶液に他の処方成分を入れるとともにpHを調
整し、全量を100mlとした。これを5℃と40℃で
保管したが、6ヶ月経ってもビオチンの析出は見られな
かった。In Example 3, 60 mg of sodium benzoate, 50 mg of caffeine and 200 mg of magnesium / potassium aspartate were added to 60 ml of purified water and dissolved, and then 300 μg of biotin was added with stirring at room temperature. Dissolution was confirmed. The other ingredients were added to the solution and the pH was adjusted to make the total volume 100 ml. This was stored at 5 ° C. and 40 ° C., but no deposition of biotin was observed even after 6 months.
【0018】室温において精製水60mlに撹拌しな
がらビオチン200μgを添加して溶解を試みたとこ
ろ、60分後に溶解していなかった。At room temperature, 200 μg of biotin was added to 60 ml of purified water while stirring to try to dissolve, but after 60 minutes, it was not dissolved.
【0019】80〜90℃に維持した精製水100m
lに撹拌しながらビオチン200μgを添加し、溶解を
試みたところ、60分後に溶解していなかった。100 m of purified water maintained at 80 to 90 ° C.
To this, 200 μg of biotin was added while stirring, and the dissolution was attempted, but it was not dissolved after 60 minutes.
Claims (12)
ることを特徴とするビオチンの溶解方法。1. A method for dissolving biotin, comprising dissolving biotin in an aqueous solution of a benzoate.
水溶液にビオチンを溶解することを特徴とするビオチン
の溶解方法。2. A method for dissolving biotin, comprising dissolving biotin in an aqueous solution in which benzoate and caffeine are dissolved.
ン酸塩を溶解させた水溶液にビオチンを溶解することを
特徴とするビオチンの溶解方法。3. A method for dissolving biotin, comprising dissolving biotin in an aqueous solution in which benzoate, caffeine and aspartate are dissolved.
請求項1〜3のいずれか記載のビオチンの溶解方法。4. The method for dissolving biotin according to claim 1, wherein the benzoate is sodium benzoate.
れ、pHが2〜5の範囲であることを特徴とする内服液
剤。5. An oral liquid preparation characterized in that biotin is dissolved in an aqueous solution of benzoate and the pH is in the range of 2 to 5.
オチンが溶解され、pHが2〜5の範囲であることを特
徴とする内服液剤。6. An oral solution, wherein biotin is dissolved in an aqueous solution of benzoate and caffeine, and the pH is in the range of 2 to 5.
ン酸塩の水溶液にビオチンが溶解され、pHが2〜5の
範囲であることを特徴とする内服液剤。7. An oral liquid preparation, wherein biotin is dissolved in an aqueous solution of benzoate, caffeine and aspartate, and the pH is in the range of 2 to 5.
請求項5〜7のいずれか記載の内服液剤。8. The liquid preparation according to claim 5, wherein the benzoate is sodium benzoate.
安息香酸塩を含有する内服液剤。9. An oral solution containing biotin and a benzoate for dissolving biotin.
めの安息香酸塩及びカフェインを含有する内服液剤。10. An oral solution containing biotin and a benzoate and caffeine for dissolving biotin.
めの安息香酸塩、カフェイン及びアスパラギン酸塩を含
有する内服液剤。11. An oral solution containing biotin and benzoate, caffeine and aspartate for dissolving biotin.
る請求項9〜11のいずれか記載の内服液剤。12. The liquid preparation for oral administration according to claim 9, wherein the benzoate is sodium benzoate.
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JP18790497A JP4134358B2 (en) | 1997-07-14 | 1997-07-14 | Biotin dissolution method and oral solution |
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JP18790497A JP4134358B2 (en) | 1997-07-14 | 1997-07-14 | Biotin dissolution method and oral solution |
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JPH1129474A true JPH1129474A (en) | 1999-02-02 |
JP4134358B2 JP4134358B2 (en) | 2008-08-20 |
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