JP2017114833A - Pharmaceutical composition for antacid - Google Patents
Pharmaceutical composition for antacid Download PDFInfo
- Publication number
- JP2017114833A JP2017114833A JP2015254665A JP2015254665A JP2017114833A JP 2017114833 A JP2017114833 A JP 2017114833A JP 2015254665 A JP2015254665 A JP 2015254665A JP 2015254665 A JP2015254665 A JP 2015254665A JP 2017114833 A JP2017114833 A JP 2017114833A
- Authority
- JP
- Japan
- Prior art keywords
- antacid
- pharmaceutical composition
- antacids
- mass
- acid
- 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
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- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 title claims abstract description 139
- 229940069428 antacid Drugs 0.000 title claims abstract description 120
- 239000003159 antacid agent Substances 0.000 title claims abstract description 120
- 230000001458 anti-acid effect Effects 0.000 title claims abstract description 68
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 61
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims abstract description 90
- 235000017557 sodium bicarbonate Nutrition 0.000 claims abstract description 45
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims abstract description 45
- 229910000019 calcium carbonate Inorganic materials 0.000 claims abstract description 33
- 239000002253 acid Substances 0.000 abstract description 29
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 abstract description 13
- 239000011777 magnesium Substances 0.000 abstract description 13
- 229910052749 magnesium Inorganic materials 0.000 abstract description 13
- 230000009858 acid secretion Effects 0.000 abstract description 12
- 229910052782 aluminium Inorganic materials 0.000 abstract description 12
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 abstract description 12
- 230000003472 neutralizing effect Effects 0.000 abstract description 11
- 230000000694 effects Effects 0.000 description 37
- 210000002784 stomach Anatomy 0.000 description 26
- 238000006386 neutralization reaction Methods 0.000 description 17
- 239000008187 granular material Substances 0.000 description 15
- 238000006243 chemical reaction Methods 0.000 description 12
- 210000004211 gastric acid Anatomy 0.000 description 12
- 230000000052 comparative effect Effects 0.000 description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 10
- 239000003795 chemical substances by application Substances 0.000 description 10
- 239000003814 drug Substances 0.000 description 10
- 229940079593 drug Drugs 0.000 description 8
- 208000024891 symptom Diseases 0.000 description 8
- -1 corrigents Substances 0.000 description 7
- 239000007788 liquid Substances 0.000 description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 6
- WMGSQTMJHBYJMQ-UHFFFAOYSA-N aluminum;magnesium;silicate Chemical compound [Mg+2].[Al+3].[O-][Si]([O-])([O-])[O-] WMGSQTMJHBYJMQ-UHFFFAOYSA-N 0.000 description 6
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 6
- 235000019700 dicalcium phosphate Nutrition 0.000 description 6
- 102000038379 digestive enzymes Human genes 0.000 description 6
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- 230000002496 gastric effect Effects 0.000 description 6
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- 238000005469 granulation Methods 0.000 description 5
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- 150000003839 salts Chemical class 0.000 description 5
- 239000000243 solution Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
- 241000287462 Phalacrocorax carbo Species 0.000 description 4
- 150000004347 all-trans-retinol derivatives Chemical class 0.000 description 4
- LHGVFZTZFXWLCP-UHFFFAOYSA-N guaiacol Chemical compound COC1=CC=CC=C1O LHGVFZTZFXWLCP-UHFFFAOYSA-N 0.000 description 4
- 230000005923 long-lasting effect Effects 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- ZQBAKBUEJOMQEX-UHFFFAOYSA-N phenyl salicylate Chemical compound OC1=CC=CC=C1C(=O)OC1=CC=CC=C1 ZQBAKBUEJOMQEX-UHFFFAOYSA-N 0.000 description 4
- 206010000087 Abdominal pain upper Diseases 0.000 description 3
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- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 3
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- 238000002360 preparation method Methods 0.000 description 3
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- 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 description 2
- IQESODSFGDRGIW-UHFFFAOYSA-H (4,6-dioxo-1,3,5,2-trioxabisman-2-yl) (4,6-dioxo-1,3,5,2-trioxabisman-2-yl)oxycarbonyl carbonate Chemical compound [Bi+3].[Bi+3].[O-]C(=O)OC([O-])=O.[O-]C(=O)OC([O-])=O.[O-]C(=O)OC([O-])=O IQESODSFGDRGIW-UHFFFAOYSA-H 0.000 description 2
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- IYLLULUTZPKQBW-UHFFFAOYSA-N Acrinol Chemical compound CC(O)C(O)=O.C1=C(N)C=CC2=C(N)C3=CC(OCC)=CC=C3N=C21 IYLLULUTZPKQBW-UHFFFAOYSA-N 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- VKJGBAJNNALVAV-UHFFFAOYSA-M Berberine chloride (TN) Chemical compound [Cl-].C1=C2CC[N+]3=CC4=C(OC)C(OC)=CC=C4C=C3C2=CC2=C1OCO2 VKJGBAJNNALVAV-UHFFFAOYSA-M 0.000 description 2
- 244000025254 Cannabis sativa Species 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 2
- 235000009917 Crataegus X brevipes Nutrition 0.000 description 2
- 235000013204 Crataegus X haemacarpa Nutrition 0.000 description 2
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Abstract
Description
本発明は、制酸用医薬組成物に関する。 The present invention relates to a pharmaceutical composition for antacids.
胃痛、胸やけ、胃もたれと言った症状は、胃液の分泌の亢進、即ち胃酸過多が原因であることが多い。そこで、胃酸を中和し、胃内ｐＨを適正範囲に調整する制酸剤が用いられている。
制酸剤としては、炭酸水素ナトリウム、炭酸カルシウム、水酸化マグネシウム、酸化マグネシウム等の、胃のｐＨを急激に上昇させる即効性の制酸剤と、メタケイ酸アルミン酸マグネシウム、ケイ酸アルミン酸マグネシウム、乾燥水酸化アルミニウムゲル、合成ケイ酸アルミニウム等の、急激な胃のｐＨの上昇はないが徐々に酸中和作用を発現する持続性の制酸剤があることが知られている。従来の制酸用医薬組成物においては、適正な胃内ｐＨを維持することを目的として、これらが組み合わされて用いられている。
Symptoms such as stomach pain, heartburn, and stomach sag are often caused by increased secretion of gastric juice, that is, hyperacidity. Therefore, antacids that neutralize gastric acid and adjust gastric pH to an appropriate range are used.
As antacids, fast-acting antacids that rapidly increase the pH of the stomach, such as sodium bicarbonate, calcium carbonate, magnesium hydroxide, magnesium oxide, magnesium aluminate metasilicate, magnesium aluminate silicate, It is known that there are long-lasting antacids such as dry aluminum hydroxide gel and synthetic aluminum silicate that do not rapidly increase the pH of the stomach but gradually develop an acid neutralizing action. Conventional pharmaceutical compositions for antacids are used in combination for the purpose of maintaining an appropriate gastric pH.
しかし、制酸剤の多くは胃酸を一過的に中和させることで、適正範囲の胃内ｐＨを超えて中和されることがあり、その場合、胃内の異常発酵や反動的胃酸分泌を引き起こす結果、症状をさらに悪化させる他、使用目的を達成できない等の問題があった。また、制酸作用の発現までに時間がかかったり、制酸作用が発現している時間が十分に長くなかったりする結果、満足な症状改善効果が得られないという問題点も有していた。 However, many antacids may be neutralized beyond the appropriate range of gastric pH by neutralizing gastric acid transiently, in which case abnormal fermentation in the stomach and reaction of gastric acid secretion As a result of this, there are problems such as worsening the symptoms and not achieving the intended purpose. Further, as a result of taking time for the antacid action to appear or the time for which the antacid action is manifested is not sufficiently long, there is a problem that a satisfactory symptom improving effect cannot be obtained.
平成１４年６月５日付で厚生労働省医薬局安全対策課から発出された「医薬品の使用上の注意の改定について」によれば、アルミニウムを含む上述の持続性の制酸剤等は、アルミニウム脳症の懸念により使用が制限されている。 According to the “Revision of Precautions for Use of Drugs” issued by the Ministry of Health, Labor and Welfare, Pharmaceutical Bureau, Safety Measures Division on June 5, 2002, the above-mentioned sustained antacids including aluminum are Use is restricted due to concerns.
そのような中、酸中和作用の即効性と持続性とを兼ね備え、反動的酸分泌を引き起こさず、さらにアルミニウムを含有しない制酸剤組成物が報告されている（特許文献１）。特許文献１においては、水酸化マグネシウム、炭酸水素ナトリウム及び炭酸カルシウムを含む制酸剤組成物が開示されている。 Under such circumstances, an antacid composition that has both immediate effect and sustainability of an acid neutralizing action, does not cause reaction acid secretion, and does not contain aluminum has been reported (Patent Document 1). In patent document 1, the antacid composition containing magnesium hydroxide, sodium hydrogencarbonate, and calcium carbonate is disclosed.
近年になって、マグネシウム含有製剤の摂取により、高齢者に対して高マグネシウム血症の危険性があるため、使用に際して専門家への事前相談を必要とすることが、平成２７年１０月２０日付の厚生労働省医薬・生活衛生局安全対策課長からの通達（「使用上の注意」の改定について）により指摘された。 In recent years, taking magnesium-containing preparations has the risk of hypermagnesemia for the elderly, so it is necessary to consult a specialist before use on October 20, 2015. Of the Ministry of Health, Labor and Welfare of the Ministry of Health, Labor and Welfare of the Ministry of Health and Welfare, safety measures section manager
本発明者らは、炭酸水素ナトリウム及び炭酸カルシウムを特定の比で配合させることにより、アルミニウム及びマグネシウムを含有せずに、酸中和作用の即効性と持続性を兼ね備え、反動的酸分泌を引き起こすおそれが極めて小さい制酸用医薬組成物が得られることを知見した。
従って、本発明は、アルミニウム及びマグネシウムを含有せずに、酸中和作用の即効性と持続性を兼ね備え、反動的酸分泌を引き起こすおそれが極めて小さい制酸用医薬組成物を提供することを課題とする。
The present inventors combine sodium hydrogen carbonate and calcium carbonate at a specific ratio, so that they do not contain aluminum and magnesium, have both immediate effect and sustainability of acid neutralization, and cause reaction acid secretion. It has been found that a pharmaceutical composition for antacid can be obtained with very little fear.
Accordingly, it is an object of the present invention to provide a pharmaceutical composition for antacids which does not contain aluminum and magnesium, has an immediate effect and durability of an acid neutralization action, and has a very low possibility of causing reaction acid secretion. And
本発明は、以下の構成を有する。 The present invention has the following configuration.
本発明の制酸用医薬組成物は、制酸成分を含む制酸用医薬組成物であって、制酸成分が炭酸水素ナトリウム及び炭酸カルシウムからなり、前記炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量が５０〜９０質量部である制酸用医薬組成物である。
本発明の制酸用医薬組成物は、制酸用医薬組成物の１００質量部に占める制酸成分の含有量が２０〜９０質量部である前記制酸用医薬組成物であることが望ましい。
また、本発明の制酸用医薬組成物は、制酸用医薬組成物の１回あたりの成人服用量として、３００〜４２０ｍｇの炭酸水素ナトリウムと、前記炭酸水素ナトリウムの１００質量部に対して５０〜９０質量部の炭酸カルシウムを含む前記制酸用医薬組成物であることが望ましい。
The pharmaceutical composition for antacids of the present invention is a pharmaceutical composition for antacids containing an antacid component, wherein the antacid component consists of sodium bicarbonate and calcium carbonate, and calcium carbonate relative to 100 parts by mass of the sodium bicarbonate. Is a pharmaceutical composition for antacids having a content of 50 to 90 parts by mass.
The antacid pharmaceutical composition of the present invention is preferably the antacid pharmaceutical composition, wherein the content of the antacid component in 100 parts by mass of the antacid pharmaceutical composition is 20 to 90 parts by mass.
Moreover, the pharmaceutical composition for antacids of the present invention has an adult dose per administration of the pharmaceutical composition for antacids of 300 to 420 mg of sodium bicarbonate and 50 parts by mass of 100 parts by mass of the sodium bicarbonate. It is desirable that the pharmaceutical composition for antacid contains ~ 90 parts by mass of calcium carbonate.
本発明の制酸用医薬組成物は、使用制限のあるアルミニウム、及び高齢者の使用に当たり事前相談の必要なマグネシウムを含有せず、かつ、酸中和作用の即効性と持続性を兼ね備え、反動的酸分泌を引き起こすおそれが極めて小さい制酸用医薬組成物である。 The pharmaceutical composition for antacids of the present invention does not contain aluminum that is restricted in use and magnesium that needs to be consulted in advance for use by the elderly, and has both immediate effect and sustainability of acid neutralization, It is a pharmaceutical composition for antacids that has a very low risk of causing acid secretion.
以下、本発明の実施の形態について説明する。以下の実施の形態は、本発明を説明するための単なる例示であって、本発明をこの実施の形態にのみ限定することは意図されない。本発明は、その趣旨を逸脱しない限り、様々な態様で実施することができる。
本明細書において引用したすべての刊行物、例えば、技術文献、及び公開公報その他の特許文献は、その全体が本明細書において参考として組み込まれる。
Embodiments of the present invention will be described below. The following embodiments are merely examples for explaining the present invention, and the present invention is not intended to be limited only to these embodiments. The present invention can be implemented in various modes without departing from the spirit of the present invention.
All publications cited herein, for example, technical literature, and publications and other patent literature, are incorporated herein by reference in their entirety.
なお、本明細書において、酸中和作用の即効性とは、胃内において胃酸を中和し、胃内のｐＨを６以上にするまでにかかる時間がおよそ１分程度以内であることを意味する。また、酸中和作用の持続性とは、胃内のｐＨを６以上にした後、再び胃内のｐＨが４若しくは３．５に下がるまでにかかる時間が３０分程度以上であることを意味する。
また、反動的酸分泌とは、胃内がアルカリ性に傾くことによって、胃壁の細胞によるこの状態を修正するための胃酸の分泌が促進されることを言う。従って、反動的酸分泌を引き起こさないためにはｐＨを７以下に維持することが望ましいが、ｐＨが７を超えると同時に反動的酸分泌が引き起こされるものではないため、胃内の最大ｐＨを７付近に抑制することが重要であり、必ずしも胃内の最大ｐＨが７を超えたからと言って、直ちに反動的酸分泌が引き起こされるものではない。
In the present specification, the immediate effect of the acid neutralization action means that it takes about 1 minute or less to neutralize the stomach acid in the stomach and bring the stomach pH to 6 or more. To do. Further, the persistence of the acid neutralization action means that it takes about 30 minutes or more after the pH in the stomach is increased to 6 or more to lower the pH in the stomach to 4 or 3.5 again. To do.
Moreover, reaction acid secretion means that secretion of gastric acid for correcting this state by cells in the stomach wall is promoted by tilting the inside of the stomach to be alkaline. Therefore, in order not to cause reaction acid secretion, it is desirable to maintain the pH at 7 or less, but since reaction acid secretion is not caused at the same time as the pH exceeds 7, the maximum pH in the stomach is 7. It is important to suppress in the vicinity, and just because the maximum pH in the stomach exceeds 7, reaction acid secretion is not immediately caused.
＜制酸用医薬組成物＞
本発明の制酸用医薬組成物は、優れた酸中和作用により、胃において過剰に分泌された胃酸による胃痛、胸やけ、胃もたれと言った症状に対する改善作用を有する。
本発明の制酸用医薬組成物は、制酸成分を含む。
<Pharmaceutical composition for antacid>
The pharmaceutical composition for antacids of the present invention has an improving action against symptoms such as stomach pain, heartburn and stomach stagnation due to gastric acid secreted excessively in the stomach by an excellent acid neutralizing action.
The pharmaceutical composition for antacids of the present invention contains an antacid component.
（制酸成分）
本明細書において制酸成分とは、胃酸を中和して胃内のｐＨを上昇させることができる酸中和作用を有する成分を言う。
本発明の制酸用医薬組成物に含有される前記制酸成分は、使用制限のあるアルミニウム、及び高齢者の使用に当たり事前相談の必要なマグネシウムを含有せず、炭酸水素ナトリウム及び炭酸カルシウムからなる。前記炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量は５０〜９０質量部であり、ある態様としては５５〜８５質量部であり、別の態様としては６０〜８０質量部であり、さらに別の態様としては６５〜８０質量部である。
炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量が上記下限値以上であれば、炭酸水素ナトリウムの酸中和作用のみならず炭酸カルシウムの酸中和作用の寄与が十分に期待でき、上記上限値以下であれば、酸中和作用の持続性が高い。
(Antacid component)
In the present specification, the antacid component refers to a component having an acid neutralizing action capable of neutralizing gastric acid and raising the pH in the stomach.
The antacid component contained in the pharmaceutical composition for antacids of the present invention does not contain aluminum that is restricted in use and magnesium that needs to be consulted in advance for use by the elderly, and consists of sodium bicarbonate and calcium carbonate. . The content of calcium carbonate with respect to 100 parts by mass of sodium bicarbonate is 50 to 90 parts by mass, as an aspect, 55 to 85 parts by mass, as another aspect, 60 to 80 parts by mass, and further The aspect is 65 to 80 parts by mass.
If the content of calcium carbonate with respect to 100 parts by mass of sodium hydrogen carbonate is not less than the above lower limit value, not only the acid neutralization effect of sodium hydrogen carbonate but also the acid neutralization effect of calcium carbonate can be sufficiently expected, and the above upper limit If it is below the value, the acid neutralizing effect is high.
本発明の制酸用医薬組成物において、前記制酸用医薬組成物の１００質量部に占める制酸成分の含有量は、２０〜９０質量部であり、ある態様としては２５〜８５質量部であり、別の態様としては３０〜８０質量部である。
制酸用医薬組成物の１００質量部に占める制酸成分の含有量が上記下限値以上であれば、十分な酸中和作用の発現が得られ、上記上限値以下であれば、１回あたりの服用量が必要以上に増えず、服用時のコンプライアンスが高まる。
In the pharmaceutical composition for antacids of the present invention, the content of the antacid component in 100 parts by mass of the pharmaceutical composition for antacids is 20 to 90 parts by mass, and as an aspect, 25 to 85 parts by mass. Yes, as another aspect, it is 30-80 mass parts.
If the content of the antacid component in 100 parts by mass of the pharmaceutical composition for antacids is not less than the above lower limit value, sufficient expression of acid neutralization can be obtained, and if not more than the above upper limit value, once per time Dosage is not increased more than necessary, and compliance is increased.
本発明の制酸用医薬組成物に含まれる制酸成分は、炭酸水素ナトリウム及び炭酸カルシウムからなる。
炭酸水素ナトリウムとしては、医療用医薬品としての炭酸水素ナトリウムや、食品添加用の炭酸水素ナトリウム等の、市販の炭酸水素ナトリウムを用いることができる。ある態様としては、日本薬局方に基づく炭酸水素ナトリウムを用いることができる。炭酸水素ナトリウムは、９９％以上の純度を有する炭酸水素ナトリウムを使用することが望ましく、別の態様としては９９．２％以上の純度を有する炭酸水素ナトリウムを使用することが望ましい。
炭酸カルシウムとしては、医療用医薬品としての炭酸カルシウムや、食品添加物用の炭酸カルシウム等の、市販の炭酸カルシウムを用いることができる。ある態様としては、化学反応により微細な結晶を析出させた沈降炭酸カルシウムを用いることができ、別の態様としては、日本薬局方に基づく沈降炭酸カルシウムを用いることができる。
The antacid component contained in the antacid pharmaceutical composition of the present invention consists of sodium bicarbonate and calcium carbonate.
As sodium hydrogen carbonate, commercially available sodium hydrogen carbonate such as sodium hydrogen carbonate as a medical drug or sodium hydrogen carbonate for food addition can be used. As an aspect, sodium hydrogencarbonate based on the Japanese Pharmacopoeia can be used. It is desirable to use sodium hydrogen carbonate having a purity of 99% or higher, and in another embodiment, sodium hydrogen carbonate having a purity of 99.2% or higher is preferably used.
As calcium carbonate, commercially available calcium carbonate such as calcium carbonate as a medical drug or calcium carbonate for food additives can be used. As one aspect, precipitated calcium carbonate in which fine crystals are precipitated by a chemical reaction can be used, and as another aspect, precipitated calcium carbonate based on the Japanese Pharmacopoeia can be used.
（その他の成分）
本発明の制酸用医薬組成物は、上記の制酸成分の他に製薬学的に許容される担体等のその他の成分を含んでもよい。
その他の成分としては、安定化剤、界面活性剤、滑沢剤、可溶化剤、緩衝剤、甘味剤、基剤、吸着剤、矯味剤、結合剤、懸濁化剤、抗酸化剤、光沢剤、香料、コーティング剤、湿潤剤、湿潤調整剤、充填剤、消泡剤、清涼化剤、着色剤、等張化剤、軟化剤、乳化剤、粘稠剤、発泡剤、ｐＨ調整剤、賦形剤、分散剤、崩壊剤、崩壊補助剤、芳香剤、防湿剤、防腐剤、保存剤、溶解剤、溶解補助剤、溶剤、流動化剤等が挙げられる。
これらのその他の成分の具体例としては、例えば、「医薬品添加物事典２００７」（日本医薬品添加剤協会、薬事日報杜、２００７年発行）に記載されたものが挙げられる。
(Other ingredients)
The pharmaceutical composition for antacids of the present invention may contain other components such as a pharmaceutically acceptable carrier in addition to the above antacid components.
Other ingredients include stabilizers, surfactants, lubricants, solubilizers, buffers, sweeteners, bases, adsorbents, corrigents, binders, suspending agents, antioxidants, gloss Agent, fragrance, coating agent, wetting agent, wetting regulator, filler, defoaming agent, cooling agent, coloring agent, tonicity agent, softening agent, emulsifier, thickener, foaming agent, pH adjusting agent, emulsifying agent Examples include a shape agent, a dispersant, a disintegrant, a disintegration aid, a fragrance, a moisture-proof agent, a preservative, a preservative, a solubilizer, a solubilizer, a solvent, and a fluidizing agent.
Specific examples of these other components include those described in “Pharmaceutical Additives Encyclopedia 2007” (Japan Pharmaceutical Additives Association, Yakuji Nippo, published in 2007).
＜制酸用医薬組成物の製造方法＞
本発明の制酸用医薬組成物は、例えば以下のように製造できる。
炭酸水素ナトリウムの１００質量部、炭酸カルシウムの５０〜９０質量部、及び必要に応じてその他の成分を撹拌型混合器で混合し、水、アルコール又はそれらの混合物を加えて２〜６分間混練する。得られた混練物を押出造粒機を用いて造粒し、箱型乾燥機や流動層造粒乾燥機等の乾燥機を用いて水、アルコール又はそれらの混合物の大半を除去し顆粒を製造する。なお、造粒方法としては、押出造粒の他、撹拌造粒、流動層造粒、乾式造粒法等の医薬品の製造に通常用いられる公知の方法を採用することができる。
また、上記の混練物を箱型乾燥機や流動層造粒乾燥機等の乾燥機を用いて水、アルコール又はそれらの混合物の大半を除去した後、必要により粉砕してもよい。
顆粒中に含まれる水、アルコール又はそれらの混合物の量は、顆粒の１００質量部に対して、ある態様として０〜１０質量％であり、別の態様として０．０１〜５質量％であり、さらに別の態様として０．０１〜３質量％である。アルコールとしては、エタノール、イソプロパノール、プロピレングリコール、ポリエチレングリコールが例示できる。
なお、造粒後、乾燥機を用いた乾燥後、又は粉砕後に、篩を用いて目的の粒度の顆粒としてもよい。また、マルメライザー等の球形整粒機を用いて球形の顆粒としてもよい。
すべての操作は２０〜３０℃程度の室温で行うことができる。
<Method for producing pharmaceutical composition for antacid>
The pharmaceutical composition for antacids of the present invention can be produced, for example, as follows.
100 parts by weight of sodium hydrogen carbonate, 50 to 90 parts by weight of calcium carbonate, and other components as necessary are mixed in a stirring mixer, and water, alcohol or a mixture thereof is added and kneaded for 2 to 6 minutes. . The resulting kneaded product is granulated using an extrusion granulator, and most of water, alcohol or a mixture thereof is removed using a dryer such as a box dryer or fluidized bed granulator to produce granules. To do. In addition, as a granulation method, the well-known method normally used for manufacture of pharmaceuticals, such as stirring granulation, a fluidized-bed granulation, the dry granulation method other than extrusion granulation, is employable.
Further, the kneaded product may be pulverized as necessary after removing most of water, alcohol or a mixture thereof using a dryer such as a box dryer or a fluidized bed granulator dryer.
The amount of water, alcohol, or a mixture thereof contained in the granule is 0 to 10% by mass as an embodiment and 0.01 to 5% by mass as another embodiment with respect to 100 parts by mass of the granule. Furthermore, it is 0.01-3 mass% as another aspect. Examples of the alcohol include ethanol, isopropanol, propylene glycol, and polyethylene glycol.
In addition, it is good also as a granule of the target particle size using a sieve after granulation, drying using a dryer, or after grinding | pulverization. Moreover, it is good also as a spherical granule using spherical granulators, such as a Malmerizer.
All operations can be performed at room temperature of about 20-30 ° C.
顆粒の粒径はｄ９０として、ある態様として１００〜１０００μｍであり、別の態様としては１５０〜７００μｍであり、さらに別の態様としては２００〜５００μｍである。顆粒の粒径が上記範囲にあれば、服用感がよく、湿潤して固化することを防止でき、流動性が高いため医薬品製造上において有利である。顆粒の粒径はふるい分け法で測定した値を用いる。 The particle diameter of the granule is d90, which is 100 to 1000 μm as an aspect, 150 to 700 μm as another aspect, and 200 to 500 μm as another aspect. When the particle size of the granules is in the above range, the feeling of taking is good, it can be prevented from being wet and solidified, and the fluidity is high. The value measured by the sieving method is used for the particle size of the granules.
上記のように製造された顆粒は、そのまま散剤、細粒剤等の顆粒剤として用いることもできるが、カプセル剤の内容物として使用することもできる。また、上記のように製造された顆粒を直接打錠し、錠剤型の医薬組成物とすることもできる。 The granules produced as described above can be used as granules such as powders and fine granules as they are, but can also be used as the contents of capsules. In addition, the granules produced as described above can be directly compressed to form a tablet-type pharmaceutical composition.
上記のように製造された顆粒や錠剤型の医薬組成物は服用感の向上、及び制酸成分やその他の成分の安定性を考慮して、糖類や高分子等でコーティングされてもよい。使用される糖類や高分子等は、その目的に応じて通常の医薬品の製造に用いられる公知の糖類や高分子等を用いることができる。 The granule or tablet-type pharmaceutical composition produced as described above may be coated with a saccharide, a polymer, or the like in consideration of improvement in the ingestion and stability of the antacid component and other components. As the saccharides and polymers used, known saccharides and polymers used for the production of ordinary pharmaceuticals can be used depending on the purpose.
＜併用薬剤＞
本発明の制酸用医薬組成物と併用できる薬剤としては、前記制酸成分以外の制酸剤、健胃剤、消化剤、整腸剤、止瀉剤、鎮痛鎮痙剤、粘膜修復剤、ビタミン類、消泡剤等が挙げられる。なお、これらの成分は、必要に応じて本発明の制酸用医薬組成物に含有されていてもよい。但し、使用制限のあるアルミニウム、又は高齢者の使用に当たり事前相談の必要なマグネシウムを含む成分、及び前記制酸成分以外の制酸剤については、本発明の制酸用医薬組成物に含有されないことが好ましい。
<Combination drug>
Examples of drugs that can be used in combination with the pharmaceutical composition for antacids of the present invention include antacids other than the antacid components, gastric agents, digestive agents, intestinal regulating agents, antidiarrheals, analgesic and antispasmodic agents, mucosal repair agents, vitamins, antifoaming agents, etc. Is mentioned. In addition, these components may be contained in the pharmaceutical composition for antacids of the present invention as necessary. However, components containing aluminum that is restricted in use, or magnesium that needs prior consultation for use by the elderly, and antacids other than the antacid components should not be contained in the pharmaceutical composition for antacids of the present invention. Is preferred.
前記制酸成分以外の制酸剤としては、乾燥水酸化アルミニウムゲル、ケイ酸アルミン酸マグネシウム、ケイ酸マグネシウム、合成ケイ酸アルミニウム、合成ヒドロタルサイト、酸化マグネシウム、水酸化アルミナマグネシウム、水酸化アルミニウムゲル、水酸化マグネシウム、炭酸マグネシウム、メタケイ酸アルミン酸マグネシウム、無水リン酸水素カルシウム、リン酸水素カルシウム、烏賊骨、石決明、ボレイ、アミノ酢酸、ジヒドロキシアルミニウムアミノアセテート、ロートエキス等が挙げられる。これらの中でも、使用制限のあるアルミニウム、及び高齢者の使用に当たり事前相談の必要なマグネシウムを含まない前記制酸成分以外の制酸剤として、無水リン酸水素カルシウム、リン酸水素カルシウム、烏賊骨、石決明、ボレイ、アミノ酢酸、ロートエキスが挙げられる。 Examples of antacids other than the antacid component include dry aluminum hydroxide gel, magnesium silicate aluminate, magnesium silicate, synthetic aluminum silicate, synthetic hydrotalcite, magnesium oxide, magnesium alumina hydroxide, aluminum hydroxide gel. , Magnesium hydroxide, magnesium carbonate, magnesium aluminate metasilicate, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate, bandit bone, stone decision, volley, aminoacetic acid, dihydroxyaluminum aminoacetate, funnel extract and the like. Among these, as antacids other than the antacid component that does not contain aluminum that is restricted in use and magnesium that needs prior consultation for use by the elderly, anhydrous calcium hydrogen phosphate, calcium hydrogen phosphate, bandit bones, Examples include stone decision, volley, aminoacetic acid, and funnel extract.
健胃剤としては、アニス実、アロエ、ウイキョウ、ウコン、ウヤク、延命草、オウゴン、オウバク、オウレン、加工大蒜、ガジュツ、カッコウ、カラムス根、乾薑、枳殻、キジツ、ケイヒ、ゲンチアナ、コウジン、コウボク、ゴシュユ、胡椒、コロンボ、コンズランゴ、サンショウ、山奈、シソシ、シュクシャ、ショウキョウ、ショウズク、青皮、石菖根、センタウリウム草、センブリ、ソウジュツ、ソヨウ、大茴香、ダイオウ、チクセツニンジン、チョウジ、チンピ、トウガラシ、トウヒ、動物胆（ユウタンを含む。）、ニガキ、ニクズク、ニンジン、ハッカ（セイヨウハッカを含む）、篳撥（ヒハツ）、ビャクジュツ、ホップ、ホミカエキス、睡菜葉（スイサイヨウ）、モッコウ、ヤクチ、リュウタン、リョウキョウ、ウイキョウ油、ケイヒ油、ショウキョウ油、ショウズク油、チョウジ油、トウヒ油、ハッカ油、レモン油、Ｌ−メントール、ＤＬ−メントール、塩酸ベタイン、グルタミン酸塩酸塩、塩化カルニチン、塩化ベタネコール、乾燥酵母等が挙げられる。 Examples of stomachic agents include aniseed fruit, aloe, fennel, turmeric, cormorant, life-prolonging grass, cormorant, cormorant, cormorant, calamand, root, dry husk, chaff, pheasant, keihi, gentian, kojin, koboku, goshuyu. , Cucumber, colombo, conzurango, salamander, yamana, shisoshi, shukusha, shrimp, shrimp, green bark, stone root, centaurium grass, embroidery, sojutsu, soyo, daikon, daiou, chikutsujinjin, clove, chimpi, chili pepper, Spruce, animal gall (including yuutan), oyster, nutmeg, carrot, mint (including mint), repellent (baboon), peafowl, hops, honey extract, sleepy leaves (sweet potato), mokko, yakchi, ryutan, Ryokyo, fennel oil, ke Heat oil, ginger oil, cardamom oil, clove oil, spruce oil, peppermint oil, lemon oil, L- menthol, DL-menthol, betaine hydrochloride, glutamic acid hydrochloride, carnitine chloride, bethanechol chloride, dry yeast and the like.
消化剤としては、でんぷん消化酵素、たん白消化酵素、脂肪消化酵素、繊維素消化酵素、ウルソデスオキシコール酸、オキシコーラン酸塩類、コール酸、胆汁末、胆汁エキス（末）、デヒドロコール酸、動物胆（ユウタンを含む。）等が挙げられる。 As digestive agents, starch digestive enzyme, protein digestive enzyme, fat digestive enzyme, fibrin digestive enzyme, ursodeoxycholic acid, oxycoranoates, cholic acid, bile powder, bile extract (powder), dehydrocholic acid, Examples include animal gall (including yutan).
整腸剤としては、整腸生菌成分、赤芽柏、アセンヤク、ウバイ、ケツメイシ、ゲンノショウコ等が挙げられる。 Examples of the intestinal regulating agent include live intestinal fungi components, red buds, asenyaku, ubai, ketsumeishi and gennoshouko.
止瀉剤としては、アクリノール、塩化ベルベリン、グアヤコール、クレオソート、サリチル酸フェニル、炭酸グアヤコール、タンニン酸ベルベリン、ジサリチル酸ビスマス、ジ硝酸ビスマス、ジ炭酸ビスマス、ジ没食子酸ビスマス、タンニン酸、タンニン酸アルブミン、メチレンチモールタンニン、カオリン、天然ケイ酸アルミニウム、ヒドロキシナフトエ酸アルミニウム、ペクチン、薬用炭、沈降炭酸カルシウム、乳酸カルシウム、リン酸水素カルシウム、アセンヤク、ウバイ、オウバク、オウレン、クジン、ゲンノショウコ、五倍子、サンザシ、センブリ、ヨウバイヒ等が挙げられる。これらの中でも、使用制限のあるアルミニウム、及び高齢者の使用に当たり事前相談の必要なマグネシウムを含まない止瀉剤として、アクリノール、塩化ベルベリン、グアヤコール、クレオソート、サリチル酸フェニル、炭酸グアヤコール、タンニン酸ベルベリン、ジサリチル酸ビスマス、ジ硝酸ビスマス、ジ炭酸ビスマス、ジ没食子酸ビスマス、タンニン酸、タンニン酸アルブミン、メチレンチモールタンニン、カオリン、ペクチン、薬用炭、沈降炭酸カルシウム、乳酸カルシウム、リン酸水素カルシウム、アセンヤク、ウバイ、オウバク、オウレン、クジン、ゲンノショウコ、五倍子、サンザシ、センブリ、ヨウバイヒが挙げられる。 Antidiarrheal agents include acrinol, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate, bismuth disalicylate, bismuth dinitrate, bismuth dicarbonate, bismuth digallate, tannic acid, albumin tannate, methylene Thymol tannin, kaolin, natural aluminum silicate, hydroxy naphthoic acid aluminum, pectin, medicinal charcoal, precipitated calcium carbonate, calcium lactate, calcium hydrogen phosphate, acacia, buckwheat, duck, auren, kudin, gentian pepper, quintuplet, hawthorn, assembly, For example, Yeobei. Among these, as an antipruritic agent that does not contain aluminum that is restricted in use and magnesium that needs to be consulted in advance for use by the elderly, acrinol, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate, diester Bismuth salicylate, bismuth dinitrate, bismuth dicarbonate, bismuth digallate, tannic acid, albumin tannate, methylenethymol tannin, kaolin, pectin, medicinal charcoal, precipitated calcium carbonate, calcium lactate, calcium hydrogen phosphate, asenyaku, ubai, Examples include butterflies, aurens, kujin, genokosho, pentaploids, hawthorn, assemblies, and yellow baboons.
鎮痛鎮痙剤としては、塩酸オキシフェンサイクリミン、塩酸ジサイクロミン、塩酸メチキセン、臭化水素酸スコポラミン、臭化メチルアトロピン、臭化メチルアニソトロピン、臭化メチルスコポラミン、臭化メチル−Ｌ−ヒヨスチアミン、臭化メチルベナクチジウム、ベラドンナエキス、ヨウ化イソプロパミド、ヨウ化ジフェニルピペリジノメチルジオキソラン、ロートエキス、ロート根総アルカロイドクエン酸塩、塩酸パパベリン、アミノ安息香酸エチル、エンゴサク、カンゾウ、コウボク、シャクヤク等が挙げられる。 Analgesic and antispasmodic agents include oxyphencyclimine hydrochloride, dicyclomine hydrochloride, methixene hydrochloride, scopolamine hydrobromide, methyl atropine bromide, methyl anisotropine bromide, methyl scopolamine bromide, methyl-L-hyostiamine bromide, bromide. Examples include methylbenactidium, belladonna extract, isopropamide iodide, diphenylpiperidinomethyldioxolane, funnel extract, funnel root total alkaloid citrate, papaverine hydrochloride, ethyl aminobenzoate, engosaku, licorice, kokuboku, peonies, etc. It is done.
粘膜修復剤としては、アズレンスルホン酸ナトリウム、アルジオキサ、グリチルリチン酸及びその塩類並びに甘草抽出物、Ｌ−グルタミン、銅クロロフィリンカリウム、銅クロロフィリンナトリウム、塩酸ヒスチジン、ブタ胃壁ペプシン分解物、ブタ胃壁酸加水分解物、メチルメチオニンスルホニウムクロライド、赤芽柏、エンゴサク、カンゾウ等が挙げられる。 Examples of mucosal repair agents include sodium azulene sulfonate, aldioxa, glycyrrhizic acid and salts thereof, and licorice extract, L-glutamine, copper chlorophyllin potassium, copper chlorophyllin sodium, histidine hydrochloride, porcine gastric wall pepsin degradation product, porcine gastric wall acid hydrolyzate , Methylmethionine sulfonium chloride, red bud, engosac, licorice and the like.
ビタミン類としては、ビタミンＢ１若しくはその誘導体又はその塩類、ニコチン酸アミド、パントテン酸カルシウム、ビオチン、ビタミンＢ２若しくはその誘導体又はその塩類、ビタミンＢ６若しくはその誘導体又はその塩類、ビタミンＣ若しくはその誘導体又はその塩類等が挙げられる。 As vitamins, vitamin B1 or a derivative thereof or a salt thereof, nicotinamide, calcium pantothenate, biotin, vitamin B2 or a derivative thereof or a salt thereof, vitamin B6 or a derivative thereof or a salt thereof, vitamin C or a derivative thereof or a salt thereof Etc.
消泡剤としては、ジメチルポリシロキサン等が挙げられる。 Examples of the antifoaming agent include dimethylpolysiloxane.
また、本発明の制酸用医薬組成物と併用できる上記以外の薬剤として、ムスカリン受容体遮断薬、ヒスタミン受容体遮断薬、プロトンポンプ阻害薬、胃粘膜保護成分、プロスタグランジン製剤、粘膜分泌促進薬を挙げることもできる。なお、これらの成分は、必要に応じて本発明の制酸用医薬組成物に含有されていてもよい。但し、使用制限のあるアルミニウム、又は高齢者の使用に当たり事前相談の必要なマグネシウムを含む成分については、本発明の制酸用医薬組成物に含有されないことが好ましい。 Other drugs that can be used in combination with the pharmaceutical composition for antacids of the present invention include muscarinic receptor blockers, histamine receptor blockers, proton pump inhibitors, gastric mucosa protective components, prostaglandin preparations, mucosal secretion promotion You can also list drugs. In addition, these components may be contained in the pharmaceutical composition for antacids of the present invention as necessary. However, it is preferable not to contain the aluminum containing restricted use or the component containing magnesium that needs prior consultation when used by the elderly in the pharmaceutical composition for antacids of the present invention.
ムスカリン受容体遮断薬としては、スコポラミン、プロパンテリン、ピレンゼピン等が挙げられる。
ヒスタミン受容体遮断薬としては、シメチジン、ラニチジン、ファモチジン等が挙げられる。
プロトンポンプ阻害薬としては、オメプラゾール、ランソプラゾール、ラベプラゾール、エソメプラゾール等が挙げられる。
胃粘膜保護成分としては、スクラルファート等が挙げられる。
プロスタグランジン製剤としては、ミソプロストール等が挙げられる。
粘膜分泌促進薬としては、レバミピド、テプレノン等が挙げられる。
Examples of muscarinic receptor blockers include scopolamine, propantheline, pirenzepine and the like.
Examples of histamine receptor blockers include cimetidine, ranitidine, famotidine and the like.
Examples of proton pump inhibitors include omeprazole, lansoprazole, rabeprazole, esomeprazole and the like.
Examples of the gastric mucosa protective component include sucralfate.
Examples of the prostaglandin preparation include misoprostol.
Examples of mucosal secretion promoting agents include rebamipide and teprenone.
＜用法用量＞
本発明の制酸用医薬組成物は、胃内に分泌された胃酸若しくは胃内で分泌される胃酸に直接作用させるため、通常経口投与される。経口投与に際しては、固体医薬組成物として、若しくは液体医薬組成物として投与することができる。
散剤及び細粒剤等の顆粒剤、カプセル剤、錠剤等の固体医薬組成物においては、不活性な添加剤、例えば滑沢剤、崩壊剤、安定化剤、溶解補助剤をさらに含有してもよい。
乳濁剤、溶液剤、懸濁剤、シロップ剤、経口ゼリー剤等の液体医薬組成物においては、水やエタノールのような不活性な希釈剤を含み、それ以外に不活性な添加剤、例えば可溶化剤、懸濁化剤、甘味剤、芳香剤、防腐剤をさらに含有してもよい。
<Dosage>
The pharmaceutical composition for antacids of the present invention is usually administered orally because it directly acts on gastric acid secreted in the stomach or gastric acid secreted in the stomach. For oral administration, it can be administered as a solid pharmaceutical composition or as a liquid pharmaceutical composition.
In solid pharmaceutical compositions such as powders and granules such as fine granules, capsules and tablets, an inert additive such as a lubricant, a disintegrant, a stabilizer, a solubilizing agent may be further contained. Good.
Liquid pharmaceutical compositions such as emulsions, solutions, suspensions, syrups, oral jellys, etc. contain inert diluents such as water and ethanol, and other inert additives such as, for example, You may further contain a solubilizer, a suspending agent, a sweetening agent, a fragrance | flavor, and an antiseptic | preservative.
本発明の制酸用医薬組成物に含有される制酸成分は、ある態様として、１回あたりの成人服用量として、３００〜４２０ｍｇの炭酸水素ナトリウムと、前記炭酸水素ナトリウムの１００質量部に対して５０〜９０質量部の炭酸カルシウムからなる。別の態様としては、１回あたりの成人服用量として、３２０〜４２０ｍｇの炭酸水素ナトリウムと、前記炭酸水素ナトリウムの１００質量部に対して５０〜９０質量部の炭酸カルシウムからなる。さらに別の態様としては、１回あたりの成人服用量として、３５０〜４２０ｍｇの炭酸水素ナトリウムと、前記炭酸水素ナトリウムの１００質量部に対して５０〜９０質量部の炭酸カルシウムからなる。
本発明の制酸用医薬組成物に含まれる炭酸水素ナトリウムの量が、１回あたりの成人服用量として、前記下限値以上であれば、十分な酸中和作用が得られ、前記上限値以下であれば、過剰な酸中和作用の発現、及びそれに伴う反動的酸分泌を抑制できる。
The antacid component contained in the pharmaceutical composition for antacids of the present invention is, as one embodiment, 300 to 420 mg of sodium bicarbonate and 100 parts by mass of the sodium bicarbonate as an adult dose per time. And 50 to 90 parts by mass of calcium carbonate. As another aspect, the dose per adult consists of 320 to 420 mg of sodium bicarbonate and 50 to 90 parts by mass of calcium carbonate with respect to 100 parts by mass of the sodium bicarbonate. In still another embodiment, the dose per adult consists of 350 to 420 mg of sodium bicarbonate and 50 to 90 parts by mass of calcium carbonate with respect to 100 parts by mass of the sodium bicarbonate.
If the amount of sodium hydrogen carbonate contained in the pharmaceutical composition for antacids of the present invention is not less than the lower limit as an adult dose per dose, a sufficient acid neutralization effect can be obtained and not more than the upper limit. If so, it is possible to suppress the expression of an excessive acid neutralizing action and the accompanying reaction acid secretion.
本発明の制酸用医薬組成物は、酸中和作用の即効性を有するため、胃痛、胸やけ、胃もたれと言った症状が生じた際、あるいは上記症状が生じると思われるタイミングで適宜服用することができる。ある態様としては、本発明の制酸用医薬組成物は上記症状が発現しやすいとされる、食前に服用することができる。食前とは、食事の３０〜６０分前の時間帯を指す。 Since the pharmaceutical composition for antacids of the present invention has an immediate effect of acid neutralization, it is appropriately taken when symptoms such as stomach pain, heartburn, and stomach stagnation occur, or when the above symptoms are expected to occur. can do. As a certain aspect, the pharmaceutical composition for antacids of the present invention can be taken before meals, in which the above symptoms are likely to occur. “Before meal” refers to a time zone 30 to 60 minutes before meal.
本発明の制酸用医薬組成物は、後述の通り、１分程度以下で酸中和作用を発現し、かつ、持続性の制酸剤を含有していないにもかかわらず、３０分程度以上の酸中和作用の持続を示す。従って、服用した直後に胃酸の中和による上記症状の緩和を達成することができ、かつ、食前に服用した場合には、空腹時の胃の内容物の滞留時間である３０分を目安に酸中和作用を持続させることができる。
また、本発明の制酸用医薬組成物の酸中和作用の持続は３０分程度以上であるため、制酸効果の発現の遅い、例えば、制酸効果の発現に３０分程度以上の時間を要するような他の薬剤と併用しても、過剰な酸中和作用を示すことがなく、安全に他の薬剤との併用が可能である。
The pharmaceutical composition for antacids of the present invention develops an acid neutralization effect in about 1 minute or less as described later, and does not contain a long-lasting antacid, but about 30 minutes or more. Shows the persistence of the acid neutralization effect. Therefore, the above symptoms can be alleviated by neutralization of stomach acid immediately after taking, and when taken before meals, the acid content can be reduced to 30 minutes, which is the residence time of stomach contents on an empty stomach. Neutralizing action can be maintained.
Further, since the duration of the acid neutralization action of the pharmaceutical composition for antacids of the present invention is about 30 minutes or more, the onset of the antacid effect is slow, for example, about 30 minutes or more is required for the onset of the antacid effect. Even when used in combination with other drugs as required, it does not exhibit an excessive acid neutralizing action and can be used in combination with other drugs safely.
さらに、本発明の制酸用医薬組成物は、制酸成分として消化酵素を含まないため、食前の服用であっても、消化酵素による胃壁や胃粘膜の自己消化が起こらず、安全に使用することが可能である。 Furthermore, since the pharmaceutical composition for antacids of the present invention does not contain digestive enzymes as an antacid component, even if taken before meals, the digestive enzymes do not cause self-digestion of the stomach wall and stomach mucous membranes and can be used safely. It is possible.
以下に実施例を挙げて本発明を具体的に説明するが、本発明はこれらの実施例に限定されない。 EXAMPLES The present invention will be specifically described below with reference to examples, but the present invention is not limited to these examples.
それぞれの実施例及び比較例で用いた各成分は以下のとおりである。 Each component used in each example and comparative example is as follows.
炭酸水素ナトリウム：日本薬局方 炭酸水素ナトリウム（重曹）（旭硝子株式会社製）
炭酸カルシウム：日本薬局方 沈降炭酸カルシウム（備北粉化工業株式会社製）
メタケイ酸アルミン酸マグネシウム：メタケイ酸アルミン酸マグネシウム（ノイシリン（登録商標））（富士化学工業株式会社製）
Sodium bicarbonate: Japanese Pharmacopoeia Sodium bicarbonate (Baking soda) (Asahi Glass Co., Ltd.)
Calcium carbonate: Japanese Pharmacopoeia Precipitated calcium carbonate (Bihoku Powder Chemical Co., Ltd.)
Magnesium aluminate metasilicate: Magnesium aluminate metasilicate (Neusilin (registered trademark)) (Fuji Chemical Industry Co., Ltd.)
実施例１
炭酸水素ナトリウム４００ｍｇ及び炭酸カルシウム３００ｍｇを混合して試料１を調製した。
試料１の制酸効果を、フックス変法試験を用いて測定した。具体的手順は以下のとおりである。
ビーカーに０．１ｍｏｌ／Ｌの塩酸の５０ｍＬを正確に量りとり、マグネチックスターラーを用いて約３００回転／分で撹拌しながら試料１を加えた。試料１を加えてから操作を終了するまでの間、液のｐＨを連続的に測定した。試料１を加えて１０分後に定量ポンプを使用して、０．１ｍｏｌ／Ｌの塩酸を２ｍＬ／分の速度で連続的に加えた。操作中は液の温度を３７±２℃に維持した。
Example 1
Sample 1 was prepared by mixing 400 mg of sodium bicarbonate and 300 mg of calcium carbonate.
The antacid effect of Sample 1 was measured using a modified Fuchs test. The specific procedure is as follows.
In a beaker, 50 mL of 0.1 mol / L hydrochloric acid was accurately weighed, and Sample 1 was added while stirring at about 300 rpm using a magnetic stirrer. From the time sample 1 was added to the end of the operation, the pH of the liquid was continuously measured. Ten minutes after adding Sample 1, 0.1 mol / L hydrochloric acid was continuously added at a rate of 2 mL / min using a metering pump. During operation, the temperature of the solution was maintained at 37 ± 2 ° C.
その結果、制酸効果発現時間は１分以下であり、制酸効果持続時間Ａは３５分であり、制酸効果持続時間Ｂは３７分であり、最大ｐＨは７．２であった。
なお、制酸効果発現時間とは、試料を添加してから液のｐＨが６に上がるまでにかかった時間であり、制酸効果持続時間Ａとは、試料を添加してから液のｐＨが６以上に上昇した後、再び液のｐＨが４に下がるまでにかかった時間であり、制酸効果持続時間Ｂとは、試料を添加してから液のｐＨが６以上に上昇した後、再び液のｐＨが３．５に下がるまでにかかった時間であり、最大ｐＨとは、制酸効果持続時間内における最大の液のｐＨ値である。
As a result, the antacid effect onset time was 1 minute or less, the antacid effect duration A was 35 minutes, the antacid effect duration B was 37 minutes, and the maximum pH was 7.2.
The antacid effect onset time is the time taken from the addition of the sample to the pH of the solution rising to 6, and the antacid effect duration A is the pH of the solution after the sample is added. The time taken for the pH of the liquid to fall to 4 again after rising to 6 or more. The antacid effect duration B is again after the pH of the liquid has risen to 6 or more after adding the sample. This is the time taken for the pH of the liquid to drop to 3.5, and the maximum pH is the maximum pH value of the liquid within the duration of the antacid effect.
比較例１〜２
試料に含まれる制酸成分を表１のように変更した以外は実施例１と同様にして液のｐＨを連続的に測定した。
制酸効果発現時間、制酸効果持続時間Ａ及び最大ｐＨの結果を表１に示す。
Comparative Examples 1-2
The pH of the solution was continuously measured in the same manner as in Example 1 except that the antacid component contained in the sample was changed as shown in Table 1.
Table 1 shows the results of the antacid effect onset time, the antacid effect duration A, and the maximum pH.
以上の結果から、本発明の制酸用医薬組成物である実施例１においては、制酸効果発現時間が１分未満であり、炭酸水素ナトリウム及びメタケイ酸アルミン酸マグネシウムを含む比較例１と比較しても、酸中和作用の即効性を有することが明らかとなった。このことから、酸中和作用の即効性を発現させるには、炭酸水素ナトリウムと炭酸カルシウムとの組合せが必要であることが分かった。
また、本発明の制酸用医薬組成物である実施例１においては、持続性の制酸剤を含んでいないにもかかわらず、持続性の制酸剤であるメタケイ酸アルミン酸マグネシウムをさらに含む比較例２と同等の制酸効果持続時間を示した。
さらに、本発明の制酸用医薬組成物である実施例１においては、最大ｐＨが比較例１及び２と同等の７．２であり、反動的酸分泌を引き起こすおそれが極めて小さいことが明らかとなった。
From the above results, in Example 1 which is a pharmaceutical composition for antacids of the present invention, the antacid effect onset time is less than 1 minute, and compared with Comparative Example 1 containing sodium bicarbonate and magnesium aluminate metasilicate. Even so, it became clear that it had an immediate effect of acid neutralization. From this, it was found that a combination of sodium hydrogen carbonate and calcium carbonate is necessary to develop the immediate effect of the acid neutralization action.
Further, Example 1 which is a pharmaceutical composition for antacids of the present invention further contains magnesium metasilicate aluminate, which is a long-lasting antacid, even though it does not contain a long-lasting antacid. An antacid effect duration equivalent to that of Comparative Example 2 was exhibited.
Furthermore, in Example 1, which is the pharmaceutical composition for antacids of the present invention, the maximum pH is 7.2, which is the same as in Comparative Examples 1 and 2, and it is clear that there is very little risk of causing reaction acid secretion. became.
なお、前述の特許文献１の比較例２では、炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量が５０〜９０質量部ではないが、制酸成分として炭酸水素ナトリウムと炭酸カルシウムのみを含んだ制酸用医薬組成物が開示されている。特許文献１の表２によれば、本明細書における制酸効果持続時間Ｂに相当する、ｐＨが３．５以下になるまでの時間は、３２分であったことが記載されている。 In addition, in the comparative example 2 of the above-mentioned patent document 1, although content of calcium carbonate with respect to 100 mass parts of sodium hydrogen carbonate is not 50-90 mass parts, only sodium hydrogen carbonate and calcium carbonate were included as an antacid component. A pharmaceutical composition for antacid is disclosed. According to Table 2 of Patent Document 1, it is described that the time until the pH becomes 3.5 or less, corresponding to the antacid effect duration B in the present specification, was 32 minutes.
制酸効果持続時間は、胃内のｐＨが通常の胃の状態のｐＨ、即ち胃酸のｐＨにおおよそ戻るまでの時間を模したものであり、以下により理論値を算出することができる。
フックス変法試験では、０．１ｍｏｌ／Ｌの塩酸を人工胃酸として使用しており、分子量８４の炭酸水素ナトリウムの１ｇは、１１９ｍＬの人工胃酸を中和することができ、分子量１００の炭酸カルシウムの１ｇは、２００ｍＬの人工胃酸を中和することができる。また、フックス変法試験では、試料添加時には５０ｍＬの人工胃液が存在し、試料添加から１０分後以降、２ｍＬ／分の人工胃液が連続的に添加される。これは、胃液の分泌を模したものである。
The duration of the antacid effect simulates the time until the pH in the stomach returns to the normal pH of the stomach, that is, the pH of the stomach acid, and the theoretical value can be calculated as follows.
In the modified Fuchs test, 0.1 mol / L hydrochloric acid is used as artificial gastric acid, and 1 g of sodium bicarbonate having a molecular weight of 84 can neutralize 119 mL of artificial gastric acid, 1 g can neutralize 200 mL of artificial gastric acid. In the modified Fuchs test, 50 mL of artificial gastric juice is present at the time of sample addition, and 2 mL / min of artificial gastric fluid is continuously added after 10 minutes from the sample addition. This mimics the secretion of gastric juice.
これらの数値から、特許文献１の比較例２、即ち炭酸水素ナトリウムの３００ｍｇと炭酸カルシウムの４００ｍｇを使用した場合（なお、炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量は１３３質量部である。）、１１５．７ｍＬの人工胃酸を中和することができるため、理論値としては全ての制酸成分が消費されるまでに４３分程度かかる。しかし、特許文献１によれば、その制酸効果持続時間は３２分である。
その一方、本発明の制酸用医薬組成物である実施例１においては、炭酸水素ナトリウムの４００ｍｇと炭酸カルシウムの３００ｍｇを使用しているため（なお、炭酸水素ナトリウムの１００質量部に対する炭酸カルシウムの含有量は７５質量部である。）、１０７．６ｍＬの人工胃酸を中和することしかできない。
従って、特許文献１の比較例２の結果から考えれば、本明細書における実施例１の制酸効果持続時間は、特許文献１の比較例２の制酸効果持続時間より短くなるはずである。しかし、それにもかかわらず本明細書における実施例１の制酸効果持続時間は、理論値である３８．８分と同等の３７分であり、特許文献１の比較例２の制酸効果持続時間より長く、特許文献１の比較例２の結果からは到底導き出されない、顕著に優れた制酸効果持続時間を有することが明らかである。
From these numerical values, Comparative Example 2 of Patent Document 1, that is, when 300 mg of sodium bicarbonate and 400 mg of calcium carbonate are used (note that the content of calcium carbonate with respect to 100 parts by mass of sodium bicarbonate is 133 parts by mass) )) Since 115.7 mL of artificial gastric acid can be neutralized, it takes about 43 minutes as a theoretical value until all antacid components are consumed. However, according to Patent Document 1, the duration of the antacid effect is 32 minutes.
On the other hand, in Example 1 which is a pharmaceutical composition for antacids of the present invention, 400 mg of sodium bicarbonate and 300 mg of calcium carbonate are used (note that calcium carbonate is added to 100 parts by mass of sodium bicarbonate. The content is 75 parts by mass.), 107.6 mL of artificial gastric acid can only be neutralized.
Therefore, considering the result of Comparative Example 2 of Patent Document 1, the antacid effect duration of Example 1 in this specification should be shorter than the antacid effect duration of Comparative Example 2 of Patent Document 1. However, the antacid effect duration of Example 1 in this specification is 37 minutes equivalent to the theoretical value of 38.8 minutes, and the antacid effect duration of Comparative Example 2 of Patent Document 1 is nevertheless. It is clear that it has a significantly superior antacid effect duration, which is longer and is not at all derived from the results of Comparative Example 2 of Patent Document 1.
本発明によれば、使用制限のあるアルミニウム、及び高齢者の使用に当たり事前相談の必要なマグネシウムを含有せず、かつ、酸中和作用の即効性と持続性を兼ね備え、反動的酸分泌を引き起こすおそれが極めて小さい制酸用医薬組成物を提供することができる。 According to the present invention, it does not contain aluminum that is restricted in use and magnesium that needs to be consulted in advance for use by the elderly, and has both immediate effect and sustainability of acid neutralization and causes reaction acid secretion. It is possible to provide a pharmaceutical composition for antacids with very little fear.
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| JPS6072832A (en) * | 1983-09-02 | 1985-04-24 | レキツト アンド コ−ルマン プロダクツ リミテツド | Drug composition |
| JPH08259445A (en) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | Medicinal composition for improving gastric emptying performance |
| JP2006528181A (en) * | 2003-07-18 | 2006-12-14 | サンタラス インコーポレイティッド | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
| JP2008500365A (en) * | 2004-05-25 | 2008-01-10 | サンタラス インコーポレイティッド | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using the same |
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| JPS6072832A (en) * | 1983-09-02 | 1985-04-24 | レキツト アンド コ−ルマン プロダクツ リミテツド | Drug composition |
| JPH08259445A (en) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | Medicinal composition for improving gastric emptying performance |
| JP2006528181A (en) * | 2003-07-18 | 2006-12-14 | サンタラス インコーポレイティッド | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using them |
| JP2008500365A (en) * | 2004-05-25 | 2008-01-10 | サンタラス インコーポレイティッド | Pharmaceutical formulations useful for inhibiting acid secretion and methods for making and using the same |
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| IRYO YAKUGAKU, vol. 28(6), JPN6019021460, 2002, pages 559 - 563, ISSN: 0004051181 * |
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