JPH0665646B2 - Medicinal nitroglycerin composition - Google Patents
Medicinal nitroglycerin compositionInfo
- Publication number
- JPH0665646B2 JPH0665646B2 JP12432282A JP12432282A JPH0665646B2 JP H0665646 B2 JPH0665646 B2 JP H0665646B2 JP 12432282 A JP12432282 A JP 12432282A JP 12432282 A JP12432282 A JP 12432282A JP H0665646 B2 JPH0665646 B2 JP H0665646B2
- Authority
- JP
- Japan
- Prior art keywords
- composition
- medicinal
- crystalline cellulose
- nitroglycerin
- present
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims description 12
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 title claims description 7
- 239000000006 Nitroglycerin Substances 0.000 title claims description 7
- 229960003711 glyceryl trinitrate Drugs 0.000 title claims description 7
- 229920002678 cellulose Polymers 0.000 claims description 13
- 239000001913 cellulose Substances 0.000 claims description 13
- 235000010980 cellulose Nutrition 0.000 description 12
- 239000003960 organic solvent Substances 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 230000035945 sensitivity Effects 0.000 description 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 229920003084 Avicel® PH-102 Polymers 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000002360 explosive Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 230000003301 hydrolyzing effect Effects 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000000304 vasodilatating effect Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Description
【発明の詳細な説明】 本発明は新規な医薬用ニトログリセリン（以下Ｎ／Ｇと
略す）組成物に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a novel pharmaceutical nitroglycerin (hereinafter abbreviated as N / G) composition.
ニトログリセリン（以下、Ｎ／Ｇと略す）は近来、すぐ
れた末梢血管拡張効果が認められ、狭心症、心筋梗塞の
治療に応用されている。一方、Ｎ／Ｇはダイナマイトの
爆発成分であつて極めて危険な物質であると同時に、そ
の蒸気を吸入することにより頭痛などの不快感を生ぜし
めるおそれがあるためにその取扱いには充分な注意が必
要となる。Nitroglycerin (hereinafter abbreviated as N / G) has recently been recognized for its excellent peripheral vasodilatory effect and has been applied to the treatment of angina and myocardial infarction. On the other hand, N / G is an explosive component of dynamite and is an extremely dangerous substance. At the same time, inhaling the vapor may cause discomfort such as headache, so be careful when handling it. Will be needed.
従来、Ｎ／Ｇを微結晶セルロースに吸着させる方法は例
えば1965年に刊行されたジャーナル・オブ・フアーマシ
ユーテイカルサイエンス、第54巻、447ページに記載が
あり公知である。しかしながら、この方法による製剤は
Ｎ／Ｇの揮散性が少なくなく十分に満足なものとは言え
ない。Conventionally, a method for adsorbing N / G on microcrystalline cellulose is known, for example, as described in Journal of Pharmaceutical Sciences, Vol. 54, p. 447, published in 1965. However, the formulation prepared by this method is not sufficiently satisfactory because it has a low volatility of N / G.
本発明は、高濃度にＮ／Ｇを吸着させても、取扱い上安
全でありかつＮ／Ｇ揮散率が比較的低い医薬用Ｎ／Ｇ組
成物の提供を目的とするものである。It is an object of the present invention to provide a medicinal N / G composition which is safe in handling and has a relatively low N / G volatilization rate even when N / G is adsorbed at a high concentration.
本発明は、限定された性質を有する結晶セルロースにＮ
／Ｇを吸着させることにより上記の如くすぐれた特徴を
有する医薬用Ｎ／Ｇ組成物を提供することに関する。The present invention provides N-based crystalline cellulose having limited properties.
The present invention relates to providing a medicinal N / G composition having excellent characteristics as described above by adsorbing / G.
すなわち、本発明は、目の開きが0.074mmの篩による篩
分残分が５〜35％を占め、かつ比容積が２〜4cc／ｇで
ある結晶性セルロース100部に、２〜20部（重量）のニ
トログリセリンを吸着させてなる医薬用ニトログリセリ
ン組成物である。That is, in the present invention, 2 to 20 parts (100 parts of crystalline cellulose having a sieve fraction residue of 5 to 35% by a sieve having an opening of 0.074 mm and a specific volume of 2 to 4 cc / g) ( It is a medicinal nitroglycerin composition obtained by adsorbing (by weight) nitroglycerin.
本発明の組成物は、医薬その他の分野に有利に利用する
ことができるが、特にＮ／Ｇを高濃度で使用する貼付剤
用途にはその低揮散性を生かして極めて有効に応用し得
る。The composition of the present invention can be advantageously used in the fields of medicine and other fields, but it can be very effectively applied to patch applications where N / G is used at a high concentration due to its low volatility.
本発明に使用される結晶性セルロースは、高純度の精製
パルプを一定の条件下で鉱酸によつて加水分解して非結
晶領域を洗滌、除去した後、磨砕、精製、乾燥して得ら
れる微粉末であり、目の開きが0.074mmの篩による篩分
残分が５〜35％であり、かつ、比容積が２〜4c.c.／ｇ
のものである。この場合、目の開きが0.074mmの篩によ
る篩分残分および／または比容積が上記範囲をはずれる
と、Ｎ／Ｇの微結晶セルロースへの均一分散、均一吸着
が困難となり安定した医薬用Ｎ／Ｇ組成物を得ることが
困難となる。The crystalline cellulose used in the present invention is obtained by hydrolyzing a high-purity refined pulp with a mineral acid under certain conditions to wash and remove an amorphous region, and then grind, purify, and dry it. It is a fine powder that has a mesh size of 0.074 mm and a sieve residue of 5 to 35%, and a specific volume of 2 to 4 c.c./g.
belongs to. In this case, if the sieve residue and / or the specific volume with a sieve having an opening of 0.074 mm deviates from the above range, it is difficult to uniformly disperse and uniformly adsorb N / G on microcrystalline cellulose, and stable N It is difficult to obtain the / G composition.
また、本発明で使用する結晶性セルロースに含有される
Ｎ／Ｇの割合は、結晶性セルロース100部に対して、２
〜20部（重量）の割合で使用する必要がある。Ｎ／Ｇの
割合が２部（重量）未満の場合には、製剤に応用した場
合の薬効が不充分であり、また、20部（重量）より多い
場合には、組成物の感度が鋭感で、取扱い安全上の危険
度が高くなり好ましくない。The ratio of N / G contained in the crystalline cellulose used in the present invention is 2 with respect to 100 parts of crystalline cellulose.
Must be used at a rate of ~ 20 parts (weight). When the ratio of N / G is less than 2 parts (weight), the drug effect when applied to the preparation is insufficient, and when it exceeds 20 parts (weight), the sensitivity of the composition is sharp. Therefore, it is not preferable because the risk of handling safety is high.
本発明の組成物は、結晶性セルロースとＮ／Ｇを直接混
合して得ることができる他、例えば結晶性セルロースに
Ｎ／Ｇが溶解した有機溶媒溶液を加え、均一に混合し、
乾燥することによつても得られる。この場合に、結晶性
セルロースの他に種々の医薬用賦形剤を添加してもよ
い。The composition of the present invention can be obtained by directly mixing crystalline cellulose and N / G, or for example, an organic solvent solution in which N / G is dissolved in crystalline cellulose is added and uniformly mixed,
It can also be obtained by drying. In this case, various pharmaceutical excipients may be added in addition to crystalline cellulose.
使用する有機溶媒は、Ｎ／Ｇが溶解する溶媒ならば特に
制限はなく、疎水性有機溶媒および親水性有機溶媒の双
方が使用できるが、特にクロロホルム、ベンゼン、メタ
ノール、エタノール、アセトンなどの揮発性溶媒が好ま
しい。The organic solvent to be used is not particularly limited as long as it dissolves N / G, and both hydrophobic organic solvent and hydrophilic organic solvent can be used, but especially volatile solvents such as chloroform, benzene, methanol, ethanol, and acetone. Solvents are preferred.
次に本発明を実施例により説明する。Next, the present invention will be described with reference to examples.
実施例１ 表−１に示す粒度及び比容積を有する結晶性セルロース
（アビセル PH101）にＮ／Ｇを10％含浸させた試料を
調製し、40℃で５日間放置したときのNG残存率を測定し
た。また比較例として、表−１に示す粒度及び比容積を
有する結晶性セルロース（アビセル PH102）及び乳糖
にＮ／Ｇを10％含浸させた試料を調製し、上記と同一条
件で放置したときのNG残存率を測定した。その結果を表
−１に示す。Example 1 Crystalline cellulose having the particle size and specific volume shown in Table-1
(Avicel PH101) with 10% N / G impregnated
Measure and measure the NG residual rate when prepared and left at 40 ° C for 5 days
It was As a comparative example, the particle size and specific volume shown in Table 1 are
Having crystalline cellulose (Avicel PH102) and lactose
Prepare a sample with 10% N / G impregnated in
The NG residual rate when left as it was was measured. Show the result
-1.
実施例−２ 目の開きが0.074mmの篩による篩粉残粉が20％、比容積
が3c.c.／ｇの結晶性セルロース（アビセル PH101）に
Ｎ／Ｇを各々5,10,20％含浸させた試料を調整し、滑降
型試験機を使用して落槌重量5kgで落槌感度試験を実施
した。また比較例として、Ｎ／Ｇ単体の落槌感度も上記
と同様の方法で測定した。 Example 2 Sieve powder with a sieve having an opening of 0.074 mm has a residual powder content of 20% and a specific volume.
3 c.c./g of crystalline cellulose (Avicel PH101)
Prepare a sample impregnated with N / G of 5, 10 and 20% respectively and slide it down.
Performs a drop hammer sensitivity test with a hammer weight of 5 kg using a type tester
did. Also, as a comparative example, the sensitivity of the N / G alone to the above is also shown.
It measured by the method similar to.
その結果を表−２に示す。The results are shown in Table-2.
表−１の結果から、本発明の結晶性セルロースはすぐれ
たＮ／Ｇ保存安定性を有していることが判る。また表−
２の結果から、本発明の医薬用Ｎ／Ｇ組成物は非常に鈍
感であり極めて安全に取扱うことができ、Ｎ／Ｇ含有製
剤用の原料として有効に使用されるものである。 From the results shown in Table 1, it can be seen that the crystalline cellulose of the present invention has excellent N / G storage stability. Also table-
From the results of No. 2, the medicinal N / G composition of the present invention is extremely insensitive, can be handled extremely safely, and is effectively used as a raw material for N / G-containing preparations.
Claims (1)
５〜35％を占め、かつ比容積が２〜4c.c.／ｇである結
晶性セルロース100部に、２〜20部（重量）のニトログ
リセリンを吸着させてなる医薬用ニトログリセリン組成
物。1. A crystalline cellulose having a sieve opening of 0.074 mm and a sieve residue of 5 to 35% and a specific volume of 2 to 4 c.c./g. A medicinal nitroglycerin composition which adsorbs a part (weight) of nitroglycerin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP12432282A JPH0665646B2 (en) | 1982-07-19 | 1982-07-19 | Medicinal nitroglycerin composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP12432282A JPH0665646B2 (en) | 1982-07-19 | 1982-07-19 | Medicinal nitroglycerin composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5916857A JPS5916857A (en) | 1984-01-28 |
| JPH0665646B2 true JPH0665646B2 (en) | 1994-08-24 |
Family
ID=14882461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP12432282A Expired - Lifetime JPH0665646B2 (en) | 1982-07-19 | 1982-07-19 | Medicinal nitroglycerin composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0665646B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018184410A (en) * | 2013-07-22 | 2018-11-22 | サンド・アクチエンゲゼルシヤフト | Formulation containing amorphous dapagliflozin |
-
1982
- 1982-07-19 JP JP12432282A patent/JPH0665646B2/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018184410A (en) * | 2013-07-22 | 2018-11-22 | サンド・アクチエンゲゼルシヤフト | Formulation containing amorphous dapagliflozin |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5916857A (en) | 1984-01-28 |
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