JPH0662442B2 - Nasal drops - Google Patents
Nasal dropsInfo
- Publication number
- JPH0662442B2 JPH0662442B2 JP4015091A JP4015091A JPH0662442B2 JP H0662442 B2 JPH0662442 B2 JP H0662442B2 JP 4015091 A JP4015091 A JP 4015091A JP 4015091 A JP4015091 A JP 4015091A JP H0662442 B2 JPH0662442 B2 JP H0662442B2
- Authority
- JP
- Japan
- Prior art keywords
- nasal
- nasal drops
- present
- antiallergic
- antihistamine
- 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
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- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【０００１】[0001]
【産業上の利用分野】本発明は抗アレルギー性点鼻薬に
関する。さらに詳しくは、速効性、持続性および殺菌力
を有する抗アレルギー性点鼻薬に関する。FIELD OF THE INVENTION The present invention relates to antiallergic nasal drops. More specifically, it relates to an antiallergic nasal drop having fast-acting, long-lasting and bactericidal activity.
【０００２】[0002]
【従来の技術】従来から抗アレルギー性点鼻薬として
は、血管収縮剤である塩酸ナファゾリンが用いられてい
る。しかし塩酸ナファゾリンは投与後10分以上経過しな
ければ薬効が発現せず、また薬効の持続時間も３〜４時
間と比較的短時間である。そのため頻回投与しなければ
ならず、連用すると鼻粘膜に第二期充血を起こすなどの
副作用を生じることがある。2. Description of the Related Art Nafazoline hydrochloride, which is a vasoconstrictor, has been used as an antiallergic nasal drop. However, naphazoline hydrochloride has no medicinal effect until 10 minutes or more after administration, and the medicinal effect lasts a relatively short time of 3 to 4 hours. Therefore, it must be administered frequently, and continuous use may cause side effects such as secondary hyperemia on the nasal mucosa.
【０００３】一方、抗ヒスタミン剤は従来からアレルギ
ー反応に際して遊離されるヒスタミンの有害な作用を抑
制し、アレルギー性鼻炎、じん麻疹などに有効であるこ
とが知られている。しかしながら抗ヒスタミン剤はアレ
ルギー性鼻炎の諸症状に対して速効性および持続性が不
充分であり、更に抗菌力がないため抗生物質と併用され
ることが多く、抗生物質の長期連用からくる全身的な副
作用を注意しなければならないという問題があった。On the other hand, antihistamines have conventionally been known to suppress the harmful effects of histamine released during allergic reactions and are effective for allergic rhinitis, urticaria and the like. However, antihistamines have insufficient fast-acting and long-lasting effects on various symptoms of allergic rhinitis, and because they do not have antibacterial activity, they are often used in combination with antibiotics, resulting in systemic side effects resulting from long-term continuous use of antibiotics. There was a problem that I had to be careful.
【０００４】またラウリル硫酸塩は、殺菌作用があり、
とくに黄色ブドウ球菌に有効であり、湿疹用石ケンなど
に用いられているが、点鼻薬として用いられることは知
られていなかった。Lauryl sulfate has a bactericidal action,
It is particularly effective against Staphylococcus aureus and is used for soap for eczema, etc., but it was not known to be used as a nasal drop.
【０００５】[0005]
【発明が解決しようとする課題】本発明はかかる現状に
鑑み、速効性、持続性および殺菌力を有し、連用によっ
ても第二期充血を起こさずまた抗生物質を併用しなくて
もアレルギー性鼻炎に著効のある点鼻薬を提供すること
を目的としてなされたものである。In view of the present situation, the present invention has fast-acting, long-lasting and bactericidal properties, and does not cause secondary hyperemia even after continuous use, and is allergic even if antibiotics are not used in combination. It was made for the purpose of providing nasal drops that are extremely effective against rhinitis.
【０００６】[0006]
【課題を解決するための手段】本発明は、抗ヒスタミン
剤とラウリル硫酸塩を含有してなる抗アレルギー性点鼻
薬に関する。The present invention relates to an antiallergic nasal drop containing an antihistamine and a lauryl sulfate.
【０００７】[0007]
【実施例】本発明者は、上記目的を達成すべく鋭意検討
を重ねた結果、抗ヒスタミン剤にラウリル硫酸塩を配合
することにより、投与後すみやかに抗アレルギー作用を
示し、その後長時間にわたって薬効を持続し、かつ連用
しても第二期充血を起こさない点鼻薬を見出し、本発明
を完成するに至った。[Examples] The present inventor has conducted extensive studies to achieve the above-mentioned object, and as a result, by blending an antihistamine with lauryl sulfate, an antiallergic action was promptly obtained after administration, and thereafter the drug effect was sustained for a long time. In addition, a nasal drop that does not cause secondary hyperemia even after continuous use was found, and the present invention was completed.
【０００８】以下、本発明の点鼻薬について説明する。The nose drops of the present invention will be described below.
【０００９】本発明の点鼻薬において用いられる抗ヒス
タミン剤としては、マレイン酸クロルフェニラミン、フ
マル酸クレマスチン、ジフェンヒドラミン、プロメタジ
ンなどがあげられるが、とりわけヒスタミンＨ1 受容体
遮断剤であるマレイン酸クロルフェニラミン、フマル酸
クレマスチンが好ましい。抗ヒスタミン剤は、ｄ体が有
効であり、ｌ体は薬効が小さい。通常はラセミ体が用い
られるが、分割してｄ体を用いてよい。Examples of the antihistamines used in the nasal drops of the present invention include chlorpheniramine maleate, clemastine fumarate, diphenhydramine, promethazine and the like. Among them, chlorpheniramine maleate which is a histamine H 1 receptor blocker, Cremastine fumarate is preferred. As for the antihistamine, the d-form is effective, and the l-form is less effective. Usually, the racemic form is used, but the d form may be used by dividing.
【００１０】本発明に用いられるラウリル硫酸塩は、通
常医薬品用として市販されているものであればよく、塩
としてはナトリウム、カリウムなどのアルカリ金属塩が
好ましい。また抗ヒスタミン剤とラウリル硫酸塩との重
量比は所望に応じて１：１〜１：200 の範囲で選ばれる
が、とくに１：１〜１：10からなるのが好ましい。The lauryl sulphate used in the present invention may be any one which is usually marketed for pharmaceuticals, and the salts are preferably alkali metal salts such as sodium and potassium. The weight ratio of the antihistamine to the lauryl sulfate is selected in the range of 1: 1 to 1: 200 as desired, but it is particularly preferably 1: 1 to 1:10.
【００１１】本発明の点鼻薬はpH5.0 〜7.5 、好ましく
はpH5.5 〜6.5 に調整される。このpH領域は粘膜繊毛上
皮運動に至適である。The nasal drops of the present invention are adjusted to pH 5.0 to 7.5, preferably pH 5.5 to 6.5. This pH range is optimal for mucociliary epithelial movement.
【００１２】pH調整用の緩衝剤としては、リン酸塩、ホ
ウ酸塩、重炭酸塩などがあげられるが、とくに好ましい
ものとしては、リン酸一水素ナトリウムとリン酸二水素
ナトリウムからなるリン酸緩衝剤があげられる。Examples of the pH adjusting buffer include phosphates, borates, and bicarbonates. Particularly preferred is a phosphoric acid consisting of sodium monohydrogen phosphate and sodium dihydrogen phosphate. A buffering agent is included.
【００１３】本発明の点鼻薬には、前記成分以外に所望
により局所の痛みをとる局所麻酔剤である塩酸プロカイ
ンや鼻腔粘膜の乾燥をおさえるグリセリンおよびパラオ
キシ安息香酸エステルなどの通常の保存剤が配合され
る。In addition to the above-mentioned components, the nasal drops of the present invention contain a conventional preservative such as procaine hydrochloride, which is a local anesthetic that causes local pain if desired, and glycerin and paraoxybenzoic acid ester, which prevent dryness of the nasal mucosa. To be done.
【００１４】本発明の点鼻薬は、前記成分に滅菌精製水
を加えて所望の濃度に調整してえられる。また抗ヒスタ
ミン剤の濃度は0.005 〜0.05重量％が好ましい。以上に
より調製された点鼻薬を適宜、通常の噴霧器またはピペ
ットを用いて各鼻腔内に成人男子においては0.5 〜10ml
好ましくは１ml投与すればよい。The nasal drops of the present invention can be obtained by adding sterile purified water to the above components to adjust the concentration to a desired level. The concentration of the antihistamine is preferably 0.005 to 0.05% by weight. The nasal drops prepared by the above procedure can be applied to each nasal cavity using an ordinary nebulizer or pipette in an amount of 0.5 to 10 ml for adult males.
Preferably, 1 ml may be administered.
【００１５】つぎに実施例をあげて本発明の点鼻薬を説
明するが、実施例は典型例であり本発明はかかる実施例
のみに限定されるものではない。Next, the nasal drops of the present invention will be described with reference to examples, but the examples are typical examples and the present invention is not limited to these examples.
【００１６】実施例１ 表１に示す処方にしたがって点鼻薬を調製した。Example 1 Nasal drops were prepared according to the formulation shown in Table 1.
【００１７】滅菌精製水にラウリル硫酸ナトリウムとグ
リセリンを溶解し、ついでリン酸一水素ナトリウムおよ
びリン酸二水素ナトリウムを溶解したのち、パラオキシ
安息香酸エチルを加えて溶解せしめ、マレイン酸クロル
フェニラミンおよび塩酸プロカインを含有する水溶液を
加えて、均一に混合したのち、滅菌精製水を加えて全量
を100 重量％に調整した。Sodium lauryl sulfate and glycerin were dissolved in sterilized purified water, and then sodium monohydrogen phosphate and sodium dihydrogen phosphate were dissolved. Ethyl paraoxybenzoate was then added and dissolved, and chlorpheniramine maleate and hydrochloric acid were dissolved. An aqueous solution containing procaine was added and uniformly mixed, and then sterile purified water was added to adjust the total amount to 100% by weight.
【００１８】比較例１〜２ 比較例１または２の製剤は、実施例１の点鼻薬から各々
マレイン酸クロルフェニラミンまたはラウリル硫酸ナト
リウムのみを除き、滅菌精製水で全量を100重量％に調
整した製剤であり、比較のため調製したものである。Comparative Examples 1 and 2 The preparations of Comparative Examples 1 and 2 were prepared by removing only chlorpheniramine maleate or sodium lauryl sulfate from the nasal drops of Example 1 and adjusting the total amount to 100% by weight with sterile purified water. Formulation, prepared for comparison.
【００１９】[0019]
【表１】 [Table 1]
【００２０】実施例２ 実施例１および比較例１、２でえられた各製剤の１mlを
アレルギー性鼻炎症およびアレルギー性鼻炎の症状が激
しく現われる蓄膿症の成人男子３名（以下甲、乙、丙で
表わす）の各鼻腔内に鼻をよくかんだのちに、滴下して
投与し、投与５分後および翌朝起床時（投与から約８時
間経過時）のくしゃみ、鼻水および鼻ずまりの各症状を
調べた。くしゃみ、鼻水、鼻づまり症状の程度はつぎの
基準にしたがって判定した。Example 2 1 ml of each of the preparations obtained in Example 1 and Comparative Examples 1 and 2 was used as 3 adult males with pyometra (hereinafter, Ko, O, and Hei), who showed severe allergic rhinitis and allergic rhinitis. The sneeze, runny nose, and stuffy nose are shown 5 minutes after administration and 5 minutes after administration and when waking up next morning (about 8 hours after administration). Examined. The degree of sneezing, runny nose, and stuffy nose symptoms were evaluated according to the following criteria.
【００２１】Ａ 強い症状がでる Ｂ 軽い症状がでる Ｃ ほとんど症状がでない 結果を表２に示す。A: Strong symptom appears B: Mild symptom appears C: Almost no symptom is shown in Table 2.
【００２２】[0022]
【表２】 [Table 2]
【００２３】表２の成績から明らかなように実施例１で
えられた製剤は、実施例１からマレイン酸クロルフェニ
ラミンを除いた比較例１または実施例１からラウリル硫
酸ナトリウムを除いた比較例２でえられた製剤に比べて
投与５分後、翌朝起床時のいづれの時点でも判定値が1.
5 〜３倍と著しく良好であり、抗ヒスタミン剤のみでは
えられない著効を示した。また血管収縮剤である塩酸ナ
ファゾリンを有効成分とする点鼻薬においては、投与後
10数分経過しなければ効力が現われずまた持続時間も２
〜３時間と短かいのに対し、本発明の点鼻薬は投与後５
分で速やかに著効を示し、その後効力が約８時間以上持
続し、翌朝起床時においても、くしゃみ、鼻水、鼻ずま
りの諸症状を抑制した。As is clear from the results in Table 2, the preparation obtained in Example 1 was the same as Comparative Example 1 in which chlorpheniramine maleate was removed or Comparative Example in which sodium lauryl sulfate was removed from Example 1. 5 minutes after administration compared to the preparation obtained in 2, the judgment value was 1. at any time when waking up the next morning.
It was remarkably good at 5 to 3 times, and showed a remarkable effect which could not be obtained only by the antihistamine. In addition, nasal drops containing naphazoline hydrochloride, a vasoconstrictor, as an active ingredient
It will not take effect until 10 minutes have passed, and the duration is 2
It is as short as ~ 3 hours, whereas the nasal drops of the present invention are 5 after administration.
The drug rapidly showed a marked effect in minutes, and then the effect persisted for about 8 hours or longer, and the various symptoms of sneezing, runny nose and stuffy nose were suppressed even when waking up the next morning.
【００２４】[0024]
【発明の効果】本発明の点鼻薬はアレルギー性鼻炎に起
因する、くしゃみ、鼻水、鼻ずまりの諸症状を速やかに
抑制し、かつ長時間その薬効を持続し、頻回、連続投与
においても塩酸ナファゾリンを主成分とする点鼻薬の副
作用である第二期充血が生じないという利点がある。ま
た本発明の点鼻薬は、鼻腔内の至適pHに調整されている
ため、粘膜の繊毛上皮運動にも至適であり、かつ血清と
等張であるため、刺激が少ない。更に、ラウリル硫酸塩
の殺菌力により、従来の抗アレルギー性点鼻薬で通常併
用される抗生物質を用いる必要がないため連用しても安
全性が非常に大である。EFFECTS OF THE INVENTION The nasal drop of the present invention rapidly suppresses various symptoms of sneezing, runny nose and stuffy nose caused by allergic rhinitis, maintains its medicinal effect for a long time, and even in frequent and continuous administration. There is an advantage that the secondary hyperemia, which is a side effect of nasal drops containing naphazoline hydrochloride as a main component, does not occur. Further, since the nasal drop of the present invention is adjusted to the optimum pH in the nasal cavity, it is also suitable for ciliary epithelial movement of the mucous membrane, and isotonic with serum, so that it causes less irritation. Furthermore, because of the bactericidal activity of lauryl sulfate, it is not necessary to use antibiotics that are usually used in combination with conventional antiallergic nasal drops, and therefore, the safety is extremely great even when used continuously.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.5 識別記号 庁内整理番号 ＦＩ 技術表示箇所 Ａ６１Ｋ 47/20 Ｃ 7433−4Ｃ Ｅ 7433−4Ｃ //(Ａ６１Ｋ 31/40 31:255） (Ａ６１Ｋ 31/44 31:255） (Ａ６１Ｋ 31/54 31:255） 9283−4Ｃ ─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. 5 Identification number Office reference number FI technical display location A61K 47/20 C 7433-4C E 7433-4C // (A61K 31/40 31: 255) (A61K 31/44 31: 255) (A61K 31/54 31: 255) 9283-4C
Claims (4)
る抗アレルギー性点鼻薬。1. An antiallergic nasal drop comprising an antihistamine and lauryl sulfate.
ニラミンまたはフマル酸クレマスチンである請求項１記
載の抗アレルギー性点鼻薬。2. The antiallergic nasal drop according to claim 1, wherein the antihistamine is chlorpheniramine maleate or clemastine fumarate.
量比が１：１〜１：200 である請求項１または２記載の
抗アレルギー性点鼻薬。3. The antiallergic nasal drop according to claim 1 or 2, wherein the weight ratio of the antihistamine to lauryl sulfate is 1: 1 to 1: 200.
１、２または３記載の抗アレルギー性点鼻薬。4. The antiallergic nasal drop according to claim 1, 2 or 3 having a pH adjusted to 5.0 to 7.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4015091A JPH0662442B2 (en) | 1991-03-06 | 1991-03-06 | Nasal drops |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP4015091A JPH0662442B2 (en) | 1991-03-06 | 1991-03-06 | Nasal drops |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH04279531A JPH04279531A (en) | 1992-10-05 |
| JPH0662442B2 true JPH0662442B2 (en) | 1994-08-17 |
Family
ID=12572740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP4015091A Expired - Lifetime JPH0662442B2 (en) | 1991-03-06 | 1991-03-06 | Nasal drops |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0662442B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1784899A (en) * | 1998-01-09 | 1999-07-26 | Taisho Pharmaceutical Co., Ltd. | Nasal drop compositions |
| IL142132A0 (en) | 1998-09-23 | 2002-03-10 | Phycogen Inc | Methods and compositions for treating receptor mediated diseases |
-
1991
- 1991-03-06 JP JP4015091A patent/JPH0662442B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JPH04279531A (en) | 1992-10-05 |
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