JPH04279531A - Nasal drop - Google Patents
Nasal dropInfo
- Publication number
- JPH04279531A JPH04279531A JP4015091A JP4015091A JPH04279531A JP H04279531 A JPH04279531 A JP H04279531A JP 4015091 A JP4015091 A JP 4015091A JP 4015091 A JP4015091 A JP 4015091A JP H04279531 A JPH04279531 A JP H04279531A
- Authority
- JP
- Japan
- Prior art keywords
- lauryl sulfate
- antiallergic
- nasal spray
- nasal
- hyperemia
- 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
- 239000007923 nasal drop Substances 0.000 title abstract description 5
- 239000000739 antihistaminic agent Substances 0.000 claims abstract description 15
- 230000003266 anti-allergic effect Effects 0.000 claims abstract description 13
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229940043264 dodecyl sulfate Drugs 0.000 claims abstract description 11
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 claims abstract description 7
- 229940046978 chlorpheniramine maleate Drugs 0.000 claims abstract description 7
- PMGQWSIVQFOFOQ-BDUVBVHRSA-N (e)-but-2-enedioic acid;(2r)-2-[2-[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidine Chemical compound OC(=O)\C=C\C(O)=O.CN1CCC[C@@H]1CCOC(C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 PMGQWSIVQFOFOQ-BDUVBVHRSA-N 0.000 claims abstract description 3
- 229960002689 clemastine fumarate Drugs 0.000 claims abstract description 3
- 239000007922 nasal spray Substances 0.000 claims description 24
- 229940097496 nasal spray Drugs 0.000 claims description 21
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims description 6
- 230000001387 anti-histamine Effects 0.000 claims description 6
- 229940125715 antihistaminic agent Drugs 0.000 abstract description 8
- 206010020565 Hyperaemia Diseases 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 6
- 239000003242 anti bacterial agent Substances 0.000 abstract description 4
- 229940100662 nasal drops Drugs 0.000 abstract description 4
- 238000002156 mixing Methods 0.000 abstract description 3
- 230000003115 biocidal effect Effects 0.000 abstract description 2
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 230000002070 germicidal effect Effects 0.000 abstract 1
- 230000002688 persistence Effects 0.000 abstract 1
- 230000003285 pharmacodynamic effect Effects 0.000 abstract 1
- 230000001105 regulatory effect Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 230000002459 sustained effect Effects 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 description 8
- 206010039085 Rhinitis allergic Diseases 0.000 description 5
- 201000010105 allergic rhinitis Diseases 0.000 description 5
- 230000000844 anti-bacterial effect Effects 0.000 description 5
- 230000000052 comparative effect Effects 0.000 description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical compound Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 0.000 description 4
- 208000036071 Rhinorrhea Diseases 0.000 description 4
- 206010039101 Rhinorrhoea Diseases 0.000 description 4
- 229960004760 naphazoline hydrochloride Drugs 0.000 description 4
- 210000001331 nose Anatomy 0.000 description 4
- 206010041232 sneezing Diseases 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 3
- 229940088710 antibiotic agent Drugs 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 230000005923 long-lasting effect Effects 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 210000003928 nasal cavity Anatomy 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 3
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 2
- 235000019799 monosodium phosphate Nutrition 0.000 description 2
- 210000002850 nasal mucosa Anatomy 0.000 description 2
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 2
- 239000005526 vasoconstrictor agent Substances 0.000 description 2
- 230000002618 waking effect Effects 0.000 description 2
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical class OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 206010014568 Empyema Diseases 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- HCBIBCJNVBAKAB-UHFFFAOYSA-N Procaine hydrochloride Chemical compound Cl.CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 HCBIBCJNVBAKAB-UHFFFAOYSA-N 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 208000024780 Urticaria Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- -1 alkali metal salt Chemical class 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 238000007664 blowing Methods 0.000 description 1
- 150000001642 boronic acid derivatives Chemical class 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 230000001886 ciliary effect Effects 0.000 description 1
- 229960002881 clemastine Drugs 0.000 description 1
- YNNUSGIPVFPVBX-NHCUHLMSSA-N clemastine Chemical compound CN1CCC[C@@H]1CCO[C@@](C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 YNNUSGIPVFPVBX-NHCUHLMSSA-N 0.000 description 1
- 229960000520 diphenhydramine Drugs 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000009931 harmful effect Effects 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 239000000938 histamine H1 antagonist Substances 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000002075 main ingredient Substances 0.000 description 1
- 230000000420 mucociliary effect Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 208000027406 nose symptom Diseases 0.000 description 1
- 238000010979 pH adjustment Methods 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 229960001309 procaine hydrochloride Drugs 0.000 description 1
- 229960003910 promethazine Drugs 0.000 description 1
- 206010039083 rhinitis Diseases 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 230000009885 systemic effect Effects 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
Landscapes
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
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 an antiallergic nasal spray. More specifically, the present invention relates to an anti-allergic nasal spray that is fast-acting, long-lasting, and has bactericidal properties.
【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。BACKGROUND OF THE INVENTION Naphazoline hydrochloride, a vasoconstrictor, has been used as an antiallergic nasal spray. However, naphazoline hydrochloride does not exhibit its medicinal efficacy until 10 minutes or more have elapsed after administration, and the duration of its medicinal efficacy is relatively short, 3 to 4 hours. Therefore, it must be administered frequently, and continuous use may cause side effects such as secondary hyperemia in 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 been known to suppress the harmful effects of histamine released during allergic reactions, and are effective in treating allergic rhinitis, hives, and the like. However, antihistamines are not fast-acting or long-lasting enough to treat the symptoms of allergic rhinitis, and they also lack antibacterial activity, so they are often used in combination with antibiotics, resulting in systemic side effects caused by long-term antibiotic use. There was a problem that we had to be careful about.
【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。[0004] Also, lauryl sulfate has a bactericidal effect,
It is particularly effective against Staphylococcus aureus and is used in soaps for eczema, but it was not known to be used as a nasal spray.
【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。[Problems to be Solved by the Invention] In view of the current situation, the present invention has a fast-acting, long-lasting, and bactericidal effect, and does not cause secondary hyperemia even with repeated use, and does not cause allergic reactions even without the concomitant use of antibiotics. The aim was to provide a nasal spray that was highly 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。SUMMARY OF THE INVENTION The present invention relates to an antiallergic nasal spray containing an antihistamine and 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。[Example] As a result of extensive studies to achieve the above object, the present inventor has found that by incorporating lauryl sulfate into an antihistamine, it exhibits an antiallergic effect immediately after administration, and maintains its efficacy for a long period of time. The inventors have discovered a nasal spray that does not cause secondary hyperemia even when used repeatedly, and have completed the present invention.
【０００８】以下、本発明の点鼻薬について説明する。[0008] The nasal spray of the present invention will be explained 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。[0009] Antihistamines used in the nasal spray of the present invention include chlorpheniramine maleate, clemastine fumarate, diphenhydramine, promethazine, etc., but especially chlorpheniramine maleate, which is a histamine H1 receptor blocker, and fumarate. Acid clemastine is preferred. As for antihistamines, the d-form is effective, and the l-form is less effective. Usually, a racemate is used, but the d-isomer may be used after splitting.
【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
。[0010] The lauryl sulfate used in the present invention may be one that is normally commercially available for pharmaceutical use, and the salt is preferably an alkali metal salt such as sodium or potassium. Further, the weight ratio of the antihistamine to the lauryl sulfate is selected within the range of 1:1 to 1:200 as desired, but is 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。[0011] The nasal spray of the present invention has a pH of 5.0 to 7.5.
, preferably adjusted to 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。Buffers for pH adjustment include phosphates,
Examples include borates and bicarbonates, and particularly preferred are phosphate buffers consisting of sodium monohydrogen phosphate and sodium dihydrogen phosphate.
【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 ingredients, the nasal spray of the present invention may optionally contain conventional preservatives such as procaine hydrochloride, which is a local anesthetic to relieve local pain, and glycerin and paraoxybenzoic acid ester, which suppress dryness of the nasal mucosa. 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 spray of the present invention can be obtained by adding sterile purified water to the above ingredients to adjust the concentration to a desired level. The concentration of the antihistamine agent is preferably 0.005 to 0.05% by weight. For adult males, 0.5 to 10 ml, preferably 1 ml, of the nasal spray prepared as described above may be administered into each nasal cavity using an ordinary sprayer or pipette.
【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 spray of the present invention will be explained 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。After dissolving sodium lauryl sulfate and glycerin in sterile purified water, then dissolving sodium monohydrogen phosphate and sodium dihydrogen phosphate, ethyl paraoxybenzoate was added and dissolved, and chlorpheniramine maleate and hydrochloric acid were dissolved. After adding an aqueous solution containing procaine and mixing uniformly, 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 spray of Example 1, and adjusting the total amount to 100% by weight with sterile purified water. This is a 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 formulation obtained in Example 1 and Comparative Examples 1 and 2
After thoroughly blowing the nose into each nasal cavity of three adult males (hereinafter referred to as A, O, and C) with allergic rhinitis and empyema who exhibit severe symptoms of allergic rhinitis, the drug was instilled and administered. minutes later and upon waking the next morning (approximately 8 minutes after administration)
Symptoms of sneezing, runny nose, and stuffy nose (over time) were investigated. The severity of sneezing, runny nose, and stuffy nose symptoms was determined 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。0021 A. Severe symptoms appear. B. Mild symptoms occur. C. Almost no symptoms The results are 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 is the same as Comparative Example 1 in which chlorpheniramine maleate was removed from Example 1, or Comparative Example 1 in which sodium lauryl sulfate was removed from Example 1. Compared to the preparation obtained in step 2, the judgment value was 1 at both 5 minutes after administration and when waking up the next morning.
．． It was 5 to 3 times better, indicating a remarkable effect that cannot be obtained with antihistamines alone. In addition, nasal sprays containing naphazoline hydrochloride, a vasoconstrictor, as an active ingredient do not become effective until more than 10 minutes have passed after administration, and the duration is short, 2 to 3 hours. Nasal drops quickly become effective within 5 minutes after administration, and their effectiveness lasts for about 8 hours or more, and even when you wake up the next morning, you will not experience sneezing, runny nose, or
Suppressed symptoms of stuffy nose.
【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 spray of the present invention quickly suppresses various symptoms such as sneezing, runny nose, and stuffy nose caused by allergic rhinitis, maintains its efficacy for a long time, and even with frequent and continuous administration. It has the advantage of not causing secondary hyperemia, which is a side effect of nasal sprays containing naphazoline hydrochloride as the main ingredient. Furthermore, the nasal spray of the present invention is adjusted to the optimal pH within the nasal cavity, so it is optimal for the movement of the ciliary epithelium of the mucous membrane, and is isotonic with serum, so it is less irritating. Furthermore, due to the bactericidal power of lauryl sulfate, there is no need to use antibiotics, which are commonly used in conventional anti-allergic nasal sprays, making it extremely safe even when used repeatedly.
Claims (4)
なる抗アレルギー性点鼻薬。[Claim 1] An anti-allergic nasal spray comprising an antihistamine and lauryl sulfate.
ェ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。[Claim 2] Claim 1 wherein the antihistamine is chlorpheniramine maleate or clemastine fumarate.
Antiallergic nasal spray as described.
重量比が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. Claim 1 or 2, wherein the weight ratio of the antihistamine and lauryl sulfate is 1:1 to 1:200.
Antiallergic nasal spray as described.
てなる請求項１、２または３記載の抗アレルギー性点鼻
薬。4. The antiallergic nasal spray according to claim 1, wherein the pH is 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 true JPH04279531A (en) | 1992-10-05 |
| JPH0662442B2 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) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999034776A1 (en) * | 1998-01-09 | 1999-07-15 | Taisho Pharmaceutical Co., Ltd. | Nasal drop compositions |
| WO2000016764A3 (en) * | 1998-09-23 | 2000-11-23 | Phycogen Inc | Pharmaceutical compositions comprising derivatives of sulphur acids |
-
1991
- 1991-03-06 JP JP4015091A patent/JPH0662442B2/en not_active Expired - Lifetime
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999034776A1 (en) * | 1998-01-09 | 1999-07-15 | Taisho Pharmaceutical Co., Ltd. | Nasal drop compositions |
| WO2000016764A3 (en) * | 1998-09-23 | 2000-11-23 | Phycogen Inc | Pharmaceutical compositions comprising derivatives of sulphur acids |
| JP2002526444A (en) * | 1998-09-23 | 2002-08-20 | サイコゲン インク． | Methods and compositions for treating receptor-mediated diseases |
| US7087661B1 (en) | 1998-09-23 | 2006-08-08 | Cernofina, Llc | Safe and effective biofilm inhibitory compounds and health-related uses thereof |
| US7108861B1 (en) | 1998-09-23 | 2006-09-19 | Cernofina, Llc | Environmentally benign crop protection agents |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0662442B2 (en) | 1994-08-17 |
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