JPH02138132A - Transcutaneous absorption drug - Google Patents
Transcutaneous absorption drugInfo
- Publication number
- JPH02138132A JPH02138132A JP29303588A JP29303588A JPH02138132A JP H02138132 A JPH02138132 A JP H02138132A JP 29303588 A JP29303588 A JP 29303588A JP 29303588 A JP29303588 A JP 29303588A JP H02138132 A JPH02138132 A JP H02138132A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- acid
- drug
- transcutaneous
- absorption
- 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.)
- Pending
Links
- 238000010521 absorption reaction Methods 0.000 title claims abstract description 19
- 239000003814 drug Substances 0.000 title abstract description 13
- 229940079593 drug Drugs 0.000 title abstract description 12
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 3
- 238000002360 preparation method Methods 0.000 claims description 15
- 239000004615 ingredient Substances 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 abstract description 4
- 239000008777 Glycerylphosphorylcholine Substances 0.000 abstract description 2
- 229960004956 glycerylphosphorylcholine Drugs 0.000 abstract description 2
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 16
- -1 amide compounds Chemical class 0.000 description 15
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- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 8
- 229960001047 methyl salicylate Drugs 0.000 description 8
- 239000008280 blood Substances 0.000 description 7
- 210000004369 blood Anatomy 0.000 description 7
- 230000000694 effects Effects 0.000 description 6
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- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 description 2
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- LRBQNJMCXXYXIU-NRMVVENXSA-N tannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-NRMVVENXSA-N 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- 229960002494 tetracaine hydrochloride Drugs 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 1
- HWCKGOZZJDHMNC-UHFFFAOYSA-M tetraethylammonium bromide Chemical compound [Br-].CC[N+](CC)(CC)CC HWCKGOZZJDHMNC-UHFFFAOYSA-M 0.000 description 1
- 229960004559 theobromine Drugs 0.000 description 1
- 235000019157 thiamine Nutrition 0.000 description 1
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- 239000011721 thiamine Substances 0.000 description 1
- SRVJKTDHMYAMHA-WUXMJOGZSA-N thioacetazone Chemical compound CC(=O)NC1=CC=C(\C=N\NC(N)=S)C=C1 SRVJKTDHMYAMHA-WUXMJOGZSA-N 0.000 description 1
- 229960003231 thioacetazone Drugs 0.000 description 1
- QGVNJRROSLYGKF-UHFFFAOYSA-N thiobarbital Chemical compound CCC1(CC)C(=O)NC(=S)NC1=O QGVNJRROSLYGKF-UHFFFAOYSA-N 0.000 description 1
- 229950009883 tocopheryl nicotinate Drugs 0.000 description 1
- 108010021724 tonin Proteins 0.000 description 1
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 description 1
- 229960000401 tranexamic acid Drugs 0.000 description 1
- YFDSDPIBEUFTMI-UHFFFAOYSA-N tribromoethanol Chemical compound OCC(Br)(Br)Br YFDSDPIBEUFTMI-UHFFFAOYSA-N 0.000 description 1
- 229950004616 tribromoethanol Drugs 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- 229960004319 trichloroacetic acid Drugs 0.000 description 1
- JFJZZMVDLULRGK-URLMMPGGSA-O tubocurarine Chemical compound C([C@H]1[N+](C)(C)CCC=2C=C(C(=C(OC3=CC=C(C=C3)C[C@H]3C=4C=C(C(=CC=4CCN3C)OC)O3)C=21)O)OC)C1=CC=C(O)C3=C1 JFJZZMVDLULRGK-URLMMPGGSA-O 0.000 description 1
- 229960001844 tubocurarine Drugs 0.000 description 1
- 235000013976 turmeric Nutrition 0.000 description 1
- 229960003732 tyramine Drugs 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 description 1
- 235000005282 vitamin D3 Nutrition 0.000 description 1
- 239000011647 vitamin D3 Substances 0.000 description 1
- 235000012711 vitamin K3 Nutrition 0.000 description 1
- 239000011652 vitamin K3 Substances 0.000 description 1
- 229940021056 vitamin d3 Drugs 0.000 description 1
- 229940041603 vitamin k 3 Drugs 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 description 1
- 229960000317 yohimbine Drugs 0.000 description 1
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
Abstract
Description
【発明の詳細な説明】 〔産業上の利用分野〕 本発明は、経皮吸収製剤に関する。[Detailed description of the invention] [Industrial application field] The present invention relates to transdermal absorption preparations.
薬物の投与方法としては、従来から経口投与。 Traditionally, drugs have been administered orally.
陵内投与、静脈内注射等が通常行われており、中でも、
経口投与がその手軽さから広く用いられている。Intracranial administration, intravenous injection, etc. are usually performed, among which,
Oral administration is widely used because of its ease of use.
しかしながら、経口投与の場合には胃揚障古食欲不振等
の副作用を惹起することがあり、また、吸収後肝臓の初
回通過効果により標的臓器に到達する前に失活してしま
うことがあった。However, when administered orally, it may cause side effects such as gastric bloat and anorexia, and it may be inactivated before reaching the target organ due to the first pass effect of the liver after absorption. .
近年、かかる欠点を解消し、副作用を軽減し、より安全
に薬理効果を発現させる目的で、経皮投与による外用剤
の開発が行ｌわれ、−布製品化されている。経皮投与で
は、薬効の発現が適用した局所に働く場合と全身に吸収
されて働（場合とに分類される。いずれの場合でも、あ
る程度皮膚を浸透する必要がある。しかしながら、皮膚
特に最外層を形成する角質層は、体内への物質透過に対
する防御壁であるため、薬効成分が皮Ｉｆを透過しｔｌ
ｔい事が問題点として挙げられる。そこで皮膚を透過し
やすくするため、経皮吸収促進剤の利用やプロドラック
化等の技術が注目されている。In recent years, in order to eliminate such drawbacks, reduce side effects, and more safely express pharmacological effects, external preparations for transdermal administration have been developed and are being made into fabric products. Transdermal administration is classified into two types: the effect of the drug is exerted locally, or it is absorbed throughout the body. In either case, it is necessary to penetrate the skin to some extent. The stratum corneum, which forms the skin, is a protective wall against the penetration of substances into the body, so medicinal ingredients can penetrate the skin If.
The problem is that it is ugly. Therefore, in order to make it easier to penetrate the skin, technologies such as the use of transdermal absorption enhancers and the production of prodrugs are attracting attention.
上記目的に用いられる、経皮吸収促進剤とじては、ジメ
チルスルフォキサイド、ジメチルホルムアミド、ジメチ
ルアセトアミド等のアミド化合物；ｌ−ドデシルアザナ
イクロへブタン−２−オン等のアザシクロアルカン−２
−オン誘導体；イソプロピルミリステート、イソプロパ
ツールミリステート２ ジエチルセバケート等のエステ
ル；クロトニル−Ｎ−エチル−〇−トルイジン等が挙げ
られる。Transdermal absorption enhancers used for the above purpose include amide compounds such as dimethyl sulfoxide, dimethylformamide, and dimethylacetamide; azacycloalkane-2 such as l-dodecyl azanaiclohebutan-2-one
-one derivatives; esters such as isopropyl myristate, isopropatol myristate 2, diethyl sebacate; and crotonyl-N-ethyl-〇-toluidine.
しかしながら、従来の経皮吸収促進剤は、皮膚刺激性を
示したり、効果が十分とは言えず、更に、水溶性の物質
が少なく実用上問題があった。However, conventional transdermal absorption enhancers exhibit skin irritation, are not sufficiently effective, and have practical problems due to the lack of water-soluble substances.
また、プロドラック化は、技術的に困難なものや薬効が
損なわれるものが多く、−船釣応用が難しい。In addition, the production of prodrugs is often technically difficult or the drug's efficacy is impaired, making it difficult to apply to boat fishing.
本発明は、優れた経皮吸収性を示すヶ経皮吸収製剤を提
供することを目的としている。An object of the present invention is to provide a transdermal absorption preparation that exhibits excellent transdermal absorption properties.
（式中１７は炭素数９〜２１のアルキル基を示す）で表
わされる化合物（以下ＬＰＤと略記する）及び薬効成分
を含有する経皮吸収製剤である。(In the formula, 17 represents an alkyl group having 9 to 21 carbon atoms) This is a percutaneous absorption preparation containing a compound (hereinafter abbreviated as LPD) and a medicinal ingredient.
本発明に用い・られる一般式（１１１２＋で表わされる
ＬＰＤは公知の物質であり、その配合量は大略０．０５
〜１０重量％であるが、併含される薬効成分により適切
な配合量を選択すればよい。LPD represented by the general formula (1112+) used in the present invention is a known substance, and its blending amount is approximately 0.05
~10% by weight, but an appropriate amount may be selected depending on the medicinal ingredients contained.
本発明に用いられる薬効成分とは、医薬品や医薬部外品
に於いて主剤として扱われるものずべてを指し、経皮も
しくは経粘膜吸収により投与が可能な薬物であれば特に
制限されない。例えば、トリブロモエタノール、バルビ
タール等バルビッール酸誘導体、チオバルビッール酸誘
導体、プロムワレリル尿素、スルホナール、カノコソウ
末、カノコソウチンキ、センキュウ、トウキ、サフラン
。The medicinal ingredients used in the present invention refer to all substances that are used as main ingredients in pharmaceuticals and quasi-drugs, and are not particularly limited as long as they can be administered through transdermal or transmucosal absorption. For example, tribromoethanol, barbital acid derivatives such as barbital, thiobarbital acid derivatives, promvaleryl urea, sulfonal, valerian powder, valerian tincture, nebula, valerian root, saffron.
クロルプロマジン、レセルピン メブロバメート。Chlorpromazine, reserpine, mebrobamate.
フェノチアジン誘導体、ラウオルフィアーアルカロイト
、ジフェニルメタン誘導体、オキサゾリジン誘導体、フ
ェニルアセチル尿素、アセトアミド）パ、フエナセチン
、シンナピリン、アンチピリンアミノピリン、スルビリ
ン、サリチル酸、サリチル酸ナトリウム７ サリチル酸
カルシウム、アセチルサリチル酸、サリチル酸メチル、
サリチルアミド、キニーネ、アズレン、メフエネミン
カフェイン、安息香酸ナトリウムカフェイン、アンフェ
タミン、メタンフェタミン１ ビクロトキシン、カルフ
ル、ニケタミド１ ベンテトラゾール、ジモルホラミン
、ロヘリン、イミプラミン ジメチルアミノエタノール
等の中枢神経作用薬、塩酸コカイン、塩酸プロ力イン、
塩酸テトラカイン、塩酸リドカイン、ｅ−アミノ安息香
酸エチル、ヘンシル゛アルコール、ウレタン、ｐ−アミ
ノ安息香酸ブチル、オキシインドール、ツボクラリン、
クラーレネオスチグミン等の体性神経及び骨格筋作用薬
、アセチルコリン、アドレナリン、エフェドリン。Phenothiazine derivatives, Rauwolfia alkaloids, diphenylmethane derivatives, oxazolidine derivatives, phenylacetylurea, acetamide), phenacetin, cinnapirin, antipyrine aminopyrine, sulvirine, salicylic acid, sodium salicylate 7, calcium salicylate, acetylsalicylic acid, methyl salicylate,
salicylamide, quinine, azulene, mefenemine
Caffeine, Sodium Benzoate Caffeine, Amphetamine, Methamphetamine 1 Bicrotoxin, Carfur, Niketamide 1 Bentetrazole, Dimorpholamine, Loherin, Imipramine Central nervous system agents such as dimethylaminoethanol, Cocaine hydrochloride, Propylene hydrochloride,
Tetracaine hydrochloride, lidocaine hydrochloride, ethyl e-aminobenzoate, hensyl alcohol, urethane, butyl p-aminobenzoate, oxindole, tubocurarine,
Somatic nerve and skeletal muscle agonists such as clareneostigmine, acetylcholine, epinephrine, and ephedrine.
メチルエフェドリン、チラミン、フェニレフリンイソプ
レテレノール、ナファゾリン、ハ、７カクアルカロイド
２ ヨヒンビン１ ピロカルピン、エゼリン、ネオスナ
グミン、ブラリドキン１１．アトロビン、ホマトロピン
、スコポラミン、臭化メチルスコポラミン、ニコチン、
ヘキサメトニウム、デカメトニウム、臭化テトラエチル
アンモニウム バパヘリン、ラオフィリレ、安、１に酸
ヘンシル、テオブロミン等の自律神経作用薬、ジフェン
ヒドラミン、シメンヒドリナート、プロメタシン トン
ジルアミン、マレイン酸クロルフェニラミン等の抗アレ
ルギー集、ジギタリス、Ｇ−ストロファンチン、ジゴキ
シン、キトキシン。硫酸キニジン塩酸プロ力インアミド
、ジクマロール、亜硝酸すトリウム、亜硝酸アミル、ケ
リン、ベントリニうム、ヘラトルムアルカロイド、レセ
ルピン、フタラジン誘導体、カリクレイン、ニアラミド
、ピロカルピン等の循環器系作用薬、ノスカビン、トコ
ン、リコリン、セネガ、オンジ、キキョウ、チクセツニ
ンジン、トーニン、ユーカリ油、シャゼンシ等の呼吸器
官作用薬、ジアスラーゼ５バンクレアチン、含糖ペプシ
ン、塩酸リモナーゼ、ウルツデスオキシコール酸、ウコ
ン等の消化器官作用薬、尿素、クレアチン、デキストラ
ン、マーサリル。Methylephedrine, tyramine, phenylephrine isopreterenol, naphazoline, ha, 7ka alkaloids 2 yohimbine 1 pilocarpine, eserine, neosnagmin, bralidoquine 11. Atrophin, homatropine, scopolamine, methylscopolamine bromide, nicotine,
Autonomic nerve agents such as hexamethonium, decamethonium, tetraethylammonium bromide, bapaherin, laofirile, anthyl, hensyl, theobromine, anti-allergic drugs such as diphenhydramine, cymenhydrinate, promethacin, tonzylamine, chlorpheniramine maleate, digitalis , G-strophanthin, digoxin, chitoxin. Quinidine sulfate hydrochloride protonamide, dicoumarol, sthorium nitrite, amyl nitrite, chelin, ventolinium, heratolum alkaloids, reserpine, phthalazine derivatives, kallikrein, nyaramide, pilocarpine and other cardiovascular agents, noscabine, ipecac, Respiratory organ-active drugs such as lycorine, senega, onji, bellflower, ginseng, tonin, eucalyptus oil, and chazenshi; digestive organ-active drugs such as diasurase 5 bank creatine, saccharide pepsin, hydrochloric limonase, urtudesoxycholic acid, and turmeric. , urea, creatine, dextran, Marsalil.
クロ１コチアジド、ヒドロクロロチアジド、スピロノラ
クトン、キササゲ等の泌尿器官作用薬、タンニン酸、縮
合型タンニン、五倍子、グリチルリチン酸ジカリウム２
グリチルリチン酸モノアンモニウム ジイソプロピルア
ミンジクロロアセテート。Urinary system active agents such as chlorothiazide, hydrochlorothiazide, spironolactone, and catalpa, tannic acid, condensed tannins, pentadium, dipotassium glycyrrhizinate 2
Monoammonium glycyrrhizinate diisopropylamine dichloroacetate.
グリチルレチン酸、Ｔ−アミノ酪酸、ランシック酸、ト
コフェロール、アセチルトコフェロールニコチン酸トコ
フェロール、アラントイン、εアミノカプロン酸、トリ
クロロ酢酸、乳酸、サリチル酸メチル、トウガラシチン
キ、イクタモール。Glycyrrhetinic acid, T-aminobutyric acid, ransic acid, tocopherol, acetyl tocopherol tocopherol nicotinate, allantoin, epsilon aminocaproic acid, trichloroacetic acid, lactic acid, methyl salicylate, capsicum tincture, ictamol.
ジアノコバラミン等の外皮粘膜作用薬、ヘパリン。Integumentary mucosal agents such as dianocobalamin, heparin.
ジクマロール、トラネキサム酸、ヘパリンナトリウム、
フィトナジオン、インドメタシン、メナジオン、１−ロ
ンボプラスナン、アスコルビン酸誘導体、フラボノイド
誘導体等の血液造血系作用薬、トリプトファン スレオ
ニン、バリン、イソロイノン、じ１イシン メチオニン
、フェニルアラニンヒスチジン、グルタミン酸、シトス
テロール、レチノール、コレカルシフェロール、エルゴ
カルンフェロール、ピリドキンン、チアミン２ Ｐ−ア
ミノ安息香酸、リボフラビン、ニコチン酸アミドパント
テン酸、ビオチン等の物質代謝作用薬、チロキシン誘導
体、メチルチオウラシル、パラソルモン、インシュリン
、グルカゴン、糖質コルチコイド、を質コルチコイじ、
コルチゾン、ヒドロコルチゾン、プレドニゾロン、アレ
ドロジエン、テストステロン、メチルテストステロン、
エストラジオール、エチニルエストラジオール、エスト
ロン、ジエチルスチルベスチロール、プロゲステロン、
プロラクチン、オキシトシン、ハブプレノシン、コルチ
コステロン等のホルモン類、（ナントニン、マクリ、カ
イニン酸、チモール、塩化メチルロザニリン、クレンビ
、スルファミン アセトスルファミン、スルファチアゾ
ール、ストレプトマイシン、カナマイシン、バイオマイ
シン、Ｐ−アミンサリチル酸ｍ ４体、イソニアシト、
チオアセタゾン、ペニシリン、デヒドロ酢酸、パラオキ
シＩ安息香酸エステル、プロ力インペニシリン、クロラ
ムソエニコール、エリスロマイシン、テトラサイクリン
等の駆虫薬・抗病原微生物薬・抗生物質や５−フルオロ
ウラシル、６−メルカプトプリン、アラビノフラノミル
アデニン、コルヒチン等が挙げられる。dicumarol, tranexamic acid, heparin sodium,
Blood hematopoietic system agents such as phytonadione, indomethacin, menadione, 1-romboprasnan, ascorbic acid derivatives, flavonoid derivatives, tryptophan threonine, valine, isoloinone, di-isine methionine, phenylalanine histidine, glutamic acid, sitosterol, retinol, cholecalciferol , ergocarnpherol, pyridoquine, thiamine 2 P-aminobenzoic acid, riboflavin, nicotinamide pantothenic acid, biotin and other metabolic agents, thyroxine derivatives, methylthiouracil, parathormone, insulin, glucagon, glucocorticoids, etc. Colchikoji,
Cortisone, hydrocortisone, prednisolone, alledrogien, testosterone, methyltestosterone,
Estradiol, ethinyl estradiol, estrone, diethylstilbestirol, progesterone,
Hormones such as prolactin, oxytocin, hubprenocin, corticosterone, (nantonin, macri, kainic acid, thymol, methylrosaniline chloride, clembi, sulfamine acetosulfamine, sulfathiazole, streptomycin, kanamycin, biomycin, P-amine salicylic acid m4 body, isoniacito,
Anthelmintics, anti-pathogenic microbial drugs, antibiotics such as thioacetazone, penicillin, dehydroacetic acid, paraoxy I benzoic acid ester, penicillin, chloramsoenicol, erythromycin, tetracycline, 5-fluorouracil, 6-mercaptopurine, arabic Examples include nofuranomyladenine and colchicine.
薬効成分の配合量は種類によって限定できないが、大略
０．０１−１０重量％となるように配合することが望ま
しい。Although the amount of medicinal ingredients to be blended cannot be limited depending on the type, it is desirable to blend the medicinal ingredients to approximately 0.01-10% by weight.
本発明に於いて経皮吸収製剤とは、角質層を経由する皮
膚外用製剤の他に、眼粘膜、鼻粘膜、膣粘膜、直腸粘膜
等の粘膜を経由する経粘膜吸収製剤も包含し、これを皮
膚外用製剤として使用する場合には、剤型として例えば
軟膏剤、ローション剤、スプレー剤、リニメント剤、パ
スタ剤、パップ剤として適用する他、更に皮膚化粧料や
毛髪化粧料に添加して使用することも出来る。また、こ
れを経粘膜投与製剤として使用する場合には、剤型とし
て半開、軟膏、ソフトカプセル、バッカル錠、舌下錠２
点鼻剤等により製剤化出来る。In the present invention, transdermal absorption preparations include not only preparations for external use on the skin that pass through the stratum corneum, but also transmucosal preparations that pass through mucous membranes such as ocular mucosa, nasal mucosa, vaginal mucosa, and rectal mucosa. When used as an external skin preparation, it can be applied in the form of an ointment, lotion, spray, liniment, paste, poultice, or added to skin cosmetics or hair cosmetics. You can also do that. In addition, when using this as a transmucosal administration preparation, the dosage form may be semi-open, ointment, soft capsule, buccal tablet, or sublingual tablet.
It can be formulated into nasal sprays, etc.
以下実施例、比較例及び実験例の記載にて本発明の詳細
な説明する。The present invention will be described in detail below with reference to Examples, Comparative Examples, and Experimental Examples.
実施例−１
−Ｃ式＋１１で表わされるＬＰＤのうちで＾
る、ｌ−バルミトイル−３−グリセリルホスホリルコリ
ン５．０ ｇ 、サリチル酸メチル５．０ ｇを秤量し
、精製水を加えて１００ｇとする。この混合物を ８０
℃にて均一に溶解した後、室温まで冷ＪＪＩし、本発明
のサリチル酸メチル外用剤を調製した。Example 1 5.0 g of l-valmitoyl-3-glycerylphosphorylcholine and 5.0 g of methyl salicylate, both of which are LPDs represented by formula C+11, are weighed and purified water is added to make 100 g. This mixture is 80
After uniformly dissolving at ℃, cooling JJI was carried out to room temperature to prepare the external preparation of methyl salicylate of the present invention.
実験例−１
実施例−１のサリチル酸メチル外用剤の経皮吸収性を次
の方法にて検討した。Experimental Example 1 The percutaneous absorption of the external methyl salicylate preparation of Example 1 was investigated using the following method.
体重約２００ｇの雄性ラット背部をバリカンで刺毛し、
試料０．１ｇ（サリチル酸メチル含量５ｍｇ）を、皮膚
約４ｃｍ’に塗布した。塗布後１．２．４．６．１２時
間後に採血を行った。サリチル酸メチルの血中濃度は、
これをサリチル酸に変換した後、高速液体クロマトグラ
フィーを用いて常法により測定した。その結果を第１図
に示す。尚、対照は市販のサリチル酸メチル軟膏０．１
ｇ（サリチル酸含量５ｍｇ）を用いた。The back of a male rat weighing approximately 200 g was pricked with hair clippers.
0.1 g of sample (methyl salicylate content 5 mg) was applied to approximately 4 cm' of skin. Blood was collected 1.2.4.6.12 hours after application. The blood concentration of methyl salicylate is
After converting this into salicylic acid, it was measured by a conventional method using high performance liquid chromatography. The results are shown in FIG. The control was commercially available methyl salicylate ointment 0.1
g (salicylic acid content: 5 mg) was used.
第１図から明らかなように、本発明品を塗布した場合、
対照に比べてサリチル酸の血中濃度が高＜、ＬＰＤの経
皮吸収促進効果が認められた。As is clear from Fig. 1, when the product of the present invention is applied,
The blood concentration of salicylic acid was higher than that of the control, and the effect of promoting transdermal absorption of LPD was observed.
実施例−２，比較例−１
下記、組成の如（、Ｉ４ｃでラヘルしたインドメタノン
（以下”Ｃ−ＩＭと略記する）を含有する本発明の軟膏
及び比較用の軟膏を調整し経皮吸収（組成）
ｌ−ステアロイル−３
リンを用いた。Example 2, Comparative Example 1 An ointment of the present invention and a comparative ointment containing I4c-labeled indomethane (hereinafter abbreviated as "C-IM") were prepared as shown below and administered transdermally. Absorption (composition) l-stearoyl-3 phosphorus was used.
グリセリルホスポリルコ
（調整方法）
組成中１〜５を水浴上で加温し、７５℃に保ちながら、
６．７を８０℃にて加温溶解した液を徐々に加え、かき
混ぜ、加温をやめ固まるまでがき混ぜる。Glycerylphosporylco (preparation method) Heat components 1 to 5 in the composition on a water bath, and while keeping it at 75°C,
Gradually add the solution obtained by heating and dissolving 6.7 at 80℃, stir, and then stop heating and stir until solidified.
実験例−２
実施例−２，比較例＝１で調整した試料０．１ ｇ（１
μＣｉ ／ ０．１ ｇ ）を、実験例−１と同様の操
作にてラットに塗布し、１．２．４．６．１２時間後の
血液を取り、液体シンチレーションカウンターにて放射
活性を測定し、血中”Ｃ−１Ｍ量を求めた。第２図にそ
の結果を示す。Experimental Example-2 0.1 g (1
μCi/0.1 g) was applied to rats in the same manner as in Experimental Example 1, blood was taken 1.2.4.6.12 hours later, and radioactivity was measured using a liquid scintillation counter. The amount of "C-1M" in the blood was determined. The results are shown in FIG.
第２図から明らかなように、本発明の軟膏が比較例のも
のより高い吸収性を示すことは明らかである。As is clear from FIG. 2, it is clear that the ointment of the present invention exhibits higher absorbency than that of the comparative example.
実施例−３
グリセリン４５ｇ、ホウ酸４．５２．チモール０、０５
ｇ 、 Ｌ Ｐ Ｄ ２ ｇ 、 ’ｊ ＩＪ ｆ
ル酸メ−Ｊ−ル０．５ ｇ 。Example-3 45g of glycerin, 4.52g of boric acid. Thymol 0,05
g , L P D 2 g , 'j IJ f
0.5 g of male acid.
及びハツカ油０．０５ ｇを５０℃に均一に混和し、更
にカオリン細末４７．８５ ｇを加えて、かゆ状とし、
ガーゼに包んで本発明のパップ剤を調整した。and 0.05 g of peppermint oil were mixed uniformly at 50°C, and 47.85 g of fine kaolin powder was added to form a porridge.
A poultice of the present invention was prepared by wrapping it in gauze.
面、ここで用いたＬＰＤは、−Ｃ式（２）で表わされ、
２〜バルミトイル−３−グリセリルホスボリルイノント
ールを用いた。The LPD used here is expressed by -C formula (2),
2-valmitoyl-3-glycerylphosphorylinonthole was used.
実施例−４
一１ｉｓｔ式ｉｌｌで表わされるＬ Ｉ） Ｄのうちで
Ｏθ
バルミトイル〜３−グリセリルホスボリルエタノールア
ミン１０ｇ、インドメタシンＩＯｇを秤量し、精製水を
加えて１００ｇとする。この混合物６０℃に加温し、か
きまぜゲル状とし、直腸投与製剤とした。Example 4 10g of Oθ valmitoyl-3-glycerylphosphoborylethanolamine and IOg of indomethacin were weighed out of L I) D expressed by the formula ill, and purified water was added to make 100g. This mixture was heated to 60° C. and stirred to form a gel, which was then used as a preparation for rectal administration.
実験例−３
実験例−１と同様の方法にて実施例４及び市ｌＩ〃のイ
ンドメタシン半開を対照に吸収性を評価した。Experimental Example 3 Absorbency was evaluated in the same manner as in Experimental Example 1 using Example 4 and Ichi I's half-open indomethacin as a control.
その結果を第３図に示す。The results are shown in FIG.
第３図から明らかなように、本発明品を塗布した場合、
対照に比べてインドメタシンの血中濃度が高く、ＬＰＤ
の経皮吸収促進効果が認められた。As is clear from Fig. 3, when the product of the present invention is applied,
Blood concentration of indomethacin was higher than in controls, and LPD
The effect of promoting transdermal absorption was observed.
以上、記述した如く、ＬＰＤ及び薬効成分を含有する本
発明の経皮吸収製剤が優れた吸収性を示すことは、明ら
かである。As described above, it is clear that the transdermal absorption preparation of the present invention containing LPD and a medicinal ingredient exhibits excellent absorbability.
第１図は実験例１の結果を示す図、第２図は実験例２の
結果を示す図、第３図は実験例３の結果を示す図である
。
（賢管省わ）FIG. 1 is a diagram showing the results of Experimental Example 1, FIG. 2 is a diagram showing the results of Experimental Example 2, and FIG. 3 is a diagram showing the results of Experimental Example 3. (Wise management)
Claims (1)
式、表等があります▼、▲数式、化学式、表等がありま
す▼ を示す）で表わされる化合物及び薬効成分を含有する経
皮吸収製剤。[Claims] The following general formula (1) or (2) ▲ There are mathematical formulas, chemical formulas, tables, etc. ▼ (1) ▲ There are mathematical formulas, chemical formulas, tables, etc. ▼ (2) (In the formula, R is the number of carbon atoms The alkyl group of 9 to 21, Transdermal absorption preparation containing ingredients.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29303588A JPH02138132A (en) | 1988-11-18 | 1988-11-18 | Transcutaneous absorption drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP29303588A JPH02138132A (en) | 1988-11-18 | 1988-11-18 | Transcutaneous absorption drug |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH02138132A true JPH02138132A (en) | 1990-05-28 |
Family
ID=17789649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP29303588A Pending JPH02138132A (en) | 1988-11-18 | 1988-11-18 | Transcutaneous absorption drug |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH02138132A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994003180A1 (en) * | 1992-07-30 | 1994-02-17 | Prime European Therapeuticals S.P.A. | Pharmacologically active glycerophosphoderivatives |
| WO1995035091A1 (en) * | 1994-06-21 | 1995-12-28 | Institute For Advanced Skin Research Inc. | Skin activator having glycosaminoglycan production accelerator activity |
| US5565439A (en) * | 1992-11-24 | 1996-10-15 | The Procter & Gamble Company | Methods of using lysophosphatidic acid for treating hyperproliferative conditions |
-
1988
- 1988-11-18 JP JP29303588A patent/JPH02138132A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994003180A1 (en) * | 1992-07-30 | 1994-02-17 | Prime European Therapeuticals S.P.A. | Pharmacologically active glycerophosphoderivatives |
| US5565439A (en) * | 1992-11-24 | 1996-10-15 | The Procter & Gamble Company | Methods of using lysophosphatidic acid for treating hyperproliferative conditions |
| WO1995035091A1 (en) * | 1994-06-21 | 1995-12-28 | Institute For Advanced Skin Research Inc. | Skin activator having glycosaminoglycan production accelerator activity |
| WO1995035092A1 (en) * | 1994-06-21 | 1995-12-28 | Institute For Advanced Skin Research Inc. | Skin activator having glycosaminoglycan production accelerator activity |
| WO1995035090A1 (en) * | 1994-06-21 | 1995-12-28 | Institute For Advanced Skin Research Inc. | Skin activator having glycosaminoglycan production accelerator activity |
| US5723136A (en) * | 1994-06-21 | 1998-03-03 | Institute For Advanced Skin Research, Inc. | Skin activator with glycosaminoglycan production-accelerating effect |
| US5849309A (en) * | 1994-06-21 | 1998-12-15 | Institute For Advanced Skin Research Inc. | Skin activator with glycosaminoglycan production-accelerating effect |
| US6019989A (en) * | 1994-06-21 | 2000-02-01 | Institute For Advanced Skin Research Inc. | Skin activator with glycosaminoglycan production-accelerating effect |
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