JPS63196516A - Novel medicinal composition and manufacture - Google Patents
Novel medicinal composition and manufactureInfo
- Publication number
- JPS63196516A JPS63196516A JP2490587A JP2490587A JPS63196516A JP S63196516 A JPS63196516 A JP S63196516A JP 2490587 A JP2490587 A JP 2490587A JP 2490587 A JP2490587 A JP 2490587A JP S63196516 A JPS63196516 A JP S63196516A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- lozenge
- citric acid
- weight
- sorbitol
- 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
- 239000000203 mixture Substances 0.000 title claims description 13
- 238000004519 manufacturing process Methods 0.000 title claims 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 63
- 239000007937 lozenge Substances 0.000 claims description 34
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 25
- 239000002253 acid Substances 0.000 claims description 25
- 239000000600 sorbitol Substances 0.000 claims description 25
- 235000015165 citric acid Nutrition 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 15
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 12
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 12
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims description 12
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 11
- 230000003444 anaesthetic effect Effects 0.000 claims description 8
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 6
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 6
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 6
- 239000001361 adipic acid Substances 0.000 claims description 6
- 235000011037 adipic acid Nutrition 0.000 claims description 6
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 6
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 6
- 238000002425 crystallisation Methods 0.000 claims description 6
- 230000008025 crystallization Effects 0.000 claims description 6
- 239000001530 fumaric acid Substances 0.000 claims description 6
- 235000011087 fumaric acid Nutrition 0.000 claims description 6
- 239000004310 lactic acid Substances 0.000 claims description 6
- 235000014655 lactic acid Nutrition 0.000 claims description 6
- 239000001630 malic acid Substances 0.000 claims description 6
- 235000011090 malic acid Nutrition 0.000 claims description 6
- 235000011007 phosphoric acid Nutrition 0.000 claims description 6
- 239000011975 tartaric acid Substances 0.000 claims description 6
- 235000002906 tartaric acid Nutrition 0.000 claims description 6
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 238000001704 evaporation Methods 0.000 claims description 2
- 239000003589 local anesthetic agent Substances 0.000 claims description 2
- 238000002156 mixing Methods 0.000 claims description 2
- 238000010025 steaming Methods 0.000 claims description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 22
- 238000011084 recovery Methods 0.000 description 8
- 238000009472 formulation Methods 0.000 description 7
- 229960000385 dyclonine Drugs 0.000 description 6
- BZEWSEKUUPWQDQ-UHFFFAOYSA-N dyclonine Chemical compound C1=CC(OCCCC)=CC=C1C(=O)CCN1CCCCC1 BZEWSEKUUPWQDQ-UHFFFAOYSA-N 0.000 description 6
- 239000013078 crystal Substances 0.000 description 4
- 235000009508 confectionery Nutrition 0.000 description 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 150000007523 nucleic acids Chemical class 0.000 description 2
- 102000039446 nucleic acids Human genes 0.000 description 2
- 108020004707 nucleic acids Proteins 0.000 description 2
- QXCGBYNEYRXFEK-UHFFFAOYSA-N 1-[4-(3-methylbutoxy)phenyl]-3-piperidin-1-ylpropan-1-one Chemical compound C1=CC(OCCC(C)C)=CC=C1C(=O)CCN1CCCCC1 QXCGBYNEYRXFEK-UHFFFAOYSA-N 0.000 description 1
- SVPKNMBRVBMTLB-UHFFFAOYSA-N 2,3-dichloronaphthalene-1,4-dione Chemical compound C1=CC=C2C(=O)C(Cl)=C(Cl)C(=O)C2=C1 SVPKNMBRVBMTLB-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- 206010068319 Oropharyngeal pain Diseases 0.000 description 1
- 206010033372 Pain and discomfort Diseases 0.000 description 1
- 201000007100 Pharyngitis Diseases 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000010411 cooking Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- KNZADIMHVBBPOA-UHFFFAOYSA-N dyclonine hydrochloride Chemical compound [Cl-].C1=CC(OCCCC)=CC=C1C(=O)CC[NH+]1CCCCC1 KNZADIMHVBBPOA-UHFFFAOYSA-N 0.000 description 1
- 229960003462 dyclonine hydrochloride Drugs 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 210000002379 periodontal ligament Anatomy 0.000 description 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 208000003265 stomatitis Diseases 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
(57)【要約】本公報は電子出願前の出願データであるた
め要約のデータは記録されません。(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.
Description
【発明の詳細な説明】
〔発明の目的〕
産業上の利用分野
本発明はソルビトール基剤に、麻酔剤として効果的な量
の式（１）
（式中、Ｒは２〜８個の炭素原子を有するアルキルであ
る）で表わされる化合物の医薬として適当な酸付加塩の
添加の前にまたは同時にロゼンジ剤の約０．１〜１．０
約重量％の量でり°エン酸、フマール酸、リンゴ酸、酒
石酸、乳酸、アジピン酸及び燐酸からなる群から選択さ
れた医薬として適当な酸または約ｏ、ｏｏｓ〜約０．０
１−の量の塩酸を添加したものからなり、かつ核酸の量
は核酸付加塩を安定化しかつ望ましくないソルビトール
の結晶化を避けるのに充分である麻酔剤ロゼンジ剤に関
係するもので６る口
従来の技術
この分野ではアルコキシ基が２〜８個の炭素原子を有す
る３−ピペリジノ−ｐ−アルコ中りプロビオフエノン類
の酸付加塩を硬質キャンディ基剤と混合することにより
麻酔剤ロゼンジ剤を製造することか知られている（米国
特許第４．１３９．６２７号明細１１）。この特許によ
れば、特定の量のクエン酸、フマール酸、リンゴ酸、酒
石酸、乳酸、アジピン酸及び燐酸からなる群から選択さ
れた医薬として適当な酸が麻酔剤として効果的な量の活
性剤の添加の前にまたは同時に硬質キャンディ基剤に添
加される。この酸は３−ピペリジノ−ｐ−アルコキシグ
ロビオフエノン塩を溶解硬質キャンディ基剤と混合する
とき起きる分解を防ぐ目的で添加される。DETAILED DESCRIPTION OF THE INVENTION OBJECTS OF THE INVENTION Industrial Field of Application The present invention provides a sorbitol base with an anesthetically effective amount of the formula (1) (wherein R is 2 to 8 carbon atoms). from about 0.1 to 1.0 of the lozenge before or simultaneously with the addition of the pharmaceutically suitable acid addition salt of the compound represented by
% by weight of a pharmaceutically suitable acid selected from the group consisting of enoic acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid or from about 0,00 to about 0.0
1-6 of anesthetic lozenges, wherein the amount of nucleic acid is sufficient to stabilize the nucleic acid addition salt and avoid undesirable sorbitol crystallization. BACKGROUND OF THE INVENTION In this field, anesthetic lozenges have been prepared by mixing acid addition salts of 3-piperidino-p-alcoprobiophenones in which the alkoxy group has 2 to 8 carbon atoms with a hard candy base. It is known to produce (U.S. Pat. No. 4,139,627, specification 11). According to this patent, a specified amount of a pharmaceutically suitable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid is used as an anesthetically effective amount of the active agent. is added to the hard candy base prior to or simultaneously with the addition of. This acid is added to prevent decomposition that occurs when the 3-piperidino-p-alkoxyglobiophenone salt is mixed with the molten hard candy base.
この分野ではまた０、５〜５％の販、好ましくはクエン
酸を、結晶化を防ぐことにより、ソルビトールを安定化
させる目的で添加することにより安定化するととも知ら
れている。It is also known in the art to stabilize sorbitol by adding 0.5 to 5% sorbitol, preferably citric acid, for the purpose of stabilizing sorbitol by preventing crystallization.
発明が解決しようとする問題
本発明において、米国特許第３．７３８．８４５号明細
書中に記載されたことは逆に、クエン酸のような酸が添
加されたときでさえ、ソルビトールは結晶化することが
見出された０クエン酸または他の同様な好適な酸を添加
すると、ソルビトールは結晶を形成し、それは無定形物
質ではない。本発明において、クエン酸のような酸は酸
性媒体を保持し、かつロゼンジ剤を外観土兄にくくする
ような結晶のような望ましくない結晶を避けるが、該特
許が言及するようにソルビトール自体の結晶化を完全に
避けるのではないことが見出された。Problem to be Solved by the Invention In the present invention, contrary to what was described in U.S. Pat. No. 3,738,845, sorbitol does not crystallize even when an acid such as citric acid is added. It has been found that upon addition of citric acid or other similar suitable acids, sorbitol forms crystals and it is not an amorphous substance. In the present invention, an acid such as citric acid retains the acidic medium and avoids undesirable crystals such as crystals that would make the lozenge look dull, but as the patent mentions, crystals of sorbitol itself. It was found that this does not completely avoid the
問題を解決するための手段
本発明は麻酔剤として効果的な量の上記式（１）で表わ
される３−ピペリジノ−ｐ−アルコキシプロビオフエノ
ンの酸付加塩の添加の前Ｖｃｔた社同時にソルビトール
基剤に約０．１〜約１．０″Ｉｉ量チのクエン酸、フマ
ール酸、リンゴ酸、酒石酸、乳酸、アジピン酸及び燐酸
からなる群から選択された医薬として適当な酸または約
ｏ、ｏｏｓ〜約０．０１％の塩酸を添加すると、塩を安
定化し、かっソルビ） −ルの望ましくない結晶化のみ
を防ぐが、ソルビトール自体の結晶化を完全には防止で
きないという知見に基ずく。得られた生成物は外観が良
くかつ麻酔剤を使用者まで運搬するのに効果的である透
明なソルビトール麻酔剤ロゼンジ剤である。Means for Solving the Problems The present invention discloses that prior to the addition of an acid addition salt of 3-piperidino-p-alkoxyprobiophenone represented by the above formula (1) in an effective amount as an anesthetic, Vct and sorbitol groups are simultaneously added. The agent contains about 0.1 to about 1.0" of a pharmaceutically suitable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid, and phosphoric acid or about 0,000 s. Based on the finding that addition of ~0.01% hydrochloric acid stabilizes the salt and prevents only the undesired crystallization of sorbitol, but does not completely prevent crystallization of sorbitol itself. The resulting product is a clear sorbitol anesthetic lozenge that is aesthetically pleasing and effective in transporting the anesthetic to the user.
作用・効果
本発明による典型的な実施態様において、生成物は先ず
ソルビトール溶液から希釈剤（水）を蒸発させることに
より製造される。医薬として適当な酸、例えばクエン酸
は蒸煮の前にあるいは麻酔剤として効果的な量の３−ピ
ペリジノ−ｐ−アルフキシグロピオフエノンの酸付加塩
の添加の前にまたはそれと同時に酸性化溶液として給線
される。In a typical embodiment according to the invention, the product is prepared by first evaporating the diluent (water) from a sorbitol solution. A pharmaceutically suitable acid, such as citric acid, is added to the acidified solution prior to cooking or prior to or simultaneously with the addition of an anesthetically effective amount of the acid addition salt of 3-piperidino-p-alfoxyglopiofenone. It is fed as.
任意の望ましい風味剤及び／または着色剤が添加され、
全混合物は充分にブレンドされる。次いで。Any desired flavoring and/or coloring agents are added;
The entire mixture is thoroughly blended. Next.
混合物は適当な寸法の金型中に入れられ、冷却により硬
化されることにより硬實結晶性ンルビトールロゼンジ剤
が製造される。The mixture is placed in a mold of appropriate size and hardened by cooling to produce a hard crystalline nrubitol lozenge.
３−ピペリジノ−ｐ−ｎ−ブト中シプロビオフエノン、
すなわちジクロニン塩酸塩（ｄｙｅｌｏｎｉｎｅｈｙｄ
ｒｏｅｈｌｏｒｉｄ・）が好ましい局所麻酔剤であるが
、本発明は３−ピペリジノ−ｐ−ｎ−オクチルオキシプ
ロピオフェノン、３−ピペリジノ−ｐ−ｎ−エトキシプ
ロビオフエノ／、３−ビペＩＪ シノーｐ−ｎ−アモキ
シグロビオフエノン、３−ピペリシノーｐ−イソブトキ
シ−プロビオフェノン、３−ピペリジノ−ｐ −５ｅｅ
−プトキシグロピオフエノン、３−ピペリジノ−ｐ−ｎ
−プロポキングロビオフエノン、３−ピペリジノ−ｐ−
イソアモキシプロピオフエノン、３−ピペリジノ−ｐ−
イングロポキングロビオフエノン、３−ピペリジノ−ｐ
−ｎ−へプテルオ中ジープロピオフェノン及び３−ピ
ペリジノ−ｐ−ｎ−へキシルオキシプロピオフェノンの
ようなこのクラスの他の化合物にとっても等しく有用で
ある。cyprobiofuenone in 3-piperidino-pn-buto;
That is, dyclonine hydrochloride (dyeloninehydrochloride)
roehlorid) is the preferred local anesthetic, but the present invention uses 3-piperidino-pn-octyloxypropiophenone, 3-piperidino-pn-ethoxyprobiofueno/, 3-bipeIJ sinop -n-amoxyglobiophenone, 3-piperisino-p-isobutoxy-probiophenone, 3-piperidino-p-5ee
-Ptoxyglopiofenone, 3-piperidino-p-n
-propoquine globiofenone, 3-piperidino-p-
Isoamoxypropiophenone, 3-piperidino-p-
Inglopoquine globiofuenone, 3-piperidino-p
Other compounds of this class are equally useful, such as di-propiophenone and 3-piperidino-pn-hexyloxypropiophenone.
同様に、塩酸塩がそれが容易に入手できるので好ましい
が、これらピペリジノ化合物の他の医薬として適当な塩
、例えば臭化水素酸、フマール酸、リンゴ酸、酒石酸、
乳酸、アジピン酸、燐酸、硫酸、メタンスルホン酸、ナ
フテンジスルホン酸等と共に形成されたものも同様に使
用できる◎得られたロゼンジ剤はその麻酔性質の結果と
して軽度の咽喉炎、軽度の口内刺激症、口内炎の疼痛及
び不快並びに歯根膜処置及び軽度の口内手術の後の疼痛
及び不快の緩和を提供する。Similarly, although the hydrochloride salt is preferred due to its ready availability, other pharmaceutically suitable salts of these piperidino compounds such as hydrobromic acid, fumaric acid, malic acid, tartaric acid,
Those formed with lactic acid, adipic acid, phosphoric acid, sulfuric acid, methanesulfonic acid, naphthendisulfonic acid, etc. can be used as well.The resulting lozenges cause mild sore throat and mild oral irritation as a result of their anesthetic properties. , provides relief from the pain and discomfort of stomatitis and after periodontal ligament procedures and minor oral surgery.
以下、実施例により更に詳しく本発明を例示するが、本
発明はこれらに限定されない。EXAMPLES Hereinafter, the present invention will be illustrated in more detail with reference to Examples, but the present invention is not limited thereto.
実施例１
ジクロニン回収
３チ月 １０３．２チ
１２ケ月 ９９・４％
２６ケ月 １０２．７ ％
ソルビトールをクエン酸と共に蒸煮することにより水を
蒸発させた。次いで、ジクローンＨＣｔ及び残りの成分
を添加し、混合物を充分ブレンドし、次いで金型中に入
れることによ、す、ソルビトールロゼンジ剤を得た。Example 1 Dyclonine recovery 3 months 103.2 days 12 months 99.4% 26 months 102.7% Water was evaporated by steaming sorbitol with citric acid. Diclone HCt and the remaining ingredients were then added, the mixture was thoroughly blended and then placed into a mold to obtain a sorbitol lozenge.
実施例２
ジクロニン回収
３チ月 １１６．０％
１２チ月 １０５．６ ％
２６ケ月 一
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。Example 2 Dyclonine recovery 3 months 116.0% 12 months 105.6% 26 months According to the method described in Example 1, a sorbitol lozenge with the above formulation was manufactured.
ジクロニ／回収
３チ月 １１１．６％
１２チ月 １０５．３チ
・′２６２６チ 一
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。Dicloni/Recovery 3 months 111.6% 12 months 105.3 days 2626 days A sorbitol lozenge with the above formulation was manufactured according to the method described in Example 1.
実施例４
チ 呼
ジクロニン回収
３チ月 １０７．６％
１２チ月 ９７．１ ％
２６ケ月 ９５．６ ％
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。Example 4 Diclonine recovery: 3 months 107.6% 12 months 97.1% 26 months 95.6% According to the method described in Example 1, sorbitol lozenges with the above formulation were manufactured.
実施例５
％ 岬
ジクロニン回収 ９６．７ ’Ａ
２チ月 ＲＴ
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。Example 5 % Misaki Dyclonine Recovery 96.7'A 2 months RT According to the method described in Example 1, sorbitol lozenges of the above formulation were prepared.
実施例６ ジクロニン回収 １０１．７ Ｔ。Example 6 Dyclonine recovery 101.7T.
２チ月 ＲＴ
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。2 months RT According to the method described in Example 1, sorbitol lozenges with the above formulation were manufactured.
実施例７
ジクロニン回収 １００．ＯＳ
２チ月ＲＴ
実施例１に記載した方法に従って、上記処方のソルビト
ールロゼンジ剤を製造した。Example 7 Dyclonine recovery 100. OS 2 months RT According to the method described in Example 1, sorbitol lozenges with the above formulation were manufactured.
実施例８
− 雫
ジクロニン回収 ９８．３チ
２チ月 ＲＴ
実施例１に記載した方法に従い、上記処方のソルビトー
ルロゼンジ剤を製造した。Example 8 - Recovery of dyclonine drops 98.3 x 2 months RT According to the method described in Example 1, a sorbitol lozenge with the above formulation was manufactured.
代理人 弁理士 秋 沢 政 光 他１名 自ｉ発手わｌＩ：、搾１↑正截Ｙ 昭和６２年３月ｌＯ口Agent Patent Attorney Masaaki Akizawa 1 other person Self-motivated hand:, squeeze 1 ↑ Masaki Y March 1986 lO mouth
Claims (18)
る）で表わされる化合物の医薬として適当な酸付加塩、
及びロゼンジ剤の約０．１〜約１．０重量％のクエン酸
、フマール酸、リンゴ酸、酒石酸、乳酸、アジピン酸及
び燐酸からなる群から選択された医薬として適当な酸ま
たは約０．００５〜約０．０１％ソルビトール基剤中で
十分に混合された塩酸を含み、該酸の量は該酸付加塩を
安定化しかつソルビトールの望ましくない結晶化を避け
るのに充分なものであることを特徴とするロゼンジ剤。(1) Formula for the amount effective as an anesthetic (I) ▲There are mathematical formulas, chemical formulas, tables, etc.▼(I) (wherein R is alkyl having 2 to 8 carbon atoms) pharmaceutically suitable acid addition salts of the compounds;
and from about 0.1 to about 1.0% by weight of the lozenge of a pharmaceutically suitable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid, and phosphoric acid or about 0.005% by weight of the lozenge. - about 0.01% hydrochloric acid in a sorbitol base, and the amount of acid is sufficient to stabilize the acid addition salt and avoid undesirable crystallization of the sorbitol. Characteristic lozenge agent.
載のロゼンジ剤。(2) The lozenge according to claim (1), wherein the acid is citric acid.
囲第（１）項記載のロゼンジ剤。(3) The lozenge according to claim (1), containing 0.4% by weight of citric acid.
囲第（１）項記載のロゼンジ剤。(4) The lozenge according to claim (1), containing 0.1% by weight of citric acid.
囲第（１）項記載のロゼンジ剤。(5) The lozenge according to claim (1), containing 0.3% by weight of citric acid.
囲第（１）項記載のロゼンジ剤。(6) The lozenge according to claim (1), containing 0.6% by weight of citric acid.
囲第（１）項記載のロゼンジ剤。(7) The lozenge according to claim (1), containing 1.0% by weight of citric acid.
る特許請求の範囲第（１）項記載のロゼンジ剤。(8) The lozenge according to claim (1), which contains about 0.005 to about 0.01% by weight of hydrochloric acid.
のロゼンジ剤。(9) The lozenge according to claim (1), wherein the salt is a hydrochloride.
項記載のロゼンジ剤。(10) Claim No. (1) in which R is n-butyl
Lozenges as described in section.
）項記載のロゼンジ剤。(11) R is n-propyl Claim (1)
Lozenges described in ).
ある特許請求の範囲第（１）項記載のロゼンジ剤。(12) The lozenge according to claim (1), wherein R is n-butyl and the salt is a hydrochloride.
して酸はクエン酸である特許請求の範囲第（１）項記載
のロゼンジ剤。(13) The lozenge according to claim (1), wherein R is n-butyl, the salt is hydrochloride, and the acid is citric acid.
ら水を蒸発させ、ロゼンジ剤の約０．１〜約１．０重量
％のクエン酸、フマール酸、リンゴ酸、酒石酸、乳酸、
アジピン酸及び燐酸からなる群から選択された医薬とし
て適当な酸または約０．００５〜約０．０１％の塩酸を
酸性化溶液として、蒸煮の前または麻酔剤として効果的
な量の式（ I ） ▲数式、化学式、表等があります▼（ I ） （式中、Ｒは２〜８個の炭素原子を有するアルキルであ
る）で表わされる化合物の医薬として適当な酸付加塩の
添加の前に添加し、尚該酸の量は酸付加塩を安定化しか
つソルビトールの望ましくない結晶化を避けるのに充分
なものであり、混合物をブレンドし、そして混合物を硬
化させることにより硬質結晶性ソルビトールロゼンジ剤
を形成させることを特徴とする局所麻酔剤ロゼンジ剤を
製造する方法。(14) evaporating the water from the sorbitol solution by heating the lozenge to about 0.1 to about 1.0% by weight of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid;
A pharmaceutically suitable acid selected from the group consisting of adipic acid and phosphoric acid or from about 0.005 to about 0.01% hydrochloric acid as an acidifying solution prior to steaming or as an anesthetic in an effective amount of the formula (I) ) ▲Mathematical formulas, chemical formulas, tables, etc.▼ (I) Before addition of a pharmaceutically suitable acid addition salt of the compound represented by (I) (wherein R is alkyl having 2 to 8 carbon atoms) adding the acid in an amount sufficient to stabilize the acid addition salt and avoid undesirable crystallization of the sorbitol, blending the mixture, and curing the mixture to form a hard crystalline sorbitol lozenge. A method for producing a local anesthetic lozenge, which comprises forming a lozenge.
項記載の方法。(15) Claim No. (14) in which the acid is citric acid
The method described in section.
範囲第（１４）項記載の方法。(16) The method according to claim (14), wherein about 0.4% citric acid is added.
範囲第（１４）項記載の方法。(17) The method according to claim (14), wherein about 0.1% citric acid is added.
範囲第（１４）項記載の方法。(18) The method according to claim (14), wherein about 0.3% citric acid is added.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2490587A JPS63196516A (en) | 1987-02-06 | 1987-02-06 | Novel medicinal composition and manufacture |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2490587A JPS63196516A (en) | 1987-02-06 | 1987-02-06 | Novel medicinal composition and manufacture |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS63196516A true JPS63196516A (en) | 1988-08-15 |
Family
ID=12151191
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2490587A Pending JPS63196516A (en) | 1987-02-06 | 1987-02-06 | Novel medicinal composition and manufacture |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS63196516A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AT407111B (en) * | 1998-12-22 | 2000-12-27 | Gergely Dr & Co | SUGAR- AND / OR SUGAR-ALCOHOLIC MATRIX MATERIAL AND METHOD FOR THE PRODUCTION THEREOF |
-
1987
- 1987-02-06 JP JP2490587A patent/JPS63196516A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AT407111B (en) * | 1998-12-22 | 2000-12-27 | Gergely Dr & Co | SUGAR- AND / OR SUGAR-ALCOHOLIC MATRIX MATERIAL AND METHOD FOR THE PRODUCTION THEREOF |
| US6541034B1 (en) | 1998-12-22 | 2003-04-01 | Gerhard Gergely | Matrix material containing sugars and/or sugar alcohols and process for its preparation |
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