JPH021409A - Ointment preparation - Google Patents
Ointment preparationInfo
- Publication number
- JPH021409A JPH021409A JP1077102A JP7710289A JPH021409A JP H021409 A JPH021409 A JP H021409A JP 1077102 A JP1077102 A JP 1077102A JP 7710289 A JP7710289 A JP 7710289A JP H021409 A JPH021409 A JP H021409A
- Authority
- JP
- Japan
- Prior art keywords
- polyethylene glycol
- base
- ointment
- cyclic
- saccharide
- 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
- 238000002360 preparation method Methods 0.000 title claims abstract description 4
- 239000002674 ointment Substances 0.000 title claims description 27
- 238000001035 drying Methods 0.000 claims abstract description 13
- 229920000592 inorganic polymer Polymers 0.000 claims abstract description 10
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical class C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 claims abstract description 7
- 150000001720 carbohydrates Chemical class 0.000 claims abstract description 6
- 239000000203 mixture Substances 0.000 abstract description 14
- 229920001353 Dextrin Polymers 0.000 abstract description 9
- 239000004375 Dextrin Substances 0.000 abstract description 9
- 235000019425 dextrin Nutrition 0.000 abstract description 9
- 229940068918 polyethylene glycol 400 Drugs 0.000 abstract description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 7
- 229920001223 polyethylene glycol Polymers 0.000 abstract description 6
- 206010040943 Skin Ulcer Diseases 0.000 abstract description 5
- 238000010521 absorption reaction Methods 0.000 abstract description 5
- 231100000019 skin ulcer Toxicity 0.000 abstract description 5
- 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 abstract description 4
- 239000002202 Polyethylene glycol Substances 0.000 abstract description 4
- 239000011734 sodium Substances 0.000 abstract description 4
- 229910052708 sodium Inorganic materials 0.000 abstract description 4
- -1 sodium N<6> Chemical class 0.000 abstract description 3
- 230000007062 hydrolysis Effects 0.000 abstract description 2
- 238000006460 hydrolysis reaction Methods 0.000 abstract description 2
- 229920001282 polysaccharide Polymers 0.000 abstract 2
- 239000004698 Polyethylene Substances 0.000 abstract 1
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 abstract 1
- 238000002156 mixing Methods 0.000 abstract 1
- 229920000573 polyethylene Polymers 0.000 abstract 1
- 239000004020 conductor Substances 0.000 description 9
- 125000004122 cyclic group Chemical group 0.000 description 9
- 229910019142 PO4 Inorganic materials 0.000 description 5
- 229940024546 aluminum hydroxide gel Drugs 0.000 description 5
- SMYKVLBUSSNXMV-UHFFFAOYSA-K aluminum;trihydroxide;hydrate Chemical compound O.[OH-].[OH-].[OH-].[Al+3] SMYKVLBUSSNXMV-UHFFFAOYSA-K 0.000 description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 5
- 239000010452 phosphate Substances 0.000 description 5
- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 5
- 238000009472 formulation Methods 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 150000008163 sugars Chemical class 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- 229920000858 Cyclodextrin Polymers 0.000 description 2
- 229920002307 Dextran Polymers 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 229940095074 cyclic amp Drugs 0.000 description 2
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- NFFYGAVXFCQEOT-FRJWGUMJSA-N n-[9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-6-yl]butanamide Chemical compound C1=NC=2C(NC(=O)CCC)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NFFYGAVXFCQEOT-FRJWGUMJSA-N 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 239000003883 ointment base Substances 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 1
- WQZBIMQFROXVSY-MCDZGGTQSA-N (2r,3r,4s,5r)-2-(6-aminopurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol;sodium Chemical compound [Na].C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O WQZBIMQFROXVSY-MCDZGGTQSA-N 0.000 description 1
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 description 1
- DTAIVWRIZJOEEQ-IWCJZZDYSA-N C(C1=CC=CC=C1)C=1N([C@H]2[C@H](S)[C@H](O)[C@@H](CO)O2)C=2N=CN=C(C2N1)N Chemical compound C(C1=CC=CC=C1)C=1N([C@H]2[C@H](S)[C@H](O)[C@@H](CO)O2)C=2N=CN=C(C2N1)N DTAIVWRIZJOEEQ-IWCJZZDYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 239000001116 FEMA 4028 Substances 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 description 1
- 229940043377 alpha-cyclodextrin Drugs 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 1
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 1
- 229960004853 betadex Drugs 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- DTPCFIHYWYONMD-UHFFFAOYSA-N decaethylene glycol Polymers OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO DTPCFIHYWYONMD-UHFFFAOYSA-N 0.000 description 1
- GDVKFRBCXAPAQJ-UHFFFAOYSA-A dialuminum;hexamagnesium;carbonate;hexadecahydroxide Chemical compound [OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-]C([O-])=O GDVKFRBCXAPAQJ-UHFFFAOYSA-A 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000000416 exudates and transudate Anatomy 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 229960001545 hydrotalcite Drugs 0.000 description 1
- 229910001701 hydrotalcite Inorganic materials 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- XCOBTUNSZUJCDH-UHFFFAOYSA-B lithium magnesium sodium silicate Chemical compound [Li+].[Li+].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Na+].[Na+].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3.O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3.O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3.O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3.O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3.O1[Si](O2)([O-])O[Si]3([O-])O[Si]1([O-])O[Si]2([O-])O3 XCOBTUNSZUJCDH-UHFFFAOYSA-B 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229940057847 polyethylene glycol 600 Drugs 0.000 description 1
- 229940085675 polyethylene glycol 800 Drugs 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000003351 stiffener Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
〈産業上の利用分野〉
本発明はサイクリックＡＭＰ話導体を含有する軟膏製剤
に関する。DETAILED DESCRIPTION OF THE INVENTION <Industrial Field of Application> The present invention relates to an ointment formulation containing a cyclic AMP conductor.
〈従来技術〉
従来より各種皮膚潰瘍の治療剤としては、抗生物質や抗
菌剤、酵素等を含有した軟膏、皮虜清拭液または吸水性
の高分子等の粉末、創傷被覆剤等が使用されて来ている
。特に皮膚潰瘍のような浸出液が多い湿潤面には吸水性
、乾燥性を有する軟膏が多用されている。<Prior art> Conventionally, ointments containing antibiotics, antibacterial agents, enzymes, etc., powders of water-absorbing polymers, wound dressings, etc. have been used as therapeutic agents for various skin ulcers. It's coming. In particular, ointments with water-absorbing and drying properties are often used for moist surfaces such as skin ulcers that have a lot of exudate.
一方、サイクリックＡＭＰ誘導体の各種皮膚潰瘍に対す
る効果は特願昭６１−１３９７４９号で示されたように
有効性が明かにされている。On the other hand, the effectiveness of cyclic AMP derivatives against various skin ulcers has been demonstrated as shown in Japanese Patent Application No. 139749/1983.
これらサイクリックＡＭＰｉ導体を各種皮膚潰瘍に用い
る際に最も有効であろうと考えられる基剤は、先に述べ
たように吸水性、乾燥性を有する基剤である。しかしな
がら、これら吸水性、乾燥性を有する基剤は、基剤中に
微量の水分を含有している。従って、サイクリックＡＭ
Ｐ９導体をこの基剤中に分散、溶解すると、サイクリッ
ク八Ｍ Ｐ ３３導体が徐々に加水分解を起こして長期
間にわたる使用が困難になる。When using these cyclic AMPi conductors for various skin ulcers, the base material considered to be most effective is a base material that has water absorption and drying properties as described above. However, these water-absorbing and drying bases contain a trace amount of water. Therefore, cyclic AM
When the P9 conductor is dispersed and dissolved in this base, the cyclic 8M P33 conductor gradually undergoes hydrolysis, making it difficult to use for a long period of time.
〈発明が解決した問題点〉
そこで発明者らはこれらの情況に鑑み、サイクリックＡ
ＭＰ誘導体を含有する吸水性、乾燥性を有する基剤から
なる軟膏の安定化方法について鋭意検討した結果、糖類
および／または無機高分子を併用すれば有効性が変らず
、かつサイクリックＡＭＰ９導体が安定化されることを
見いだし、本発明を完成するに至った。<Problems solved by the invention> In view of these circumstances, the inventors developed a cyclic A
As a result of intensive studies on the method of stabilizing an ointment consisting of a water-absorbing and drying base containing an MP derivative, we found that the effectiveness does not change if saccharides and/or inorganic polymers are used in combination, and that the cyclic AMP9 conductor The present inventors have found that the present invention can be stabilized, and have completed the present invention.
〈発明の構成〉
すなわち本発明は、サイクリックＡＭＰ９導体を含有す
る吸水性、乾燥性を有する基剤中に、１！頚および／ま
たは無機高分子を含有することを特徴とする軟膏製剤に
関する。<Structure of the Invention> That is, the present invention provides a water-absorbing and drying base containing a cyclic AMP9 conductor containing 1! The present invention relates to an ointment formulation characterized by containing an ointment and/or an inorganic polymer.
本発明におけるサイクリック ＡＭＰ話導体とはナトリ
ウムＮ６，２°−Ｏ−ジブチリルアデノシン３゛、５°
−サイクリックホスフェート（以下 ＤＢｃＡＭＰ）
、ナトリウム２°−〇−ブチリルアデノシン３’、５’
−サイクリックホスフェート（以下２−０−ＭＢｃＡＭ
Ｐ） 、ナトリウムＮ６−プチリルアデノシン３゛、５
°−サイクリックホスフェート（以下Ｎ６−ＭＢｃＡＭ
Ｐ） 、ナトリウムアデノシン３“、５°−サイクリッ
クホスフェート（以下ｃＡＭＰ） 、８−ベンジルチオ
Ｎ６−プチリルアデノシン３°、５°−サイクリックホ
スフェート（以下ＢＴＢｃＡＭＰ） 、 ８−ベンジル
チオアデノシン３°、５°−サイクリックホスフェート
（以下ＢＴ−ｃＡＭＰ）等を挙げることが出来る。もち
ろん、こわらの二種以上の混合物も使用することが出来
る。The cyclic AMP conductor in the present invention is sodium N6,2°-O-dibutyryladenosine 3°,5°
-Cyclic phosphate (hereinafter referred to as DBcAMP)
, sodium 2°-〇-butyryl adenosine 3', 5'
- cyclic phosphate (hereinafter 2-0-MBcAM
P), sodium N6-butyryladenosine 3゛, 5
°-cyclic phosphate (hereinafter N6-MBcAM
P), sodium adenosine 3", 5°-cyclic phosphate (hereinafter referred to as cAMP), 8-benzylthio N6-butyryladenosine 3°, 5°-cyclic phosphate (hereinafter referred to as BTBcAMP), 8-benzylthioadenosine 3°, 5 Examples include °-cyclic phosphate (hereinafter referred to as BT-cAMP), etc. Of course, a mixture of two or more types of stiffeners can also be used.
また、本発明において使用される吸水性、乾燥性を有す
る基剤としては、各種分子量を有するポリエチレングリ
コール類、グリセリン、プロピレングリコール、ブチレ
ングリコール等の多価アルコール類、もしくはこれらと
ステアリルアルコール、セチルアルコール等の高級アル
コールとの混合物等に代表される基剤である。これら吸
水性、乾燥性を有する基剤の組み合わせの比率はなんら
限定されるものではないが、特に一種または二種以上の
分子量のポリエチレングリコールの組み合わせからなる
基剤、例えばポリエチレングリコール４００とポリエチ
レングリコール４０００の等１混合物などが好ましい。In addition, the water-absorbing and drying base used in the present invention includes polyethylene glycols having various molecular weights, polyhydric alcohols such as glycerin, propylene glycol, and butylene glycol, or their combination with stearyl alcohol and cetyl alcohol. It is a base typified by a mixture with a higher alcohol such as The ratio of the combination of these water-absorbing and drying bases is not limited in any way, but in particular bases consisting of a combination of one or more polyethylene glycols with molecular weights, such as polyethylene glycol 400 and polyethylene glycol 4000. A mixture of the following is preferred.
本発明における軟膏製剤の安定化のために使用される糖
類としてはデキストリン、デキストラン、α、β、γ−
シクロデキストリン等が挙げられる。これら糖類は軟膏
基剤中に分散させれば良く、その比率はなんら限定され
るべきものではないが、好ましくは基剤１００重量部に
対し０．５〜２０重量部重量部上りわけ１〜ｌＯ重量部
程度加えるのが適している。Examples of sugars used to stabilize the ointment formulation in the present invention include dextrin, dextran, α-, β-, γ-
Examples include cyclodextrin. These saccharides may be dispersed in the ointment base, and the ratio thereof is not limited in any way, but preferably 0.5 to 20 parts by weight per 100 parts by weight of the base. It is appropriate to add about parts by weight.
また、本発明において安定化のために使用される無機高
分子としては、乾燥水酸化アルミニウムゲル、合成ケイ
酸マグネシウム、ハイドロタルサイト等が挙げられる。Further, examples of inorganic polymers used for stabilization in the present invention include dry aluminum hydroxide gel, synthetic magnesium silicate, hydrotalcite, and the like.
これら無機高分子も軟膏基剤中に分散させれば良く、そ
の比率はなんら限定されるべきものではないが、好まし
くは基剤１００重量部に対し０．１〜１０重量部重量部
上りわけ０．５〜２重量部加えるにが適している。These inorganic polymers may also be dispersed in the ointment base, and the ratio should not be limited in any way, but preferably 0.1 to 10 parts by weight per 100 parts by weight of the base. It is suitable to add .5 to 2 parts by weight.
本発明の軟膏製剤は上記の成分以外に香料、着色剤、カ
ルボキシメチルセルロースの如き水溶性高分子化合物を
含有してもよい。The ointment preparation of the present invention may contain fragrances, colorants, and water-soluble polymer compounds such as carboxymethyl cellulose in addition to the above-mentioned components.
本発明の軟膏製剤を製するには、通常の軟膏の製造方法
に従えば良い。すなわち、吸水性、乾燥性を有する基剤
を６０〜７０℃で加温溶解させ、これに糖類および／ま
たは無機高分子を添加し十分分散させた後、所定量のサ
イクリックＡＭＰ誘導体を添加し、溶解させた後冷却し
て軟膏状とする。The ointment formulation of the present invention can be produced by following a conventional ointment production method. That is, a base having water absorption and drying properties is dissolved by heating at 60 to 70°C, and after adding sugars and/or inorganic polymers and sufficiently dispersing them, a predetermined amount of a cyclic AMP derivative is added. After dissolving, it is cooled to form an ointment.
〈発明の効果〉
かくして得られた軟膏は、単に吸水性、乾燥性を有する
基剤中にサイクリックＡ Ｍ Ｐ 誘導体を溶解させた
軟膏よりも安定性か改善され、本発明の目的を達するこ
とが出来る。<Effects of the Invention> The thus obtained ointment has improved stability compared to an ointment in which a cyclic A M P derivative is simply dissolved in a water-absorbing and drying base, thereby achieving the object of the present invention. I can do it.
次に本発明を対象例、実施例および試験例により説明す
るが、本発明はこれらによってなんら限定されるもので
はない。Next, the present invention will be explained with reference to target examples, working examples, and test examples, but the present invention is not limited to these in any way.
対照例
ポリエチレングリコール４００５７．３５ｇ、ポリエチ
レングリコール４０００ ４０ｇを １００ｍ１ビーカ
ーに取り、マントルヒータ中で約６５℃で溶解した。こ
れにＤＢｃＡＭＰ ２．６５ｇを加えた後、Ｔ、に、ホ
モミキサーＭ型で５分間攪拌し、ＤＢｃＡＭＰを溶解し
た。その後水冷して軟膏１００ｇを製した。Control Example 57.35 g of polyethylene glycol 400 and 40 g of polyethylene glycol 4000 were placed in a 100 ml beaker and melted at about 65° C. in a mantle heater. After adding 2.65 g of DBcAMP to this, the mixture was stirred for 5 minutes using a homomixer type M to dissolve DBcAMP. Thereafter, the mixture was cooled with water to prepare 100 g of ointment.
実施例１
ポリエチレングリコール４００ ５６．１ｇ１ ポリエ
チレングリコール４０００４０ｇを対照例と同様に溶解
した。これにデキストリン １．２５ｇを添加し、Ｔ、
に、ホモミキサーＭ型で５分間子分に分散した。モして
ＤＢｃＡＭＰ ２．６５ｇを添加して、以後対照例と同
様にして軟膏を製した。Example 1 Polyethylene glycol 400 56.1 g 1 Polyethylene glycol 400040 g was dissolved in the same manner as in the control example. Add 1.25g of dextrin to this,
Then, the mixture was dispersed into the molecules using a homomixer type M for 5 minutes. Then, 2.65 g of DBcAMP was added thereto, and an ointment was prepared in the same manner as in the control example.
実施例２
実施例１のデキストリンの代りにデキストランＴ２Ｏを
同量添加して、軟膏を製した。Example 2 An ointment was prepared by adding the same amount of dextran T2O instead of the dextrin in Example 1.
実施例３
ポリエチレングリコール４００ ５２ｇ、ポリエチレン
グリコール４０００４０ｇを対照例と同様に溶解した。Example 3 52 g of polyethylene glycol 400 and 40 g of polyethylene glycol 4000 were dissolved in the same manner as in the control example.
これにβ−シクロデキストリン５ｇを添加し、Ｔ、に、
ホモミキサーＭ型で５分間子分に分散した。Add 5g of β-cyclodextrin to this, add T,
The particles were dispersed in a homomixer type M for 5 minutes.
更にＤＢｃＡＭＰ ３ｇを添加して、以後対照例と同
様にして軟膏を製した。Further, 3 g of DBcAMP was added and an ointment was prepared in the same manner as in the control example.
実施例４
ポリエチレングリコール８００ ４７ｇ、ポリエチレン
グリコール４０００４０ｇを対照例と同様に溶解した。Example 4 47 g of polyethylene glycol 800 and 40 g of polyethylene glycol 400,000 were dissolved in the same manner as in the control example.
これにデキストリン １０ｇを添加し、Ｔ、に、ホモミ
キサーＭ型で５分間子分に分散した。更にＤＢｃＡＭＰ
３ｇを添加して、以後対照例と同様にして軟膏を製
した。10 g of dextrin was added to this and dispersed in the molecules for 5 minutes using a homomixer type M. Furthermore, DBcAMP
3 g was added, and an ointment was then prepared in the same manner as in the control example.
実施例５
実施例４のデキストリンの代りにα−シクロデキストリ
ン４０ｇを添加して、軟膏を製した。Example 5 In place of the dextrin in Example 4, 40 g of α-cyclodextrin was added to prepare an ointment.
実施例６
ポリエチレングリコール６００ ５６ｇ、ポリエチレン
グリコール４０００４０ｇを対照例と同様に溶解した。Example 6 56 g of polyethylene glycol 600 and 40 g of polyethylene glycol 4000 were dissolved in the same manner as in the control example.
これに乾燥水酸化アルミニウムゲルＩｇを添加し、Ｔ、
に、ホモミキサーＭ型で５分間子分に分散した。更にＤ
ＢｃＡＭＰ ３ｇを添加して、以後対照例と同様にし
て軟膏を製した。Dry aluminum hydroxide gel Ig was added to this, T,
Then, the mixture was dispersed into the molecules using a homomixer type M for 5 minutes. Further D
After adding 3 g of BcAMP, an ointment was prepared in the same manner as in the control example.
実施例７
ポリエチレングリコール５００ ５６ｇ、ポリエチレン
グリコール４０００３０ｇを対照例と同様に溶解した。Example 7 56 g of polyethylene glycol 500 and 30 g of polyethylene glycol 4000 were dissolved in the same manner as in the control example.
これにデキストリンＬＯｇおよび乾燥水酸化アルミニウ
ムゲル１ｇを添加し、Ｔ；に、ホモミキサーＭ型で５分
間子分に分散した。更にＤＢｃＡＭＰ ３ｇを添加し
て、以後対照例と同様にして軟膏を製した。Dextrin LOg and 1 g of dry aluminum hydroxide gel were added to this and dispersed in the molecules for 5 minutes using a homomixer type M. Further, 3 g of DBcAMP was added and an ointment was prepared in the same manner as in the control example.
実施例８
ポリエチレングリコール４００ ６７ｇ、ポリエチレン
グリコール４０００２８ｇを対照例と同様に溶解した。Example 8 67 g of polyethylene glycol 400 and 400,028 g of polyethylene glycol 400 were dissolved in the same manner as in the control example.
これにデキストリン１ｇおよび乾燥水酸化アルミニウム
ゲル１ｇを添加し、Ｔ、に、ホモミキサーＭ型で５分間
子分に分散した。更にＤＢｃＡＭＰ ３ｇを添加して
、以後対照例と同様にして軟膏を製した。To this was added 1 g of dextrin and 1 g of dry aluminum hydroxide gel, and the mixture was dispersed in a homomixer type M for 5 minutes. Further, 3 g of DBcAMP was added and an ointment was prepared in the same manner as in the control example.
実施例９
ポリエチレングリコール４００ ６７ｇ、ポリエチレン
グリコール４０００２６ｇを対照例と同様に溶解した。Example 9 67 g of polyethylene glycol 400 and 400,026 g of polyethylene glycol 400 were dissolved in the same manner as in the control example.
これにデキストリン３ｇおよび乾燥水酸化アルミニウム
ゲルＩｇを添加し、Ｔ、に、ホモミキサーＭ型で５分間
子分に分散した。更にＤＢｃＡＭＰ ３ｇを添加して
、以後対照例と同様にして軟膏を製した。To this was added 3 g of dextrin and Ig of dry aluminum hydroxide gel, and the mixture was dispersed in a homomixer type M for 5 minutes. Further, 3 g of DBcAMP was added and an ointment was prepared in the same manner as in the control example.
試験例
対照例および実施例１〜９で得られた軟膏をガラスビン
に充填し、５０℃の空気高温槽中で保存試験を実施した
。１力月後のＤＢｃＡＭＰの含量を液体クロマトグラム
法（Ｊｏｕｒｎａｌ ｏｆ ｃｈｒｏｍａｔｏｇｒａｐ
ｈｙｖｏｌ、２３８，４９５頁、１９８２年、参照）で
定量した。この結果を表１に示した。Test Examples The ointments obtained in the control example and Examples 1 to 9 were filled into glass bottles, and a storage test was conducted in a high temperature air bath at 50°C. The content of DBcAMP after 1 month was determined by liquid chromatography method (Journal of chromatography).
hyvol, 238, p. 495, 1982). The results are shown in Table 1.
表Ｉ ＤＢｃＡＭＰの安定性試験結果これらの結果よ
り、単に吸水性、乾燥性を有する基剤中にサイクリック
八Ｍ Ｐ ３に導体を溶解させた軟膏よりも糖類および
／または無機高分子を添加することによりサイクリック
ＡＭＰＪ導体の安定性が改善されることが分かり、本発
明の目的を達することが出来た。Table I Stability test results of DBcAMP Based on these results, sugars and/or inorganic polymers are added rather than an ointment in which a conductor is dissolved in cyclic 8M P3 in a base that simply has water absorption and drying properties. It was found that the stability of the cyclic AMPJ conductor was improved by this, and the object of the present invention was achieved.
Claims (1)
よび／または無機高分子を配合したことを特徴とするサ
イクリックＡＭＰ誘導体含有軟膏製剤。A cyclic AMP derivative-containing ointment preparation, which uses a water-absorbing and drying base, and contains a saccharide and/or an inorganic polymer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1077102A JP2971888B2 (en) | 1988-03-30 | 1989-03-29 | Ointment preparation |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63-77915 | 1988-03-30 | ||
| JP7791588 | 1988-03-30 | ||
| JP1077102A JP2971888B2 (en) | 1988-03-30 | 1989-03-29 | Ointment preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH021409A true JPH021409A (en) | 1990-01-05 |
| JP2971888B2 JP2971888B2 (en) | 1999-11-08 |
Family
ID=26418199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1077102A Expired - Lifetime JP2971888B2 (en) | 1988-03-30 | 1989-03-29 | Ointment preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2971888B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6223194B1 (en) | 1997-06-11 | 2001-04-24 | Nec Corporation | Adaptive filter, step size control method thereof, and record medium therefor |
-
1989
- 1989-03-29 JP JP1077102A patent/JP2971888B2/en not_active Expired - Lifetime
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6223194B1 (en) | 1997-06-11 | 2001-04-24 | Nec Corporation | Adaptive filter, step size control method thereof, and record medium therefor |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2971888B2 (en) | 1999-11-08 |
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