JPS5824409B2 - The best way to get started - Google Patents
The best way to get startedInfo
- Publication number
- JPS5824409B2 JPS5824409B2 JP12523575A JP12523575A JPS5824409B2 JP S5824409 B2 JPS5824409 B2 JP S5824409B2 JP 12523575 A JP12523575 A JP 12523575A JP 12523575 A JP12523575 A JP 12523575A JP S5824409 B2 JPS5824409 B2 JP S5824409B2
- Authority
- JP
- Japan
- Prior art keywords
- liquid
- binder
- powder
- amount
- case
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
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- 239000007788 liquid Substances 0.000 claims description 24
- 239000000843 powder Substances 0.000 claims description 18
- 239000011230 binding agent Substances 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 8
- 239000002245 particle Substances 0.000 claims description 8
- 239000013543 active substance Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 239000000463 material Substances 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 4
- 239000008298 dragée Substances 0.000 claims description 3
- 239000006185 dispersion Substances 0.000 description 12
- 229920003023 plastic Polymers 0.000 description 10
- 239000004033 plastic Substances 0.000 description 10
- 238000000576 coating method Methods 0.000 description 6
- 239000011248 coating agent Substances 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 239000000178 monomer Substances 0.000 description 5
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 4
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 239000008188 pellet Substances 0.000 description 4
- 239000007921 spray Substances 0.000 description 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 4
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- -1 diethylamino- Chemical class 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 229920002554 vinyl polymer Polymers 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 238000010410 dusting Methods 0.000 description 2
- 125000004185 ester group Chemical group 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 238000009495 sugar coating Methods 0.000 description 2
- 229920001567 vinyl ester resin Polymers 0.000 description 2
- OEPOKWHJYJXUGD-UHFFFAOYSA-N 2-(3-phenylmethoxyphenyl)-1,3-thiazole-4-carbaldehyde Chemical compound O=CC1=CSC(C=2C=C(OCC=3C=CC=CC=3)C=CC=2)=N1 OEPOKWHJYJXUGD-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 229920000178 Acrylic resin Polymers 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- BZHJMEDXRYGGRV-UHFFFAOYSA-N Vinyl chloride Chemical compound ClC=C BZHJMEDXRYGGRV-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 125000005396 acrylic acid ester group Chemical group 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 150000001805 chlorine compounds Chemical class 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 description 1
- 125000005265 dialkylamine group Chemical group 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 239000003844 drug implant Substances 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 125000005397 methacrylic acid ester group Chemical group 0.000 description 1
- UIDWQGRXEVDFCA-XCVCLJGOSA-N nifurtoinol Chemical compound O=C1N(CO)C(=O)CN1\N=C\C1=CC=C([N+]([O-])=O)O1 UIDWQGRXEVDFCA-XCVCLJGOSA-N 0.000 description 1
- 229960002592 nifurtoinol Drugs 0.000 description 1
- 150000002825 nitriles Chemical class 0.000 description 1
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000013076 target substance Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
- A61J3/06—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of pills, lozenges or dragees
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Preparation (AREA)
- Medical Preparation Storing Or Oral Administration Devices (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Description
【発明の詳細な説明】
原発明（特許第８９３５８３号（特公昭５２−１８２４
８号公報））は、揮発性液体および作用物質含有粉末（
その場合これら成分の一方は該液体に可溶な結合剤を含
有する）を、糖衣釜中で運動する種物質に交互に施し、
その場合それぞれ添加される液体の量を、引続き添加す
べき粉末の量の臨界液体吸収量に一致させることによる
小球状薬剤の製造方法に関する。[Detailed description of the invention] Original invention (Patent No. 893583 (Japanese Patent Publication No. 52-1824)
No. 8)) is a volatile liquid and active substance-containing powder (
in which one of these components contains a binder soluble in the liquid) are applied alternately to the seed material moving in a dragee;
The present invention relates to a process for the production of medicaments in the form of small spheres, by adjusting the amount of liquid added in each case to the critical liquid uptake of the amount of powder to be subsequently added.
この場合゛°臨界液体量′”とは、これに所属する粉末
量で粘着性でも崩壊性でもないコンパウンドを形成する
ような液体量を表わす。In this case, the term ``critical liquid quantity'' refers to the liquid quantity such that the powder quantity to which it belongs forms a compound that is neither sticky nor disintegrating.
全てのそれぞれの場合の゛臨界液体量″を簡単かつ正確
に測定することができる多数の試験法は、原発明明細書
に記載されている。A large number of test methods are described in the original patent specification which make it possible to simply and accurately determine the "critical liquid quantity" in every respective case.
一般に、臨界液体吸収量は、粉末１００ｙ′に対し液体
約１０〜３０グである。Generally, the critical liquid uptake is about 10 to 30 grams of liquid per 100 y' of powder.
原発明により使用すべき液体の代表例は、ポリビニルピ
ロリドンまたはポリビニルアルコールのアルコール水溶
液である。A typical example of a liquid to be used according to the invention is an alcoholic aqueous solution of polyvinylpyrrolidone or polyvinylalcohol.
２つの成分から前述の割合で形成されたコンパウンドは
、これから常用の種物質上に中間乾燥することなく小球
状薬剤を形成することができるような強度を有する。The compound formed from the two components in the proportions described above has such strength that it can be formed into drug spherules on conventional seed materials without intermediate drying.
所望の最終粒径に達した際に初めて乾燥工程を接続する
。Only when the desired final particle size is reached is a drying step carried out.
ところで、原発明による方法には、結合剤が使用される
揮発性液体に可溶であることは根本的に重要なことでは
ないことが判明した。However, it has been found that for the process according to the invention it is not of fundamental importance that the binder is soluble in the volatile liquid used.
原発明明細書に記載された他の実施例によれば、結合剤
は水中に分散せる粒子の形で存在する。According to another embodiment described in the original specification, the binder is present in the form of particles that are dispersed in water.
従って、成層のため粉末成分と一緒に使用される液体は
、プラスチック水性分散液である。The liquid used together with the powder component for layering is therefore a plastic aqueous dispersion.
有利に、プラスチック分散液は、固形物含量５〜５０重
量％のものが使用される。Preferably, plastic dispersions with a solids content of 5 to 50% by weight are used.
その場合臨界液体吸収量は結合剤溶液におけると同じく
、粉末１００ Ｐａり分散液１０〜３０グの程度の大き
さである。In this case, the critical liquid uptake, as in the binder solution, is of the order of magnitude of 100 to 30 g of dispersion per 100 Pa of powder.
分散液中に分散せるプラスチックの構造は、小球の製法
によるよりも強く、生体内での小球状薬剤の所望の挙動
により決定される。The structure of the plastic dispersed in the dispersion is determined by the desired behavior of the globular drug in vivo, rather than by the globule manufacturing method.
その作用物質をもっばら拡散により放出すべき小球状薬
剤には、アクリル酸またはメタクリル酸のエステル、ビ
ニルエステル、スチロール、塩化ビニルまたは他の非水
溶性モノマーのみから構成されていてもよい完全に非水
溶性のプラスチックの分散液が適当である。Globular drugs whose active substances are to be released primarily by diffusion include completely non-containing agents which may be composed solely of esters of acrylic or methacrylic acid, vinyl esters, styrene, vinyl chloride or other water-insoluble monomers. Dispersions of water-soluble plastics are suitable.
これに反し、小球状薬剤が、胃の酸性雰囲気中で、また
は腸の弱アルカリ性雰囲気中で溶解するかまたは少（と
も強く膨潤すべき場合は、親水基を有するプラスチック
の分散液が使用される。On the other hand, if the small spherical drug should dissolve in the acidic atmosphere of the stomach or in the slightly alkaline atmosphere of the intestine or swell slightly (but strongly), dispersions of plastics with hydrophilic groups are used. .
有利に、西ドイツ国特許明細書第２１３５０７３号に記
載されているような前記種類のプラスチック分散液が使
用される。Preference is given to using plastic dispersions of the type described in German Patent Specification No. 21 35 073.
これらプラスチックは、その１０〜５５重量％が、カル
ボキシル基および／またはモノアルキル−またはジアル
キルアミンエステル基を有するモノマーから構成されて
いる。These plastics are composed of 10 to 55% by weight of monomers having carboxyl groups and/or monoalkyl- or dialkylamine ester groups.
この群からの有利なモノマーは、アクリル酸およびメタ
クリル酸並びにそれらのジエチルアミノ−、ジメチルア
ミノ−またはブチルアミノエチルエステルである。Preferred monomers from this group are acrylic acid and methacrylic acid and their diethylamino-, dimethylamino- or butylaminoethyl esters.
該共重合体の残りの４５〜９０重量％は、他のビニルモ
ノマー、例えばアクリル酸またはメタクリル酸と脂肪族
アルコール、グリコールまたはグリセリンとのエステル
、並びに前記の酸のニトリルまたはアミド、ビニルエス
テル、塩化ビニル、塩化ビニリデン、オレフィン、スチ
ロール等である。The remaining 45-90% by weight of the copolymer comprises other vinyl monomers, such as esters of acrylic or methacrylic acid with aliphatic alcohols, glycols or glycerin, as well as nitriles or amides, vinyl esters, chlorides of the aforementioned acids. Vinyl, vinylidene chloride, olefin, styrene, etc.
プラスチック水分散液の高い固形分と同時に低粘度によ
り、結合剤溶液を使用した場合に可能であるよりも、結
合剤含量の着るしく高い小球状薬剤を製造することがで
きる。The high solids content and at the same time low viscosity of the aqueous plastic dispersion makes it possible to produce small spherical drugs with a significantly higher binder content than is possible using binder solutions.
このプラスチック含量は、出来上った小球状薬剤の重量
の１０％にまですることができる。This plastic content can be up to 10% of the weight of the finished drug pellets.
これにより、作用物質の放出を遅延させることが可能と
なる。This makes it possible to delay the release of the active substance.
本発明のもう１つの利点は、結合剤有機溶液を使用する
際すでに環境保護の理由からその回収が不可避である有
機溶剤を一緒に使用しないことである。Another advantage of the invention is that when using the binder organic solution, no organic solvents are used together, the recovery of which is already unavoidable for reasons of environmental protection.
該小球状薬剤は、自体公知の方法で、場合により作用物
質の放出に影響を与えることのできる付加的被覆を設け
、かつゼラチンカプセルに充填することができる。The drug spherules can be filled in gelatin capsules in a manner known per se, optionally with an additional coating that can influence the release of the active substance.
以下に本発明を実施例につき詳説する。The present invention will be explained in detail below using examples.
例１
糖衣釜中へ、粒径０．５〜０．８ ｍｍを有する穂高２
０ｋｇを装入する。Example 1 Hotaka 2 with particle size 0.5-0.8 mm into sugar coating pot
Charge 0 kg.
微粉砕せる乳糖混合物２２ｋｇを、散布粉末として使用
する。22 kg of the pulverized lactose mixture are used as dusting powder.
結合剤としては、メタクリル酸エステルとアクリル酸エ
ステルとの共重合体を主成分とするアクリル樹脂の５０
％分散液を使用する。As a binder, 50% of acrylic resin whose main component is a copolymer of methacrylic acid ester and acrylic acid ester is used.
% dispersion is used.
予備試験において、臨界液体吸収量として１４ｍ１／１
００グが得られた。In preliminary tests, the critical liquid absorption capacity was 14m1/1.
00g was obtained.
スプレーガンを使用し、分散液それぞれ０．２８１を、
釜中で回転する装入物上へ噴霧する。Using a spray gun, add 0.281 each of the dispersions,
Spray onto the rotating charge in the kettle.
その後直ちに、前記粉末混合物２ｋｇを、湿った装入物
上へ散布する。Immediately thereafter, 2 kg of the powder mixture are sprinkled onto the wet charge.
粉末が結晶ないしは粒により収容された後、装入物を再
び自由に回転させ、この工程を、散布混合物の全量が被
覆に使用されるまで繰返す。After the powder has been contained in the crystals or granules, the charge is allowed to rotate freely again and the process is repeated until the entire amount of the spreading mixture has been used for coating.
被覆が行なわれた後、こうして製造されたベレットを篩
上で篩別し、かつ乾燥型中で乾燥する。After coating has taken place, the pellets thus produced are screened on a sieve and dried in a drying mold.
この場合結合剤の分量は、散布せる粉末量に対し７％で
ある。In this case, the amount of binder is 7%, based on the amount of powder to be spread.
出来上ったペレットの収量はほぼ４２ｋｇである。The yield of finished pellets is approximately 42 kg.
例２
糖衣釜中へ、粒径０．５〜０．８ｍｍを有する穂高２０
ｋｇを装入する。Example 2 Hotaka 20 with particle size 0.5-0.8 mm into sugar coating pot
Charge kg.
乳糖、ヒドロキシメチルニトロフラントイン（６１％）
およびコリトン−２５より成る微粉砕混合物２２ゆを散
布粉末として使用する。Lactose, hydroxymethylnitrofurantoin (61%)
and Koliton-25 are used as the dusting powder.
結合剤としては、メタクリル酸とエチルアクリレートを
主成分とする３０％プラスチック水性分散液を使用する
。A 30% aqueous plastic dispersion based on methacrylic acid and ethyl acrylate is used as a binder.
予備試験において、限界液体吸収量としての所要量２１
■／１００ Ｐが得られた。In a preliminary test, the required amount 21 as the critical liquid absorption amount
■/100P was obtained.
スプレーガンを使用し、初めに分散液０．３２ｋｇを、
釜中で回転する装入物上へ噴霧する。Using a spray gun, first add 0.32 kg of the dispersion.
Spray onto the rotating charge in the kettle.
その後直ちに、前記の粉末混合物１．５ｋｙを湿った装
入物上へ散布する。Immediately thereafter, 1.5 ky of the powder mixture described above is sprinkled onto the wet charge.
粉末が結晶ないしは粒により収容された後、この装入物
を再び自由に回転させ、この工程を、散布混合物の全量
が被覆に使用されるまで繰り返す。After the powder has been contained in the crystals or granules, the charge is allowed to rotate freely again and the process is repeated until the entire amount of the spreading mixture has been used for coating.
５回の被覆後に、それぞれ添加すべき液体量は０．６３
１に、および粉末量は３ｋｙに増大する。After 5 coatings, the amount of liquid to be added each time is 0.63
1 and the powder amount increases to 3ky.
被覆が行なわれた後、こうして製造されたベレットを篩
上で篩別し、かつ乾燥型中で乾燥する。After coating has taken place, the pellets thus produced are screened on a sieve and dried in a drying mold.
この場合結合剤の分量は、散布せる粉末量に対し４．８
％である。In this case, the amount of binder is 4.8% of the amount of powder to be spread.
%.
出来上ったペレットの収量はほぼ４２ｋｇである。The yield of finished pellets is approximately 42 kg.
例３
例２による方法を繰返すが、但し装入物として穂高の代
りに、適当な造粒法により得られた、各粒子が粒径０．
５〜０．８ｍｍを有する種物質としての作用物質顆粒を
使用する。Example 3 The procedure according to Example 2 is repeated, except that instead of Hotaka as charge, each particle, obtained by a suitable granulation method, has a particle size of 0.
Active substance granules as seed material are used with a diameter of 5 to 0.8 mm.
臨界液体吸収量は２０ｒｒＬｌ／１００グ（固体物質）
である。Critical liquid absorption amount is 20rrLl/100g (solid material)
It is.
以下に本発明の実施態様を記載する。Embodiments of the invention are described below.
（１）水中に分散せる結合剤は、その１０〜５５重量％
が、カルボキシル基および／またはモノアルキルーまた
はジアルキルアミノアルキルエステル基を有するモノマ
ーから構成されているビニル重合体より成ることを特徴
とする特許請求の範囲記載の方法。(1) The binder to be dispersed in water is 10 to 55% by weight.
2. A method according to claim 1, characterized in that the vinyl polymer is composed of monomers having carboxyl groups and/or monoalkyl- or dialkylaminoalkyl ester groups.
追加の関係
原発明（特許第８９３５８３号（特公昭５２−１８２４
８号公報））は、揮発性液体および作用物質含有粉末（
その場合これら成分の一方は該液体に可溶な結合剤を含
有する）を、糖衣釜中で運動する種物質に交互に施すこ
とにより小球状薬剤を製造する方法に関するものである
が、本発明は原発明における揮発性液体に可溶な結合剤
に代え該結合剤を水に分散可能な粒子の形で存在させて
、原発明の目的物質である小球状薬剤を製造する方法の
発明であって、特許法第３１条第１号に該当するもので
ある。Additional related original invention (Patent No. 893583 (Japanese Patent Publication No. 52-1824)
No. 8)) is a volatile liquid and active substance-containing powder (
The present invention relates to a method for producing drug spherules by alternately applying medicaments (one of which contains a binder soluble in the liquid) to a seed material moving in a dragee. is an invention of a method for producing a small spherical drug, which is the target substance of the original invention, by using a binder in the form of water-dispersible particles instead of the volatile liquid-soluble binder in the original invention. Therefore, it falls under Article 31, Item 1 of the Patent Act.
Claims (1)
ら成分の一方は該液体に可溶な結合剤を含有する）を、
糖衣釜中で運動する種物質に交互に施し、その場合それ
ぞれ添加される液体の量を、引続き添加すべき粉末の量
の臨界液体吸収量に一致させることにより小球状薬剤を
製造するに当り、揮発性液体として水が使用され、かつ
結合剤が水中に分散せる粒子の形で使用されることを特
徴とする小球状薬剤の製法。1 a volatile liquid and an active substance-containing powder, in which case one of these components contains a binder soluble in said liquid,
In the production of medicaments in the form of small spheres by applying them alternately to a seed material moving in a dragee, the amount of liquid added in each case being matched to the critical liquid uptake of the amount of powder to be subsequently added, A process for the preparation of small spherical drugs, characterized in that water is used as volatile liquid and the binder is used in the form of particles dispersed in the water.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19742449384 DE2449384A1 (en) | 1974-10-17 | 1974-10-17 | METHOD OF MANUFACTURING MEDICINAL CONES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5163926A JPS5163926A (en) | 1976-06-02 |
| JPS5824409B2 true JPS5824409B2 (en) | 1983-05-20 |
Family
ID=5928494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP12523575A Expired JPS5824409B2 (en) | 1974-10-17 | 1975-10-17 | The best way to get started |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JPS5824409B2 (en) |
| AT (1) | AT342205B (en) |
| BE (1) | BE833953A (en) |
| DE (1) | DE2449384A1 (en) |
| FR (1) | FR2287898A2 (en) |
| GB (1) | GB1485229A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0558809U (en) * | 1992-10-22 | 1993-08-03 | 三菱自動車工業株式会社 | Engine oil return structure |
| KR20240030556A (en) * | 2022-08-31 | 2024-03-07 | 한국로봇융합연구원 | Pressing module and pipe joining robot |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AUPN327695A0 (en) * | 1995-05-30 | 1995-06-22 | Chemeq Pty. Limited | Chemotherapeutic compositions |
| KR20090037951A (en) | 2006-07-25 | 2009-04-16 | 교와 가부시키가이샤 | Sugar preparation and preparation method thereof |
-
1974
- 1974-10-17 DE DE19742449384 patent/DE2449384A1/en active Pending
-
1975
- 1975-07-16 AT AT552175A patent/AT342205B/en not_active IP Right Cessation
- 1975-09-02 FR FR7526923A patent/FR2287898A2/en active Granted
- 1975-09-29 BE BE160486A patent/BE833953A/en not_active IP Right Cessation
- 1975-10-17 GB GB4277075A patent/GB1485229A/en not_active Expired
- 1975-10-17 JP JP12523575A patent/JPS5824409B2/en not_active Expired
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0558809U (en) * | 1992-10-22 | 1993-08-03 | 三菱自動車工業株式会社 | Engine oil return structure |
| KR20240030556A (en) * | 2022-08-31 | 2024-03-07 | 한국로봇융합연구원 | Pressing module and pipe joining robot |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5163926A (en) | 1976-06-02 |
| AT342205B (en) | 1978-03-28 |
| BE833953A (en) | 1976-01-16 |
| FR2287898B2 (en) | 1979-01-19 |
| DE2449384A1 (en) | 1976-04-29 |
| FR2287898A2 (en) | 1976-05-14 |
| ATA552175A (en) | 1977-07-15 |
| GB1485229A (en) | 1977-09-08 |
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