JPS62262740A - Microcapsule or matrix granulated powder having wall film composed of shellac - Google Patents
Microcapsule or matrix granulated powder having wall film composed of shellacInfo
- Publication number
- JPS62262740A JPS62262740A JP10750386A JP10750386A JPS62262740A JP S62262740 A JPS62262740 A JP S62262740A JP 10750386 A JP10750386 A JP 10750386A JP 10750386 A JP10750386 A JP 10750386A JP S62262740 A JPS62262740 A JP S62262740A
- Authority
- JP
- Japan
- Prior art keywords
- shellac
- microcapsules
- microcapsule
- substance
- solution
- 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
- 239000003094 microcapsule Substances 0.000 title claims abstract description 46
- 229920001800 Shellac Polymers 0.000 title claims abstract description 31
- 239000004208 shellac Substances 0.000 title claims abstract description 31
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 title claims abstract description 31
- 229940113147 shellac Drugs 0.000 title claims abstract description 31
- 235000013874 shellac Nutrition 0.000 title claims abstract description 31
- 239000011159 matrix material Substances 0.000 title claims abstract description 14
- 239000000843 powder Substances 0.000 title abstract description 10
- 239000000463 material Substances 0.000 claims description 25
- 239000008187 granular material Substances 0.000 claims description 24
- 238000001694 spray drying Methods 0.000 claims description 24
- 239000000126 substance Substances 0.000 abstract description 23
- 239000003814 drug Substances 0.000 abstract description 22
- 229940079593 drug Drugs 0.000 abstract description 18
- 239000000243 solution Substances 0.000 abstract description 16
- 239000002245 particle Substances 0.000 abstract description 14
- 239000000049 pigment Substances 0.000 abstract description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 9
- 239000007864 aqueous solution Substances 0.000 abstract description 8
- 239000002537 cosmetic Substances 0.000 abstract description 8
- 239000011347 resin Substances 0.000 abstract description 5
- 229920005989 resin Polymers 0.000 abstract description 5
- 229920001187 thermosetting polymer Polymers 0.000 abstract description 4
- 239000003431 cross linking reagent Substances 0.000 abstract description 3
- 239000006185 dispersion Substances 0.000 abstract description 2
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 238000007796 conventional method Methods 0.000 abstract 1
- 239000011782 vitamin Substances 0.000 abstract 1
- 229940088594 vitamin Drugs 0.000 abstract 1
- 229930003231 vitamin Natural products 0.000 abstract 1
- 235000013343 vitamin Nutrition 0.000 abstract 1
- 150000003722 vitamin derivatives Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 description 25
- 239000010408 film Substances 0.000 description 14
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 10
- 210000004379 membrane Anatomy 0.000 description 10
- 239000012528 membrane Substances 0.000 description 10
- 239000003086 colorant Substances 0.000 description 9
- 239000012530 fluid Substances 0.000 description 9
- 239000011162 core material Substances 0.000 description 8
- 230000000968 intestinal effect Effects 0.000 description 7
- 238000004090 dissolution Methods 0.000 description 6
- 238000005469 granulation Methods 0.000 description 6
- 230000003179 granulation Effects 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 210000003491 skin Anatomy 0.000 description 6
- IRERQBUNZFJFGC-UHFFFAOYSA-L azure blue Chemical compound [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Al+3].[Al+3].[Al+3].[Al+3].[Al+3].[Al+3].[S-]S[S-].[O-][Si]([O-])([O-])[O-].[O-][Si]([O-])([O-])[O-].[O-][Si]([O-])([O-])[O-].[O-][Si]([O-])([O-])[O-].[O-][Si]([O-])([O-])[O-].[O-][Si]([O-])([O-])[O-] IRERQBUNZFJFGC-UHFFFAOYSA-L 0.000 description 5
- 238000010828 elution Methods 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 229960005489 paracetamol Drugs 0.000 description 5
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 239000010419 fine particle Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 238000005507 spraying Methods 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 230000002776 aggregation Effects 0.000 description 2
- 239000003905 agrochemical Substances 0.000 description 2
- 229960005070 ascorbic acid Drugs 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- 229960001948 caffeine Drugs 0.000 description 2
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000004040 coloring Methods 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 2
- 229960004172 pyridoxine hydrochloride Drugs 0.000 description 2
- 235000019171 pyridoxine hydrochloride Nutrition 0.000 description 2
- 239000011764 pyridoxine hydrochloride Substances 0.000 description 2
- 210000001732 sebaceous gland Anatomy 0.000 description 2
- 230000036559 skin health Effects 0.000 description 2
- 238000010998 test method Methods 0.000 description 2
- 235000013799 ultramarine blue Nutrition 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-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
- GVIRAXRGZUXHCI-UHFFFAOYSA-N 2-acetyloxycarbonylbenzoic acid Chemical compound CC(=O)OC(=O)C1=CC=CC=C1C(O)=O GVIRAXRGZUXHCI-UHFFFAOYSA-N 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
- 235000003255 Carthamus tinctorius Nutrition 0.000 description 1
- 244000020518 Carthamus tinctorius Species 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- RWSOTUBLDIXVET-UHFFFAOYSA-N Dihydrogen sulfide Chemical compound S RWSOTUBLDIXVET-UHFFFAOYSA-N 0.000 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 1
- 208000010201 Exanthema Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 238000012695 Interfacial polymerization Methods 0.000 description 1
- 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 1
- 235000019596 Masking bitterness Nutrition 0.000 description 1
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 206010040880 Skin irritation Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 230000000711 cancerogenic effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 201000005884 exanthem Diseases 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 235000013402 health food Nutrition 0.000 description 1
- 229910000037 hydrogen sulfide Inorganic materials 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 238000013095 identification testing Methods 0.000 description 1
- 239000003317 industrial substance Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000001023 inorganic pigment Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 239000000025 natural resin Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000012860 organic pigment Substances 0.000 description 1
- 230000002688 persistence Effects 0.000 description 1
- 239000008017 pharmaceutical colorant Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 238000005191 phase separation Methods 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 238000006116 polymerization reaction Methods 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 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
- 239000011148 porous material Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 235000021067 refined food Nutrition 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000000979 retarding effect Effects 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
- 239000011257 shell material Substances 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 239000012756 surface treatment agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 210000004243 sweat Anatomy 0.000 description 1
- 210000000106 sweat gland Anatomy 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- -1 trimesololmelamine Polymers 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
- B01J13/02—Making microcapsules or microballoons
Abstract
Description
【発明の詳細な説明】
〔イ〕 発明の目的
本発明は、天然の熱硬化性樹脂である、シエランクを壁
膜材として用い、噴霧乾燥造粒機によって得られること
を特徴とする新規なマイクロカプセル又は、マトリック
ス顆粒に関する。[Detailed Description of the Invention] [A] Object of the Invention The present invention provides a novel microorganism that uses Sierran, a natural thermosetting resin, as a wall film material and is obtained by a spray drying granulator. Concerning capsules or matrix granules.
「産業上の利用分野」
本発明による、マイクロカプセル又は、マトリックス顆
粒は、着色料（例えば、各種の有機及び無Ｉｍ顔料、タ
ール系色素、天然色素）、各種の医薬品、農薬、香料、
他の工業分野で用いられる薬剤のｍ安定化、粉体特性の
改良などに有効である。"Industrial Application Fields" The microcapsules or matrix granules according to the present invention can be used for coloring agents (e.g., various organic and Im-free pigments, tar-based pigments, natural pigments), various pharmaceuticals, agricultural chemicals, fragrances,
It is effective for stabilizing drugs used in other industrial fields and improving powder properties.
１従来の技術」
／エラツクを用い、これを壁膜材となし、噴霧乾燥造粒
機を用いて、薬物（薬剤）をマイクロカプセル又は、マ
トリックス顆粒となした例は、他に見当らない。1. Prior Art There is no other example in which a drug (drug) is made into microcapsules or matrix granules by using Elac as a wall material and using a spray drying granulator.
（１）ンエラックに関する公知技術の調査シェラツクは
、天然樹脂中、唯一の熱硬化性樹脂として知られ、耐油
性、耐水性の被膜形成能があり、その被膜は光沢の付与
、防湿、腸溶性コーティングの目的で、錠剤や、糖衣錠
の表面処理剤として、古くから利用されてきている。(1) Survey of known technologies related to Shellac Shellac is known as the only thermosetting resin among natural resins, and has the ability to form oil- and water-resistant films, and its films can provide gloss, moisture-proofing, and enteric coating. It has been used for a long time as a surface treatment agent for tablets and sugar-coated tablets.
（２）噴霧乾燥造粒機によるマイクロカプセルの製造に
関する公知技術の調査
従来から、噴霧乾燥造粒機を用いたマイクロカプセル化
法は、公知であり、例えば、それを示す刊行物としては
、次表（第１表）のごとくの方法が知られている。(2) Investigation of known techniques related to the production of microcapsules using a spray-drying granulator The microencapsulation method using a spray-drying granulator has been known, for example, the following publications show it: The methods shown in Table (Table 1) are known.
マイクロカプセル化法としては、第１表に示すごとく、
噴霧乾燥造粒法の他、界面重合法、イン１′；イツ重合
法、液中乾燥法、相分離法、コアセルベーンコン法、界
面析出法などが知られている。As the microencapsulation method, as shown in Table 1,
In addition to the spray-drying granulation method, interfacial polymerization methods, in-1' polymerization methods, submerged drying methods, phase separation methods, core cell vane-con method, interfacial precipitation methods, and the like are known.
（第１表）
噴霧乾燥造粒機を用いたマイクロカプセル比例１尭明が
解決しようとする問題点」
本発明は、噴霧乾燥造粒法として知られる手段をもとに
、各種の薬物の安定性の向上と除放性を賦与した、微細
なマイクロカプセルまたは、マトリ／ラス顆粒を得るこ
とにある。(Table 1) Proportion of microcapsules using a spray-drying granulator 1 Problems to be solved by Kyomei The present invention is based on a means known as the spray-drying granulation method, to stabilize various drugs. The object of the present invention is to obtain fine microcapsules or matrix/ras granules that have improved properties and sustained release properties.
すなわち、各種の工業的な分野に用いられる物質（成分
）のなかには、きまざまな製剤化の欠点があり、原体の
状態で、即、必要となす目的分野への利用が困難なもの
が多い。In other words, many of the substances (ingredients) used in various industrial fields have various drawbacks in formulation, making it difficult to immediately use them in their original form for the desired purpose. .
例えば、医薬品の製剤化における薬物、あるいは、化粧
料などに用いられる着色料などについてみれば、次の様
な事柄に直面する。For example, when we look at drugs used in pharmaceutical formulations or colorants used in cosmetics, we are faced with the following problems.
（１）化粧品に用いられる着色料の例
一般的に有機、無機顔料は、耐光性、耐溶媒性が強い、
しかし、その処方中の系のｐＨによって、安定性を欠く
ものがある０例えば、群青などでは、酸性領域では非常
に不安定である。一方、法定色素であるタール系色素で
は、耐久性に乏しく、油溶剤等によって滲みを生じ易い
、又、皮膚や粘膜に接触した場合、吸着諮れ易く、洗浄
による除去が難しい、さらに、皮膚の汗腺、皮脂腺、毛
穴などをふさぎ、皮膚の健康上、好ましくないような場
合もある。(1) Examples of colorants used in cosmetics Generally, organic and inorganic pigments have strong light resistance and solvent resistance.
However, depending on the pH of the system in which it is formulated, it may lack stability; for example, ultramarine blue is very unstable in an acidic region. On the other hand, tar-based pigments, which are legal pigments, have poor durability and are easily smeared by oil solvents, etc., and when they come into contact with the skin or mucous membranes, they tend to be adsorbed and are difficult to remove by washing. It can block sweat glands, sebaceous glands, and pores, which can be unfavorable for skin health.
又、天然色素は、安全性の高いものが多く、又、各種の
薬理的効果が期待できるものが多い反面、耐光性、耐熱
性、ｐＨ１金属イオンなどの影響を受は易いものが多い
。Moreover, while many natural pigments are highly safe and can be expected to have various pharmacological effects, many of them are easily affected by light resistance, heat resistance, pH 1 metal ions, etc.
（２）医薬品に用いられる薬物の側
限薬品における、薬物のマイクロカプセル化も、前記と
同様にして、耐光性、耐溶媒性、処方中のｐＨ１服用後
の胃又は、腸内における溶解性の調節、きらに、製剤化
後の安定性の向上、製剤化移れた製品の小型化のためな
どの手段として用いられてきた。(2) In the same way as mentioned above, microencapsulation of drugs in side-limiting drugs used in pharmaceuticals also improves light resistance, solvent resistance, and solubility in the stomach or intestines after taking the drug at a pH of 1 in the formulation. It has been used as a means for regulating, controlling, improving stability after formulation, and reducing the size of formulated products.
そして、前項で知られた公知なマイクロカプセル化法に
は、それぞれに、一長一短があり、例えば、製造コスト
の面からは、製造工程が簡単な噴霧乾燥造粒機を用いた
マイクロカプセル化法は、他のマイクロカプセル化法に
比べて有利であるとされてきた。Each of the known microencapsulation methods mentioned in the previous section has its advantages and disadvantages.For example, from the viewpoint of manufacturing costs, the microencapsulation method using a spray drying granulator, which has a simple manufacturing process, , has been shown to be advantageous compared to other microencapsulation methods.
しかし、どの公知なマイクロカプセル化法にあっても、
壁膜材として利用できるものは、それぞれの操作によっ
て、ごく限定きれると共に、さらに芯物質の利用目的に
適合した壁膜材となると、さらに限られていた。However, with any known microencapsulation method,
The materials that can be used as wall membrane materials are very limited depending on the respective operations, and the wall membrane materials that are suitable for the purpose of using the core substance are even more limited.
薬物のマイクロカプセルを、噴霧乾燥造粒法を用いて製
造する場合にも、例外ではない、つまり、噴霧乾燥造粒
機を用いた、マイクロカプセル化法においても、壁膜物
の選択が重要な鍵となる。There is no exception when manufacturing drug microcapsules using the spray drying granulation method.In other words, even in the microencapsulation method using a spray drying granulation machine, the selection of the wall material is important. This is the key.
従来、ｑ！霧乾燥造粒機を用いて得られるマイクロカプ
セル化に当って、それに用いられる公知な壁膜材として
は、ゼラチン、アルギン酸、乳糖、デキストリン、β−
サイクロデキストリン、ポリビニルアルコール、トリメ
ゾロールメラミン、ポリビニールピロリドン、メチルセ
ルロース、セルロースアセチルフタレート、ヒドロキシ
プロピルセルロース、アクリル酸系樹脂（オイドラギッ
トなど）が知られている。Conventionally, q! Known wall materials used for microcapsules obtained using a fog drying granulator include gelatin, alginic acid, lactose, dextrin, and β-
Known examples include cyclodextrin, polyvinyl alcohol, trimesololmelamine, polyvinylpyrrolidone, methylcellulose, cellulose acetyl phthalate, hydroxypropylcellulose, and acrylic acid resins (Eudragit, etc.).
しかし、これらの壁膜材にも、それぞれ一長一短があっ
た。又、これらの壁膜材を用いて得られたマイクロカプ
セルも、その芯物質が、目的とする用途（分野）に適合
しないものが多かった。However, each of these wall membrane materials has its advantages and disadvantages. Furthermore, many of the microcapsules obtained using these wall membrane materials have core substances that are not suitable for the intended use (field).
したがって、本発明が解決しようとする問題点は、より
広範囲な薬物（物質）を、最も操作性の良い、噴霧乾燥
造粒機を用いて、マイクロカプセルとなすに怒り、それ
に最適な、壁膜材を発掘することである。Therefore, the problem to be solved by the present invention is to process a wider range of drugs (substances) into microcapsules using the spray drying granulator, which is the most convenient to operate, and which is ideal for making wall membranes. It is to excavate the material.
ｃ口〕 発明の構成
本発明は、公知なマイクロカプセル化法の−っである、
噴霧乾燥造粒機を用い、広範囲な粉体物質を芯となし、
これを、シェラツクで被覆させた、微細なマイクロカプ
セル又は、マトリックス顆粒となすことにある。[c] Structure of the invention The present invention is a known microencapsulation method.
Using a spray drying granulator, a wide range of powder materials are used as the core,
The purpose is to form this into fine microcapsules or matrix granules coated with shellac.
「問題点を解決するための手段、
以下に、本発明を具体的に開示するために、実施例等に
より説明する。``Means for Solving the Problems'' Below, in order to specifically disclose the present invention, the present invention will be explained using Examples.
「実施例−１４着色料のマイクロカプセル化例（Ａ）
水性シェラツクの５％含有水溶液１１に、ベニバナ抽出
カーサミン２００ｇを分散きせ、公知な噴霧乾燥造粒装
置を用い、通常の操作により、その造粒物を得た。"Example 14 Microencapsulation example of colorant (A) 200 g of safflower extracted cursamine was dispersed in 5% aqueous shellac solution 11. Granules were obtained.
得られた造粒物の粒度分布は、第１ｖＩ！Ｊに示すごと
くであった。The particle size distribution of the obtained granules was 1vI! It was as shown in J.
すなわち、粒子の径は、アトマイザ−回転数の増加にと
もなって、微細化きれること。That is, the diameter of the particles becomes finer as the atomizer rotation speed increases.
また、その得られた微細粒の壁膜は、シェラツクで構成
きれ、しかも、その膜は透明な皮膜を形成する。Moreover, the obtained wall film of fine grains can be composed of shellac, and moreover, the film forms a transparent film.
（Ｂ）
水性シェラツクの２％、５％、１０％を含有きせた水溶
液１２を、それぞれに、あらかじめ製しておき、その各
水溶液中に、１０ミクロン以下の微粉砕した群青を、攪
拌しながら分散させ、噴霧乾燥造粒機を用いて、アトマ
イザ−回転数２５゜０００ｒｐｍで造粒する。(B) Prepare aqueous solutions 12 containing 2%, 5%, and 10% of aqueous shellac in advance, and add finely ground ultramarine of 10 microns or less into each aqueous solution while stirring. The mixture is dispersed and granulated using a spray drying granulator at an atomizer rotation speed of 25°,000 rpm.
得られた、群青のマイクロカプセルは、そのいずれもが
、５０ミクロン以下の微粒子として得られる。The obtained ultramarine microcapsules are all obtained as fine particles of 50 microns or less.
尚、得られた群青のマイクロカプセルには、化粧品厘料
基準の群青の確認試験法に言う、希塩酸の中に添カロし
ても、硫化水素の臭いの発生は認められなかった。Furthermore, even when the ultramarine microcapsules obtained were added to dilute hydrochloric acid, which is specified in the ultramarine blue identification test method specified in cosmetics standards, no hydrogen sulfide odor was observed.
（Ｃ）
前記（Ａ）〜（Ｂ）の実施例に準拠し、シェラツクの水
溶液中に、次（第２表）に示す、各色素類を分散し、噴
霧乾燥造粒機を用いて行なうと、そのほとんどの物質を
、微細なマイクロカプセルとすることが出来た。造粒に
当っては、壁膜材として用いたシェラ７りの水溶液中の
濃度と、アトマイザ−回転数を任意にｉｔすることによ
り、芯物質の利用分野（目的）に応じた、マイクロカプ
セルを、製造することが出来る。但し、シェラツクの水
溶液中（系）で、溶解する物質は、マトリックス顆粒と
して得られる。(C) Based on the examples (A) to (B) above, each coloring matter shown below (Table 2) is dispersed in an aqueous solution of shellac and carried out using a spray drying granulator. , most of the substances could be made into fine microcapsules. During granulation, microcapsules can be formed according to the field of use (purpose) of the core material by arbitrarily adjusting the concentration of Shella 7 used as a wall membrane material in the aqueous solution and the rotation speed of the atomizer. , can be manufactured. However, in the aqueous solution (system) of shellac, the substances dissolved are obtained as matrix granules.
（第２表） 実施例Ｃで用いた芯物質
１実施例−２」医薬品ｗ、ｙ＋物質の例（Ｄ）
アルカリ剤を用いて可溶化した、水溶性シェラツクの５
％含有溶液１１に、２００メツシユ以下に、微粉砕した
、アセトアミノフェン１５０ｇを分散させ、噴霧乾燥造
粒機により造粒する。(Table 2) Core substance used in Example C 1 Example-2 Example of drug w, y + substance (D) Water-soluble shellac 5 solubilized using an alkaline agent
% containing solution 11 is dispersed with 150 g of finely pulverized acetaminophen to 200 mesh or less, and granulated using a spray drying granulator.
この際、噴霧時のアトマイザ−回転速度を、１ｏ、ｏ
ｏ ｏ、１５，０００．２５．ＯＯＯｒｐｍと変化させ
、それぞれに対応した場合のマイクロカプセル化された
、アセトアミノフェンについて、その粒度分布状態をみ
ると、第２図に示すごとくとなった。At this time, the atomizer rotation speed during spraying was set to 1o, o
o o, 15,000.25. When looking at the particle size distribution of microencapsulated acetaminophen in the case of varying OOO rpm, the results are as shown in FIG. 2.
すなわち、回転のスピードの上昇は、これにともなって
、平均粒子径が小きくなる。That is, as the rotation speed increases, the average particle diameter becomes smaller.
一方、上記の方法により得られた、アセトアミノフェン
のマイクロカプセルについて、人工胃液（ｐＨ１−２）
、人工腸液（ｐＨ７，２）により、その溶出特性につい
て試験すれば、第３図に示すごとくの結果が得られ、溶
出速度の遅延効果が著明であることがわかった。On the other hand, regarding acetaminophen microcapsules obtained by the above method, artificial gastric fluid (pH 1-2)
When the dissolution characteristics were tested using artificial intestinal fluid (pH 7.2), the results shown in FIG. 3 were obtained, and it was found that the effect of retarding the dissolution rate was remarkable.
（第３図の試験条件）
試験液二日周・第１液、第２液
液量：９００ｕＱ
液ｉＥ１：３７℃±０．５
バスケット回転速度：１１００ｒｐ
きらに、この効果は、人工胃液中における方が、とくに
優れており、これは、シェランクが耐酸性を有している
ことと一致し、マイクロカプセル壁膜材として、有利な
ものである。(Test conditions shown in Figure 3) Test liquid 2-day cycle, 1st and 2nd liquid volume: 900uQ Liquid iE1: 37℃±0.5 Basket rotation speed: 1100rp This is consistent with the fact that shellanc has acid resistance, and is advantageous as a microcapsule wall material.
（Ｅ）
アルカリで可溶化きせ、ｐＨを７．０に再ＭＪ１４整し
た、水性シェラツクの２．２％（イ）、５．０％（ロ）
、８．６％（ハ）の各々の溶液１２中に、２００メツシ
ユ以下に微粉化したカフェイン２００ｇを分散させ、噴
霧乾燥造粒機によって造粒する。(E) 2.2% (a) and 5.0% (b) of aqueous shellac solubilized with alkali and adjusted to pH 7.0 by MJ14.
, 8.6% (c), 200 g of caffeine pulverized to 200 mesh or less is dispersed in each of the solutions 12 and granulated using a spray drying granulator.
その効果を求めるために、例えば、噴霧時のアトマイザ
−回転速度は、２０．ＯＯＯｒｐｍに設定し、噴霧乾燥
造粒条件としては、入ロ温度■１５０°Ｃ１出ロ温度−
１００°Ｃで、上記の実施例（Ｅ）に採用したシェラ／
りの濃度に対応した、溶出率（人工腸液ｐＨ７，２にお
ける）を求めてみると、第４図に示したごとくとなり、
得られたマイクロカプセルの膜のｆｋ（率）に対応して
、溶出時間を変化きせることが出来る。In order to determine the effect, for example, the atomizer rotation speed during spraying is set at 20. OOOrpm, and the spray drying granulation conditions are as follows: Input temperature: 150°C1 Output temperature: -
At 100°C, Sierra/
When calculating the dissolution rate (at artificial intestinal fluid pH 7.2) corresponding to the concentration of
The elution time can be changed depending on the fk (rate) of the obtained microcapsule membrane.
つまり、第４図中の符号からは、水性シェラツク溶液（
イ）の濃度では、得られたマイクロカプセルの壁膜が１
０％、（ロ）では２０％、（ハ）では３０％と、厚くな
り、これにともなって、腸溶液中での薬物の放出速度も
、次第に遅延されることとなる。In other words, from the symbols in Fig. 4, the aqueous shellac solution (
At the concentration of b), the wall membrane of the obtained microcapsules is 1
The thickness increases to 0%, 20% in (b), and 30% in (c), and accordingly, the release rate of the drug in the intestinal solution is gradually delayed.
尚、第４図の試験法は、第３図における条件下で、人工
腸液（日周・第２液）を用いて実施した。The test method shown in FIG. 4 was carried out under the conditions shown in FIG. 3 using artificial intestinal fluid (diurnal/second fluid).
（Ｆ）
前記の実施例−１の（Ａ）又は（Ｂ）、ｔらに、実施例
−２の（Ｄ）や、（Ｅ）に準じて、次の医薬品原料物質
（第３表）について、マイクロカプセルを得たが、その
いずれもが、微細なマイクロカプセルとして、効率的に
出来ることがわかった。尚、第３表中には、ンエラック
の水溶液（系）の中で、溶解する物質も含まれるが、こ
れらはマトリックス顆粒として得られる。(F) Regarding the following pharmaceutical raw materials (Table 3) according to (A) or (B), t, etc. of Example-1, and (D) or (E) of Example-2, , microcapsules were obtained, and it was found that both of them can be efficiently produced as fine microcapsules. Table 3 also includes substances that dissolve in the aqueous solution (system) of NELAC, but these are obtained as matrix granules.
（第３表） 実施例Ｆで用いた芯物質
（Ｇ）
アルカリ剤を用いて可溶化した、水溶性シェラ／りの１
０％水溶液１２に、塩酸ピリドキシン１００ｇを加えて
溶解させ、噴霧乾燥造粒機を用いて、アトマイザ−回転
速度１５．ＯＯＯｒｐｍにて造粒する。(Table 3) Core material (G) used in Example F Water-soluble Sierra/Rino 1 solubilized using an alkaline agent
Add 100 g of pyridoxine hydrochloride to 0% aqueous solution 12, dissolve it, and use a spray drying granulator at an atomizer rotation speed of 15. Granulate at OOO rpm.
得られた造粒物は、平均粒子径１００ミクロン程のマト
リックス造粒物として得られた。The obtained granules were obtained as matrix granules with an average particle diameter of about 100 microns.
（Ｈ）
シェラツクの１０％エタノール溶液１１！に、８０メ７
シュ以下１００メツシュ以上に篩過した、アスコルビン
酸２００ｇを加えて分散許せ、噴霧乾燥造粒機を用いて
造粒する。(H) 10% ethanol solution of shellac 11! To, 80 meters 7
Add 200 g of ascorbic acid, which has been sieved to 100 mesh or more, to allow dispersion, and granulate using a spray drying granulator.
得られた造粒物は、２５０ミクロンの平均粒子径を持つ
、球状マイクロカプセルとして得られた。The resulting granules were obtained as spherical microcapsules with an average particle diameter of 250 microns.
第５図は、上記（Ｇ）、第６図は、上記（Ｈ）で示芒れ
る、それぞれの造粒物の溶出！ｉ（率）についての結果
を示すグラフであるが、それぞれ、未処理薬物と対比し
て、明らかに溶出時間が延長されることである。Figure 5 shows the elution of the respective granules shown in (G) above, and Figure 6 shows the elution of the respective granules shown in (H) above. Graph showing the results for i (rate), respectively, the elution time is clearly prolonged compared to the untreated drug.
なお、第５〜６図で示きれる、その試験法（条件）は、
次の通りである。The test method (conditions) shown in Figures 5 and 6 are as follows:
It is as follows.
（第５図の試験条件）
溶出液：６局・第２液（ｐＨ７，２）
液 量：９００謔
液 温：３７℃±０．５
バスケット回転数：１０１００ｒ
ｐ第６［１の試験条件）
溶出液：精製水
液 量 ： ９００餞
液 温 ； ３７℃± ０．５
バスケット回転数：１１００ｒｐ
〔ハ〕 発明の効果
本発明は、粉体物質の多くを、シェラツクを壁膜材とな
す、噴霧乾燥造粒機を用いた、マイクロカプセルにある
。(Test conditions in Figure 5) Eluate: 6 stations, 2nd solution (pH 7, 2) Liquid volume: 900 ml Temperature: 37°C ± 0.5 Basket rotation speed: 10100 r P No. 6 [Test conditions in 1] Eluent: Purified water Amount: 900% solution Temperature: 37°C ± 0.5 Basket rotation speed: 1100 rp [C] Effects of the invention The present invention provides a method for spraying most of the powder material using shellac as the wall material. It is in microcapsules using a dry granulator.
すなわち、シェラツク溶液中に、分散する性質を有する
、あらゆる粉体物質を、シェラツクで被覆させた、微細
な、球状マイクロカプセル又は、マトリックス顆粒を得
ることにある。That is, the object is to obtain fine, spherical microcapsules or matrix granules coated with shellac of any powder substance that has the property of being dispersed in a shellac solution.
本発明で示すごとく、その操作は、他のマイクロカプセ
ル化法に比べ、操作性に優れ、大幅なコストダウンが可
能であり、広範囲の物質に利用出来ることである。As shown in the present invention, its operation is superior to other microencapsulation methods, allows for significant cost reduction, and can be used for a wide range of substances.
とくに、最終的に得られた、マイクロカプセルは、透明
なシェラｙり膜で形成されており、しかも真球状で得ら
れることである。In particular, the finally obtained microcapsules are formed of a transparent Shelley film and are perfectly spherical.
このために、とくに色素類では、その色素自体の有する
色彩を、損なうことなく、シェラツク特有の光沢膜性を
発揮してくれることである。For this reason, pigments in particular exhibit the glossy film properties unique to shellac without impairing the color of the pigment itself.
もちろん、用いた壁膜材であるシェラツタの溶液中で、
溶解する物質も造粒できるが、この場合では、得られる
造粒物が、マトリ７クス状の球状細粒として得られるわ
けである。Of course, in a solution of Shera ivy, which is the wall material used,
Dissolved substances can also be granulated, but in this case, the resulting granules are obtained as matrix-like spherical fine particles.
つまり、末法によれば、シェラツク溶液中で分散浮れる
粉体物質であれば、そのすべてが真球状°マイクロカプ
セルとして得られ、シェラツクの溶液中で溶解するよう
な物質では、マイクロカプセルとはならないが、球状の
マトリックス顆粒とすることが出来る。In other words, according to the powder method, any powder substance that can be dispersed and floated in a shellac solution will be obtained as true spherical microcapsules, and any substance that dissolves in a shellac solution will not form microcapsules. However, it can be made into spherical matrix granules.
本発明による、シェラツクを壁膜材となす、マイクロカ
プセルの用途は、そのシェラツクの特性である、優れた
耐水性、耐油性を、充分に発揮することと、その透明な
薄い膜の形成にある。The purpose of the microcapsules using shellac as a wall material according to the present invention is to fully exhibit the excellent water resistance and oil resistance, which are the characteristics of shellac, and to form a transparent thin film. .
これらの特性は、例えば、化粧品等に用いる着色料など
には、最適なものとなる。These properties are optimal for colorants used in cosmetics and the like.
すなわち、一般に、着色料は、色素の均一性、隠ぺい力
、皮膚への吸着力などの性能を高めるために、微粉細化
が求められるも、その一方では、微粉が進むにつれて、
その粉体粒子間において、二次的な凝集が発生し易くな
る。又、微粉体とすれば、それによって、皮脂腺、毛根
、皮膚表面組織への付着性が向上するも、その残留性が
高まり、皮膚の健康上、好ましくない結果を与える場合
が、懸念きれるが、本発明により、シェラツクを壁膜材
となした１色料（色素類）であれば、このような問題点
も改良きれ、着色料としての本来の役目が発揮されるこ
ととなる。In other words, in general, colorants are required to be finely divided in order to improve performance such as pigment uniformity, hiding power, and adsorption power to the skin.
Secondary aggregation is likely to occur between the powder particles. In addition, if it is made into a fine powder, it improves its adhesion to sebaceous glands, hair roots, and skin surface tissues, but there is a concern that it may increase its persistence and cause unfavorable results in terms of skin health. According to the present invention, if a single colorant (pigment) using shellac as a wall film material is used, such problems can be overcome and the original role as a colorant can be fulfilled.
一方、透明な薄い壁膜を形成し、マイクロカプセルに応
用される壁膜としては、この他に、例えば、ポリアクリ
ル酸ソーダなどの利用が開発されている。しかし、充分
な耐水性、耐油性を求めるには、架橋剤を併用するなど
の操作を必要とするのに対して、シェラツクの場合は、
熱硬化性樹脂であることから、架橋剤を必要とせず、耐
水、耐油性の壁膜を形成できる点から、そのメリットは
大きいものがある。On the other hand, as a wall film that forms a transparent thin wall film and is applied to microcapsules, other materials such as sodium polyacrylate have been developed. However, in order to obtain sufficient water resistance and oil resistance, operations such as the combined use of crosslinking agents are required, whereas in the case of shellac,
Since it is a thermosetting resin, it has great advantages in that it does not require a crosslinking agent and can form a water- and oil-resistant wall film.
皮膚に対する安全性の見地からすれば、これまで、相当
の着色料が、皮膚刺激性、あるいは、色素カブレなどを
起こす原因とされ、タール系色素類のなかには、色素自
体の色彩は良好であっても、それが皮膚に直接的に塗布
されると、これが浸透して、アレルギー作用、発癌作用
を引き起こす原因となるものも多く、そのために使用が
禁止きれたもの、あるいは、使用範囲を限定きれて用い
る必要のあるものも多いが、本発明によるシェラ／りを
壁膜材として、マイクロカプセルとなしたものであれば
、表皮上にあって、耐水性、耐油性を発揮し、皮詣、汗
等の影響を受けても、芯の内容物質である着色料は、シ
ェラ／りの膜内に、溶出することなく、目的となす、色
彩効果のみを発揮することとなり、その安全性の点でも
充分なものとなる。From the viewpoint of safety for the skin, a considerable amount of colorants have been considered to cause skin irritation or pigment rash, and some tar-based pigments have a good coloring themselves. However, when it is applied directly to the skin, it penetrates and causes allergic and carcinogenic effects, and for this reason, its use has been prohibited or its range of use has been limited. There are many things that need to be used, but if the shell material according to the present invention is used as a wall material and is made into microcapsules, it will be on the epidermis and exhibit water and oil resistance, and will be resistant to skin damage and sweat. Even under the influence of such factors, the coloring agent contained in the core will not be eluted into the shella/li film, and will only produce the desired color effect, and from a safety point of view. It will be sufficient.
従来、噴霧乾燥造粒機を用いた、マイクロカプセルを製
造するに当って、各種の壁膜材が知られてきたが、皮膚
（肌）に直接に触れるような条件下で用いられる、化粧
品や医薬部外品などの製剤にも、安心して用いられるも
のとなると、ごく限られており、その限られた壁膜材で
は、本発明のごとく、多種多様な物質を、すべて、マイ
クロカプセルとなし、実用に供することは出来ないでい
たわけである。Conventionally, various wall membrane materials have been known for manufacturing microcapsules using a spray drying granulator, but they are not suitable for use in cosmetics or other products that are used under conditions where they come in direct contact with the skin. There are only a limited number of wall membrane materials that can be safely used in preparations such as quasi-drugs, and as in the present invention, a wide variety of substances can be contained in microcapsules. However, it was not possible to put it into practical use.
本発明によれば、実施例で示した物質に限定する必要は
なく、シェラツク溶液中で分散出来る物質であれば、す
へてを、マイクロカプセルとすることが可能である。According to the present invention, there is no need to limit the materials to those shown in the examples, and any material that can be dispersed in a shellac solution can be used as microcapsules.
しかも、従来の公知な噴霧乾燥造粒機を用いて製造出来
、又、そのために、とくに、特別の複雑な操作も不要に
して、非常に微細なマイクロカプセルが得られることは
、製法上からも大変有利である。Moreover, it can be produced using a conventional, well-known spray drying granulator, and therefore, very fine microcapsules can be obtained without any special complicated operations. It is very advantageous.
本発明によるマイクロカプセルの平均粒子径は、５〜７
０ミクロン程度の微細な粒子であり、さらに、その物質
を内包したマイクロカプセルは、粒子間での凝集が起こ
らない。The average particle size of the microcapsules according to the present invention is 5 to 7.
They are fine particles of about 0 microns, and furthermore, microcapsules containing the substance do not cause aggregation between particles.
又、本発明によって得られたマイクロカプセルは、水や
油に対して良好な分散性を発揮するために、例えば、化
粧品の各種形態の処方中にも任意に配合出来る。Furthermore, since the microcapsules obtained according to the present invention exhibit good dispersibility in water and oil, they can be optionally incorporated into the formulation of various forms of cosmetics, for example.
一方、医薬品の製剤化に当っては、従来の顆粒を、さら
に小型化し、しかもシェラツク被膜の耐水、耐油性能を
充分発揮して、安定性が非常に向上すると共に、形状が
均一で、しかも光沢性があり、苦味等を遮へいし、無味
、無臭の薬剤として製造出来るなどの利点がある。On the other hand, when formulating pharmaceuticals, conventional granules can be further miniaturized, and the shellac coating can fully demonstrate the water and oil resistance properties, greatly improving stability, uniform shape, and gloss. It has the advantages of being resistant to bitterness, masking bitterness, etc., and being able to be produced as a tasteless and odorless drug.
メ、流動性も良好であり、硬カプセルへの充填、あるい
は、膜厚をコントロールすれば、直接、高圧打錠機にか
けて、錠剤となすことも出来る。さらに、他の薬剤との
併用において、従来、製剤化上、配合禁忌とされた物質
（薬品類）とも、本発明によるマイクロカプセルを用い
ることにより、混合（併用処方）出来ることなど、その
もたらす効果は太きいものがある。Furthermore, it has good fluidity and can be filled into hard capsules or, if the film thickness is controlled, can be made into tablets by directly applying it to a high-pressure tablet machine. Furthermore, when used in combination with other drugs, the microcapsules of the present invention can be used to mix (combined prescription) with substances (drugs) that have traditionally been contraindicated for formulation. There are some thick ones.
本発明によれば、製造法が簡単であり、コスト的には、
従来の単なる造粒物（ｗｔ粒）と、はぼ同様にして安価
で出来るために、本発明によるマイクロカプセル化され
た物質は、医薬品や化粧品の分野のみならず、加工食品
（健康食品を含む）、農薬、香料、工業薬品（有機、無
機を含む）、その他、各種の工業分野において、利用出
来ることが大きな特徴である。According to the present invention, the manufacturing method is simple, and in terms of cost,
The microencapsulated substance of the present invention can be used not only in the fields of pharmaceuticals and cosmetics, but also in processed foods (including health foods) because it can be produced at low cost and in the same way as conventional simple granules (wt granules). ), agricultural chemicals, fragrances, industrial chemicals (including organic and inorganic), and other various industrial fields.
第１図は、実施例−１の（Ａ）で得られた、カーサミン
の粒子径と、噴霧乾燥造粒機のアトマイザ−回転速度と
の関係においてみた、粒度分布の状態を示すグラフ。
第２図は、実施例−２の（Ｄ）で得られた、アセトアミ
ノフェンのマイクロカプセルの粒子径と、噴霧乾燥造粒
機のアトマイザ−回転速度との関係においてみた、粒度
分布の状態を示すグラフ、第３図は、実施例−２の（Ｄ
）において、アトマイザ−回転速度を、１５．ＯＯＯｒ
ｐｍに設定し、１％もれたアセトアミノフェンのマイク
ロカプセルの、人工胃液中、人工腸液中における溶出状
態について、示したグラフ。
第４図は、実施例−２の（Ｅ）で得られた、カフェイン
のマイクロカプセルの、人工腸液中における、溶出状態
を示したグラフ。
第５図は、実施例−２の（Ｇ）で得られた、塩酸ピリド
キシンのマトリックス造粒物の、人工腸液中における、
溶出状態について、示したグラフ。
第６図は、実施例−２の（Ｈ）で得られた、アスコルビ
ン酸のマイクロカプセルの、精製水中における溶出状態
を示すグラフ。
ｉ′ｏｐＪｌシ
第４図
第５図
ｉ６図
ｉｎ ／Ｊｔｐ ４０ ｍ？９ａ（幻ｒ続補市占（
方式） ６％式％（
］FIG. 1 is a graph showing the state of the particle size distribution as seen in the relationship between the particle size of Carsamine obtained in Example 1 (A) and the atomizer rotation speed of the spray drying granulator. Figure 2 shows the state of the particle size distribution as seen in the relationship between the particle size of the acetaminophen microcapsules obtained in Example 2 (D) and the atomizer rotation speed of the spray drying granulator. The graph shown in FIG. 3 is the (D
), the atomizer rotation speed is set to 15. OOOr
Graph showing the dissolution state of acetaminophen microcapsules set at pm and leaking 1% in simulated gastric fluid and simulated intestinal fluid. FIG. 4 is a graph showing the dissolution state of the caffeine microcapsules obtained in Example-2 (E) in artificial intestinal fluid. FIG. 5 shows the matrix granules of pyridoxine hydrochloride obtained in Example 2 (G) in artificial intestinal fluid.
A graph showing the elution state. FIG. 6 is a graph showing the dissolution state of ascorbic acid microcapsules obtained in Example-2 (H) in purified water. i'opJl しFigure 4Figure 5Figure i6Figure in /Jtp 40 m? 9a (phantom r continuation supplementary city fortune telling)
Method) 6% formula% ( )
Claims (1)
得られることを特徴とする、マイクロカプセル又はマト
リックス顆粒。(1) Microcapsules or matrix granules, characterized in that the wall material is made of shellac and is obtained by a spray drying granulator.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10750386A JPS62262740A (en) | 1986-05-09 | 1986-05-09 | Microcapsule or matrix granulated powder having wall film composed of shellac |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10750386A JPS62262740A (en) | 1986-05-09 | 1986-05-09 | Microcapsule or matrix granulated powder having wall film composed of shellac |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS62262740A true JPS62262740A (en) | 1987-11-14 |
Family
ID=14460858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10750386A Pending JPS62262740A (en) | 1986-05-09 | 1986-05-09 | Microcapsule or matrix granulated powder having wall film composed of shellac |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS62262740A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0605933A1 (en) * | 1992-12-24 | 1994-07-13 | PHARMATECH GmbH | Process for preparing pseudo-latices and micro- or nanoparticles and compositions containing them |
| FR2825293A1 (en) * | 2001-06-05 | 2002-12-06 | Coletica | WATER-INSOLUBLE SOLID PARTICLES TREATED, PREPARATION AND USE |
| JP2009055850A (en) * | 2007-08-31 | 2009-03-19 | T Hasegawa Co Ltd | Sustained release dried material |
-
1986
- 1986-05-09 JP JP10750386A patent/JPS62262740A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0605933A1 (en) * | 1992-12-24 | 1994-07-13 | PHARMATECH GmbH | Process for preparing pseudo-latices and micro- or nanoparticles and compositions containing them |
| FR2825293A1 (en) * | 2001-06-05 | 2002-12-06 | Coletica | WATER-INSOLUBLE SOLID PARTICLES TREATED, PREPARATION AND USE |
| US6548170B2 (en) | 2001-06-05 | 2003-04-15 | Coletica | Treated water-insoluble solid particles, preparation and use |
| JP2009055850A (en) * | 2007-08-31 | 2009-03-19 | T Hasegawa Co Ltd | Sustained release dried material |
| JP4732408B2 (en) * | 2007-08-31 | 2011-07-27 | 長谷川香料株式会社 | Sustained release dry matter |
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