JP2018184388A - Solid composition - Google Patents
Solid composition Download PDFInfo
- Publication number
- JP2018184388A JP2018184388A JP2018078107A JP2018078107A JP2018184388A JP 2018184388 A JP2018184388 A JP 2018184388A JP 2018078107 A JP2018078107 A JP 2018078107A JP 2018078107 A JP2018078107 A JP 2018078107A JP 2018184388 A JP2018184388 A JP 2018184388A
- Authority
- JP
- Japan
- Prior art keywords
- solid composition
- tablet
- powder
- cassis extract
- extract
- 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
- 239000008247 solid mixture Substances 0.000 title claims abstract description 32
- 239000003826 tablet Substances 0.000 claims abstract description 29
- 235000001466 Ribes nigrum Nutrition 0.000 claims abstract description 25
- 241001312569 Ribes nigrum Species 0.000 claims abstract description 25
- 239000000284 extract Substances 0.000 claims abstract description 25
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims abstract description 16
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims abstract description 16
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims abstract description 16
- 229920002678 cellulose Polymers 0.000 claims abstract description 11
- 239000001913 cellulose Substances 0.000 claims abstract description 11
- 239000008187 granular material Substances 0.000 claims abstract description 5
- 239000002775 capsule Substances 0.000 claims abstract description 4
- 238000002156 mixing Methods 0.000 claims abstract description 4
- 239000006187 pill Substances 0.000 claims abstract description 4
- 239000000843 powder Substances 0.000 claims description 21
- 238000007906 compression Methods 0.000 claims description 12
- 230000006835 compression Effects 0.000 claims description 12
- DATAGRPVKZEWHA-YFKPBYRVSA-N N(5)-ethyl-L-glutamine Chemical compound CCNC(=O)CC[C@H]([NH3+])C([O-])=O DATAGRPVKZEWHA-YFKPBYRVSA-N 0.000 claims description 9
- CBOJBBMQJBVCMW-BTVCFUMJSA-N (2r,3r,4s,5r)-2-amino-3,4,5,6-tetrahydroxyhexanal;hydrochloride Chemical compound Cl.O=C[C@H](N)[C@@H](O)[C@H](O)[C@H](O)CO CBOJBBMQJBVCMW-BTVCFUMJSA-N 0.000 claims description 4
- GGTYBZJRPHEQDG-WCCKRBBISA-N (2s)-2,5-diaminopentanoic acid hydrochloride Chemical compound Cl.NCCC[C@H](N)C(O)=O GGTYBZJRPHEQDG-WCCKRBBISA-N 0.000 claims description 4
- 229960001911 glucosamine hydrochloride Drugs 0.000 claims description 4
- 238000003475 lamination Methods 0.000 claims description 4
- 229940026510 theanine Drugs 0.000 claims description 3
- 229960003244 ornithine hydrochloride Drugs 0.000 claims description 2
- 235000013305 food Nutrition 0.000 abstract description 8
- 239000003814 drug Substances 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 4
- 239000007910 chewable tablet Substances 0.000 abstract description 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract description 2
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 229940068682 chewable tablet Drugs 0.000 abstract 1
- 238000005187 foaming Methods 0.000 abstract 1
- 210000000214 mouth Anatomy 0.000 abstract 1
- 229940127557 pharmaceutical product Drugs 0.000 abstract 1
- 229940023488 pill Drugs 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- 239000002245 particle Substances 0.000 description 5
- 239000011230 binding agent Substances 0.000 description 4
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 3
- 239000011575 calcium Substances 0.000 description 3
- 229910052791 calcium Inorganic materials 0.000 description 3
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 3
- 235000013539 calcium stearate Nutrition 0.000 description 3
- 239000008116 calcium stearate Substances 0.000 description 3
- 239000007884 disintegrant Substances 0.000 description 3
- 229910052500 inorganic mineral Inorganic materials 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 239000011707 mineral Substances 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 241000196324 Embryophyta Species 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- 235000001537 Ribes X gardonianum Nutrition 0.000 description 2
- 235000001535 Ribes X utile Nutrition 0.000 description 2
- 235000016919 Ribes petraeum Nutrition 0.000 description 2
- 244000281247 Ribes rubrum Species 0.000 description 2
- 235000002355 Ribes spicatum Nutrition 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 229940024606 amino acid Drugs 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- VEVZSMAEJFVWIL-UHFFFAOYSA-O cyanidin cation Chemical compound [O+]=1C2=CC(O)=CC(O)=C2C=C(O)C=1C1=CC=C(O)C(O)=C1 VEVZSMAEJFVWIL-UHFFFAOYSA-O 0.000 description 2
- 235000013399 edible fruits Nutrition 0.000 description 2
- -1 fluidizers Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 150000002337 glycosamines Chemical class 0.000 description 2
- 235000010755 mineral Nutrition 0.000 description 2
- 239000007901 soft capsule Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 description 1
- TWCMVXMQHSVIOJ-UHFFFAOYSA-N Aglycone of yadanzioside D Natural products COC(=O)C12OCC34C(CC5C(=CC(O)C(O)C5(C)C3C(O)C1O)C)OC(=O)C(OC(=O)C)C24 TWCMVXMQHSVIOJ-UHFFFAOYSA-N 0.000 description 1
- PLMKQQMDOMTZGG-UHFFFAOYSA-N Astrantiagenin E-methylester Natural products CC12CCC(O)C(C)(CO)C1CCC1(C)C2CC=C2C3CC(C)(C)CCC3(C(=O)OC)CCC21C PLMKQQMDOMTZGG-UHFFFAOYSA-N 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- GCPYCNBGGPHOBD-UHFFFAOYSA-N Delphinidin Natural products OC1=Cc2c(O)cc(O)cc2OC1=C3C=C(O)C(=O)C(=C3)O GCPYCNBGGPHOBD-UHFFFAOYSA-N 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 1
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 description 1
- DATAGRPVKZEWHA-UHFFFAOYSA-N L-gamma-glutamyl-n-ethylamine Natural products CCNC(=O)CCC(N)C(O)=O DATAGRPVKZEWHA-UHFFFAOYSA-N 0.000 description 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 description 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 description 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 description 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 description 1
- OVRNDRQMDRJTHS-UHFFFAOYSA-N N-acelyl-D-glucosamine Natural products CC(=O)NC1C(O)OC(CO)C(O)C1O OVRNDRQMDRJTHS-UHFFFAOYSA-N 0.000 description 1
- OVRNDRQMDRJTHS-FMDGEEDCSA-N N-acetyl-beta-D-glucosamine Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O OVRNDRQMDRJTHS-FMDGEEDCSA-N 0.000 description 1
- MBLBDJOUHNCFQT-LXGUWJNJSA-N N-acetylglucosamine Natural products CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO MBLBDJOUHNCFQT-LXGUWJNJSA-N 0.000 description 1
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 description 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 1
- BUGBHKTXTAQXES-UHFFFAOYSA-N Selenium Chemical compound [Se] BUGBHKTXTAQXES-UHFFFAOYSA-N 0.000 description 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
- 235000010208 anthocyanin Nutrition 0.000 description 1
- 229930002877 anthocyanin Natural products 0.000 description 1
- 239000004410 anthocyanin Substances 0.000 description 1
- 150000004636 anthocyanins Chemical class 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 229950008138 carmellose Drugs 0.000 description 1
- 229960002173 citrulline Drugs 0.000 description 1
- 235000013477 citrulline Nutrition 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 235000007336 cyanidin Nutrition 0.000 description 1
- 235000007242 delphinidin Nutrition 0.000 description 1
- FFNDMZIBVDSQFI-UHFFFAOYSA-N delphinidin chloride Chemical compound [Cl-].[O+]=1C2=CC(O)=CC(O)=C2C=C(O)C=1C1=CC(O)=C(O)C(O)=C1 FFNDMZIBVDSQFI-UHFFFAOYSA-N 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000007938 effervescent tablet Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 229960002442 glucosamine Drugs 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- PFOARMALXZGCHY-UHFFFAOYSA-N homoegonol Natural products C1=C(OC)C(OC)=CC=C1C1=CC2=CC(CCCO)=CC(OC)=C2O1 PFOARMALXZGCHY-UHFFFAOYSA-N 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 229960000310 isoleucine Drugs 0.000 description 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 description 1
- 229960003136 leucine Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229950006780 n-acetylglucosamine Drugs 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 229960003104 ornithine Drugs 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000000419 plant extract Substances 0.000 description 1
- 150000008442 polyphenolic compounds Chemical class 0.000 description 1
- 235000013824 polyphenols Nutrition 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229910052711 selenium Inorganic materials 0.000 description 1
- 239000011669 selenium Substances 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- 229960004295 valine Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
Landscapes
- Coloring Foods And Improving Nutritive Qualities (AREA)
- General Preparation And Processing Of Foods (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
本発明は、カシス抽出物及びヒドロキシプロピルセルロースを配合した固形組成物に関し、医薬品、医薬部外品及び食品等の分野において利用され得る。 The present invention relates to a solid composition containing a cassis extract and hydroxypropylcellulose, and can be used in the fields of pharmaceuticals, quasi drugs and foods.
カシス抽出物は、スグリ属の植物であるカシスの果実から抽出・精製された粉末である。ポリフェノール成分、特に色素成分であるアントシアニンを多く含み、アグリコンとしてはデルフィニジン及びシアニジンを多く含有する。ビタミンCも多く含み、その他にもビタミンAやビタミンE、カルシウムや鉄などのビタミン・ミネラル類なども含む。アイケアや血流改善に関する作用が報告されており、広い利用が期待できる植物抽出物である。カシス抽出物の製剤化にあたり、一般的には、賦形剤、結合剤、崩壊剤、滑沢剤、矯味剤、pH調整剤等の種々の添加剤が用いられており、ソフトカプセル剤（特許文献１参照）や内服液剤（特許文献２参照）など複数の製剤が考案されている。 Cassis extract is a powder extracted and purified from the fruits of Cassis, a plant of the genus Currant. It contains a large amount of polyphenol component, especially anthocyanin, which is a pigment component, and aglycone contains a large amount of delphinidin and cyanidin. It contains a lot of vitamin C, and also contains vitamins A and E, vitamins and minerals such as calcium and iron. It is a plant extract that has been reported to be effective for eye care and blood flow improvement and can be widely used. In the formulation of cassis extract, various additives such as excipients, binders, disintegrants, lubricants, corrigents, pH adjusters are generally used, and soft capsules (patent document 1) and internal use liquids (see Patent Document 2) have been devised.
ヒドロキシプロピルセルロースは主に錠剤や顆粒剤等の固形製剤を製造する際に使用される結合剤の一種である。粒子同士の結合力を高めるために使用されるが、粒子同士の結合力が不足したまま固形製剤化すると、例えば、打錠機にて製錠する際にキャッピングやラミネーションといった打錠障害が生じてしまい、錠剤が得られず、或いは錠剤を得られても充分な硬度を有しないため、包装・流通の過程で錠剤の割れや欠けなどを引き起こし、商品性の低下を招きかねない。したがって、カシス抽出物の製剤化においても、ヒドロキシプロピルセルロースは、カシス抽出物の粒子同士の結合力を高めるために、或いはカシス抽出物と他の圧縮成形性の悪い成分の粒子同士の結合力を高めるために有用である。 Hydroxypropyl cellulose is a kind of binder mainly used when producing solid preparations such as tablets and granules. It is used to increase the bonding force between particles, but if a solid preparation is made with insufficient bonding force between particles, for example, tableting troubles such as capping and lamination occur when tableting with a tableting machine. In other words, tablets cannot be obtained, or even if tablets are obtained, they do not have sufficient hardness, which may cause breakage or chipping of the tablets during packaging and distribution, leading to a decrease in commercial properties. Therefore, even in the formulation of a cassis extract, hydroxypropyl cellulose increases the binding force between the particles of the cassis extract or the binding force between the particles of the cassis extract and other components having poor compression moldability. Useful for enhancing.
しかしながら、カシス抽出物と組み合わせた際に生じる課題についてはこれまで知られていない。 However, the problems that occur when combined with cassis extract are not known so far.
本発明者らはカシス抽出物の製剤化にあたり種々検討していたところ、カシス抽出物とヒドロキシプロピルセルロースを組み合わせた製剤は崩壊時間が長く、崩壊性に課題があるという知見を得た。従って、本発明の課題は、崩壊性を確保したカシス抽出物及びヒドロキシプロピルセルロース含有固形組成物を提供することにある。 The inventors of the present invention have made various studies in preparing a cassis extract, and have found that a combination of a cassis extract and hydroxypropylcellulose has a long disintegration time and has a problem in disintegration. Therefore, the subject of this invention is providing the cassis extract and the hydroxypropyl cellulose containing solid composition which ensured disintegration.
本発明者らは、上記課題を解決するために鋭意検討した結果、カシス抽出物、ヒドロキシプロピルセルロース、及び結晶セルロースを配合した錠剤は、崩壊時間が短いことを見出し、本発明を完成するに至った。 As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that a tablet containing cassis extract, hydroxypropyl cellulose, and crystalline cellulose has a short disintegration time, and completed the present invention. It was.
かかる知見により得られた本発明の態様は次のとおりである。
（１）カシス抽出物、ヒドロキシプロピルセルロース及び結晶セルロースを含有することを特徴とする固形組成物、
（２）結晶セルロースの配合量が固形組成物全体に対して５〜９０質量％である（１）に記載の固形組成物、
（３）さらに、グルコサミン塩酸塩、テアニン、オルニチン塩酸塩からなる群から選ばれる少なくとも１種を含むことを特徴とする（１）又は（２）に記載の固形組成物、
（４）さらに、圧縮成形性の悪い粉末を含む（１）又は（２）に記載の固形組成物であって、圧縮成形性の悪い粉末が、該粉末のみを圧縮成形し錠剤にした際にキャッピング又はラミネーションを生じる粉末であるか、引張破断強度が４Ｎ／ｍｍ２以下の粉末のいずれかである、固形組成物、
（５）錠剤、カプセル剤、顆粒剤、又は丸剤の形態である（１）〜（４）のいずれかに記載の固形組成物、
である。
The embodiments of the present invention obtained from such findings are as follows.
(1) A solid composition comprising a cassis extract, hydroxypropyl cellulose and crystalline cellulose;
(2) The solid composition according to (1), wherein the blending amount of crystalline cellulose is 5 to 90% by mass with respect to the entire solid composition,
(3) The solid composition according to (1) or (2), further comprising at least one selected from the group consisting of glucosamine hydrochloride, theanine, ornithine hydrochloride,
(4) The solid composition according to (1) or (2), further comprising a powder having poor compression moldability, wherein the powder having poor compression moldability is compressed only into the powder to form a tablet. A solid composition that is either a powder that causes capping or lamination, or a powder having a tensile strength at break of 4 N / mm 2 or less,
(5) The solid composition according to any one of (1) to (4), which is in the form of a tablet, capsule, granule, or pill,
It is.
本発明により、崩壊性が確保されたカシス抽出物及びヒドロキシプロピルセルロース含有固形組成物を提供することが可能となる。 According to the present invention, it is possible to provide a cassis extract and a hydroxypropylcellulose-containing solid composition in which disintegration is ensured.
本発明におけるカシス抽出物は、スグリ属の植物であるカシスの果実から抽出・精製された粉末であり、アイケアや血流改善等の目的で使用されている。本発明では、何れのカシス抽出物を用いてもよく、製法等について特に制限はないが、水及び／又はエタノールなどの有機溶媒で抽出して得られる抽出物の他に、市販品を使用することもできる 。カシス抽出物の含有量は特に限定されないが、固形組成物全体に対して、通常、５〜８０質量％、好ましくは１０〜７０質量％、より好ましくは２０〜６０質量％である。 The cassis extract in the present invention is a powder extracted and purified from the fruits of cassis, a plant of the genus Currant, and is used for purposes such as eye care and blood flow improvement. In the present invention, any cassis extract may be used, and the production method is not particularly limited, but a commercially available product is used in addition to the extract obtained by extraction with water and / or an organic solvent such as ethanol. You can also Although content of a cassis extract is not specifically limited, It is 5-80 mass% normally with respect to the whole solid composition, Preferably it is 10-70 mass%, More preferably, it is 20-60 mass%.
本発明におけるヒドロキシプロピルセルロースは、結合剤として公知のものである。ヒドロキシプロピルセルロースの含有量は、特に限定されないが、固形組成物全体に対して、通常、３〜３０質量％、好ましくは５〜３０質量％、より好ましくは５〜２０質量％である。 本発明における結晶セルロースは、賦形剤として公知のものである。結晶セルロースの含有量は、特に限定されないが、固形組成物全体に対して、通常、５〜９０質量％、好ましくは５〜８０質量％、より好ましくは５〜７０質量％である。 The hydroxypropyl cellulose in the present invention is known as a binder. The content of hydroxypropyl cellulose is not particularly limited, but is usually 3 to 30% by mass, preferably 5 to 30% by mass, and more preferably 5 to 20% by mass with respect to the entire solid composition. The crystalline cellulose in the present invention is known as an excipient. Although content of crystalline cellulose is not specifically limited, Usually, it is 5-90 mass% with respect to the whole solid composition, Preferably it is 5-80 mass%, More preferably, it is 5-70 mass%.
本発明にはカシス抽出物、ヒドロキシプロピルセルロース、結晶セルロースの他に圧縮成形性の悪い粉体を配合することができる。圧縮成形性の悪い粉体とは、単発式打錠機にて該粉体２００ｍｇのみを、打錠圧１５ｋＮ、圧縮時間９０秒間で成形し、錠径８ｍｍの錠剤とする際にキャッピング又はラミネーションを起こす粉末であるか、又は錠剤とした際の引張破断強度が、４Ｎ／ｍｍ２以下、好ましくは２Ｎ／ｍｍ２以下、より好ましくは１Ｎ／ｍｍ２以下となる粉末である。圧縮成形性の悪い粉体の含有量は、特に限定されないが、固形組成物全体に対して、通常、５〜８５質量％、好ましくは１０〜８０質量％、より好ましくは２５〜７５質量％である。なお、引張破断強度は次式で表される。錠剤の厚み及び錠剤が破壊された際の荷重の測定は、マイクロメータ及び硬度計を用いて行うことができる。 In the present invention, in addition to the cassis extract, hydroxypropyl cellulose, and crystalline cellulose, a powder having poor compression moldability can be blended. A powder with poor compression moldability means capping or lamination when only 200 mg of the powder is molded with a tableting pressure of 15 kN and a compression time of 90 seconds using a single-punch tableting machine to form tablets with a tablet diameter of 8 mm. It is a powder that wakes up or has a tensile strength at break of 4 N / mm 2 or less, preferably 2 N / mm 2 or less, more preferably 1 N / mm 2 or less. The content of the powder having poor compression moldability is not particularly limited, but is usually 5 to 85% by mass, preferably 10 to 80% by mass, and more preferably 25 to 75% by mass with respect to the entire solid composition. is there. The tensile strength at break is expressed by the following formula. The thickness of the tablet and the load when the tablet is broken can be measured using a micrometer and a hardness meter.
本発明の圧縮成形性の悪い粉末としては、粒子間の結合力が低いものであり、例えば、アミノ糖、アミノ酸、ミネラルなどが挙げられる。より具体的には、アミノ糖としては、グルコサミン、N-アセチルグルコサミン、アミノ酸としては、バリン、ロイシン、イソロイシン、テアニン、オルニチン、シトルリン、ミネラルとしては、カルシウム、セレン、そしてそれらの塩などが挙げられる。 The powder having poor compression moldability of the present invention has a low bonding force between particles, and examples thereof include amino sugars, amino acids, and minerals. More specifically, amino sugars include glucosamine, N-acetylglucosamine, amino acids include valine, leucine, isoleucine, theanine, ornithine, citrulline, minerals include calcium, selenium, and salts thereof. .
本発明の固形組成物は、例えば、医薬品、医薬部外品、食品などに幅広く利用することができる固形組成物であり、例えば、医薬製剤、医薬部外品製剤、特定保健用食品、栄養機能食品、特別用途食品、機能性表示食品、健康補助食品（サプリメント）、又は食品用製剤であり得る。 The solid composition of the present invention is a solid composition that can be widely used for, for example, pharmaceuticals, quasi drugs, foods, etc., for example, pharmaceutical preparations, quasi drugs, food for specified health use, nutritional function It may be a food, a special-purpose food, a functional label food, a health supplement (supplement), or a food preparation.
本発明の固形組成物は、本発明の効果を損なわない範囲でその他の成分を配合できる。例えば、賦形剤、滑沢剤、結合剤、崩壊剤、流動化剤、分散剤、コーティング剤等を配合し、さらに必要に応じて、抗酸化剤、着色剤、香料、矯味剤、保存剤、ｐＨ調整剤等を配合することができる。 The solid composition of this invention can mix | blend another component in the range which does not impair the effect of this invention. For example, excipients, lubricants, binders, disintegrants, fluidizers, dispersants, coating agents, etc. are blended, and if necessary, antioxidants, coloring agents, fragrances, flavoring agents, preservatives , PH adjusting agents and the like can be blended.
本発明の固形組成物の形態は特に制限されず、通常使用され得る任意の剤形をとることができる。例えば、錠剤（素錠、口腔内速崩壊錠、咀嚼可能錠、発泡錠、トローチ剤、コーティング錠などを含む）、カプセル剤（ソフトカプセル剤、ハードカプセル剤）、顆粒剤、丸剤などとして提供することができる。 The form of the solid composition of the present invention is not particularly limited, and can take any dosage form that can be usually used. For example, providing as tablets (including uncoated tablets, intraoral quick disintegrating tablets, chewable tablets, effervescent tablets, troches, coated tablets, etc.), capsules (soft capsules, hard capsules), granules, pills, etc. Can do.
本発明の固形組成物は、当該技術分野における慣用の方法をそのまま又は適宜応用して製造することができる。例えば、カシス抽出物、ヒドロキシプロピルセルロース、結晶セルロース及び任意の崩壊剤、滑沢剤を混合した後、圧縮成形することで錠剤とすることができる。 The solid composition of the present invention can be produced by applying a conventional method in the technical field as it is or appropriately. For example, a cassis extract, hydroxypropyl cellulose, crystalline cellulose, an optional disintegrant, and a lubricant are mixed, and then compressed into a tablet.
以下に、実施例、比較例を挙げ、本発明をさらに詳細に説明するが、本発明は以下に限定されるものではない。 Hereinafter, the present invention will be described in more detail with reference to Examples and Comparative Examples, but the present invention is not limited to the following.
（実施例１〜８及び比較例１〜５）
表１〜表３に記載の組成となるように各成分を秤量し、ステアリン酸カルシウムを除く成分を混合・篩過した。その後、ステアリン酸カルシウムを合わせ、再度篩過し、打錠用粉体とした。得られた打錠用粉体を単発式打錠機にて打錠し、錠剤を調製した。なお、カルメロースカルシウム、微粒二酸化ケイ素、ステアリン酸カルシウムについては、何れの実施例及び比較例においてもそれぞれ同量配合した。また、カシス抽出物は市販の水抽出物を使用した。
(Examples 1-8 and Comparative Examples 1-5)
Each component was weighed so as to have the composition described in Tables 1 to 3, and the components except calcium stearate were mixed and sieved. Thereafter, calcium stearate was combined and sieved again to obtain a tableting powder. The obtained powder for tableting was tableted with a single tableting machine to prepare tablets. Carmellose calcium, fine silicon dioxide, and calcium stearate were blended in the same amounts in each of the examples and comparative examples. As the cassis extract, a commercially available water extract was used.
試験例
実施例１〜８及び比較例１〜５の錠剤３錠について、崩壊試験を実施した。試験は、第１７改正日本薬局方「崩壊試験法」に準じた装置を用い、補助盤を使用した上で、ガラス管内に試料の残留物が認められなくなった時間を崩壊時間とした。表１〜表３には、試験した３錠のうち最も長い崩壊時間を示した。なお、崩壊時間が６０分を超えた場合は、「６０min以上」と記載した。
Test Example A disintegration test was performed on three tablets of Examples 1 to 8 and Comparative Examples 1 to 5. The test was performed using a device according to the 17th revised Japanese Pharmacopoeia "Disintegration Test Method", using an auxiliary panel, and the time when no sample residue was observed in the glass tube was defined as the disintegration time. Tables 1 to 3 show the longest disintegration time among the 3 tablets tested. In addition, when disintegration time exceeded 60 minutes, it described as "60 min or more."
表１〜表３の結果より、結晶セルロースを含む実施例１〜８はデキストリン等の他の添加剤を含む比較例１〜５に比べて崩壊時間を短縮できることがわかった。 From the results of Tables 1 to 3, it was found that Examples 1 to 8 containing crystalline cellulose can shorten the disintegration time as compared with Comparative Examples 1 to 5 containing other additives such as dextrin.
（引張破断強度の測定）
グルコサミン塩酸塩２００ｍｇを、単発式打錠機にて打錠圧１５ｋＮ、圧縮時間９０秒間で成形し、錠径８ｍｍの錠剤を調製したが、キャッピングが生じ錠剤が得られなかった。また、L-テアニン、L-オルニチン塩酸塩についても同様に引張破断強度の測定をしたところ、それぞれ０．７４Ｎ／ｍｍ２、１．０８Ｎ／ｍｍ２であった。
このことから、グルコサミン塩酸塩、L-テアニン、L-オルニチン塩酸塩は圧縮成形性の悪い粉体であることが分かった。
(Measurement of tensile strength at break)
200 mg of glucosamine hydrochloride was molded with a single tableting machine at a tableting pressure of 15 kN and a compression time of 90 seconds to prepare tablets with a tablet diameter of 8 mm, but capping occurred and no tablets were obtained. Also, L- theanine, was measured tensile strength Similarly for L- ornithine hydrochloride, respectively 0.74 N / mm 2, was 1.08 N / mm 2.
This indicates that glucosamine hydrochloride, L-theanine, and L-ornithine hydrochloride are powders with poor compression moldability.
本発明により、崩壊性を確保したカシス抽出物及びヒドロキシプロピルセルロース含有固形組成物を提供することが可能となった。 According to the present invention, it is possible to provide a cassis extract and a hydroxypropylcellulose-containing solid composition that ensure disintegration.
Claims (5)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2017087562 | 2017-04-26 | ||
| JP2017087562 | 2017-04-26 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018184388A true JP2018184388A (en) | 2018-11-22 |
| JP7235193B2 JP7235193B2 (en) | 2023-03-08 |
Family
ID=64355498
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018078107A Active JP7235193B2 (en) | 2017-04-26 | 2018-04-16 | solid composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP7235193B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021073988A (en) * | 2019-11-05 | 2021-05-20 | 花王株式会社 | Granular composition |
Citations (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001211858A (en) * | 2000-02-04 | 2001-08-07 | Api Co Ltd | Cranberry juice powdery composition and health food using the same |
| JP2002145780A (en) * | 2000-11-10 | 2002-05-22 | Rohto Pharmaceut Co Ltd | Amino sugar-containing pharmaceutical preparation |
| JP2005047861A (en) * | 2003-07-30 | 2005-02-24 | Shionogi & Co Ltd | Stable tablet containing crystalline cellulose |
| JP2007161706A (en) * | 2005-11-15 | 2007-06-28 | Taisho Pharmaceut Co Ltd | Antyusan-containing tablet |
| JP2007230870A (en) * | 2006-02-27 | 2007-09-13 | Unitika Ltd | Brain function ameliorant |
| JP2009280518A (en) * | 2008-05-21 | 2009-12-03 | Kowa Co | Formulation containing ethenzamide with suppressed sublimation of ethenzamide |
| JP2011513204A (en) * | 2008-03-11 | 2011-04-28 | 武田薬品工業株式会社 | Orally disintegrating solid preparation |
| JP2012056859A (en) * | 2010-09-07 | 2012-03-22 | Toa Yakuhin Kk | Granular agent having masked bitter taste and disagreeable taste of galenicals, and intraorally rapidly disintegrating tablet |
| JP2013001688A (en) * | 2011-06-20 | 2013-01-07 | Sankyo:Kk | Arthritis improvement composition |
| JP2015189743A (en) * | 2014-03-28 | 2015-11-02 | 小林製薬株式会社 | oral composition |
| JP2016088918A (en) * | 2014-11-11 | 2016-05-23 | 大山乳業農業協同組合 | Therapeutic/prophylactic composition for breast inflammation, and therapeutic/prophylactic method for breast inflammation |
| JP2016108327A (en) * | 2014-12-05 | 2016-06-20 | 大正製薬株式会社 | Solid composition |
| WO2016121925A1 (en) * | 2015-01-30 | 2016-08-04 | 協和発酵バイオ株式会社 | Tablet containing high proportion of functional substance, and manufacturing method for said tablet |
| KR20160098906A (en) * | 2015-02-11 | 2016-08-19 | 담양군 | A method for preparation of an effervescent tablet comprising an extract of blueberry |
| JP2017061577A (en) * | 2012-05-31 | 2017-03-30 | 旭化成株式会社 | Cellulose powder |
-
2018
- 2018-04-16 JP JP2018078107A patent/JP7235193B2/en active Active
Patent Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001211858A (en) * | 2000-02-04 | 2001-08-07 | Api Co Ltd | Cranberry juice powdery composition and health food using the same |
| JP2002145780A (en) * | 2000-11-10 | 2002-05-22 | Rohto Pharmaceut Co Ltd | Amino sugar-containing pharmaceutical preparation |
| JP2005047861A (en) * | 2003-07-30 | 2005-02-24 | Shionogi & Co Ltd | Stable tablet containing crystalline cellulose |
| JP2007161706A (en) * | 2005-11-15 | 2007-06-28 | Taisho Pharmaceut Co Ltd | Antyusan-containing tablet |
| JP2007230870A (en) * | 2006-02-27 | 2007-09-13 | Unitika Ltd | Brain function ameliorant |
| JP2011513204A (en) * | 2008-03-11 | 2011-04-28 | 武田薬品工業株式会社 | Orally disintegrating solid preparation |
| JP2009280518A (en) * | 2008-05-21 | 2009-12-03 | Kowa Co | Formulation containing ethenzamide with suppressed sublimation of ethenzamide |
| JP2012056859A (en) * | 2010-09-07 | 2012-03-22 | Toa Yakuhin Kk | Granular agent having masked bitter taste and disagreeable taste of galenicals, and intraorally rapidly disintegrating tablet |
| JP2013001688A (en) * | 2011-06-20 | 2013-01-07 | Sankyo:Kk | Arthritis improvement composition |
| JP2017061577A (en) * | 2012-05-31 | 2017-03-30 | 旭化成株式会社 | Cellulose powder |
| JP2015189743A (en) * | 2014-03-28 | 2015-11-02 | 小林製薬株式会社 | oral composition |
| JP2016088918A (en) * | 2014-11-11 | 2016-05-23 | 大山乳業農業協同組合 | Therapeutic/prophylactic composition for breast inflammation, and therapeutic/prophylactic method for breast inflammation |
| JP2016108327A (en) * | 2014-12-05 | 2016-06-20 | 大正製薬株式会社 | Solid composition |
| JP2017061576A (en) * | 2014-12-05 | 2017-03-30 | 大正製薬株式会社 | Solid composition |
| WO2016121925A1 (en) * | 2015-01-30 | 2016-08-04 | 協和発酵バイオ株式会社 | Tablet containing high proportion of functional substance, and manufacturing method for said tablet |
| KR20160098906A (en) * | 2015-02-11 | 2016-08-19 | 담양군 | A method for preparation of an effervescent tablet comprising an extract of blueberry |
Non-Patent Citations (2)
| Title |
|---|
| "コンタクトレンズユーザーの心と体のゆがみを整えるサプリメントLAFERRIEYE（ラフェリアイ）新発売 メニコ, JPN6022011405, ISSN: 0004894857 * |
| "ラフェリアイ60日分", 2022.03.15, インターネット, 2022.03.15検索, <URL HTTPS://MENICON-LIFESCIENCE-O, JPN6022011407, ISSN: 0004894858 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021073988A (en) * | 2019-11-05 | 2021-05-20 | 花王株式会社 | Granular composition |
| JP6994551B2 (en) | 2019-11-05 | 2022-01-14 | 花王株式会社 | Granule composition |
| JP2022022413A (en) * | 2019-11-05 | 2022-02-03 | 花王株式会社 | Granular composition |
| JP7277553B2 (en) | 2019-11-05 | 2023-05-19 | 花王株式会社 | Granule composition |
Also Published As
| Publication number | Publication date |
|---|---|
| JP7235193B2 (en) | 2023-03-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK2136653T3 (en) | STORED LIQUID LIQUID FOR TABLETING | |
| CA2709958C (en) | Use of an extract made of leaves of ginkgo biloba | |
| US11058643B2 (en) | Composition for outer layer of solid preparation, and easy-to-take solid preparation including said composition for outer layer | |
| AU2014271645B2 (en) | Oral cavity patch | |
| Rajakumari et al. | Dietary supplements containing vitamins and minerals: Formulation, optimization and evaluation | |
| JP4689468B2 (en) | Tablet and production method thereof | |
| PAL et al. | Formulation and evaluation of nutraceutical tablet using herbal drurs by direct compression method | |
| JP6032917B2 (en) | tablet | |
| JP2018184388A (en) | Solid composition | |
| MX2011002400A (en) | Pharmaceutical solid preparation having active ingredients separated by boundary therein. | |
| WO2006090640A1 (en) | Tablet composition containing amino acid and process for producing tablet | |
| CN109833304B (en) | Composition for solid preparation, solid preparation and method for producing same | |
| Alhmoud et al. | Combination of surfactants with other excipients: Effects on drug release and dimensional changes in matrices | |
| JP2008228694A (en) | Tablet made from royal jelly powder, and method for producing the same | |
| JP2019112358A (en) | Cellulose including compact for suppressing separation segregation | |
| JP2019210262A (en) | Orally disintegrating tablet | |
| Khan et al. | Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression. | |
| JP5843986B2 (en) | Granular pharmaceutical composition | |
| JP2018184387A (en) | Solid composition | |
| JP2013087170A (en) | Hydroxypropyl cellulose fine particle | |
| US9675666B2 (en) | Immediate-release tablet formulation, composition for tablets and method for manufacturing immediate-release tablet formulation | |
| EP3815681A1 (en) | Capsule filling composition, method of producing capsule formulation with the use of capsule filling composition, and capsule formulation | |
| Goyal et al. | Formulation and Evaluation of Once-daily Sustained Release Venlafaxine hydrochloride Tablet using Hydrophilic matrix. | |
| KR102387742B1 (en) | Co-granules of xanthan gum and acacia gum | |
| WO2023275891A1 (en) | Prolonged release tablet containing metformin hydrochloride |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20210408 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20220329 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20220527 |
|
| RD02 | Notification of acceptance of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7422 Effective date: 20220527 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220616 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20221012 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20221129 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20230125 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20230207 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7235193 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |