TWI230063B - Liquid medicament - Google Patents
Liquid medicament Download PDFInfo
- Publication number
- TWI230063B TWI230063B TW091111118A TW91111118A TWI230063B TW I230063 B TWI230063 B TW I230063B TW 091111118 A TW091111118 A TW 091111118A TW 91111118 A TW91111118 A TW 91111118A TW I230063 B TWI230063 B TW I230063B
- Authority
- TW
- Taiwan
- Prior art keywords
- acid
- fudosteine
- patent application
- sweetness
- sweetener
- Prior art date
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- 239000007788 liquid Substances 0.000 title claims abstract description 27
- 239000003814 drug Substances 0.000 title abstract 4
- KINWYTAUPKOPCQ-YFKPBYRVSA-N Fudosteine Chemical compound OC(=O)[C@@H](N)CSCCCO KINWYTAUPKOPCQ-YFKPBYRVSA-N 0.000 claims abstract description 48
- 229950006783 fudosteine Drugs 0.000 claims abstract description 48
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 18
- 239000003765 sweetening agent Substances 0.000 claims abstract description 18
- 150000005846 sugar alcohols Chemical class 0.000 claims abstract description 11
- 239000002253 acid Substances 0.000 claims abstract description 9
- 239000000463 material Substances 0.000 claims abstract 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims description 9
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims description 9
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims description 9
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 7
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 6
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 6
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 6
- 230000002079 cooperative effect Effects 0.000 claims description 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 6
- 244000228451 Stevia rebaudiana Species 0.000 claims description 5
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 5
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 claims description 5
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 4
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- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical class OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 3
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- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 3
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- 239000001530 fumaric acid Substances 0.000 claims description 3
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- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- -1 glycerin fatty acid ester Chemical class 0.000 description 10
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- 238000001556 precipitation Methods 0.000 description 7
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- MIDXCONKKJTLDX-UHFFFAOYSA-N 3,5-dimethylcyclopentane-1,2-dione Chemical compound CC1CC(C)C(=O)C1=O MIDXCONKKJTLDX-UHFFFAOYSA-N 0.000 description 6
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- 235000011007 phosphoric acid Nutrition 0.000 description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
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- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 150000007513 acids Chemical class 0.000 description 4
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- 229920000609 methyl cellulose Polymers 0.000 description 1
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- 150000004712 monophosphates Chemical class 0.000 description 1
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- 229920000573 polyethylene Polymers 0.000 description 1
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- 229940057838 polyethylene glycol 4000 Drugs 0.000 description 1
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- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
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- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 1
- 235000010483 polyoxyethylene sorbitan monopalmitate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229950008882 polysorbate Drugs 0.000 description 1
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- 239000003755 preservative agent Substances 0.000 description 1
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- YXJHJCDOUFKMBG-BMZHGHOISA-M riboflavin sodium Chemical compound [Na+].OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)[N-]C2=O YXJHJCDOUFKMBG-BMZHGHOISA-M 0.000 description 1
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 1
- 239000013049 sediment Substances 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- BMSYINVLSXEZEN-UHFFFAOYSA-M sodium;benzoic acid;dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O.OC(=O)C1=CC=CC=C1 BMSYINVLSXEZEN-UHFFFAOYSA-M 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
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- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 235000021012 strawberries Nutrition 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
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Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/35—Allergens
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/10—Expectorants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Immunology (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Infusion, Injection, And Reservoir Apparatuses (AREA)
Description
1230063 A7 B7 五、發明説明() (請先閲讀背面之注意事項再填寫本頁) 本發明之醫藥劑中,有效成分所包含之福多司痰( Fudosteine)的含有量,不特別制約,但約爲1〜2 〇 w t / v〇l% (以下、以「%」所示),最佳爲2〜1〇%, 更佳爲4〜8 %。 又,溶解福多司痰(Fudosteine)之溶媒,可使用水,進 一步因應其必要,亦可加入無水乙醇、乙醇、丙二醇、濃 甘油、甘油、甘油脂肪酸酯、聚環氧乙烷硬化篦麻油6 〇 、聚氧乙烯3 5篦麻油、聚山梨酸酯2 〇、聚山梨酸酯 40、聚山梨酸酯60、聚山梨酸酯80、聚乙二醇 200、聚乙二醇300、聚乙二醇400、聚乙二醇 6 0 0、聚乙二醇4 0 0 〇、聚氧乙烯月桂醇醚等之溶媒 〇 經濟部智慧財產局員工消費合作社印製 另一方面,本發明所添加之酸,例如有機酸及無機酸 。其中無機酸係可利用鹽酸、磷酸、硫酸等,又,有機酸 係可使用酢酸、磷酸、檸檬酸、酒石酸、乳酸、富馬酸、 號拍酸、已一酸、葡糖酸 '葡糖酸—d 一內醋等。而此些 酸,可使用單獨或2種以上之混合物。加入上記之酸,可 使本發明醫藥液劑之p Η爲酸性,而其p H最佳爲5 ·〇 以下,更佳爲4.0〜2·5。 本發明之醫藥液劑,進一步作爲甜味劑,最佳爲配合 糖醇、海藻糖或高甜味度甜味料。配合糖醇之例爲,例如 趨兀醛糖或酮糖之羰基而所得之鏈狀多價醇及環式糖醇。 具體而g之,例如碳數3〜1 1之d -山梨糖醇、d —甘 露糖醇、木糖醇、原藻糖醇、D 一阿糖醇、甜醇等之鏈狀 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 1230063 A7 B7 五、發明説明() 多價醇、麥芽醇、巴糖、木糖、肌醇、乳糖醇等之環式糖 醇,但最佳可使用D —山梨糖醇、D -甘露糖醇、木糖醇 、原藻糖醇。又,高甜味度甜味料之例係例如甜菊、阿斯 巴甜、T甜蛋白(thaumaUn )、蔗糖、糖精或其鹽、甘草 酸或其鹽,其中,最佳爲可使用甜菊、阿斯巴甜、糖精、 糖精鈉鹽。此種甜味劑係可使用兩種以上組合。 本發明之醫藥劑中,配合糖醇或海藻糖時之添加量係 爲1〜50%,最佳爲5〜4〇%,更佳爲1〇〜30% 。又,配合高甜味度甜味料時之添加量係爲〇 · 〇 1〜 1 .· 0。配合此範圍之量的甘味劑,可防止液劑之褐變且 掩蔽福多司痰(Fudosteine)所具有之特異味道。 又,本發明之醫藥液劑,係可添加藥學上可接受之任 易成份。此種成份係例示爲藻酸鈉、羥乙烯基聚合物、殘 甲基千維素納、結晶千維素·殘甲基千維素納、經乙基纖 維素、羥丙基纖維素、羥丙基甲基纖維素、聚乙燒醇等之 粘稠劑、山梨酸或其鹽、苯甲酸或其鹽、對羥苯甲酸酯類 (封键苯甲酸乙醋、對經苯甲酸甲酷、對經苯甲酸丁醋、 對羥苯甲酸丙酯)等之保存劑、天然著色料(焦糖、石一 胡蘿蔔素等)、合成著色料(食用色素、磷酸核黃素鈉等 )等之著色料、橙油、檸檬油、薄荷醇、香草酵、水果類 香料(草苺、鳳梨、柳橙、蘋果、檸檬、萊姆、葡萄柚等 )、草藥香料(草本植物、薄荷等)、飲料類香料(可可 亞、紅氽、淸涼飮料等)、點心類香料(巧克力、優格等 )等之香料等。 本紙張尺度適用中國國家椟準(CNS ) A4規格(2丨0X297公釐) -7 - (請先閱讀背面之注意事項再填寫本頁)
、1T f. 經濟部智慧財產局員工消費合作社印製 1230063 A7 __________ 五、發明説明(5 ) 由以上所得之本發明之醫藥液劑係可利用作爲經口之 福多司痰(Fudosteine)。 (請先閱讀背面之注意事項再填寫本頁) 實施例 以下,例舉以下實施例,更進一步詳細說明本發明, 本發明並不制約於此實施例。 實施例1 對於福多司痰(Fudosteine)之p Η的影響之檢討: 將含有福多司痰(Fudosteine) 8 g之水溶液的Ρ Η,可 使用適量之磷酸或氫化鈉,調整ρΗ2至ΡΗ7,調整全 量表示如表1,製造以精製水作爲全量1 〇 〇 m 1之各種 的p Η之去痰液劑。將此液劑以7 〇 保存7天.,再調查 $谷液中之福多司痰(Fudosteine)的殘存率、有無變色及產生 沉澱。福多司痰(Fudosteine)之殘存率係經高速液體光譜法 (Η P L C )而定量福多司痰(Fudosteine)量,而由此算出 。又,變色及沉澱之有無係依以下基準之目測觀察而評價 。其結果表示如表1。 經濟部智慧財產局員工消費合作社印製 變色評價基準; 評價:內容 (一):液劑之顏色無變化。 (± ):液劑之顏色些許變化 (+ ):液劑之顏色變化 (+ + ):液劑之顏色顯著變化 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) -8 - 1230063 A7 __ _ 五、發明説明() 沉澱評價之標準: (一):不產生沉著 土 源 沉 許 些 生 產 僅 澱 沉 生 產 果 結 表 ρΗ7·0 ρΗ6.0 pH5.0 pH4.0 pH3.5 ρΗ3·0 ρΗ2.5 ρΗ2.0 定量値 99.4 100.4 100.1 101.1 100.3 100.7 100.0 99.9 」^率%) __變色 ++ + 土 一 - - - - - • 土 土 (讀先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 經由此結果,確認福多司痰(F u d 〇 s t e i n e)之液劑爲ρ Η 5 · 〇以下,特別是ρΗ3 · 0至4 · 0之範圍內爲安定 。又,7天後之各pH之變化,幾乎爲誤差範圍內。 實施例2 福多司痰(Fudosteine)液劑中之ρ Η調節劑之種類的檢 討: 含有福多司痰(Fudosteine) 8 g之水溶液中,加入表2 所示之各種酸,調整P Η爲3 · 5後,以精製水製造全量 1 0 0 m 1之福多司痰(F u d 〇 s t e i n e)液劑。將此以7 〇 °C保 存7天,評價有無變色與試驗例1相同。其結果如表2所 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) -9 - 五 l23〇〇63 A7 二發明説明(7) (結果) 表2 定量値 變色 ^^___ 殘存率(%) —_ 鹽酸 99.7 一 磷酸 100.5 ^___ 硫酸 100.3 - 酢酸 101.2 -_蘋果酸 99.3 〜_檸檬酸 100.7 _酒石酸 100.7 __ 乳酸 99.5 __富馬酸 98.8 - (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 經其結果之本發明之醫藥液劑,確認可使用無機酸、 有機酸。又,7天後之各種酸的ρ Η變化係幾乎於誤差範 圍內。 實施例3 福多司痰(Fudosteine)液劑中之甜味劑之之種類的檢討 可使用含有福多司痰(Fudosteme) 8 g及表3所示之甜 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) -10 - 1230063 A7 B7 g 五、發明说明() (請先閱讀背面之注意事項再填寫本頁} 味劑2 0 g之水溶液、磷酸而調整P Η爲3 · 5,以精製 水製造全量1 0 0之福多司痰(Fudosteine)液劑。將此以 7 0 °C保存7天,評價有無變色之與實施例1相同。其結 果如表3所示。 (結果) 表 定量値 殘存率(%) 變色 精製白糖 90.5 葡萄糖 78.8 + + 果糠 90.7 + + 異性化糖 90.8 + + 山梨糖 100.7 甘露糖醇 99.3 木糖醇 100.3 原藻糖醇 99.5 海藻糖 100.2 澴原麥芽糖* 9 9.9 隹 經濟部智慧財產局員工消費合作社印製 *麥芽糖、山梨糖、寡糖醇之混合物 可使用其結果之甜味料的糖醇、海藻糖時,確認福多 司痰(Fudosteine)之殘存率高,不能變色。又,7天後之各 種甜味劑之P Η變化係幾乎於誤差範圍內。 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 1230063 A7 _ 五、發明説明(9 ) 實施例4 福多司痰(Fudosteine)液劑中之甜味劑之種類的檢討: 可使用福多司痰(Fudosteine) 8 g及表4所示之甜味劑 〇· 1 一 〇 · 2g之水溶液、磷酸而調整pH爲3 · 5以 精製水製造全量1 〇 〇 ηι 1之福多司痰(Fudosteine)液劑。 將此以7 0 X:保存7天,評價有無變色之與實施例1相同 。其結果如表4所不。 表4 添加量(g) 定量値 殘存率(%) 變色 焦糖 0.2 100.4 阿斯巴甜 0.2 99.1 糖精鈉鹽 0.1 99.4 - 可使用經由此結果,甜味劑可使用高度甜味料,確認 福多司痰(Fudosteine)之殘存率高、又不變色。 實施例5 福多司痰(Fudosteine)液劑中之糖醇的添加量之檢討: 可使用福多司痰(Fudosteine) 8 g及表5所示之量的含 有D -山梨糖之水溶液、磷酸而調整p Η爲3 · 5,以精 製水製造全量1 0 0 m 1之福多司痰(Fudosteme)液劑。將 此以7 0 °C保存7天,檢討與實施例1相同之殘存率、變 (請先閲讀背面之注意事項再填寫本頁〕 -訂 Ρ 經濟部智慧財產局員工消費合作社印製 本纸張尺度適用中國國家標準(CNS ) Α4規格(210X297公釐) · 12 - 1230063 A7 B7 10、 五、發明説明() 色之有無及沉澱之發生。其結果如表5所示。 (結果) 表5 定量値 變色 沈澱 殘存率(%) 0% 99.6 細 10% 99.4 - • 20% 99.0 30% 99.3 雜 40% 99.9 土 + 5 0% 100.4 + + (請先閲讀背面之注意事項再填寫本頁) 訂 經由此結果,確認糖醇之含有量爲4 0 %以下,特別 爲30%以下可得之安定液劑。又,7天後之D—山梨糖 之含量不同的p Η之變化係幾乎於誤差範圍內。 實施例6 福多司痰(Fudosteine)配合經口醫藥液劑: 經由下記處方、一般之方法而調製經口醫藥液劑。此 P Η係爲3 . 7。 (處方) 福多司痰(Fudosteine) 8 g D —山梨糖 1 5 g 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) -13 - f 經濟部智慧財產局員工消費合作社印製 1230063 A7 B7 五、發明説明(焦糖 Η 安息香酸鈉 蘋果酸香料(優格類) 精製水之全量 1 0 0 m g 7 0 m g 適量 1 Ο 0 m g 1 Ο Ο m 1 此係爲福多司痰(Fudosteine)含量低及不產生變色、沉 源之女疋製劑。又,掩蓋D-山梨糖、香料添加之福多司 痰(Fudosteine)的特異味。 (請先閱讀背面之注意事項再填寫本頁) 8 g 經濟部智慧財產局員工消費合作社印製 原藻糖醇 焦糖 安息香酸鈉 磷酸 香料(柳橙類 精製水之全量 實施例7 福多司痰(F u d 〇 s t e i n e)配合經口醫藥液劑: 經由下記處方、一般方法而調製經口醫藥液劑◊此 P Η係爲3 · 7。 (處方) 福多司痰(Fudosteine) 2 0 g 1 0 0 m g 7 0 m g 適量 1 0 0 m g 10 0ml 此係爲福多司痰(Fudosteine)含量低下及變色、不產生 沉澱之安定製劑。又,掩蓋原藻糖醇、香料添加的特異味 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) _ 14 - 1230063 kl B7 ' "~γι —--- 五、發明説明() 〇 實施例8 (請先閱讀背面之注意事項再填寫本頁) 福多司痰(Fudosteine)配合經ρ醫藥液劑: 依據下S5處方、一般方法而調製經口醫藥液劑。此 P Η係爲3 , 7。 (處方) 福多司痰(Fudosteine) 8 g 還原麥芽糖 20g (麥芽醇、山梨糖、低聚糖醇之混合物) 焦糖 1 0 0 m g 安息香酸鈉 7 0 m g 蘋果酸 適量 香料(薄荷醇類) 1 0 0 g 精製水之全量 100ml 此爲去痰量含量低及變色、不產生沉澱之安定製劑。 又’掩盖海彳架糖、香料添加的福多司疲(FU(j〇steine)之特異 的味道。 經濟部智慧財產局員工消費合作社印製 實施例9 福多司痰(Fudosteine)配合經口醫藥液劑: 依據下記處方、一般方法而調製經口醫藥液劑。此 P Η係爲3 · 7。 (處方) 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公釐) _ 15 - 1230063 kl B7 13、 五、發明説明(^) 福多司痰(Fudosteine) 8 g 海藻糖 焦糖 安息香酸鈉 磷酸 香料(巧克力類) 精製水之全量 2 0 g 1 0 0 m g 7 0 m g 適量 1 0 0 m g 10 0ml 此爲福多司痰(F u d o s t e i n e)含量低及變色、不$ I座生彳几搬 之安定製劑。又,掩蓋海藻糖、香料添加的福多司疲( Fudosteine)之特異味道。 實施例1 ο 福多司痰(F u d o s t e i n e)配合經口醫藥液劑: 依據下記處方、一般之方法而調製經口醫藥液劑 P Η係爲3 . 7。 (處方) 福多司痰(Fudosteine) 8 g (讀先閱讀背面之注意事項再填寫本頁) 訂 f 經濟部智慧財產局員工消費合作社印製 甜菊 焦糖 安息香酸鈉 蘋果酸 香料(草莓類) 精製水之全量 1 0 0 m g 1 0 0 m g 7 0 m g 適量 1 0 0 m g 10 0ml 此爲福多司痰(?1^051以]^)含量低下及變色、不產生幻 本紙張尺度適用中周國家標準(CNS ) A4規格(210X 297公釐) -16 - A7 1230063 B7 —_— 五、發明説明() 澱之安定製劑。又,掩蓋甜菊、香料添加之去痰液劑之特 異味。 產業上之利用可能性 本發明之醫藥液劑,含有福多司痰(Fudosteine)且安定 性高、長期保存,不產生變色與沉澱之安定製劑。又,配 合甜味料之糖醇、海藻糖或高甜味度甜味料的本發明之醫 藥液劑,不產生液劑之褐變且可掩蓋福多司痰(Fudosteine) 之特異味道。 因此,本發明之醫藥液劑係作爲易攝取之經口液劑、 福多司痰(Fudosteine)等之商品性高者。 (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) -17 -
Claims (1)
- 「、申請專利範圍 ^— 第91] 111 18號專利申請案 中文申請專利範圍修正本 民國93年]2月2〇日修正 1 · 一種醫藥液劑,其特徵係爲含有福多司瘐( Fudosteine )及酸,且ρ Η爲2 .〇〜5 ·〇者。 二·如申請專利範圍第丄項之醫藥液劑,其中甜味劑 係:含有糖醇、海藻糖或高甜度甜味料’該糖醇或海藻糖 的a有星爲4 0質量%以下,高甜度甜味料的含有量爲 〇 ·〇1〜1·〇質量%。 3 ·如申請專利範圍第2項之醫藥液劑,其中,糖醇 係D -山梨糖醇、D 一甘露糖醇、木糖醇或原藻糖醇。 4 ·如申請專利範圍第2項之醫藥液劑,其中,高甜 度甜味料係甜菊、阿斯巴甜、糖精或糖精鈉鹽。 5 ·如申請專利範圍第1項或第2項之醫藥液劑,其 中,酸係一種或二種以上選自磷酸、硫酸'蘋果酸、酒石 酸、乳酸及富馬酸所成之群。 裝— (請先閱讀背面之注意事項再填寫本頁} -訂 經濟部智慧財產局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) Ad規格(210X297公釐)
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Country | Link |
---|---|
US (1) | US7592372B2 (zh) |
EP (1) | EP1391202B1 (zh) |
JP (1) | JP3805646B2 (zh) |
KR (1) | KR100900064B1 (zh) |
CN (1) | CN1259910C (zh) |
AT (1) | ATE518523T1 (zh) |
CA (1) | CA2448083C (zh) |
ES (1) | ES2366945T3 (zh) |
TW (1) | TWI230063B (zh) |
WO (1) | WO2002096407A1 (zh) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100404026C (zh) * | 2005-09-23 | 2008-07-23 | 北京德众万全药物技术开发有限公司 | 一种含福多司坦的口服药物组合物 |
CN101152172B (zh) * | 2006-09-29 | 2010-05-12 | 北京德众万全药物技术开发有限公司 | 一种福多司坦口服固体组合物 |
JP2009001548A (ja) * | 2007-05-21 | 2009-01-08 | Daiichi Sankyo Healthcare Co Ltd | トレハロースからなる気道杯細胞過形成抑制剤。 |
EP2065038A1 (en) | 2007-11-30 | 2009-06-03 | Pharnext | New therapeutic approaches for treating Charcot-Marie-Tooth disease |
EP2263665A1 (en) * | 2009-06-02 | 2010-12-22 | Pharnext | New compositions for treating CMT and related disorders |
US9393241B2 (en) | 2009-06-02 | 2016-07-19 | Pharnext | Compositions for treating CMT and related disorders |
WO2014195394A1 (en) | 2013-06-05 | 2014-12-11 | Pharnext | Stable oral solutions for combined api |
US10383870B2 (en) | 2016-06-10 | 2019-08-20 | Pharnext | Early treatment of CMT disease |
CN106361689A (zh) * | 2016-09-24 | 2017-02-01 | 北京万全德众医药生物技术有限公司 | 一种福多司坦口服溶液及其制备方法 |
CN109925300A (zh) * | 2017-12-19 | 2019-06-25 | 北京盈科瑞创新药物研究有限公司 | 一种福多司坦雾化吸入用溶液制剂及其制备方法 |
JP2021004196A (ja) * | 2019-06-26 | 2021-01-14 | 物産フードサイエンス株式会社 | 菌数抑制剤、体臭抑制剤および腋臭症予防改善剤 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US147605A (en) * | 1874-02-17 | Improvement in grindlng-mills | ||
FR2187326B1 (zh) * | 1972-06-15 | 1975-10-17 | Rech Pharm Scientifiques | |
JPH0813737B2 (ja) * | 1986-12-19 | 1996-02-14 | 杏林製薬株式会社 | シロツプ剤 |
JPH0788352B2 (ja) * | 1988-06-16 | 1995-09-27 | エスエス製薬株式会社 | ヒドロキシアルキルシステイン誘導体およびこれを含有する去痰剤 |
US5010069A (en) * | 1989-05-15 | 1991-04-23 | Marion Laboratories, Inc. | Stable liquid form of 5-aminosalicylic acid |
JPH0558888A (ja) | 1991-09-06 | 1993-03-09 | Kyorin Pharmaceut Co Ltd | 吸入剤 |
JPH0558887A (ja) | 1991-09-06 | 1993-03-09 | Kyorin Pharmaceut Co Ltd | 吸入剤 |
JP4098850B2 (ja) | 1997-07-16 | 2008-06-11 | 久光製薬株式会社 | S−(3−ヒドロキシプロピル)−l−システインを含有する経口用製剤 |
JP2000256192A (ja) | 1999-03-05 | 2000-09-19 | Nissho Corp | カルボシステイン製剤 |
-
2001
- 2001-05-25 JP JP2001156840A patent/JP3805646B2/ja not_active Expired - Fee Related
-
2002
- 2002-05-24 CA CA2448083A patent/CA2448083C/en not_active Expired - Lifetime
- 2002-05-24 ES ES02726488T patent/ES2366945T3/es not_active Expired - Lifetime
- 2002-05-24 KR KR1020037015168A patent/KR100900064B1/ko active IP Right Grant
- 2002-05-24 TW TW091111118A patent/TWI230063B/zh not_active IP Right Cessation
- 2002-05-24 AT AT02726488T patent/ATE518523T1/de not_active IP Right Cessation
- 2002-05-24 CN CNB028105753A patent/CN1259910C/zh not_active Expired - Lifetime
- 2002-05-24 US US10/477,758 patent/US7592372B2/en not_active Expired - Lifetime
- 2002-05-24 WO PCT/JP2002/005043 patent/WO2002096407A1/ja active Application Filing
- 2002-05-24 EP EP02726488A patent/EP1391202B1/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
JP3805646B2 (ja) | 2006-08-02 |
ES2366945T3 (es) | 2011-10-26 |
CN1511033A (zh) | 2004-07-07 |
WO2002096407A1 (fr) | 2002-12-05 |
CA2448083C (en) | 2011-03-29 |
KR20040005976A (ko) | 2004-01-16 |
KR100900064B1 (ko) | 2009-05-28 |
CN1259910C (zh) | 2006-06-21 |
CA2448083A1 (en) | 2002-12-05 |
EP1391202A4 (en) | 2010-03-17 |
JP2002348236A (ja) | 2002-12-04 |
ATE518523T1 (de) | 2011-08-15 |
EP1391202A1 (en) | 2004-02-25 |
US20040147609A1 (en) | 2004-07-29 |
US7592372B2 (en) | 2009-09-22 |
EP1391202B1 (en) | 2011-08-03 |
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