JP2017137295A - ドルゾラミド、高分子およびホウ酸を含有する医薬組成物 - Google Patents
ドルゾラミド、高分子およびホウ酸を含有する医薬組成物 Download PDFInfo
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- JP2017137295A JP2017137295A JP2016227521A JP2016227521A JP2017137295A JP 2017137295 A JP2017137295 A JP 2017137295A JP 2016227521 A JP2016227521 A JP 2016227521A JP 2016227521 A JP2016227521 A JP 2016227521A JP 2017137295 A JP2017137295 A JP 2017137295A
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- dorzolamide
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- 229960002167 sodium tartrate Drugs 0.000 description 1
- 235000011004 sodium tartrates Nutrition 0.000 description 1
- RBWSWDPRDBEWCR-RKJRWTFHSA-N sodium;(2r)-2-[(2r)-3,4-dihydroxy-5-oxo-2h-furan-2-yl]-2-hydroxyethanolate Chemical compound [Na+].[O-]C[C@@H](O)[C@H]1OC(=O)C(O)=C1O RBWSWDPRDBEWCR-RKJRWTFHSA-N 0.000 description 1
- HLWRUJAIJJEZDL-UHFFFAOYSA-M sodium;2-[2-[bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetate Chemical compound [Na+].OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC([O-])=O HLWRUJAIJJEZDL-UHFFFAOYSA-M 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
- 229960002368 travoprost Drugs 0.000 description 1
- MKPLKVHSHYCHOC-AHTXBMBWSA-N travoprost Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC=CC(C(F)(F)F)=C1 MKPLKVHSHYCHOC-AHTXBMBWSA-N 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- WUUHFRRPHJEEKV-UHFFFAOYSA-N tripotassium borate Chemical compound [K+].[K+].[K+].[O-]B([O-])[O-] WUUHFRRPHJEEKV-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- BSVBQGMMJUBVOD-UHFFFAOYSA-N trisodium borate Chemical compound [Na+].[Na+].[Na+].[O-]B([O-])[O-] BSVBQGMMJUBVOD-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 229950008081 unoprostone isopropyl Drugs 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
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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
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/382—Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
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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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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Abstract
【解決手段】本発明に係る医薬組成物によれば、ドルゾラミド又はその塩、及び、高分子を含有するpH6.0以下の医薬組成物に、ホウ酸又はその塩を含有することにより、医薬組成物の経時的な粘度低下が抑制される。
【選択図】なし
Description
以下に本発明の代表的な製剤例を示す。なお、下記製剤例において各成分の配合量は製剤1mL中の含量である。
ドルゾラミド 10mg
ヒドロキシエチルセルロース 5mg
ホウ酸 10mg
希塩酸 適量
水酸化ナトリウム 適量
精製水 適量
pH 5.65
ドルゾラミド 10mg
ヒドロキシプロピルメチルセルロース 5mg
ホウ酸 10mg
希塩酸 適量
水酸化ナトリウム 適量
精製水 適量
pH 5.65
1.被験製剤の調製
<実施例1の製剤の調製>
ヒドロキシエチルセルロースを正確に0.57g秤量し、滅菌精製水約80gに投入した。約60℃で加温しながら撹拌溶解した後室温にて放冷した。滅菌精製水を加え全量100gに調整した。均一に撹拌後、高圧蒸気滅菌(121℃、30分)し、0.57%ヒドロキシエチルセルロース溶液とした。0.57%ヒドロキシエチルセルロース溶液8.333gにドルゾラミド塩酸塩0.1113gを投入し、撹拌溶解した。さらに1N水酸化ナトリウムを添加し、pH5.65に調整した。滅菌精製水を加え全量10gに調整することにより、実施例1の製剤を調製した。調製したサンプルはガラス容器(ラボランパック スクリュー管瓶No.5 品番「9−852−07」)に充填し、遮光下、60℃で8週間保管した。
上記記載と同様の方法で調製した0.57%ヒドロキシエチルセルロース溶液8.333gにドルゾラミド塩酸塩0.1113gを投入し撹拌溶解した後、ホウ酸0.1gを投入し撹拌溶解した。さらに1N水酸化ナトリウムを添加し、pH5.65に調整した。滅菌精製水を加え全量10gに調整することにより、比較例1の製剤を調製した。調製したサンプルはガラス容器(ラボランパック スクリュー管瓶No.5 品番「9−852−07」)に充填し、遮光下、60℃で8週間保管した。
第十六改正日本薬局方「第2法 回転粘度計法」に従い、円すい‐平板形回転粘度計を用いて、調製直後及び調製後1、2、4、8週間における各製剤の粘度を測定した。測定条件は以下の通り実施した。
・測定機器:VISCOMETER DV-II+PRO(BROOKFIELD)
・回転数(RPM):0.1
・測定温度:25℃
試験結果を表1に示す。
1.被験製剤の調製
<比較例1の製剤の調製>
ヒドロキシエチルセルロースを正確に0.57g秤量し、滅菌精製水約80gに投入した。約60℃で加温しながら撹拌溶解した後室温にて放冷した。滅菌精製水を加え全量100gに調整した。均一に撹拌後、高圧蒸気滅菌(121℃、30分)し、0.57%ヒドロキシエチルセルロース溶液とした。0.57%ヒドロキシエチルセルロース溶液8.333gにドルゾラミド塩酸塩0.1113gを投入し、撹拌溶解した。さらに1N水酸化ナトリウムを添加し、pH5.65に調整した。滅菌精製水を加え全量10gに調整することにより、比較例1の製剤を調製した。調製したサンプルはガラス容器(ラボランパック スクリュー管瓶No.5 品番「9−852−07」)に充填し、遮光下、60℃で8週間保管した。
上記記載と同様の方法で調製した0.57%ヒドロキシエチルセルロース溶液8.333gにドルゾラミド塩酸塩0.1113gを投入し撹拌溶解した後、ホウ酸0.1gを投入し撹拌溶解した。さらに1N水酸化ナトリウムを添加し、pH5.65に調整した。滅菌精製水を加え全量10gに調整することにより、実施例1の製剤を調製した。調製したサンプルはガラス容器(ラボランパック スクリュー管瓶No.5 品番「9−852−07」)に充填し、遮光下、60℃で8週間保管した。
Claims (11)
- ドルゾラミド又はその塩、高分子、及びホウ酸又はその塩を含有し、そしてpHが6.0以下である、医薬組成物。
- ドルゾラミド又はその塩がドルゾラミド塩酸塩である、請求項1に記載の医薬組成物。
- ドルゾラミド又はその塩の含有量が0.1〜5%(w/w)である、請求項1又は2に記載の医薬組成物。
- 高分子が、セルロース系高分子及びカルボキシビニルポリマーよりなる群から選択される1又は複数の高分子である、請求項1〜3のいずれか一項に記載の医薬組成物。
- セルロース系高分子が、ヒドロキシエチルセルロース、ヒドロキシメチルセルロース、ヒドロキシプロピルメチルセルロース及びカルボキシビニルポリマーよりなる群から選択される1又は複数のセルロース系高分子である、請求項4に記載の医薬組成物。
- 高分子の含有量が0.001〜10%(w/w)である、請求項1〜5のいずれか一項に記載の医薬組成物。
- ホウ酸又はその塩の含有量が0.001〜10%(w/w)である、請求項1〜6のいずれか一項に記載の医薬組成物。
- pHが3.0〜6.0である、請求項1〜7のいずれか一項に記載の医薬組成物。
- 医薬組成物の粘度が、25℃において50〜700(mPa・s)である、請求項1〜8のいずれか一項に記載の医薬組成物。
- ドルゾラミド又はその塩及び高分子を含有し、pHが6.0以下である医薬組成物にホウ酸又はその塩を含有させることによる、医薬組成物の粘度低下を防止する方法。
- pHが6.0以下である医薬を製造するための、ドルゾラミド又はその塩、高分子、及びホウ酸又はその塩の使用。
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