Nova Patents
JP2012167106A

Controlled-release hydrocodone formulation

Abstract

Problem to be solved.To provide a solid controlled-release oral formulation suitable for administration of every 24 hours to a human patient.

Solution.The solid controlled-release oral formulation includes, (a) a pharmaceutically acceptable matrix including an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof and controlled release material or (b) an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof coated onto a plurality of inert pharmaceutically acceptable beads and overcoated with a controlled-release material, and provides a C/Cratio of 0.55 to about 0.85 after administration, and provides a therapeutic effect for at least about 24 hours dosing in a human patient.

Term

Projected expiry 23 April 2032.

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4 claims: 3 independent, 1 dependent

  1. 1
    A solid oral release controlled formulation suitable for administration to human patients every 24 hours, the formulation being selected from the group consisting of hydrocodone bitartrate and gum, cellulose ether, acrylic resin, wax, shelac, and fats and oils. The formulation contains 0-35% in 1 hour, 10-70% in 4 hours, 20-75% in 8 hours, 30-80% in 12 hours, 40-90 in 18 hours. The solid oral release control, which gives an in vitro release rate of hydrocodone choline bitartrate greater than 60% in 24 hours and the amount of hydrocodone choline bitartrate contained in the formulation is equivalent to 5-60 mg of hydrocodone. Formulation. ヒト患者への24時間おきの投与に適する固体経口放出制御製剤であって、 該製剤が、重酒石酸ヒドロコドン、並びに、ガム、セルロースエーテル、アクリル樹脂、ワックス、シェラック、及び油脂からなる群より選択される放出制御物質を含有し、 該製剤が、1時間で0~35%、4時間で10~70%、8時間で20~75%、12時間で30~80%、18時間で40~90%、かつ24時間で60%より高値の重酒石酸ヒドロコドンのインビトロ放出速度を与え、 前記製剤中に含まれる前記重酒石酸ヒドロコドンの量が、ヒドロコドンの5~60mgと等価である、前記固体経口放出制御製剤。
  2. 2
    A solid oral release controlled formulation suitable for administration to human patients every 24 hours, wherein the formulation contains granules containing at least one hydrophobic and / or hydrophilic substance, and hydrocodone choline bitartrate. However, it is 0 to 35% in 1 hour, 10 to 70% in 4 hours, 20 to 75% in 8 hours, 30 to 80% in 12 hours, 40 to 90% in 18 hours, and higher than 60% in 24 hours. The solid oral release controlled formulation that provides the in vitro release rate of hydrocodone bitartrate and the amount of hydrocodone choline contained in the formulation is equivalent to 5-60 mg of hydrocodone. ヒト患者への24時間おきの投与に適する固体経口放出制御製剤であって、 該製剤が、疎水性および/または親水性物質少なくとも1種を含有する顆粒、並びに重酒石酸ヒドロコドンを含有し、 該製剤が、1時間で0~35%、4時間で10~70%、8時間で20~75%、12時間で30~80%、18時間で40~90%、かつ24時間で60%より高値の重酒石酸ヒドロコドンのインビトロ放出速度を与え、 前記製剤中に含まれる前記重酒石酸ヒドロコドンの量が、ヒドロコドンの5~60mgと等価である、前記固体経口放出制御製剤。
  3. 4
    (a)(i)重酒石酸ヒドロコドン、及びポリ(アルキレンオキシド)を含む重合体ヒドロゲルを含有する薬剤層と、(ii)ポリアルキレンオキシドおよびカルボキシアルキルセルロースからなる群から選択されるオスモポリマー、抗酸化剤、及び潤滑剤を含む置換層と、を含む二層コア部;および (b)前記重酒石酸ヒドロコドンの放出のための通路を配置した、二層コア部を包囲する半透過性壁部、を含有する徐放性経口製剤であって、 前記半透過性壁部が、セルロースエステル重合体、セルロースエーテル重合体およびセルロースエステル-エーテル重合体からなる群から選択される、前記徐放性経口製剤。 A drug layer containing a polymer hydrogel containing (a) (i) hydrocholine bitartrate and poly (alkylene oxide), and (ii) an osmopolymer selected from the group consisting of polyalkylene oxide and carboxyalkyl cellulose, antioxidant. A bilayer core containing an agent and a substituent containing a lubricant;and (b) a semi-permeable wall surrounding the bilayer core, which is provided with a passage for the release of the hydrocodon bitartrate. The sustained-release oral preparation to be contained, wherein the semi-permeable wall portion is selected from the group consisting of a cellulose ester polymer, a cellulose ether polymer and a cellulose ester-ether polymer.
Independent claims3