Controlled release oral dosage formulations comprising a core and one or more barrier layers

An oral preparation and barrier layer technology, which is applied in the field of controlled release preparations of pharmaceutically active agents, can solve the problems of reduced surface area of ​​dosage forms, reduced release rate, reduced drug concentration, etc.

Active Publication Date: 2009-08-26
JAGOTEC AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, over time, as the thickness of the colloidal matrix increases, the drug concentration in the dosage form decreases, the surface area of ​​the dosage form decreases, and the release rate decreases

Method used

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  • Controlled release oral dosage formulations comprising a core and one or more barrier layers
  • Controlled release oral dosage formulations comprising a core and one or more barrier layers
  • Controlled release oral dosage formulations comprising a core and one or more barrier layers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1. Three-layer tablet containing 40 mg of nisoldipine

[0096] Three different formulations were prepared, each containing 40 mg of nisoldipine. These formulations are referred to as Formulation A, Formulation B, and Formulation C, as described in Tables 1-3. Formulation C was coated with an enteric coating (5% weight gain) containing S100 (methacrylic acid copolymer type B) and Combination of L100 (methacrylic acid copolymer type A). Formulations A and B from Colorcon, West Point, PA II seal coat for coating.

[0097] Table 1 Components of Formulation A

[0098]

[0099] Table 2 Components of Formulation B

[0100]

[0101]

[0102] Table 3 Components of Formulation C

[0103]

[0104]

[0105] The formulations described above were prepared as follows:

[0106] core or central layer

[0107] 1. Stir nisoldipine and sodium lauryl sulfate in a high shear mixer for two minutes. Lactose monohydrate, povidone, methacrylic acid copolymer ...

Embodiment 2

[0130] Embodiment 2. The study of relative bioavailability of Nisoldipine 40mg extended-release tablet under fasting condition

[0131] The pharmacokinetic parameters of Formulations A-C described in Example 1 were compared with those of the reference formulation (Formulation D). The reference preparation is Delayed-release nisoldipine (40 mg). is a core-wrapped formulation consisting of a core containing nisoldipine coated with an immediate release coat also containing nisoldipine. given in Table 4 components and their concentrations.

[0132] The goal of this single-dose, open-label, randomized study was to compare the performance of the test formulation (nisoldipine 40 mg extended-release tablet) described in Example 1 with an equivalent oral dose under fasting conditions when administered to healthy individuals. Commercially available reference products ( 40mg extended-release tablet) absorption rate and oral bioavailability.

[0133] Table 4 Components (Formul...

Embodiment 3

[0156] Embodiment 3. The study of the relative bioavailability of Nisoldipine 40mg extended-release tablet under feeding condition (fed condition)

[0157] The goal of this study was to compare formulation A described in the examples with the market formulation food effect. In order to determine the food effect of formulations A and Sular, the pharmacokinetic data of these two formulations under fasted conditions in Example 2 were used as reference. The same 32 individuals from Example 2 were recruited for the food effect study.

[0158] Twenty-six (26) individuals completed the study. According to the randomization schedule, individuals receive their assigned treatment in the first period and additional treatment in subsequent periods. Dosing days were separated by a washout period of at least 7 days. An equal number of individuals were randomly assigned to each possible treatment order. Blood samples were collected and analyzed as described in Example 2. Table 9 shows...

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Abstract

Controlled release oral dosage formulations containing one or more active agent, and methods of use thereof, are provided for the once-a-day treatment. The formulation can be in the form of a trilayer tablet containing a core or central layer and one or more barrier layers. The core may contain one or more enteric materials or polymeric materials which modulates the release of the active agent.

Description

[0001] This application claims priority to US Provisional Patent Application No. 60 / 824,043, filed August 30, 2006, and US Provisional Patent Application No. 60 / 824,054, filed August 30, 2006. technical field [0002] The present invention relates generally to the field of controlled or modified release formulations of pharmaceutically active agents. Background technique [0003] Controlled-release formulations refer to pharmaceutical compositions that release the drug at a predetermined rate and / or for a predetermined time after administration so as to maintain the desired pharmacological activity for a desired period of time. Such formulations deliver the drug to the body for a predetermined period of time or at a predetermined site of absorption, thereby maintaining drug levels at therapeutic levels for a longer period of time than conventional (e.g., immediate release) formulations. within range. [0004] Dosage forms comprising a core, where the core contains the drug ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/32A61K9/36A61K9/16A61K9/24A61K9/26
Inventor G·韦尼奥P·格勒尼耶A·尼安米斯
Owner JAGOTEC AG
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