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Controlled Release Formulations

a technology of controlled release and formulation, applied in the direction of biocide, cardiovascular disorder, drug composition, etc., can solve the problems of reducing the surface area of the dosage form and the rate of release, and achieve the effect of modulating the release of the active agen

Inactive Publication Date: 2008-03-06
JAGOTEC AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] The core may contain one or more polymeric materials that modulate (i.e. slow and / or accelerate) the release of the active agent. The concentration of the polymeric material is from about 1% to about 95% by weight. The central layer and / or the barrier layers may also contain one or adjuvants, which, in combination with the polymeric materials, further modulate release of the active agent. The concentration of the adjuvant(s) is from about 1% to about 25% by weight of the compositions, preferably from about 5% to about 15% by weight of the composition.

Problems solved by technology

However, over time, as the thickness of the gel matrix increases, the drug concentration in the dosage form decreases, the surface area of the dosage form decreases and as a result the rate of release decreases.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Trilayer Tablets Containing 40 mg of Nisoldipine

[0084] Three different formulations, each of which contained 40 mg of Nisoldipine, were prepared. The formulations are identified as Formulation A, Formulation B, and Formulation C and are described in Tables 1-3. Formulation C was coated with an enteric coating (5% weight gain) containing a combination of Eudragit® S100 (methacrylic acid copolymer type B) and Eudragit® L100 (methacrylic acid copolymer type A). Formulations A and B were coated with an OPADRY® II seal coat available from Colorcon, West Point, Pa.

TABLE 1Composition of Formulation AFirstSecondBarrierBarrierWeightLayerCoreLayerTotal% (of theIngredient(mg / tab)(mg / tab)(mg / tab)(mg)tablet)Nisoldipine40.0040.007.1Lactose Monohydrate, NF76.532.3557.375166.2329.5Ferric Oxide, NF (yellow)0.200.150.350.1Hypromellose, USP, type 220853.6553.659.5(Methocel ® K4M)Sodium lauryl sulfate, NF50.0050.008.9Methacrylic Acid Copolymer,21.4021.403.8Type B, NF (S)Hypromellose Phthalate, NF26....

example 2

Relative Bioavailability Study of Nisoldipine 40 mg Extended Release Tablets Under Fasting Conditions

[0112] The pharmacokinetic parameters of formulations A-C described in Example 1 were compared to those of a reference formulation (Formulation D). The reference formulation was SULAR® Nisoldipine Extended Release (40 mg). SULAR® is a coat-core formulation consisting of a core containing Nisoldipine, coated with an immediate release coating which also contains Nisoldipine. The components of SULAR®, and their concentrations, are given in Table 4.

[0113] The objective of this single-dose, open-label, randomized study was to compare, under fasting conditions, the rate of absorption and oral bioavailability of a test formulation of nisoldipine 40 mg extended-release tablets described in Example 1 to an equivalent oral dose of the commercially available reference product, Sular® 40 mg extended-release tablets, when administered to healthy subjects.

TABLE 4Composition of SULAR ® (Formula...

example 3

Relative Bioavailability Study of Nisoldipine 40 mg Extended Release Tablets Under Fed Conditions

[0124] The objective of this study was to compare the food effect of the Formulation A described in Example versus the food effect of the Sular® market formulation. To determine the food effects for Formulation A and Sular, the pharmacokinetic data for these two formulations from Example 2 under fasting conditions were used as a reference. The same 32 subjects from Example 2 were enrolled in the food effect study.

[0125] Twenty-six (26) subjects completed the study. In the first period, subjects received the assigned treatment and received the alternate treatment during the subsequent period according to the randomization scheme. Dosing days were separated by a washout period of at least 7 days. An equal number of subjects were randomly assigned to each possible sequence of treatments. Blood samples were taken and analyzed as described in Example 2. Table 9 shows pharmacokinetic data fo...

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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

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority to U.S. Provisional Application No. 60 / 824,043, filed on Aug. 30, 2006 and U.S. Provisional Application No. 60 / 824,054, filed on Aug. 30, 2006.FIELD OF THE INVENTION [0002] This invention is generally in the field of controlled or modified release formulations of pharmaceutically active agents. BACKGROUND OF THE INVENTION [0003] A controlled release formulation is a pharmaceutical composition capable of releasing a drug at a pre-determined rate and / or at a pre-determined time after administration to maintain a desirable pharmacological activity for some desirable period of time. Such preparations provide a supply of a drug to the body during a predetermined period of time or at a predetermined absorption site and thus maintain drug levels in a therapeutic range for longer periods of time than conventional, e.g. immediate release formulations. [0004] Dosage forms comprising a core containing a drug disper...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/4418A61P9/00
CPCA61K9/2086A61K9/2866A61K9/2846A61K31/4422A61P43/00A61P9/00A61P9/10A61P9/12Y02A50/30A61K9/28A61K9/0053A61K9/2027A61K9/2886
Inventor GRENIER, PASCALNHAMIAS, ALAINVERGNAULT, GUY
Owner JAGOTEC AG
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