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Controlled release solid oral dosage formulations comprising nisoldipine

A technology for oral preparations and preparations, which is applied in the field of controlled release preparations and can solve the problems of high side effects and expensive instruments.

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

AI Technical Summary

Problems solved by technology

[0006] Although the pericentric technique has been shown to be safe for delivery of calcium channel blockers, studies have shown that the pericentric system has slightly higher side effects than other drug delivery systems, particularly in relation to the drug nifedipine (Defina et al. , Ann Pharmacother. 31(7-8):819-822(1997))
The core-wrapping technique also requires the use of specific instruments, which can be expensive

Method used

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  • Controlled release solid oral dosage formulations comprising nisoldipine
  • Controlled release solid oral dosage formulations comprising nisoldipine
  • Controlled release solid oral dosage formulations comprising nisoldipine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] Example 1. Three-layer tablet containing 40 mg of nisoldipine

[0124] 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 Eudragit S100 (methacrylic acid copolymer type B) and Eudragit Combination of L100 (methacrylic acid copolymer type A). Formulations A and B as OPADRY from Colorcon, West Point, PA II seal coat for coating.

[0125] Table 1 Components of Formulation A

[0126]

[0127]

[0128] Table 2 Components of Formulation B

[0129]

[0130]

[0131] Table 3 Components of Formulation C

[0132]

[0133] The formulations described above were prepared as follows:

[0134] core or central layer

[0135] 1. Stir nisoldipine and sodium lauryl sulfate in a high shear mixer for two minutes. Lactose monohydrate, povidone...

Embodiment 2

[0158]Embodiment 2. The study of relative bioavailability of Nisoldipine 40mg extended-release tablet under fasting conditions

[0159] 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 SULAR Delayed-release nisoldipine (40 mg). SULAR is a core-wrapped formulation consisting of a core containing nisoldipine coated with an immediate release coat also containing nisoldipine. SULAR is given in Table 4 components and their concentrations.

[0160] 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 (SULAR 40mg extended-release tablet) absorption rate and oral bioavailability.

[0161] T...

Embodiment 3

[0185] Embodiment 3. The relative bioavailability research of Nisoldipine 40mg extended-release tablet under feeding conditions

[0186] The objective of this study was to compare the formulation A described in the examples with the market formulation SULAR food effect. To determine formulation A and SULAR The pharmacokinetic data of these two preparations under fasting conditions in Example 2 are used as a reference. The same 32 individuals from Example 2 were recruited for the food effect study.

[0187] 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 formulation A (treatment E) a...

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Abstract

Controlled release oral dosage formulations containing calcium channel blockers, and methods of use thereof, are provided for the once-a-day treatment of cardiovascular disorders, such as hypertension, angina, and cardiac arrhythmia. The active agent is preferably a dihydropyridine calcium channel blocker, such as nisoldipine. The formulation provides an increase in the bioavailability of the calcium channel blocker as compared to the bioavailability of the calcium channel blocker in other drug delivery formulations known in the art. In one embodiment, the formulation provides an increase in the bioavailability of the calcium channel blocker, nisoldipine, as compared to the same dose of nisoldipine in the coat-core version of the drug (SULAR TM ). The formulation can be in the form of a trilayer tablet containing a core or central layer and one or more barrier layers.

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 to controlled release formulations containing calcium channel blockers and methods of their use. More particularly, the present methods and compositions relate to oral dosage forms containing nisoldipine for the once-a-day treatment of hypertension and other cardiovascular disorders. Background technique [0003] Calcium channel blockers are a class of heterogeneous drugs that prevent or slow calcium entry into cells by modulating cellular calcium channels (Remington, The Science and Practice of pharmacy, Nineteenth Edition, Mack Publishing Company, Eaton, Pa., p.963( 1995). The regulation of calcium entry into the cells of the cardiovascular system is of great importance for the normal functioning of this system. Cardiac and vascu...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K9/36A61K9/16A61K9/24A61K9/26A61K31/4422
Inventor G·韦尼奥P·格勒尼耶A·尼安米斯
Owner JAGOTEC AG
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