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Enhanced formulations of lamotrigine

A technology for lamotrigine preparations, applied in the field of enhanced lamotrigine preparations, capable of solving problems such as inability to enhance the release of lamotrigine

Inactive Publication Date: 2010-08-04
SUPERNUS PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this approach failed to enhance the release of lamotrigine in buffered media with a pH greater than or equal to 6.8

Method used

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  • Enhanced formulations of lamotrigine
  • Enhanced formulations of lamotrigine
  • Enhanced formulations of lamotrigine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment I

[0039] Example 1. Lamotrigine Immediate Release ("IR") Granules for Control

[0040] Table 1 provides the composition of two control formulations of lamotrigine IR particles (Formulation A and Formulation B). Formulations A and B were prepared as follows: The dry ingredients were mixed in a KG-5 high shear granulator (Key International, Englishtown, NJ). The granules were then extruded using a DG-L2Dome granulator (LCI Corporation, Charlotte, NC). The extrudate was pelletized using a QJ-400G pelletizer (LCI Corporation, Charlotte, NC). The granules were dried overnight in an oven at 40°C. Dissolution tests were carried out in acidic (pH 1.1) and phosphate buffer (pH 6.8) media. The dissolution profile is shown in image 3 with Figure 4 middle. Both formulations exhibited a pH-dependent release profile.

[0041]

Embodiment II

[0042] Embodiment II. Lamotrigine tablet composition of the present invention

[0043] Table 2 provides the composition of Formulation C according to the invention. The formulation was granulated using a Key high shear granulator with water as the granulation liquid. Drug and excipients were added to the bowl and dry mixed at a paddle speed of ~260 RPM for approximately 1 minute. A total of 112 g of deionized water was added to achieve granulation. The batch was dried in a fluidized bed dryer (GPCG-1) with a final product temperature not exceeding 50°C. The moisture content of the granules was measured using a moisture analyzer and was 1.53% by weight. The dried granules are screened through a No. 18 mesh screen, blended with magnesium stearate and compressed on a rotary tablet machine. The target tablet weight and hardness were 333 mg and 8-10 kp, respectively. Tablet dissolution was tested in acidic (pH 1.1), phosphate buffered saline (pH 6.8), and media switch in which...

Embodiment III

[0045] Example III. Lamotrigine extended release (CR-F, CR-M, and CR-S) clinical batches.

[0046] Three inventive samples were produced to provide fast, medium, and slow sustained release profiles (lamotrigine CR-F, CR-M, and CR-S, respectively). The compositions of these samples are given in Table 3. These samples were produced according to the same processing steps as provided in Example II. The product was used in human pharmacokinetic (PK) studies.

[0047]

[0048] Image 6 The dissolution profile of these samples in phosphate buffered saline medium (pH 6.8) is shown.

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Abstract

A once-a-day, extended-release formulation of lamothgine, exhibiting a significantly similar release rate throughout the Gl tract irrespective of the pH of the environment, is provided. The formulation comprises lamothgine, an organic acid, a release enhancing polymer and a release controlling polymer. The use of the formulation for the treatment of the neurological disorders is also disclosed.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Application 11 / 779,562, filed July 18, 2007, the disclosure of which is incorporated herein by reference in its entirety. Background of the invention [0003] Lamotrigine, whose chemical name is 3,5-diamino-6-(2,3-dichlorophenyl)-partial-triazine, is a phenyltriazine antiepileptic drug. The drug is typically used in monotherapy and as an additional anti-inflammatory drug for partial-onset seizures and primary and secondary generalized tonic-clonic seizures in adults and pediatric patients (ie, children ≥ 2 years of age). Adjunctive treatment with epilepsy drugs. Lamotrigine is also indicated for seizures associated with myoclonic agitation petit mals and as maintenance therapy for bipolar I disorder to delay emotional exacerbations in patients treated with standard therapies for acute emotional exacerbations (eg, Depression, mania, hypomania, mixed acute episodes). [0004] Lamot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K31/53
CPCA61K9/1652A61K9/2054A61K9/205A61K9/1617A61K9/1641A61K9/2027A61K9/1623A61K9/2031A61K9/1635A61P25/00A61P25/08A61P25/18A61P25/24
Inventor A·凯达纳K·爱德华兹P·P·布哈特
Owner SUPERNUS PHARM INC
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