Fast Dispersing Dosage Form Containing Levetiracetam

一种分散、快速的技术，应用在治疗对左乙拉西坦治疗上应答的疾病,病症或疾病状况,制备所述剂型领域，能够解决没有公开合适剂型、低脆性硬度等问题

Active Publication Date: 2019-01-15
APRECIA PHARMA LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] It would be advantageous to provide a rapidly dispersing orodispersible solid oral dosage form comprising levetiracetam which exhibits low friability and sufficient hardness to withstand storage and handling while exhibiting a very fast disintegration rate; No such suitable dosage form containing LEV is disclosed

Method used

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  • Fast Dispersing Dosage Form Containing Levetiracetam
  • Fast Dispersing Dosage Form Containing Levetiracetam
  • Fast Dispersing Dosage Form Containing Levetiracetam

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127] Embodiment 1 prepares the orodispersible dosage form of three-dimensional printing

[0128] The following method was used to prepare a three-dimensionally printed orodispersible dosage form comprising a matrix comprising LEVs. The composition and amounts used for the printing fluid and loose powder are as follows:

[0129]

[0130]

[0131] An incremental layer of loose powder of predetermined thickness is spread over the previous powder layer, and printing fluid is applied in droplets to bind the particles therein according to a predetermined saturation level, row spacing, and printing fluid flow rate. This two-step process was completed until a substrate containing the target amount of printed incremental layers was obtained.

[0132]Any three-dimensional printer device components known or described herein can be used, but these exemplary formulations can be prepared with a Coriolis Instrument (Dimatix / Spectra Technology Integration, model: CoriolisRP1). The p...

Embodiment 2

[0136] Example 2 Fast Dispersing Flakes with Altered Structure in Different Bulk Layers

[0137] Preparation of taste-masked three-dimensionally printed orodispersible dosage forms with altered structure in the bulking layer

[0138] According to the 3DP method described above, but it can be carried out in several different ways to prepare dosage forms of different structures varying in hardness and bulk layer composition. The following method provides a hardness of the upper and lower surfaces of the wafer that is greater than the hardness of the inner portion of the wafer. This strategy facilitates the generation of parts in flakes with different mechanical properties. This approach is used to design flakes where the composition of the top and bottom layers differs from that of the middle layer. This design results in flakes with stronger top and bottom layers, which increase hardness and reduce brittleness, and a large middle part with less hardness, which allows the flak...

Embodiment 3

[0149] The characterization of embodiment 3 dosage forms

[0150] The following method was used to characterize the 3D printed solid porous dispersion matrix.

[0151] brittleness

[0152] The resistance of the matrix to fracture was analyzed using the Tablet Friability Test (USP method ). The test used a VanKel brittleness tester (Model 45-2000, Varian, USA) equipped with a drum size of 285 mm in diameter and 39 mm in depth, rotated 100 times at 25 rpm. A minimum of 10 flakes are dropped per revolution through curved protrusions extending from the middle of the drum to the outer wall. Thus, at each inversion, the tablets are rolled or slid about 130 mm onto the drum or onto the tablets next to each other. All loose powder was removed from the tablet and the tablet was weighed before and after 100 cycles.

[0153] surface material

[0154] The matrix was inspected visually with or without a microscope. The surface texture is analyzed to determine whether it is rough ...

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Abstract

The present invention discloses a high dose rapidly dispersing three-dimensional printing dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water in a time period of less than about 10 seconds. Also disclosed are methods of making the dosage forms and methods of treating diseases, conditions or disorders that are therapeutically responsive to levetiracetam. The invention also provides methods for preparing the dosage forms.

Description

technical field [0001] The present invention relates to a fast dispersing (orodispersing) dosage form of levetiracetam. In particular, the dosage form disperses in a period of less than about 15 seconds when placed in the mouth of a subject. The invention also relates to methods of use of said dosage forms for the treatment of diseases, disorders or conditions that are therapeutically responsive to levetiracetam. The invention also provides a process for preparing said dosage form. Background technique [0002] Contains levetiracetam (LEV; (S)-2-(2-oxopyrrolidin-1-yl)butanamide; (-)-(S)-α-ethyl-2-oxo-1- Pyrrolidineacetamide; described in U.S. 4,943,639) is known in solid oral dosage forms (FDA Electronic Orange Book). Solid tablets are currently available under the trade name Obtained (NDA N021035, UCB, Inc., date of approval November 30, 1999; see the instructions in the package http: / / dailymed.nlm.nih.gov / dailymed / drugInfo.cfm? id=9870 ). These tablets are known...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4015
CPCA61K45/06A61K31/4015A61K9/0056A61K9/2095A61K9/2027A61P21/02A61P25/08A61P25/28A61K9/70A61K9/7007
Inventor J·雅各布斯N·夸勒T·G·韦斯特D·C·蒙克豪斯H·L·苏尔普勒南N·B·雅音
Owner APRECIA PHARMA LLC
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