Pulsatile drug delivery system for treating morning akinesia

A drug and pulse release technology, applied in the directions of drug delivery, drug combination, capsule delivery, etc., can solve the problem of undetermined ER preparation scores, and achieve the effect of improving nighttime sleep patterns

Pending Publication Date: 2019-04-26
康特拉医药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] ER combination formulations maintain plasma levodopa concentrations longer in the therapeutic window, providing patients with longer ON time and

Method used

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  • Pulsatile drug delivery system for treating morning akinesia
  • Pulsatile drug delivery system for treating morning akinesia
  • Pulsatile drug delivery system for treating morning akinesia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0280] Mix lactose with microcrystalline cellulose, sodium starch glycolate, and model compound (niacinamide) in a drum mixer for 5 minutes. Then magnesium stearate was added and mixed for 30 seconds. The mixture was compressed into tablets, each tablet having a weight of 6.6 mg, a size of 2 mm, and each tablet containing 0.28 mg of model compound. The tablet thickness is about 1.7 mm.

[0281] lactose

[0282] The model compound mini-tablets were film-coated with a semipermeable membrane based on ethylcellulose in a fluidized bed. The film composition is given in the table below. For 325g chips, 1000g film solution is produced to enable film coating to the desired tablet weight increase of up to 25.0%, including a 10% production loss excess. The spraying conditions are controlled so that the outlet air temperature is 28-30°C. To achieve the required weight gains of 20%, 23%, and 25%, 682.0 g, 784.9 g, and 853.1 g membrane solution were applied, respectively.

[0283] E...

Embodiment 2

[0286] The microtablets of Example 1 were film-coated with an ethylcellulose-based semipermeable membrane in a fluidized bed. The film composition is given in the table below. For 325g chips, 1000g of membrane solution is produced to enable film coating to the required tablet weight increase of up to 25.0%, including a 10% production loss excess. The spraying conditions are controlled so that the outlet air temperature is 28-29°C. To achieve the required weight gains of 10%, 15%, 20%, and 25%, 341.3g, 511.9g, 682.5g, and 853.1g membrane solutions were applied, respectively.

[0287] Ethyl cellulose 7cps

[0288] The USP2 paddle device was used to test the dissolution of 44 microtablets. Each container contains 600 ml isotonic sodium chloride solution and is rotated at 75 rpm. The re-taken samples were quantified on a spectrophotometer at 260 nm. Result in Figure 3A Shown in.

Embodiment 3

[0290] As described in Example 2, the microtablets of Example 1 were film-coated with the following film composition:

[0291] Ethyl cellulose 7cps

[0292] Test the mini-tablets as described in Example 2 and the results are in Figure 3B Given in.

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Abstract

Provided herewith is a pharmaceutical composition comprising, separately or together, a pulsatile release component comprising levodopa and a DOPA decarboxylase inhibitor for the management of OFF-time episodes in patients with Parkinson's disease.

Description

Technical field [0001] The present invention relates to a pulsed drug delivery system, which can delay the burst release of levodopa and DOPA decarboxylase inhibitors (including carbidopa) in the small intestine, thereby improving the management of morning exercise inability in patients with Parkinson's disease. Background technique [0002] Dyskinesia is often caused by impaired regulation of dopamine neurotransmission. Parkinson's disease (PD) is an example of dyskinesia associated with dysfunction of dopamine neurotransmission, which is caused by the progressive degeneration of dopamine neurons. In order to replace the lost dopamine, oral levodopa (L-DOPA, a precursor of dopamine) is currently used to treat PD motor symptoms. Oral levodopa must be emptied from the stomach and absorbed in the proximal small intestine. Levodopa is converted into dopamine in the brain and stored in neurons until the body needs it for exercise. It remains the single most effective agent for mana...

Claims

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Application Information

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IPC IPC(8): A61K31/165A61K31/194A61K31/195A61K31/198A61K9/00A61P25/16
CPCA61K31/165A61K31/194A61K31/195A61K31/198A61K9/1652A61K9/2054A61K9/2059A61K9/2081A61K9/2866A61K9/4808A61P25/16A61P43/00A61K9/2013A61K9/2072A61K9/2077A61K9/2833A61K45/06A61K9/2018A61K9/2027A61K9/2086
Inventor J·B·汉森M·S·汤姆森A·V·富勒顿本特·霍嘉德P·G·尼尔森
Owner 康特拉医药股份有限公司
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