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Niraparib oral controlled-release and sustained-release pharmaceutical composition and uses thereof

A technology for controlled release drugs and compositions, which is applied in the field of PARP enzyme inhibitor drugs and niraparib sustained and controlled release pharmaceutical compositions, and can solve problems that have nothing to do with research on oral sustained and controlled release preparations of niraparib.

Inactive Publication Date: 2018-06-26
SCI RAINBOW BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] According to the patent search, there is no preparation patent related to niraparib at present, and there is no related research on oral sustained-release preparations of niraparib. In order to further improve the clinical efficacy of niraparib, precisely control its blood drug Concentration and enzyme inhibition level, reduce the adverse reactions of tumor patients after medication, improve the compliance of patients taking medication, and reduce storage and production costs. The invention discloses a niraparib pharmaceutical composition with controllable release behavior in vivo

Method used

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  • Niraparib oral controlled-release and sustained-release pharmaceutical composition and uses thereof
  • Niraparib oral controlled-release and sustained-release pharmaceutical composition and uses thereof
  • Niraparib oral controlled-release and sustained-release pharmaceutical composition and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0086] The preparation method of Niraparib osmotic pump controlled-release tablet comprises the following steps: 1. preparation of Niraparib in improved dissolution form; 2. preparation of drug-containing layer; 3. preparation of push layer; 4. preparation of double-layer tablet; Preparation of the selected double-layer isolation coating; ⑥ Preparation of the controlled-release coating; ⑦ Perforation of the controlled-release coating of the osmotic pump tablet; ⑧ An optional aesthetic coating layer; ⑨ An optional immediate-release drug-containing layer. The above ②-⑨ can be carried out by conventional pressing and coating methods well known to those skilled in the art.

[0087] The tablet with the immediate-release drug-containing layer outside the rigid membrane shell is an osmotic pump rapid-sustained double-release tablet, while the tablet without an immediate-release drug-containing layer outside the rigid membrane shell is an ordinary osmotic pump controlled-release tablet...

specific Embodiment

[0126] The following examples generally describe the preparation methods and / or characterization results of typical compositions of the present invention, and all percentages are by weight unless otherwise indicated. The following examples are specific illustrations of the present invention, but should not be considered as limiting the scope of the present invention. In the following examples, various procedures and methods not described in detail are conventional methods well known in the art.

[0127] Experimental animals: 6 Beagle dogs, half male and half male, weighing 8-10 kg. The sources are all from Beijing Masi Biotechnology Co., Ltd. The test animals were adaptively fed in the experimental site of the Experimental Animal Center of Shanghai Institute of Materia Medica 14 days before the test day.

[0128] Using a single-punch tablet press (TDP-1, Guangzhou Xulang Machinery Equipment Co., Ltd.)

Embodiment 1

[0129] Example 1 Fast and slow double-effect release matrix tablet (200 tablets)

[0130]

[0131] Immediate-release layer: After the prescription amount of Niraparib is mixed with the solubilizing matrix excipient Soluplus and micropowder silica gel, it is prepared into a solid dispersion by melt extrusion, crushed, and passed through a 60-mesh sieve. Agent crospovidone PVPP XL and lubricant magnesium stearate are mixed evenly and ready for tableting;

[0132] Sustained-release layer: Niraparib of prescription quantity and solubilization matrix excipient copovidone (PVP VA64) and micropowder silica gel are prepared into solid dispersion with the above-mentioned melt extrusion method, and then with the release rate adjustment of prescription quantity with slow release layer Release matrix material HPMC K15M (BASF, Germany) and lubricant magnesium stearate, mix well, and wait for tabletting.

[0133] Tablet compression: the direct compression method is used to make matrix t...

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Abstract

The invention discloses a niraparib oral controlled-release and sustained-release pharmaceutical composition and uses thereof. According to the presebt invention, by regulating the niraparib release behavior, the in vivo absorption rate and the absorption time of niraparib can be controlled, and the blood concentration and the blood concentration fluctuation range of niraparib in vivo can be regulated, such that the in vivo PARP enzyme inhibition activity of niraparib can be efficiently and permanently provided so as to provide the antitumor treatment effect in the high-efficiency and low-toxicity manner; a purpose of the present invention is to control the in vivo blood concentration and the efficacy providing of niraparib through the controlled-release and sustained-release preparation so as to improve the treatment effect of the drug and reduce the toxic-side effect of the drug; and the efficient and long-acting PARP enzyme activity inhibition pharmaceutical composition is providedfor patients, wherein the antitumor effect is improved, the acting time is long, the compliance is good, and the toxic-side effect is low.

Description

technical field [0001] The present invention relates to the field of biopharmaceuticals, in particular to a sustained and controlled release pharmaceutical composition of niraparib and its use in the preparation of PARP enzyme inhibitors for DNA repair deficient tumors. The composition according to the present invention has Controlled release behavior, in vivo plasma concentration and PARP enzyme inhibitory activity. Background technique [0002] Niraparib (Niraparib), chemical name: (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide, molecular formula C 19 h 20 N 4 O, with a molecular weight of 320.39, has the following chemical structure: [0003] [0004] Niraparib is a PARP enzyme inhibitor developed by the American biopharmaceutical company Tesaro. At the end of June 2016, Tesaro broke the news of major new drug research. The results of the Phase III clinical trial of the new anti-cancer drug Niraparib are surprisingly good Unexpectedly, this also caused ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62A61K9/24A61K31/454A61P35/00A61P35/04
CPCA61K9/0002A61K9/2081A61K9/2086A61K9/5084A61K31/454A61P35/00A61P35/04A61K31/4439
Inventor 不公告发明人
Owner SCI RAINBOW BIOPHARMA CO LTD
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