Methods for treating cardiovascular disorders

一种心血管、疾病的技术，应用在治疗心血管疾病领域，能够解决难以实现治疗性释放、高溶解性和高渗透性、难以配制缓释等问题

Inactive Publication Date: 2014-07-02
WOCKHARDT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been found that due to the high solubility and high permeability of metoprolol, it is difficult to formulate and obtain sustained release of a once-daily formulation in a matrix dosage form
Furthermore, the preparation of fixed-dose combinations containing extended-release metoprolol is a significant challenge because of the difficulty in achieving the desired therapeutic release of the combination when combined into a single unit dosage form

Method used

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  • Methods for treating cardiovascular disorders
  • Methods for treating cardiovascular disorders
  • Methods for treating cardiovascular disorders

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0154]Embodiment 1: Metoprolol succinate ER / amlodipine besylate tablet

[0155] Table 1: Metoprolol succinate ER / Amlodipine besylate; Eq50mg tartrate / 10mg

[0156]

[0157]

[0158] method:

[0159] The microcrystalline cellulose spheres were provided with a capping layer I of ethyl cellulose. These block-coated pellets were subjected to metoprolol succinate layering with a binder in an aqueous solvent. Drug layered pills with Ethylcellulose and Opadry have ER Coating-I. Sustained release coating of Eudragit-II was provided using plasticizer, triethyl citrate and talc. The ER coated pellets were provided with a seal coat II followed by a PEG coat in a suitable solvent system. These PEG-coated pellets were mixed with Prosolv, amlodipine besylate, croscarmellose sodium, PEG and sodium stearyl fumarate and compressed into tablets. Coat the core tablet with Opadry.

[0160] Dissolution studies were performed on the tablets obtained from Example 1. The results of the...

Embodiment 2

[0163] Embodiment 2: Metoprolol succinate ER / amlodipine besylate tablet

[0164] Table 3: Metoprolol succinate ER / Amlodipine besylate; Eq25mg tartrate / 2.5mg

[0165]

[0166]

[0167] method:

[0168] The microcrystalline cellulose spheres were provided with a capping layer I of ethyl cellulose. These block-coated pellets were subjected to metoprolol succinate layering with a binder in an aqueous solvent system. Drug-layered pills with Ethylcellulose and Opadry had ER Coating-I. Sustained release coating-II of Eudragit was provided with plasticizer, triethyl citrate and talc. The ER coated pellets were provided with a seal coat II followed by a PEG coating in a suitable solvent system. These PEG coated pellets were mixed with Prosolv, croscarmellose sodium, PEG and sodium stearyl fumarate and compressed into tablets. Coat the core tablet with Opadry.

[0169] Dissolution studies were performed on the tablets obtained from Example 2. The results of the dissolutio...

Embodiment 3

[0173] Embodiment 3: Metoprolol succinate ER / amlodipine besylate tablet

[0174] Table 5: Metoprolol succinate ER / Amlodipine besylate; Eq25mg tartrate / 5m x

[0175]

[0176]

[0177] method:

[0178] The microcrystalline cellulose pellet spheroids were provided with an ethyl cellulose seal layer I. These block-coated pellets were subjected to metoprolol succinate layering with a binder in an aqueous solvent system. Drug-layered pills with Ethylcellulose and Opadry had ER Coating-I. Sustained release coating-II of Eudragit was provided with plasticizer, triethyl citrate and talc. The ER coated pellets were provided with a seal coat II followed by a PEG coating in a suitable solvent system. These PEG coated pellets were mixed with Prosolv, croscarmellose sodium, PEG and sodium stearyl fumarate and compressed into tablets. Using Opadry as a binder, the prepared metoprolol succinate core tablet was coated with amlodipine besylate. Prepared core tablets were coated w...

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PUM

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Abstract

There is provided a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more calcium channel blocker, angiotensin II receptor blocker or angiotensin converting enzyme inhibitor along with one or more rate controlling excipient.

Description

field of invention [0001] The present invention relates to a once-daily therapeutically synergistic pharmaceutical dosage form for the treatment of cardiovascular disease, wherein said dosage form comprises sustained-release metoprolol (metoprolol) and one or more calcium channel blockers, angiotensin A fixed dose combination of an II receptor blocker or an angiotensin converting enzyme (ACE) inhibitor and one or more rate controlling excipients. Background of the invention [0002] "Cardiovascular disease or cardiovascular disorder" is intended to mean any cardiovascular disease or cardiovascular disorder known in the art, including congestive heart failure, diabetes-related complications, hyperhomocysteinemia, hypercholesterolemia disease, atherosclerosis, inflammatory heart disease, valvular heart disease, restenosis, hypertension (such as pulmonary hypertension, unstable hypertension, essential hypertension, low renin hypertension, salt-sensitive hypertension , low reni...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/135A61K31/41A61K31/4422A61K38/55A61P9/00A61P9/12
CPCA61K31/4418A61K31/41A61K31/138A61K45/06A61K31/40A61P9/00A61P9/04A61P9/10A61P9/12A61P13/12A61P25/28A61K31/135A61K2300/00A61K31/4422
Inventor M·M·科古勒P·D·纳克哈特A·古普塔G·K·简恩
Owner WOCKHARDT LTD
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