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Sustained releasing minipills of diltiazem hydrochloride and its preparation

A diltiazem hydrochloride, sustained-release technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, cardiovascular system diseases, etc., can solve the problem of not considering the rhythm of hypertensive angina pectoris, large-dose burst release, and preparation safety. Sexual Influence, etc.

Active Publication Date: 2004-11-17
KAMP PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN1133709 discloses a preparation method of diltiazem hydrochloride controlled-release tablets. Diltiazem hydrochloride controlled-release tablets are a unit dosage form and have the possibility of large-dose burst release, which may cause great danger to the patient's body and greatly affect the safety of the preparation. It has an impact, and diltiazem hydrochloride controlled-release tablets do not take into account the chronological rhythm of the onset of hypertensive angina pectoris. This dosage form only achieves the purpose of sustained release in the traditional sense, without combining the rhythm of disease onset and the chronopharmacological characteristics of therapeutic drugs. To achieve the purpose of time release

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Diltiazem hydrochloride delayed-release pellet capsule and preparation method thereof:

[0046] The first pellet:

[0047] Dosage (one dose)

[0048] Blank ball core: sucrose and starch (1:1) 115mg

[0049] Drug layer: diltiazem hydrochloride 90mg

[0050] Hypromellose E3 (HPMC E3) 5mg

[0051] Swelling layer: Hypromellose E5 (HPMC E5) 40.9mg

[0052] Sodium Lauryl Sulfate 10mg

[0053] Controlled release layer: ethylcellulose aqueous dispersion (surelease®) 34mg

[0054] The second pellet:

[0055] Blank ball core: sucrose and starch (1:1) 115mg

[0056] Drug layer: diltiazem hydrochloride 90mg

[0057] Hypromellose E3 (HPMC E3) 5mg

[0058] Swelling layer: Hypromellose E5 (HPMC E5) 40.9mg

[0059] Sodium Lauryl Sulfate 5mg

[0060] Controlled release layer: ethylcellulose aqueous dispersion (surelease®) 78.5mg

[0061] The preparation method is as follows: step 1, 16 g of diltiaze...

Embodiment 2

[0073] The first pellet:

[0074] Blank core: sucrose and dextrin (1:1) 167mg

[0075] Drug layer: diltiazem hydrochloride 90mg

[0076] Methylcellulose 2.5mg

[0077] Hypromellose E3 2.5mg

[0078] Swelling layer: Hypromellose E5 (HPMC E5) 51.4mg

[0079] Tween 20 12.9mg

[0080] Controlled release layer: ethylcellulose aqueous dispersion (surelease®) 61.7mg

[0081] The second pellet:

[0082] Blank core: sucrose and dextrin (1:1) 167mg

[0083] Drug layer: diltiazem hydrochloride 90mg

[0084] Methylcellulose 2.5mg

[0085] Hypromellose E3 2.5mg

[0086] Swelling layer: Hypromellose E5 (HPMC E5) 51.4mg

[0087] Tween 20 6.4mg

[0088] Controlled release layer: ethylcellulose aqueous dispersion (surelease®) 98.7mg

[0089] The preparation method is the same as in Example 1, and the mixing ratio of the two pellets is 1:1.

[0090] test results:

[0091] Dissolution rate of the first pellet:

[0092] Time: 6 hours ...

Embodiment 3

[0101] The first pellet:

[0102] Blank core: microcrystalline cellulose 115mg

[0103] Drug layer: diltiazem hydrochloride 90mg

[0104] Povidone 5mg

[0105]Swelling layer: hydroxypropylmethylcellulose E5 (HPMC E5) 20mg

[0106] Low-substituted hydroxypropyl cellulose 20mg

[0107] Tween 80 10mg

[0108] Controlled release layer: ethylcellulose aqueous dispersion (surelease®) 34mg

[0109] The second pellet:

[0110] Blank core: microcrystalline cellulose 115mg

[0111] Drug Layer: Diltiazem Hydrochloride 90mg

[0112] Povidone 5mg

[0113] Swelling layer: Hypromellose E5 (HPMC E5) 20mg

[0114] Low-substituted hydroxypropyl cellulose 20mg

[0115] Tween 80 5mg

[0116] Controlled release layer: Ethylcellulose aqueous dispersion (surelease®) 78.5 mg

[0117] The preparation method is the same as in Example 1, and the mixing ratio of the two pellets is 3:4.

[0118] Dissolution rate of the first pellet:

[01...

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PUM

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Abstract

The invention discloses a Diltiazem Hydrochloride slow release type micro-drop pill and the process for preparation, which comprises mixing two or more Diltiazem Hydrochloride micro-drop pills by a finite proportion, packing into hard gelatin capsule or pressing into tablet. The preparation can be used for the prevention and cure of hypertension and stenocardia diseases triggered by blood pressure and heart rate rise within several hours after getting up.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a delayed-release and then sustained-release dosage form of diltiazem hydrochloride, namely diltiazem hydrochloride delayed-release pellets. Background technique [0002] Diltiazem hydrochloride [chemical name: cis-(+)-5-[(2-dimethoxyphenyl)-3-acetoxy-2,3-dihydro-1,5-benzothiazem-4 (5H)-Kone hydrochloride], white or off-white crystal or crystalline powder, odorless, bitter, soluble in water, methanol or chloroform, insoluble in ether or benzene. As a calcium ion antagonist, diltiazem hydrochloride is related to the inhibition of calcium ion influx when the myocardium and vascular smooth muscle are depolarized. It can relax vascular smooth muscle, reduce peripheral vascular resistance, and lower blood pressure; The degree is related, and those with normal blood pressure only have a slight drop in blood pressure. It can effectively dilate the epicardial and subendocard...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/52A61K31/554A61P9/10A61P9/12
Inventor 朱家壁陈盛君
Owner KAMP PHARMA
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