Timed controlled-release amlodipine capsule and preparation method thereof

An amlodipine and time-controlled technology, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the increased risk of toxicity, difficulty in taking medication, drug tolerance, etc. problems, to achieve the effect of improving compliance, reducing the difficulty of taking medicine, and increasing compliance

Active Publication Date: 2014-04-02
RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Similarly, the therapeutic effects, toxic reactions, and internal processes of drugs also have time rhythms. For example, the best time for administration of high blood pressure is at 3 o'clock in the morning, which also brings difficulties to patients.
Traditional sustained-release preparations control the blood drug concentration at a certain effective level for a long period of time, which is likely to cause drug tolerance and addiction
Moreover, the sustained-release preparations continue to release the drug during the time period when the drug is not needed (that is, the peak valley period and the plateau period), which greatly increases the risk of toxicity

Method used

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  • Timed controlled-release amlodipine capsule and preparation method thereof
  • Timed controlled-release amlodipine capsule and preparation method thereof
  • Timed controlled-release amlodipine capsule and preparation method thereof

Examples

Experimental program
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preparation example Construction

[0028]1) Preparation of non-permeable capsules: Dissolve non-permeable capsule materials and plasticizers in organic solvents at a concentration of 9.5-12.0% (W / V). Organic solvents are methanol, ethanol, dichloromethane, At least one of chloroform, ether, ethyl acetate, acetone, and petroleum ether; fill the prepared solution into gastric-soluble capsules, volatilize the solvent in the refrigerator or at room temperature, soak in water after the solvent is evaporated, and remove the gastric-soluble capsule. Capsule body, that is, obtain a non-permeable capsule body with one end closed and one end open;

[0029] 2) Preparation of amlodipine powder or tablet core: the drug can be drug powder or tablet; mix amlodipine and excipients (filler, stabilizer, disintegrant, lubricant) uniformly to obtain drug powder, or The drug powder is directly compressed to form a tablet core;

[0030] 3) Preparation of time-delayed embolic tablets: mix the blocking agent, porogen and lubricant ev...

Embodiment

[0033] a) Preparation of non-permeable capsules

[0034] Dissolve 12.5 g of ethyl cellulose (EC) in 100 ml of mixed solvent (dichloromethane: absolute ethanol: ethyl acetate = 4: 0.8: 0.2) to prepare an ethyl cellulose solution with a mass concentration of 125 g / L , and then pour it into the No. 1 capsule so that the liquid level is flush with the mouth of the capsule. Quickly put it in a 4°C refrigerator to evaporate the solvent, then soak the outer capsule body in water to obtain a non-permeable capsule body.

[0035] b) Preparation of drugs

[0036]

[0037] Mix amlodipine besylate, microcrystalline cellulose, calcium hydrogen phosphate anhydrous, sodium carboxymethyl starch and magnesium stearate evenly according to the prescription amount.

[0038] c) Preparation of time-delayed embolic tablets

[0039]

[0040]

[0041]

[0042] Weigh hypromellose E-50, direct-pressed lactose, and magnesium stearate, mix them evenly, and press them into tablets with a 5.5...

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Abstract

The invention relates to a timed controlled-release amlodipine capsule and a preparation method thereof. The amlodipine capsule comprises an impervious capsule body, a floating aid, amlodipine powder or tablet, a time-lag embolism tablet and a gastric soluble capsule cap, wherein the impervious capsule body has a structure with one closed end and one opened end and is filled with the floating aid and the amlodipine powder or tablet, the time-lag embolism tablet is encapsulated at an opening of the impervious capsule body, and the gastric soluble capsule cap is used for covering the impervious capsule body. The timed controlled-release amlodipine capsule can lastingly float in gastric juice for a set time and then quickly release active pharmaceutical ingredients, the seepage phenomenon is not caused within the lag time, the active pharmaceutical ingredients-amlodipine are released after a certain time lag, the lag time and the time-lag reproducibility are effectively controlled by the components and the component ratio of the time-lag embolism tablet, and a drug release mechanism is that the time lag is controlled by dissolving the time-lag embolism tablet. Therefore, a patient can conveniently take medicines for treatment and the compliance of the patient with the treatment is improved.

Description

technical field [0001] The invention relates to an amlodipine time-selected controlled-release capsule and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Amlodipine is a dihydropyridine calcium antagonist (calcium antagonist or slow channel blocker). The contraction of cardiac and smooth muscles depends on the entry of extracellular calcium ions into the cells through specific ion channels. Amlodipine can selectively inhibit the transmembrane entry of calcium ions into smooth muscle cells and cardiomyocytes, and its effect on smooth muscle is greater than that on cardiac muscle. Its interaction with the calcium channel is determined by the progressive rate of its binding and dissociation to the receptor site, so the pharmacological effect occurs gradually. It is also a peripheral artery dilator, acting directly on vascular smooth muscle, reducing peripheral vascular resistance, thereby lowering blood pressure. Aml...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/4422A61K47/38A61K47/32A61K47/26A61K47/12A61K47/04A61P9/12A61P9/10
Inventor 沈梦妮周志亮陈叶明孙川棣胡玮
Owner RUNZE PHARMACEUTICAL (SUZHOU) CO LTD
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