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Felodipine controlled release formulation and preparation method thereof

A technology for controlled release preparations and preparations, which is applied to non-active ingredients medical preparations, pharmaceutical formulas, and medical preparations containing active ingredients, etc. Patient's inconvenience and other problems

Active Publication Date: 2012-05-23
HANGZHOU MINSHENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the felodipine sustained-release tablet has a long action time and reduces the number of times of taking, it cannot control its delayed release for the "morning peak phenomenon" of hypertension
In short, the current felodipine preparations are difficult for hypertensive patients to avoid the dangerous moment in the morning, and getting up to take the medicine in the early morning has brought a lot of inconvenience to the life of the patients

Method used

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  • Felodipine controlled release formulation and preparation method thereof
  • Felodipine controlled release formulation and preparation method thereof
  • Felodipine controlled release formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of felodipine controlled-release preparation

[0045] Prescription (per 1000 tablets):

[0046] Tablet core: Felodipine 5g, HPMC K100LV19.5g, HPMC K100M6.5g, sodium chloride 22.75g, lactose 9.75g, crospovidone 6.5g, silicon dioxide 0.7g, medicinal ethanol 38.9g;

[0047] Coating layer: HPMC K100LV 180g, lactose 270g, magnesium stearate 2.25g, silicon dioxide 4.5g, medicinal ethanol 305g.

[0048] Preparation:

[0049] (1) Tablet cores are granulated separately and pressed into tablets (φ5.5mm shallow concave punch);

[0050] (2) The coating layer is granulated separately;

[0051] (3) Press-coated chips (φ12mm shallow concave punch): first fill part of the coating layer particles in the die hole, then place the tablet core in the center of the die hole, add the remaining coating layer particles, and then press to form a chip-coated chip.

[0052] Determination of in vitro release: according to the national drug standard WS 1 -(X-152)-2005Z Felodipine Su...

Embodiment 2

[0055] Preparation of felodipine controlled-release preparation

[0056] Prescription (per 1000 tablets):

[0057] Tablet core: Felodipine 5g, HPMC K100LV 19.5g, lactose 32.5g, crospovidone 13g, silicon dioxide 0.7g, medicinal ethanol 37.1g;

[0058] Coating layer: HPMC K100LV 180g, lactose 270g, magnesium stearate 2.25g, silicon dioxide 4.5g, medicinal ethanol 305g.

[0059] Preparation method: as described under Example 1.

[0060] In vitro release assay: as described under Example 1. The experimental data are shown in Table 2 and attached figure 2 .

[0061] The results showed that the release time of the drug was 5-6 hours after taking the drug, and the release time was up to 9 hours.

Embodiment 3

[0063] Preparation of felodipine controlled-release preparation

[0064] Prescription (per 1000 tablets):

[0065] Tablet core: Felodipine 5g, HPMC K100LV 48.75g, sodium chloride 13g, crospovidone 3.25g, silicon dioxide 0.7g, medicinal ethanol 40g;

[0066] Coating layer: HPMC K100LV 180g, lactose 270g, magnesium stearate 2.25g, silicon dioxide 4.5g, medicinal ethanol 305g.

[0067] Preparation method: as described under Example 1.

[0068] In vitro release assay: as described under Example 1. The experimental data are shown in Table 3 and attached image 3 .

[0069] The results showed that the release time of the drug was 5-6 hours after taking the drug, and the release time was 12 hours.

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Abstract

The invention provides a felodipine controlled release preparation for delaying the release and the preparation method thereof. The controlled release preparation can delay the release for 4 to 6 hours and then continue to release for some time to increase the duration time of a drug. Patients can take the drug before sleeping, the effective dosage of the drug is released continuously beginning from next morning, so that the effect of the drug and the occurrence of a disease appear at the same rhythm. As a result, the patients of high blood pressure can safely pass the high occurrence time ofcardiovascular events, which overcomes the inconvenience of common preparations cause by taking the drug early in the morning for the 'Morning Blood Pressure Surge' of high blood pressure.

Description

(1) Technical field [0001] The invention relates to a controlled-release preparation of antihypertensive drug felodipine and a preparation method thereof. (2) Background technology [0002] Felodipine (Fel) is a dihydropyridine calcium antagonist with extremely high selectivity to blood vessels. The drug can significantly lower blood pressure and total peripheral vascular resistance (TPR), increase coronary blood flow, improve cardiac function, without negative conduction and inotropic effects. The drug is well absorbed orally, and has a wide range of therapeutic doses (5-40 mg / day). It is mainly metabolized by the liver, and has no effect on metabolism in patients with renal insufficiency. The clinical research results show that it is effective in treating essential hypertension, etc., and has the advantages of long-term effect and less adverse reactions. These advantages make the drug a promising new calcium antagonist. [0003] The blood pressure of the human body show...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/4422A61K47/38A61K47/36A61P9/12
Inventor 骆快燕郭殿武徐伟良刘洋吴春霞
Owner HANGZHOU MINSHENG PHARM CO LTD
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