Felodipine metoprolol succinate sustained-release tablet and preparation method thereof

A technology of metoprolol succinate and sustained-release tablets, which can be applied in the fields of pharmaceutical formulations, cardiovascular system diseases, block delivery, etc., and can solve the problems of easy local release, rupture of pellet sustained-release coating, irritation, etc. , to achieve an easily acceptable effect

Inactive Publication Date: 2015-03-25
NANJING KEKANG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this patent prepares it into a common preparation, which makes the blood drug concentration fluctuate greatly after the patient takes it, which will cause relatively large adverse reactions
[0006] In the patent of CN 102784143 A, a single-layer osmotic pump controlled-release preparation containing metoprolol and felodipine was applied for, which can realize the synchronous constant-rate release of metoprolol and felodipine, but the osmotic pump The production process of the preparation is complicated and the cost is high; and the individual differences in the body are large, and the release is unstable at the same time, whi

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Sustained Release Tablet Prescription (1000 Tablets)

[0035] Felodipine sustained-release granules:

[0036] Felodipine 5g

[0037] Polyoxyl 40 Hydrogenated Castor Oil 6g

[0038] Propyl gallate 0.5g

[0039] Lactose 50g

[0040] Hypromellose K100 LV 140g

[0041] Calcium carbonate 70g

[0042]85% ethanol 90g

[0043] Metoprolol succinate pellets:

[0044] Metoprolol Succinate 47.5g

[0045] Silica pellet core 20g

[0046] Povidone K 30 3g

[0047] Starch 2g

[0048] Ethylcellulose (10cps) 30g

[0049] Triethyl citrate 6g

[0050] Talc powder 8g

[0051] Hypromellose K100 LV (binder) 0.3 g

[0052] Hypromellose K100 LV (pore former) 3g

[0053] 70% ethanol 600g

[0054] Other additions:

[0055] Macrogol 6000 4g

[0056] Magnesium Stearate 3g

[0057] The preparation process is as follows:

[0058] Preparation of felodipine sustained-release granules:

[0059] Add felodipine and propyl galla...

Embodiment 2

[0070] Sustained Release Tablet Prescription (1000 Tablets)

[0071] Felodipine sustained-release granules:

[0072] Felodipine 5g

[0073] Polyoxyl 40 Hydrogenated Castor Oil 6g

[0074] Propyl gallate 0.5g

[0075] Lactose 80g

[0076] Hypromellose K100 LV 100g

[0077] Calcium hydrogen phosphate 90g

[0078] 85% ethanol 100g

[0079] Metoprolol succinate pellets:

[0080] Metoprolol Succinate 47.5g

[0081] Microcrystalline Cellulose Core 35g

[0082] Povidone K30 4g

[0083] Starch 2g

[0084] Ethylcellulose (10cps) 50g

[0085] Triethyl citrate 10g

[0086] Talc powder 8g

[0087] Hypromellose K100 LV (binder) 0.8 g

[0088] Hypromellose K100 LV (pore former) 5g

[0089] 70% ethanol 600g

[0090] Other additions:

[0091] Magnesium Stearate 6g

[0092] Preparation process is with embodiment 1.

Embodiment

[0093] Example 3 Comparison of Curve Similarity of Drug Release Curves

[0094] The comparison of the release profiles of controlled-release and sustained-release preparations can reflect the release

[0095] Differences in drug behavior. There are many methods for comparing the similarity of release curves reported in the literature, among which the similarity factor f 2 Recommended by the FDA as the preferred method for comparing the similarity of two dissolution profiles. f 2 It can be used as a parameter for evaluating the difference between the dissolution curves of preparations when the process or excipients in the prescription are changed, and as a parameter for evaluating the difference between the dissolution curves of the developed preparations and the commercially available preparations.

[0096] Similarity factor f 2 = 50log[[1+1 / n ∑ W t (R t -T t ) 2 ] -0.5 ×100]

[0097] where R t is the cumulative drug release percentage of the reference preparation a...

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Abstract

The invention relates to the field of pharmaceutical preparations and particularly relates to a felodipine metoprolol succinate sustained-release tablet and a preparation method thereof. The felodipine metoprolol succinate sustained-release tablet is prepared by the following steps: preparing metroprolol succinate into sustained-release pellets; mixing with felodipine sustained-release granules; and adding other auxiliary materials and tabletting. The sustained-release tablet is characterized in that the preparation comprises metoprolol pellets, felodipine sustained-release granules and other auxiliary materials. By adjusting the components and proportion of the felodipine sustained-release granules, not only can the release of felodipine be controlled, but also the release of metroprolol succinate can be adjusted. By adopting a special preparation process of pellet tablets, as the components in the formula are properly selected and proportioned, the felodipine metoprolol succinate sustained-release tablet is simple in preparation process, good in repeatability and easy for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a felodipine metoprolol succinate sustained-release tablet and a preparation method thereof, in particular to a method comprising metoprolol succinate sustained-release pellets, felodipine sustained-release granules and Sustained-release tablet of other auxiliary materials and preparation method thereof. Background technique [0002] Felodipine is a vasoselective calcium antagonist that lowers arterial blood pressure by reducing peripheral vascular resistance. Due to its high selectivity to arteriolar smooth muscle, it has no direct effect on myocardial contractility and cardiac conduction within the therapeutic dose range, and because it has no effect on venous smooth muscle and adrenergic vascular tension regulation, it does not cause orthostatic hypotension. This product has a slight natriuretic and diuretic effect, so it does not cause fluid retention. It is clinica...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/16A61K31/4422A61K31/138A61K47/38A61P9/12A61P9/00
Inventor 张栋张春霞
Owner NANJING KEKANG BIOTECH
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