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Lisinopril controlled-release tablet and preparation method thereof

A slow-release tablet and delayed-release technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, drug combinations, etc., can solve the problems of complex preparation process, affecting the stability of preparations, and many coating ingredients

Inactive Publication Date: 2013-04-03
石雷 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The release mechanism of this system is unique, but there are many coating ingredients and the preparation process is complicated. The characteristics of rhythm changes in hypertension and the design of drug administration

Method used

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  • Lisinopril controlled-release tablet and preparation method thereof
  • Lisinopril controlled-release tablet and preparation method thereof
  • Lisinopril controlled-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Lisinopril delayed-release sustained-release tablets, which are composed of a core containing lisinopril and a coating layer wrapped around the core. The weight of each tablet core is 200 mg. The coating layer The weight gain is 8.7mg, calculated based on the total weight of the tablet, the coating layer accounts for 4.2% of the total weight of the tablet. In this embodiment, the dosage of the following prescriptions containing lisinopril-containing tablet cores and coating layers is calculated according to the amount of 1500 tablets, and the prescription of the described tablet cores containing lisinopril is as follows:

[0046] Lisinopril: 45g;

[0047] Lactose: 120g;

[0048] Hydroxypropyl methylcellulose (HPMC K4M): 120g;

[0049] Polyvinylpyrrolidone (PVP): 9.0g;

[0050] Magnesium stearate: 3.0g;

[0051] Micronized silica gel: 3.0g.

[0052] The prescription of the coating layer is as follows:

[0053] Ethyl cellulose: 10g;

[0054] Polyethylene glycol: 3.0g.

[0055] The pre...

Embodiment 2

[0060] Lisinopril delayed-release sustained-release tablets, which are composed of a core containing lisinopril and a coating layer wrapped around the core. The weight of each tablet core is 200 mg. The coating layer The weight gain is 9.3mg, calculated based on the total weight of the tablet, the coating layer accounts for 4.4% of the total weight of the tablet. In this embodiment, the dosage of the following prescriptions containing lisinopril-containing tablet cores and coating layers is calculated according to the amount of 1500 tablets, and the prescription of the described tablet cores containing lisinopril is as follows:

[0061] Lisinopril: 45g;

[0062] Microcrystalline cellulose: 75g;

[0063] Hydroxypropyl methylcellulose (HPMC K4M): 165g;

[0064] Polyvinylpyrrolidone (PVP): 9.0g;

[0065] Magnesium stearate: 3.0g;

[0066] Micronized silica gel: 3.0g.

[0067] The prescription of the coating layer is as follows:

[0068] Ethyl cellulose: 10g;

[0069] Polyethylene glycol: 4.0...

Embodiment 3

[0075] Lisinopril delayed-release sustained-release tablets, which are composed of a core containing lisinopril and a coating layer wrapped around the core. The weight of each tablet core is 200 mg. The coating layer The weight gain is 9.3mg, calculated based on the total weight of the tablet, the coating layer accounts for 4.4% of the total weight of the tablet. In this embodiment, the dosage of the following prescriptions containing lisinopril-containing tablet cores and coating layers is calculated according to the amount of 1500 tablets, and the prescription of the described tablet cores containing lisinopril is as follows:

[0076] Lisinopril: 45g; starch: 120g; hydroxypropyl methylcellulose (HPMC K15M): 120g; ethyl cellulose: 9.0g; magnesium stearate: 3.0g; micronized silica gel: 3.0g.

[0077] The prescription of the coating layer is as follows:

[0078] Cellulose acetate: 10g; polyethylene glycol: 4.0g.

[0079] The preparation method of lisinopril delayed-release sustained-r...

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Abstract

The invention relates to a lisinopril controlled-release tablet and a preparation method thereof, belonging to the field of pharmaceutic preparation technology and solving the problem that existing lisinpopril controlled-release tablet cannot delay release and release mildly. The tablet consists of core of the tablet containing lisinopril and a coating wrapped outside the core of the tablet, the core of the tablet containing the lisinopril comprises the following components by weight percent: 5.0%-20% of lisinopril, 25%-55% of framework material, 20%-50% of filler, and1.0%-3.0% of lubricant, the coating comprises the following components in weight percent: 60%-90% of water insoluble coating material and 10%-40% of pore-foaming agent. The method comprises the preparation of core of the tablet containing lisinpopril, the preparation of coating liquor, and the preparation of the tablet by wrapping the coating liquor outside the core of table so as to form the coating. The lisinopril controlled-release tablet can delay release and release mildly, and the method is simple and beneficial to industrialization.

Description

Technical field [0001] The invention relates to a lisinopril preparation, more specifically to a lisinopril delayed-release sustained-release tablet and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] The chemical name of lisinopril is N-{N-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl}-L-proline, and its molecular formula is C 21 H 31 N 3 O 5 , The molecular weight is 405.49, and its chemical structure is as follows: [0003] [0004] Lisinopril is a new generation of angiotensin-converting enzyme inhibitors. It lowers blood pressure by inhibiting the renin-angiotensin-aldosterone system and is mainly suitable for the treatment of essential hypertension. [0005] However, the onset of hypertension has the characteristics of a circadian rhythm. The blood pressure of the human body shows rhythmic changes within 24 hours. It rapidly rises to the peak within a few hours after waking up in the morning, and drops to t...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K9/36A61K38/05A61K47/38A61K47/36A61P9/12
Inventor 吴悦昀石雷陈丹丹潘佩瑶
Owner 石雷
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