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Tablet containing olmesartan medoxomil and amlodipine and preparation method of tablet

A technology of olmesartan medoxomil and amlodipine besylate, which is applied in the field of tablets containing olmesartan medoxomil and amlodipine and its preparation, can solve the problem of low overall level of blood drug concentration, limited complementary effect, and poor blood drug concentration. problems such as low concentration, to achieve the effect of reducing the incidence of adverse drug reactions, increasing the dissolution rate, and reducing the incidence

Active Publication Date: 2013-04-03
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, because amlodipine besylate is almost insoluble in water, it is slowly absorbed in the human body, and generally reaches the peak blood concentration 6-12 hours after taking the medicine, and the overall level of blood drug concentration is low, especially the initial blood drug concentration after administration. Concentrations are very low; whereas olmesartan medoxomil reaches peak plasma concentration within 1-2 hours of administration
Apparently, in the common compound preparation of amlodipine besylate and olmesartan medoxomil, the time difference between the two active ingredients when they reach the peak plasma concentration after simultaneous administration is relatively far, and the synergistic, additive and complementary effects are very limited. And there are adverse reactions such as dizziness and lower extremity edema

Method used

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  • Tablet containing olmesartan medoxomil and amlodipine and preparation method of tablet
  • Tablet containing olmesartan medoxomil and amlodipine and preparation method of tablet
  • Tablet containing olmesartan medoxomil and amlodipine and preparation method of tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dissolve 50g of amlodipine besylate in 2.2L of dichloromethane, add 436g of hydroxypropyl methylcellulose, stir to dissolve, and rotate to evaporate below 45°C. After dichloromethane is evaporated, quickly pour it into a petri dish and lay it flat. Place it in the freezer layer of the refrigerator for about 5 hours, then freeze-dry it for 20 hours, wait for embrittlement, take it out and pulverize it and pass it through an 80-mesh sieve to obtain a solid dispersion of amlodipine besylate.

Embodiment 2

[0026] Dissolve 50g of amlodipine besylate in 1.7L of methanol, add 520g of hydroxypropyl methylcellulose, stir to dissolve, and rotate to evaporate below 45°C. After evaporating methanol, quickly pour it into a petri dish and spread it in a freezer layer. Stand for about 6 hours, then freeze-dry for 24 hours, wait for embrittlement, take out and pulverize and pass through an 80-mesh sieve to obtain amlodipine besylate solid dispersion. Example 3

Embodiment 3

[0027]

[0028] Preparation process: Weigh and mix the amlodipine besylate solid dispersion prepared in Example 1, olmesartan medoxomil, mannitol, lactose, sodium carboxymethyl starch and magnesium stearate, and press into 1000 tablets.

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PUM

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Abstract

The invention discloses a tablet containing olmesartan medoxomil and amlodipine. The tablet is prepared from amlodipine besylate solid dispersion, olmesartan medoxomil and pharmaceutic adjuvants, wherein the amlodipine besylate solid dispersion consists of amlodipine besylate and hydroxypropyl methyl cellulose according to the weight rate of 1: (7-12). The amlodipine besylate in the compound tablets can be rapidly dissolved out and absorbed by organisms; and after orally taken by hypertensive, the olmesartan medoxomil and amlodipine-containing tablet plays the roles of enhancing the synergistic hypotensive effect of two active ingredients and remarkably reducing the adverse drug reaction.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a tablet containing olmesartan medoxomil and amlodipine and a preparation method thereof. Background technique [0002] The occurrence of hypertension is caused by various factors such as hyperactivity of the sympathetic nervous system, renal water and sodium retention, and activation of the renin-angiotensin-aldosterone system (RAAS), and the existing antihypertensive drugs can only target a certain pathogenesis The mechanism works, and the antihypertensive effective rate of any antihypertensive drug is only 25%-50%. In order to effectively control blood pressure, 70% of hypertensive patients need to use antihypertensive drugs in combination. The 2007 European Society of Hypertension (ESH) / European Society of Cardiology (ESC) hypertension guidelines pointed out that the initial blood pressure is grade 2 or 3 hypertension, and patients with normal ...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K31/4178A61K9/20A61P9/12
Inventor 蔡萧芳晋伟
Owner NANJING CHIA TAI TIANQING PHARMA
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