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Manidipine hydrochloride compound

A technique for manidipine hydrochloride and compounds, applied in the field of manidipine hydrochloride compounds and their preparation, capable of solving the problems of unsatisfactory pharmacodynamics or pharmacokinetic performance of second-generation calcium antagonists

Active Publication Date: 2015-07-15
海思科制药(眉山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The second-generation calcium antagonists are divided into two subclasses. Class A is basically a slow-release and controlled-release preparation of the first-generation calcium antagonists, which is satisfactory for mild to moderate hypertension, while class B consists of several new second-generation calcium antagonists. Hydropyridine compounds with improved pharmacodynamic or pharmacokinetic properties, but the pharmacodynamic or pharmacokinetic properties of the second-generation calcium antagonists are still unsatisfactory

Method used

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  • Manidipine hydrochloride compound
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  • Manidipine hydrochloride compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The synthetic route of manidipine compound of the present invention sees attached figure 1 .

[0023] The total yield of the reaction is 81%. Its powder X-ray diffraction: using Cu-K radiation, the X-ray powder diffraction pattern is shown in the attached figure 2 ; Differential thermal analysis (DSC) diagram see attached image 3 .

Embodiment 2

[0024] The preparation of embodiment 2-compound tablet of the present invention

[0025] prescription:

[0026] Manidipine hydrochloride (embodiment 1)

10g

Hypromellose

2.5g

purified water

10g

lactose

80g

Poloxamer 188

7.5g

Magnesium stearate

0.5% of the total weight of the pellets

production

1000 pieces

[0027] Preparation method:

[0028] ① Pass manidipine hydrochloride through a 200-mesh sieve for later use, and pass lactose and hydroxypropyl methylcellulose through a 100-mesh sieve for later use;

[0029] ②Mix the prescription amount of lactose and hydroxypropyl methylcellulose evenly in equal increments, and set aside;

[0030] ③ Dissolve Poloxamer 188 in purified water, add manidipine hydrochloride and mix well, set aside;

[0031] ④ Add the mixture of lactose and hydroxypropyl methylcellulose into the high-efficiency wet granulator, stir and mix for 300 seconds, add the mixture ...

experiment example

[0032] Experimental example-clinical research of tablet of the present invention

[0033] In order to evaluate the effectiveness and safety of the Manidipine Hydrochloride Tablets of the present invention in treating mild to moderate essential hypertension, a randomized, double-blind, double-dummy, parallel-controlled multicenter phase II clinical study of Amlodipine Tablets was carried out. The results reported below.

[0034] 1. Clinical effectiveness research

[0035] A total of 238 cases were randomly enrolled in the test, of which 119 cases were enrolled in the test group, 11 cases were dropped out, and 108 cases were completed without elimination; 119 cases were enrolled in the control group, 7 cases were dropped out, 1 case was eliminated, and 111 cases were completed. Test group: half a tablet of manidipine hydrochloride (10 mg, Example 1) + 1 tablet of amlodipine analog tablet; the dosage of the drug was doubled for patients with unsatisfactory antihypertensive effec...

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Abstract

The invention provides a manidipine hydrochloride compound. Manidipine hydrochloride is a lipophilic third generation dihydropyridine calcium channel blocker, and is mainly used for inhibiting calcium influx by inhibiting L type calcium channels on vascular smooth muscle, so as to realize relaxation of vascular smooth muscle and reduce blood pressure.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a manidipine hydrochloride compound and a preparation method thereof. Background technique [0002] Hypertension is a cardiovascular and cerebrovascular disease that seriously threatens people's health. The incidence of hypertension has been on the rise in recent years, and tends to be younger. It not only has a high prevalence rate, but also easily causes damage to the heart, brain, kidney and other organs. It is the main risk factor for cerebrovascular accident and coronary heart disease, and seriously threatens human health and life. According to the statistics of the World Health Organization in 2006, there are 400 million hypertensive patients in the world, and the number of hypertensive patients in China has exceeded 100 million, with more than 3 million new patients every year. According to the forecast of the World Health Organization, by 2020, non-communica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90A61K31/496A61P9/12
Inventor 万华向志祥冯卫黄莎莎
Owner 海思科制药(眉山)有限公司
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