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Treatment composition containing amlodipine series salt and pril medicament

A kind of technology of amlodipine salt and composition, which is applied in the field of combined medicine kits, can solve the problems such as lack of solubility, intractable benzenesulfonic acid, slow onset of amlodipine and the like

Inactive Publication Date: 2010-02-24
BEIJING ROCK PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, amlodipine besylate does not have good enough solubility in water, especially when it is close to the physiological pH7.4 state. As we all know, amlodipine itself has the weakness of slow onset of action, which will further affect amlodipine The bioavailability and onset time of dipine, in addition, amlodipine besylate does not have sufficient photostability and high temperature stability
At the same time, the use of benzenesulfonic acid in the production process has disadvantages, namely, benzenesulfonic acid is difficult to handle industrially due to its corrosion and toxicity, and its highly hygroscopic nature also requires specific transportation and use steps

Method used

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  • Treatment composition containing amlodipine series salt and pril medicament
  • Treatment composition containing amlodipine series salt and pril medicament
  • Treatment composition containing amlodipine series salt and pril medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1 General Preparation Method of Benazepril Hydrochloride / Amlodipine Niacin Common Tablets

[0089] Benazepril hydrochloride and nicotinic acid amlodipine were crushed separately, passed through a 80-mesh sieve, and set aside; lactose, microcrystalline cellulose, pregelatinized starch, sodium carboxymethyl starch, povidone K30, cross-linked carboxymethyl cellulose Sodium plain and magnesium stearate are passed through 80 mesh sieves respectively, and set aside.

[0090] Make povidone K30 or pregelatinized starch into a suitable viscosity adhesive with pure water. In addition to magnesium stearate, mix other raw materials and auxiliary materials according to the equal incremental dilution method, and then use the prepared adhesive to make a soft material, dry below 80°C, granulate, and add stearic acid in the prescribed amount Magnesium, mixed evenly, compressed into tablets. Or mix the raw materials and auxiliary materials of the prescribed amount, ...

Embodiment 2

[0091] Example 2 General Preparation Method of Benazepril Hydrochloride / Amlodipine Series Salt Compound Capsules

[0092] The compound capsules include 6 dosage combinations of benazepril hydrochloride and amlodipine nicotinate, respectively including amlodipine nicotinate (calculated as amlodipine base) and benazepril hydrochloride (calculated as benazepril hydrochloride) Total) 2.5mg / 10mg, 5mg / 10mg, 5mg / 20mg, 10mg / 20mg, 5mg / 40mg and 10mg / 40mg. Its preparation method is as follows (preparation amount is 1000):

[0093]

[0094]

[0095] The capsule core of benazepril hydrochloride is firstly prepared, and the preparation method is as follows: pulverizing and mixing benazepril hydrochloride, lactose and pregelatinized starch, and then adding water to make granules. The wet granules are then sieved and dried. Then mix and pulverize with crospovidone and microcrystalline cellulose. The resulting mixture is then compressed into capsule cores. The capsule core is...

Embodiment 3

[0096] Embodiment 3 Light fastness experiment

[0097] The pharmaceutical composition of the research product amlodipine series salts (5 mg) and benazepril hydrochloride (80 mg) is as described in Examples 1-4 (specifically the following table). The research article and the reference article (amlodipine besylate / benazepril hydrochloride composition) were exposed to an incandescent lamp (220V, 100W) at 50°C and placed 30cm above the sample for 4 weeks, and then each combination was measured related substances. From the above results, it is obvious that, compared with the reference substance, the study product exhibits the same effect except the L-amlodipine aspartic acid / benazepril hydrochloride and amlodipine maleate / benazepril hydrochloride compositions. Improved light fastness (arranged from high stability to low stability in the following table according to the stability of the related substance-related compositions produced).

[0098] Table 2....

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Abstract

The invention relates to an amlodipine series salt, which particularly comprises nicotinate, camsilate, pyroglutamate, L-aspartate, maleate and mesylate. The invention also relates to a pril compoundor a pharmaceutical composition of a medicinal salt of the pril compound and a preparation method thereof, and a drug combination medicine box containing a composition of the amlodipine series salt and a composition of sartan compounds. The composition of the invention comprises the following components: a) a certain amount of an amlodipine salt; b) a certain amount of the pril compound or a medicinal salt of the pril compound; and c) a medicinal carrier or a diluting agent. The composition or the medicine box can be used for treating the patients suffering from hypertension, angina pectoris,atherosclerosis, and / or hypersphyxia and treating the patients (including the human beings) having heart danger symptoms.

Description

technical field [0001] The present invention relates to amlodipine series salts, specifically including nicotinate, camphorsulfonate, pyroglutamate, L-aspartate, maleate and methanesulfonate, and the Composition and preparation method thereof, the present invention also relates to a medicine kit comprising the amlodipine series salt composition and the combined drug of pril. The above compositions or kits can be used to treat patients with hypertension, angina pectoris, atherosclerosis, and / or combined hypertension and patients with cardiac risk symptoms (including humans). Background technique [0002] Hypertension has become one of the main killers endangering human health. At present, the incidence of hypertension in some European and American countries has reached 20%. According to statistics, 43 million people in the United States suffer from hypertension; the average incidence of hypertension in my country is 11.88%, and more than 140 million people in my country suff...

Claims

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Application Information

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IPC IPC(8): A61K31/4422A61K45/00A61P9/12A61P3/10A61P9/04A61K31/55A61K31/40A61K31/675A61K31/401A61K31/472A61K31/404
Inventor 王海勇陈艳明付俊昌
Owner BEIJING ROCK PHARMA
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