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Mexiletine Hydrochloride slow release reagent and preparing method thereof

A technology for mexiletine hydrochloride and sustained-release preparations, applied in the field of chemical pharmaceutical preparations, can solve the problems of unsatisfactory efficacy of mexiletine hydrochloride, high incidence of adverse drug reactions, and short duration of treatment effect, and improve medication compliance. , the effect of prolonging the duration of the curative effect and reducing the frequency of taking the medicine

Inactive Publication Date: 2007-09-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large fluctuation of blood drug concentration in the body of ordinary oral preparations (ordinary tablets and capsules), the peak-to-valley ratio is large, the peak concentration is easy to exceed the minimum toxic concentration, and the maintenance time within the therapeutically effective concentration range is relatively short, resulting in continuous therapeutic effect. The time is short, so the curative effect of mexiletine hydrochloride is unsatisfactory, and the incidence of adverse drug reactions is high; the common oral preparations that have been marketed usually need to be taken 3 to 4 times a day, and the number of times of taking medicine is many, which brings a lot of inconvenience to the patient. The phenomenon of missed doses is prone to occur, resulting in poor medication compliance of patients

Method used

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  • Mexiletine Hydrochloride slow release reagent and preparing method thereof
  • Mexiletine Hydrochloride slow release reagent and preparing method thereof
  • Mexiletine Hydrochloride slow release reagent and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Mexiletine Hydrochloride 100g

[0043] Hydroxypropyl Methyl Cellulose 122g

[0044] Lactose 124g

[0045] Micronized silica gel 2g

[0046] Magnesium Stearate 2g

[0047] Made into 1000 pieces

[0048] Preparation method: crush mexiletine hydrochloride, hydroxypropyl methylcellulose and other pharmaceutical excipients through a 100-mesh sieve, weigh according to the prescription, pass through an 80-mesh sieve for a second time and mix well, measure the content, and calculate the tablet weight , compressed into tablets with a circular die with a diameter of 8.0mm, the tablet shape is circular, each tablet contains 100mg of mexiletine hydrochloride, and the tablet weight is 350mg. After inspection, it is packaged to obtain mexiletine hydrochloride sustained-release tablets after passing the test.

[0049] test results:

[0050] Carry out according to " Chinese Pharmacopoeia " 2005 version about the rotating basket method of in vitro drug release test detection of su...

Embodiment 2

[0052] Mexiletine Hydrochloride 150g

[0053] Hydroxypropyl Methyl Cellulose 140g

[0054] Polyvinylpyrrolidone (PVP K30) 10g

[0055] 80% ethanol appropriate amount

[0056] Lactose 48g

[0057] Magnesium Stearate 2g

[0058] Made into 1000 pieces

[0059] Preparation method: Grind mexiletine hydrochloride, hydroxypropyl methylcellulose and other pharmaceutical excipients through a 100-mesh sieve respectively, weigh them according to the prescription amount, mix them uniformly by using the method of equal increments, and add 80% ethanol, to prepare soft material, pass the soft material through 18 mesh sieve to make granules, dry the wet granules at 55-65°C for 2 hours, granulate with 18 mesh sieve, add the prescribed amount of stearin to the dry granules after granulation Magnesium acid, mix well, measure the content, calculate the tablet weight, press the tablet with a circular die with a diameter of 8.0mm, the tablet shape is round, each tablet contains 150mg of mexile...

Embodiment 3

[0063] (1) Tablet core: Mexiletine hydrochloride 200g

[0064] 10% PVP K30 ethanol solution appropriate amount

[0065] Lactose 60g

[0066] Magnesium Stearate 2g

[0067] (2) Coating solution: ethyl cellulose 25%

[0068] Polyethylene glycol (PEG) 10%

[0069] Dibutyl sebacate (DBS) 30%

[0070] Appropriate amount of purified water

[0071] Made into 1000 capsules

[0072] Preparation method: crush mexiletine hydrochloride and lactose through a 100-mesh sieve respectively, weigh according to the prescription amount, and mix uniformly using the method of equal volume increments. Add an appropriate amount of 10% PVP K30 ethanol solution to the above-mentioned homogeneously mixed materials to prepare a soft material , pass the soft material through a 18-mesh sieve to make granules, dry the wet granules at 55-65°C for 2 hours, and sieve the granules with an 18-mesh sieve, add the above-mentioned si...

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Abstract

The slow released mexiletine hydrochloride preparation consists of mexiletine hydrochloride as active component in 20-70 wt%, slow releasing material in 10-60 wt%, and medicinal supplementary material. It is prepared into slow released tablet or capsule through sieving the materials, mixing, pelletizing, and tabletting or encapsulating. It has both fast releasing and slow releasing feature, fast acting, high bioavailability, long acting period, taking safety and other advantages.

Description

Technical field: [0001] The invention relates to the field of chemical pharmaceutical preparations, discloses a pharmaceutical composition containing mexiletine hydrochloride as an active ingredient, in particular to a mexiletine hydrochloride slow-release preparation for oral treatment of arrhythmia and a preparation method. Background technique: [0002] Arrhythmia (Cardiac arrhythmia) is a common clinical symptom of the cardiovascular system. Arrhythmia can occur regardless of whether the heart has organic disease. . Heart disease, systemic blood and electrolyte disorders, and autonomic nervous system dysfunction may change the electrophysiological state of the myocardium and become the direct and indirect causes of arrhythmia. This factor can induce arrhythmia in a single form, and can also interfere with the normal electrical activity of the myocardium at the same time, leading to the occurrence of arrhythmia. Clinically, most patients with myocardial infarction will ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/20A61K9/48A61K31/138A61P9/06
Inventor 阮邹荣单江
Owner ZHEJIANG UNIV
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