CN105055352A - Trimetazidine hydrochloride tablets and preparation method thereof - Google Patents

Abstract

The invention belongs to the technical field of medicine and particularly relates to trimetazidine hydrochloride tablets and a preparation method thereof. The trimetazidine hydrochloride tablets are prepared from raw materials as follows: trimetazidine hydrochloride, filler, a binder, a lubricant and a wetting agent. The trimetazidine hydrochloride tablets solve the problems of poor compressibility and difficulty in forming of the trimetazidine hydrochloride as the raw material. The invention further provides the preparation method of the trimetazidine hydrochloride tablets. The compressibility of the prepared trimetazidine hydrochloride tablets is improved, the trimetazidine hydrochloride tablets are formed easily, the use value of the trimetazidine hydrochloride tablets can be increased better, trimetazidine hydrochloride is prepared into tablets to facilitate taking of a patient, pain of the patient can be relieved timely, the process is simple, the quality is stable, a production process meets the requirement of GMP (Good Manufacture Practice of Drugs), and the trimetazidine hydrochloride tablets and the preparation method are applicable to industrial mass production.

Description

Trimetazidine Hydrochloride Tablets in healthy and preparation method thereof

Technical field

The invention belongs to medical art, be specifically related to a kind of Trimetazidine Hydrochloride Tablets in healthy and preparation method thereof.

Background technology

Trimetazidine Hydrochloride Tablets in healthy is clinical is applicable to arteria coronaria functional defect, angina pectoris, the angina pectoris that hemodynamics drug treatment alone is invalid, diabetic coronary artery disease, old myocardial infarction etc.Trimetazidine Hydrochloride Tablets in healthy belongs to other class antianginal cardiovascular drugses; trimetazidine is by the energy metabolism of Cell protection under anoxia or ischemia; stop the decline of intracellular ATP levels; thus ensure that the normal function of ionic pump and the normal operation of permeable membrane sodium-potassium stream, maintain the stable of intracellular environment.Zooscopy finds: trimetazidine: help to maintain heart and the energy metabolism of neural sensation organ in ischemia and hypoxia situation.The change of the permeable membrane ion flow reducing intracellular acidosis and caused by ischemia.While this effect of generation, hematodinamics is had no significant effect.Its curative effect is reliable, and side effect is little, toleration.The Trimetazidine Hydrochloride Tablets in healthy of auspicious positive pharmaceutical manufacturing enjoys a good market both at home and abroad market, relieves slight illness to countless patient.Also good economic benefit and social benefit is achieved.

Angina pectoris is coronary insufficiency, cardiac muscle sharply, caused by ischemia and anoxia be the clinical syndrome of main manifestations with ictal chest pain or chest discomfort.Update shows, and China's cardiovascular patient prevalence is in lasting ascent stage, reaches 2.3 hundred million before ill total number, on average just has 1 people to suffer from heart disease in every 5 adults.The patient that cardiovascular diseases's disease is died from the whole nation every year has 3,500,000.The paathogenic factor that to be all the cardiovascular risk factors of generally acknowledging at present the be cardiovascular disease such as smoking, diabetes, hypertension, obesity, hyperlipidemia is important, along with the increase of living-pattern preservation and operating pressure, cardiovascular patient prevalence is in lasting ascent stage.

Summary of the invention

Bad for existing Trimetazidine Hydrochloride compressibility, the shortcoming that molding is more difficult, the object of this invention is to provide a kind of Trimetazidine Hydrochloride Tablets in healthy, compressibility strengthens, easy-formation, better can improve the use value of Trimetazidine Hydrochloride Tablets in healthy, the present invention also provides its preparation method, technique is simple, steady quality.

A kind of Trimetazidine Hydrochloride Tablets in healthy, be made up of the raw material of following parts by weight:

Trimetazidine Hydrochloride 2.2-2.4 part, filler 6.0-6.2 part, binding agent 0.4-0.5 part, lubricant 0.3-0.4 part and wetting agent 1.2-1.4 part.

Wherein:

Binding agent is selected from ethyl cellulose, PVP K30, one or more in polyethylene glycol 6000, methylcellulose or hypromellose; Binding agent effectively can play adhesive effect, adds compressibility.

Filler be selected from starch, pregelatinized Starch, lactose, microcrystalline Cellulose, dextrin or mannitol one or more.

Lubricant be selected from Pulvis Talci, magnesium stearate, silicon dioxide or Stepanol MG one or more.

Wetting agent is selected from one or more of arabic gum alcoholic solution or tragakanta alcoholic solution.Wherein: it is 20% arabic gum alcoholic solution that arabic gum alcoholic solution is preferably concentration; Tragakanta alcoholic solution is preferably the tragakanta alcoholic solution that concentration is 20%.

The preparation method of described Trimetazidine Hydrochloride Tablets in healthy, is prepared by following preparation method:

(1) Trimetazidine Hydrochloride is crossed 22 order mesh screens;

(2) Trimetazidine Hydrochloride, filler and binding agent mix homogeneously that step (1) obtains is taken;

(3) add wetting agent, granulate with 18 order mesh screens, dry, granulate;

(4) add lubricant always mixed rear tabletting, obtain Trimetazidine Hydrochloride Tablets in healthy.

The present invention adopts effective ingredient and special solid preparation adjuvant to prepare Trimetazidine Hydrochloride Tablets in healthy, and adopt filler and wetting agent synergism, filler brings out cohesive through wetting agent, adds compressibility; Lubricant adds the mobility of granule simultaneously, indirectly adds compressibility.

The invention solves the problem that the compressibility of Trimetazidine Hydrochloride is poor, make Trimetazidine Hydrochloride make tablet easily, be conducive to playing its therapeutic effect.

The present invention compared with prior art, has following beneficial effect:

(1) the invention solves raw material Trimetazidine Hydrochloride compressibility bad, the shortcoming that molding is more difficult, Trimetazidine Hydrochloride Tablets in healthy compressibility prepared by the present invention strengthens, easy-formation, better can improve the use value of Trimetazidine Hydrochloride Tablets in healthy, making tablet facilitates patient to take, and is conducive to removing patient's slight illness in time.

(2) Trimetazidine Hydrochloride Tablets in healthy preparation method technique of the present invention is simple, steady quality, and production process meets the requirement of GMP, is applicable to industrialized great production.

(3) Trimetazidine Hydrochloride Tablets in healthy that prepared by the present invention is conducive to giving full play to Trimetazidine Hydrochloride Tablets in healthy therapeutical effect, can be used for the prophylactic treatment of angina pectoris attacks, the complementary symptomatic treatment of dizzy and tinnitus, this medicine is the stronger anti-anginal drug of effect, and the persistent period is longer.There is the effect to antiadrenergic drug, norepinephrine and vassopressin, can vascular resistance be reduced, increase coronary flow and surrounding loop blood flow, promote the generation of myocardial metabolism and cardiac energy.Heart working load can be lowered simultaneously.Reduce the consumption of myocardial oxygen consumption and cardiac energy, thus improve the equilibrium of supply and demand of myocardium oxygen.Still can increase the toleration to cardiotonic glycoside.

Detailed description of the invention

Below in conjunction with embodiment, the present invention will be further described.

Embodiment 1

1, prescription

2, technique

Trimetazidine Hydrochloride is crossed 22 order mesh screens.2.2kg Trimetazidine Hydrochloride, 2.8kg microcrystalline Cellulose, 3.4kg pregelatinized Starch and 0.4kg polyethylene glycol 6000 mix homogeneously is taken by prescription.Add the tragakanta alcoholic solution that 1.3kg concentration is 20%, granulate with 18 order mesh screens, dry, granulate.Add 0.3kg Stepanol MG and 0.1kg magnesium stearate always mixed after tabletting namely obtain Trimetazidine Hydrochloride Tablets in healthy of the present invention.

Embodiment 2

1, prescription

2, technique

Trimetazidine Hydrochloride is crossed 22 order mesh screens.2.4kg Trimetazidine Hydrochloride, 2.7kg mannitol, 3.3kg lactose and 0.5kg methylcellulose mix homogeneously is taken by prescription.Add the arabic gum alcoholic solution that 1.4kg concentration is 20%, granulate with 18 order mesh screens, dry, granulate.Add 0.15kg silicon dioxide and 0.15kg Pulvis Talci always mixed after tabletting namely obtain Trimetazidine Hydrochloride Tablets in healthy of the present invention.

Embodiment 3

1, prescription

2, technique

Trimetazidine Hydrochloride is crossed 22 order mesh screens.2.3kg Trimetazidine Hydrochloride, 2.9kg dextrin, 3.2kg lactose and 0.4kg hypromellose mix homogeneously is taken by prescription.Add the arabic gum alcoholic solution that 1.2kg concentration is 20%, granulate with 18 order mesh screens, dry, granulate.Add 0.1kg Stepanol MG and 0.2kg Pulvis Talci always mixed after tabletting namely obtain Trimetazidine Hydrochloride Tablets in healthy of the present invention.

Embodiment 4

1, prescription

2, technique

Trimetazidine Hydrochloride is crossed 22 order mesh screens.2.2kg Trimetazidine Hydrochloride, 2.4kg starch, 3.6kg dextrin and 0.5kg ethyl cellulose mix homogeneously is taken by prescription.Add the tragakanta alcoholic solution that 1.3kg concentration is 20%, granulate with 18 order mesh screens, dry, granulate.Add 0.2kg Stepanol MG and 0.1kg silicon dioxide always mixed after tabletting namely obtain Trimetazidine Hydrochloride Tablets in healthy of the present invention.

Embodiment 5

1, prescription

2, technique

Trimetazidine Hydrochloride is crossed 22 order mesh screens.2.4kg Trimetazidine Hydrochloride, 6.1kg microcrystalline Cellulose and 0.4kg PVP K30 mix homogeneously is taken by prescription.Add the arabic gum alcoholic solution that 1.4kg concentration is 20%, granulate with 18 order mesh screens, dry, granulate.Add 0.3kg magnesium stearate always mixed after tabletting namely obtain Trimetazidine Hydrochloride Tablets in healthy of the present invention.

According to the relevant regulations of national Bureau of Drugs Supervision standard YBH13562005 and CP2010, detect the product that embodiment 1-5 prepares, concrete outcome is in table 1.

The testing result of the product that table 1 embodiment 1-5 prepares

Sample source	Dissolution	Weight differential	Hardness	Friability	Disintegration
						Embodiment 1	98％	2.3％	112.7N	0.49％	6.5min
Embodiment 2	99％	3.5％	124.1N	0.43％	5.7min
						Embodiment 3	97％	4.1％	131.4N	0.34％	6.2min
Embodiment 4	101％	3.3％	119.3N	0.38％	5.2min
						Embodiment 5	100％	3.2％	109.9N	0.51％	6.0min

Claims (8)

1. a Trimetazidine Hydrochloride Tablets in healthy, is characterized in that: be made up of the raw material of following parts by weight:

Trimetazidine Hydrochloride 2.2-2.4 part, filler 6.0-6.2 part, binding agent 0.4-0.5 part, lubricant 0.3-0.4 part and wetting agent 1.2-1.4 part.

2. Trimetazidine Hydrochloride Tablets in healthy according to claim 1, is characterized in that: binding agent is selected from ethyl cellulose, PVP K30, one or more in polyethylene glycol 6000, methylcellulose or hypromellose.

3. Trimetazidine Hydrochloride Tablets in healthy according to claim 1, is characterized in that: filler be selected from starch, pregelatinized Starch, lactose, microcrystalline Cellulose, dextrin or mannitol one or more.

4. Trimetazidine Hydrochloride Tablets in healthy according to claim 1, is characterized in that: lubricant be selected from Pulvis Talci, magnesium stearate, silicon dioxide or Stepanol MG one or more.

5. Trimetazidine Hydrochloride Tablets in healthy according to claim 1, is characterized in that: wetting agent is selected from one or more of arabic gum alcoholic solution or tragakanta alcoholic solution.

6. Trimetazidine Hydrochloride Tablets in healthy according to claim 5, is characterized in that: arabic gum alcoholic solution is concentration is 20% arabic gum alcoholic solution.

7. Trimetazidine Hydrochloride Tablets in healthy according to claim 5, is characterized in that: tragakanta alcoholic solution to be concentration be 20% tragakanta alcoholic solution.

8. a preparation method for the arbitrary described Trimetazidine Hydrochloride Tablets in healthy of claim 1-7, is characterized in that: be prepared by following preparation method:

(1) Trimetazidine Hydrochloride is crossed 22 order mesh screens;

(2) Trimetazidine Hydrochloride, filler and binding agent mix homogeneously that step (1) obtains is taken;

(3) add wetting agent, granulate with 18 order mesh screens, dry, granulate;

(4) add lubricant always mixed rear tabletting, obtain Trimetazidine Hydrochloride Tablets in healthy.