Sustained-release micro-pellet of trimetazidine and preparation process thereof

A technology of trimetazidine and sustained-release pellets, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Problems such as short concentration maintenance time

Inactive Publication Date: 2007-07-11
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are two disadvantages in the formation process of the controlled-release film: one is that the film-forming temperature of the film material is high, and a large amount of plasticizer must be added to promote the film-forming process, and the plasticizer has a great influence on the release behavior of the drug, which is very unfavorable. It is beneficial to maintain a stable drug release curve; the second is that if the water dispersion coating of the above-mentioned film material is used, heat treatment must be carried out at 40°C to 60°C for more than 24h after completion, which not only makes the process complicated, but also greatly increases the production cost. Drug stability is also unfavorable
[0024] The currently commercially available trimetazidine hydrochloride tablets (trade name: Wanshuangli) are rapidly absorbed after oral administration, and reach the peak plasma level in less than 2 hours. The elimination half-life is about 6 hours. It needs to be taken at least 3 times a day. Therefore, the blood drug concentration in the body is prone to "peak and valley" phenomenon, which not only maintains the effective blood drug concentration for a short time, but also has serious side effects and poor patient compliance.
Especially when taking the medicine at night, the time interval until the morning is long, and the blood drug concentration is very low in the morning, so the drug effect cannot be exerted smoothly

Method used

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  • Sustained-release micro-pellet of trimetazidine and preparation process thereof
  • Sustained-release micro-pellet of trimetazidine and preparation process thereof
  • Sustained-release micro-pellet of trimetazidine and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1 Preparation of pill core containing medicine

[0067] (1) Prescription:

[0068] Trimetazidine Hydrochloride 250g

[0069] Microcrystalline Cellulose 750g

[0070] 50% ethanol appropriate amount

[0071] (2) Preparation process:

[0072] Get trimetazidine crude drug, pulverize and pass through a 100-mesh sieve, add microcrystalline cellulose, and fully mix; add an appropriate amount of wetting agent (such as 50% ethanol) to the mixed material to make soft material; Put it into the extruder and extrude it into a strip-shaped extrudate; quickly add the extrudate to the spheronizer for spheronizing, and take it out after a certain period of time to make pellets; bake the prepared pellets at 50°C for 3~ After 6 hours, dry pellets were obtained. Results The micropills were smooth and spherical in appearance. At this time, capsules could be filled directly or film-coated with water-soluble coating materials to obtain immediate-release micropills.

Embodiment 2

[0074] Coat the pellet core (that is, uncoated immediate-release pellets) prepared in Example 1 with Kollicoat SR 30D to obtain trimetazidine sustained-release pellets.

[0075] (1) Prescription of coating solution:

[0076] Kollicoat SR 30D 100g

[0077] Propylene glycol 3g

[0078] Talc powder 12g

[0079] water 250g

[0080] (2) Preparation process:

[0081] Mix Kollicoat SR 30D and water evenly, add propylene glycol and talcum powder, stir at high speed and homogenize to obtain the coating solution. Using low-spray micro-fluidized bed equipment, add 120 g of uncoated trimetazidine immediate-release pellets of 18 to 24 meshes into the fluidization chamber, use a spray gun with a nozzle diameter of 1 mm, and adjust the fan frequency converter to make the blast flow approx. 125L·min-1, so that most of the pellets are blown up 7-12cm in the fluidization chamber, the atomizing gas pressure is adjusted to 0.2Mpa, and the flow rate of the constant flow pump is 0.9-1.2mL·min-...

Embodiment 3

[0084] The drug-containing pellet cores (ie uncoated immediate-release pellets) prepared in Example 1 were coated according to the following coating solution prescription to obtain trimetazidine sustained-release pellets.

[0085] (1) Prescription of coating solution:

[0086] Eudragit NE 30D 100g

[0087] 5% HPMC solution 8mL

[0088] Talc powder 40g

[0089] water 110g

[0090] (2) Preparation process:

[0091] Take Eudragit NE 30D, HPMC and talcum powder according to the above prescription, homogenize at a high speed, and then coat. After the clothes are finished, put them in a constant temperature oven at 40°C and dry them for 6 hours. 150 mg of coated pellets (equivalent to 35 mg of trimetazidine hydrochloride) was installed in each capsule, and the release rate was measured by the method described in Example 2, and the results are shown in Figure 2.

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Abstract

The invention relates to a slow-release micro drop whose active component is Humeitashen or other salt, wherein it is formed by element and film layer that controlling the drug release, whose weight ratio is 20:1-5:1; the Humeitashen content of element is 10-60%. The invention mainly uses protrusion method to prepare drop, and uses fluidize bed to pack.

Description

Technical field: [0001] The invention belongs to the technical field of drug sustained-release preparations, and specifically relates to a sustained-release pellet containing an active ingredient trimetazidine or a pharmaceutically acceptable salt thereof and a preparation method thereof. technical background: [0002] The chemical name of trimetazidine is 1-(2,3,4-trimethoxybenzyl)piperazine, and its structural formula is as follows: [0003] [0004] Trimetazidine can form a salt with acid. At present, its dihydrochloride has been widely used clinically at home and abroad, mainly for the preventive treatment of angina pectoris, and the auxiliary symptomatic treatment of vertigo and tinnitus. With the gradual deepening of clinical research, trimetazidine is expected to become the first-line anti-myocardial ischemia drug. [0005] Trimetazidine belongs to the class of other antianginal cardiovascular drugs. Trimetazidine prevents the decrease of intracellular ATP level ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22A61K9/52A61K31/495A61K47/38A61K47/34A61K47/32A61P9/10A61K47/10
Inventor 陈修毅
Owner SHANDONG INST OF PHARMA IND
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