BG860Y1 - Medicamentous form of dipyridamol - Google Patents

Abstract

The utility model relates to solid medicamentous form of dipyridamol which has improved adhesion of the coating to the tablet core, high values of the indicator degree of solubility of dipyridamol and such physicomechanical qualities of the tablet core enabling the process of pelleting to be made without any pervious isolation of the tablet cores. The medicamentous form, a coated tablet and a pellet of dipyridamol contains dipyridamol from 25 to 75 mg in a dosage form and lactose, the weight ratio between dipyridamol and lactose being from 1:0.5 to 1:1.5, gelatin from 0.8 to 1.5 wt.% and wheat starch up to 10 wt.% of the mass of the tablet core. The quantities of the lubrication and sliding substance as a sum amount up to 3.0% of the tablet mass.

Description

(54) DIPIRIDAMOL PHARMACEUTICAL FORM

Technical field

A useful model relates to the composition of a coated tablet and the dragee of 2,6-bis- (diethanolamino) -4,8-dipiperidino-pyrimido [5,4-b] pyrimidine or dipyridamole, which is widely used as a coronary vasodilator, as a means suppressing platelet aggregation.

BACKGROUND OF THE INVENTION

The solubility of dipyridamole in water is known to be highly dependent on the pH of the medium. It is known that upon administration of some oral dosage forms (DE 2 831164), large fluctuations in the level of dipyridamole in the blood are observed. These fluctuations are reduced by the inclusion in the oral dosage form of an acidic substance (DE 3124090), for example fumaric acid, tartaric acid, citric acid and the like. The other ingredients are sodium starch glycolate, polyvinylpyrrolidone, magnesium stearate.

According to EP0121901, the adjuvants to a mixture of dipyridamole, or a salt thereof, with a pharmaceutically acceptable acid, are: sodium starch glycolate, crospovidone, croscarmellose, polyvinylpyrrolidone, magnesium stearate, lactose, colloidal silica. The disadvantage of these compositions is that the granulation must be carried out by mixing with isopropanol, which is an environmentally undesirable reagent.

A known dosage form is dipyridamole, a dragee and coated tablet, containing as the drug substance dipyridamole 25 mg or 75 mg as excipients: lactose, wheat starch, colloidal silica, microcrystalline cellulose, talc, magnesium stearate, and dragee coating [R].

A disadvantage of this dosage form is the cracking of the dragees during the coating process and / or during storage.

The technical nature of the utility model

The problem is to create a stable and wrappingable dosage form containing dipyridamole from 25 to 100 mg and meeting the pharmacopoeial requirements for the degree of dissolution of dipyridamole from the dosage form.

According to a useful model, the dipyridamole tablets contain lactose in a weight ratio of dipyridamole / lactose - from 1 / 0.5 to 1 / 1.5; gelatin from 0.8 to 1.5 wt. % and wheat starch up to 10 wt. % by weight of the tablet core, with the amounts of lubricant and glidant (as a sum) up to 3.0 percent by weight of the tablet.

The beneficial effect is to improve the adhesion of the coating to the tablet core and to achieve high values of the dissolution rate of dipyridamole from the dosage form.

The dosage form is obtained by the method of wet granulation with aqueous gelatin solution and subsequent powdering and tabletting. The good physicomechanical properties of the tablet core allow the dredging process to be performed without first isolating the tablet cores.

Exemplary embodiments of the utility model

The composition is illustrated, without limitation, by the following exemplary compositions wherein the amounts are given in g:

Example 1 Example 2 Dipyridamole 0,0250 0,0250 Lactose 0,0368 0,0370 Microcrystalline cellulose 0,0066 0,0084 Wheat starch 0,0080 0,0060 Gelatin 0,0010 0,0006 Talc 0,0012 0,0016 Magnesium stearate 0,0008 0,0008 Colloidal silica 0,0006 0,0006

The weight of the new dosage form containing dipyridamole 25 mg has been reduced from 0.090 to 0.080 g, resulting in material savings and cheaper product.

Example 3 Example 4 Dipyridamole 0,0750 0,0750 Lactose 0,0460 0.0522 Microcrystalline cellulose 0,0095 - Wheat starch 0,0120 0,0150 Gelatin 0,0015 0,0018 Talc 0,0030 0,0030 Magnesium stearate 0,0015 0,0015 Colloidal silica 0,0015 0,0015

Claims

Claims (1)

Claims 1. Dosage form - tablet and coated tablet of 2,6-bis- (diethanolamino) -4,8-dipiperidino-pyrimido [5,4- (1] pyrimidine (dipyridamole), including excipients: lactose, wheat starch, colloidal silica, microcrystalline cellulose, magnesium stearate, characterized in that it contains dipyridamole from 25 to 75 mg in one dosage form and lactose, in weight ratios of dipyridamole / lactose - from 1 / 0.5 to 1 / 1.5; gelatin from 0.8 to 1.5 wt.% and wheat starch to Wt.% by weight of tablet core, the amounts of lubricant and glidant k a sum equivalent to up to 3.0% by weight of the tablet. Expert: M. Stankova Publication of the Patent Office of the Republic of Bulgaria 1797 Sofia, 52-B Dr. GM Dimitrov Blvd. Editor: E. Sinkova Cf. № 43496 Circulation: 40 CP