TWI252762B - A long-term effective pharmaceutical preparation containing tamsulosin and preparation thereof - Google Patents

Abstract

This invention relates to a long-term effective pharmaceutical preparation containing tamsulosin, which comprises an effective amount of tamsulosin or pharmaceutically acceptable salt, 10 to 65% (w/w) hydrophobic macromolecular cellulose as a release modulator, 20 to 65% (w/w) circular particle forming agent, and 10 to 40% (w/w) diluent. This invention also relates to a producing method for long-term effective pharmaceutical preparation containing tamsulosin, comprising: (a) mixing effective amount of tamsulosin or pharmaceutically acceptable salt, 10 to 65% (w/w) hydrophobic macromolecular cellulose as release modulator, 20 to 65% (w/w) circular particle forming agent, and 10 to 40% (w/w) diluent; (b) annealing the mixture of (a) and appropriate solvent; and (c) squeezing the result of (b) for granulation.

Description

1252762 发明, INSTRUCTION DESCRIPTION: TECHNICAL FIELD OF THE INVENTION The present invention relates to Tamsulosin long-acting dosage forms and methods of manufacture. [Prior Art] The tamsulosin action sequence is to reduce the prostatic pressure of the intraurethral pressure curve by blocking the urethra and the anterior glandular r-receptor, thereby improving the urinary dysfunction associated with prostatic hypertrophy. According to U.S. Patent No. 4,772,475, an acrylic polymer or an acrylic acid copolymer or a cellulose derivative is added to a conventional tamsulosin oral sustained release microparticle drug as a sustained release agent, and more than 5% is added. Percent by weight of microcrystalline cellulose. However, in the process of making the pellets, the addition of a high percentage of microcrystalline cellulose causes excessive friction when the composition is mixed, which causes the temperature of the production process to rise, and the acrylic polymer to form a gel at high temperatures. Not conducive to process and pellet formation. Therefore, there is a need for a problem that can mix the same sentence while overcoming the high temperature in the process and difficult to granulate in the process, so that the manufactured drug can have a stable drug effect, and the sustained release effect of Tamsuloxin (Tamsui〇) The pharmaceutical composition of the sin) substance allows the composition to maintain the pharmacological properties of the original active substance for use by a patient. SUMMARY OF THE INVENTION The present invention relates to a long-acting dosage form comprising Tamsul Gsin comprising an effective amount of tamsulosin or a pharmaceutically acceptable salt thereof: 10-65% (w/w ) Cellulose hydrophobic polymer compound as a release rate regulator and 20-65% (w/w) round granule forming agent and i〇_4〇% (w/(7) dilution

Claims (1)

1252762 Picking up, harvesting, profit-making range: 1. A long-acting, right-effect, sorrowful, sirloin containing Tamsulosin or its pharmaceutically acceptable 蹯65% (w/w) The fiber cone goes to _ & , > phoenix, 10·, ', ί staff "water-based polymer compound as a release agent and 2 0 - 6 S. / , /, double-buy control pot / 〇 (W / W) Round granule forming agent and l〇-4〇% (W/w) diluent; /, medium, and davidin hydrophobic polymer compound is selected from the group consisting of sodium cellulose, sodium benzoate S_ 'IM 6 Cellulose, propyl propyl fluorene fiber ^ in the group of propylmethylcellulose acetate succinate and acetic acid 0 benzene-external crystalline cellulose. The long acting dosage form forming agent described in item i of the patent application scope is selected from the group consisting of glycerides or waxy substances. Stomach 3 is a long-acting dosage form as described in item 2 of the patent application, and the straight medium-shaped granules form a sword #ώ ^ rm ^ "self-containing triacetin, glyceryl stearate, glycerol glycerine, paraffin And the group of brown wax waxes. 4. The long-acting dosage form according to claim 1, wherein the tamsulosin content is 0.03-3% (w/w) of the composition. 5. The long-acting dosage form described in the scope of claim 2 is administered orally. 』I /, 中六海. As claimed in the long-acting dosage form of claim 1, the outer layer of the Lizhong gas long-acting agent further comprises more than one film coat. Eight " 7 such as the long-acting dosage form described in claim 1 of the patent scope, the middle release agent system, AAX-T ^ self-scented lactose, starch, mannitol, sodium methicone, " ^, in the group of microcrystalline cellulose, talc, hard citric acid, hard acetate, fumarate, and glutaric acid ester. 18 1252762 8 · — Contains i曰,, such as *. : - Soyin's long-acting dosage form manufacturing method, including (a) mixing an effective amount of tamsulosin or i killing l-65% (w/w) cellulose hydrophobic "sub-Western acceptable salt" , regulators and 20-65% 〇v/w) knife ^ not as a release rate agent;) due to open "杻 forming agent and i〇,% (w / w) dilution (b) the mixture of (a) Appropriate amount of solvent refining, · CO will (b) the results obtained by extrusion granulation; wherein 'cellulosic hydrophobic polymer compound based cellulose nano, cellulose acetate, ethyl cellulose = methamphate, C In the group of methyl cellulose acetate succinic acid and B::: cellulosic cellulose. - 夂一微结/9 · The manufacturing method according to item 8 of the patent application is granule forming agent In the group containing glycerin and vinegar and sacrificial substances, round 10 · The system described in claim 9 of the patent scope. The round granule forming agent is selected from the group consisting of triacetin and glycerol In the group of acid glycerides, paraffin waxes and palm waxes, the acid esters, 1 1 · the long-acting dosage form of the manufacturer as described in claim 8 The layer is formed into a film coat of more than one layer by the film coating liquid. wherein the film is as described in claim 8, wherein the diluent is selected from the group consisting of lactose, starch, mannitol, method 'in which, sodium powder, microcrystalline Cellulose, talcum powder, hard-brewed acid,:: a group of vitamins sodium fumarate sodium stearate and glutaric acid ester. "Yi salt, 19