A kind of tamsulosin sustained-release pellets and preparation method thereof

Abstract

The invention provides a tamsulosin sustained-release pellet, comprising a pill core and a sustained-release coating layer, the sustained-release coating layer comprising a hydrophobic matrix and a pH-sensitive hydrophilic polymer, the polymer polymerized The pH value of the change in solubility of the substance is between 1 and 14, so that the drug can be released at different pH values, and it can also be used as a carrier for controlling the release of tamsulosin, which simplifies the prescription, reduces the difficulty of preparation, and is easier for industrial mass production. The inventors have surprisingly found that the formulation can be used to prepare various sustained-release dosage forms of tamsulosin, independent of the physicochemical properties of tamsulosin.

Description

technical field

[0001] The invention relates to the field of tamsulosin preparations, in particular to slow-release pellets for changing the release behavior of tamsulosin and a preparation method thereof. Background technique

[0002] Pellets (small pills, Pellets is the English name) refer to small spherical oral dosage forms with a diameter of about 1 mm, generally not more than 2.5 mm. According to the release speed, the pellets mainly include immediate-release pellets and sustained-release or controlled-release pellets. Immediate-release pellets are pellets made of drugs and general excipients with a relatively fast release rate. Generally, the dissolution rate in 30 minutes should not be less than 70%. A certain amount of disintegrant or surfactant is often added to the pellet prescription , to ensure rapid disintegration and drug dissolution of the pellets. Sustained-release or controlled-release pellets can be divided into (1) skeleton sustained-release pellets: dr...

Examples

Embodiment 1

[0015] Embodiment 1 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0016] The prescription of preparation and preparation method thereof are:

[0017] prescription

[0018] Pill heart:

[0019]

[0020] Coating:

[0021] Carbomer 8g

[0022] Ethylcellulose 9g

[0023] Triethyl citrate 3g

[0024] Preparation:

[0025] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0026] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0027] Put the desustained-release pellets into capsules.

[0028] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned pellets, mi...

Embodiment 2

[0030] Embodiment 2 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0031] The prescription of preparation and preparation method thereof are:

[0032] prescription

[0033] Pill heart:

[0034]

[0035] Coating:

[0036] Sodium alginate 15g

[0037] Ethyl cellulose 29g

[0038] Magnesium stearate 6g

[0039] Preparation:

[0040] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0041] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0042] Put the desustained-release pellets into capsules.

[0043] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned...

Embodiment 3

[0045] Embodiment 3 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0046] The prescription of preparation and preparation method thereof are:

[0047] prescription

[0048] Pill heart:

[0049]

[0050] Coating:

[0051]

[0052] Preparation:

[0053] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0054] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0055] Put the desustained-release pellets into capsules.

[0056] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned pellets, mix, and press into tablets of suitable size.

[0057] The release ra...

technical field

[0001] The invention relates to the field of tamsulosin preparations, in particular to slow-release pellets for changing the release behavior of tamsulosin and a preparation method thereof. Background technique

[0002] Pellets (small pills, Pellets is the English name) refer to small spherical oral dosage forms with a diameter of about 1 mm, generally not more than 2.5 mm. According to the release speed, the pellets mainly include immediate-release pellets and sustained-release or controlled-release pellets. Immediate-release pellets are pellets made of drugs and general excipients with a relatively fast release rate. Generally, the dissolution rate in 30 minutes should not be less than 70%. A certain amount of disintegrant or surfactant is often added to the pellet prescription , to ensure rapid disintegration and drug dissolution of the pellets. Sustained-release or controlled-release pellets can be divided into (1) skeleton sustained-release pellets: dr...

Examples

Embodiment 1

[0015] Embodiment 1 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0016] The prescription of preparation and preparation method thereof are:

[0017] prescription

[0018] Pill heart:

[0019]

[0020] Coating:

[0021] Carbomer 8g

[0022] Ethylcellulose 9g

[0023] Triethyl citrate 3g

[0024] Preparation:

[0025] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0026] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0027] Put the desustained-release pellets into capsules.

[0028] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned pellets, mi...

Embodiment 2

[0030] Embodiment 2 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0031] The prescription of preparation and preparation method thereof are:

[0032] prescription

[0033] Pill heart:

[0034]

[0035] Coating:

[0036] Sodium alginate 15g

[0037] Ethyl cellulose 29g

[0038] Magnesium stearate 6g

[0039] Preparation:

[0040] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0041] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0042] Put the desustained-release pellets into capsules.

[0043] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned...

Embodiment 3

[0045] Embodiment 3 Tamsulosin sustained-release pellets and tablets (1000 preparation units)

[0046] The prescription of preparation and preparation method thereof are:

[0047] prescription

[0048] Pill heart:

[0049]

[0050] Coating:

[0051]

[0052] Preparation:

[0053] Take povidone and add 80% ethanol to dissolve, and use it as a binder for later use; put the components in other pellet formulations in an extrusion spheronizer, add a binder to prepare a pellet core, and dry it in a fluidized bed at 60°C;

[0054] Take the core of the ball, put it in the coating pan, spray the coating ingredients dissolved in acetone for coating, and dry for 1 hour after coating. Then dry at 40° C. for 12 hours to obtain sustained-release pellets.

[0055] Put the desustained-release pellets into capsules.

[0056] Or add microcrystalline cellulose and magnesium stearate to the above-mentioned pellets, mix, and press into tablets of suitable size.

[0057] The release ra...

Images