Ketoprofen lansoprazole sustained-release pellets, as well as preparation method and preparation thereof

Abstract

The invention discloses ketoprofen lansoprazole sustained-release pellets. The pellets comprise the following components in parts by weight: 30-50 parts of ketoprofen, 3-5 parts of lansoprazole, 60-100 parts of filler, 3-5 parts of retardant, and 0-2 parts of lubricant, wherein the filler is one or more of starch, saccharose, lactose and microcrystalline cellulose, the retardant is ethyl cellulose, and the lubricant is one or more of magnesium stearate, talcum powder and polyethylene glycol 6000. Compound sustained-release pellets prepared from ketoprofen and lansoprazole have the advantages of high bioavailability, small local irritation, uniform medicine absorption speed and the like; the sustained-release pellets are coated, so that the medicament stability can be improved, the bitter taste of the pellets can be effectively covered, and the compliance of patient administration can be strengthened; sustained-release pellet tablets or sustained-release pellet capsules which are further prepared from the sustained-release pellets or coated pellets are convenient to carry and take; ketoprofen lansoprazole sustained-release pellets prepared by adopting an extrusion spheronization method or centrifugal granulation method are simple in operation, easy to control quality, narrow in size distribution range, good in roundness and smooth in surface, and are suitable for further coating, subpackaging or preparing.

Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a sustained-release pellet, a preparation method of the sustained-release pellet, and coated pellets, sustained-release pellets and sustained-release pellets further prepared by using the sustained-release pellet. Micropill capsules. Background technique

[0002] Pellets are spherical entities with a diameter of less than 2.5mm composed of drugs and excipients. They can be made into immediate-release, sustained-release or controlled-release pellets according to different needs. They are usually packed in bags, filled in hard capsules or made into tablets. take. In recent years, the development of micropills has attracted widespread attention, and more and more varieties are on the market. Its main features are: (1) The distribution area of ​​the drug on the surface of the gastrointestinal tract increases, and the therapeutic concentration can be quickly reached...

Examples

Embodiment 1

[0022] Embodiment 1, the preparation of ketoprofensoprazole sustained-release pellets

[0023] prescription

[0024]

[0025]

[0026] method Ketoprofen, lansoprazole, microcrystalline cellulose, polyethylene glycol 6000 and ethyl cellulose are pulverized into fine powders with a fineness of more than 100 mesh respectively; , microcrystalline cellulose, polyethylene glycol 6000 and ethyl cellulose, mix evenly, add water to make a soft material, put it in an extrusion spheronizer, set the extrusion sieve to 1.0mm, and the extrusion speed to 90r / min 1. The spheronization speed is 480r / min, the spheronization time is 8min, and the pellets are made, dried at 40°C, sieved, and the pellets with a particle size of 20-24 meshes are collected to obtain the product.

[0027] quality The yield of pellets with a particle size of 20-24 mesh is 95%; the pellets have good roundness and smooth surface, and the in vitro release rates at 1, 4, 8, 12, and 16 hours are 7.6, 18.6, 37...

Embodiment 2

[0028] Embodiment 2, the preparation of ketoprofensoprazole sustained-release pellets

[0029] prescription

[0030]

[0031] method Ketoprofen, lansoprazole, microcrystalline cellulose, lactose, magnesium stearate, talcum powder and ethyl cellulose are pulverized into the fine powder that fineness is above 100 mesh respectively; Get the ketoprofen of prescription quantity, Lansoprazole, microcrystalline cellulose, lactose, magnesium stearate, talcum powder and ethyl cellulose, mixed evenly, adding povidone K30 ethanol solution with a mass fraction of 2% to make a soft material, extruding and rolling In the machine, set the extrusion sieve hole to 1.0mm, the extrusion speed to 100r / min, the spheronization speed to 500r / min, and the spheronization time to 6min to make pellets, dry at 35-45°C, sieve, and collect for 20-20 Micropellets with a particle size of 24 meshes are available.

[0032] quality The yield of pellets with a particle size of 20-24 mesh was 89%; the...

Embodiment 3

[0033] Embodiment 3, the preparation of ketoprofensoprazole sustained-release pellets

[0034]prescription

[0035]

[0036] method Ketoprofen, lansoprazole, microcrystalline cellulose, lactose and ethyl cellulose are respectively pulverized into fine powders with a fineness of more than 100 mesh; , lactose and ethyl cellulose, mix evenly, add ethanol with a volume fraction of 45% to make a soft material, put it in an extrusion spheronizer, set the extrusion sieve to 1.0mm, the extrusion speed to 110r / min, and spheronize The rotation speed is 460r / min, the spheronization time is 5min, and the pellets are made, dried at 45°C, sieved, and pellets with a particle size of 20-24 meshes are collected to obtain the product.

[0037] quality The yield of pellets with a particle size of 20-24 mesh was 87%. The pellets had good roundness and smooth surface. 79.7%.

technical field

[0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a sustained-release pellet, a preparation method of the sustained-release pellet, and coated pellets, sustained-release pellets and sustained-release pellets further prepared by using the sustained-release pellet. Micropill capsules. Background technique

[0002] Pellets are spherical entities with a diameter of less than 2.5mm composed of drugs and excipients. They can be made into immediate-release, sustained-release or controlled-release pellets according to different needs. They are usually packed in bags, filled in hard capsules or made into tablets. take. In recent years, the development of micropills has attracted widespread attention, and more and more varieties are on the market. Its main features are: (1) The distribution area of ​​the drug on the surface of the gastrointestinal tract increases, and the therapeutic concentration can be quickly reached...

Examples

Embodiment 1

[0022] Embodiment 1, the preparation of ketoprofensoprazole sustained-release pellets

[0023] prescription

[0024]

[0025]

[0026] method Ketoprofen, lansoprazole, microcrystalline cellulose, polyethylene glycol 6000 and ethyl cellulose are pulverized into fine powders with a fineness of more than 100 mesh respectively; , microcrystalline cellulose, polyethylene glycol 6000 and ethyl cellulose, mix evenly, add water to make a soft material, put it in an extrusion spheronizer, set the extrusion sieve to 1.0mm, and the extrusion speed to 90r / min 1. The spheronization speed is 480r / min, the spheronization time is 8min, and the pellets are made, dried at 40°C, sieved, and the pellets with a particle size of 20-24 meshes are collected to obtain the product.

[0027] quality The yield of pellets with a particle size of 20-24 mesh is 95%; the pellets have good roundness and smooth surface, and the in vitro release rates at 1, 4, 8, 12, and 16 hours are 7.6, 18.6, 37...

Embodiment 2

[0028] Embodiment 2, the preparation of ketoprofensoprazole sustained-release pellets

[0029] prescription

[0030]

[0031] method Ketoprofen, lansoprazole, microcrystalline cellulose, lactose, magnesium stearate, talcum powder and ethyl cellulose are pulverized into the fine powder that fineness is above 100 mesh respectively; Get the ketoprofen of prescription quantity, Lansoprazole, microcrystalline cellulose, lactose, magnesium stearate, talcum powder and ethyl cellulose, mixed evenly, adding povidone K30 ethanol solution with a mass fraction of 2% to make a soft material, extruding and rolling In the machine, set the extrusion sieve hole to 1.0mm, the extrusion speed to 100r / min, the spheronization speed to 500r / min, and the spheronization time to 6min to make pellets, dry at 35-45°C, sieve, and collect for 20-20 Micropellets with a particle size of 24 meshes are available.

[0032] quality The yield of pellets with a particle size of 20-24 mesh was 89%; the...

Embodiment 3

[0033] Embodiment 3, the preparation of ketoprofensoprazole sustained-release pellets

[0034]prescription

[0035]

[0036] method Ketoprofen, lansoprazole, microcrystalline cellulose, lactose and ethyl cellulose are respectively pulverized into fine powders with a fineness of more than 100 mesh; , lactose and ethyl cellulose, mix evenly, add ethanol with a volume fraction of 45% to make a soft material, put it in an extrusion spheronizer, set the extrusion sieve to 1.0mm, the extrusion speed to 110r / min, and spheronize The rotation speed is 460r / min, the spheronization time is 5min, and the pellets are made, dried at 45°C, sieved, and pellets with a particle size of 20-24 meshes are collected to obtain the product.

[0037] quality The yield of pellets with a particle size of 20-24 mesh was 87%. The pellets had good roundness and smooth surface. 79.7%.

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