Etodolac double-layered osmotic pump controlled release tablets, and preparation method thereof

Abstract

The invention belongs to the field of medicines, and specifically discloses etodolac double-layered osmotic pump controlled release tablets, and a preparation method thereof. The etodolac double-layered osmotic pump controlled release tablets provided by the invention are double-layered tablets with semi permeable membranes. The upper layers of the tablets are medicine-containing layers comprising medicines and auxiliary materials, and the lower layers are assisting layers composed of polymers and osmotically active substances. The etodolac double-layered osmotic pump controlled release tablets provided by the invention have advantages of stable in vivo blood-drug level, and long effective blood-drug level duration.

Description

technical field

[0001] The invention belongs to the field of medicine, and more specifically, the invention discloses an osmotic pump controlled-release tablet and a preparation method thereof. Background technique

[0002] Etodolac is a pyranose carboxylic acid non-steroidal anti-inflammatory drug developed by France in the mid-1970s. It has analgesic and anti-inflammatory properties. It can reduce the level of uric acid in human blood to treat gout (USA Patent 4,633,354), and treat rheumatoid arthritis by reducing rheumatoid factor in blood (US Patent 4,742,076), which is a new generation of cyclooxygenase highly selective anti-inflammatory drugs. Its anti-inflammatory and analgesic effect is exact, high in safety, gastrointestinal adverse reactions and renal function damage rarely occur, and it is widely used clinically to treat postoperative pain, relieve symptoms of rheumatoid arthritis, osteoarthritis and arthritis The bone pathological changes caused by it are recomm...

Examples

Embodiment 1

[0033] Party:

[0034] Drug-containing layer (specification 100mg / tablet)

[0035] etodolac 100mg

[0036] PEO (polyoxyethylene) VROH or CMC-Na (sodium carboxymethylcellulose) or HPMC K4M (Hypromellose) or CP 971NF (Carbomer)) 186mg

[0037] Booster layer (mg / tablet)

[0038] CMS-Na56

[0039] HPMC K100M 45

[0040] CP 971NF 11.6

[0041] pvp K30 twenty two

[0042] NaCl 32.5

[0043] Fe 2 o 3 1.55

[0044] Coating prescription (mg)

[0045] CA 15

[0046]PEG 3

[0047] Acetone 1000ml

[0048] In this experiment, PEO VROH (polyoxyethylene), CMC-Na (sodium carboxymethyl cellulose), HPMC K4M (Hydroxypropylmethylcellulose), CP 971NF One of the (carbomer) is used as the drug carrier of the drug-containing layer, and the influence of the polymer carrier on drug release is investigated.

[0049] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, add an app...

Embodiment 2

[0054] Party:

[0055] Drug-containing layer (specification 100mg / tablet)

[0056] etodolac 35% 100mg

[0057] PEO VROH 30%; 50%; 65% respectively 86mg; 143mg; 186mg

[0058] Booster layer (mg / tablet)

[0059] CMS-Na56

[0060] HPMC K100M 45

[0061] CP 971NF 11.6

[0062] pvp K30 twenty two

[0063] NaCl 32.5

[0064] Fe 2 o 3 1.55

[0065] Coating prescription (mg)

[0066] CA 15

[0067] PEG 3

[0068] Acetone 1000ml

[0069] The amount of PEO used in this experiment was 30%, 50% and 65%, respectively. The release rate of the controlled-release tablets within 24 hours was measured according to the release rate method, indicating that different amounts of polyoxyethylene had an effect on the cumulative release of the drug within 24 hours.

[0070] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, use an appropriate amount of isopropanol to make a sof...

Embodiment 3

[0075] Party:

[0076] Drug-containing layer (specification 100mg / tablet)

[0077] etodolac 100mg

[0078] PEO VROH 186mg

[0079] Booster layer (mg / tablet)

[0080] CMS-Na 46; 56; 66

[0081] HPMC K100M 45

[0082] CP 971NF 11.6

[0083] pvp K30 twenty two

[0084] NaCl 32.5

[0085] Fe 2 o 3 1.55

[0086] Coating prescription (mg)

[0087] CA 15

[0088] PEG 3

[0089] Acetone 1000ml

[0090] Keep other prescriptions of the booster layer unchanged, change the dosage of CMS-Na to 46mg, 56mg, 66mg, measure the release rate of the controlled-release tablet within 24h according to the release rate measurement method, and investigate its influence on the release rate.

[0091] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, use an appropriate amount of isopropanol to make a soft material, granulate with a 16-mesh sieve, dry at 40°C, and g...

technical field

[0001] The invention belongs to the field of medicine, and more specifically, the invention discloses an osmotic pump controlled-release tablet and a preparation method thereof. Background technique

[0002] Etodolac is a pyranose carboxylic acid non-steroidal anti-inflammatory drug developed by France in the mid-1970s. It has analgesic and anti-inflammatory properties. It can reduce the level of uric acid in human blood to treat gout (USA Patent 4,633,354), and treat rheumatoid arthritis by reducing rheumatoid factor in blood (US Patent 4,742,076), which is a new generation of cyclooxygenase highly selective anti-inflammatory drugs. Its anti-inflammatory and analgesic effect is exact, high in safety, gastrointestinal adverse reactions and renal function damage rarely occur, and it is widely used clinically to treat postoperative pain, relieve symptoms of rheumatoid arthritis, osteoarthritis and arthritis The bone pathological changes caused by it are recomm...

Examples

Embodiment 1

[0033] Party:

[0034] Drug-containing layer (specification 100mg / tablet)

[0035] etodolac 100mg

[0036] PEO (polyoxyethylene) VROH or CMC-Na (sodium carboxymethylcellulose) or HPMC K4M (Hypromellose) or CP 971NF (Carbomer)) 186mg

[0037] Booster layer (mg / tablet)

[0038] CMS-Na56

[0039] HPMC K100M 45

[0040] CP 971NF 11.6

[0041] pvp K30 twenty two

[0042] NaCl 32.5

[0043] Fe 2 o 3 1.55

[0044] Coating prescription (mg)

[0045] CA 15

[0046]PEG 3

[0047] Acetone 1000ml

[0048] In this experiment, PEO VROH (polyoxyethylene), CMC-Na (sodium carboxymethyl cellulose), HPMC K4M (Hydroxypropylmethylcellulose), CP 971NF One of the (carbomer) is used as the drug carrier of the drug-containing layer, and the influence of the polymer carrier on drug release is investigated.

[0049] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, add an app...

Embodiment 2

[0054] Party:

[0055] Drug-containing layer (specification 100mg / tablet)

[0056] etodolac 35% 100mg

[0057] PEO VROH 30%; 50%; 65% respectively 86mg; 143mg; 186mg

[0058] Booster layer (mg / tablet)

[0059] CMS-Na56

[0060] HPMC K100M 45

[0061] CP 971NF 11.6

[0062] pvp K30 twenty two

[0063] NaCl 32.5

[0064] Fe 2 o 3 1.55

[0065] Coating prescription (mg)

[0066] CA 15

[0067] PEG 3

[0068] Acetone 1000ml

[0069] The amount of PEO used in this experiment was 30%, 50% and 65%, respectively. The release rate of the controlled-release tablets within 24 hours was measured according to the release rate method, indicating that different amounts of polyoxyethylene had an effect on the cumulative release of the drug within 24 hours.

[0070] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, use an appropriate amount of isopropanol to make a sof...

Embodiment 3

[0075] Party:

[0076] Drug-containing layer (specification 100mg / tablet)

[0077] etodolac 100mg

[0078] PEO VROH 186mg

[0079] Booster layer (mg / tablet)

[0080] CMS-Na 46; 56; 66

[0081] HPMC K100M 45

[0082] CP 971NF 11.6

[0083] pvp K30 twenty two

[0084] NaCl 32.5

[0085] Fe 2 o 3 1.55

[0086] Coating prescription (mg)

[0087] CA 15

[0088] PEG 3

[0089] Acetone 1000ml

[0090] Keep other prescriptions of the booster layer unchanged, change the dosage of CMS-Na to 46mg, 56mg, 66mg, measure the release rate of the controlled-release tablet within 24h according to the release rate measurement method, and investigate its influence on the release rate.

[0091] Preparation method: crush etodolac and drug-containing layer auxiliary materials, pass through a 60-mesh sieve, mix well, use an appropriate amount of isopropanol to make a soft material, granulate with a 16-mesh sieve, dry at 40°C, and g...

Images