Sustained release composns preparation of Fudosteine and clarithromycin

Abstract

A slowly-releasing composite medicine for treating the diseases in respiratory system is prepared from Fuduositan (15-30 Wt %), clarithromycin (10-40), and auxiliary (rest) including paralyser.

Description

Technical field

[0001] The present invention relates to a medicine. More specifically, the present invention relates to a sustained-release combined preparation of Fudostan and clarithromycin. Background technique

[0002] The chemical name of Fudosteine ​​is (-)-(R)-2-amino-3-(3-hydroxypropylmercapto)propionic acid, which was developed by Japan's SS Pharmaceutical Company and licensed to Japan's Yoshitomi Pharmaceutical the company. The drug was officially launched in 2002 under the trade names of Cleanal (SS Company) and Spelear (Gifford Company). Fudosteine ​​is a new cysteine ​​derivative with a stronger expectorant effect. At present, there are imported preparations of such drugs as ethylcysteine ​​and carbonylmethylcysteine ​​on the market in my country. The curative effect of these drugs is not very satisfactory, especially their toxic side effects are very strong, and their chemical properties are unstable. The expectorant effect of Fudosteine ​​is 3 times that of carbony...

Examples

Embodiment 1

[0033] The formula of the sustained-release combination preparation of Fudosteine ​​and clarithromycin in this example is:

[0034] Fudosteine...200g

[0035] Clarithromycin............ 250g

[0036] Lactose............220g

[0037] Low viscosity hydroxypropyl cellulose...30g

[0038] High viscosity hydroxypropyl cellulose...200g

[0039] Talc powder.........................40g

[0040] Magnesium stearate............10g

[0041] Film coat.........................40g

[0042] Make 1000 tablets, each containing 200mg Fudosteine ​​and 250mg clarithromycin.

[0043] Specific preparation method:

[0044] Weigh Fudosteine, clarithromycin, hypromellose and lactose according to the prescription and mix them at high speed for 10 minutes in a KJz-10 rapid stirring granulator. Use distilled water to prepare suitable soft materials and screen them with 18-20 mesh. After drying at 60°C with hot air, the 18-mesh sieve is sized and mixed with talc powder and magnesium stearate, and compressed int...

Embodiment 2

[0046] The formula of the sustained-release combination preparation of Fudosteine ​​and clarithromycin in this example is:

[0047] Fudosteine...400g

[0048] Clarithromycin............500g

[0049] Lactose............220g

[0050] Low viscosity hydroxypropyl cellulose...30g

[0051] High viscosity hydroxypropyl cellulose...200g

[0052] Talc powder.........................40g

[0053] Magnesium stearate............10g

[0054] Film coat.........................40g

[0055] With this prescription, the preparation method of Example 1 is basically followed, but a 40% ethanol aqueous solution is used to prepare a suitable soft material. A total of 1,000 Fudosteine ​​and Clarithromycin sustained-release tablets were prepared, each containing 400mg Fudosteine ​​and 500mg Clarithromycin.

Embodiment 3

[0057] In the sustained-release combination preparation of Fudosteine ​​and clarithromycin of this embodiment, the formulation of the drug pellets is:

[0058] Fudosteine...200g

[0059] Clarithromycin............ 250g

[0060] Lactose............220g

[0061] Low viscosity hydroxypropyl cellulose...30g

[0062] High viscosity hydroxypropyl cellulose...200g

[0063] Microcrystalline cellulose............25g

[0064] Water..................appropriate

[0065] Coating liquid formula:

[0066] Acrylic resin RS100......100g

[0067] Triethyl citrate...10g

[0068] Polyethylene glycol 6000.........20g

[0069] Ethanol............850ml

[0070] Make 1000 capsules, each containing 200mg Fudosteine ​​and 250mg Clarithromycin.

[0071] Specific preparation method:

[0072] Mix the mixture in the pellet formula uniformly, use distilled water or ethanol aqueous solution in the coating pan to make pellet cores, and then dry at 40-50℃ to obtain dry cores; weigh; After removing the fine powder...

Technical field

[0001] The present invention relates to a medicine. More specifically, the present invention relates to a sustained-release combined preparation of Fudostan and clarithromycin. Background technique

[0002] The chemical name of Fudosteine ​​is (-)-(R)-2-amino-3-(3-hydroxypropylmercapto)propionic acid, which was developed by Japan's SS Pharmaceutical Company and licensed to Japan's Yoshitomi Pharmaceutical the company. The drug was officially launched in 2002 under the trade names of Cleanal (SS Company) and Spelear (Gifford Company). Fudosteine ​​is a new cysteine ​​derivative with a stronger expectorant effect. At present, there are imported preparations of such drugs as ethylcysteine ​​and carbonylmethylcysteine ​​on the market in my country. The curative effect of these drugs is not very satisfactory, especially their toxic side effects are very strong, and their chemical properties are unstable. The expectorant effect of Fudosteine ​​is 3 times that of carbony...

Examples

Embodiment 1

[0033] The formula of the sustained-release combination preparation of Fudosteine ​​and clarithromycin in this example is:

[0034] Fudosteine...200g

[0035] Clarithromycin............ 250g

[0036] Lactose............220g

[0037] Low viscosity hydroxypropyl cellulose...30g

[0038] High viscosity hydroxypropyl cellulose...200g

[0039] Talc powder.........................40g

[0040] Magnesium stearate............10g

[0041] Film coat.........................40g

[0042] Make 1000 tablets, each containing 200mg Fudosteine ​​and 250mg clarithromycin.

[0043] Specific preparation method:

[0044] Weigh Fudosteine, clarithromycin, hypromellose and lactose according to the prescription and mix them at high speed for 10 minutes in a KJz-10 rapid stirring granulator. Use distilled water to prepare suitable soft materials and screen them with 18-20 mesh. After drying at 60°C with hot air, the 18-mesh sieve is sized and mixed with talc powder and magnesium stearate, and compressed int...

Embodiment 2

[0046] The formula of the sustained-release combination preparation of Fudosteine ​​and clarithromycin in this example is:

[0047] Fudosteine...400g

[0048] Clarithromycin............500g

[0049] Lactose............220g

[0050] Low viscosity hydroxypropyl cellulose...30g

[0051] High viscosity hydroxypropyl cellulose...200g

[0052] Talc powder.........................40g

[0053] Magnesium stearate............10g

[0054] Film coat.........................40g

[0055] With this prescription, the preparation method of Example 1 is basically followed, but a 40% ethanol aqueous solution is used to prepare a suitable soft material. A total of 1,000 Fudosteine ​​and Clarithromycin sustained-release tablets were prepared, each containing 400mg Fudosteine ​​and 500mg Clarithromycin.

Embodiment 3

[0057] In the sustained-release combination preparation of Fudosteine ​​and clarithromycin of this embodiment, the formulation of the drug pellets is:

[0058] Fudosteine...200g

[0059] Clarithromycin............ 250g

[0060] Lactose............220g

[0061] Low viscosity hydroxypropyl cellulose...30g

[0062] High viscosity hydroxypropyl cellulose...200g

[0063] Microcrystalline cellulose............25g

[0064] Water..................appropriate

[0065] Coating liquid formula:

[0066] Acrylic resin RS100......100g

[0067] Triethyl citrate...10g

[0068] Polyethylene glycol 6000.........20g

[0069] Ethanol............850ml

[0070] Make 1000 capsules, each containing 200mg Fudosteine ​​and 250mg Clarithromycin.

[0071] Specific preparation method:

[0072] Mix the mixture in the pellet formula uniformly, use distilled water or ethanol aqueous solution in the coating pan to make pellet cores, and then dry at 40-50℃ to obtain dry cores; weigh; After removing the fine powder...