Design and optimization of rifaximin macroparticles for  colon targeting

N.A.

Makale detayları

Design and optimization of rifaximin macroparticles for colon targeting

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1609-1618

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347589

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 This study is focused to design a colon specific pellet formulation of rifaximin based on the combination of time-dependent and pH sensitive delivery system using Quality-by-Design QbD approach for better and promising treatment of inflammatory bowel disease IBD. An extrusionspheronization process was utilized for the preparation of core macroparticles using ethyl cellulose EC as matrix former and microcrystalline cellulose MCC as a spheronizing aid. Two critical process parameters CPPs i.e., spheronization time and spheronizer speed were taken as independent factors while aspect ratio, sphericity, carrs index, and particle size were taken as dependent responses to optimize the composition of the core macroparticles. To regulate the drug release, core macroparticles were coated with Eudragit NE40D and Eudragit FS30D to impart time-dependent and pH sensitive release of drug. The optimized coated macroparticles were characterized for drug content and in vitrodrug release in different pH media of stomach and intestine. The coating levels of the inner and outer polymers were further optimized for the time required for 10 , 50  and 90  drug release. The result showed that the 90 of drug of P3 and P4 formulation were found to be released in 10.87 and 13.19hrs respectively. When exposed to Scanning Electron Microscopy the images of coated macroparticles suggested a uniform and smooth coat of polymers over the surface of macroparticles. This formulation reduces the dose and the side effects due to its specific targeting at the site of inflammation makes it a better choice over the tablets. The result indicates that the developed formulation may possibly reduce the dosing frequency and side effects associated with the conventional tablet formulation for the site-specific targeting at inflammation site.

 This study is focused to design a colon specific pellet formulation of rifaximin based on the combination of time-dependent and pH sensitive delivery system using Quality-by-Design QbD approach for better and promising treatment of inflammatory bowel disease IBD. An extrusionspheronization process was utilized for the preparation of core macroparticles using ethyl cellulose EC as matrix former and microcrystalline cellulose MCC as a spheronizing aid. Two critical process parameters CPPs i.e., spheronization time and spheronizer speed were taken as independent factors while aspect ratio, sphericity, carrs index, and particle size were taken as dependent responses to optimize the composition of the core macroparticles. To regulate the drug release, core macroparticles were coated with Eudragit NE40D and Eudragit FS30D to impart time-dependent and pH sensitive release of drug. The optimized coated macroparticles were characterized for drug content and in vitrodrug release in different pH media of stomach and intestine. The coating levels of the inner and outer polymers were further optimized for the time required for 10 , 50  and 90  drug release. The result showed that the 90 of drug of P3 and P4 formulation were found to be released in 10.87 and 13.19hrs respectively. When exposed to Scanning Electron Microscopy the images of coated macroparticles suggested a uniform and smooth coat of polymers over the surface of macroparticles. This formulation reduces the dose and the side effects due to its specific targeting at the site of inflammation makes it a better choice over the tablets. The result indicates that the developed formulation may possibly reduce the dosing frequency and side effects associated with the conventional tablet formulation for the site-specific targeting at inflammation site.

 This study is focused to design a colon specific pellet formulation of rifaximin based on the combination of time-dependent and pH sensitive delivery system using Quality-by-Design QbD approach for better and promising treatment of inflammatory bowel disease IBD. An extrusionspheronization process was utilized for the preparation of core macroparticles using ethyl cellulose EC as matrix former and microcrystalline cellulose MCC as a spheronizing aid. Two critical process parameters CPPs i.e., spheronization time and spheronizer speed were taken as independent factors while aspect ratio, sphericity, carrs index, and particle size were taken as dependent responses to optimize the composition of the core macroparticles. To regulate the drug release, core macroparticles were coated with Eudragit NE40D and Eudragit FS30D to impart time-dependent and pH sensitive release of drug. The optimized coated macroparticles were characterized for drug content and in vitrodrug release in different pH media of stomach and intestine. The coating levels of the inner and outer polymers were further optimized for the time required for 10 , 50  and 90  drug release. The result showed that the 90 of drug of P3 and P4 formulation were found to be released in 10.87 and 13.19hrs respectively. When exposed to Scanning Electron Microscopy the images of coated macroparticles suggested a uniform and smooth coat of polymers over the surface of macroparticles. This formulation reduces the dose and the side effects due to its specific targeting at the site of inflammation makes it a better choice over the tablets. The result indicates that the developed formulation may possibly reduce the dosing frequency and side effects associated with the conventional tablet formulation for the site-specific targeting at inflammation site.

 This study is focused to design a colon specific pellet formulation of rifaximin based on the combination of time-dependent and pH sensitive delivery system using Quality-by-Design QbD approach for better and promising treatment of inflammatory bowel disease IBD. An extrusionspheronization process was utilized for the preparation of core macroparticles using ethyl cellulose EC as matrix former and microcrystalline cellulose MCC as a spheronizing aid. Two critical process parameters CPPs i.e., spheronization time and spheronizer speed were taken as independent factors while aspect ratio, sphericity, carrs index, and particle size were taken as dependent responses to optimize the composition of the core macroparticles. To regulate the drug release, core macroparticles were coated with Eudragit NE40D and Eudragit FS30D to impart time-dependent and pH sensitive release of drug. The optimized coated macroparticles were characterized for drug content and in vitrodrug release in different pH media of stomach and intestine. The coating levels of the inner and outer polymers were further optimized for the time required for 10 , 50  and 90  drug release. The result showed that the 90 of drug of P3 and P4 formulation were found to be released in 10.87 and 13.19hrs respectively. When exposed to Scanning Electron Microscopy the images of coated macroparticles suggested a uniform and smooth coat of polymers over the surface of macroparticles. This formulation reduces the dose and the side effects due to its specific targeting at the site of inflammation makes it a better choice over the tablets. The result indicates that the developed formulation may possibly reduce the dosing frequency and side effects associated with the conventional tablet formulation for the site-specific targeting at inflammation site.

Makale detayları

Design and optimization of rifaximin macroparticles for colon targeting

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1609-1618

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347589

pISSN:

2630-6344

Macroparticles

colon targeted

rifaximin

Eudragit

MCC

Optimization

Sayı

Makale detayları

Design and optimization of rifaximin macroparticles for colon targeting

Yazarlar: N.A.

Yayıncı: Marmara University

Ana Başlıklar: Pharmaceutical Delivery Technologies

Dergi: Journal of Research in Pharmacy Vol.28 Issue 5, pp.1609-1618

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001347589

pISSN: 2630-6344

Macroparticles

colon targeted

rifaximin

Eudragit

MCC

Optimization

Sayı

Yazarlar:

N.A.

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1609-1618

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347589

pISSN:

2630-6344