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Pramod Salve ¹

Affiliations
1 University Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University Campus, Mahatma Fuley Shaikshanik Parisar, Amravati Road, Nagpur-440 033 (MS), IN

Abstract

Mesalamine is an inflammatory agent to treat inflammation of digestive tract (crohn’s disease) and mild to moderate ulcerative colitis. It shows inflammatory activity by blocking cyclooxygenase and prostaglandins production in colon. The multiple unit dosage form of mesalamine in the form of pellets was prepared. The parameters like moisture content, speed of spheronization and spheronization aid (MCC PH 101) were optimized. The pellets were loaded with 40% drug, 90% moisture content, 1% binder PVP K-30 and spheronization speed of 1500 rpm were found to be parameters for pelletization. For drug release in colon inner coating using Eudragit RL RS 30 and outer coating using Eudragit FS 30D was done. In vitro drug release studies clearly revealed that 15% coating levels of eudragit FS 30D withstand acidic media and 1% drug release was observed which was optimum coating level for colon targeting. With aqueous dispersion of eudragit FS 30D (outer coat) at 15% coating level, 1% drug release was observed in pH 1.2 buffer for 2 hours and sustained drug release for 8 hours was obtained in pH 7.2 phosphate buffer. When pH of dissolution media was increased from 6.8 to 7.2, drug release was found to increase from 8.45 to 96.05%. As compared with formulation containing croscarmellose sodium, release rate was decreased with formulation containing crospovidone. Hence, film coated pellets can be used for colonic release of mesalamine.

Keywords

Colonic Release, Mesalamine, Eudragit RL Rs 30 and FS 30D.

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Pramod Salve ¹, Suvarna Pise ¹, Nikhil Bali ¹

Affiliations
1 University Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University Campus, Mahatma Jyotiba Fuley Shaikshanik Parisar, Amravati Road, Nagpur-440033, (M.S), IN

Abstract

Solid lipid nanoparticles (SLN) loaded formulation as an alternative to oral and parenteral delivery of rivastigmine tartarate (RT), a water-soluble drug by using Precirol ATO 5 and tween 80. The SLN prepared by hot high pressure homogenization method. RT-loaded SLN were stable up to one month of storage .The SLN was found to be zeta potential value of -10 mV, polydispersity index was found in the range 0.3-0.6 with average particle size distribution of 214 nm. The encapsulation efficiency (EE %) was found to be 59.23%. The folding endurance, thickness, drug content uniformity of RT-loaded transdermal patch was found to be 160±1.05 folds, 0.26±0.05mm, 98.63±0.16% respectively. The percent moisture content, percent moisture loss, percent elongation break test was found to be 4.2±0.26%, 3.9±0.31%, 9.23±0.93% respectively. The ex vivo skin permeation and in vitro drug release kinetics has shown 96.90±0.69% permeation and 95.70±0.87% drug release respectively. The RT-SLN loaded transdermal patch was prepared using Eudragit RS100 and Eudragit RL100 and PEG 400 as plasticizer. Formulation was optimized by using full 32 factorial design expert 10. Ex vivo study showed maximum drug release with 24 hours.

Keywords

Rivastigmine Tartarate, Precirol ATO 5, Tween 80, Solid Lipid Nanoparticles, High Pressure Homogenization, Eudragit RS 100, Eudragit RL 100.

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