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P. S. Salve ¹

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

Abstract

Fungal infection caused by fungus called dermatophyte infects top layer of skin, hair or nails. An allylamine antifungal agent terbinafine hydrochloride is used topically and orally. Its topical administration is preferred but barrier properties of stratum corneum decreases absorption and requires frequent application. It has low oral bioavailability due to hepatic first pass metabolism and many systemic adverse effects. Niosomes have been reported to enhance residence time of drugs in stratum corneum and epidermis, while reducing systemic absorption and improve penetration of entrapped drug across skin. Niosomes of terbinafine hydrochloride were prepared by film hydration method in size range of 0.24 to 9.4 m. Maximum entrapment efficiency was observed in formulation containing span 60 at 1:1 molar ratio of cholesterol and surfactant. Zeta potential values of niosomes containing span 60 (1:1) were more stable than other niosomal formulations. Niosomes were incorporated in 1.5 %w/v carbopol gel at pH 6.8-7.0. In in vitro antifungal study against candida albicans, vesicular systems were found to be more effective than conventional gel. The formulations containing tween 60 (1.5:1) and span 80 (1:1) were found to have maximum zone of inhibition. In ex vivo percutaneous permeation studies, niosomal formulations have shown superior skin penetration and drug deposition as compared to conventional formulation. The formulation containing tween 80 has shown higher drug deposition in rat skin as compared to other formulations. The niosomal vesicles can be used to enhance penetration and deposition of terbinafine hydrochloride in skin.

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P. S. Salve ¹

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

Abstract

The present study was focused to achieve controlled and predictable delivery of highly water soluble drug. Drug: ion exchange resin complex was encapsulated with main emphasis on drug: resin ratio, core: coat ratio and polymer composition. Studies clearly showed that resinate in 1:1 ratio, core: coat ratio of 1:2 and eudragit RS: RL ratio of 70:30 were the optimum composition for desired release profile. At the same time it was demonstrated that solvent composition and stirring speed affect quality of polymeric beads. Salbutamol sulphate being highly soluble and permeable drug, often presents challenge in formulation its controlled delivery product. Dissolution studies reveal that mechanism of drug release followed Higuchi equation, signifying drug release by Fickian diffusion. Also for same the X-ray diffraction, FT-IR, SEM and stability studies. Ion exchange resin beads of Salbutamol sulphate showed promising results for controlled drug release.

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P. S. Salve ¹

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

Abstract

The hydrodynamically balanced system (HBS) is based on the gel forming hydrocolloids which swells when comes in contact with water resulting in dosage form with density less than unity10,11. The orientation of charged hydrophilic groups towards water results in HBS phenomenon. Hydrocolloids used are hydroxypropylmethyl cellulose derivatives. The present study deals with formulation of diltiazem HCl HBS. The effect of polymer viscosity, processing parameter on floating characteristics and drug release was studied. A direct compression method and 1:1 to 1:5 ratio of drug: HPMC K4M, K15M and K100M were used for development of HBS. The floating characteristic and in vitro drug release was studied in pH 1.2 buffer. The effect of hardness on floating behavior of HBS was studied. An increase in hardness resulted in non-floating dosage form. The HBS tablets containing 1:1 ratio of drug: polymer were found to be non-floating even at low hardness values. Hence, by varying the hardness, the floating characters can be obtained. Invitro drug release profile reveals that increase in drug: HPMC ratio resulted in retardation of drug release.

Keywords

The Hydrodynamically Balanced System, Floating, Hardness.

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P. S. Salve ¹

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

Abstract

The floating beads of ibuprofen were developed to provide controlled release in stomach. The beads were developed by ionotropic gelation of low methoxy pectin with calcium ions. The drug loading was kept at 25, 50 and 75 %w/w of low methoxy pectin (LMP). Sesame oil was used to provide floating characteristic in 10, 20 and 30 %w/w of (LMP). The beads were cross-linked with 2, 4 and 10 %w/v CaCl2 solution and further coated with 1 %w/v solution of deacetylated chitosan in 3 %w/v acetic acid. The interaction of low methoxy pectin with calcium ions and deacetylated chitosan was studied by differential scanning calorimetry, x-ray diffraction spectroscopy and FT-IR spectroscopy. The in-vitro buoyancy studies were carried in pH 1.2 buffer. The polymeric beads containing 20 and 30 %w/v oil showed excellent floating while beads containing 10 %w/v oil were found to be non-floating. The dissolution studies were carried in pH 1.2 buffer, pH 1.2 buffer containing 1% SLS and pH 6.8 phosphate buffer. A significantly low amount of drug release was observed in pH 1.2 buffer due to limited solubility of obuprofen in acidic media and faster drug release was observed in pH 6.8 phosphate buffer. A faster drug release was observed in pH 1.2 buffer containing sodium lauryl sulphate.

Keywords

Ionotropic Gelation, Floating, Controlled Release, Polymeric Beads.

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P. S. Salve ¹

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

Abstract

The present study deals with formulation of sustained release tablet of ibuprofen for colon targeting. Tablets were prepared using combination of guar and xanthan gum. The drug excipient interaction studies were carried out by FTIR and DSC. The prepared matrixes (GG :XG, 4:6) form enzyme controlled delivery systems with nearly 50 to 60% w/w of the tablet content being constituted by polysaccharides degradable by colonic microflora. Biodegradability studies of guar and xanthan gum was carried out in presence of 4% w/v RCC and galactomannase enzyme (0.1 mg/ml.) by viscosity measurement using Brookfield viscometer and significant decrease in viscosity was found with 4% RCC after 24 h incubation. In vitro drug release studies shows that guar and xanthan gum in 4:6 has optimum release in a controlled manner for 24 h.

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