Formulation and in vitro Evaluation of Eudragit® Microspheres of Stavudine

Sahoo, Sabuj; Mallick, Abdul Arif; Barik, B. B.; Senapati, Prakash Chandra

doi:10.4314/tjpr.v4i1.14622

Cited by 31 publications

(39 citation statements)

References 12 publications

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“…Slope values (n > 1.0) suggest that the drug permeation from transdermal patches (T-2 to T-7) followed the super case II transport mechanism, possibly owing to chain disentanglement and swelling of hydrophilic polymer, HPMC. Formulation T-7 with ERL as the rate-controlling membrane and Span 80 was found to be better, since constant and about 90% of the drug permeation was observed up to 24 h. The higher proportion of quaternary ammonium groups in ERL resulted in rapid hydration and drug release, whereas the lower proportion of ammonium groups in ERS is responsible for prolonged release of carvedilol (17). T-7 Fig.…”

Section: Resultsmentioning

confidence: 99%

Development and evaluation of carvedilol transdermal patches

Tanwar¹,

Chauhan²,

Sharma³

2007

Acta Pharmaceutica

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Carvedilol is a novel, multiple-action cardiovascular drug that is currently approved in many countries for the treatment of hypertension. The reduction in blood pressure produced by carvedilol results primarily from beta-adrenoceptor blockade and vasodilation, the latter resulting from alpha 1-adrenoceptor blockade. These actions as well as several other carvedilol activities are associated with cardioprotection in animal models that occurs to a degree that is greater than that observed with other drugs. The multiple actions of carvedilol may also provide the underlying rationale for the use of the drug in the treatment of coronary artery disease and congestive heart failure (1).Carvedilol is well absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism in the liver; its absolute bioavailability is about 25%. It has a half-life of 2.2 ± 0.3 h; longer half-lives of about 6 h have been measured at lower concentrations (2, 3). Transdermal patches of carvedilol with a HPMC-drug reservoir were prepared by the solvent evaporation technique. In this investigation, the membranes of Eudragit RL100 and Eudragit RS100 were cast to achieve controlled release of the drug. The prepared patches possessed satisfactory physicochemical characteristics. Thickness, mass and drug content were uniform in prepared batches. Moisture vapour transmission through the patches followed zero-order kinetics. In vitro permeation studies were performed using a K-C diffusion cell across hairless guinea pig skin and followed the super case II transport mechanism. The effects of non-ionic surfactants Tween 80 and Span 80 on drug permeation were studied. The non--ionic surfactants in the patches increased the permeation rate, Span 80 exhibiting better enhancement relative to Tween 80. The patches were seemingly free of potentially hazardous skin irritation.

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Section: Resultsmentioning

confidence: 99%

Development and evaluation of carvedilol transdermal patches

Tanwar¹,

Chauhan²,

Sharma³

2007

Acta Pharmaceutica

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“…1 filter paper and the filtrate was centrifuged using a tabletop centrifuge to remove the polymeric debris.Then the polymeric debris was washed twice with fresh solvent (water) to extract any adhered drug. The clear supernatant solution was then analyzed for glipizide content by a UV spectrophotometer (JASCO-V500, Japan) at the λ max value of 275 nm [5][6][7] . The complete extraction of drug was confirmed by repeating the extraction process on the already extracted polymeric debris.…”

Section: Percent Yield and Entrapment Efficiencymentioning

confidence: 99%

Evaluation of Entrapment Efficiency of Glipizide Microsphere

Arora¹

2012

iosrphr

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“…The drug (D4T, thymidine) is an FDA-approved drug for clinical use in the treatment of HIV infection, AIDS, and AIDS-related conditions. 7 According to Bio-pharmaceutics Classification System (BCS), D4T can be assigned to BCS class I. 7 D4T is typically administered orally as a capsule and an oral solution.…”

Section: Introductionmentioning

confidence: 99%

“…7 According to Bio-pharmaceutics Classification System (BCS), D4T can be assigned to BCS class I. 7 D4T is typically administered orally as a capsule and an oral solution. The virustatic drug has a very short half-life (1.30 h).…”

Section: Introductionmentioning

confidence: 99%

Microspheres Embedded In Microbeads: A Novel Approach to Improve Various Controlled Release Characteristics of Highly Water Soluble Drug through Ionic Gelation Method

Sahoo¹,

Swain²,

Sen³

et al. 2015

IJPER

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The major hindrance behind the preparation of gellan microbeads by simple ionic gelation technique with aqueous soluble drugs is their low entrapment efficiency and sometimes its faster dissolution characteristics. This limits the employment of such a simple method for the preparation of microbeads of water-soluble drugs like stavudine. In the present study a novel attempt has been undertaken by embedding stavudine loaded Eudragit RSPO microspheres into gellan microbeads by ionotropic gelation method with an aim to improve its controlled drug delivery characteristics. The prepared microbeads were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy, and optical microscopy for surface topography, drug polymer interaction and particle size analysis respectively. Other studies like drug content, encapsulation efficiency and drug release studies were also carried out. The resulting microspheres embedded in microbeads were free flowing in nature with mean particle size ranging from 544.2-564.2 µm. SEM photomicrographs distinctly shows the microspheres embedded within the microbeads effectively with a smooth surface topography and the gellan microbeads containing D4T only are spherical in nature with rough surface. The FTIR study ascertained the compatibility of the drug within the formulation. The microspheres embedded in microbeads had enhanced percentage of drug content, drug entrapment efficiency and controlled release characteristics as compared to beads containing stavudine only. The mechanism of drug release from the formulations were found to follow non Fickian type diffusion with "n" value between 0.5 to 1but in case of stavudine loaded Eudragit RSPO microspheresit was found to be Fickian type.

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Formulation and in vitro Evaluation of Eudragit® Microspheres of Stavudine

Cited by 31 publications

References 12 publications

Development and evaluation of carvedilol transdermal patches

Development and evaluation of carvedilol transdermal patches

Evaluation of Entrapment Efficiency of Glipizide Microsphere

Microspheres Embedded In Microbeads: A Novel Approach to Improve Various Controlled Release Characteristics of Highly Water Soluble Drug through Ionic Gelation Method

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