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ABSTRACT: Microcrystalline cellulose (MCC) is the most widely used extrusion-spheronization aid but is associated with several limitations such as adsorption of actives, longer dissolution time, and degradation of some sensitive drugs such as ranitidine.
This article reviews a number of natural, semisynthetic, and synthetic agents, such as cross-linked polyvinylpyrrolidone, carrageenan, chitosan, pectinic acid, modified starches, coprocessed MCC, glycerides, chitosan, sodium alginate, and β-cyclodextrin (CD) for their potential as alternative extrusion-spheronization aids to MCC.
Alternative spheronizing aids were characterized and evaluated based on their intrinsic properties such as solubility, water absorption and retention capacity, rheology, surface properties, binding capacity, drug release, and pellets properties such as sphericity, porosity, and friability with respect to MCC.
Crospovidone, carrageenan, chitosan, pectinic acid, glycerides, β-CD, and cellulose derivatives are effective alternative spheronizing aids and can be used to prepare pellets without any plasticizer or lubricant. But pellets with polyethylene oxide can only be produced with the use of plasticizer and/or lubricant. However, none of them succeeded to provide the same flexibility in formulation and processing during extrusion-spheronization as observed for MCC (e.g., less water-holding capacity, narrow liquid range providing the correct rheology for extrusion-spheronization, addition of binder required to obtain sufficient mechanical strength).
Drug Development and Industrial Pharmacy 11/2010; 36(11):1364-76. · 1.49 Impact Factor
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ABSTRACT: Microcrystalline cellulose (MCC) is well established as an extrusion spheronisation aid for the preparation of pellets. Crospovidone (Polyplasdone XL-10) is compared with microcrystalline cellulose for the preparation of melt-in-mouth pellets. Taste-masked fexofenadine hydrochloride was incorporated in the melt-in-mouth formulation. Crospovidone was found to be well suited as extrusion-spheronisation aid for the preparation of melt-in-mouth pellets. The great advantage of crospovidone is, however, the disintegrating properties of the pellets after only a short time of exposure to liquid. Crospovidone was successfully employed as an extrusion-spheronisation aid to produce melt-in-mouth pellets obviating the need of a traditional extrusion-spheronisation aid, MCC. Dual properties of Crospovidone were explored viz. as an extrusion-spheronisation aid and a disintegrant.
AAPS PharmSciTech 06/2010; 11(2):917-23. · 1.43 Impact Factor
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ABSTRACT: The present paper was focused on exploiting Plackett-Burman design to screen the effect of nine factors--poly (ethylene oxide) molecular weight (X(1)), poly (ethylene oxide) amount (X(2)), ethylcellulose amount (X(4)), drug solubility (X(5)), drug amount (X(6)), sodium chloride amount (X(7)), citric acid amount (X(8)), polyethylene glycol amount (X(9)), and glycerin amount (X(11)) on the release of drugs from the extended release extrudates, i.e., release rate and release mechanism. The experiments were carried out according to a nine-factor 12-run statistical model and subjected to an 8-h dissolution study in phosphate buffer pH 6.8. The significance of the model was indicated by the ANOVA and the residual analysis. Poly (ethylene oxide) amount, ethylcellulose amount and drug solubility had significant effect on the T90 values whereas poly (ethylene oxide) amount and ethylcellulose amount had significant effect on the n value.
AAPS PharmSciTech 06/2010; 11(2):936-44. · 1.43 Impact Factor
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ABSTRACT: This paper discusses the development of a stability-indicating reversed-phase LC method for analysis of cholecalciferol as
the bulk drug and in formulations. The mobile phase was acetonitrile–methanol–water 50:50:2 (v/v). The calibration plot for the drug was linear in the range 0.4–10μgmL−1. The method was accurate and precise with limits of detection and quantitation of 64 and 215ng, respectively. Mean recovery
was 100.71%. The method was used for analysis of cholecalciferol in pharmaceutical formulations in the presence of its degradation
products and commonly used excipients.
Chromatographia 01/2009; 69(3):385-388. · 1.20 Impact Factor
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ABSTRACT: This article focuses on preparation and evaluation of a once a day ophthalmic delivery system for ciprofloxacin hydrochloride based on the concept of pH-triggered in situ gelation. The in situ gelling system involves the use of polyacrylic acid (Carbopol 980NF) as a phase transition polymer, hydroxypropyl methylcellulose (Methocel K100LV) as a release retardant, and ion exchange resin as a complexing agent. Ciprofloxacin hydrochloride was complexed with ion exchange resin to avoid incompatibility between drug and polyacrylic acid. The developed formulation was stable, and nonirritant to rabbit eyes and in vitro drug release was found to be around 98% over a period of 24 hours.
Drug Development and Industrial Pharmacy 05/2008; 34(4):445-52. · 1.49 Impact Factor
