Sustained Release from Inert Wax Matrixes I: Drug-Wax Combinations

Schroeder, Hans G.; Dakkuri, Adnan; DeLuca, Patrick P.

doi:10.1002/jps.2600670320

Cited by 19 publications

(4 citation statements)

References 7 publications

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“…Such behaviour is unlikely to result in any dissolution enhancement of ND. Similar trends were obtained with tripelennamine HCl –carnauba wax and tolazoline‐carnauba wax binary systems [22]…”

Section: Resultssupporting

confidence: 81%

Eutectic, monotectic and immiscibility systems of nimesulide with water-soluble carriers: phase equilibria, solid-state characterisation and in-vivo/pharmacodynamic evaluation

Abdelkader

Abdallah

Salem

et al. 2014

Journal of Pharmacy and Pharmacology

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Section: Resultssupporting

confidence: 81%

Eutectic, monotectic and immiscibility systems of nimesulide with water-soluble carriers: phase equilibria, solid-state characterisation and in-vivo/pharmacodynamic evaluation

Abdelkader

Abdallah

Salem

et al. 2014

Journal of Pharmacy and Pharmacology

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“…However, the properties of a eutectic mixture would be expected to differ from those of a simple mixture, if particle size and solubility of the drug were altered, then the dissolution characteristics and the in vivo availability could be influenced. Therefore, an investigation of the matrix-type sustained-release dosage form should commence with some basic phase studies to determine whether a drug-wax interaction occurs and a t what composition a eutectic mixture exists (17).…”

Section: Resultsmentioning

confidence: 99%

Formulation of Controlled-Release Baclofen Matrix Tablets II: Influence of Some Hydrophobic Excipients on the Release Rate and In Vitro Evaluation

2008

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The aim of this study was to investigate the influence of polymer level and type of some hydrophobic polymers, including hydrogenated castor oil (HCO); Eudragit RS100 (E-RS100); Eudragit L100 (E-L100), and some fillers namely mannitol [soluble filler], Dibasic calcium phosphate dihydrate (Emcompress) and anhydrous dibasic calcium phosphate [insoluble fillers] on the release rate and mechanism of baclofen from matrix tablets prepared by a hot-melt granulation process (wax tablets) and wet granulation process (E-RS100 and E-L100 tablets). Statistically significant differences were found among the drug release profile from different classes of polymeric matrices. Higher polymeric content (40%) in the matrix decreased the release rate of drug because of increased tortuosity and decreased porosity. At lower polymeric level (20%), the rate and extent of drug release was elevated. HCO was found to cause the strongest retardation of drug. On the other hand, replacement of Emcompress or anhydrous dibasic calcium phosphate for mannitol significantly retarded the release rate of baclofen, except for E-L100 (pH-dependent polymer). Emcompress surface alkalinity and in-situ increase in pH of the matrix microenvironment enhanced the dissolution and erosion of these matrix tablets. The release kinetics was found to be governed by the type and content of the excipients (polymer or filler). The prepared tablets showed no significant change in drug release rate when stored at ambient room conditions for 6 months.

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“…The clearance mechanisms and any long-term hazards associated with paraffin wax in alveolar regions of lung were not investigated and are still unknown. Waxes have been used to control the release of drugs in microsphere products (16,25). In addition, waxes have been used to monitor lung deposition and clearance mechanisms.…”

Section: Discussionmentioning

confidence: 99%

Controlled dissolution from wax-coated aerosol particles in canine lungs

Pillai

Yeates²,

Miller

et al. 1998

Journal of Applied Physiology

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Treatment of pulmonary and systemic diseases may be improved and toxicity reduced by pulmonary deposition of drug-containing aerosols exhibiting delayed dissolution. Aqueous disodium fluorescein and pentamidine aerosols were dried, concentrated, and condensation coated with paraffin wax. The apparent mass median aerodynamic diameters of the coated fluorescein particles were 2.8-4.0 microns. Wax-to-fluorescein ratios were 0.38-1.05. The dissolution half times determined using a single-pass flow system were 1.5 min for uncoated fluorescein and 0.8 min for uncoated pentamidine. These increased over threefold when the aerosols were coated with paraffin wax to maxima of 5.3 and 2.6 min, respectively. Wax-coated aerosols generated from fluorescein mixed with 99mTc-labeled iron oxide colloid delivered to the canine lungs demonstrated a 3.4-fold increase in the absorption half time of disodium fluorescein compared with uncoated fluorescein (11.2 vs. 38.4 min). The absence of changes in pulmonary function on inhalation of these wax-coated aerosols, together with a high drug load and delayed release, establishes a foundation for future therapeutic applications.

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Sustained Release from Inert Wax Matrixes I: Drug-Wax Combinations

Cited by 19 publications

References 7 publications

Eutectic, monotectic and immiscibility systems of nimesulide with water-soluble carriers: phase equilibria, solid-state characterisation and in-vivo/pharmacodynamic evaluation

Eutectic, monotectic and immiscibility systems of nimesulide with water-soluble carriers: phase equilibria, solid-state characterisation and in-vivo/pharmacodynamic evaluation

Formulation of Controlled-Release Baclofen Matrix Tablets II: Influence of Some Hydrophobic Excipients on the Release Rate and In Vitro Evaluation

Controlled dissolution from wax-coated aerosol particles in canine lungs

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