The Kinetics of Drug Release from Ethylcellulose Solid Dispersions

Najib, Naji M.; Suleiman, Muhannad T.

doi:10.3109/03639048509087779

Cited by 114 publications

(48 citation statements)

References 10 publications

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“…For a gastroretentive system, drug release in the fed state condition is one of the important optimization criteria, hence solubility modulation of RHCl in varying molar environments of CA 398-10-coated NaCl crystals at pH 2.5 (low fed) and pH 6.5 (high fed) was assessed (21). The aim of solubility modulation was to achieve the target solubility range of 30-150 mg/mL that was presumed to be sufficient for osmotically regulated delivery of RHCl.…”

Section: Solubility Modulation Of Rhclmentioning

confidence: 99%

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

2012

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Abstract. A nondisintegrating, floating asymmetric membrane capsule (FAMC) was developed to achieve site-specific osmotic flow of a highly water-soluble drug, ranitidine hydrochloride (RHCl), in a controlled manner. Solubility suppression of RHCl was achieved by the common ion effect, using optimized coated sodium chloride as a formulation component. The capsular wall of FAMC was prepared by the phase inversion process wherein the polymeric membrane was precipitated on glass pins by dipping them in a solution of cellulose acetate followed by quenching. Central composite design was utilized to investigate the influence of independent variables, namely, level(s) of membrane former, pore former, and osmogen, on percent cumulative drug release (response). The release mechanism of RHCl through FAMC was confirmed as osmotic pumping. The asymmetry of the membrane was characterized by scanning electron microscopy that revealed a dense nonporous outer region of membrane supported by an inner porous region. Differential scanning calorimetry indicated no incompatibility between the drug and excipients. In vitro drug release in three biorelevant media, pH 2.5 (low fed), pH 4.5 (intermediate fed), and pH 6.5 (high fed), demonstrated pH-independent release of RHCl (P>0.05). Floating ability for 12 h of the optimized FAMC9 was visually examined during the in vitro release studies that showed maximal drug release with zero-order kinetics (r 2 00.9991). Thus, a novel osmotically regulated floating capsular system was developed for site-specific delivery of RHCl.

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Section: Solubility Modulation Of Rhclmentioning

confidence: 99%

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

2012

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“…The zero-order rate [18] ( Equation 1) describes systems where the drug release is independent on its concentration, and this is applicable to the dosage forms like transdermal system, coated forms, osmotic system as well as matrix tablets with low soluble drugs. Where, Q t is the amount of drug released at time t, k 0 is release rate constants for zero-order.…”

Section: Kinetics Of Drug Releasementioning

confidence: 99%

Modified solvent evaporation technique for purpose and categorization of Novel Floating Microspheres of Metronidazole: Optimization of pharmacokinetics, in-vitro and stability study using special process capricious like Emulsifier concentration, stirring rate

Bhardwaj¹,

Gupta²,

Chaurasia³

et al. 2017

IJRDPL

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Purpose of present study involves the development of floating microspheres of metronidazole as a model drug, using the modified solvent diffusion evaporation technique. Eudragit S100 and Eudragis RS100 were used in the different ratio as polymers for development of microspheres. The microspheres were characterized for surface morphology by SEM, yield, buoyancy, incorporation efficiency and micromeritic properties. The in-vitro drug release studies were performed in simulated gastric fluid at pH 1.2. Different kinetic models were also applied on drug release from selected formulations. Stability studies were additionally subjected for optimized formulations. The yield of microspheres was good. Microspheres showed satisfactory flow properties. SEM confirmed the spherical size, perforated smooth surface and a hollow cavity in them. Microspheres exhibited floating properties for more than 10 hours. Stability studies showed no significant change in residual drug content of floating Microspheres.

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“…The zero order describes the systems, where the drug release is independent of its concentration. [26] The first order equation describes the release from systems, where release rate is concentration dependent. [27] According to Higuchi model, the drug release from the insoluble matrix is directly proportional to square root of time and is based on Fickian diffusion.…”

Section: Release Models and Kineticsmentioning

confidence: 99%

Untitled

Kumaravelrajan¹

2016

AJP

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Introduction: A system that can deliver multidrugs at a controlled rate is very important to the treatment of various chronic diseases such as diabetes, asthma, and hypertension. In general, both highly and poorly water-soluble drugs are not good candidates for elementary osmotic delivery, so in the present investigation nifedipine-hydroxyproyl-β-cyclodextrin (1:1) inclusion complex was used to modulate the solubility of nifedipine (NP) within the core and metoprolol was used not only as the active ingredient but also as osmotic agent. Materials and Methods: NP-cyclodextrin complex was prepared by coprecipitation method. The tablets were prepared and coated with cellulose acetate phthalate-containing dibutyl phthalate as plasticizer at various concentrations. The coated tablets drilled for orifice. The orifice size, level of plasticizer, and coating thickness were used as formulation variables. Finally, the optimized formulation was studied for different pH, agitational speed, and release mechanism. The optimized formulation was also subjected to in vivo prediction for the desired C max and C min using superposition method. Results: Formulation variables such as orifice size, level of plasticizer, and coat thickness of semipermeable membrane were found to affect the drug release from the developed formulations. The optimal elementary osmotic pump was found to deliver both drugs at a rate of approximately zero order for up to 10 h independent of pH and agitational intensity but dependent on the osmotic pressure of the release media. Conclusion: Hence, the prototype design of the system could be applied to other combinations of drugs used for cardiovascular diseases, diabetes, etc.

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The Kinetics of Drug Release from Ethylcellulose Solid Dispersions

Cited by 114 publications

References 10 publications

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

Osmotically Regulated Floating Asymmetric Membrane Capsule for Controlled Site-Specific Delivery of Ranitidine Hydrochloride: Optimization by Central Composite Design

Modified solvent evaporation technique for purpose and categorization of Novel Floating Microspheres of Metronidazole: Optimization of pharmacokinetics, in-vitro and stability study using special process capricious like Emulsifier concentration, stirring rate

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