Sustained Release from Inert Wax Matrixes II: Effect of Surfactants on Tripelennamine Hydrochloride Release

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

doi:10.1002/jps.2600670321

Cited by 36 publications

(11 citation statements)

References 6 publications

(1 reference statement)

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“…Bees wax and cetyl alcohol can be used for sustained release of metformin HCl. The mechanism of drug release from wax matrices has been a matter of controversy since wax matrices tend to be more heterogeneous than other matrices (Dakkuri A et al 1978). The study reveals that, the release of water soluble drug, metformin HCl exhibited diffusion dominated mechanism.…”

Section: Resultsmentioning

confidence: 92%

Design and release characteristics of sustained release tablet containing metformin HCl

Basak¹,

Kumar²,

Ramalingam³

2008

Rev. Bras. Cienc. Farm.

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Section: Resultsmentioning

confidence: 92%

Design and release characteristics of sustained release tablet containing metformin HCl

Basak¹,

Kumar²,

Ramalingam³

2008

Rev. Bras. Cienc. Farm.

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“…Firstly, it is possible that the surfactant lowers the interfacial tension between the product and the dissolution fluid; secondly, it is possible that the surfactant acts as a wicking agent, causing the fluid to enter the dosage form; the surfactant may then dissolve and form pores (or other disruptions) from which the drug release may be affected (21). The same results were reported on the effect of surfactants on the dissolution profiles of flurbiprofen (22).…”

Section: And Discussionmentioning

confidence: 56%

“…Two possible mechanisms have been postulated as to why surfactants increase the rate of drug release from matrix formulations (21,22). Firstly, it is possible that the surfactant lowers the interfacial tension between the product and the dissolution fluid; secondly, it is possible that the surfactant acts as a wicking agent, causing the fluid to enter the dosage form; the surfactant may then dissolve and form pores (or other disruptions) from which the drug release may be affected (21).…”

Section: And Discussionmentioning

confidence: 99%

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Nokhodchi

Hassanzadeh²,

Monajjemzadeh³

et al. 2008

Acta Pharmaceutica

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Various methods are available to formulate water soluble drugs into sustained release dosage forms by retarding the dissolution rate. One of the methods used to control drug release and thereby prolong therapeutic activity is to use hydrophilic and lipophilic polymers. In this study, the effects of various polymers such as hydroxypropyl methylcellulose (HPMC), ethylcellulose (EC) and sodium carboxymethylcellulose (CMC) and surfactants (sodium lauryl sulphate, cetyltrimethylammonium bromide and Arlacel 60) on the release rate of captopril were investigated. The results showed that an increase in the amount of HPMC K15M resulted in reduction of the release rate of captopril from these matrices. When HPMC was partly replaced by NaCMC (the ratio of HPMC/NaCMC was 5:1), the release rate of the drug significantly decreased. However, there was no significant difference in release rate of captopril from matrices produced with ratios of 5:1 and 2:1 of HPMC/NaCMC. The presence of lactose in matrices containing HPMC and NaCMC increased the release rate of captopril. It was interesting to note that although partial replacement of HPMC by EC reduced the release rate of the drug (ratio of HPMC/EC 2:1), the release rate was increased when the ratio of HPMC/EC was reduced to 1:1. The effects of various surfactants on the release rate of captopril from HPMC/EC (1:1) matrices were also investigated. The results showed that the surfactants did not significantly change the release rate of the drug. Release data were examined kinetically and the ideal kinetic models were estimated for the drug release. The kinetic analysis of drug release data from various formulations showed that incorporation of surfactants in HPMC/EC matrices did not produce a zero-order release pattern.

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“…a-e The triangular-dimensional contour diagrams illustrating the effect of HVO, NaCMC, and MCC on the release of Cilostazol; a 1-h drug release percent, b 4-h drug release percent, c 8-h drug release percent, d 12-h drug release percent, and e overlay plot kind of matrixes. For example, in some cases, it has been reported that the mechanism of release from wax matrices involves the leaching of drug by the eluting medium, while others indicated that it is diffusion controlled and is best described by Higuchi model (30,38). In the current study, the release exponent (n) of the optimized solid dispersion based disintegration mediated wax matrix (Global solution observed; GS o ) was 0.85 (r 2 =0.999 and K=0.132), suggesting a non-Fickian (anomalous) release, with reasonably an equal preponderance of the diffusion and zero-order mechanisms.…”

Section: Release Rate Kineticsmentioning

confidence: 99%

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

Verma

Rudraraju²

2014

AAPS PharmSciTech

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Abstract. The objective of this study was to develop a solid dispersion based controlled release system for drug substances that are poorly soluble in water. A wax-based disintegration mediated controlled release system was designed based on the fact that an amorphous drug can crystallize out from hydrophilic matrices. For this study, cilostazol (CIL) was selected as the model drug, as it exhibits poor aqueous solubility. An amorphous solid dispersion was prepared to assist the drug to attain a supersaturated state. Povidone was used as carrier for solid dispersion (spray drying technique), hydrogenated vegetable oil (HVO) as wax matrix former, and sodium carboxymethyl cellulose (NaCMC) as a disintegrant. The extreme vertices mixture design (EVMD) was applied to optimize the designed and developed composition. The optimized formulation provided a dissolution pattern which was equivalent to the predicted curve, ascertaining that the optimal formulation could be accomplished with EVMD. The release profile of CIL was described by the Higuchi's model better than zero-order, first-order, and Hixson-Crowell's model, which indicated that the supersaturation state of CIL dominated to allow drug release by diffusion rather than disintegration regulated release as is generally observed by Hixson-Crowell's model. The optimized composition was evaluated for disintegration, dissolution, XRD, and stability studies. It was found that the amorphous state as well as the dissolution profile of CIL was maintained under the accelerated conditions of 40°C/75% RH for 6 months.

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Sustained Release from Inert Wax Matrixes II: Effect of Surfactants on Tripelennamine Hydrochloride Release

Cited by 36 publications

References 6 publications

Design and release characteristics of sustained release tablet containing metformin HCl

Design and release characteristics of sustained release tablet containing metformin HCl

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Disintegration Mediated Controlled Release Supersaturating Solid Dispersion Formulation of an Insoluble Drug: Design, Development, Optimization, and In Vitro Evaluation

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