A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches

Jeans, Christopher W.; Heard, Charles Martin

doi:10.1016/s0378-5173(99)00215-x

Cited by 18 publications

(5 citation statements)

References 11 publications

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“…The in vivo skin absorption profile of PQ was also investigated through employment of a TTS based on ethyl cellulose polymer, indicating controlled and systemic delivery of the drug over a period of 40 h [102]. The permeation of PQ across full-thickness excised human skin from two acrylate transdermal adhesives was also studied, suggesting that a relatively simple transdermal adhesive patch formulation incorporating PQ can deliver suitable doses to provide new treatment and prophylaxis regimens for P. vivax and P. ovale malaria [103].…”

Section: A Yet Unveiled Mechanism Of Actionmentioning

confidence: 99%

Primaquine revisited six decades after its discovery

Vale¹,

Moreira²,

Gomes³

2009

European Journal of Medicinal Chemistry

321

308

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Section: A Yet Unveiled Mechanism Of Actionmentioning

confidence: 99%

Primaquine revisited six decades after its discovery

Vale¹,

Moreira²,

Gomes³

2009

European Journal of Medicinal Chemistry

321

308

View full text Add to dashboard Cite

“…The target skin permeation rate for TIZ was calculated using the following equation (Jeans and Heard, 1999) using available pharmacokinetic data (Moffat et al, 2006):…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

“…In the present study, Transcutol ® increased flux of TIZ and, from the available literature, it appears that the effect of Transcutol  may well depend on the nature of the drug being tested. Much of the literature reports a reduction in flux in the presence of Transcutol  ; however, these studies employed relatively hydrophobic drugs such as hydrocortisone, primaquine, dexamethasone, melatonin, glibenclamide, and glipizide (Kikwai et al, 2002;Minghetti et al, 2007;Panchagnula and Ritschel, 1991;Jeans and Heard, 1999;Zhao and Singh, 2000;Vaddi et al, 2001;Morimoto et al, 2002;Mayorga, 1996;Kogan and Garti, 2006;Udupa, 2002, 2003;Williams and Barry, 2004). In contrast, TIZ is a hydrophilic drug and increased permeation was observed in the presence of Transcutol ® which is in agreement with the results of Aboofazeli et al (2002) for another hydrophilic drug, nicardipine hydrochloride.…”

Section: In Vitro Skin Permeation Studiesmentioning

confidence: 99%

A combined approach of chemical enhancers and sonophoresis for the transdermal delivery of tizanidine hydrochloride

et al. 2009

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“…They demonstrated that acrylate PSA with a carboxyl group provided the lowest permeation rate, which may be due to the high affinity of ketoprofen for PSA. Jeans and Heard (1999) reported that the chemical nature of PSA can affect the solubility of drug and the PSAs containing acidic side-chains were not compatible with the basic form of primaquine. Therefore, we suggest that there was an interaction between the secondary amino group of tulobuterol and the carboxyl group of the acrylate polymer and that a drug's chemical structure and the functional group in PSAs must be considered in order to formulate a transdermal patch system.…”

Section: Effect Of Acrylic Polymer On Skin Permeation Of Tulobuterol mentioning

confidence: 99%

Characterization of monolithic matrix patch system containing tulobuterol

et al. 2008

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The aim of this study was to investigate the effect of the functional groups in acrylic adhesive on tulobuterol uptake, release rate and permeation rate across rat dorsal skin. In addition, the relationship between these parameters was identified in order to formulate the monolithic matrix patch system. Seven acrylate pressure sensitive adhesives were used in this study with three different functional groups as follows: (1) no functionality (DT-4098), (2) hydroxyl group (DT-2287, DT-2510, DT-2525, DT-2516), and (3) carboxyl group (DT-2353, DT-2852). Tulobuterol-uptake in PSA was determined by the drug-uptake method. The amount of tulobuterol-uptake in acrylic polymers with a carboxyl group was higher than those in acrylate pressure sensitive adhesives with either a hydroxyl group or a nonfunctional group. The release rate of tulobuterol from the monolithic patches was evaluated and DT-2353 and DT-2852, which contained a carboxyl group, showed lower release rates of tulobuterol than the other acrylate pressure sensitive adhesives. The skin permeation of tulobuterol was investigated using excised rat dorsal skin and the permeation rate of tulobuterol from DT-2353 and DT-2852 was also lower than the other acrylate pressure sensitive adhesives. Taking into consideration the relationship between all the parameters, pressure sensitive adhesives can be categorized into two groups: those containing a carboxylic acid functional group and those containing a non-carboxylic group. These results indicate that there was an interaction between the secondary amino group of tulobuterol and the carboxyl group of the acrylate polymer. Therefore, we suggest that a drug's chemical structure and functional groups in pressure sensitive adhesives must be considered in order to formulate a transdermal patch system.

show abstract

A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches

Cited by 18 publications

References 11 publications

Primaquine revisited six decades after its discovery

Primaquine revisited six decades after its discovery

A combined approach of chemical enhancers and sonophoresis for the transdermal delivery of tizanidine hydrochloride

Characterization of monolithic matrix patch system containing tulobuterol

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