Bioavailability of estradiol from two matrix transdermal delivery systems: Menorest® and Climara®

Andersson, Tomas; Stehle, B.; Davidsson, Bertil; Höglund, Peter

doi:10.1016/s0378-5122(99)00088-2

Cited by 25 publications

(10 citation statements)

References 9 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Experimental results obtained in this study showed no significant change in E 2 plasma values under conditions of patch removal and reapplication with transdermal matrix technology. Our results are in contrast to a very recently published clinical study, where the investigators found a significant E 2 plasma concentration increase after patch removal 36. At the time they conducted their clinical study, the authors were not aware that substantial E 2 circadian variation existed and that several blood samples have to be taken to detect C max of the day.…”

Section: Discussioncontrasting

confidence: 99%

“…The lack of taking periodicity in plasma E 2 into consideration will produce differences in the E 2 bioavailability determination 15. Therefore, published results in clinical studies concerning the patch removal and reapplication problem17,36 might be explained by not taking into account circadian variation in plasma values. If patches are not compared under identical conditions, including the same sampling time, inconsistent results can be produced easily.…”

Section: Discussionmentioning

confidence: 99%

“…Also, the same group found, in contrast to their first observation, no statistically significant difference between 1 month and 6 months, when another patch was compared. We reported earlier that in contrast to the reservoir type technology, E 2 plasma profile produced by matrix technology exhibits a periodic variation during the day,15 which was recently confirmed by another group 18. Therefore, comparisons on the basis of one sample per patient are difficult to justify.…”

Section: Introductionmentioning

confidence: 97%

See 2 more Smart Citations

17β‐Estradiol Matrixpatch Removal and Reapplication in Postmenopausal Women: Experimental Results

Rohr

Saeger-Lorenz

2002

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Section: Discussioncontrasting

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 97%

See 1 more Smart Citation

17β‐Estradiol Matrixpatch Removal and Reapplication in Postmenopausal Women: Experimental Results

Rohr

Saeger-Lorenz

2002

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…This response pattern can be explained by (a) different skeletal sites responding individually to estradiol and (b) the recently reported second order polynomial correlation established for another range of patches between serum estradiol levels and the lumbar spine BMD response [12]. The concentration-response curve peaks at around 80 pg estradiol/ml -the average peak value seen in women treated with the 50 mg/day patch of that series [3,18] and thus a value exceeded by up to 50% of them but only by 5% or less with the E-50 patch of the Evorel series of patches [6]. A dose-response curve of similar characteristics for hip BMD can be constructed for a 7-day patch range with a maximum response at about 70 mg estradiol/day [17].…”

Section: Discussionmentioning

confidence: 92%

Effects of Transdermal Estradiol Delivered by a Matrix Patch on Bone Density in Hysterectomized, Postmenopausal Women: A 2-year Placebo-Controlled Trial

Arrenbrecht

Boermans

2002

Osteoporosis International

View full text Add to dashboard Cite

This 2-year, double-masked, randomized, placebo-controlled trial was designed to evaluate the safety and efficacy in preventing bone loss in postmenopausal women of two doses of transdermal 17betaestradiol (estradiol) delivered by a matrix patch, compared with placebo. One hundred and sixty healthy, hysterectomized postmenopausal volunteers aged 40-60 years with serum estradiol levels < 20 pg/ml were started on treatment at four centers in The Netherlands. Every 6 months, bone mineral density (BMD) was measured by dual-energy X-ray absorptiometry (DXA) at the lumbar spine, non-dominant wrist and left hip, and markers of bone turnover were assessed in urine and serum. The treatment arms were: estradiol, 100 microg/day (E-100, n = 53), oestradiol, 50 microg/day (E-50, n = 54), placebo (P-100, placebo to E-100, n = 27 or P-50, placebo to E-50, n = 26). Treatment was continued for up to 2 years. After 24 months, BMD of the lumbar spine in the E-100 group differed by 7.7% [5.8-9.5%] (mean [95% confidence interval]) from the placebo group and showed a mean (s.e.m.) increase in BMD from baseline of 5.9% (0.69%). For the E-50 group the difference compared with placebo was 6.2% [4.4-8.0%] and the absolute increase was 4.5% (0.62%); in the placebo group, the absolute change was -2.3% (0.48%). In the total wrist, the changes were: E-100: difference compared with placebo 2.5% [1.5 3.6%], absolute increase 0.6% (0.3%); E-50: difference compared with placebo 2.9% [1.8-3.9%], absolute increase 0.7% (0.25%); and absolute change on placebo: -2.5% (0.35%). In the total hip, the changes were: E-100: difference compared with placebo 3.7% [2.2-5.2%], absolute increase 2.8% (0.5%); E-50: difference compared with placebo: 3.2% [1,8-4.7%], absolute change 2.4% (0.36%); and absolute change on placebo -1.4% (0.66%). Three markers of bone turnover--serum bone-specific alkaline phosphatase, serum osteocalcin and urinary CTX--fell significantly during the trial. Breast pain was reported by 8% of women on placebo, by 6% of women on E-50 and by 17% of women on E-100. Estradiol delivered by the E-50 matrix patch effectively reversed bone loss in hysterectomized postmenopausal women with few side-effects. The marginal additional gain in BMD with the higher dose may be offset by a more important side effect profile.

show abstract

“…The process of drug release in most controlledrelease devices including transdermal patches is governed by diffusion 25 and the polymer matrix has a strong influence on the diffusivity as the motion of a small molecule is restricted by the three-dimensional network of polymer chains. The alteration of the crosslinking and the modification of structural arrangements of polymers by using different blends of polymer were already reported.…”

Section: Discussionmentioning

confidence: 99%

Design, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt

Arora

Mukherjee

2002

Journal of Pharmaceutical Sciences

162

117

View full text Add to dashboard Cite

Bioavailability of estradiol from two matrix transdermal delivery systems: Menorest® and Climara®

Cited by 25 publications

References 9 publications

17β‐Estradiol Matrixpatch Removal and Reapplication in Postmenopausal Women: Experimental Results

17β‐Estradiol Matrixpatch Removal and Reapplication in Postmenopausal Women: Experimental Results

Effects of Transdermal Estradiol Delivered by a Matrix Patch on Bone Density in Hysterectomized, Postmenopausal Women: A 2-year Placebo-Controlled Trial

Design, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt

Contact Info

Product

Resources

About