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At least 1,567 records · Page 87Linked to original sources
PubMed1998

Absorption, metabolism, and disposition of [14C]SDZ ENA 713, an acetylcholinesterase inhibitor, in minipigs following oral, intravenous, and dermal administration.

PURPOSE: SDZ ENA 713 (rivastigmine) is an acetylcholinesterase inhibitor intended for therapeutic use in Alzheimer's disease. The present study compared the pharmacokinetics of [14C]SDZ ENA 713 after intravenous, oral, and dermal administration to male minipigs, and also examined the effects of dose level and skin abrasion on transdermal absorption. METHODS: Four groups of 3 minipigs each received a single intravenous (0.1 mg/kg), single oral (1.0 mg/kg), or topical doses of 18 mg or 54 mg of [14C]SDZ ENA 713. Topical doses were administered as dermal patches on two occasions 10 days apart. On Study Day 1, test patches were applied to a virgin skin site. Placebo patches were applied to a separate skin site and were replaced daily during Days 1-10. On Study Day 11, test patches were applied to the site on which the placebo patches had been previously applied. After each dose, serial blood and quantitative urine and feces were collected at designated intervals for 7 days. Concentrations of radioactivity, parent drug, and metabolite ZNS 114-666 were measured in whole blood. Radioactivity was also determined in excreta, skin application sites (at study termination), and on used dermal patches (at 24 hr after application). RESULTS: Oral doses of [14C]SDZ ENA 713 were rapidly (tmax = 0.83 hr) and efficiently (ca. 93%) absorbed, although the bioavailability of the parent drug was low, ca. 0.5%, apparently due to extensive first-pass metabolism. Radioactivity was excreted mainly in the urine (approximately 90%) with a half-life of 56 hr, slightly longer than that observed after an intravenous dose, 46 hr. After dermal administration of [14C]SDZ ENA 713 to a virgin skin site, absorption was 8% at both dose levels investigated. Following daily application of placebo patches for 10 days, absorption from a [14C]SDZ ENA 713 dermal patch increased by approximately twofold, 17% and 19% of the 18 mg and 54 mg doses, respectively. The increase is possibly due to hydration or abrasion of the skin as a result of repeated application and removal of the adhesive patches. Whereas total absorption from the dermal dose was smaller than that from the oral dose, essentially all of the absorbed drug via the dermal route reached the systemic circulation intact, thus yielding a SDZ ENA 713 bioavailability 20-40 times greater than that of the oral dose. Metabolite ZNS 114-666 was rapidly formed and accounted for <4% of total drug-related material in the systemic circulation. CONCLUSIONS: Dermal administration in minipigs provided a markedly greater bioavailability of SDZ ENA 713 than the oral route. The extent of absorption was independent of dose within the range tested, and appeared to be enhanced by hydration or abrasion of the skin application site.

Administration, Cutaneous↗
PubMed2007

Safety and efficacy of transdermal fentanyl in patients with cancer pain: phase IV, Turkish oncology group trial.

We have performed a prospective evaluation of the efficacy, safety and convenience of the transdermal therapeutic system - fentanyl (TTS-F) in Turkish cancer patients when it was newly available in Turkey. Ninety-nine patients with historically confirmed malignancy and pain entered the study; the mean age was 55.1 (16-58) years. The study duration was 28 days. Transdermal therapeutic system - fentanyl was used in opioid-naïve or pre-treated patients. Most patients reported a decrease in pain severity. Use of rescue medication decreased from day 4 to day 28. The majority of patients rated patch convenience of use as excellent. A total of 22.2% of patients experienced adverse events that were either probably related or very likely to be related to the study drug. The majority of the adverse events mentioned were related to the digestive system. Eighteen serious adverse events were reported by 13 patients. Six events were doubtfully related, and 12 events were not related to the study drug. Four patients died during the trial. None of these deaths was attributed to the study drug. In conclusion, the trial showed that TTS-F is easily managed, effective and will help to enable the appropriate opioid administration to patients who are suffering from cancer pain in Turkey.

Administration, Cutaneous↗
PubMed2004

[Slow-release transdermal fentanyl used as anesthesia aided drug in ESS operation].

OBJECTIVE: To observe the safety of slow-release transdermal fentanyl (TDF) used as anesthesia aided drug in endoscopic sinus surgery (ESS) peri-operation. METHOD: In 30 cases of ESS operation, we observed their blood pressure, pulse and degree of blood oxygen saturation (SpO2%) before the TDF patch used and 10 min, 20 min, 30 min, 60 min after the patch used, their results were compared in respective. We observed the morbidity rate of patients accompanied with nausea, vomiting, bad appetite, skin reaction and vertigo at the same time. RESULT: There were no significant difference of blood pressure before and after the patch used, and so were the pulse and SpO2%. There were no patients accompanied with vomiting, vertigo and skin reaction. Four cases accompanied with nausea and bad appetite. CONCLUSION: TDF is a safe, effective and convenient anesthesia aided drug in ESS peri-operation.

Administration, Cutaneous↗
PubMedDate not supplied

Statistical optimization of transdermal drug delivery system of terbutaline sulfate by factorial analysis.

A matrix type of transdermal drug delivery system of terbutaline sulfate was designed and developed by full 3(2) factorial method using polyvinyl alcohol (PVA) of medium molecular weight and polyvinyl pyrrolidone (PVP K-30) as matrix forming polymer and propylene glycol as plasticizer. Patches were designed to deliver 62 micrograms/cm2/hr of the drug into the systemic circulation. These were evaluated for in vitro skin permeation study through excised guinea pig skin. The permeation followed Higuchi kinetics, as its coefficients of correlation (r = 0.965-0.978) predominates over other permeation kinetics. Various physico-chemical parameters of the patches were investigated. Statistical optimization of in vitro permeation rate of the drug from the films were evaluated using two way analysis of variance (ANOVA), regression analysis.

Administration, Cutaneous↗
PubMed2006

Differential sensitivity of three experimental pain models in detecting the analgesic effects of transdermal fentanyl and buprenorphine.

This is the first randomized controlled trial that tests the analgesic efficacy of transdermally delivered opioids in healthy volunteers and that assesses the sensitivity of different experimental pain tests to detect analgesia in this setting. Transdermal application of the full agonist fentanyl (TDF: 12.5 or 25 microg/h) and the partial agonist buprenorphine (TDB: 35 microg/h) was compared in three experimental models of acute pain (heat pain, painful electrical stimulation, cold pressor) in a double-blind, randomized, placebo-controlled, 4-arm crossover study with 20 healthy subjects (15 men, 5 women). Patches were administered for 72 h and pain levels measured at baseline and 24 and 72 h, with an 11-day wash-out. The cold pressor test was most sensitive to analgesic effects, with significant reductions in area under the pain intensity curve for all active compounds at 24 h (average reductions: 14% TDF 12.5 microg/h, 35% TDF 25 microg/h, 43% TDB 35 microg/h). There were significant increases in heat pain threshold for TDF 25 microg/h and TDB 35 microg/h. Painful electrical stimulation failed to demonstrate an analgesic effect. The magnitude of analgesia in the cold pressor model showed some correlation with TDF dosage and comparable effects for the full agonist fentanyl and the partial agonist buprenorphine. We conclude that the cold pressor test was most sensitive to analgesic effects in healthy subjects and that a transdermal dose of 12.5 microg/h fentanyl achieved significant pain reduction compared with placebo. Subjects experienced opioid-typical AEs including dizziness, nausea and vomiting. No serious AEs occurred.

Administration, Cutaneous↗
PubMed1988

Substitution therapy of hypogonadal men with transdermal testosterone over one year.

Current testosterone substitution therapy either by injectable or oral testosterone esters suffers from markedly fluctuating serum testosterone levels often far above or below the physiological range. Recently, a transdermal therapeutic system (TTS) for the delivery of testosterone was developed which, when applied to the scrotum, provides smooth serum testosterone levels. Here we report results from seven hypogonadal men treated with the TTS for 14 months by applying a new patch every day. In all patients serum testosterone and dihydrotestosterone (DHT) determined 3-5 h after applying a new patch increased significantly and remained within the physiological range during the entire treatment period. The DHT/testosterone ratio remained constant. In 4 of these patients and 2 others under TTS treatment serum testosterone and DHT were also determined over a 24-h period at regular intervals. In these patients serum testosterone levels in the physiological range were seen during the entire observation period, whereas an increase in the DHT/testosterone ratio occurred towards the end of the one-day treatment phase. All patients in the 14-month treatment study were clinically well substituted and responded with good compliance. Clinical chemistry showed no abnormalities during treatment. Thus, the TTS appears to be an effective and safe new modality for the treatment of male hypogonadism.

Administration, Cutaneous↗
PubMedDate not supplied

Pulsed estrogen therapy: pharmacokinetics of intranasal 17-beta-estradiol (S21400) in postmenopausal women and comparison with oral and transdermal formulations.

Pharmacokinetics of estradiol and estrone were assessed in postmenopausal women receiving S21400, a novel 17beta-estradiol formulation administered by nasal route; the results were compared with those obtained with oral and transdermal routes. Thirty six women received three treatments: a specified dose of 17beta-estradiol (100, 300 or 450 microg) given once and as 2 doses, 12 h apart, using three parallel dose groups in a randomised, crossover study. Thereafter, a reservoir patch (50 microg/day of 17beta-estradiol) or a tablet of 2 mg micronised 17beta-estradiol were randomly administered. Plasma concentrations of estradiol and estrone were measured by radioimmunoassays. Following intranasal dosing, estradiol was rapidly absorbed with plasma concentrations reaching maximal values (approximately 1400 pg/ml with a single 300 microg dose) after 10-30 min and returning within 12 h to levels of untreated postmenopausal women. Systemic exposure to estradiol was dose proportional and independent of the treatment regimen. Moreover, the dose of 300 microg gave an estimated 24 h systemic exposure to exogenous estradiol close to that of the 50 microg/day reservoir patch or the 2 mg tablet. The mean estrone to estradiol ratio was similar and 4-fold lower than those with the patch and the tablet, respectively. In conclusion, by this new route for estrogen replacement therapy, the nasal route, the pharmacokinetics of estradiol as S21400 were linear and displayed a 'pulsed' kinetic profile, different from those obtained with the usual routes of administration.

Administration, Cutaneous↗
PubMed1990

The relationship between serum estradiol-17 beta concentrations and induced pituitary luteinizing hormone surges in postmenopausal women.

The present study was designed to evaluate the effect of different serum concentrations of estradiol-17 beta (E2) on pituitary luteinizing hormone (LH) release in postmenopausal women. Serum E2 levels were evaluated in healthy postmenopausal women while they wore two, four, and six transdermal E2 delivery systems. The mean serum E2 levels at 48 hours after application of the devices were 185.5, 338.9, and 520.5 pg/mL, respectively, which were significantly different from each other. Serum E2 levels were stable throughout the first 48 hours of patch application but declined by a mean of 54% between 48 and 72 hours. Pituitary LH surges were induced with all three serum concentrations of E2 but were present more often with the higher serum values. There were no significant differences between the mean interval of device utilization and initiation, height, or duration of the induced pituitary LH surge at any of the three serum E2 concentrations studied.

Adult↗
PubMed1994

Nicotine patch therapy for smoking cessation combined with physician advice and nurse follow-up. One-year outcome and percentage of nicotine replacement.

OBJECTIVE: To determine the efficacy of a 22-mg nicotine patch combined with the National Cancer Institute program for physician advice and nurse follow-up in providing withdrawal symptom relief, 1-year smoking cessation outcome, and percentage of nicotine replacement. DESIGN: Randomized, double-blind, placebo-controlled trial. SUBJECTS: Two-hundred forty healthy volunteers who were smoking at least 20 cigarettes per day. INTERVENTIONS: Based on the National Cancer Institute program, subjects received smoking cessation advice from a physician. Follow-up and relapse prevention were provided by a study nurse during individual counseling sessions. Subjects were randomly assigned to 8 weeks of a 22-mg nicotine or placebo patch. MAIN OUTCOME MEASURES: Abstinence from smoking was verified by expired air carbon monoxide levels. Withdrawal symptoms were recorded during patch therapy, and the percentage of nicotine replacement was calculated by dividing serum nicotine and cotinine levels at week 8 of patch therapy by levels obtained while smoking. RESULTS: Higher smoking cessation rates were observed in the active nicotine patch group at 8 weeks (46.7% vs 20%) (P < .001) and at 1 year (27.5% vs 14.2%) (P = .011). Higher smoking cessation rates were also observed in subjects assigned to the active patch who had lower serum levels of nicotine and cotinine at baseline, and withdrawal symptom relief was better in the active patch group compared with placebo. CONCLUSIONS: Clinically significant smoking cessation can be achieved using nicotine patch therapy combined with physician intervention, nurse counseling, follow-up, and relapse prevention. Smokers with lower baseline nicotine and cotinine levels had better cessation rates, which provides indirect evidence that they had more adequate nicotine replacement with this fixed dose of transdermal nicotine than those smokers with higher baseline levels.

Administration, Cutaneous↗
PubMed1993

[The noninvasive quantitative evaluation of the acute hemodynamic effects of sublingual and transdermal nitroglycerin in man].

BACKGROUND: Organic nitrates are complex vasodilators: the hemodynamic action of these drugs is different in the venous and arterial resistance and capacitance beds. The aim of our study was to obtain a quantitative, noninvasive evaluation of the acute effects of sublingual and transdermal (td) nitroglycerin (NTG). METHODS: Twenty-one pts (mean age 49 years) underwent strain-gauge plethysmography and digital photoplethysmography under control conditions, 5 min after sublingual NTG (0.4 mg), 1 hour thereafter and 2 hours after NTG td (10 mg patch). Forearm venous capacitance (CV, ml.100 ml-1) and arteriolar resistance (RA, mmHg.ml-1.100 ml.min) and the b/a ratio of arterial pulse wave (%) were measured. RESULTS: After sublingual NTG, CV increased (+24%, p < 0.01) and b/a was reduced (-35%, p < 0.01), while heart rate and RA increased (+9% and +36% respectively, both p < 0.01). Two hours after NTG td, CV increase was not statistically significant (+11%, p = 0.056), b/a was reduced (-31%, p < 0.01), heart rate and RA did not change. CONCLUSIONS: The combined use of plethysmography and digital photoplethysmography is suitable for the evaluation of vasoactive drugs such as nitrates, which have a complex profile of action on arterial and venous beds. By this method we have shown that NTG td 10 mg dilates venous beds to a low extent; this approach will be utilized in future studies aimed at elucidating dose-response and regimen effect of these drugs.

Administration, Cutaneous↗
PubMed1993

Effect of transdermally administered scopolamine on the vestibular system in humans.

In order to elucidate the effect of scopolamine on the vestibular system in humans, various experimentally-induced forms of nystagmus, i.e. caloric nystagmus, rotational nystagmus, optokinetic nystagmus, visual-vestibular interaction and optokinetic after nystagmus, were evaluated before and after the administration of two pieces of Scopoderm-TTS or placebo patches retro-auricularly. Scopolamine reduced the responses of both the caloric and optokinetic after nystagmus compared with the placebo. The possible action site of this drug is discussed.

Administration, Cutaneous↗
PubMed2005

Transdermal delivery of naltrexone and its active metabolite 6-beta-naltrexol in human skin in vitro and guinea pigs in vivo.

The aim of the present study was to evaluate the transdermal delivery of 6-beta-naltrexol (NTXOL), the active metabolite of naltrexone (NTX), across human skin and guinea pig skin in vitro and in hairless guinea pigs in vivo. NTXOL may be responsible for much of NTX's pharmacologic activity. In vitro diffusion studies on NTXOL were compared with similar studies on NTX using a formulation of propylene glycol and buffer in a flow-through diffusion cell system. In vivo guinea pig studies were carried out involving topical application of both drugs in patches containing identical formulations. The in vitro flux of NTX was about 2.3- and 5.6-fold higher than for NTXOL across guinea pig skin and human skin, respectively. NTXOL lag times were longer than NTX in both skin types. In vivo studies in guinea pigs showed that the steady-state plasma level of NTX was twofold greater than NTXOL, which correlated well with in vitro data. The results of the present study indicated that substantial levels of NTX and NTXOL could be delivered via the transdermal route, although the plasma levels of NTXOL were significantly less than NTX. Further transdermal formulation development will be investigated for permeation enhancement.

Administration, Cutaneous↗
PubMed2004

New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo.

Microemulsion systems possessing a potentially improved skin bioavailability of lidocaine were designed and explored for some characteristics. The existence of microemulsion regions was investigated in quaternary systems composed of glyceryl oleate+polyoxyl 40 fatty acid derivatives (surfactants)/tetraglycol (co-surfactant)/isopropyl palmitate/water by constructing pseudo-ternary phase diagrams at fixed co-surfactant/surfactants (CoS/S) ratios. Light scattering measurements used to determine the diameter of the internal phase revealed that lidocaine in the microemulsions increased the droplet size, implying a drug tendency to accumulate in the interfacial layers. Percutaneous penetration studies using rat skin in vitro showed that the transdermal flux of lidocaine was significantly improved by microemulsion composed of the glyceryl oleate-PEG-40 stearate combination rather than glyceryl oleate-PEG-40 hydroxylated castor oil. Two principal factors were found to govern the transdermal penetration of lidocaine from the microemulsion: water content and the CoS/S ratio. By analyzing skin layers (epidermis and dermis) for lidocaine content, significantly higher concentrations were found after rats were treated in vivo with liquid microemulsions (CoS/S=1.8, 30 wt.% water) or patches compared to those measured after application of EMLA cream. It has been suggested, therefore, that these microemulsions loaded with lidocaine would provide adequate analgesia in relatively shorter periods of time.

Administration, Cutaneous↗
PubMedDate not supplied

A comparative multicenter study of two transdermal estradiol replacement therapies in the treatment of postmenopausal symptoms.

OBJECTIVE: Comparison of the effects of treatment of two transdermal therapeutic systems for estrogen replacement therapy with regard to efficacy, tolerability, and acceptance. DESIGN: Open randomized. SETTING: Multicenter. PATIENTS AND INTERVENTIONS: A study population of 104 postmenopausal women was randomized on a 1:1 basis to treatment with one of two estradiol patches, System (Cilag) and Estraderm (Ciba-Geigy). OUTCOME MEASURES: Systolic and diastolic BP, hot flushes, night sweating, fatigue, insomnia, depression, nervousness, headache, vaginal discomfort (efficacy variables); bleeding, dermatological symptoms, comfort and adhesiveness of patch, and other possible causes of discontinuation (tolerability); general evaluation by patient (acceptance). RESULTS: Considering all efficacy variables, 53% of Systen and 46% of Estraderm patients found the therapy satisfactory. Tolerability was somewhat higher in the Systen group. Adhesiveness of the patch was significantly better for Systen. Overall, 79% of Systen patients and 62% of Estraderm patients evaluated treatment as "good" or "very good." The majority of patients in both groups found the patch very comfortable or only slightly obtrusive.

Administration, Cutaneous↗
PubMed1998

Transdermal oestrogen reduces daytime blood pressure in hypertensive women [see comment].

The aim of this study was to investigate the acute effects of transdermally administered 17-beta-oestradiol on ambulatory blood pressure (BP) in hypertensive, postmenopausal women. Thirteen postmenopausal women with ongoing treatment for hypertension were included in this placebo-controlled, double-blind cross-over study. Ambulatory recordings of BP and heart rate were performed during 24 h on two occasions, separated by at least 1 week, after application of a patch containing either 100 microg per 24 h 17-beta-oestradiol or placebo. Serum oestradiol was increased (P<0.001) during active treatment (139.2 +/- 21.1 pg/ml) compared with the baseline postmenopausal levels recorded during placebo (40.5 +/- 2.2 pg/ml). No rise in BP was found in office BP or during ambulatory recordings. Daytime BP pressure was acutely reduced by approximately 3 mm Hg during the 24 h of treatment with oestrogen (SBP n.s., DBP P<0.05), without any change in heart rate. Nocturnal dipping in SBP and DBP was present during placebo conditions, and there were no signs of an increase in dipping during treatment with 17-beta-oestradiol. This study supports previous evidence that hormone replacement therapy is safe in hypertensive women. The data in the present study also imply an acute, but small reduction of daytime BP due to transdermal oestrogen in hypertensive, postmenopausal women. Furthermore oestrogen did not blunt or increase the dipping phenomena during the night in these women.

Administration, Cutaneous↗
PubMed2003

In vitro evaluation of patch formulations for topical delivery of gentisic acid in rats.

Gentisic acid (GA) is used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity. In order to achieve effective topical delivery of GA to the active site in the skin, a matrix-type transdermal delivery system was developed. The in vitro skin permeation as well as skin deposition of GA was studied in rats. Among the five pressure-sensitive adhesives tested, DuroTak 87-2510 was the most effective to achieve the highest permeation rate of GA. Dodecylamine showed the most potent enhancement among the enhancers tested, and significantly increased the permeation rate of GA up to 112.99 (+/-30.12) microg/cm(2) per h at the concentration of 1%, when 6% GA was incorporated in DuroTak 87-2510. Moreover, a linear relationship was observed between the skin permeation rate of GA and the amount of the skin deposition after 12 h of permeation (r(2)=0.95). Thus, the in vitro skin permeation data may be useful to determine the amount of GA actually deposited in the skin.

Administration, Topical↗
PubMed2002

Acute effects of transdermal 17beta-estradiol on hemostatic variables after 24-hour treatment.

The aim of this study was to investigate the acute effects of transdermal 17beta-estradiol (Estraderm) on plasma levels of coagulatory and fibrinolytic factors in postmenopausal normotensive and hypertensive women. Eleven normotensive and 13 hypertensive women were included in this placebo-controlled crossover study. In a randomized order each subject was treated with a patch of 100 microg 17beta-estradiol or placebo for 24 hours. Serum levels of tissue type plasminogen activator (tPA) activity, plasminogen activator inhibitor-I (PAI-1) activity, tPA antigen, PAI-I antigen, FVII, FX, and fibrinogen were assayed after both treatments. There was no significant difference in serum levels of hemostatic variables after treatment with estrogen compared to levels after placebo treatment in either of the groups. Nor was there any measurable difference when comparing hypertensive and normotensive subjects.

Administration, Cutaneous↗
PubMed2004

Studies on the transdermal delivery of nimodipine from a menthol-based TTS in human volunteers.

The purpose of the present study was to design a membrane-moderated transdermal therapeutic system (TTS) of nimodipine using 2%w/w hydroxypropyl methylcellulose (HPMC) gel as a reservoir system containing menthol as penetration enhancer and 60%v/v ethanol-water as solvent system. The flux of nimodipine was markedly increased from 35.51 microg/cm2/h to 167.53+/-3.69 microg/cm2/h with the addition of 8%w/w menthol to HPMC drug reservoir. There was an increase in the flux of nimodipine through ethylene vinyl acetate (EVA) copolymer membrane with an increase in vinyl acetate content (9 to 28%w/w) of the copolymer. The permeability flux of nimodipine from the chosen EVA 2825 (with 28%w/w vinyl acetate content) was 152.05+/-2.68 microg/cm2/h, and this flux decreased to 132.69+/-1.45 microg/cm2/h on application of a water-based acrylic adhesive (TACKWHITE A 4MED) coat. However, the transdermal flux of nimodipine across EVA 2825 membrane coated with TACKWHITE A 4MED/ rat skin composite was found to be 116.05+/-2.39 microg/cm2/h, which is about 1.4 times greater than the required flux. Thus a new transdermal therapeutic system for nimodipine was designed using EVA 2825 membrane coated with a pressure-sensitive adhesive TACKWHITE 4A MED, and 2%w/w HPMC gel as reservoir containing 8%w/w of menthol as a penetration enhancer. The in vivo evaluation of nimodipine TTS patch was carried out to find the ability of the fabricated menthol-based TTS patch in providing the predetermined plasma concentration of the drug in human volunteers. The results showed that the menthol-based TTS patch of nimodipine provided steady plasma concentration of the drug with minimal fluctuations with improved bioavailability in comparison with the immediate release tablet dosage form.

Administration, Cutaneous↗