Topical Patch Research Articles

국산 소나무껍질추출물(파인엑솔®)을 함유한 제제의 피부흡수 평가

Pine bark extract is well-known as a very powerful antioxidant, anti-inflammatory, and antibiotic material. French maritime pine bark extract () of Horphag Research has monopolized the world market over 30 years. Korean red pine bark extract () was first manufactured by the patent technology of NutraPharm in Korea in 2006. Feasibility of topical gel and patch formulations of Pinexol was systematically investigated by evaluating the skin absorption of catechin as a reference compound. In vitro hairless mouse skin absorption of catechin from gel formulation was higher than that from patches. However, significant amount of catechin was also deposited inside the skin from patch formulations, which were dependent on the types of pressure sensitive adhesives. Thus, it seems to be feasible to control the topical delivery of Pinexol by using both gel and patch formulations, and be necessary to conduct further systematic investigation.

Topical patch for use on intact skin

Topical patch for use on intact skin

Efficacy of Estradiol Topical Patch in the Treatment of Symptoms of Depression following Mini-Gastric Bypass in Women

Obesity is associated with elevated levels of estrogen. Gastric bypass causes rapid weight loss and decreased levels of estrogen. Patients after gastric bypass can suffer from anxiety and depression out of proportion to the surgical outcome. This study reports the efficacy of a short-term empiric trial of topical estradiol for the treatment of mild to moderate depression and anxiety following mini-gastric bypass (MGB) in women. Postoperative MGB women were surveyed for the presence of depressive symptoms before and after MGB. The results of an empiric trial of transdermal patches of estradiol-17beta were assessed. Outcome measures were the self-reported efficacy of the patch. 711 women who had undergone MGB and had functioning e-mail addresses made up the study. 62% of patients reported depression prior to surgery. 156 patients (22%) reported depression after the operation. 130 women were treated empirically with the patch, and remission of depression was observed in 92 (71%). In response to the question "Did the estrogen patch help?", subjects reported responses of 1) Yes, fantastic, 2) Yes, somewhat, 3) Hard to say, 4) No, in 36%, 31%, 20%, 13% of respondents respectively. Patients treated with estradiol sustained antidepressant benefit of treatment after the patch was discontinued. Treatment lasted <1 month, 1-3 months, and >3 months, in 48%, 32% and 20% respectively. Treatment was well-tolerated and adverse events were rare. Depression is common in obese patients and remains a problem in a subset following the MGB operation. Transdermal estradiol replacement appears to be an effective treatment of symptoms of depression in women following MGB.

Polypharmacy as a Risk Factor in the Treatment of Type 2 Diabetes

The desire to take medicine is perhaps the greatest feature which distinguishes man from animals. — Sir William Osler (1849–1919)1 Polypharmacy is a term that has been used in health care for decades. In conventional use, it has meant the concurrent use of multiple medications in the same patient. However, this definition understates the potential for harm that polypharmacy may pose to the patient. Other definitions have appeared in the medical literature that put the problem of polypharmacy in a broader perspective. One defines polypharmacy as the “prescription, administration, or use of more medications than are clinically indicated, or when a medical regimen includes at least one unnecessary medication.”2–5 However, polypharmacy may be unavoidable, given that multiple drug therapy has become the standard of care in most chronic conditions.6 The comorbidities of diabetes commonly include hypertension, dyslipidemia, depression, and coagulopathies, each of which may require one or more drugs for adequate control. Add to this other conditions that often accompany diabetes, such as hypothyroidism, heart failure, and osteoporosis, and the total number of possible medications needed becomes significant. Polypharmacy is inevitable when treating a common chronic condition such as diabetes, given the large number of treatment options now available. The potential for polypharmacy will continue to increase with time, as additional therapeutic options become available. Before the approval of metformin in the United States in 1995, only insulin and the sulfonylureas were available for the treatment of diabetes. Now, there are five classes of oral agents, three rapid-acting insulin analogs, and two long-acting analogs, as well as the “traditional” insulins. The emergence of other forms of insulin (inhaled, topical patches), the incretin gut hormones, newer mixed peroxisome proliferator–activated receptor-α and -γ agonists, a synthetic amylin analog, and still more agents to come will increase opportunities …

Topical Ketoprofen Patch

Although oral nonsteroidal anti-inflammatory drugs (NSAIDs) are effective in the treatment of a variety of acute and chronic pain conditions, their use may be associated with serious systemic adverse effects, particularly gastrointestinal disorders. In order to minimise the incidence of systemic events related to such agents, topical NSAIDs have been developed. Topical NSAIDs, applied as gels, creams or sprays, penetrate the skin, subcutaneous fatty tissue and muscle in amounts that are sufficient to exert a therapeutic effect on peripheral and central mechanisms in the absence of high plasma concentrations. Data indicate that topical NSAIDs are effective at relieving pain in a number of acute and chronic pain indications. This review article discusses the pharmacokinetics, efficacy and tolerability of a new formulation of ketoprofen available as a topical patch. The topical patch containing ketoprofen 100mg as the active principle has been developed using a novel delivery system that dispenses therapeutic doses of the drug directly to the site of injury. Pharmacokinetic data indicate that although plasma levels of ketoprofen are higher when the drug is administered as a patch versus a gel, the total systemic bioavailability of ketoprofen 100 mg administered via a patch is no more than 10% of that reported for ketoprofen 100 mg administered orally. Because the patch facilitates ketoprofen delivery over a 24-hour period, the drug remains continually present in the tissue subjacent to the site of application. High tissue but low plasma ketoprofen concentrations mean that while tissue concentrations are high enough to exert a therapeutic effect, plasma concentrations remain low enough to not result in systemic adverse events caused by elevated serum NSAID levels. Phase III clinical trials in patients with non-articular rheumatism and traumatic painful soft tissue injuries showed that the topical ketoprofen patch was significantly more effective than placebo at reducing pain during daily activities and spontaneous pain after 7 days' treatment. Moreover, the topical ketoprofen patch was well tolerated; adverse events were primarily cutaneous in nature and occurred in a similar number of ketoprofen and placebo recipients suggesting that these events were related to the patch itself rather than the active ingredient. The incidence of gastrointestinal adverse events was low (<8% of all patients), and occurred in a similar proportion of patients receiving ketoprofen and placebo. Thus, the topical ketoprofen patch appears to be a simple, effective and safe therapeutic option for the treatment of local painful inflammation.

Topical Lidocaine Patch Therapy for Myofascial Pain

An open label study of topical lidocaine 5% patches was conducted for myofascial pain management based on the hypothesis that electrical dysfunction is a component of myofascial pain and therefore sodium channel blockade may be useful in managing myofascial pain. The efficacy of topical lidocaine patch therapy for myofascial pain impact of the therapy on associated quality of life were investigated in the one-month trial. Principal outcome measures were Brief Pain Inventory-Short Form for pain intensity and quality of life score changes. Twenty-seven patients with moderate-severe myofascial pain were enrolled. Eighteen had low back pain. Two patients reported complete pain relief and 3 reported a lot of relief. Mean improvements for average pain intensity (7, 14, and 28 days), general activity (7 and 28 days), mood and sleep (7, 14, and 28 days), walking (14 and 28 days), ability to work, relationships, and enjoyment of life (28 days) were significant (P < 0.05). These results suggest lidocaine patches may be useful in the management of myofascial pain.

(212) Topical Lidocaine Patch Produces a Significant Improvement in Quality of Life Indicators in Treated PHN Patients: Results of a Multicenter Open-Label Trial

(212) Topical Lidocaine Patch Produces a Significant Improvement in Quality of Life Indicators in Treated PHN Patients: Results of a Multicenter Open-Label Trial

Topical Diclofenac Patch Relieves Minor Sports Injury Pain: Results of a Multicenter Controlled Clinical Trial

Sports-related soft tissue injuries, such as sprains, strains, and contusions, are a common painful condition. Current treatment includes oral nonsteroidal anti-inflammatory drugs (NSAIDs), which have a high incidence of intolerable gastrointestinal side effects. Topically applied drugs have the potential to act locally in the soft tissues without systemic effects. This study assessed the efficacy and safety of topical diclofenac (NSAID) patch applied directly to the painful injury site for the treatment of acute minor sports injury pain. Adult subjects ( N = 222) were recruited from two communities for a multicenter, randomized, placebo-controlled, parallel design study. All subjects had suffered a painful minor sports injury within the prior 72 hours of study entry. Either a diclofenac epolamine or placebo topical patch was applied directly to the skin overlying the painful injured site twice daily for 2 weeks. Measures of pain intensity were performed in a daily diary and at clinic visits on days 3, 7, and 14. Diclofenac patch was superior to placebo patch in relieving pain. Statistical significance was seen on clinic days 3 ( P = 0.036) and 14 ( P = 0.048), as well as the daily diary pain ratings at days 3, 7, and 14 ( P ≤ 0.044). No statistically significant differences were seen in any safety or side-effect measures with the diclofenac patch as compared to the placebo patch. Diclofenac epolamine patch is an effective and safe pain reliever for treatment of minor sports injury pain. The advantages of this novel therapy include its ease of use and lack of systemic side effects.

Topical lidocaine patch relieves postherpetic neuralgia more effectively than a vehicle topical patch: results of an enriched enrollment study

This study compared the efficacy of topical lidocaine patches versus vehicle (placebo) patches applied directly to the painful skin of subjects with postherpetic neuralgia (PHN) utilizing an `enriched enrollment' study design. All subjects had been successfully treated with topical lidocaine patches on a regular basis for at least 1 month prior to study enrollment. Subjects were enrolled in a randomized, two-treatment period, vehicle-controlled, cross-over study. The primary efficacy variable was `time to exit'; subjects were allowed to exit either treatment period if their pain relief score decreased by 2 or more categories on a 6-item Pain Relief Scale for any 2 consecutive days. The median time to exit with the lidocaine patch phase was greater than 14 days, whereas the vehicle patch exit time was 3.8 days ( P<0.001). At study completion, 25/32 (78.1%) of subjects preferred the lidocaine patch treatment phase as compared with 3/32 (9.4%) the placebo patch phase ( P<0.001). No statistical difference was noted between the active and placebo treatments with regards to side effects. Thus, topical lidocaine patch provides significantly more pain relief for PHN than does a vehicle patch. Topical lidocaine patch is a novel therapy for PHN that is effective, does not cause systemic side effects, and is simple to use.

Pharmacokinetic comparison of oral and local action transcutaneous flurbiprofen in healthy volunteers

Flurbiprofen is a propionic acid-derived non-steroidal anti-inflammatory drug (NSAID) used widely in the treatment of rheumatism and non-arthritic pain. The pharmacokinetics of topically and orally administered flurbiprofen were compared in a two-part, open study involving healthy adult volunteers. In the first (cross-over) part of the study, 12 Caucasians were randomized to receive either a single oral dose of 50 mg flurbiprofen or a single topical application of a novel 40 mg flurbiprofen-containing patch on the right wrist for 12 h. In the second part of the study, each subject applied a flurbiprofen-containing patch twice daily to the same wrist for 7 days. Plasma concentrations of flurbiprofen and urinary concentrations of the NSAID and its metabolites were measured by high-performance liquid chromatography assay, to enable comparison of the pharmacokinetic parameters for delivery of the drug by both routes. Maximum concentrations of the NSAID in plasma (Cmax) were much lower after a single application of the topical 40 mg flurbiprofen patch than after a single oral dose of 50 mg of the NSAID (mean +/- SD: 43 +/- 16 ng/ml versus 5999 +/- 1300 ng/ml, respectively). After repeated application of the topical patch, Cmax increased only slightly to 103 +/- 57 ng/ml. The mean relative bioavailability of flurbiprofen from the patch was 3.5 +/- 1.7%, calculated from plasma area under the curve data and 4.4 +/- 2.8% from urinary excretion data.(ABSTRACT TRUNCATED AT 250 WORDS)

Issues in contemporary drug delivery. Part VI: Advanced cardiac drug formulations.

To identify and discuss the clinical utility of new delivery systems and formulations of cardiac drugs. Studies describing or evaluating new drug delivery systems for cardiac drugs were identified through a MEDLINE literature search. All studies describing or evaluating new delivery systems for cardiac drugs were reviewed. Data were abstracted and evaluated by each author independently. The most common oral sustained-release formulations include the wax-matrix system, the gastrointestinal therapeutic system (GITS), and the spheroidal oral drug absorption system (SODAS). The wax-matrix delivery system is limited by the occurrence of "dose-dumping." In a low-pH setting, the wax-matrix formulation may dissolve too rapidly, liberating the entire dose in a short period of time. The clinical relevance of this phenomenon is unknown. The GITS and SODAS formulations are less likely to be affected by pH and food. Nitroglycerin is available by many routes of administration. The topical patch forms are convenient to use, but are associated with the development of tolerance. A buccal formulation incorporates a relatively short onset of effect with a three- or four-times-daily dosing regimen. Although tolerance is less of a problem with buccal nitroglycerin than with topical nitrates, this formulation is less convenient to use because of buccal irritation and interference with eating and talking. A new spray formulation of nitroglycerin offers longer shelf-life storage stability and an easier mode of administration. The spray canister is stable for three years compared with 12 weeks for an opened bottle of sublingual nitroglycerin tablets. Sublingual administration of oral cardiac drugs offers the potential for a more rapid onset of effects. Although nifedipine is often given sublingually, objective data indicate that it is not absorbed buccally but rather in the stomach. It appears that the chew-and-swallow route is most appropriate for nifedipine. Captopril is absorbed sublingually but its efficacy has not been demonstrated. Transdermal clonidine improves compliance and is associated with fewer adverse effects than oral clonidine. Transdermal formulations of beta-blockers are currently being evaluated. Further advancements in the development of novel delivery systems for cardiac drugs are expected in the future.