• Journal of Pharmaceutical Investigation
• /
• v.29 no.4
• /
• pp.343-348
• /
• 1999

The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

• The Journal of Korean Orthopaedic Ultrasound Society
• /
• v.7 no.1
• /
• pp.7-12
• /
• 2014

Purpose:The effectiveness of transdermal buprenorphine patch on the patients with frozen state of frozen shoulder was evaluated. Materials and Methods: Between March and September in 2013, 127 patients with pain and limited range of motion in shoulder joint over 6 months were included. Every patient was confirmed the diagnosis through MRI or ultrasonogram and each patient received intra-articular injection of steroid once. After 2~4 weeks, every patient was interviewed via telephone survey and finally 105 patients were included, 54 patients received only oral NSAIDs (NP group) while 51 patients received additional transdermal buprenorphine patch (BP group). Pain and functional visual analog scale (PVAS, FVAS), American Shoulder Elbow Society (ASES) score was checked. Results: Generally, every outcome variables showed improvements in both groups (p<0.001). PVAS score after treatment showed superior result in NP group but it was not significant (p=0.088). In ASES score, NP group had superior result than BP group and it had significant difference. Similarly in FVAS, NP group showed superior result but the data before treatment was significantly different (p=0.028) Conclusion: Transdermal buprenorphine patch didn't show superior treatment result in the patient with frozen state of frozen shoulder which was applied with oral NSAIDs after single intra-articular glenohumeral steroid injection in short-term follow-up.

• Clinical and Experimental Reproductive Medicine
• /
• v.43 no.4
• /
• pp.228-232
• /
• 2016

Objective: The aim of this study was to investigate the impact of pretreatment with transdermal estradiol ($E_2$) compared to oral contraceptive pills (OCPs) on controlled ovarian stimulation (COS) response in normal responders undergoing fresh in vitro fertilization (IVF)-embryo transfer (ET) cycles. Methods: A retrospective cohort study was performed of normal responders undergoing fresh IVF-ET cycles who received pretreatment with transdermal $E_2$ versus OCPs prior to fresh IVF-ET. The total days of ovarian stimulation, total dosage of gonadotropins, total number of oocytes, and mature oocytes retrieved were noted. Pregnancy outcomes after ET were also recorded. Results: A total of 2,092 patients met the inclusion criteria: 1,057 and 1,035 patients in the transdermal $E_2$ and OCP groups, respectively. Patients in the OCP group had a longer duration of COS ($10.7{\pm}1.63days$, p< 0.01) than the $E_2$ group ($9.92{\pm}1.94days$). Patients in the OCP group also required higher cumulative doses of gonadotropins ($2,657.3{\pm}1,187.9IU$) than those in the $E_2$ group ($2,550.1{\pm}1,270.2IU$, p= 0.002). No statistically significant differences were found in the total and mature oocytes retrieved or in the rates of biochemical pregnancy, clinical pregnancy, spontaneous miscarriage, and live birth between the groups. Conclusion: Our findings suggest that compared to OCPs, pretreatment with transdermal $E_2$ is associated with a shorter duration of ovarian stimulation and lower gonadotropin utilization, without compromising the oocyte yield or pregnancy outcomes in normal-responder patients undergoing fresh IVF.

• Journal of Pharmaceutical Investigation
• /
• v.29 no.2
• /
• pp.111-115
• /
• 1999

We have studied the transdermal flux of prostaglandin $E_1$ $(PGE_1)$ from a hydrogel patch through hairless mouse skin, to test the possibility of developing a transdermal delivery system. Karaya gum patch containing $PGE_1$ was prepared by casting method. $PGE_1$ was stable in the patch for 10 weeks. The effect of current application, enhancer (propylene glycol monolaurate : PGML), adhesive and patch thickness on the flux was studied using side-by-side diffusion cell. Passive flux of $PGE_1$ was negligible. Cathodal delivery increased the flux about 20 fold. As the concentrations of PGML increased, flux increased. When 5% PGML was used as the enhancer, maximum flux by cathodal iontophoresis was $55\;{\mu}g/cm^2\;hr$. It increased about 2 folds to $100\;{\mu}g/cm^2\;hr$, when the amount of PGML used was 9%. Large increase in flux and the decrease in time to reach maximum flux were observed when the skin was pretreated with neat PGML (maximum flux obtained was about $200\;{\mu}g/cm^2\;hr$). Use of adhesive decreased the flux significantly. To the contrary of our expectation, increase in current density decreased the flux. These flux data together with the stability data indicate that, though the onset of sufficient delivery occur after 1-2 hours of application, therapeutic amount of $PGE_1$ can be delivered through skin using iontophoresis and penetration enhancer.

• Journal of Pharmaceutical Investigation
• /
• v.40 no.1
• /
• pp.33-38
• /
• 2010

Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. $Crovol^{(R)}$ PK40 and $Crovol^{(R)}$ A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% $Crovol^{(R)}$ A40 as permeation enhancer, in $80\;{\mu}m$ thick Duro-$Tak^{(R)}$ 87-9301 matrix.

• The Korean Journal of Pain
• /
• v.12 no.2
• /
• pp.211-216
• /
• 1999

Background: Transdermal fentanyl patch (TDFP) is a simple, noninvasive analgesic with continuous effect. The aim of this study was to evaluate the postoperative analgesic effect of TDFP. Methods: Sixty healthy patients undergoing cesarean section were divided into 3 groups. Postoperative pain was controlled with different methods; Group I: application of TDFP-$25{\mu}g/hr$, Group II: intramuscular injection of ketoprofen; Group III: continuous epidural block. Pain scores (numerical rating scale, NRS), number of patients who needed additive ketoprofen injections and side effects were recorded at 8, 20, 32, 44 hours postoperatively. Results: There was no significanant difference in pain score between Group I and Group II. The numbers of patients who need additive ketoprofen injections were lower in group I than group II. Pruritis (25%), nausea/vomiting (10%), leg numbness (40%) was experienced in group III, but not in Group I & II. Conclusions: TDFP-$25{\mu}g/hr$ for postoperative pain control is simpler and more convinient than intramuscular injection of analgesics.

• Journal of the Korean Applied Science and Technology
• /
• v.29 no.4
• /
• pp.552-560
• /
• 2012

Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

• Journal of Pharmaceutical Investigation
• /
• v.41 no.1
• /
• pp.1-7
• /
• 2011

The effects of different formulation variables including pressure sensitive adhesive (PSA), permeation enhancer, thickness of the matrix and loading amount of drug on the transdermal absorption of galantamine were investigated across the hairless mouse skin. The permeation profile of galantamine was different depending on the types of PSA, loading amount of drug, thickness of the matrix and type of enhancer used. Highest flux of galantamine was obtained from acrylic PSA but crystals were formed in the patch within 72 h. Among the PSAs screened, crystal formation was not observed only in the patches formulated in Styrene Butadiene Styrene (SBS) matrix. Permeation rate increased linearly as the concentration of galantamine in SBS matrix increased from 2.5 to 15% w/w. Among the enhancers screened, Brij$^{(R)}$ 30 provided highest flux of galantamine. Matrix thickness of 80 ${\mu}m$ was optimum for maintaining adhesiveness as well as consistently delivering galantamine for longer period of time.

• The Korean Journal of Pain
• /
• v.24 no.2
• /
• pp.74-80
• /
• 2011

Background: Lidocaine patch (L5P) has demonstrated short-term efficacy in treating both acute surgical pain and chronic neuropathic pain with tolerable side effects. Percutaneous endoscopic lumbar discectomy (PELD) is the mainstay of minimally invasive spine surgery (MISS). Sufficient analgesia during PELD surgery makes the patient consider it real MISS. This study was performed to evaluate the efficacy and adverse effects of lidocaine patch in patients who underwent PELD under local anesthesia. Methods: L5P (L group) or placebo (P group) was randomly applied on the skin of the back covering the anticipated path of the working channel before 1 hour of surgery in 100 patients who underwent a single level PELD at L4-L5. Efficacy of the lidocaine patch was assessed by patient's numeric rating scale (NRS) of pain at each stage during the surgery and by a 5-scale grading of the satisfaction with the anesthesia of the operator and patients after surgery. Results: Mean NRS scores at the stages of needle insertion, skin incision, serial dilation and insertion of working channel, and subcutaneous suture were significantly lower in the L group than the P group. Postoperative operator's and patients' satisfaction scores were also significantly higher in L group than in the P group. There were subtle adverse effects in both groups. Conclusions: L5P provided better pain relief during PELD, especially at the stage of needle insertion, skin incision, serial dilation and insertion of working channel, and subcutaneous suture. It also provided higher patient and operator postoperative satisfaction, with only subtle adverse effects.

• Journal of the Korean Applied Science and Technology
• /
• v.27 no.4
• /
• pp.407-414
• /
• 2010

New biological treatments were being developed at a record place, but their potential could be compromised by a significant obstacle: the delivery of these drugs into a body. Pharmaceutical delivery is now nearly as important as product. New systems are being developed, and Drug Delivery Markets Series cover these new systems. Transdermal Delivery System(TDS) is often used as a method of drug dosage into the epidermic skin. An approach used to delivery drugs through the skin for therapeutic use as an alternative to oral, intravascular, subcutaneous and transmucosal routes. Various transdermal drug delivery technologies are described including the use of suitable formulations, carriers and penetration enhancers. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other methods of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharides, such as karaya gum and glucomannan, were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, drug contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in fibric acid(ciprofibrate) such as lipophilic drug in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate. Especially, this result suggests a possible use of polysaccharide gel ointment matrix as a transdermal delivery system of anti-hyperlipoproteinemic agent.