• Biomolecules & Therapeutics
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• v.9 no.4
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• pp.298-306
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

• Bulletin of the Korean Chemical Society
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• v.28 no.4
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• pp.561-566
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• 2007

Adenosine kinase (AK) is a ubiquitous intracellular enzyme, which catalyzes the phosphorylation of adenosine (ADO) to adenosine monophosphate (AMP). AK inhibitors have therapeutic potential as analgesic and antiinflammatory agents. A chemical feature based pharmacophore model has been generated from known AK inhibitors (26 training set compounds) by HypoGen module implemented in CATALYST software. The top ranked hypothesis (Hypo1) contained four features of two hydrogen-bond acceptors (HBA) and two hydrophobic aromatics (Z). Hypo1 was validated by 124 test set molecules with a correlation coefficient of 0.905 between experimental and estimated activity. It was also validated by CatScramble method. Thus, the Hypo1 was exploited for searching new lead compounds over 238,819 chemical compounds in NCI database and then the selected compounds were screened based on restriction estimated activity and Lipinski's rules to evaluate their drug-like properties. Finally we could obtain 72 new lead candidates and the two best compound structures from them were posted.

• Journal of the Korean Society of Manufacturing Process Engineers
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• v.18 no.7
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• pp.71-76
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• 2019

The diffusion of the drug component of the inflammatory patch into the living tissue was analyzed by laser induced plasma spectroscopy (LIBS). Calcium element, which is a diffusion catalyst of the drug in the inflammatory analgesic patch, is transferred into the body through the diffusion process of the substance. The test pieces used in the experiment are pig skin tissues which are similar to human skin. As a result, the diffusion coefficient D of the calcium element was found to be average $8.24{\times}10^{-2}({\mu}m^2/s)$. Experimental results showed that the most influential factors on the diffusion of materials were temperature variables.

• Restorative Dentistry and Endodontics
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• v.17 no.1
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• pp.10-21
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• 1992

The purpose of this study was to investigate the analgesic effect of eugenol, capsaicin and demethoxy-NE. Young adult cats, weighing 2.0 to 3.0kg, were used. Each animal was anesthetized (${\alpha}$-chloralose 60mg per kg body weight) and divided into four groups; control, eugenol, capsaicin and demethoxy-NE group. The anterior digastric muscles were exposed and a pair of electrodes was inserted to record the electromyograms. To expose the pulp, each canine teeth was prepared with a low speed bur under cooling and used for recording anterior digastric muscular EMGs evoked by noxious stimulation of dental pulp. To observe effects on jaw opening reflex, inferior alveolar nerve of both sides were exposed for drug application and wire electrodes were inserted in anterior digstric muscle for recording the EMGs. To observe effects on action potential, saphenous nerves of both sides were exposed and three tissue pools were made from surrounding tissue. The most distal pool was used for applying stimulation, the most proximal one for recording of action potential, and the other one for drug application. One side of inferior alveolar nerve and saphenous nerve were used for eugenol, capsaicin, or demethoxy-NE application, the other side of nerve for control experiments(only vehicle application). Anterior digastric muscular EMGs evoked by noxious stimulation of dental pulp were recorded before drug application, immediate after drug application, at 60 and 120 minutes, and 5 days after drug application. Action potentials were recorded before drug application, immediate after 30 minutes drug application, at 30, 60 and 120 minutes after drug had been washed out. The results were as follows; 1. Eugenol had a continuous blocking effect on the anterior digastric muscular EMGs evoked by noxious pulp stimulation and after 5 days, showed completely blocking effect. 2. After 5 days, demethoxy-NE applied to dental pulp had a considerable blocking effect on the jaw opening retlex evoked by noxious stimulation but capsaicin had no significant effect. 3. After 5 days, eugenol group showed the strongest blocking effect among the all experimental groups on the jaw opening reflex evoked by noxious stimulation of dental pulp and capsaicin group showed the weakest blocking effect. 4. Eugenol had a completely blocking effect on the action potential conductivity of peripheral nerve. Capsaicin and demethoxy-NE had the blocking effect on the action potential conductivity of ${\alpha}$-and C-nerve fibers. 5. Capsaicin, demethoxy-NE and eugenol applied to inferior alveolar nerve surppressed the jaw opening reflex evoked by noxious stimulation of dental pulp.

• KSBB Journal
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• v.25 no.3
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• pp.297-302
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• 2010

Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drug with analgesic and antipyretic effects. The most common side effects from ketoprofen after oral administration are gastrointestinal irritation, diarrhea, abdominal pain and retention of fluid. Ketoprofen was formulated as water-soluble gels to reduce these side effects. To increase the skin permeability of ketoprofen, microsphere containing ketoprofen was prepared with chitosan and ploy-$\varepsilon$-caprolactone. And then prepared microsphere was manufactured as an adhesive hydrogel with polyvinylpyrrolidone K-25, polyethylene glycol 4000, and various permeation enhancers. The flux and permeability of ketoprofen were evaluated. As the concentration of tween 80 and enhancers increased, the flux of ketroprofen was accelerated. Also the permeation rate was facilitated by enhancers, but did not affect the lag time. From these results, the adhesive hydrogel using microsphere could be a good delivery system for ketoprofen to improve the skin permeation.

• Korean Journal of Pharmacognosy
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• v.40 no.4
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• pp.286-288
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• 2009

'SogDan(續斷)' is one of the crude drugs used mainly as a tonic and analgesic. The botanical origin of the crude drug has never been studied pharmacognostically. To clarify the botanical origin of SogDan from Korea, the anatomical characteristics of Phlomis umbrosa Turcz. and Phlomis koraiensis Nakai were studied. As a result, it was clarified that SogDan from Korea was the root of Phlomis umbrosa.

• The Korean Journal of Pharmacology
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• v.15 no.1_2 s.25
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• pp.39-43
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• 1979

Piroxicam is known to be a new nonsteroidal anti-inflammatory drug which has anti-inflammatory, antiedema, antigranuloma and analgesic activities through the mechanism of inhibition of prostaglandin synthetase. Clinical survey for piroxicam was carried cut on 40 cases of rheumatoid arthritis and 30 cases of degenerative arthritis who visited University Hospital from Feb. to June, 1979. Following results could be obtained: 1) In rheumatoid and degenerative arthritis, the effect of piroxicam was significant in decrease of joint pain, shortening of duration of morning stiffness, decrease in number of swollen joints, improvement of joint stiffness, decrease of E.S.R., increase of mean grip strength and decrease of articular index. 2) Side effects, almost all in G-I troubles were encountered in 6 cases in 40 cases of rheumatoid arthritis and 4 cases in 30 cases of degenerative arthritis.

• Korean Journal of Pharmacognosy
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• v.15 no.4
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• pp.188-193
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• 1984

It was previously indicated that 'Samulanshintang' had been examined for effects of the anticonvulsive, antipyretic, analgesic, sedative and antispasmodic actions. In order to investigate the effect on the cardiovascular system and anemic rabbits induced by phenlhydrazine HCl, pharmacological studies have been carried out with extract. The results of this investigation were summarized as follows: The relaxation of bronchial smooth muscle and antihistamine action were recognized. Antihypertensive and vasodilating actions due to vascular smooth muscle relaxation were noted in frogs and rabbits. 'Samulanshintang' lowered the rate of anemia induced by phenylhydrazine and rapidly recovered from the anemia state.

• Journal of Dental Anesthesia and Pain Medicine
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• v.16 no.1
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• pp.55-59
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• 2016

Dental treatment under sedation requires various sedation depths depending on the invasiveness of the procedure and patient drug sensitivity. Inappropriate sedation depth may cause patient discomfort or endangerment. For these reasons, patient-controlled sedation (PCS) pumps are commonly used. Patients are able to control the sedation depths themselves by pushing the demand button after the practitioner sets up the bolus dose and lock-out time. Dexmedetomidine is an ${\alpha}$-2 adrenoreceptor agonist with sedative, analgesic, and anxiolytic properties. It has been widely used for sedation for its minimal respiratory depression; however, there are few studies on PCS using dexmedetomidine. This study assessed the applicability of dexmedetomidine to PCS.

• Journal of Pharmaceutical Investigation
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• v.16 no.3
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• pp.124-131
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• 1986

Pharmacological activities of Paeoniae Radix alba were studied with water extract (F-I), parched preparation (F-II) and 25% ethanol-treated preparation (F-III) of it. The results were summerized as follows; 1) Analgesic actions were recognized with F-I, F-II and F-III. 2) Sedative actions were recognized with F-I and F-III. 3) Prolonged effect of sleeping time were recognized significantly with F-I and F-III. 4) Antipyretic actions were recognized with F-1, F-II and F-III in rabbits. 5) F-I, F-II and F-III showed the antagonic action against contraction of isolated-ileum induced by acetylcholine, barium chloride and histamine in mice and guinea-pigs.