• Applied Chemistry for Engineering
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• v.17 no.2
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• pp.138-143
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• 2006

Ethosome is a liquid crystalline vesicle prepared by hydration of ethanol-dissolved lecithin with a solution containing hydrophilic components. Investigation of factors affecting the entrapment efficiency and particle size of ethosomes was carried out, because the high entrapment efficiency and small particle size are prerequisite in developing ethosomes as a drug delivery system. The variations of properties of ethosomes with constituent composition and preparation method were examined using a calcein as a hydrophilic marker. It was observed that the amount of ethanol and calcein solution, phosphatidyl choline content in lecithin, preparation temperature, stirring rate, and PBS addition method had a considerable effect on the properties of ethosome. Sonication treatment resulted in the reduction of entrapment efficiency of ethosome, which was due to the release of entrapped components in the vesicles by strong sonication vibration.

• Journal of Pharmaceutical Investigation
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• v.39 no.3
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• pp.221-226
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• 2009

The purpose of the present study was to evaluate the bioequivalence of two alprazolam tablets, Xanax 0.25 mg (Pharmacia Korea Pharm. Co., Ltd.) and Zyren 0.25 mg (Kwang Dong Pharm. Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The alprazolam release from two alprazolam tablets in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solutions and water). The dissolution profiles of two alprazolam tablets were very similar at all dissolution media. Twenty four healthy male volunteers were divided into two groups with a randomized 2${\times}$2 cross-over study. After four tablets (1 mg alprazolam) were orally administrated, blood was taken and the concentrations of alprazolam in serum were determined using LC/MS/MS. The pharmacokinetic parameters such as $AUC_t$, $C_max$ and $T_max$were determined. Our results showed that the differences in $AUC_t$, $C_max$ and $T_max$ between two alprazolam tablets based on the Xanax were -11.65%, -4.44% and -39.31%, respectively. There were no sequence effects between two tablets in these parameter. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25)(e.g., log(0.8386)${\sim}$log(0.9453) and log(0.8596)${\sim}$log(1.1040) for $AUC_t$, $C_max$, respectively). Thus, Zyren 0.25 mg tablet was bioequivalent to Xanax 0.25 mg tablet.

• Biomaterials and Biomechanics in Bioengineering
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• v.1 no.1
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• pp.27-39
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• 2014

We have previously described a new multilayer alginate microcapsule system, and the goals of the present study were to assess the in vitro function of islets encapsulated in its inner layer, and the angiogenic ability of FGF-1 delivered from the external layer in an omentum pouch. Following isolation and culture, islets were encapsulated in the inner core of microspheres ($500-600{\mu}m$ in diameter) with a semi-permeable poly-L-ornithine (PLO) membrane separating two alginate layers, and both unencapsulated and encapsulated islet function was assessed by a dynamic glucose perifusion. For angiogenesis experiments, one group of microcapsules without FGF-1 (control) and another (test) containing FGF-1 with heparin encapsulated in the external layer were made. One hundred microcapsules of each group were transplanted in Lewis rats (n = 5/group) and were retrieved after 14 days for assessment of angiogenesis. Glucose perifusion of unencapsulated and encapsulated islets resulted in similar stimulation indices. The release of FGF-1 resulted in increased vascular density compared to controls. In conclusion, islets encapsulated in the core of multilayer alginate microcapsules maintain functionality and the microcapsule's external layer is effective in delivery of FGF-1 to enhance graft neovascularization in a retrievable omentum pouch.

• Journal of the Korean Society of Laryngology, Phoniatrics and Logopedics
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• v.23 no.2
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• pp.111-118
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• 2012

Botulinum toxin is a potent neurotoxin that is produced by the bacterium Clostridium botulinum. The agent causes muscle paralysis by preventing the release of acetylcholine at the neuromuscular junction of striated muscle. Botulinum toxin A (Botox, AllerganInc., Irvine, California) is the most potent of seven distinct toxin subtypes that are produced by the bacterium. The toxin was initially used clinically in the treatment of strabismus caused by hypertonicity of the extraocular muscles and was sub-sequently described in the treatment of multiple disorders of muscular spasticity and dystonia. In treating patients with Botox for blepharospasm, Carruthers and Carruthers [5] noticed an improvement in glabellar rhytids. This ultimately led to the introduction and development of Botox as a mainstay in the treatment of hyperfunctional facial lines in the upper face. Since its approval by the U.S. Food and Drug Administration for the treatment of facial rhytids (2002), botulinum toxin A has expanded into wide-spread clinical use. Forehead, glabellar, and periocular rhytids are the most frequently treated facial regions. Indications for alternative uses for Botox in facial plastic and reconstructive surgery are expanding. These include a variety of well-established procedures that use Botox as an adjunctive agent to enhance results. In addition, Botox injection is finding increased usefulness as an independent modality for facial rejuvenation and rehabilitation. The agent is used beyond its role in facial rhytids as an effective agent in the management of dynamic disorders of the face and neck. Botox injection allows the physician to precisely manipulate the balance between complex and conflicting muscular interactions, thus resetting their equilibrium state and exerting a clinical effect. This article will address some of the new and unique indications on Botox injection in the face (the lower face and neck, combination with fillers). Important points in terms of its clinical relevance will be stressed, such as an understanding of functional facial anatomy, the importance of precise injections, and correct dosing all are critical to obtaining natural outcomes.

• Journal of Embryo Transfer
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• v.26 no.1
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• pp.1-7
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• 2011

The purpose of this study was to determine the relationship between conception rate and other parameters (body condition score; BCS, progesterone concentrations and follicle size) before estrus induction with CIDR(intravaginal progesterone-releasing controlled internal drug release). The conception rate in cows with < 2.75, 2.75 to 3.25, and 3.25 <, BCS regardless of AI (artificial insemination) time was 46.6%, 63.3%, and 46.6% at CIDR insertion, respectively. The conception rate regardless of BCS was 54.9% in cows inseminated based on detected estrus, and 48.7% in cows inseminated at 72 to 80 hours (timed artificial insemination, TAI) after removal of CIDR. The conception rate regardless of AI time was 40.0% in cows with low progesterone concentrations (less than 1.0 ng/ml), and 56.6% in cows with high progesterone concentrations (more than 1.0 ng/ml) at CIDR injection. The conception rate regardless of progesterone concentrations was 53.8% in cows inseminated based on detected estrus, and 38.0% in cows of TAI after removal of CIDR. The conception rate regardless of AI time was 43.3% in cows with small follicle (less than 5 mm), 53.3% in cows between 5 mm to 10 mm of follicle, and 63.3% in cows with large folliclc (more than 10 mm) at CIDR injection, respectively. The conception rate regardless of follicle size was 58.4% in cows inseminated based on detected estrus, and 45.9% in cows of TAI after removal of CIDR. These results indicated that if the cows with BCS 2.75 to 3.25, active corpus luteum, and/or large dominant follicle (more than 10 mm) are used for estrus induction, the conception rate will be greater.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.202-210
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• 1997

Protective effect of DA-9601, an extract of Artemisia Herb, against ethanol-induced gastric mucosal injury was evaluated in rats. In the prophylactic study, DA-9601 exhibited total protection (99.4%) against absolute ethanol-induced gastropathy, And the protective effect of DA-9601 lasted up to 2 hours, which was longer than those of other contemporary mucoprotectants. In the treatment study, DA-9601 significantly facilitated the healing of 70% ethanol-induced mucosal damage, which was superior to cetraxate, a commonly used anti-ulcer drug. The mechanisms of mucoprotection of DA-9601 were also assessed. DA-9601 increased the release of prostaglandin E$_2$ from murine neutrophils in a dose-dependent manner in vitro. The cytoprotective effect of DA-9601 against ethanol-induced mucosal damage was significantly diminished by the concommitant injection of N$\omega$-nitro-L-arginine methyl ester (L-NAME, 5 mg/kg, i.v.), a non-specific nitric oxide (NO) synthase inhibitor, while it was not affected by preinjection of indomethacin (5 mg/kg, s.c.), a prostaglandins-depletor. And it was found that DA-9601 significantly enhanced adaptive cytoprotective action of 10% ethanol against absolute ethanol (56.9$\pm$6.5 vs 23.0$\pm$3.3 mm$^2$, p<0.05, mean$\pm$SEM), though its exact underlying mechanism remains to be clarified. The present fin[lings demonstrate that DA-9601 exerts gastroprotecticv actions for the stomach against ethanol through several different underlying mechanisms, in which prostanglandins and NO are involved. In conclusion, the results obtained suggest that DA-9601 can be useful both in prevention and treatment of ethanol-induced gastric damage.

• Journal of Pharmaceutical Investigation
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• v.41 no.4
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• pp.239-247
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• 2011

Simvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in the biosynthesis of cholesterol. Simvastatin has good permeability, but it also has low solubility (BCS class II), which reduces its bioavailability. To overcome this problem, a solid dispersion is formed using a spray-dryer with polymeric material carrier to potentially enhance the dissolution rate and extend drug absorption. As carriers for solid dispersion, Gelucire$^{(R)}$44/14 and Gelucire$^{(R)}$ 50/13 are semisolid excipients that greatly improve the bioavailability of poorly-soluble drugs. To avoid any toxic effects of an organic solvent, we used aqueous medium to melt Tween$^{(R)}$ 80 and distilled water. The structural behaviors of the raw materials and the solid dispersion were analyzed by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The DSC and PXRD data indicated that the crystalline structure of simvastatin was transformed to an amorphous structure through solid dispersion. Then, solid dispersion-based tablets containing 20 mg simvastatin were prepared with excipients. Dissolution tests were performed in distilled water and artificial intestinal fluid using the USP paddle II method. Compared with that of the commercial tablet (Zocor$^{(R)}$ 20 mg), the release of simvastatin from solid dispersion based-tablet was more efficient. Although the stability study is not complete, this solid dispersion system is expected to deliver poorly water-soluble drugs with enhanced bioavailability and less toxicity.

• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.35-47
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• 1992

Hydrogel coated ring shaped ocular inserts (containing the antibiotic, tylosin tartrate) were used in an evaluation of the effectiveness of polymeric ocular drug release devices for treating infectious bovine keratoconjunctivitis. The in vivo experiments represent the first experiments using hydrogel ocular inserts containing an antibiotic for treating infectious bovine keratoconjunctivitis. In the infection tests, ten calves. were challenged with $2.4{\times}10^8{\sim}1.6{\times}10^9$ Moraxella bovis (a bacterium) colonies per eye following two ten minute ultraviolet radiation eye preconditioning exposures. Ninety five percent of the eyes (19 of 20 eyes) were successfully infected by this method. All infected eyes were monitored for the presence of the bacteria quantitiatively, and clinical observations were made for 14 days. The test was performed by three consecutive steps: 1) inoculation with 2 ultraviolet (UV) radiations, 2) growth of bacterial colonies and 3) treatment with medicated ring-shaped devices. The first. bacteriological measurements after 2 UV exposures were performed at day 3 of the tests. At day 7 after inoculation of both eyes of a calf with M. bovis, a medicated or a non-medicated ring-shaped device was inserted into each eye of a calf. The eye receiving the non-medicated ring was taken as a control for comparison with the eye that received a medicated ring. During the next 7 day period following a medicated ring insertion, the number of bacteria in the treated eyes dropped dramatically to negligible levels (0 to 30 colony forming units/swab), while the control eyes which received a non-medicated ring still exhibited a relatively high number of bacteria ($10^3\;to\;10^6$ colony forming units/swab). The number of bacteria was significantly reduced by the antibiotic released from the medicated ocular insert.

• Clinics in Shoulder and Elbow
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• v.7 no.1
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• pp.41-45
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• 2004

In adhesive capsulitis of the shoulder of no response to nonoperative treatment, an arthroscopic capsular release and manipulation improves range of motion and pain relief. We performed an arthroscopic examination in the stiff shoulder, of which she had no response to nonoperative treatment, after the conservative treatment of a clavicular shaft fracture by motorcycle-driver traffic accident. We found the intra-articular 'rotator interval bridging scar adhesion' between subscapularis tendon and antero-superior glenoid fossa under the rotator interval which was no adhesion and contracture itself. We performed the scar adhesion removal and synovectomy, maintaining the rotator interval. We recommended nonsteroidal anti-inflammatory drug for postoperative pain relief and continuous active and passive range of motion (ROM) exercise to gain motions. Preoperatively, active and passive range of motion were 70° for forward elevation, 60° for abduction and especially 0° for external rotation. After postoperative 2 months, active ROM were 150° for forward elevation, 130° for abduction and 80° for external rotation. After postoperative 6 months, passive and active ROM were full. UCLA score improved from preoperative 9 points to postoperative 29 points.

• BMB Reports
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• v.34 no.1
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• pp.80-84
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• 2001

The human papillomavirus E7 protein can form a specific complex with a retinoblastoma tumor suppressor gene product (p105-Rb) that results in the release of the E2F transcription factor, which is critical for the growth-deregulation and transforming properties of the viral E7 oncoprotein. In an attempt to apply interaction between the E7 oncoprotein and a target cellular protein Rb for an in vitro screening system for drugs against human papillomavirus infection, we primarily investigated the E7Rb binding through a pull down assay and enzyme-linked immunosorbent assay. The pull down assay showed that both glutathione S-transferase-tagged E7 and His-tagged E7 immobilized on resins specifically produced complexes with bacterially expressed Rb in a dose-dependent manner, as determined by immunoblot analyses. This result coincided with that of an enzyme-linked immunosorbent assay, which is a useful system for the mass screening of potential drugs. Taken together, this screening system (based on the interaction between E7 and Rb) can be a promising system in the development of drugs against cervical cancers caused by human papillomavirus infection.