• Korean Journal of Pharmacognosy
• /
• v.20 no.3
• /
• pp.175-179
• /
• 1989

From crude drug preparation(Soshiho-Tang) ginseng sapogenins were identified by TLC and $ginsenoside-Rb_1$ was determined quantitatively by HPLC. Panaxadiol, pandaxatriol, acid-hydrolysates of ginseng saponin, were identified by TLC with benzene/acetone(4 : 1, v/v). Rf values of which were measured as 0.26 and 0.14, respectively. The content of $ginsenoside-Rb_1$ was determined by HPLC on $Lichrosorb-NH_2$ column with $CH_3CN/H_2O/n-BuOH$(80 : 20 : 10, v/v). Its recovery rate in the extract granules, was as relatively low as $19.8{\pm}1.4%$ compared to the content in raw red ginseng.

• Journal of Pharmaceutical Investigation
• /
• v.41 no.4
• /
• pp.227-232
• /
• 2011

Alnus japonica has been known to exert antioxidative, anti-inflammatory, anti-cancer and immune response inhibitory effects. The aim of this study was to figure out the characteristics of extracts obtained with different extraction solvent such as water, 100% ethanol, 70% ethanol or 70% methanol because characteristic components such as oregonin and hirsutanone extracted from Alnus japonica might be essential for the biological activity. For this purpose, oregonin and hirsutanon of four extracts, index ingredient of Alnus japonica, were analyzed with HPLC and physicochemical studies such as SEM, particle size and zeta potential were conducted. In cell cytotoxicity study, extract of water showed the highest cytotoxicity among four extracts. In case of oregonin, 70% MeOH and water extracts showed high contents and in case of hirsutanone, all extracts showed similar contents except 70% EtOH extracts. The extract of 70% MeOH from Alnus japonica for both oregonin and hirsutanone appeared to have the highest content. Both oregonin and hirsutanone extracted from Alnus japonica using 70% methanol showed stability in pH 1.2.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.6
• /
• pp.453-460
• /
• 2005

4-Aminopyridine (AP) is a potassium channel blocker used in the treatment of neurological disorders such as multiple sclerosis and Alzheimer disease. AP‘s window of therapeutic effect appears to correlate with its plasma halflife (3.5 hours). It demonstrates pH-dependent solubility because of a weakly basic drug. In addition, the resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study is to design sustained release matrix tablet containing AP, overcoming this problem. $Eudragit^{\circledR}$ L 100 (EuL) and sodium alginate were used in an effort to achieve pH independent drug release. The effect of sodium alginate and EuL on drug release from matrix tablet was investigated. The drug release behavior from the different tablets was analyzed by $t_{20%},\;t_{40%},\;t_{60%}$, The exponential diffusion coefficient n, kinetic constant K were calculated according to the Korsmeyer-Peppas equation. The drug release from matrix tablets prepared with sodium alginate was decreased with increasing the content of sodium alginate in pH 7.4 while there is no significant difference in pH 1.2. The exponent n values were determined to be approximately 0.5 and 0.8 respectively, in both pH 1.2 and 7.4. These values indicate diffusion-based anomalous mechanism and erosion-based anomalous mechanism, respectively. The drug release from sodium alginate matrix tablets prepared with solid dispersion of EuL containing drug showed a slow drug release in an acidic medium and a more fast drug release in phosphate medium, compared with sodium alginate matrix tablets prepared with physical mixture. These results may be attributed to the gel forming ability of sodium alginate and pH dependent solubility of EuL. Therefore, sustained-release AP matrix tablets using sodium alginate and EuL were successfully prepared.

• YAKHAK HOEJI
• /
• v.36 no.3
• /
• pp.212-219
• /
• 1992

Although oral route is the most convenient route for drug administration, the short and variable transit of drug through GI tract restricts the sustained drug absorption after oral administration. Thus, for sustained absorption of drugs, it is desirable to prolong the GI transit time by retaining the dosage forms in the stomach. In this study, the enzyme-digestible swelling hydrogel was synthesized by heating the mixed solution of N-vinyl-2-pyrrolidone[monomer], acrylated albumin[crosslinking agent] and proxyphylline[drug] at $65^{\circ}C$ for 10 hours in the cylindrical test tube. The resultant hydrogel tablet (diameter; 0.77 cm, thickness; 0.47 cm) was designed to swell in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the drug release. After releasing drug, the hydrogel was expected to be degraded by pepsin, an enzyme in the stomach, and eventually solubilized. Actually, the hydrogel synthesized in the study swelled to a size larger than the diameter of the pylorus ($1.3{\pm}0.7$ cm) and slowly digested in the presence of pepsin. Drug release from the hydrogel was prolonged up to about 12 hours. The swelling kinetics was dependent on albumin acrylation time, drug content and gel thickness. Particularly the gel thickness was the most important factor that influences on drug release. By adjusting these factors, the albumin-crosslinked hydrogel was expected to be retained in the stomach for up to 60 hours and used as a potential platform of drugs for long-term GI absorption.

• 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.

• Korean Journal of Food Science and Technology
• /
• v.33 no.5
• /
• pp.514-520
• /
• 2001

Naturally occurring sulfur dioxide in medicinal herbs(crude drug materials) and its origin was investigated. Sulfur dioxide content in 28 kinds (101 samples) of medicinal herbs was studied by two different methods, Monnier-Williams and acid-distillation ion chromatography. Generally, less than 5 ppm of sulfur dioxide was found from the tested herbs. In some herbs, Monnier-Williams method showed higher level of sulfur dioxide than acid-distillation ion chromatography probably due to the presence of volatile organic acid presence in herbs. Naturally occurring sulfur dioxide measured in medicinal herbs may be derived from sulfur compounds of medicinal herbs.

• Journal of Life Science
• /
• v.24 no.4
• /
• pp.437-446
• /
• 2014

Problems appear when triptans are taken orally. For example, the bioavailability of triptan is reduced by the digestive system, and the drug level in the blood reduces rapidly over time; there is also a possibility of gastrointestinal disorder. To improve side effects, a transdermal patch has been prepared in hydrogel form. The polymer matrix that makes up the hydrogel uses PVA; PEG is used as an additive to induce inter/intra hydrogen bonding of the PVA and almotriptan drug is added. In addition, to accelerate micro-phase separation between PVA chains, liquid nitrogen is used. In FT-IR analysis, the absorption bands of PVA, PEG, and almotriptan were found. The degree of crystallinity, the water uptake ability and tensile strength were increased with increasing PEG content. In drug release tests, the amount of drug released increased depending on the PEG content. In this study, hydrogels with 10 wt% PEG showed better performance in drug release. Approximately 60% of the total drug amount was released in 2 hr, and the drug continued to release for 1 day. Thus, the prepared hydrogel patch is suitable as a transdermal formulation for the second dose administration of triptans to patients who require recurrent migraine treatment within 24 hr after the first administration.

• Korean Journal of Food Science and Technology
• /
• v.37 no.6
• /
• pp.912-917
• /
• 2005

Physicochemical components of dried green algae, Seaweed fulvescens (Capsosiphon fulvescens) with $96.02{\pm}0.02%$ moisture content, were investigated. Crude protein, crude lipid, ash and carbohydrate content of C. fulvescens were $31.76{\pm}0.26,\;1.01{\pm}0.21,\;13.58{\pm}0.62\;and\;53.65{\pm}0.73$, respectively. Predominant minerals were Na, Mg, Ca, K and P. Fe $(122.83{\pm}11.19mg/%)\;and\;Se\;(0.90{\pm}0.07mg%)$ contents in were higher than those of other seaweeds. Major free sugars were identified as fructose, glucose, sucrose, maltose and galactose. Organic acid including L-malic acid, citric acid, tartaric acid and d-malic acid were detected. Most abundant amino acids were glutamic acid, aspartic acid and alanine. Main fatty acids were palmitic acid, linolenic acid and stearidonic acid, with 58.37% polyenes.

• Biomolecules & Therapeutics
• /
• v.21 no.2
• /
• pp.173-179
• /
• 2013

Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

• Journal of Pharmaceutical Investigation
• /
• v.29 no.1
• /
• pp.37-45
• /
• 1999

ABSTRACT-A self-microemulsifying drug delivery system (SMEDDS) was developed to enhance the solubility and dissolution rate of poorly water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The system was optimized by evaluating the solubility of DDB and the microemulsion existence range after the preparation of microemulsions with varying compositions of triacetin and surfactant-cosurfactant mixtures (Labrasol as surfactant (S) and the combination of Transcutol, Cremophor RH 40 and Plurol oleique as cosurfactant (CoS)). SMEDDS in this study markedly improved the solubility of DDB in water up to 10 mg/ml and the size of the o/w microemulsion droplets measured by dynamic light scattering showed a narrow monodisperse size distribution with an average diameter less than 50 nm. The microemulsion existing range is increased proportional to the ratio of S/CoS, however, it decreased remarkably as the oil content was more than 20%. In vitro dissolution study of SMEDDS showed a significantly increased dissolution rate of DDB in water (> 12 fold over DDB powder), and SMEDDS also had significantly greater permeability of DDB in Caco-2 cell compared to powders.