• Proceedings of the PSK Conference
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• 2003.10b
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• pp.232.1-232.1
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• 2003

Purpose. To develop a hard gelatine capsule containing meloxicam (Yuhan Meloxam capsule$\^$TM/), in vitro dissolution characteristics and bioavailability in beagle dog were compared with commercial product (Mobic capsule$\^$TM/). Methods. Meloxicam capsule$\^$TM/ was prepared by powder filling method using meloxicam, lactose, magnesium stearate, and others. The release of Meloxicam capsule$\^$TM/ and Mobic capsule$\^$Tm/ were monitored by USP dissolution method under various dissolution donditions - dissolution medium (pH 1.2, 4.0, 6.8 and water). (omitted)

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.11 no.1
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• pp.69-81
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• 1998

The aim of this study was to investigate the effects of Chungdaesan(CDS) by various administration routes on skin anaphylactic reaction. The most classic and popular skin reaction in vivo is passive cutaneous anaphylaxis(PCA) In this study, therefore, the author investigated the effect of CDS on PCA reaction activated by anti-dinitrophenyl immunoglobulin E antibody The results showed that CDS potently suppressed orally, topically, intraperitoneally, and intradermally administered. However, it did not show suppressive activity when intravenously administered. In addition CDS significantly inhibited anti-DNP IgE induced mast degranulation in mice skin. Moreover, CDS suppressed anaphylactic histamine release from mast cells induced by anti-dinitrophenyl immunoglobulin E antibody. These results indicate that CDS suppresses the PCA reaction by stabilization of mast cells in vivo and in vitro am] also suggest that the differential activity following administration routes may be caused by the difference of bioavailability.

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.242.1-242.1
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• 2001

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1092-1096
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• 2005

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.267-275
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• 2002

A self-microemulsifying drug delivery system (SMEDDS) was developed to increase the dissolution rate, solubility, and ultimately bioavailability of a poorly water soluble drug, lovastatin. SMEDDS was thε mixtures of oils, surfactants, and cosurfactants, which emulsify under conditions of gentle agitation, similar to those which would be encountered in the gastro-intestinal (GI) tract. Various types of self-emulsifying formulations were prepared using four types of oil (Capryol 90, Lauroglycol 90, Labrafil M 1944 CS and Labrafil M 2125), two surfactants (Cremophor EL and Tween 80), and three cosurfactants (Carbitol, PEG 400 and propylene glycol). Thε efficiency of emulsification was studied using a laser diffraction size analyzer to determine particle size distributions of the resultant emulsions. Optimized formulations selected for bioavailability assessment were Carpryol 90 (40%), Cremophor EL (30%) and Carbitol (30%). SMEDDS containing lovastatin (20 mg and 5 mg) were compared to a conventional lovastatin tablet $(Mevacor^{\circledR},\;20\;mg/tab)$ by the oral administration as prefilled hard gelatin capsules to fasted beagle dogs for in vivo study. The arεa under the serum concentration-time curve from time zero to the last measured time in serum, $AUC_{0{\rightarrow}24h}$, was significantly greater in SMEDDS, suggesting that bioavailability increase 130% and 192% by the SMEDDS, respectively. The self-emulsifying formulations of lovastatin afforded the improvement in absolute oral bioavailability relative to previous data of lovastatin tablet formulation. These data indicate the utility of dispersed self-emulsifying formulations for the oral delivery of lovastatin and potentially other poorly absorbed drugs.

• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.471-481
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• 2005

In Korea, generic drug and bioequivalence test are the hot issues since a new medical system of separation of dispensary from medical practice was started in 2000. The KFDA(Korea FDA) had revised several times ${\ulcorner}Guidance\;for\;bioequivalence\;test{\lrcorner}$. In vitro dissolution test has been extensively used as a quality control tool for solid oral dosage forms. In an effort to minimize unnecessary human testing, in vitro/in vivo correlations (IVIVC) between in vitro dissolution and in vivo bioavailability are increasingly becoming an integral part on extended release drug product development. The recently published US guidance, ${\ulcorner}Extended\;release\;oral\;dosage\;forms\;:\;development,\;evaluation,\;and\;application\;of\;in\;vitro/in\;vivo\;correlations{\lrcorner}$ will be helpful for us to make our own guideline.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.272-272
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• 1996

While ranitidine is well known to be absorbed rapidly, the underlying cause of variable bioavailability in intra- and inter-subjects has not been clarified yet. Intestinal permeability is a key controlling factor for oral absorption of highly soluble drugs, In the present study, intestinal ferfusions have been conducted to determine the intestinal permeabilities(Peffs) of ranitidine in the rats, dogs and humans and compared to the estimated fractions of dose absorbed (FAs) in humans. A new in vivo methodology, using a regional segmental perfusion technique, has been used in the dogs and humans. In situ single-pass perfusion experiments have been performed in the rats. In the dog and human studies, perfusion experiments have been conducted on two periods to determine the intrasubject variability, There was low significant intrasubject variation as compared to intersubject variation. The Peffs of ranitidine were 33%, 51%, and 45% inthe rats, dogs and humans, respectively. The FAs were approximately the same for all three species models, suggesting rats and dogs are good animal models for estimating the oral absorption of ranitidine in humans. In addition, the estimated extent of absorption of this drug is consistent with the average bioavailability, indicating that ranitidine has permeability-limited absorption characteristics. Supported by FDA Grant FD01462.

• The Journal of the Convergence on Culture Technology
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• v.6 no.2
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• pp.567-572
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• 2020

The purpose of this study was to investigate the effects of Anti-Thrombotic Activities and Cardiovascular Improvement of Fermented Garlic Extracts. The incidence of cardiovascular diseases (CVDs) is increasing rapidly in developed countries, with CVDs now representing the leading cause of morbidity and mortality. Natural products and ethnomedicines have been shown to reduce the risk of CVDs. Garlic is a medicinal plant used throughout the world for its anti-inflammatory, antioxidant, and antiplatelet activities. We hypothesized that fermented preparations of these products may possess stronger antiplatelet effects than the non-fermented forms owing to the increased bioavailability of the bioactive compounds produced during fermentation. Therefore, we compared these compounds via in vitro and ex vivo platelet aggregation assays by using standard light transmission aggregometry and ex vivo granule secretions from rat platelets. We found that fermented preparations exerted more potent and significant inhibition of platelet aggregation both in vitro and ex vivo. Likewise, ATP release from dense granules of platelets was also significantly inhibited in fermented preparation-treated rat platelets compared to that in non-fermented preparation-treated ones. We concluded that fermented preparations exerted more potent effects on platelet function both in vitro and ex vivo, possibly as a result of the increased bioavailability of active compounds produced during fermentation. We therefore suggest that fermented products may be potent therapeutics against platelet-related CVDs and can be used as antiplatelet and antithrombotic agents.

• YAKHAK HOEJI
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• v.39 no.6
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• pp.577-584
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• 1995

On the combination of antacid, the pharmacokinetics and gastric adhesion of [$^{14}c$]aceglutamide aluminium complex([$^{14}C$]AGA) were examined in rats. Specially, this study was focused on the drug interaction that the co-administration of antacid may affect the oral absorption and gastric adhesion of aceglutamide aluminium complex(AGA). In the study of the oral co-administration of [$^{14}C$] AGA and antacid(aluminium hydroxide and magnesium hydroxide(AM)), the radioactivity of plasma and urinary recovery was lower than that of [$^{14}C$]AGA alone administered group. However, the cumulative recovery of radioactivity in feces was increased significantly. The comparative bioavailability of [$^{14}C$] AGA from the plasma concentration-time curve and urinary recovery was about 60%. In vitro, the effect of antacid on the gastric adhesion of AGA was not significatly different between AGA and AGA/antacid treatment. And it accorded well with the result of in vivo experiment. In conclusion, on the combination of antacid, the oral absorption of AGA was decreased by the gastric adhesion was not affected in respect of drug interaction.

• CELLMED
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• v.2 no.4
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• pp.31.1-31.7
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• 2012

Curcuma longa belongs to the family Zingiberaceae and can be found in the tropical and subtropical regions of the world. It is widely used in Asiatic countries, especially India and South East Asia where it is cultivated commercially as a condiment. Its rhizomes exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacterial, antioxidant effects, nematocidal activities, antiproliferative and antiangiogenic activities and are of pharmaceutical importance. Another relevant medicinal property exhibited by it is antidiabetic property which is reviewed here. Studies on the efficacy of crude C.longa extracts against type 2 diabetes in murine models reveal that it demonstrates a hypoglycemic effect by lowering the blood glucose levels under in vivo conditions. Clinical studies have revealed the safety of curucmin (major principle component exhibiting pharmaceutical properties from C.longa) on humans but with very low bioavailability. In view of its effective hypoglycemic effect and its low bioavailability, further studies are needed for the characterization of the bioactive principles and formulating the development of C.longa extracts as a novel anti-diabetic therapeutic agent.