• Journal of Pharmaceutical Investigation
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• 제29권1호
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• pp.37-45
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• 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.

• Journal of Pharmaceutical Investigation
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• 제40권5호
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• pp.263-267
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• 2010

Nanoemulsions have been widely investigated for many years because of their attractive and unique characteristics. Nanoemulsions are composed of oil, surfactant, co-surfactant and water. Especially, cosurfactant plays a critical role in formation of nanoemulsions. In pharmaceutical area, a pre-concentrate form of nanoemulsions which is known as self-nanoemulsifying drug delivery systems (SNEDDS) was available for some water-insoluble drugs. In this study, we investigated the functional behaviors of cosurfactant in design of SNEDDS and nanoemulsions. Cremophor RH 40$^{(R)}$, Propylene carbonate and medium chain triglyceride were selected for surfactant, cosurfactant and oil, respectively. Cyclosporine was employed as a drug. Phase diagrams showed the area of isotropic o/w region which forms o/w nanoemulsions was not significantly affected by the compositional ratio of cosurfactant. But, drug solubilization capacity, droplet size of nanoemulsions and drug release rate were greatly affected by the cosurfactant.

• Journal of Pharmaceutical Investigation
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• 제38권6호
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• pp.429-432
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• 2008

Drug delivery systems (DDS) have entered mainstream in the pharmaceutical industry in the recent years. Major pharmaceutical companies as well as small or medium-sized biotechnology companies are developing various DDS-based products. We have established Drug Delivery System Company Database, which is an online searchable database of companies that develop DDS-based products and technologies or supply formulations and/or materials. Company summary, products and key technologies are listed in the database. DDS technology fields also include administration routes and indications of drugs. DDS terminologies, Statistical analysis, Useful Links, Glossary and Comments pages are also provided.

• Journal of Ginseng Research
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• 제44권2호
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• pp.222-228
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• 2020

Background: 20(S)-ginsenoside-Rg3 (C₄₂H₇₂O₁₃), a natural triterpenoid saponin, is extracted from red ginseng. The increasing use of 20(S)-ginsenoside Rg3 has raised product safety concerns. Methods: In acute toxicity, 20(S)-ginsenoside Rg3 was singly and orally administrated to Kunming mice and Sprague-Dawley (SD) rats at the maximum doses of 1600 mg/kg and 800 mg/kg, respectively. In the 26-week toxicity study, we used repeated oral administration of 20(S)-ginsenoside Rg3 in SD rats over 26 weeks at doses of 0, 20, 60, or 180 mg/kg. Moreover, a 4-week recovery period was scheduled to observe the persistence, delayed occurrence, and reversibility of toxic effects. Results: The result of acute toxicity shows that oral administration of 20(S)-ginsenoside Rg3 to mice and rats did not induce mortality or toxicity up to 1600 and 800 mg/kg, respectively. During a 26-week administration period and a 4-week withdrawal period (recovery period), there were no significant differences in clinical signs, body weight, food consumption, urinalysis parameters, biochemical and hematological values, or histopathological findings. Conclusion: The mean oral lethal dose (LD₅₀) of 20(S)-ginsenoside Rg3, in acute toxicity, is above 1600 mg/kg and 800 mg/kg in mice and rats, respectively. In a repeated-dose 26-week oral toxicity study, the no-observed-adverse-effect level for female and male SD rats was 180 mg/kg.

• Journal of Pharmaceutical Investigation
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• 제40권spc호
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• pp.113-118
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• 2010

Pharmaceutical technology has primarily focused on the development of the best dosage forms depending on the route of administration. The design of dosage forms is greatly influenced by the route of administration. Due to a variety of advantages such as avoidance of first-pass effect, abundant blood supply and easy access to the absorption site, the oral cavity has frequently been selected as a site for drug delivery. Since the oral cavity is relatively unique from the anatomical and physiological viewpoint, one should always consider these conditions when designing the drug delivery systems for the oral cavity. In this regard, the current review paper was prepared to summarize the essential features of the drug delivery systems utilized in the oral cavity, along with the introduction of various dosage forms developed to date.

• 폴리머
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• 제36권2호
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• pp.149-154
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• 2012

생체적합성을 가진 키토산과 강력한 항산화제로 알려진 리포산을 합성하여 만든 양친매성 고분자를 이용하여 약물전달시스템으로서의 응용 가능성을 알아보았다. 수용액 상에서 자기조립의 성질을 가지는 양친매성 고분자는 나노입자를 형성하고 이 입자 안에 항암제로 널리 쓰이는 5-fluorouracil을 고체분산법을 이용하여 봉입하였다. 최적의 약물전달체를 얻기 위하여 키토산에 결합된 리포산의 비율을 조절하여 입자크기 및 약물봉입률을 비교하였다. DLS를 이용하여 측정한 나노입자는 약 250 nm 정도의 크기를 가졌고 그 봉입률은 10% 내외로 측정되었다. 42%의 리포산 치환율을 가지는 공중합체가 약물전달체로서 가장 우수한 성능을 보여주었다.

• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.149-153
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• 1992

The applicability of sodium alginate as a carrier of 5-fluorouracil as an oral delivery system was investigated. Hydrophobicity of sodium alginate was controlled by introducing cetyl group to this polymer. The effects of degree of esterification for n-cetyl partial ester on the rate of release of 5-fluorouracil in artificial gastric juice and artificial intestinal juice were examined. The release rete of the drug in the gastric juice was mainly affected by the diffusion of the drug. The release rate of the drug in the intestinal juice could be controlled by the degree of esterification. The alginate matrices may be a valuable addition as the carrier of 5-fluorouracil for an oral delivery system.

• 한국정밀공학회:학술대회논문집
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• 한국정밀공학회 2010년도 추계학술대회 논문집
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• pp.447-448
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• 2010

• Journal of Pharmaceutical Investigation
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• 제31권3호
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• pp.181-184
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• 2001

The purpose of this study was to develop transdermal drug delivery system (TDDS) for the combination of physostigmine and procyclidine. The effects of various pressure sensitive adhesives (PSA) on the percutaneous absorption of procyclidine across hairless mouse skin were evaluated to select an appropriate PSA. In addition, the influences of various vehicles on the percutaneous absorption of procyclidine from PSA matrix across hairless mouse skin were evaluated using flow-through diffusion cell system at $37^{\circ}C$. Physostigmine did not have any influence on the permeation rate of procyclidine. The flux of procyclidine was the highest in silicone and PIB and was relatively lower in SIS, Acryl, and SBS adhesive matrices, however, their use was limited by the crystallization of the drug in the matrix. Among acrylic adhesives, the permeability of procyclidine was the highest from poly (ethylene oxide) grafted acrylic adhesive. Some enhancers show different enhancing effect depending on the drug, however, many of the tested enhancers showed enhancing effect for the permeation of both procyclidine and physostigmine to some extent. $Crovol^{\circledR}$ EP 40 showed the highest enhancing effect on the permeation of both compounds. The size of TDDS to provide required permeation rate was estimated to be $35\;cm^2$ based on available information.

• Archives of Pharmacal Research
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• 제19권1호
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• pp.1-5
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• 1996

Laminated films composed of drug-containing reservoir layer and drug-free membrane were prepared. Zero-order drug release with lag time was achieved by laminating drug-free film onto the reservoir layer, while burst effect was observed on cast-on film. The rate controlling membrane was either attached to or cast directly into the reservoir. The release rate was independent on the reservoir composition but dependent on the composition of rate-controlling membrane. In growth inhibitory test of cephalexin from Eudragit RS film to Streptococcus Mutans, the disk even after release test for 72 hours showed more bacterial growth inhibition than that of control. Permeation of drug through rat skin was proportional to the HPC fraction in the film. We could control the release of cephalexin from the film by changing the fraction of Eudragit RS, HPC and DEP content. Consequently, Eudragit RS/HPC film was found to be very effective system for local delivery of drugs.