• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.287-293
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• 1997

To make a stable o/w emulsion, the effects of egg lecithin as an emulsifier and polyvinylpyrrolidone (PVP) as an auxiliary emulsifier on the physical stability of emulsion were investigated. The oil-in-water emulsion system was manufactured by microfluidizer and evaluated the physical stability. Average particle size and size distribution of emulsion was measured by dynamic light scattering analyzer and interfacial tension was measured. From the interfacial tension tested, critical micelle concentration of the egg lecithin was 0.1 %w/v and optimal concentration for the preparation of emulsion was 1.0 %w/v. The mean particle size was about $0.2\;{\mu}m$ which was suitable for injections. The short-term accelerated stability studies were conducted by centrifugation, freeze-thaw method and shaking of the emulsion samples. The addition of PVP was caused the reduction in the particle size and improved the physical stability of emulsion. These results suggested that a mixed interfacial film comprising the egg lecithin and PVP was formed at the o/w interface and it was effective in preventing phase separation under thermic or mechanical stress. We used antineoplaston A10 (A10) as a model drug which is peptide and amino acid derivative having a action to the living organism against the development of neoplastic growth by a nonimmunological progress. It has a poor solubility in water and there may be a difficulty in formulation of A10. Emulsion formulation study about A10 was performed. Solubility of A10 in emulsion was about five times as high as that in water. From the results of solubility and partition coefficient, almost A10 molecules in o/w emulsion exist in the interface between oil and water.

• 대한화장품학회지
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• 제49권3호
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• pp.231-245
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• 2023

화장품 업계에서는 미백, 주름, 항산화, 항노화 등 기능성 화장품의 신소재 개발과 더불어 실제로 피부에 적용 시 피부흡수율을 높이는 기술이 중요하다. 이에 본 연구에서는 실험설계법인 반응표면분석법(RSM)을 활용하여 나노에멀젼 제형을 최적화하고자 하였다. Glabridin을 활성성분으로 하여 고압유화 방법으로 나노에멀젼을 제조하였으며, 최종적으로 최적화한 나노에멀젼의 피부흡수율을 평가하였다. RSM 인자로서 계면활성제 함량, 콜레스테롤 함량, 오일 함량, 폴리올 함량, 고압유화 압력, 고압유화 횟수를 달리하여 나노에멀젼을 제조하였다. 그 중 입자 크기에 가장 큰 영향을 미치는 인자인 계면활성제 함량, 오일 함량, 고압유화 압력, 고압유화 횟수를 독립변수로 하였고, 나노에멀젼의 입자 크기와 피부흡수율을 반응변수로 하였다. 중심점 5 회 반복실험을 포함하여 총 29 회 실험이 무작위로 수행되었으며, 제조된 나노에멀젼의 입자 크기와 피부흡수율을 측정하였다. 그 결과를 바탕으로 최소 입자 크기, 최대 피부흡수율을 갖는 제형을 최적화하였으며, 계면활성제 함량 5.0 wt%. 오일 함량 2.0 wt%, 고압유화 압력 1,000 bar, 고압유화 횟수 4 pass를 최적 조건으로 도출하였다. 최적 조건으로 제조한 나노에멀젼의 물성으로 입자 크기는 111.6 ± 0.2 nm, 다분산지수는 0.247 ± 0.014, 제타전위는 -56.7 ± 1.2 mV로 측정되었다. 나노에멀젼과 일반 에멀젼 피부흡수 시험 결과, 24 h 후 나노에멀젼의 누적 투과량은 79.53 ± 0.23%이며, 대조군으로서 에멀젼의 누적 투과량은 66.54 ± 1.45%로 나노에멀젼이 에멀젼보다 13% 높았다.

• 약학회지
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• 제37권4호
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• pp.370-382
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• 1993

In order for formulation of rectal containing OMZ, the OMZ suppositories were prepared using water-soluble base, PEG 4000 base and oil-soluble base, Witepsol H 15. Chemical stability of OMZ in suppositories was increased when Witepsol H 15 was used as a suppository base and arginine was added as a stabilizer. The decomposition of OMZ in suppository bases followed the first-order kinetics and their rate constants were 0.11 day $^{1}(t_{1/2}$=/6.25 days) for Witepsol H 15 suppository and 0.48 day $^{1}(t_{1/2}$=/1.43 days) for PEG 4000 suppository, respectively. On the other hand, the decomposition rate constants of Witepsol suppository and PEG suppository stabilized with arginine were 3.89$\times$10$^{-3}$(t$_{1/2}$=171.1 days) and 8.76$\times$10$^{-3}$ day $^{1}(t_{1/2}=79.9 days), respectively. Shelf-lives of the Witepsol and PEG suppositories stabilized with arginine were t$_{90%}$=291.8 days and t$_{90%}$=282.1 days at $35^{\circ}C$ and 75% RH, respectively. The dissolution test of OMZ suppositories was performed by rotating dialysis cell(RDC) method and the release rate constant was calculated by the simplified Higuchi's equation, Q'=K' t$^{1/2}$. Dissolution of OMZ from suppositories was augmented as arginine was added, particle size of OMZ was reduced and a suitable surfactant such as SLS was added. RDC method was more appropriate and available than Paddle method to evaluate the dissolution rate of lipophilic-base suppositoies. Arginine was found to be a very useful exipient for the enhancement of stability and dissolution of OMZ in suppositories.

• Parasites, Hosts and Diseases
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• 제55권4호
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• pp.409-416
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• 2017

The high prevalence of pediculosis capitis, commonly known as head lice (Pediculus humanus capitis) infestation, has led to the preparation of a community-based pediculicidal ointment, which is made of common household items and the extract of Tinospora crispa stem. The present study aimed to evaluate the safety, efficacy, and physicochemical characteristics of the T. crispa pediculicidal ointment. The physicochemical properties of the ointment were characterized, and safety was determined using acute dermal irritation test (OECD 404), while the efficacy was assessed using an in vitro pediculicidal assay. Furthermore, the chemical compounds present in T. crispa were identified using liquid-liquid extraction followed by ultra-performance liquid chromatography quadruple time-of-flight mass spectrometric (UPLC-qTOF/MS) analysis. The community-based ointment formulation was light yellow in color, homogeneous, smooth, with distinct aromatic odor and pH of $6.92{\pm}0.09$. It has spreadability value of $15.04{\pm}0.98g{\cdot}cm/sec$ and has thixotropic behavior. It was also found to be non-irritant, with a primary irritation index value of 0.15. Moreover, it was comparable to the pediculicidal activity of the positive control $Kwell^{(R)}$, a commercially available 1% permethrin shampoo (P>0.05), and was significantly different to the activity of the negative control ointment, a mixture of palm oil and candle wax (P<0.05). These findings suggested that the community-based T. crispa pediculicidal ointment is safe and effective, having acceptable physicochemical characteristics. Its activity can be attributed to the presence of compounds moupinamide and physalin I.

• Journal of Nutrition and Health
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• 제13권4호
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• pp.199-206
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• 1980

원성군 시범종합영양사업을 위한 어린이용 고영양 보충식품(HNLC Supplementary Foods)의 개발을 시도하였다. MFM-KIST Extrusion Cooking System에 의한 일연의 실험결과, CSS-3, CSS-4 및 BSS-4 등의 제품이 영양학적, 식품가공학적 경제적 그리고 기호성등의 여러가지 면에서 바람직하였다. 특히 CSS-4 제품(기본 원료구성 : 옥수수가루 68%, 탈지대두분 20%, 참깨 가루 2%, 옥수수 기름 4%, 설탕 4%, 식염 1%, 비타민, 무기질성분 및 첨가물 1%)은 영양강화 간편식품으로서 가공생산성 및 기호성이 가장 만족스러웠으나, 제품의 다양성 및 원료수급면을 고려하여 위 개발제품들을 모두 필요에 따라 활용할 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제35권4호
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• pp.233-241
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• 2005

Ursolic acid (UA), a bioactive triterpene acid, has been known to increase collagen content in human skin in addition to other actions such as anti-inflammatory, skin-tumor prevention and anti-invasion. However, it is poorly soluble in water. Therefore, we firstly prepared microemulsion system with benzyl alcohol, ethanol and Cremophor EL, RH 40 and Brij 35 as surfactant in order to increase solubility of UA and then prepared microemulsion was dispersed in o/w cream base for the topical delivery of UA in an effort to improve anti-wrinkle effect. The pseudo-ternary phase diagrams were developed and various microemulsion formulations were prepared using benzyl alcohol as an oil, Cremophor EL, RH 40 and Brij 35 as a surfactant. The droplet size of microemulsions was characterized by dynamic light scattering. The accumulation of VA in the skin from topical cream was evaluated in vitro using hairless mouse skins. The mean droplet size was $26.8{\pm}6.6$ nm for microemulsions II with Cremophor EL. All UA creams showed pseudoplastic flow and hysterisis loop in their rheogram, depending on the type of materials added in topical creams. The in vitro accumulation data demonstrated the UA topical cream prepared with the combination of Poloxamer 407 and Xanthan gum as a copolymer showed higher accumulation percentage than those prepared with either Poloxamer 407 or Xanthan gum. These results suggest that UA topical cream using microemulsion systems may be promising for the topical delivery of UA.

• 약학회지
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• 제42권2호
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• pp.187-195
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• 1998

In order to ameliorate disadvantages of buccal ointments and mucoadhesive tablets used for the treatment of aphthosis, a thin mucoadhesive patch containing triamcinolone acetoni de was designed and evaluated for the pharmaceutical properties. The adhesive gel layer consisting of Noveon AA-1, hydroxypropylcellulose-M and ethylcellulose N 100, and the protective gel layer of ethylcellulose N 100, Eudragit RSPO and castor oil have been formulated and various properties such as viscosity of drug gel layer, thickness, in vitro adhesion time, adhesive strength, surface pH, content uniformity and drug release are tested. The mean viscosity of drug-containing gel layer was found to increase with increasing amount of Noveon OAA-1 or hydroxypropylcellulose-M. The optimum formulation showed the thickness of 171 ${\mu}$m, surface pH of 4.6, in vitro adhesion time of 8 hours and adhesive strength of 272.7g/sheet. The drug content of each patch was relatively homogeneous with the value of 273${\pm}$6.77g. Drug release study showed that compared to mucoadhesive tablet, the patch showed a faster drug release. Drug release was delayed by hydroxypropylcellulose-M, but not by ethylcellulose N 100. The patches prepared were nonirritant and the muco adhesion was better than the commercial product (AftachR) on the market. Based on these results, this mucoadhesive patch is expected to be an effective dosage form for the treatment of aphthosis.

• 한국미생물·생명공학회지
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• 제37권4호
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• pp.399-404
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• 2009

재조합 대장균으로부터 회수된 고순도 베타카로틴을 첨가한 기능성 화장품의 제조방법을 개발하고 이의 임상실험을 수행하여 개발된 화장품의 주름개선 성능을 평가하였다. 베타카로틴의 유효성, 각종 피부흡수 및 사용성, 질감 등을 고려하여 화장품을 처방하였다. 베타카로틴의 첨가량은 피부에 독성을 나타내지 않고 콜라겐생합성 촉진효과가 우수하며 베타카로틴 자체의 특유한 붉은 색소가 피부에 묻어나오지 않을 정도인 화장품 kg 당 1 mg으로 결정하였다. 베타카로틴을 용해시키기 위하여 식용오일을 사용하였고 항산화물질인 vitamin E(tocopheryl acetate)를 첨가함으로써 제품의 장기간 보관 시 베타카로틴의 안정성과 유효성에 도움을 주게 하였다. 유화제 및 유화안정제는 2.0% 첨가함으로써 유상과 수상이 분리되지 않도록 하였다. 유연제인 dimethicone을 0.35% 첨가함으로써 백탁 현상을 제거하고 피부에 대한 사용감을 좋게 하였다. 보습작용을 보이는 sorbitol을 첨가함으로써, 건조한 환경에 대한 피부트러블을 최소화하게 하였다. 제품의 안정도를 조사하였다. 60일간의 실험에서 상온에 보관된 제품의 pH는 변화가 거의 없었고 0, 25, $40^{\circ}C$의 온도서 물리 화학적 변화가 없는 안정한 상태를 유지하였다. 뿐만 아니라 광제품의 주름개선 성능을 평가하기 위하여 20명의 피시험자를 대상으로 화장품의 인체적용시험을 실시하였다. 시험자의 평가결과 4주 후 피험자의 38%가 주름이 감소하였고 8주 후에는 68%가 주름이 개선되었다.

• 대한화장품학회지
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• 제41권3호
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• pp.201-208
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• 2015

오가노겔은 반고형상이며 3차원의 네트워크 구조로 이루어진 친유성 용매로 이루어져 있다. 본 연구에서는 유상과 수상에서 모두 난용성 특징을 가진 제니스테인을 포함하는 레시틴 오가노겔을 개발하였다. 이 시스템은 안정할 뿐만 아니라 경피 흡수 실험에서도 높은 흡수율을 보였다. 본 오가노겔 제형에 적합한 원료들을 선별한 결과, 수화된 레시틴, 해바라기유, dipropylene glycol (DPG), polyethylene glycol (PEG)이 이 시스템에서 주로 사용되었다. 레시틴 오가노겔의 제조에 적합한 원료의 함량은 phase ternary diagram 작성을 통하여 결정하였다. 제조된 레시틴 오가노겔을 organoleptic characteristics, stability, pH, rheology, phase transition temperatures, microscopic analysis, skin penetration 실험을 통해 평가하였다. 본 연구 결과를 통해 본 논문에서 제시하는 레시틴 오가노겔 제형은 안정한 상태에서 난용성 물질을 높은 농도로 피부에 효과적으로 전달할 수 있는 제형으로 활용될 수 있을 것이라 생각된다.

• 대한화장품학회지
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• 제42권2호
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• pp.135-143
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• 2016

본 연구에서는 파이토케미컬 펩타이드 유도체를 포함하는 니오좀 및 리포좀 제형의 안정성을 조사하였다. 여러 가지 조건에서 레시틴 혹은 계면활성제를 이용하여 제조된 리포좀 중에서 sodium palmitoyl sarcosinate와 마카다미아넛 오일을 이용한 니오좀의 안정성이 제일 우수하였다. 파이토케미컬 펩타이드 함유 니오좀(N9)의 형태는 TEM으로 확인하였으며, 입자크기는 95.7 nm로 관찰되었다. N9의 안정성은 Turbiscan 결과 ($0^{\circ}$와 $45^{\circ}$)와 제타포텐셜(-78.19 mV)로 확인하였다. N9의 펩타이드 봉입률은 BCA assay 결과 65.2%로 관찰되었다.