• Archives of Pharmacal Research
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• 제25권4호
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• pp.534-540
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• 2002

To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.

• 약학회지
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• 제47권3호
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• pp.154-158
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• 2003

Lincomycin, a selective tyrosinase blocker, has been thought to be effective in the treatment of melanogenesis, ephelis, post inflammatory pigmentation, and facial discoloration. In an attempt to develop a transdermal perparation for lincomycin, this study was designed to examine the appropriate contents of various surfactants and ethanol in the cream preparation. Frans type diffusion cell was used to investigate permeation efficiency of the preparation, and lincomycin in the receptor phase was measured by HPLC. After having a 1.5 hrs of leg time, the permeability of lincomycin was rapidly increased by adding surfactants, and varied with different types of surfactants after 10 hrs, the permeability of Brij 56$^{(R)}$ preparation (501.4$\pm$45 $\mu\textrm{g}$/mι) was greater than that either of Labrasol$^{(R)}$ (263.9$\pm$33.7 $\mu\textrm{g}$/mι) or Tween$^{(R)}$20(386.2$\pm$26.7 $\mu\textrm{g}$/mι). Ethanol also increased the permeability of lincomycin.mycin.

• Journal of Plant Biotechnology
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• 제5권1호
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• pp.7-11
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• 2003

The TCM (traditional Chinese medicine) transdermal plaster (also known as "cataplasma") are flexible adhesive patches used for treatment of any pain, resulted from arthritis, sprain and bruise, tendovaginitis, lumbar spine protrude, neuralgia, hyperosteogeny ache, abdominal discomfort and metastatic cancer, etc. This paper provides a review of the TCM transdermal agents for pain palliation and the preparation of these herbal patches.l patches.

• Biomolecules & Therapeutics
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• 제16권3호
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• pp.210-214
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• 2008

The pharmacokinetic parameters and bioavailability of pranoprofen from the gel were measured to determine the enhancing effect of octanoic acid on the transdermal absorption of pranoprofen in rats. 8 mg/kg of pranoprofen was administered from gel with octanoic acid (the enhancer group) or that without octanoic acid (the control group) via the transdermal route, and the results were compared with those obtained from the intravenously (0.5 mg/kg, IV group) or orally administered group (4 mg/kg, oral group). The AUC of the control, the enhancer, the IV, and the oral groups were $20.2{\pm}5.1$, $50.7{\pm}12.7$, $19.9{\pm}2.5$, and $70.5{\pm}17.6\;ug/ml{\cdot}h$ respectively. The average $C_{max}$ of the control and the enhancer group were $0.93{\pm}0.23$ and $2.82{\pm}0.71\;ug/ml$, respectively, and the mean $T_{max}$ of the control and the enhancer group was 7.00 h. The relative bioavailability of the transdermally administered pranoprofen gel containing octanoic acid was approximately 2.50 times higher than the control group, showing a relatively constant, sustained blood concentration with minimal fluctuation. This suggests that it might be feasible to develop a pranoprofen gel preparation containing an enhancer for the transdermal administration, which is more convenient dosage form than the oral dosage forms.

• Archives of Pharmacal Research
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• 제27권3호
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• pp.351-356
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• 2004

A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.261.1-261.1
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• 2000

• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.247-252
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• 2000

The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

• 대한화학회지
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• 제37권5호
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• pp.527-536
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• 1993

Chitin을 강알칼리로 탈아세틸화시켜 합성한 chitosan을 증류수에 팽윤시킨 다음 글리세린을 가하여 교반하였다. 이 고분자 용액에 약물인 silver sulfadiazine을 가하여 경피흡수용 고분자 matrix을 제조하였다. 이렇게 제조된 고분자 matrix로부터 약물의 방출거동과 고분자 matrix 변수와의 상관관계 등을 조사함으로써 지속적이고 조절된 경피흡수제형으로서의 사용 가능성과 특성을 조사하였다. 고분자 matrix 내의 약물의 함유량과 matrix의 두께가 증가할수록 약물의 방출시간은 더 지연되었다. 그러나 글리세린의 함유량이 증가함에 따라 약물의 방출시간은 오히려 감소하였다. 약물의 함유량, 글리세린의 함유량 및 matrix의 두께가 증가할수록 겉보기 방출속도상수(K)값도 증가하였다.이상과 같이 chitosan은 의약의 방출조절형제제로서 가능성을 나타냈으며, 약물로 사용된 silver sulfadiazine의 방출거동은 Higuchi model에 따른 확산으로 생각되었다.

• 약학회지
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• 제43권4호
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• pp.447-457
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• 1999

The purpose of this study is to prepare the adhesive type patch containing flurbiprofen, and to demonstrate the feasibility of flurbiprofen administration through the intact skin using adhesive type patch preparation. For this purpose, two pressure sensitive adhesives, Polyisobutylene(PIB) and $Gelva^{\circledR}737$, were selected from the chemical grade of polymers, and the adhesive type patches of flurbiprofen were prepared. The release rate of flurbiprofen from the PIB-based adhesive patch was higher than that from $Gelva^{\circledR}737$ based adhesive patch. The release rate of flurbiprofen from the PIB-based A-type patch with 1.0mm, 1.5mm or 2.0mm thicknesses followed the first order kinetics. In the skin permeation study, using male hairless mouse skin, a monophasic skin permeation profile was observed with 1% flurbiprofen loading dose. The inclusion of palmitic acid or SLS(0.25~0.5%) as an enhancer produced a remarkable enhancement in the skin permeation rate of flurbiprofen, and the percentile ratio of drug and enhancer appeared to be important for the effective enhancement. In the in vivo percutaneous absorption study, the plasma concentration of the optimal formulation was significantly (p<0.01) higher than that of the conventional cataplasma ($Bifen^{\circledR}$). These studies demonstrate a good feasibility of flurbiprofen administration through the intact skin using a transdermal patch, and show a possibility of the development of flurbiprofen patches.

• Journal of Pharmaceutical Investigation
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• 제29권4호
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• pp.329-335
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• 1999

Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic bronchitis and pulmonary emphysema. For the purpose of developing a transdermal preparation for clenbuterol, we attempted to select an optimal solvent system and permeation enhancer among fatty acids and fatty alcohols which are known to accelerate the penetration of various drugs in permeation experiments using hairless mouse skin and Franz diffusion cell. Apparent partition coefficient of clenbuterol was increased as pH of buffer solution was increased and solubility of clenbuterol was increased as the percent of propylene glycol(PG) in buffer solution(pH 10) was increased. Permeability of clenbuterol from different buffer(pH 10)/PG solvent mixtures was decreased as the percent of PG in pH 10 buffer solution was increased and among the various enhancers studied, lauryl alcohol was found to be the most effective enhancer, increasing the permeability of clenbuterol approximately 76-fold compared with control. Lauryl alcohol$(0{\sim}2%)$ enhanced the permeability of clenbuterol concentration-dependently. In this study, the optimal solvent system for the penetration of clenbuterol was found to be 50/50 buffer(pH 10)/PG solvent mixture containing 2% lauryl alcohol.