• Journal of Pharmaceutical Investigation
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• 제33권1호
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• pp.1-5
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• 2003

Physicochemical changes of poloxamer-based gel containing capsaicin analog (N-[3-(3,4-dimethylphenyl)propyl]-4-(2-aminoethoxy)-3-methoxyphenyl acetamide) such as drug content, viscosity and surface tension were investigated during the storage conditions at three different temperatures (25, 40 and $60^{\circ}C$) over 90 days. No noticeable changes of color were observed when stored at 25 and $40^{\circ}C$. However, the color of white poloxamer gels turned yellow during storage at $60^{\circ}C$. The drug contents were unchanged during storage at $25^{\circ}C$ but had tendency to decrease at $40^{\circ}C$. The drug contents were highly decreased over 40-50% when stored at $60^{\circ}C$. The viscosity of a poloxamer-based gel was unchanged during storage at 25 and $40^{\circ}C$ but greatly increased at $60^{\circ}C$. The surface tension of a poloxamer-based gel was not changed at three different temperatures. The storage conditions of a poloxamer-based gel containing capsaicin analog can be considered for further clinical applications.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1997년도 춘계학술대회
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• pp.115-115
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• 1997

A new capsaicin analog modified with 4-hydroxyl and alkyl chain of capsaicin was a very potent antiinflammatory analgesic drug and may be clinically useful for those who have rheumatoid arthritis, diabetic neuropathy and cancer. The purpose of this study was to investigate histopathology after short and long term application of poloxamer-based gels, and percutaneous absorption of various topical formulations. Poloxamer-based gel was prepared by cold method using poloxamer 407. The poloxamer gels was applied to dorsal sites of hairless mouse skin during one week or one month for the evaluation of skin irritation. The applied site was then sectioned for histopathologic examination. The topical formulations were also prepared using CMC, HPMC, MC, carbopol and glycerylmono stearate. Skin variation of poloxamer gels was studied using excised hairless mouse, rat, hamster and human penis skin. Franz-type diffusion cells were used far skin penetration of drug against receptor phase filled with about 10$m\ell$ of 0.9% saline solution kept at 32$^{\circ}C$. The concentration of drug was determined by the reverse phased C18, Symmetry HPLC with fluorometeric detector. No skin erythema was observed after dorsal application of poloxamer-based gels for one week or one month. No histopathologic changes was also examined, suggesting no skin toxicity of poloxamer-based gels. The order of flux rate was HPMC > MC ( CMC > poloxamer >> glycerylmono stearate ( carbopol. There was a skin variation of poloxamer gels. The flux rate of poloxamer gels was highest in case of hairless mouse followed by rat, human and hamster skin. The Partial support-Ministry of Science and Engineering (HAN project).

• 폴리머
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• 제39권3호
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• pp.480-486
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• 2015

조직과 장기 유착은 외과적 수술 후 부작용으로 자주 발생된다. 이러한 조직 유착을 방지하기 위하여 유착부위에 장벽을 형성하여 장기 유착을 방지할 수 있는 온도감응성 하이드로젤 유착방지제를 제조하고자 하였다. 폴록사머, 키토산과 표피성장인자를 가지고 온도감응성 키토산 하이드로젤을 제조하였다. 제조한 키토산 하이드로젤은 인체 내 온도와 유사한 $35^{\circ}C$에서 졸-젤 전이현상을 보였고, 1분 이내에 빠르게 젤화되었다. 키토산 하이드로젤은 표피성장인자를 7일 동안 천천히 방출하였고, 마우스모델에서 평가한 결과 조직 유착 방지를 효과적으로 하는 것을 확인하였다. 온도 감응성과 항균성을 갖는 키토산 하이드로젤이 장기 부착의 증가와 표피성장인자를 천천히 방출하는 유착방지제로서 유용하게 사용될 수 있다.

• Biomolecules & Therapeutics
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• 제6권2호
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• pp.213-218
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• 1998

A novel in situ-gelling and mucoadhesive acetaminophen liquid suppository was developed to improve the patient compliance of conventional solid suppository. In this study, acetaminophen liquid suppository, Likipe $n_{R}$, ［aminophen/Poloxamer 407/Poloxamer 188/so4ium alginate (5/15/19/0.6%)] with relation temperature at 30-36 "C and suitable gel strength and bioadhesive force, dissolution pattern similar to conventional solid type suppository, Suspe $n_{R}$, was developed. Furthermore, the bioequivalence of two acetaminophen products was evaluated in 16 normal male volunteers (age 22-27 yr, body weight 56-72 kg) following sidle rectal administration. Test product was Likipe $n_{R}$ suppository (Dong-Wha Pharm. Corp., Korea)and reference product was Suspe $n_{R}$204-212 suppository (Hanmi Pharm. Corp., Korea). Both products contain 125 mg of acetaminophen. Four Suppositories of the test and the reference product were administered to the volunteers, respectively, by randomized two period cross-over study (2$\times$2 Latin square method). The determination of acetaminophen was accomplished using HPLC. Average drug concentrations at each sampling time and pharmacokinetic parameters calculated were not significantly different between two products (p>0.05); the area under the curve to last sampling time (24 hr) (AU $Co_{-2}$4h/) (30.14$\pm$8.64 vs 27.98$\pm$ 6.53 $\mu$g .h/ml), maximum plasma concentration ( $C_{max}$) (3.29$\pm$0.87 vs 3.60$\pm$0.66 $\mu$g/ml) and time to maximum plasma concentration ( $T_{max}$) (2.91 $\pm$0.55 vs 2.69$\pm$0.60 h). The differences of mean AUCo $_{24h}$, C-a. and T-between the two products (7.18%, 9.58% and 7.53%, respectively) were less than 20%. The power (1-7) and treatment difference ($\Delta$) for AU $Co_{24h}$, $C_{max}$ and $T_{max}$ were more than 0.8 and less than 0.2, respectively at $\alpha$=0.1. The confidence limits for AU $Co_{24h}$, $C_{max}$ and $T_{max}$ (-0.81 ~13.55%, -1.56~ 17.60 and -3.81 ~18.87%, respectively) were less than $\pm$ 20% at $\alpha$=0.1. These results suggest that the bioavailability of Likipe $n_{R}$ suppository is not significantly different from that of Suspe $n_{R}$ suppsitory. Therefore, two products are bio-equivalent based on the current results.results.lts.sults.results.lts.