• Archives of Pharmacal Research
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• 제29권10호
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• pp.928-933
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• 2006

Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

• 한국응용과학기술학회지
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• 제35권1호
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• pp.141-150
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• 2018

홍합 족사 단백질은 수분이 있는 표면에서도 강한 접착력을 가진다. 홍합 연구에 대표가 되는 marine blue mussel을 통해 9가지 단백질의 구조와 기능이 보고되었으며, 이 단백질들은 홍합 족사를 구성하는 실(threads)과 플래크(plaques)를 형성한다. 알려진 바에 의하면, 히드록시기 2개가 포함된 카테콜 기능기를 가진 DOPA 물질이 계면접착(adhesion)과 내부결합(cohesion) 과정에서 중요한 역할을 하는 것으로 알려져 있다. 본 논문에서는, 최근 10년간 활발히 연구된 계면접착과 내부응력 메카니즘에 대해 소개하고 평가하였다. 또한, 접착력을 갖는 기능기를 활용한 발전된 접착소재의 개발, 바이오접착제와 의료용 소재로 응용가능성에 대해 살펴보았다. 홍합 단백질이 다시 관심의 대상이 되면서, 바이오소재로 사용될 가능성이 커지고 있음이 주목된다.

• Journal of Pharmaceutical Investigation
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• 제24권3호
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• pp.155-165
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• 1994

Some mucoadhesive polymers such as hydroxypropylcelluose (HPC) and carbopol-934 (CP) have been employed for the preparation of mucoadhesive polymeric systems, and their physical properties including mucoadhesion, swelling, and drug release were evaluated. A new simple experimental technique that can quantitatively measure the bioadhesive properties of various polymeric systems has been developed by the methods of detachment force test. As the polymeric systems, the discs of freeze-dried HPC/CP solid dispersions were prepared. The mucosa used in these tests were upper, middle, and lower parts of small intestine of male rats weighing $300{\sim}350\;g$. Detachment forces were increased as the mole fraction of CP increased in discs of HPC/CP solid dispersions. In the points of intestinal site dependence of mucoadhesion, the solid dispersions revealed non-specific mucoadhesion to the intestine. Swelling and drug release characteristics of mucoadhesive polymeric systems were studied extensively to find out the feasibility for the oral controlled delivery systems. Swelling ratio, expressed as the final height/initial height, has been determined in various pH buffer solutions. Hydrochlorothiazide (HCT) was employed as a model drug for release study. Apparent swelling and drug release rate constants, $K_s$ and $K_r$ respectively, were obtained from the square-root time plot of either swelling ratio or released amount of drug, particularly for the time periods before reaching the equilibrium. As a result, the swelling ratio of HPC/CP solid dispersions was increased as the weight percentage of CP increased. Similarly, the release of HCT from the solid dispersions was dependent on pH changes and CP contents, resulted in the slower release of HCT with the increases of pH and CP contents.

• 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.

• 대한치과보철학회지
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• 제44권1호
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• pp.112-123
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• 2006

Purpose: The biocompatibility and bio-adhesive property of a dental implant abutment are important for proper soft tissue healing and maintenance of osseointegration of implant. However, studies of soft tissue healing and mucosal attachment of various materials of implant abutment other than titanium are still needed. In this study, cell attachment, proliferation, cytotoxicity of human gingival fibroblast for ceramic, gold alloy, Ni-Cr alloy and, commercially available pure titanium as a control were evaluated, using MTS and scanning electron microscopy. Materials and Methods: Specimen was designed to disc, 4mm diameter and 1mm thickness, made of ceramic, gold alloy, Ni-Cr alloy and commercially available pure titanium. Primary culture of human gingival fibroblasts were grown in Dulbecco's modified Eagle's medium with 10% fetal bovine serum and 1% antibiotics. Cells were inoculated in the multiwell plates placed the specimen disc. Cell Titer 96 AQucous One Solution Cell Proliferation Assay were done after 1hour 3hours, 24hours, 3days, 5days of incubation. The discs were processed for scanning electron micrography to evaluate cell attachment and morphologic change. Results: The results were obtained as fellows. 1. The ceramic showed high cell attachment and proliferation and low cytotoxicity, which is as much bioadhesive and biocompatible as titanium. 2. The gold alloy represented limited proliferation of human gingival fibroblast and the highest cytotoxicity among tested materials (p<0.05). 3. The Ni-Cr alloy limited the proliferaion of the human gingival fibroblast compared to titanium(p<0.05) but cytotoxicity on the bottom of well was not so considerable, compared to titanium. 4. On the scanning electron micrographs , the ceramic showed good attachment and proliferation of human gingival fibroblast, which was similar to titanium. But gold alloy and Ni-Cr alloy showed the shrinkage of gingival fibroblast both after 24 hours and 3 days. On 5th day, small amount of the human gingival fibroblast proliferation was observed on the Ni-Cr alloy, while the shrinkage of gingival fibroblast was still observed on the gold alloy. Conclusions: These results suggest that the ceramic abutment is as biocompatible as titanium to make proper mucosal seal. The gold alloy has a high cytotoxicity to limit proliferation of gingival fibroblast, which suggest limited use on the anterior tooth where soft tissue healing is recommeded.

• 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.

• Journal of Korean Neurosurgical Society
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• 제30권7호
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• pp.891-895
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• 2001

Objective : Although surgical clipping of intracranial aneurysm is the definite method of treatment, there remains a small number of patients in whom surgical clipping is not technically possible. In such difficult cases, surgeon has to consider other therapeutic alternatives. In this report, we analyze our aneurysmal cases treated by wrapping and coating method and evaluate their surgical outcome and follow-up results. Method : Among the total of 877 patients operated from 1990 to 1999 for intracranial aneurysms at our hospital, 40 cases(4.6%) were treated by wrapping and coating method. They included 24 cases of single ruptured aneurysms and 16 with unruptured ones in multiple aneurysms. Wrapping with temporalis muscle and/or muslin gauze and coating with bioadhesive agent such as fibrin glue were performed. Result : Wrapping and coating method was performed mostly to the anterior communicating artery aneurysm (35%), and mostly because of the broad-based neck of an aneurysm(43%). At the time of discharge, 30 out of 40 patients(80%) showed favourable outcome and three cases died. The patients were monitored for average of 37 months(3-75 months). Among 24 cases with single ruptured aneurysm, 4 cases(17%) had early rebleeding within 6 months from the initial hemorrhage, and such rebleeding occurred within the first postoperative month in 3 cases. However, there was no rebleeding after the 6 months. Among 16 patients whose aneurysms were unruptured ones, none of them showed bleeding episode. Conclusion : It seems likely that the wrapping and coating method would be some help to prevent the rebleeding of an intracranial aneurysm. In order to obtain more accurate results regarding the efficacy of such method, it will be necessary to perform a multi-center study for longer follow-up periods and various wrapping and coating materials.

• 보존과학회지
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• 제36권6호
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• pp.541-548
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• 2020

휘발성 유기 화합물 기반의 접착제를 대체하고자 천연 재료에 대한 수요가 늘고 있지만, 제조 및 생산의 전 과정에서 휘발성 유기화합물 사용을 일절 배제할 경우, 제조의 곤란, 생산성 및 보존성의 저하 등의 단점이 나타났다. 본 연구에서는 해조류의 카라기난 성분을 이용해 천연바이오 접착제를 제조하고 종이 접착제로서의 가능성을 확인해보고자 하였다. 카라기난을 이용한 액상형 바이오 종이 접착제의 제조에서 carrageenan의 겔화는 접착제의 제조과정, 발림성, 균일성, 접착 강도의 문제를 나타내게 된다. 이를 위하여 추출된 전체 carrageenan 중에서 λ-carrageenan만을 분리하여 사용하였으며 이로 인하여 매우 안정된 종이 접착제의 제조가 가능하였다. 최종 조성은 λ-carrageenan 52.0 ± 1.0%, polyvinylpyrrolidone 30.5 ± 0.5%, ethylhexylglycerin 1.0 ± 0.05%, glycerin 1.5 ± 0.05%, dextrine 13.5 ± 0.5%, 식품용 소포제 FD330A 0.6 ± 0.05%의 조성이었다. 이들이 나타내는 점도는 1.13 ± 0.07 × 10⁵ cPs (25℃), pH 6.22, 건조속도 15 min, △b^* -10.79, △E^*ab 8.18의 자외선 열화 결과를 나타내고 있었으며 44.63 kgf/cm²의 매우 우수한 접착 강도를 나타내고 있었다. 이 접착제는 TVOC, HCHO 및 중금속 모두에서 불검출 결과를 나타내었으며 총호기성생균수 측정과 ASTM G 21-15 시험법에 의하여 곰팡이 challenge test에서도 곰팡이에 대한 우수한 저항성 결과를 나타내고 있어서 접착제의 항속성에서도 우수한 결과를 나타내고 있는 것으로 보인다.