• Journal of Pharmaceutical Investigation
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• 제41권5호
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• pp.279-288
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• 2011

The Dexamethasone (DEX) loaded chitosan microspheres were prepared by thermal denaturation and chemical cross-linking method using a dierent concentration of glutaraldehyde as chemical cross-linking agent. The prepared microspheres were evaluated for the percentage of Drug Loading (DL), Encapsulation Efficiency (EE) and surface morphology by Scanning Electron Microscopy (SEM). DL and EE were found to be maximum range of 10.0 to 10.79 % and 58.19 to 64.73 % respectively. The SEM Photographs of the resultant microspheres exhibited fairly smooth surfaces and predominantly spherical in appearance. In addition, Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) shown that there was no interaction between the drug and polymer. In vitro and in vivo release studies revealed that the release of dexamethasone was sustained and extended up to 63 days and effectively controlled by the extent of cross-linking agent. Non-clinical parameters such as paw volume, hematological parameters like Erythrocyte Sedimentation Rate (ESR), Paced Cell Volume (PCV), Total Leucocytes Count (TLC), Hemoglobin (Hb), Differential Cell Count (DCC) were investigated in Fruend's Complete Adjuvant (FCA) induced arthritic rats. Radiology and histopathological studies were also performed in order to evaluate the therapeutic efficacy of the DEX-loaded microspheres in extenuating the rat arthritic model.

• Journal of Pharmaceutical Investigation
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• 제40권5호
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• pp.285-289
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• 2010

Manufacturing a multi-layered tablet such as Xatral XL$^{(R)}$ is more complex and expensive than monolayered tablets, but mono-layered tablets may have less favorable release properties depending on the pharmacodynamics and pharmacokinetics of the active ingredient. We therefore sought to develop a monolayer tablet with a similar dissolution profile to the commercial alfuzosin sustained-release triple layered tablet (Xatral XL$^{(R)}$). We prepared four different mono-layered alfuzosin tablets with different concentrations of hydroxypropyl methycellulose and PVP K-90. Fomulation III with alfuzosion/mg-stearate/ HPMC/ PVP K-90 (10/5/110/95 mg/tab) has a similar dissolution rate to Xatral XL$^{(R)}$, with a similarity factor score of 81.4. However, the swelling and erosion rates of the two formulations were different, and NIR analysis showed differences in the mechanisms of drug release. Thus, although formulation III and Xatral XL$^{(R)}$ show similar dissolution rates, the mechanisms of drug release are different.

• Macromolecular Research
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• 제13권1호
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• pp.54-61
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• 2005

We prepared temperature-sensitive liposomes (TS-liposomes) modified with a thermo sensitive polymer, such as poly(N-isopropylacrylamide) (PNIPAAm), to increase the degree of drug release from liposomes at the hyperthermic temperature. A PNIPAAm hydrogel containing TS-Iiposomes was also prepared to obtain a hydrogel complex at body temperature. In addition, a depot system for local drug delivery using the polymer hydrogel was developed to enhance therapeutic efficacy and prevent severe side effects in the whole body. The PNIPAAm-mod­ified TS-liposome was fixed into the PNIPAAm hydrogel having a high temperature-sensitivity. The release behavior of calcein, a model drug, from TS-liposomes in the PNIPAAm hydrogel was then initiated by external hyperthermia; the results indicated that sustained release as a function of temperature and time was caused by the thermosensitivity of the liposome surface and diffusion of the drug into the PNIPAAm hydrogel. Our results indicated that TS-liposomes in a PNIPAAm hydrogel represented a plausible system for local drug delivery.

• KSBB Journal
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• 제14권3호
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• pp.297-302
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• 1999

Poly(DL-lactide)로 피막된 고분자 매트릭스를 약물전달시스템에 이용하기 위해 키토산, 키토산 염산염 및 술폰화 키토산으로 제조되었다. 모델 약물로 프레드니솔론을 사용하는 본 약물방출에 관한 연구는 pH 1.2 염산 용액에서 실험을 하였다. 약물 방출 속도는 고분자 매트릭스의 함유량이 증가할 수록 감소하였다. 피막된 고분자 매트릭스의 종류에 따라 지연된 약물의 방출시간은 키토산의 경우가 가장 길었으며, 술폰화 키토산, 키토산 염산염의 순서였다. DL-PLA로 피막된 고분자 매트릭스가 피막되지 않는 고분자 매트릭스 보다 약물 방출시간이 2배 정도의 지연되었을 뿐만 아니라 초기에 약물 과잉방출 현상도 작아 피막된 경우가 방출 조절형 제재로서 더 바람직한 결과를 보였다. 따라서 DL-PLA로 피막된 고분자 매트릭스는 장시간의 약물 방출을 위한 약물전달체로써의 응용이 기대된다.

• KSBB Journal
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• 제11권6호
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• pp.676-680
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• 1996

키토산을 10%-아세트산에 팽윤시킨 용액과 SD 를 인산염 완충용액에 녹인 용액을 흔합하여 키토산 매트릭스를 제조하였다. 키토산 매트릭스로부터 pH 7 7.4와 pH 1.2에서 약물방출 거통을 규명하고 지속적이고 조절된 약물방출형 제제로서의 사용 가능성 을 고찰하였다. 키토산 매트릭스내의 약물 함유량이 증가함에 따 라 약물 방출 시간이 늦어졌으며, pH 1.2에서보다 p pH 7.4에서 약물 방출 시간이 더 지연되었다. 그 이 유는 약물전달체가 엽기성 용액에서보다 산성 용액 에서 팽윤를 더 잘하기 때문이라고 생각된다. 약물 방출 속도에 있어서는 pH 7.4에서보다 pH 1.2에서 더 빨랐으며, 겉보기 방출속도상수(K)값도 역시 증가하였다. 결과적으로 본 실험에셔 약물전달체로 사 용된 키토산은 방출조절형 제제로서 그 가능성을 타진할 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제26권4호
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• pp.299-308
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• 1996

In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours, respectively. In the relative strength test for PVA hydrogel, PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH powder hollow type suppository were $196.37{\pm}5.63\;ng/ml$, 1105.26 ng/ml/min and 8.66 min, respectively. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH-EC-SDS(PPH : EC=1:3) were $91.30{\pm]14.14\;ng/ml$, 554.69 ng/ml/min, 235.99 min, respectively.

• Archives of Plastic Surgery
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• 제35권3호
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• pp.235-242
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• 2008

Purpose: Due to increasing interest in the treatment of spinal cord injuries, many histopathological studies have been conducted to prove that many neurotrophic factors including growth hormone are important for regeneration of the injured spinal cord. Growth hormone has to be given everyday, however, and this negatively affects compliance in clinical trials. Recently, the invention of sustained release growth hormone (SRGH) that can be given just once a week may both help the regeneration of injured spinal cord and, at the same time, be more compliant and convenient for clinical patients. Methods: In this study, thirty 7-week-old female Spraque-Dawley rats were subjected to a weight-driven impact spinal cord injury. They were divided into 3 groups and Group I and II were injected with SRGH once a week for 4 weeks; Group I were injected into the injured spinal cord area, while Group II were injected into the peritoneal cavity. Meanwhile, Group III were injected with normal saline solution. The functional outcome was evaluated using the Basso-Beattie-Bresnahan motor rating score and the inclined plane test was done 4 weeks after the first injection. Histopathological examination was performed at the same time and the amount of residual white matter was measured in all groups. Results: After 4 weeks, Groups I and II showed greater improvement than Group III(the control group) in the functional test. In the control group, invasion of atypical phagocytes, axonal degeneration, edema and cavity formation in the posterior site of spinal cord gray matter was observed in histopatholgical examination. The rate of residual white matter in Group III was less than in the other groups. Conclusion: Data showed significant functional and histopathological improvement in the groups treated with SRGH into the spinal and peritoneal cavity compared with the control group. SRGH is therefore beneficial because it helps with regeneration of the injured spinal cord and improves the compliance and convenience of patients.

• Journal of Pharmaceutical Investigation
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• 제32권3호
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• pp.185-190
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• 2002

To improve the solubility of poorly water-soluble drug and to develop a sustained release tablets, the need for the technique, the formation of solid dispersion with polymeric materials that can potentially enhance the dissolution rate and extent of drug absorption was considered in this study. The 1:1, 1:4, and 1:5 solid dispersions were prepared by spray drying method using PVP K30, ethanol and methylene chloride. The dissolution test was carried out at in phosphate buffer solution at $37^{\circ}C$ in 100 rpm. Solid dispersed drugs were examined using differential scanning calorimetry and scanning electron microscopy, wherein it was found that felodipine is amorphous in the PVP K30 solid dispersion. Felodifine SR tablets were prepared by direct compressing the powder mixture composed of solid dispersed felodipine, lactose, Eudragit and magnesium stearate using a single punch press. In order to develop a sustained-release preparation containing solid dispersed felodipine, a comparative dissolution study was done using commercially existing product as control. The dissolution rate of intact felodipine, solid dispersed felodipine and its physical mixture, respectively, were compared by the dissolution rates for 30 minutes. The dissolution rates of felodipine for 30 minutes from 1:1, 1:4, 1:5 PVP K30 solid dispersion were 70%, 78% and 90%. However, dissolution rate offelodipine from the physical mixture was 5% of drug for 30 minutes. Our developed product Felodipine SR Tablet showed dissolution of 17%, 50% and 89% for 1, 4, and 7 hours. This designed oral delivery system is easy to manufacture, and drug releases behavior is highly reproducible and offers advantages over the existing commercial product. The dissolution rate of felodipine was significantly enhanced, following the formation of solid dispersion. The solid dispersion technique with water-soluble polymer could be used to develop a solid dispersed felodipine SR tablet.

• Archives of Pharmacal Research
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• 제28권6호
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• pp.736-742
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• 2005

Xyloglucan (XG), which exhibits thermal sol to gel transition, non-toxicity, and low gelation concentration, is of interest in the development of sustained release carriers for drug delivery. Drug-loaded XG beads were prepared by extruding dropwise a dispersion of indomethacin in aqueous XG solution (2 wt.-$\%$) through a syringe into corn oil. Enteric coating of XG bead was performed using Eudragit L 100 to improve the stability of XG bead in gastrointestinal (GI) track and to achieve gastroresistant drug release. Release behavior of indomethacin from XG beads in vitro was investigated as a function of loading content of drug, pH of release medium, and concentration of coating agent. Adhesive force of XG was also measured using the tensile test. Uniform-sized spherical beads with particle diameters ranging from 692 $\pm$ 30 to 819 $\pm$ 50 $\mu$m were obtained. The effect of drug content on the release of indomethacin from XG beads depended on the medium pH. Release of indomethacin from XG beads was retarded by coating with Eudragit and increased rapidly with the change in medium pH from 1.2 to 7.4. Adhesive force of XG was stronger than that of Carbopol 943 P, a well-known commercial mucoadhesive polymer, in wet state. Results indicate the enteric-coated XG beads may be suitable as a carrier for oral drug delivery of irritant drug in the stomach.

• 폴리머
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• 제36권2호
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• pp.202-207
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• 2012

슈도모나스를 함유하는 poly(${\varepsilon}$-caprolactone)(PCL) 마이크로캡슐은 다중에멀젼 시스템에 의하여 제조하였고, 제조조건에 따른 마이크로캡슐의 특성과 방출거동에 대하여 조사하였다. 마이크로캡슐의 형태와 입도분포는 주사전자현미경과 입도분석기를 이용하여 관찰하였고, 방출거동은 액체배양법을 통하여 확인하였다. 다양한 제조조건에 따라 제조된 마이크로캡슐은 10~60 ${\mu}m$의 입자크기와 표면이 매끈하고 균일한 구형의 마이크로캡슐이 형성됨을 확인하였다. 열분석 결과, 마이크로캡슐은 약 $58^{\circ}C$에서 용융피크를 나타내었고 벽재물질의 함량 증가에 따라 용융열이 증가함으로써 벽재의 두께는 PCL 함량에 비례함을 확인할 수 있었다. 또한 슈도모나스의 방출속도는 유화제 함량, 교반속도, PCL 함량에 따라 조절이 가능하며 이는 유화제 함량과 교반속도 증가에 따른 입자 크기의 감소에 의한 비표면적 증가와 벽재물질의 두께 증가에 인한 방출속도의 감소에 의한 것으로 판단된다.