• Genomics & Informatics
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• v.7 no.3
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• pp.163-167
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• 2009

Since its first release in 2007, the National Institute of Food and Drug Safety Evaluation (NIFDS) has provided pharmacogenomic and comparative information specific to Koreans to allow regulatory reviewers and researchers to adapt their working practices to pharmacogenomics. The highlights of this year's additions include "Drug Information", "Gene Information" and "Pharmacogenomic information in the drug labels" sections. These new additions provide information on 737 genes, 719 drugs and pharmacogenomic data of the labels or relabels of 253 approved drugs as of November 2008. The latest version of the Korean Pharmacogenomic Database (KPD, release 2.0) has expanded significantly since its previous release. More SNP and haplotype information has been added to the database with the latest version of the KPD containing approximately four times as many SNPs and haplotypes than the previous version (719 vs. 152, and 30 vs. 7 respectively). Through the "SNP" and "Haplotype" sections, the KPD provides unique Korean SNP and haplotype information as well as comparative information of other populations (Japanese, Chinese, European, African) to offer a range of pharmacogenomic data that can help reviewers and the public understand pharmacogenomic information. The quality and quantity of information in the KPD has also been improved considerably. This data can be found at: http://www.nitr.go.kr/nitr/contents/m134700/view.do/.

• Journal of Pharmaceutical Investigation
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• v.22 no.3
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• pp.205-210
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• 1992

In order to develop a controlled-release oral drug delivery system (DDS) of theophylline (TP), microporous membrane-coated tablets were prepared and evaluated in vitro and in vivo. Rapidly water-soluble core tablets of TP (300 mg) were prepared by wet granulation and compression technique, Then the core tablets were spray-coated with polyvinylchloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of coating suspensions on the pharmaceutical characteristics such as membrane strength and dissolution was investigated in vitro. The membranes remained unbroken in pH 1.2 buffer at $37^{\circ}C$ at least for 2 hours after the disintergration test. TP was released from the coated-released tablets at a zero-order rate over 8 hours. The release at pH 1.2 and 4.0 was similar in rate but a little more rapid than that at pH 6.8. The coated tablets were administered to three healthy male volunteers and their saliva profiles of TP were compared with those from the commercial sustained release TP tablets such as Slobid and Asconthin. Saliva TP concentrations from the coated tablets were successfully sustained over 48 hours after the dosing and were comparable to those of the commercial sustained-release tablets. The membrane-coating technique is very simple and does not need any sophisticated equipments. In this respect, the membrane-coated tablets may be superior to the commercial sustained-release tablets and this technique is worth adopting by the pharmaceutical industries.

• Macromolecular Research
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• v.11 no.4
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• pp.283-290
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• 2003

Organic drugs including aspirin, omeprazole, and naproxen with three different levels of octanol/water partition coefficient were examined for their release behavior from the amphiphilic PCL-b-PEO-b-PCL (PCEC) matrix. Scanning electron micrograph (SEM) of PCEC illustrated a well defined two-phase morphology consisted of dispersed poly(ethylene oxide) (PEO) domain and continuous polycaprolactone (PCL) phase. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) experiments veri tied that three model drugs are dissolved as a molecular dispersion in PCEC matrix. The release of hydrophilic aspirin closely followed the water absorption profile of the matrix indicating that its major fraction is present in PEO domain. However, substantial amount of aspirin present in less hydrophilic region displayed discontinuous biphasic release pattern. In the case of omeprazole with intermediate hydrophobicity consistent release behavior was observed for a period of 24 hrs after the rapid liberation of ca. 10% of the drug presumably partitioned in PEO phase. It was ascribed to the fact that the progressive hydration of PCEC matrix gradually increased the chance of drug/water exposure to compensate the exhaustion of device. Naproxen with the highest octanol/water distribution coefficient among three model drugs exhibited a limited release of 35% for 24 hrs. Finally, hydroxypropyl methylcellulose phthalate (HPMCP)/PCEC blend matrix demonstrated an accelerated and quantitative release of hydrophobic naproxen by generating high porosity and thereby expanding polymer/water interface.

• Macromolecular Research
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• v.8 no.2
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• pp.80-88
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• 2000

Biodegradable microspheres were prepared with poly(L-lactide-co-glycolide) (PLGA, 75 : 25 by mole ratio) by an oil/oil solvent evaporation method for the sustained release of anti-AIDS virus agent, AZT The microspheres of relatively narrow size distribution (7.6$\pm$ 3.8 ㎛) were obtained by controlling the fabrication conditions. The shape of microspheres prepared was smooth and spherical. The efficiency of AZT loading into the PLGA microsphere was over 93% compared to that below 15% for microspheres by a conventional water/oil/water method. The effects of Preparation conditions on the morphology and in vitro AZT release pattern were investigated. in vitro release studies showed that different release pattern and release rates could be achieved by simply modifying factors in the fabrication conditions such as the type and amount of surfactant, initial amount of loaded drug, the temperature of solvent evaporation, and so on. PLCA microspheres prepared by 5% of initial drug loading, 1.0% (w/w) of surfactant concentration, and 25$\^{C}$ of solvent evaporation temperature were free from initial burst effect and a near-zero order sustained release was observed. Possible mechanisms of the near-zero order sustained release for our system have been proposed.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.61-70
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• 1982

Sulfisoxazole, a chemotherapeutic agent, was microencapsulated with ethylcellulose by means of phase separation form cyclohexane by temperatture change. The size distribution was determined by use of standard sieves and the effect of core to wall ratio was noted. To examine their shapes and usrface characteristics, the microcapsules were observed with a scanning electron microscope. Release of the drug from microcapsules into pH 7.5 buffer medium was studied. The release pattern was found to have similar properties to the release of a drug from an insoluble porous matrix reported. The apparent diffusion coefficient of sulfisoxazole was measured for the transport of the drug from the core of microcapsules into the surronding sink condition. The apparent diffusion coefficient increased with increasing capsule size.

• YAKHAK HOEJI
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• v.44 no.3
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• pp.251-256
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• 2000

Sterically stabilized liposomes (SSL) composed of distearoylphosphatidylcholine, cholesterol, dicetylphosphate and distearoylphosphatiodylethanolamine-N-poly(ethyleneglycol) 2000 (DSPE-PEG 2000) were made by reverse phase evaporation method to prolong biological half-life and decrease toxic side effect of drug. Streptozocin (572), a water-soluble antitumor agent with short half-life, was selected as a model drug. The size of SSL was controlled by polycarbonate extrusion to 100 nm which is adequate size for long circulation in plasma. The release rate of drugs from SSL in PBS was evaluated. And the stability of STZ-containing liposomes against drug leakage into rat plasma was evaluated in order to investigate the interaction of liposome and plasma protein. Incorporation of DSPE-PEG 2000 into conventional liposomes significantly decreased the drug leakage into rat plasma.

• Polymer(Korea)
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• v.32 no.2
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• pp.103-108
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• 2008

Osmotic pellet, which consisted of water-swellable seed layer, drug layer, and porous membrane layer, has been widely utilized in oral drug delivery system. In this work, we describe the preparation of osmotic pellet with nifedipine as model drug and a mixture of cellulose acetate (CA) and Eudragit RS as membrane layer, and then examined the drug release behavior on the variation of the thickness change of membrane layer (CA and Eudragit RS) and release media. Furthermore, we examined the nifedipine release behavior using sodium alginate as a potential membrane candidate. Osmotic pellet was obtained in the quantitative yield by fluidized bed coater. Osmotic pellet exhibited the round morphology and the size ranging $1500{\sim}1700{\mu}m$ in SEM. The nifedipine release decreased as the thickness of membrane layer (CA and Eudragit RS) increased. In addition, it observed that there is difference of release amount in between intestinal juice (pH 6.8) and gastric juice (pH 1.2). In the case of osmotic pellet coated with sodium alginate, nifedipine release behavior depended on the crosslinking of sodium alginate layer. In conclusion, we found that various membrane layers could control the release amount of nifedipine.

• Journal of Biomedical Engineering Research
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• v.36 no.6
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• pp.291-295
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• 2015

Various types of implantable drug delivery devices have attracted significant attention for several decades to improve drug bioavailability and reduce side effects, thus enhancing therapeutic efficacy and patients' compliance. However, when implanted into the body, the devices may be influenced by the changes in physiological condition, such as temperature, pH or ionic concentration. Thus, the drug release rates could be also altered concurrently. Therefore, in this work, we employed an implantable ALZET$^{(R)}$ Osmotic Pump, which has been widely used to locally deliver various therapeutic agents and examined the effect of pH, temperature and ionic concentration on its drug release rate. For this, we performed in vitro cell tests to simulate the condition of local tissues influenced by the altered drug release rates, where we used diclofenac sodium as a model drug.

• Polymer(Korea)
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• v.30 no.2
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• pp.112-117
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• 2006

To improve the type error of osmotic tablet which is one of the drug delivery system, osmotic granule could be manufactured by fluidized bed coating. It has drug layer containing different amount of osmogant and is coated with membrane including different types of binder. We confirmed that the morphology of osmotic granule was different at each coating step. The more mont of osmotic agent, the faster drug release was observed due to increasing the driving force for drug release from osmotic granule. And drug release from osmotic granule coated with membrane using different types of binder was differed by solubility of binders to water. The formation of pore in membrane was confirmed by SEM and DSC Membrane using water soluble binder released more amount of drug. From these results, we assured that difference of osmotic pressure between the inside and the outside of granule and porosity of membrane have an effect on drug release from osmotic granule.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.302.1-302.1
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• 2001