• Archives of Pharmacal Research
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• 제25권5호
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• pp.572-584
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• 2002

Rapid development in molecular biology and recent advancement in recombinant technology increase identification and commercialization of potential protein drugs. Traditional forms of administrations for the peptide and protein drugs often rely on their parenteral injection, since the bioavailability of these therapeutic agents is poor when administered nonparenterally. Tremendous efforts by numerous investigators in the world have been put to improve protein formulations and as a result, a few successful formulations have been developed including sustained-release human growth hormone. For a promising protein delivery technology, efficacy and safety are the first requirement to meet. However, these systems still require periodic injection and increase the incidence of patient compliance. The development of an oral dosage form that improves the absorption of peptide and especially protein drugs is the most desirable formulation but one of the greatest challenges in the pharmaceutical field. The major barriers to developing oral formulations for peptides and proteins are metabolic enzymes and impermeable mucosal tissues in the intestine. Furthermore, chemical and conformational instability of protein drugs is not a small issue in protein pharmaceuticals. Conventional pharmaceutical approaches to address these barriers, which have been successful with traditional organic drug molecules, have not been effective for peptide and protein formulations. It is likely that effective oral formulations for peptides and proteins will remain highly compound specific. A number of innovative oral drug delivery approaches have been recently developed, including the drug entrapment within small vesicles or their passage through the intestinal paracellular pathway. This review provides a summary of the novel approaches currently in progress in the protein oral delivery followed by factors affecting protein oral absorption.

• 한국임상약학회지
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• 제10권3호
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• pp.130-139
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• 2000

This study is intended to set the criteria for the classification of prescription and non-prescription drugs, and classify hospital pharmacy formulations according to the criteria. 717 hospital pharmacy formulations were collected ken the Center for review and evaluation of health insurance, and national provincial offices. Hospital pharmacy formulations were evaluated based on the 'Guidelines on the Hospital Pharmacy Formulations (Notification No. 2000-46)'by the Ministry of Health and Welfare. Drug classification advisory committee was composed of twelve medical and pharmaceutical specialists, and suggested opinions on the drug classification. Among 717 formulations, 651 drugs $(90.8\%)$ satisfied the basic conditions for the hospital pharmacy formulations. 312 formulations $(43.5\%)$ were classified as drugs for the disinfection and tests. For the rest of them, 231 formulations were classified as prescription drugs whereas 108 drugs were as non-prescription drugs. 56 non-prescription drugs were included as hospital formulations, because there were no therapeutic alternatives. Iu sum 599 drugs $(83.5\%)$ were suggested as hospital pharmacy formulations. The study also recommends pharmaceutical companies to produce drugs of limited commercial value, and doctors to change their unique prescribing behavior in order to prevent the abuse of hospital pharmacy formulations.

• Archives of Pharmacal Research
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• 제28권8호
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• pp.977-982
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• 2005

The aim of this study was to compare two formulations of film-coated pellets containing c1arithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of filmcoated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the $AUC_{0-24h}$ was found to be $96.2\%\;and\;58.7\%$ for F-1 and F-2 compared with IR, and the $T_{max}$ was delayed.

• 약학회지
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• 제18권4호
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• pp.236-242
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• 1974

Extrusion-spheronization processing combination was used to produce spherical granules with experimental formulations which contain microcrystalline cellulose as a diluent. The produced granules were compared on the basis of the following physical properties ; (a) bulk density, (e) porosity, (f) friabillity and (g) dissolution rate. With the specific experimental formulations used in this study, the increased plate rotational speeds of Marumerizer (400-1200rpm) produced continually more spherical material and also the obtained data indicated that the particle size distribution and dissolution rate depend upon the amount of microcrystalline cellulose used. As a result, the spherical granule preparation with microcrystalline cellulose has good properties in flow rate, packing propertyu and friability and offers a suitable method of granule preparation in pharmaceutical industry.

• Archives of Pharmacal Research
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• 제29권12호
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• pp.1187-1192
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• 2006

The aims of this study were to encapsulate arbutin (AR) in liposome to enhance the skin-whitening activity, and to investigate the effect of liposome formulation on the entrapment efficiency (EE%), skin permeation rate and skin deposition. The liposomes were prepared by a film dispersion method with several different formulations and were separated from the solution by using the gel-filtration method. The physical (size distribution, morphology) and chemical (drug entrapment efficiency, hairless mouse skin permeation and deposition) properties of liposomes were characterized. The entrapment efficiency in all liposome formulations varied between 4.35% and 17.63%, and was dependent on the lipid content. The particle sizes of liposomes were in the range of $179.9{\sim}212.8\;nm$ in all liposome formulations. Although the permeation rate of AR in the liposome formulations decreased compared with AR solution, the deposition amount of AR in the epidermis/dermis layers increased in AR liposomal formulation. These results suggest that liposomal formulation could enhance the skin deposition of hydrophilic skin-whitening agents, thereby enhancing their activities.

• Journal of Pharmaceutical Investigation
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• 제34권5호
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• pp.407-411
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• 2004

New formulations of amlodipine maleate tablet have been investigated to enhance the stability of the drug against light and humidity. Three kinds of amlodipine maleate tablets were prepared. One is prepared by previously known formulation (formulation C), the others were by new formulations using hydrophilic polymer $(Opadry^{\circledR})$ coated granules (formulations A and B). Amlodipine maleate powder was coated with $Opadry^{\circledR}$ to produce the coated granules and it was mixed with other excipients to produce the tabletting mass of new formulations A and B. Dissolution rate of newly formulated tablets was over 80% within 10 minutes in 0.01 M HCl medium, and its dissolution pattern was similar to that of $Norvasc^{\circledR}$ tablet. After 6 months storage under accelerated conditions, residual drug contents of tested formulations (A and B) were not significantly different from formulation C, ranging from 96.2 to 100.4%. Meanwhile, dissolution amount of formulation C was significantly reduced compared to that of formulation A (p<0.05), showing formulation A was more stable than unprotected formulation C at the accelerated conditions. Results of appearance, hardness and disintegration remained unchanged during stability study. In conclusion, it showed that the new formulations had enhanced the stability characteristics and hydrophilic coating technique was an alternative and promising method to improve the stability of amlodipine maleate tablet.

• 대한화장품학회지
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• 제38권1호
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• pp.1-13
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• 2012

본 총설에서는 기포의 화장품 이용에 대해서 논의하고자 하였다. 기포의 생성은 기포형성제와 기포 생성 장치 등을 이용하며 생성된 기포는 다양한 특성을 나타낸다. 기포는 기체의 용매에 대한 분산 형태로 발생된다. 기포의 안정성과 유변학적인 성질 등을 평가하는 것은 기포를 제형으로 이용하기 위한 출발점이다. 기포의 의약품과 화장품에 대한 이용은 점차 증가 추세에 있다. 의약품의 경우 기포 제형은 직장(rectal), 질(vaginal) 및 피부(dermal)용으로 대별될 수 있으며 화장품 영역의 경우 기포 제형은 모발 및 메이크업 영역에서는 헤어 무스, 파운데이션 등에서 이용되고 있으며 기초화장품에서는 자외선 차단 화장품에 이용되고 있다. 최근 유효성분의 안정화 및 유효성분의 피부 전달 측면에서 많은 연구와 특허가 출원되고 있어 향후 기능성화장품의 새로운 제형으로 활용이 기대된다.

• Journal of Pharmaceutical Investigation
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• 제40권spc호
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• pp.83-95
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• 2010

Over the years, nanoparticle drug delivery systems have demonstrated versatile potentials in biological, medical and pharmaceutical applications. In the pharmaceutical industry nanotechnology research has mainly focused on providing controlled drug release, targeting their delivery to specific organs, and developing parenteral formulations for poorly water soluble drugs to improve their bioavailability. Achievement in polymer industry has generated numerous polymers applicable to designing nanoparticles. From viewpoints of product development, a nanocarrier material should meet requirements for biodegradability, biocompatibility, availability, and regulatory approval crieteria. Albumin is indeed a material that fulfills such requirements. Also, the commercialization of a first albumin-bound paclitaxel nanoparticle product (Abraxane$^{TM}$) has sparked renewed interests in the application of albumin in the development of nanoparticle formulations. This paper reviews the intrinsic properties of albumin, its suitability as a nanocarrier material, and albumin-based parenteral formulation approaches. Particularly discussed in detail are albumin-based particulate injectables such as Abraxane$^{TM}$. Information on key roles of albumin in the nab$^{TM}$ technology and representative manufacturing processes of albumin particulate products are provided. It is likely that albumin-based particulate technology would extend its applications in delivering drugs, polypeptides, proteins, vaccines, nucleic acids, and genes.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.47-54
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• 1995

Transdermal patch formulations of estradiol to treat post-menopausal symptoms and prevent osteoporosis in women were developed and evaluated for the permeation characteristics through the excised hairless mouse abdorminal skin and the uterotropic effect on the ovariectomized rabbits. The design of patch formulations was optimized by varying several formulation parameters, such as type of enhancers, amount of enhancers, amount of drug loading and coating thickness. Compared to a commercially available transdermal product, several patch formulations showed the similar skin permeation profiles (following zero-order kinetics), but their skin permeation rates were lasted for the longer period (a week). In one-week uterotropic efficacy test in the ovariectimized rabbits, the selected patch formulations showed the positive effect in atrophy of the urogenital epithelium. The mean values of uterus weight in rabbits after application of patches containing estradiol were much higher than those in control group (containing no drug).

• Archives of Pharmacal Research
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• 제13권3호
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• pp.215-220
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• 1990

Two different, derivative spectrophotometric and gas-liquid chromatographic, procedures for direct quantitation of caffeine and some commonly dispensed antihistaminics in bulk forms, in their laboratory prepared mmixtures and in dosage formulations, have been investigated. The limit, sensitivity reproducibility and accuracy of each method were studied for each individual drug substance and in some usual pharmaceutical formulations.