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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Journal of Pharmaceutical Investigation
Journal Basic Information
Journal DOI :
The Korean Society of Pharmaceutical Sciences and Technology
Editor in Chief :
Volume & Issues
Volume 40, Issue 6 - Dec 2010
Volume 40, Issue 5 - Oct 2010
Volume 40, Issue 4 - Aug 2010
Volume 40, Issue 3 - Jun 2010
Volume 40, Issue spc - May 2010
Volume 40, Issue 2 - Apr 2010
Volume 40, Issue 1 - Feb 2010
Selecting the target year
Pharmaceutical Usefulness of Biopharmaceutics Classification System: Overview and New Trend
Youn, Yu-Seok ; Lee, Ju-Ho ; Jeong, Seong-Hoon ; Shin, Beom-Soo ; Park, Eun-Seok ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 1~7
DOI : 10.4333/KPS.2010.40.S.001
Since the introduction of the biopharmaceutics classification system (BCS) in 1995, it has viewed as an effective tool to categorize drugs in terms of prediction for bioavailability (BA) and bioequivalence (BE). The BCS consist of four drug categories: class I (highly soluble and highly permeable), class II (low soluble and highly permeable), class III (highly soluble and low permeable) and class IV (low soluble and low permeable), and almost all drugs belong to one of these categories. Likewise, classifying drugs into four categories according to their solubility and permeability is simple and relatively not controversial, and thus the FDA adopted the BCS as a science-based approach in establishing a series of regulatory guidance for the industry. Actually, many pharmaceutical companies have gained a lot of benefits, which directly connect to cost loss and failure decrease in the early stage of drug development. Recently, instead of solubility, using dissolution characteristics (e.g. intrinsic dissolution rate) have provided an improvement in the classification in correlating more closely with in vivo drug dissolution rather than solubility by itself. Furthermore, a newly modified-version of BCS, biopharmaceutics drug disposition classification system (BDDCS), which classify drugs into four categories according to solubility and metabolism, has been introduced and gained much attention as a new insight in respect with the drug classification. This report gives a brief overview of the BCS and its implication, and also introduces the recent new trend of drug classification.
Drug Polymorphism and its Importance on Drug Development Process
Jeong, Seong-Hoon ; Youn, Yu-Seok ; Shin, Beom-Soo ; Park, Eun-Seok ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 9~17
DOI : 10.4333/KPS.2010.40.S.009
Polymorphism has been recognized to be a critical issue throughout the drug product development process. Most of solid phase drugs have polymorphism, which has generated a great deal of interest and the field has been evolving rapidly. Preferably, thermodynamically most stable form of a drug substance is selected to obtain consistent bioavailability over its shelf life and various storage conditions. Moreover, it has the lowest potential for conversion from one polymorphic form to another. However, metastable or amorphous forms may be used intentionally to induce faster dissolution rate for rapid drug absorption and higher efficacy. For pharmaceutical industry, polymorphism is one of the key activities in form selection process together with salt selection. This article introduces the main features in the investigation of solid form selection especially polymorphic behavior with thermodynamic backgrounds, physicochemical properties with solubility, dissolution, and mechanical properties, and characterization techniques for proper analysis. The final form can be recommended based on the physicochemical and biopharmaceutical properties and by the processability, scalability and safety considerations. Pharmaceutical scientists especially in charge of formulation need to be well aware of the above issues to assure product quality.
Current Methodologies for Membrane Permeability Assessment
Shin, Beom-Soo ; Youn, Yu-Seok ; Jeong, Seong-Hoon ; Park, Eun-Seok ; Lee, Mann-Hyung ; Yoo, Sun-Dong ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 19~31
DOI : 10.4333/KPS.2010.40.S.019
Orally administrated drugs permeate the biological membrane by various transport mechanisms. The oral absorption potential is closely related to the physicochemical properties of the drug and interaction with the physiological factors surrounding the site of absorption. Assessment of the drug membrane permeability is an integral part of the early stage drug developmental process. Appropriate selection of the permeability screening method at the right stage of drug development process is important in achieving successful developmental outcomes. This review aims at introducing currently available in vitro and in vivo screening methods for the membrane permeability assessment.
Hyaluronic Acid in Drug Delivery Systems
Jin, Yu-Jin ; Ubonvan, Termsarasab ; Kim, Dae-Duk ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 33~43
DOI : 10.4333/KPS.2010.40.S.033
Hyaluronic acid (HA) is a biodegradable, biocompatible, non-toxic, non-immunogenic and non-inflammatory linear polysaccharide, which has been used for various medical applications including arthritis treatment, wound healing, ocular surgery, and tissue augmentation. Because of its mucoadhesive property and safety, HA has received much attention as a tool for drug delivery system development. It has been used as a drug delivery carrier in both nonparenteral and parenteral routes. The nonparenteral application includes the ocular and nasal delivery systems. On the other hand, its use in parenteral systems has been considered important as in the case of sustained release formulation of protein drugs through subcutaneous injection. Particles and hydrogels by various methods using HA and HA derivatives as well as by conjugation with other polymer have been the focus of many studies. Furthermore, the affinity of HA to the CD44 receptor which is overexpressed in various tumor cells makes HA an important means of cancer targeted drug delivery. Current trends and development of HA as a tool for drug delivery will be outlined in this review.
Functional Polymers for Drug Delivery Systems in Nanomedicines
Lee, Eun-Seong ; Kim, Ji-Hoon ; Yun, Jeong-Min ; Lee, Kyung-Soo ; Park, Ga-Young ; Lee, Beom-Jin ; Oh, Kyung-Taek ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 45~61
DOI : 10.4333/KPS.2010.40.S.045
Polymeric based nanomedicines have been developed for diagnosing, treating, and preventing diseases in human body. The nanosized drug delivery systems having various structures such as micelles, nanogels, drug-conjugates, and polyplex were investigated for a great goal in pharmaceutics: increasing therapeutic efficacy for diseases and decreasing drug toxicity for normal tissues. The functional polymers used for constituting these drug delivery systems should have several favorable properties such as stimuli-responsibility and biodegrdability for controlled drug release, and solublization capacity for programmed drug encapsulation. This review discusses recent developments and trends of functional polymers (e.g., pH-sensitive polymers, biodegradable polymers, and cationic polymers) used for nanosized drug carriers.
Solid Lipid Nanoparticles as Drug Delivery System for Water-Insoluble Drugs
Li, Rihua ; Lim, Soo-Jeong ; Choi, Han-Gon ; Lee, Mi-Kyung ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 63~73
DOI : 10.4333/KPS.2010.40.S.063
Solid lipid nanoparticles (SLNs) have emerged to combine the advantages of polymeric nanoparticles and lipid emulsions in early 1990s. SLNs can present several desirable properties derived from the solid state core. When formulating SLNs, there should be careful considerations about the physical state of the inner solid lipid core and its polymorphism and supercooling behavior. In this review, SLNs were compared to lipid emulsion and emulsion of supercooled melt to understand the unusual behaviors compared to lipid emulsions and to have insights into stability and release mechanism. SLNs have been regarded as biocompatible system because lipids are usually well-tolerable ingredients than polymers. Several studies showed good tolerability of SLNs in terms of cytotoxicity and hemolysis. Similar to various other nanoparticulate drug delivery systems, SLNs can also change biodistribution of the incorporated drugs in a way to enhance therapeutic effect. Most of all, large scale production of SLNs was extablished wihtout using organic solvents. Although there is no SLN product in the market till date, several advantagious properties of SLNs and the progress we have seen so far would make commercial product of SLNs possible before long and encourage research community to apply SLN-based formulations for water-insoluble drugs.
Nano-sized Drug Carriers and Key Factors for Lymphatic Delivery
Choi, Ji-Hoon ; Lee, Yong-Bok ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 75~82
DOI : 10.4333/KPS.2010.40.S.075
Specific diseases like cancer and acquired immune deficiency syndrome (AIDS) occur at various organs including lymphatics and spread through lymphatic system. Thus, if therapeutic agents for such diseases are more distributed or targeted to lymphatic system, we can obtain several advantages like reduction of systemic side effect and increase of efficacy. For these reasons, much interest has been focused on the nature of lymphatics and a lot of studies for lymphatic delivery of drugs have been carried out. Because lymphatics consist of single layer endothelium and have high permeability compared with blood capillaries, especially, the studies using nano-sized carriers have been performed. Polymeric nano-particle, liposome, and lipid-based vehicle have been adopted for lymphatic delivery as carriers. According to the administration route and the kind of carrier, the extent of lymphatic delivery efficiency of nano-sized carriers has been changed and influenced by several factors such as size, charge, hydrophobicity and surface feature of carrier. In this review, we summarized the key factors which affect lymphatic uptake and the major features of carriers for achieving the lymphatic delivery. Lymphatic delivery of drug using nano-sized carriers has many fold improved ability of lymphatic delivery compared with that of conventional dosage forms, but it has not shown whole lymph selectivity yet. Even though nano-sized carriers still have the potential and worth to study as lymphatic drug delivery technology as before, full understanding of delivery mechanism and influencing factors, and setting of pharmacokinetic model are required for more ideal lymphatic delivery of drug.
Parenteral Formulations Based on Albumin Particulate Technology
Lee, Hong-Hwa ; Lee, Min-Jung ; Heo, Sun-Ju ; Sah, Hong-Kee ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 83~95
DOI : 10.4333/KPS.2010.40.S.083
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
) 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
. Information on key roles of albumin in the nab
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.
Surface-attached Solid Dispersion
Park, Young-Joon ; Oh, Dong-Hoon ; Yan, Yi-Dong ; Seo, Yoon-Gee ; Lee, Sung-Neug ; Choi, Han-Gon ; Yong, Chul-Soon ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 97~102
DOI : 10.4333/KPS.2010.40.S.097
A novel surface-attached solid dispersion is designed to improve the solubility and oral bioavailability of poorly water-soluble drugs without crystalline change. Accordingly, it draws increasing interest because of excellent stability and no pollution for accomplishing enhanced solubility and bioavailability, which have recently been highlighted in connection with a number of higher value-added poorly water-soluble drugs. In addition, excellent stability can be attained when the poorly water-soluble drugs are not dissolved but dispersed in water and provide no crystallinity change. This solid dispersion is given by means of attaching the dissolved carriers such as hydrophilic polymer and surfactant to the surface of dispersed drug particles followed by changing the hydrophobic drug to hydrophilic form. The aim of the present review is to outline the preparation, physicochemical property and bioavailability of novel surface-attached solid dispersion with improved solubility and bioavailability of poorly water-soluble drugs without crystalline change.
Controlled-Release Pelletized Dosage Forms Using the Extrusion-Spheronization Process
Rhee, Yun-Seok ; Lee, Jae-Hwi ; Lee, Beom-Jin ; Park, Eun-Seok ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 103~112
DOI : 10.4333/KPS.2010.40.S.103
Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.
Pharmaceutical Devices for Oral Cavity-based Local and Systemic Drug Delivery
Yun, Gyi-Ae ; Choi, Sung-Up ; Park, Ki-Hwan ; Rhee, Yun-Seok ; Lee, Beom-Jin ; Lee, Jae-Hwi ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 113~118
DOI : 10.4333/KPS.2010.40.S.113
Pharmaceutical technology has primarily focused on the development of the best dosage forms depending on the route of administration. The design of dosage forms is greatly influenced by the route of administration. Due to a variety of advantages such as avoidance of first-pass effect, abundant blood supply and easy access to the absorption site, the oral cavity has frequently been selected as a site for drug delivery. Since the oral cavity is relatively unique from the anatomical and physiological viewpoint, one should always consider these conditions when designing the drug delivery systems for the oral cavity. In this regard, the current review paper was prepared to summarize the essential features of the drug delivery systems utilized in the oral cavity, along with the introduction of various dosage forms developed to date.
Non-viral siRNA Delivery Systems
Won, Young-Wook ; Jang, Yeon-Lim ; Kim, Jin-Seok ; Jeong, Ji-Hoon ; Kim, Yong-Hee ;
Journal of Pharmaceutical Investigation, volume 40, issue spc, 2010, Pages 119~129
DOI : 10.4333/KPS.2010.40.S.119
The emergence of new biological drugs based on RNA interference (RNAi) technology has been one of the most attractive issues in the field of gene therapy for years. However, the use of siRNA therapeutics in clinical settings is still limited due to lack of appropriate delivery systems for the highly charged macromolecular drug. In this review, recent development of major non-viral siRNA delivery systems, including lipid, liposome, polymer, and peptide-based carriers, is to be summarized.