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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 20, Issue 4 - Dec 1990
Volume 20, Issue 3 - Sep 1990
Volume 20, Issue 3 - Sep 1990
Volume 20, Issue 2 - Jun 1990
Volume 20, Issue 1 - Mar 1990
Selecting the target year
Albumin-Mediated Hepatic Uptake of Drugs
Han, Yong-Hae ; Shim, Chang-Koo ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 179~191
A central dogma of pharmacology is that only unbound drug is capable of translocation across biological membrane. Thus, hepatic uptake is assumed to be solely determined by the unbound concentration of the diffusible moiety at the surface of the liver cell. However, an increasing number of experimental observations with xenobiotics that are normally very extensively bound to plasma proteins (>99%) appear to be inconsistent with these assumptions. This suggested that in addition to progressive spontaneous dissociation within the liver sinusoids and space of Disse, direct interactions of the albumin-drug complex at the plasma membrane may facilitate dissociation of the complex. To explain this phenomena. called albumin-mediated uptake, 4 mechanisms have been suggested. The validity of such hypotheses needs to be examined by the further study. Because albumin-mediated uptake has also been observed to occur in other plasma proteins, protein-mediated uptake rather than albumin-mediated uptake seems to be acceptable.
Enhancement of Dissolution Properties of Poorly Soluble Drugs (V)-Enhanced Dissolution of Furosemide by Cogrinding or Coprecipitating with Povidone-
Shin, Sang-Chul ; Oh, In-Joon ; Koh, Ik-Bae ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 193~198
To increase the dissolution rate of furosemide, cogrinding or coprecipitating of furosemide with povidone was carried out. The ground mixture of furosemide with povidone was prepared by cogrinding in a ceramic ball mill and the coprecipitate was prepared by solvent method using methanol. The povidone ground mixture and the coprecipitate showed a faster and more enhanced dissolution rate than the physical mixture or intact furosemide. The IR, DTA and TGA studies showed the physicochemical modifications of furosemide from the ground mixture and the coprecipitate. An interaction, in the ground mixture and in the coprecipitate, such as association between the functional groups of furosemide and povidone might occur in the molecular level. The coprecipitating and cogrinding techniques with povidone provided a promising way to increase the dissolution rate of poorly soluble drugs.
Pharmacokinetics of Propranolol in Rabbits with Hepatic Failure
Lee, Jin-Hwan ; An, Seon-Yeob ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 199~203
The pharmacokinetics of propranolol administered orally (10 me/kg) was investgated in the rabbits of carbon tetrachloride induced hepatic failure. The plasma concentration and relative bioavailability of propranolol were increased significantly in hepatic failure rabbits, compared with those of normal rabbits. There were significant relationship between GOT, GPT value and bioavailability parameters of propranolol. In short, dosage regimen of propranolol is considered to be adjusted in dose size and dosing interval using GOT or GPT an index.
Effect of Azone on Penetration of Antiviral Agents through Hairless Mouse Skin
Choi, Seung-Ho ; Kim, Johng-Kap ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 205~208
1-Dodecylazacycloheptan-2-one (Azone) is a new agent that enhances the percutaneous penetration of a number of different chemicals. BVDU and FEAU were evaluated for their potential efficacy in the treatment of cutaneous herpes simplex virus infections by in vitro studies through hairless mouse skin. This study demonstrates the value of penetration enhancing agent (Azone) and the need for a predictable evaluations in the development of topical antiviral agents.
Efficacy Test of Commercial Digestives Containing Antacids, Digestive Enzymes and Herbal Drugs (II)-Digestive Activity Test-
Kim, Chong-Koo ; Jang, Jung-Yun ; Lah, Woon-Young ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 209~215
The activities of s-amylase,
and protease of three combination products containing digestive enzymes, antacids and herbal drugs on the Korean market were estimated. The effects of antacids and herbal drugs on the activities of digestive enzymes were investigated. Starch-saccarifying activity of s-amylase, starch-dextrinizing activity of
and protein-peptic activity of protease were estimated by Somogy, Mc'Credy, and Casein-Folin method, respectivley. The optimal pH of s-amylase,
and protease were pH 5.0, 4.8 and 7.0, rcspectively. The digestive activities at optimal pH continued about eight hours. The digestive activities of individual enzymes were reduced to 40-90% by antacids and were affected somewhat positively or negatively by herbal drugs. Enzyme activities of the combination products were also affected by pH and reaction time.
Synthesis of pt(II) Complexes Containing Diphosphines and Evaluation of Antitumor Activity
Noh, Young-Soo ; Masahide, Noji ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 217~222
New antitumor-active pt(II) complexes of trans-l-diamine cyclohexane containing diphosphines as a leaving group were synthesized. The structures of the pt(II) complexes were determined by analyzing the infrared and
magnetic resonance spectra. Antitumor activities of the pt(II) complexes were tested against murine leukemia
according to the protocol of the National Cancer Institute. All the pt(II) complexes Synthesized were antitumor-active. In particular, water-soluble
exhibited excellent antitumor activity, giving T/C % values of 341 and 356 respectively, each with four cured mice out of six at a dose of 25 mg/kg. These pt(II) complexes are considered to be worthy of further development.
Drug Delivery into the Blood-Brain Barrier by Endogenous Substances-A Role of Amine and Monocarboxylic Acid Carrier Systems for the Drug Transport-
Kang, Young-Sook ;
Journal of Pharmaceutical Investigation, volume 20, issue 4, 1990, Pages 223~228
The contribution of endogenous transport systems to the blood-brain barrier (BBB) transport of basic and acidic drugs was studied by using a carotid injection technique in rats and an isolated bovine cerebrovascular disease state were compared between the normotensive rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) which have been well established as an animal model with pathogenic similarities to humans. Basic drugs such as eperisone, thiamine and scopolamine inhibited, in a concentration dependent manner the in vivo uptake of
through BBB, whereas amino acids and acidic drugs such as salicylic acid and valproic acid did not inhibit the uptake. The uptake of
by B-CAP increased with time and showed a remarkable temperature dependency. The uptake of
by B-CAP showed the very similar inhibitory effects as observed in the in vivo brain uptake, and was competitively inhibited by a basic drug, eperisone. The in vivo BBB uptakes of
acid were dependent on pH of the injectate and the concentration of drugs. Several acidic drugs such such as salicylic acid, benzoic acid and valproic acid inhibited the in vivo uptake of
acid, whereas amino acid, choline and a basic drug such as eperisone did not inhibit the uptake. The uptake of acetic acid by B-CAP was competitively inhibited by salicylic acid. The permeability surface area product (PS) through BBB for
in SHRSP was significantly lower than that in WKY. The concentration of choline in the brain dialysate in SHRSP was about half of that in WKY, while no significant difference was observed in the plasma concentration of choline between SHRSP and WKY. No significant difference was observed in the transport of monocarboxylic acids, glucose and neutral amino acid through BBB between SHRSP and WKY. From these results, it was concluded that BBB transport system of choline contributes to the transport of basic drugs through BBB, that acidic drugs can be transported via a moncarboxylic acid BBB transport system and that the specific dysfuntion of the BBB choline transport in SHRSP was ascribed to the reduction of the maximum velocity of choline concentration in the brain interstitial fluids.