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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 26, Issue 4 - Dec 1996
Volume 26, Issue 3 - Sep 1996
Volume 26, Issue 2 - Jun 1996
Volume 26, Issue 1 - Mar 1996
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Preparation and Evaluation of Ketoprofen-incorporated Solid Lipid Nanoparticles (SLN)
Baek, Myoung-Ki ; Lee, Sang-Young ; Jee, Ung-Kil ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 245~256
Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about
, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative,
and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN.
was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.
A Study on the Solubilization and Physical Properties of Sanjoinine-A
Sheu, Kwang-Gyou ; Lee, Chi-Ho ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 257~261
The seeds of Zizyphus Jujuba have been used as an antianxiety agent for the treatment of insomnia from the earliest times. Sanjoinine-A, isolated from the seeds of Zizyphus Jujuba, have been found to have a minor tranquilizer activity. However this drug is poorly soluble in water. In order to increase the dissolution rate of sanjoinine-A, solid dispersions with PVP-MC and inclusion complex with
were prepared and evaluated. All of these systems increased the dissolution rate of sanjoinine A comparing with sanjoinine-A free base. From pH-rate profile of sanjoinine-A at
, it was found that sanjoinine A was relatively stable in acidic solution, but unstable in basic solution.
Study on Preparation and Drug Release of Sulconazole Nitrate Gels
Hyun, Jong-Mok ; Kim, Kyung-Kook ; Jee, Ung-Kil ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 263~271
Sulconazole nitrate(SCN), an imidazole derivative which has been effective in the treatment of dermatophytosis, tinea versicolor and candidiasis, was formulated as a gel containing drug, poloxamer 407, ethanol and propylene glycol. The resulting SCN gels were evaluated with respect to their viscosity, drug release rate, skin permeation rate. The apparent viscosity of SCN gel increased in proportion to poloxamer 407, drug and propylene glycol concentration. In case ethanol was added, the apparent viscosity decreased. The drug release rate of SCN gel increased in proportion to temperature and ethanol concentration. But the drug release rate decreased as the concentration of poloxamer 407 increased. The increase of drug concentration induced nonlinear increase of drug release rate. When propylene glycol was added at the level of 10%, the drug release rate increased but from 15% it decreased. The skin permeation rate decreased in high concentration of poloxamer 407. The skin permeation rate of SCN gel containing 15% ethanol increased about twice than that of gel without ethanol. The increase of drug concentration induced nonlinear increase of skin permeation rate. When propylene glycol was added at the level of 10%, the skin permeation rate increased but from 15% it decreased.
Preparation and Evaluation of Chondroitin Sulfate/Gelatin Microspheres Containing Dexamethasone 21-Acetate
Yong, Chul-Soon ; Kim, Young-Ju ; Oh, Doo-Man ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 273~280
Chondroitin sulfate/gelatin microspheres containing dexamethasone 21-acetate were prepared by complex coacervation method and their release patterns were examined in vitro. Microspheres prepared with a small amount of crosslinking agent had smooth surface and few pores, but those with a large amount of crosslinking agent were more porous and less spherical. In vitro release patterns were varied by changing polymer/drug weight ratio and amount of crosslinking agent. The release rate of dexamethasone 21-acetate in the presence of collagenase was faster than that in the absence of collagenase. Anti-inflammatory effect of dexamethasone 21-acetate microspheres was more efficient than that of dexamethasone 21-acetate solution in carrageenan-induced arthritis in the rat. On the basis of the above results, we might expect the degradation and drug release rate of these microspheres to be regulated by the degree of crosslinking and the level of enzymes. In patients with severe rheumatoid arthritis who have high concentration of collagenase, more drug would be released from the microspheres. An intra-articular injection therapy of rheumatoid arthritis with desired release kinetics could be developed to enhance patient compliance and therapeutic index.
Release of 5-Fluorouracil from Ethylene-Vinyl Acetate Matrices Containing Hydrophilic Additives
Oh, Seaung-Youl ; Yoo, Young-Mee ; Kim, Sung-Soo ; Shin, Byung-Chul ; Yuk, Soon-Hong ; Lee, Hai-Bang ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 281~289
In our previous work, we have studied the effect of lactose and sodium alginate (SA) on the rate of release of 5-fluorouracil (5-FU) from ethylene-vinyl acetate (EVA) matrix. These hydrophilic additives promoted the rate of 5-FU release and the increase in rate was larger when SA was used. Both additives showed better ability to increase the rate than 5-FU itself. In this paper, we extended our study to another hydrophilic additive, Carbopol 940 (CP). Compared to SA or lactose, CP increased the rate of 5-FU release markedly. Release rate increased as the loading amount and the pH of the release medium increased. After release experiment, matrix volume increased up to 15 times of that before release experiment, depending on the amount of CP dispersed in the matrix and the pH of the release medium. On the other hand, the volume of the matrix containing lactose or SA decreased. The weight changes of the dry matrix before and after release experiment imply that CP is not released out of the matrix, to the contrary of lactose and SA. Scanning electron microscope study clearly showed that large cavities and pores are generated on the surface and the inside of the matrix. These results indicate that the mechanism by which CP increases the release rate is quite different from that of monomeric additives such as lactose or SA.
Entrapment of Plasmid DNA in Liposomes
Song, Mi-Hyang ; Lee, Mann-Hyung ; Yong, Chul-Soon ; Oh, Doo-Man ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 291~297
vector plasmid DNA with various lipid composition were prepared by the thin-film method. Size distribution, shape and the efficiency of plasmid DNA encapsulation were investigated. Effect of sonication time on the plasmid DNA entrapment in liposomes and stability at
were also examined. Sizes of neutral liposomes were about 100-200 nm and above
, and those of cationic liposomes were about 400-600 nm and above
. Shapes of liposomes entrapped plasmid DNA were spherical. Proper sonication time for better entrapment was below 15 minutes and stability at
was decreased rapidly after 1 day. Plasmid DNA entrapments of complex liposomes of various lipids were higher than those of liposomes made from one sort of lipid. Plasmid DNA entrapments of cationic liposomes were higher than those of neutral liposomes.
Controlled Release of Propranolol Hydrochloride(PPH) from PPH-Solid Dispersion System-Polyvinyl Alcohol Hydrogel Hollow Type Suppository
Chung, Jeen-Hoon ; Lee, Jeong-Yeon ; Ku, Young-Soon ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 299~308
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
and MRT of PPH powder hollow type suppository were
, 1105.26 ng/ml/min and 8.66 min, respectively. The
and MRT of PPH-EC-SDS(PPH : EC=1:3) were
, 554.69 ng/ml/min, 235.99 min, respectively.
Increase of Cellular Alkaline Phosphatase Activity by Levamisole in Kidney Cells
Hwang, Joon-Il ; Kim, Jong-Hwan ; Kim, Joo-Il ; Lee, Kyung-Tae ; Kwon, Chang-Hoo ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 309~314
The purpose of this study is to explain the relationship between the pharmacological mechanism of levamisole and the cellular activity of cellular alkaline phosphatase (ALPase) in kidney cells. The results of our investigation were as follows. 1. Cellular ALPase activity in Macacus rhesus monkey kidney cells (MA 104 cells) and primary cultured rabbit kidney proximal tubular cells treated with levamisole was increased about two or three times than control. However, 50% of ALPase activity in cultured medium was inhibited by levamisole itself. 2. The proliferation of MA 104 and cultured rabbit kidney proximal tubular cells was linearly decreased in paralleled with increase of levamisole concentration
with MTT test. 3. In the heat stability tests, the inhibition of ALPase activity with and without levamisole at
in MA 104 cells showed different
values. 4. HPLC analysis of levamisole metabolites produced by cultured MA 104 cells suggested that the formation of a metabolite, that may be associated with its increase of cellular ALPase activity. Based on these results, we assumed that the increase of cellular ALPase activity by levamisole was evoked by modification of the ALPase catalytic sites.
Iontophoresis of Insulin Through Rabbit Skin
Shin, Byung-Chul ; Oh, Seung-Youl ; Lee, Hai-Bang ; Park, Young-Do ; Lee, Kyung-Hun ;
Journal of Pharmaceutical Investigation, volume 26, issue 4, 1996, Pages 315~321
It has been indicated that problems associated with insulin iontophoresis are low bioavailability, slow absorption rate and the use of high dosage. Pretreatment of skin as a method of solving these problems was used in alloxan-induced diabetic white rabbits. Skins were treated with skin needle, electric razor, knife razor and scotch tape. Transport data shows that insulin delivery was enhanced significantly by the treatment which disrupt the barrier properties of stratum corneum. The data also shows that insulin absorption lasted for several hours after the cessation of iontophoresis. The degree of skin treatment was estimated by measuring the electrical resistance of skin. When the skins were treated with skin needle and electric razor, the standard deviations of resistance were small, which suggests the possibility of uniform delivery of insulin. The dermal responses after the invasive delivery were evaluated in accordance with OECD Guideline. It seems that electrical resistance of the skin correlate well with the dermal irritation.