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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 16, Issue 4 - Dec 1986
Volume 16, Issue 3 - Sep 1986
Volume 16, Issue 2 - Jun 1986
Volume 16, Issue 1 - Mar 1986
Selecting the target year
Pharmaceutical Study on Clonixin Argininate
Jee, Ung-Kil ; La, Sung-Bum ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 43~54
To increase the bioavailability of clonixin, clonixin argininate was prepared and compared with clonixin by determining solubility, pKa, lipid-water partition coefficient, dissolution rate and in vivo tests. The results are summerized as followings; 1) The solubility of clonixin argininate was increased by 20 times in water, about 1.2 times in pH 1.2 and pH 8.0 buffer solution, and about 1.8 times in pH 6.8 buffer solution compared with that of clonixin. 2) pKa values of clonixin, clonixin lysinate and clonixin argininate were 6.32, 7.20 and 7.45, respectively. 3) The lipid-water partition coefficient of clonixin argininate was increased more than that of the clonixin in n-hexane, carbon tetrachloride, chloroform, methylene chloride, and n-butanol, but the partition coefficient of clonixin was increased more than that of clonixin argininate in benzene/pH 1.2 buffer solution, ether/pH 8.0 buffer solution, and 3-methylbutyl acetate/pH 1.2, pH 8.0 buffer solution. 4) The time required to dissolve 60%
of clonixin argininate was about 1.5 min. in water and pH 1.2 buffer solution, and about 5 min. in pH 6.8 buffer solution.
of clonixin lysinate was about 1.5 min. in water, about 1.8 min. in pH 6.8 buffer solution, and about 8 min. in pH 1.2 buffer solution. But
of clonixin was about 96 min. in pH 6.8 buffer solution, over 2 hours in water and pH 1.2 buffer solution. 5) Anti-inflammatory effect of clonixin argininate was increased more than that of clonixin over 6 hours, and that of clonixin lysinate was followed by lapse of time. 6) Analgesic effect of clonixin argininate was increased by 1.5 times more than that of clonixin and the effect of clonixin argininate was nearly identical with that of clonixin lysinate. 7) The absorption rates (Ka) of clonixin, clonixin lysinate and clonixin argininate were
in situ, respectively.
Dissolution Enhancements of Tiaprofenic Acid by
Chun, In-Koo ; Park, In-Sook ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 55~67
Inclusion complexation of tiaprofenic acid (TPA) with cyclodextrins
in aqueous solution and in solid phase was investigated by solubility method, measurement of partition coefficient, ultra-violet, circular dichroism, infrared spectroscopies, powder X-ray diffractometry and differential scanning calorimetry. Investigations were made to prepare inclusion complexes of TPA with
in solid powdered form by coprecipitation, freeze-drying, spray-drying and co-pulverization methods. The coprecipitation, freeze-drying and spray-drying methods were successful in obtaining inclusion complexes. The results showed that the latter two methods might be originally superior to the former in obtaining powdered inclusion completes. Especially, it was shown by powder X-ray diffractometry that spray-dried
physical mixture, and spray-dried
complex were amorphous. The dissolution behaviours of
systems prepared by above four methods were compared with those of TPA alone and
physical mixture, and the rates of dissolution of TPA in pH 1.2 buffer were greatly enhanced by inclusion complexation and copulverization.
The Preparation and Evaluation of Oil in Water Microemulsion
Min, Shin-Hong ; Yang, Joong-Ik ; Kwon, Jong-Won ; Jheong, Dae-Sik ; Jheong, Yeoub ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 68~71
Oil in water microemulsion which has many pharmaceutical applications was prepared and evaluated. As oil sources and emulsifier, two grades of oil and egg phosphatide were used, respectively. Vacuum high shear mixing and high pressure homogenizing were performed and in the homogenizing step, effect of the number of passes in the homogenizer on the stability of microemulsion was studied, using Coulter counter, photographic microscope and pH-meter. From above results, it was concluded that the stability of microemulsion made of refined soy-bean oil was better than that of food grade soybean oil and by five passes in the homogenizer at 6,000 psi, we could make stable microemulsion with average particle diameter below
, with no particle above
and no significant change during 6 weeks stored.
High Performance Liquid Chromatographic Determination and Content Uniformity of Aclatonium Napadisilate Preparation
Kim, Myun-Chong ; Park, Sae-Ho ; Roh, Hwoe-Suk ; Kim, Yong-Ju ; Huh, Jae-Doo ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 72~75
A convenient high performance liquid chromatographic method was established for the quantitative determination and content uniformity test of aclatonium napadisilate preparation. This method was more simple to make the sample solution for injection, and easy to determine the content in the preparation. Aclatonium napadisilate was chromatographed using a
, and acetonitrile-water mixture (83:17) as an eluent at a flow rate of 1.8 ml/min. RI-detector response was linear over a range of
aclatonium napadisilate under above conditions. Reproducibility studies gave relative standard deviation of 1.29%.
Studies on Bioavailability of Berberine Pamoate (I)
Yang, Jae-Heon ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 76~84
Berberine is one of alkaloids extracted from Phellodendri Cortex or Coptidis Rhizoma and has extensively used as an antibacterial and antidiarrheal drug. In order to increase the bioavailability of berberine preparation, berberine pamoate was synthesized and investigated on its usage in vitro and in vivo. Berberine was more rapidly extracted from herbal plants by hot water extraction method than soxhlet extraction method. Berberine pamoate was easily synthesized from berberine hydrochloride and potassium pamoate solution and identified using the infrared spectrum. Quantitative analysis of berberine was possible in methanol solution by fluorometric determination. The dissolution rate of berberine pamoate was more decreased than that of berberine hydrochloride in simulated gastric fluid and simulated intestinal fluid. The remaining proportion of berberine pamoate in the small intestine of rat was maintained at high concentration for a long time as compared with that of berberine hydrochloride.
Studies on Effects of Antibiotics on Pyrogen Tests
Shin, Kwang-Bum ; Song, Young-Joon ; Kim, Jung-Woo ;
Journal of Pharmaceutical Investigation, volume 16, issue 2, 1986, Pages 85~88
To estimate the effect of some injectable antibiotics (ampicillin sodium, cefazolin sodium, cephaloridine, cefuroxime sodium and chloramphenicol sodium succinate) on pyrogen tests, the Limulus amebocyte lysate (LAL) test and an ultrafiltration technique were used. The rabbit pyrogen test was also used in the case of cafazolin sodium. At high antibiotic concentrations, these samples which were artificially contaminated with endotoxin inhibited the gelation reaction of LAL. But the gelation reaction occurred when most of the antibiotic was removed by ultrafiltration. Likewise, cefazolin sodium interfered not only with the LAL test but also with the rabbit pyrogen test. From these results it can be said that special modification to eliminate interference should be taken into consideration for valid method of pyrogen tests in the parenteral products containing these antibiotics.