• Archives of Pharmacal Research
• /
• v.29 no.11
• /
• pp.1055-1060
• /
• 2006

The objective of this study was to formulate itraconazole semisolid dosage forms and characterize their physicochemical properties. Itraconazole and excipients such as polysorbate 80, fatty acids, fatty alcohols, oils and organic acids were melted at $160^{\circ}C$. The fused solution was then cooled immediately at $-10^{\circ}C$ to make wax-like semisolid preparations. Their physicochemical attributes were first characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy and nuclear magnetic resonance spectrometry. The solubility of itraconazole in semisolid preparations and their dispersability in the simulated gastric fluid were also determined. Our semisolid preparations did not show any distinct endothermic peak of a crystalline form of itraconazole around $160-163^{\circ}C$. This suggested that it was changed into amorphous one, when it was formulated into semisolid preparations. In addition, the distinctive functional peaks and chemical shifts of itraconazole were well retained after processing into semisolid preparations. It could be inferred from the data that itraconazole was stable during incorporation into semisolid preparations by the hot melt technique. In particular, itraconazole semisolid preparations composed of polysorbate 80, fatty acids and organic acids showed good solubility and dissolution when dispersed in an aqueous medium. It was anticipated that the semisolid dosage forms would be industrially applicable to improving the bioavailability of poorly water-soluble drugs.

• Korean Journal of Clinical Pharmacy
• /
• v.21 no.4
• /
• pp.347-352
• /
• 2011

Health insurance review & Assessment service (HIRA) has enforced cutting the drug costs when physicians prescribe split extended release drugs, starting from December, 2010. The objective of this study is to analyze extended release and enteric coated drugs on pharmaceutical reimbursement list in Korea, and to investigate the impact and barriers of the health insurance review on splitting extended-release formulation drugs. By using the ingredient code, extended release and enteric coated formulations make up 7.8% of all drugs in April, 2011. The most frequently used drugs are agent affecting circulatory and digestive system. From the extended release and enteric coated formulations (n=112), 34.8% (n=39) were not available in other dosage forms. According to questionnaire survey for 169 pharmacists (response rate: 73.8%), the rate of splitting and crushing of extended release and enteric coated drugs decreased. When pharmacists correct physician's prescription errors, the biggest problem was lack of other dosage forms. So it is necessary to develop variety of other dosage forms, and computerized checking system for splitting extended-release drugs. It is also important to inform physicians and patients in regard to the problems of split prescription of extended release and enteric coated drugs.

• Journal of the Korean Chemical Society
• /
• v.55 no.4
• /
• pp.620-625
• /
• 2011

A simple, rapid potentiometric back titration of Isoniazid (INH) in the presence of Rifampicin (RIF) in tablets and syrups is described. The method is based on the oxidation of INH by a known excess of copper (II) ion and the back titration of unreacted copper (II) ion potentiometrically with ascorbic acid using a lab-made Copper Based Mercury Film Electrode (CBMFE). The titration conditions have been optimized for the determination of 1.0-10.0 mg of INH in pure and dosage forms. The precision and accuracy of the method have been assessed by the application of lack-of-fit test and other statistical methods. Interference was not caused by RIF and other excipients present in dosage forms. Application of the method for INH assay in tablets and syrups was validated by comparison of the results of proposed method with that of the British Pharmacopoeia (BP) method using F- and t- statistical tests of significance.

• Journal of Pharmaceutical Investigation
• /
• v.37 no.6
• /
• pp.403-411
• /
• 2007

The importance of pharmaceutical additives is increasing and the sorts and application categories are being classified in detail. International pharmaceutical council based on IPEC-America, IPEC-Europe and JPEC was established for specifications, safety and efficacy, approval regulations of pharmaceutical additives in 1992. Therefore, scrutinized examination of pharmaceutical additives used for already approved domestic drug was performed under the supervision of KFDA and nomenclature on application categories of pharmaceutical additives was summarized and endowed their glossary. Additionally, the boundaries of pharmaceutical additives according to the dosage forms based on the principle of the dosage forms of Korean pharmacopoeia were classified. These informations could be available for standards & experimental methods, approval, evaluation, audit of drug and contribution for national welfare.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
• /
• v.21 no.2
• /
• pp.120-125
• /
• 2008

Objectives : Medication is important in treatment for children, but prescribing traditional herbal medicine for them is very difficult. The aim of this study was to evaluate the preference for new and traditional dosage form of Onchung-eum. Methods : A total of 24 children who visited Oriental Medical Center of Daegu Hanny University during one month since March 2008 were included in this study. They compared new dosage form of Onchung-eum with traditional thing and evaluated items such as taste, perfume, color, sensation of chewing and texture. Results : As a whole they prefered new dosage form more than traditional thing in a sensory test. And 13(54%) children choose new dosage form as the better one. Conclusions : Considering the above results, the new dosage form might be efficacious to be taken by children. Further studies in other methods and new dosage forms are needed to make prescribing it for children easily.

• Journal of Pharmaceutical Investigation
• /
• v.18 no.3
• /
• pp.147-155
• /
• 1988

• Journal of Pharmaceutical Investigation
• /
• v.26 no.2
• /
• pp.119-124
• /
• 1996

To develop oral controlled release dosage forms, ionic interactions between polymers and drugs were evaluated. Hydroxypropylmethyl cellulose and carboxymethylene were used as model nonionic and ionic polymers, respectively. 5-fluorouracil, propranolol-HCl and sodium salicylate were selected as model nonionic, cationic and anionic, respectively. Polymer-drug mixtures were compressed into tablets and drug release kinetics from these tablets were determined. Drug release from the tablets made of the nonionic polymer was not affected by the charge of drugs, rather, was regulated by the solubility of drugs in different pH releasing media. However, drug release kinetics were significantly affected when drug-polymer ionic interactions exist. Enhanced drug release was observed from anionic drug-anionic polymer tablets due to ionic repulsion, whereas drug release was retarded in cationic drug-anionic polymer tablets owing to ionic attractive force. Therefore, the results suggested that the polymer-drug interactions are important factors in designing controlled release dosage forms.

• Analytical Science and Technology
• /
• v.34 no.2
• /
• pp.46-55
• /
• 2021

Evaluation of drug-excipient compatibility is one of the basic steps in the preformulation of pharmaceutical dosage forms. Some reactive excipients have been known so far which may cause stability problems for drug molecules in pharmaceutical dosage forms. The aim of this study was to evaluate drugexcipient compatibility of gliclazide with some common pharmaceutical excipients, known for their ability to incorporate in drug-excipient interactions. Binary mixtures were prepared using lactose, magnesium stearate, polyvinylpyrrolidone, sodium starch glycolate, polyethylene glycol 2000 and dicalcium phosphate. Based on the results; gliclazide was incompatible with all tested excipients; but not with dicalcium phosphate. DSC (Differential Scanning Calorimetry) results were in accordance with HPLC (High Pressure liquid chromatography) data and were more predictive than FTIR (Fourier Transform Infrared Spectroscopy). Drug and reactive excipients incompatibility was fully discussed and documented. It is advisable to avoid incompatible excipients or carefully monitor the drug stability when incorporating such excipients in final formulation designs.

• Proceedings of the PSK Conference
• /
• 2000.04a
• /
• pp.202.3-203
• /
• 2000

• Journal of Pharmaceutical Investigation
• /
• v.27 no.4
• /
• pp.295-301
• /
• 1997

Nitrendipine, a slightly soluble calcium channel blocking agent forms a solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$, which exhibits better dissolution characteristics than the uncomplexed drug. The dissolution rate of nitrendipine was markedly increased in solid dispersion system in pharmacopeial disintegration media at pH 1.2 and pH 6.8. Four different dosage forms of nitrendipine were administered to rats: (a) nitrendipine in the solution of PEG 400; (b) nitrendipine solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 by solvent evaporation method and administered in capsule form; (c) physical mixture of nitrendipine with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 and administered in capsule form; (d) nitrendipine alone administered in capsule form. Relative bioavailability after the oral administration of various dosage forms to rats with a dose of 10 mg/kg equivalent to nitrendipine was compared with that of nitrendipine in the solution of PEG 400. The AUC of solid dispersion was significantly bigger than that of nitrendipine powder. $T_{max}$ of solid dispersion was significantly shorter and $C_{max}$ was higher than that of nitrendipine powder. These results indicate that the bioavailability of nitrendipine could be improved markedly by inclusion complexation. An interesting correlation also appears to exist between the in vitro dissolution data and the area under the plasma concentration-time curves.