• Journal of Pharmaceutical Investigation
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• 제20권1호
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• pp.7-12
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• 1990

In case of the slowly disintegrating tablets such as enzyme preparations, disintegration time (DT) may be the important factor in formulating those preparations. The effects of tablet hardness, lubricants and disintegrants on DT were investigated in this approach. Disintegration time was significantly affected by disintegrants, moderately by lubricants, but not by tablet hardness. The effect was in the order of magnesium stearate >talc, PEG, sodium benzoate in case of lubricants, and of Ac-Di-Sol>LHPC>Primogel >Kollidon in case of disintegrants. Because lubricants and disintegrants influenced the tablet hardness and DT profile showed complicated pattern, it should be remembered that all factors mentioned above should be simultaneously considered in the formulation of enzyme tablets.

• 분석과학
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• 제34권2호
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• pp.46-55
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• 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.

• 보존과학회지
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• 제35권4호
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• pp.269-277
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• 2019

Seaweed extracts, namely carrageenan obtained from Grateloupia elliptica and algin obtained from Laminaria, were employed as adhesive agents to synthesize solid adhesives for paper. Carrageenan from Grateloupia elliptica with the highest adhesive strength and lgin from Laminaria with the highest compressive strength was selected. The selected carrageenan and algin were mixed in a ratio of 7:3, and the mixture was employed as an adhesive agent. At a high temperature, sodium stearate(used as a solidifying material) oxidized the seaweed extracts. Consequently, carrageenan and algin were added to the final manufacturing process. The adhesive strength of the final synthesized solid adhesive is found to be 3.02 MPa and the compressive strength is found to be 30.5 N. Compared to the adhesive strength (2.95 MPa) and compressive strength (30.11 N) of commercial solid adhesives, the obtained results indicate superior adhesion characteristics. Furthermore, the proposed adhesive is environment-friendly because the presence of volatile organic compounds, formaldehyde, and heavy metals(such as chromium, lead, and cadmium) were not detected. Moreover, when used, the flatness of paper was twice that of commercial solid paper adhesives. Hence, the proposed adhesive can provide excellent adhesion, stability, and usability.

• Journal of Advanced Marine Engineering and Technology
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• 제7권2호
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• pp.15-21
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• 1983

Preparing for treatment and management of the emulsified fuel oil which will be generalized henceforth, this paper is an attempt to examine the viscosity-temperature characteristics of emulsified heavy fuel oil which is mixed with water and emulsifier in various mixture ratio by mechanical mixer. The experimental results are summarized as follows: 1. The viscosity-temperature characteristics of the emulsified C & B grade heavy fuel oil mixed with water of same or less weight, is changed according to log.log(v+0.6)=b-3.8log T. 2. The emulsifier has to be added to the emulsified A grade heavy fuel oil mixed with water of same or less weight, because it is instable. Especially if the emulsifier is sodium stearate, it is added more than 0.3% of the weight of oil and water. 3. In the emulsified A grade heavy fuel oil mixed with water and emulsifier, the higher the ratio of water addition becomes, the higher the viscosity is and the more the viscosity-temperature slope decreases. But the higher the ratio of emulsifier addition is, the more the viscosity-temperature slope increases. In this case, the linearity of viscosity-temperature characteristic curve is poorer than that of B and C grade heavy fuel oil. 4. In the emulsified A grade heavy fuel oil mixed with emulsifier of 0.3% or less, the emulsion type is O/W type when water addition ratio is 40%, but it is W/O type when it is 10%, 20%, 30% and 50%.

• Journal of Pharmaceutical Investigation
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• 제29권3호
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• pp.227-234
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• 1999

Solid dispersions were prepared to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) using water-soluble carriers such as povidone, copolyvidone, $2-hydroxypropyl-{\beta}-cyclodextrin (HPCD)$, sodium salicylate or sodium benzoate by solvent evaporation method. Solid dispersions were characterized by infrared spectrometry, differential scanning calorimetry (DSC) and powder X-ray diffractometry, dissolution and permeation studies. DDB tablets (7.5 mg) were prepared by compressing the powder mixtures composed of solid dispersions, lactose, com starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were also prepared by filling the mixtures in empty hard gelatin capsules (size No.1). From the DSC and powder x-ray diffractometric studies, it was found that DDB was amorphous in the HPCD or copolyvidone solid dispersions. Dissolution rates after 10 min of DDB alone and solid dispersions (1 : 10) in sodium benzoate, sodium salicylate and copolyvidone were 11.8, 23.5, 22.8 and 82.5%, respectively. Dissolution rates of DDB after 30 min from 1 : 10 and 1 : 20 copolyvidone solid dispersions were 80.5 and 95.0%, respectively. For the DDB tablets prepared using solid dispersions (1 : 20), the initial dissolution rate was dependent on carrier material, and was ranked in order, $Kollidon\;30\;{\ll}$ copolyvidone < HPCD. For the HPCD solid dispersion tablets, dissolution rate reached 97.4% after 15 min, but thereafter slowly decreased to 80.7% after 2 hr due to the precipitation of DDB. However, in the case of copolyvidone solid dispersion tablets, dissolution increased linearly and reached 93.4% after 2 hr. Reducing the volume of test medium from 900 to 300 ml markedly decreased the dissolution rate of the tablets containing 1 : 20 HPCD solid dispersions and 1 : 10 copolyvidone solid dispersion. For 1 : 20 copolyvidone solid dispersion tablets, there was no significant change in dissolution rate up to 1 hr with different volumes of test medium. Preparation of the copolyvidone solid dispersion (1 : 20) in capsules markedly delayed the dissolution (31.2 % after 2hr) due to the limited diffusion within capsules. The permeation rate $(13.4\;g/cm^2\;after\;8\;hr)$ of DDB through rabbit duodenal mucosa from copolyvidone solid dispersion (1 : 10) was markedly enhanced, when compared with drug alone or physical mixtures. From overall findings, DDB formulations containing copolyvidone solid dispersions (1 : 20) could be used to remarkably improve the dissolution rate in dosage form of powders and tablets.

• 약학회지
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• 제41권3호
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• pp.305-311
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• 1997

Sustained release-microspheres and immediate release-pellets were prepared to develop a controlled release multiparticulate system containing both water soluble and insoluble dr ug. Pseudoephedrin.HCl (EPD) and terfenadine (TRF) were used as model drugs, respectively. Sustained release-EPD microspheres were prepared by solvent evaporation method using Eudragit RL or RS as a matrix combined with pH-insensitive film coating. Smaller EPD microspheres were obtained when smaller amount of Eudragit as a matrix material or larger amount of magnesium stearate as a dispersing agent was used. However the obtained microspheres did not show syfficient sustained release characteristics. About 97% of EPD was released after 1 hr irrespective of matrix material used. Subsequent coating of the microspheres with pH-insensitive polymer such as Eudragit RS or ethylcelulose (EC) resulted good sustained in 37.5, 73.3 and 92.0% release of encapsulated EPD in distilled water after 1, 3 abd 7 hr, respectively. It corresponds to mean dissolution time (MDT) of 2.3 hr, which is much larger than that of un-coated EPD microspheres (0.0048 hr). Immediate release TRF pellets were prepared by spherically agglomerated crystallization using Eudragit E as an inert matrix and methylene chloride as a liquid binder. Using Eudragit E alone as a matrix resulted in satisfactory physical properties of the pellets such as sphericity, surface texture and flowability, but led to slower release of TRF from pellets than un-modified TRF powder (MDT of 1.70 vs 1.43 hr in pH 1.2 dissolution medium). Introducing propylene glycol or sodium lauryl sulfate as an emulsifier brought about faster release of TRF from pellets (MDT of 1.14 and 0.95 hr, respectively). In conclusion, microencapsulation by solvent evaporation combined with film coating and spherically agglomerated crystallization were successfully utilized to prepare controlled release multiparticulate system composed of sustained release EPD-microspheres and immediate release TRF pellets.

• 한국산학기술학회논문지
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• 제22권3호
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• pp.323-332
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• 2021

본 연구의 목적은 배뇨장애 치료를 위한 실로도신과 솔리페나신 숙신산염을 함유한 새로운 복합 정제를 개발하는 것이다. 이러한 목표를 달성하기 위하여 실로도신과 솔리페나신 숙신산염의 동시 정량법을 확립하였다. 두 약물은 다양한 완충액에서 1 mg/ml 이상의 수용해도 값을 나타내었으며, 실로도신과 솔리페나신 숙신산염이 함유된 시판제품의 용출은 다양한 용출조건에서 30분 이내에 완료되었다. 시차 주사 열량계를 사용하여 부형제와 약물 간 상호 반응성을 확인하여 선정된, 약물과 반응성이 없는 부형제를 사용하여 습식 과립화 방법을 사용하여 결합제와 붕해제의 사용에 따른 다양한 처방을 제조한 후 용출시험을 진행하였다. 제조한 정제의 처방 중 실로도신, 솔리페나신 숙신산염, 유당, 미결정셀룰로오스 PH101, 소듐라우릴설페이트, 포비돈 K-30, 크로스포비돈 및 스테아린산마그네슘이 8/10/56/112/2/6/6/2(w/w)의 비율로 제조된 정제는 트루패스정(실로도신 시판 제품) 및 베시케어정(솔리페나신 숙신산염 시판 제품)과의 비교용출 시험시 동등성을 나타내는 것을 확인하였다. 따라서, 본 연구를 통해 얻어진 복합 정제는 각 약물의 시판 제품과 동등한 생체이용률을 나타낼 수 있을 것으로 판단되며, 향후 배뇨 장애 치료에 복약순응도가 우수한 의약품으로 활용될 수 있을 것으로 사료된다.

• 대한본초학회지
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• 제33권2호
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• pp.9-18
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• 2018

Objectives : Hwangryunhaedok-tang (HRHDT) is one of the well-known prescription herbal drugs of Korean herbal medicine, which has been widely used for the treatment of various bacterial and inflammatory diseases. This study was conducted in order to develop the tablet formulations of HRHDT and compare its efficacy with the other commercial formulations. Methods : Corresponding herbal medicines comprising of HRHDT were extracted with water for 3 hr at $95{\sim}100^{\circ}C$ and then vacuum dried. Subsequently, some pharmaceutical excipients such as microcrystalline cellulose, croscarmellose sodium, magnesium stearate, etc were used to prepare the HRHDT tablets. The contents with characterizing components of HRHDT tablet was compared with the HRHDT decoction. The contents of characterizing components were analyzed with HPLC. Furthermore, we investigated the anti-inflammatory and anti-oxidative abilities of two different commercial HRHDT granules (HJP-1 and HJP-2) and were compared with that of the formulated HRHDT tablets. The anti-oxidant properties of HRHDR were studied using the 1,1-diphenyl-2-picryhydrazyl (DPPH) radical, contents of total flavonoid and polyphenol. In addition, based on this result the anti-inflammatory effects have verified by mechanism from LPS- treated Raw264.7 macrophages. Results : The results demonstrated that HRHDT tablets showed more anti-inflammatory and anti-oxidative effects than HJP-1, HJP-2. Moreover, it showed more superior effects in terms of dose, usability and stability than the granules. Conclusion : Hence, we concluded that in order to improve the quality and efficacy of the Korean herbal medicine, it is necessary to develop appropriate methods and establish standardized techniques for the development of good formulations.