• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.241-246
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• 2000

To develop a sustained-release preparation containing ketorolac tromethamine, two sustained-release pellet formulations were evaluated with a pharmacokinetic study as compared with a conventional commercial tablets (10 mg $Tarasyn^{TM}$, Roche Korea Ltd.). Two sustained-release formulations were as follows; formulation A was composed of an inner layer containing 75% of drug coated with $Eudragit^{TM}$ RS 100 membrane and an outer layer containing 25% of drug mixed with $Eudragit^{TM}$ NE30D, and formulation B was composed of only an inner layer containing 100% of drug coated with $Eudragit^{TM}$ RS 100 membrane. The dissolution test was performed for two formulations. In case of conventional tablets, 2.5 mg of drug per a dose was administered orally into male Albino rabbit (2.0-2.3 kg of body weight) 3 times at intervals of 4 hours. In case of two sustained formulations, 7.5 mg of drug was administered once orally. Blood samples were withdrawn periodically after the administration, and the blood concentration was determined by HPLC. The conventional tablets showed very high peak-trough fluctuation between administered doses, but two sustained formulations showed less fluctuation. Formulation A with the loading dose showed the time to reach minimum effective concentration (MEC) i.e. the onset time was less than 20 min, while Formulation B had more than 1 hr of the onset time. Formulation A had the more constant plasma level than formulation B. However, formulation B had a time lag, so the plasma level was less than MEC for an initial period of 1 hr. In formulation A, the plasma level was maintained within the therapeutic window $(0.3-5\;{\mu}g/ml)$ for a long period. Formulation A was thought to be an ideal sustained-release formulation for ketorolac tromethamine oral delivery system.

• Journal of Pharmaceutical Investigation
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• 제34권5호
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• pp.407-411
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• 2004

New formulations of amlodipine maleate tablet have been investigated to enhance the stability of the drug against light and humidity. Three kinds of amlodipine maleate tablets were prepared. One is prepared by previously known formulation (formulation C), the others were by new formulations using hydrophilic polymer $(Opadry^{\circledR})$ coated granules (formulations A and B). Amlodipine maleate powder was coated with $Opadry^{\circledR}$ to produce the coated granules and it was mixed with other excipients to produce the tabletting mass of new formulations A and B. Dissolution rate of newly formulated tablets was over 80% within 10 minutes in 0.01 M HCl medium, and its dissolution pattern was similar to that of $Norvasc^{\circledR}$ tablet. After 6 months storage under accelerated conditions, residual drug contents of tested formulations (A and B) were not significantly different from formulation C, ranging from 96.2 to 100.4%. Meanwhile, dissolution amount of formulation C was significantly reduced compared to that of formulation A (p<0.05), showing formulation A was more stable than unprotected formulation C at the accelerated conditions. Results of appearance, hardness and disintegration remained unchanged during stability study. In conclusion, it showed that the new formulations had enhanced the stability characteristics and hydrophilic coating technique was an alternative and promising method to improve the stability of amlodipine maleate tablet.

• 셀메드
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• 제10권3호
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• pp.22.1-22.7
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• 2020

Introduction: Qūbā (Tinea Corporis) is a very common disease widely prevalent worldwide. 20 - 25 % individuals suffer for this stubborn disease. Unani System of Medicine offers its treatment. There are many pharmacopoeial formulations indicated for various types of dermatophytic infections. In this study clinical efficacy and safety of the topical Unani formulation Marham Kharish Jadeed (a compound drug in the dosage form of an ointment) was assessed and compared with a standard conventional medicine. Materials and methods: A clinical study was conducted on 60 participants of qūbā randomized into test and control groups (n=30 in each group). The participants were clinically diagnosed and confirmed by microscopy of skin scrapings. The efficacy of the Unani formulation was assessed in terms of TSS score and elimination of fungal elements from the skin lesions. The data collected were analyzed statistically. Results and discussion: The study showed that the Unani formulation had comparatively better efficacy clinically than conventional medicine Terbinafine hydrochloride 1% cream in terms of reduction of itching, erythema, scaling, peripheral raised margins of the lesion comparing to baseline. In this study, 27 participants in test group and 18 participants in control group were completely cured (≥75% reduction in TSS Score with Mycological Cure) after 4 weeks of treatment. The efficacy of the Unani formulation was found significant statistically. The individual drugs of the formulations having analgesic (Musakkin), blood purifier (Muṣaffi-i-Dam), demulcent (Mulaṭṭif), antifungal (Qātil-i-fafūndῑ), detergent (Jālῑ), refrigerant (Mubarrid) and antiseptic (Dāfi'-i-'Ufūnat) properties might be responsible for the efficacy of Unani formulation. Conclusion: The findings of the study suggested that the Unani formulation was found effective and safe in the management of qūbā. No local and systemic adverse effect was reported during the study.

• Biomolecules & Therapeutics
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• 제26권2호
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• pp.218-223
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• 2018

The liver is an essential organ for the detoxification of exogenous xenobiotics, drugs and toxic substances. The incidence rate of non-alcoholic liver injury increases due to dietary habit change and drug use increase. Our previous study demonstrated that Ecklonia stolonifera (ES) formulation has hepatoprotective effect against alcohol-induced liver injury in rat and tacrine-induced hepatotoxicity in HepG2 cells. This present study was designated to elucidate hepatoprotective effects of ES formulation against carbon tetrachloride ($CCl_4$)-induced liver injury in Sprague Dawley rat. Sixty rats were randomly divided into six groups. The rats were treated orally with ES formulation and silymarin (served as positive control, only 100 mg/kg/day) at a dose of 50, 100, or 200 mg/kg/day for 21 days. Seven days after treatment, liver injury was induced by intraperitoneal injection of $CCl_4$ (1.5 ml/kg, twice a week for 14 days). The administration of $CCl_4$ exhibited significant elevation of hepatic enzymes (like AST and ALT), and decrease of antioxidant related enzymes (superoxide dismutase, glutathione peroxidase and catalase) and glutathione. Then, it leaded to DNA damages (8-oxo-2'-deoxyguanosine) and lipid peroxidation (malondialdehyde). Administration of ES formulation inhibited imbalance of above factors compared to $CCl_4$ induced rat in a dose dependent manner. Real time PCR analysis indicates that CYP2E1 was upregulated in $CCl_4$ induced rat. However, increased gene expression was compromised by ES formulation treatment. These findings suggests that ES formulation could protect hepatotoxicity caused by $CCl_4$ via two pathways: elevation of antioxidant enzymes and normalization of CYP2E1 enzyme.

• Journal of Microbiology and Biotechnology
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• 제32권2호
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• pp.160-169
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• 2022

In the present study we evaluated the efficacy of a bioformulation of Streptomyces cameroonensis for control of black pod disease in cocoa and enhancement of seedling growth. The formulation developed using talc powder and cassava starch as carriers showed high shelf-life of 1.07 × 10⁶ CFU/g after six months storage at 4℃. The formulation was tested for inhibition of spore germination in Phytophthora megakarya and showed 100% inhibition at 10% (w/v) of formulation. To determine the efficacy of the formulation, we performed an in planta assay in the greenhouse on two hybrids of cocoa seedlings, the tolerant SNK413 × (♂) T79/467 and the susceptible UPA 134× (♂) SCA 12. Detached leaf assay showed a significant reduction in the disease severity index of about 67% for the tolerant hybrid and 55% for the susceptible hybrid compared to non-treated plants. A significant enhancement in stem length, leaf surface area and root weight was observed. Analysis of biochemical markers of defense showed a significant increase in total polyphenol, flavonoid, and total protein contents. There was also significant upregulation of PR-proteins such as chitinases, peroxidases and β-1, 3-glucanases following treatment of both tolerant and susceptible hybrids, though with a higher level of synthesis in the tolerant hybrids. A significant increase was also observed in polyphenol oxidase activities in plants treated with the formulation. This work demonstrated the stability and effectiveness of the S. cameroonensis powder formulation in suppressing black pod disease in cocoa and subsequently enhancing the growth of seedlings.

• Composites Research
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• 제35권3호
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• pp.182-187
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• 2022

본 논문은 다층 PCB에 사용되는 프리프레그의 물성을 파악하여 제시한 두께 실험식을 통해 PCB의 두께를 예측하기 위한 연구를 수행하였다. 프리프레그는 물성과 동박 잔존율에 의해서 PCB 제작시 두께가 감소하기 때문에 두께 실험식을 통한 정확한 PCB의 두께 예측이 필요하다. 두께 실험식에 사용되는 프리프레그의 밀도를 파악하기 위해 질량 및 두께를 측정하여 밀도를 도출하였다. 이후 CCL을 제작하기 위해 프리프레그와 동박을 적층하여 핫 프레스기를 사용하였고 광학현미경과 마이크로미터를 사용하여 두께를 측정하였다. 또한 동박 잔존율에 따른 두께 변화를 측정하기 위해 회로밀도를 다르게 구성하여 8층 PCB를 설계하였고 두께 측정 결과와 두께 실험식으로 도출된 두께를 비교하여 두께 실험식을 검증하였다. 비교 결과 CCL의 경우 2.56%, 다층 PCB의 경우 4.48%의 오차를 보였고 이를 통해 두께실험식의 신뢰성을 확인하였다.

• 대한본초학회지
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• 제33권5호
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• pp.67-72
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• 2018

Objectives : Natural extracts have been extensively studied to replace single agent drugs that cause a variety of side effects. However, studies of changes to the formulation of natural extracts has not been nearly proceed. We aimed to investigate whether pharmacological stability of hyeonggaeyeongyotang gagambang (HYT) is altered by formulation changes for foaming tablet. Methods : In this study, we performed freeze - drying of HYT, which is known to have antioxidant and anti - inflammatory properties, and then changed the formulation by foaming. Results : As a result, the foaming reaction appeared normally when HYT foamed tablets were put into water, and almost all of the substances were dissolved in the aqueous solution. In addition, we confirmed using high-performance liquid chromatograph that the geniposide used as an indicator material of HYT was stable in most of the formulations. It was confirmed that the change of HYT formulation did not affect the antioxidant efficacy by the 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid assay. Moreover, quantitative real-time PCR confirmed that the inhibitory effect of HYT on IL-$1{\beta}$ mRNA expression induced by lipopolysaccharides treatment in murine macrophage RAW 264.7 cells was similar in the solution of foaming tablet. Conclusions : These results suggest that the materials with various pharmacological effects can be stably maintained even when the formulation is changed by the foaming action of HYT. Our results are expected to provide important basic knowledge on formulation changes using various natural extracts.

• 한국환경농학회지
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• 제11권1호
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• pp.1-8
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• 1992

농약분해에 관여하는 monooxygenase와 esterase의 활성을 저해하는 것으로 알려진 PBO와 TPP를 첨가하여 제조한 신(新)다이아지논입제에 대하여 벼멸구에 대한 살충률을 조사하였고, 아울러 신(新)다이아지논 입제와 두효소를 저해하는 작용기작을 가지고 있는 tricyclazole, carbofuran 그리고 EPN을 혼합하여 제조한 혼합다이아지논입제에 대하여 담수토양중의 잔류경향을 조사하였다. 1. 살균토양과 비살균토양에서 신(新)다이아지논 입제(0.1% 첨가)의 반감기는 4.53일과 2.33일 이었고, 시판품에 비하여 각각 0.74일과 0.45일 주성분의 분해가 지연되었다. 2. 신(新)다이아지논입제(0.1% 첨가)의 벼멸구에 대한 살충률은 추천량에서는 12%, 추천 1/2량에서는 $30{\sim}60%$가 증가되었다. 3. 신(新)다이아지논 입제 (1%)중 PBO 첨가는 토양중 반감기가 0.44일 그리고 PBO-TPP첨가로 0.65일 지연되었다. 4. 혼합다이아지논 입제는 시판품에 비하여 tricyclazole, carbofuran 그리고 EPN첨가로 반감기가 2.61일, 1.04일 그리고 0.43일 지연되었으며, EPN+carbofuran을 첨가하여 제조한 혼합다이아지논 입제는 2.7일 연장되었다.

• Asian-Australasian Journal of Animal Sciences
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• 제29권11호
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• pp.1616-1624
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• 2016

The aim of present experiment was to investigate the effect of protein reduction in commercial broiler chicken rations with incorporation of de-oiled rice bran (DORB) and supplementation of limiting amino acids (valine, isoleucine, and/or tryptophan) with ration formulation either on total amino acid (TAA) or standardized ileal digestible amino acids (SIDAA). The experimental design consisted of $T_1$, TAA control; $T_2$ and $T_3$, 0.75% and 1.5% protein reduction by 3% and 6% DORB incorporation, respectively by replacing soybean meal with supplemental limiting amino acids to meet TAA requirement; $T_4$, SIDAA control, $T_5$ and $T_6$, 0.75% and 1.5% protein reduction by DORB incorporation (3% and 6%) with supplemental limiting amino acids on SIDAA basis. A total of 360 dold fast growing broiler chicks (Vencobb-400) were divided into 36 homogenous groups of ten chicks each, and six dietary treatments described were allocated randomly with six replications. During 42 days trial, the feed intake was significantly (p<0.05) reduced by TAA factor compared to SIDAA factor and protein factor significantly (p<0.05) reduced the feed intake at 1.5% reduction compared to normal protein group. This was observed only during pre-starter phase but not thereafter. The cumulative body weight gain (BWG) was significantly (p<0.05) reduced in TAA formulations with protein step-down of 1.5% ($T_3$, 1,993 g) compared to control ($T_1$, 2,067 g), while under SIDAA formulations, BWG was not affected with protein reduction of 1.5% ($T_6$, 2,076 g) compared to $T_4$ (2,129 g). The feed conversion ratio (FCR) was significantly (p<0.05) reduced in both TAA and SIDAA formulations with 1.5% protein step-down ($T_3$, 1.741; $T_6$, 1.704) compared to respective controls ($T_1$, 1.696; $T_4$, 1.663). The SIDAA formulation revealed significantly (p<0.05) higher BWG (2,095 g) and better FCR (1.684) compared to TAA formulation (2,028 g; 1.721). Intake of crude protein and all limiting amino acids (SID basis) was higher in SIDAA group than TAA group with resultant higher nitrogen retention (4.438 vs 4.027 g/bird/d). The nitrogen excretion was minimized with 1.5% protein reduction (1.608 g/bird) compared to normal protein group (1.794 g/bird). The serum uric acid concentration was significantly reduced in $T_3$ (9.45 mg/dL) as compared to $T_4$ (10.75 mg/dL). All carcass parameters were significantly (p<0.05) higher in SIDAA formulation over TAA formulation and 1.5% protein reduction significantly reduced carcass, breast and thigh yields. In conclusion, the dietary protein can be reduced by 0.75% with TAA formulation and 1.5% with SIDAA formulation through DORB incorporation and supplementation of limiting amino acids and among formulations, SIDAA formulation was better than TAA formulation.

• The Plant Pathology Journal
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• 제22권3호
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• pp.303-308
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• 2006

Ethaboxam is a fungicide controlling plant diseases caused by Oomycetes. Efforts were made to improve its fungicidal activity applying formulation technology. Fungicidal activity of ethaboxam against cucumber downy mildew caused by Pseudoperonospora cubensis was improved by incorporating polyoxyethylene cetyl ether (PCE) in a wettable powder formulation. It was found that the optimum combination ratio of PCE and ethaboxam was 3:1, and a tank-mix of $150{\mu}g/ml$ of ethaboxam and $450{\mu}g/ml$ of PCE would be as good as the standard 25 % WP formulation diluted to $250{\mu}g/ml$ ethaboxam without PCE in controlling cucumber downy mildew. Based on this results, a wettable powder (WP) co-formulation containing 15% of ethaboxam and 45% of PCE was developed in this study, and tested for its performance in the fields. This co-formulation showed significant improvement in persistence of fungicidal activity and curative efficacy of ethaboxam against cucumber downy mildew. The improved control efficacy was also confirmed for control of grape downy mildew caused by Plasmopara viticola and potato late blight caused by Phytophthora infestans in the field tests.