• Title/Summary/Keyword: new dosage form

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Pharmaceutical Formulation and Evaluation of Sustained - Release Hydrophilic Matrix Tablet of Cefatrizine Propyleneglycol Using Polyethylene Oxide (폴리에틸렌옥사이드를 이용한 세파트리진프로필렌글리콜 서방성매트릭스 정제의 제조 및 평가)

  • Lee, Eon-Hyoung;Park, Sun-Young;Jee, Ung-Kil;Kim, Dong-Chool
    • Journal of Pharmaceutical Investigation
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    • v.31 no.1
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    • pp.37-41
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    • 2001
  • Various characteristics of polyethylene oxide (PEO) are useful for drug delivery systems. In this study, PEO was used as a sustained release matrix system containing cefatrizine propyleneglycol (Cefa-PG) which is a new semi-synthetic broad-spectrum and orally active cephalosporin. Five kinds of sustained release matrix tablets were formulated with various content of PEO and other ingredients. And three types of matrix tablets were formulated of which compositions were the same but the hardness was different. It was found that PEO content influenced drug release rate. Increasing PEO content, the drug release rate from matrix tablets was decreased. In addition, Avicel, one of the ingredients of matrix components, changed the drug release from the sustained release PEO matrix tablets. With increasing Avicel content, the rate of drug release was increased. For the effect of hardness of matrix tablets, the rate of drug release is decreased with increasing hardness. In comparison of bioavailability parameters after oral administration of Cefa-PG PEO matrix tablets and general Cefa-PG capsule in beagle dog, the sustained release PEO matrix tablets is more useful than a general dosage form. $AUC^{0-12}$ of the sustained release PEO matrix tablet and the general dosage form was 1.16 and 0.644 respectively.

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The Survey on the Preferences for the New Child Dosage Forms of Oriental Herbal Medicine (신제형의 소아 약물 순응도 조사;기존의 제재와 비교하여 복용의 간편성, 맛의 개선도, 운반 및 저장의 편의성 포함)

  • Seo, Jung-Min;Yun, Hye-Jin;Kim, Sang-Chan;Hwang, Sun-Yi;Jee, Seon-Young;Cho, Dong-Hee;Son, Ji-Young;Baek, Jung-Han
    • The Journal of Pediatrics of Korean Medicine
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    • v.21 no.3
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    • pp.11-19
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    • 2007
  • Objective Medication is one the most important things in treatment for children, but prescribing traditional herbal medicine for them is very difficult. Therefore, we made 4 new forms of oriental herbal medicine that has a better taste, smell, and color. These new forms also have a texture that make medicine easier to chew. Methods We made up a question of 20 children visiting $\bigcirc\;\bigcirc$ university hospital. Results and Conclusions 1. Children preferred liquid or pill type of herbal medicine. 2. The preference sensory test of the traditional medicine and new form of medicine had not much difference. 3. On the test for preferences, it resulted as they liked the 4th form of new medicine which was with little bit more of sweet and sour taste, and the 3rdformwithnewcolors. 4. They hated traditional herbal medicine of the taste, smell, color, sensation of texture of material.

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Development of Pharmaceutical Dosage Form with New Sibutramine Salt (시부트라민 신규염을 이용한 새로운 시부트라민 제제의 개발)

  • Moon, Jin-Wook;Shin, Teak-Hwan;Lee, Dong-Wook;Cho, Jun-Young;Chang, Sung-Ju;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.40 no.1
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    • pp.15-21
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    • 2010
  • Sibutramine is an orally administered centrally-acting antiobesity agent and inhibits both noradrenaline(norephinephirine) and serotonin(5-HT) reuptake. These effects are contributed by its active metabolites, M1 and M2. However, as the free base form of sibutramine is an oil form in room temperature, it had the problem of handling and stability. Thus, this drug should be used in the form of acid salt form in the pharmaceutical application. Unfortunately, anhydrous sibutramine hydrochloride is highly hygroscopic and unstable. In order to solve the hygroscopicity of the anhydrous salt form, another sibutramine acid salt form must be developed as a hydrate form. In this study. to overcome these problems, various of sibutramine acid salt forms were prepared with the pharmaceutically available salts such as maleate, esylate, mandelate, camsylate, besylate, salicylate, tartrate, isethionate and malate forms, and their physicochemical properties were investigated. Sibutramine malate was selected for excellent solubility and stability among the listed salt forms above. Its pharmacokinetic parameters were evaluated in rats comparing with sibutramine HCl, resulting in similar parameters. In vitro dissolution study of sibutramine malate-loaded capsule was performed comparison with commercial product ($Reductil^{(R)}$) in pH 1.2, pH 4.0, pH 6.8 and water medium. Our results indicated that there were no significant differences in their dissolution profiles were similar in all tested medium. Thus, sibutramine malate-loaded capsule should be a potential candiate due to its excellent solubility, good stability and biosimilar absorption.

Solid Dispersion of an HIV Protease Inhibitor

  • Park, Jae-Hyeon;Lee, Sung-Hack;Lee, Yong-Hee;Kim, Ae-Ri
    • Journal of Pharmaceutical Investigation
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    • v.41 no.2
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    • pp.75-82
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    • 2011
  • LB71350 is an HIV protease inhibitor with poor aqueous solubility and extensive first pass effect. The purpose of the present study was to test the feasibility of solid dosage form of LB71350 with improved bioavailability utilizing solid dispersion. Three different compositions with varying ratio of (LB71350: Gelucire 44/14: Tween 20) were studied. Capsule filling of these solid dispersion compositions was tested using a semi-automatic capsule filling system. Oral bioavailability in dog was tested. Chemical and physical stability at 4, 25 and $40^{\circ}C$ was monitored by HPLC assay, dissolution test, powder XRD and microscopy. The capsule filling system yielded uniform products of drug loading up to 10%. Oral bioavailability in dog was improved compared to the aqueous suspension of crystalline LB71350. Capsules were chemically stable for up to 6 months at $40^{\circ}C$. However, there were temperature and composition dependent physical changes. Decrease in dissolution rates after storage at $40^{\circ}C$ was due to the polymorphic change. In conclusion, manufacturing process, bioavailability, and physico-chemical stability have been considered to propose a solid dispersion capsule formulation for the HIV protease inhibitor with poor physico-chemical properties. A new less soluble crystalline form identified during the physical stability test warrants further study.

Anti-inflammatory and Analgesic Activities, and Plasma Concentration of Loxoprofen Sodium Plasters (Loxoprofen sodium 플라스타의 소염, 진통 작용 및 혈중 약물 농도에 대한 연구)

  • 채주병;전홍렬;이승목;정남주;김수균;조길도;김동연
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.198-203
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    • 1999
  • Loxoprofen-Na (sodium 2-〔4-(2-oxocyclopentylmethyl)pheny)propionate dihydrate) is a potent analgesic drug. We developed loxoprofen-Na plasters to extend duration time of analgesic activity and to reduce side effect on gastrointestinal tract. Analgesic effect of Loxoprofen-Na plasters was investigated. Loxoprofen-Na plaster had good analgesic effect in rat paw pressure test, Tail-flick latency test and acetic acid-induced writhing test. Also, it had anti-inflammatory effect on carrageenan-induced rat hind paw edema. In pharmacokinetic study of Loxoprofen-Na, plasters dosage form showed that plasma drug concentration was prolonged up to 14 hours. So, we can conclude that loxoprofen-Na plasters, when applied on skin, will be a new type of drug for controlling the various local pain or inflammation.

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Development of Vaccine Delivery System and Challenges (백신 전달기술 개발 동향과 과제)

  • Jung, Hyung-Il;Kim, Jung-Dong;Kim, Mi-Roo;Dangol, Manita
    • KSBB Journal
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    • v.25 no.6
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    • pp.497-506
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    • 2010
  • Vaccine is a protective clinical measure capable of persuading immune system against infectious agents. Vaccine can be categorized as live attenuated and inactivated. Live attenuated vaccines activate immunity similar to natural infection by replicating living organisms whereas inactivated vaccines are either whole cell vaccines, eliciting immune response by killed organisms,or subunit vaccines, stimulating immunity by non-replicating sub cellular parts. The components of vaccine play a critical role in deciding the immune response mediated by the vaccine. The innate immune responds against the antigen component. Adjuvants represent an importantcomponent of vaccine for enhancing the immunogenicity of the antigens. Subunit vaccines with isolated fractions of killed and recombinant antigens are mostly co-administered with adjuvants. The delivery system of the vaccine is another essential component to ensurethat vaccine is delivered to the right target with right dosage form. Furthermore, vaccine delivery system ensures that the desired immune response is achieved by manipulating the optimal interaction of vaccine and adjuvantwith the immune cell. The aforementioned components along with routes of administration of vaccine are the key elements of a successful vaccination procedure. Vaccines can be administered either orally or by parenteral routes. Many groups had made remarkable efforts for the development of new vaccine and delivery system. The emergence of new vaccine delivery system may lead to pursue the immunization goals with better clinical practices.

Formulation and Pharmacokinetic Evaluation of Sustained Release Preparation Containing Clebopride Malate (말산클레보프리드 서방성 제제의 제조 및 약물동태학적 평가)

  • Ryou, Hae-Won;Lee, Joo-Han;Chi, Yong-Ha;Hahn, Yang-Hee;Tan, Hyun-Kwang;Lee, Kyu-Heung;Kim, Sang-Lin;Jeon, Seung-Yoon;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
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    • v.30 no.3
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    • pp.179-189
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    • 2000
  • Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner's method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.

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Preparation and characterization of green adsorbent from waste glass and its application for the removal of heavy metals from well water

  • Rashed, M. Nageeb;Gad, A.A.;AbdEldaiem, A.M.
    • Advances in environmental research
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    • v.7 no.1
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    • pp.53-71
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    • 2018
  • Waste glass disposal causes environmental problems in the cities. To find a suitable green environmental solution for this problem low cost adsorbent in this study was prepared from waste glass. An effective new green adsorbent was synthesized by hydrothermal treatment of waste glass (WG), followed by acidic activation of its surface by HCl (WGP). The prepared adsorbent was characterized by scanning electron microscopy (SEM), X-ray fluorescence (XRF), X-ray diffraction (XRD), and BET surface measurement. The developed adsorbent was used for the removal of heavy metals (Cd, Cu, Fe, Pb and Zn) from well water. Batch experiments were conducted to test the ability of the prepared adsorbent for the removal of Cd, Cu, Fe, Pb and Zn from well water. The experiments of the heavy metals adsorption by adsorbent (WGP) were performed at different metal ion concentrations, solution pH, adsorbent dosage and contact time. The Langmuir and Freundlich adsorption isotherms and kinetic models were used to verify the adsorption performance. The results indicated high removal efficiencies (99-100%) for all the studied heavy metals at pH 7 at constant contact time of 2 h. The data obtained from adsorption isotherms of metal ions at different time fitted well to linear form of the Langmuir sorption equation, and pseudo-second-order kinetic model. Application of the resulted conditions on well water demonstrated that the modified waste glass adsorbent successfully adsorbed heavy metals (Cd, Cu, Fe, Pb and Zn) from well water.

Physicochemical property and skin damage of physical mixture of valsartan and polysorbate 80 (Valsartan 및 polysorbate 80의 혼합물의 물리화학적 성질 및 피부 손상 연구)

  • Choi, Han-Gon;Sung, Jun-Ho;Oh, Dong-Hoon;Li, Dong-Xun;Cho, Kwan-Hyung;Woo, Jong-Soo;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.39 no.2
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    • pp.107-110
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    • 2009
  • To investigate the interaction and skin damage of valsartan with polysorbate 80, the physical mixture of valsartan and polysorbate 80 was prepared and then its adhesion, dispersibility, DSC and skin damage in nude rats were investigated. The physical mixture of valsartan and polysorbate 80 appeared as an aggregated form and could hardly be dispersed in water. The DSC curve showed that physical mixture disappeared the intrinsic peaks of valsartan and polysorbate 80 at about $115^{\circ}C$ and $170^{\circ}C$, respectively. It appeared a new relatively broad endothermic peak at about $150^{\circ}C$, suggesting that valsartan was chemically interacted with polysorbate 80. Furthermore, it induced the severe skin irritation and damage in nude mice. Thus, polysorbate 80 must not be used in the preparation of valsartan-loaded pharmaceutical dosage forms.

Preparation of Nanoparticles in Drug Delivery System Using Guar Derivatives and Dialysis Method

  • Na, Kun;Kim, Yu-Eun;Lee, Ki-Young
    • Journal of Microbiology and Biotechnology
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    • v.9 no.1
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    • pp.50-55
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    • 1999
  • To develop a new form of controlled release dosage for administering for indomethacin (IND), two formulations of IND-loaded nanoparticles were designed based on polysaccharide (guar) derivatives. Nanoparticles prepared by the dialysis method were characterized with respect to morphology, size distribution, drug content, and in vitro drug release. Morphological studies by scanning electron microscopy (SEM) indicated that guar acetate (GA) nanoparticles were spherical in shape and had a smooth surface. The particle size distributions of formulation I (40mg of GA) and formulation II (80mg of GA) were shown to be $250.78\pm185.13nm$ and $718\pm145.90nm$ in distilled water ($20$^{\circ}C$), respectively. The drug loading efficiencies of nanoparticles were approximately 26% and 31% for formulations I and II, respectively. The differential scanning calorimetry (DSC) results indicated that the IND was perfectly distributed within GA nanoparticles. We also found, from the X-ray diffractometry analysis, that a decrease in the degree of crystallinity of the drug occurred in the nanoparticles. No changes between the original IND and the released IND from GA nanoparticles were detected by FT-IR. Using guar acetate, it is possible to design nanoparticles which allow the controlled release of IND over an extended period of time.

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