• Title/Summary/Keyword: Dosage form

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Enhancement of Nitrendipine Bioavailability in Rats by its Solid Dispersion with $Hydroxypropyl-{\beta}-Cyclodextrin$ after Oral Administration (흰쥐에 경구 투여시 히드록시프로필-베타-시클로덱스트린과 니트렌디핀 고체분산에 의한 생체이용률 증가)

  • Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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    • pp.295-301
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    • 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.

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Guideline of Improvement and Evaluation of Prescribing Errors in Colorectal Chemotherapy (대장암 항암 화학요법의 처방 오류 평가 및 개선안 제시)

  • Lim, Hyun-Soo;Lim, Sung Cil
    • Korean Journal of Clinical Pharmacy
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    • v.23 no.2
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    • pp.158-166
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    • 2013
  • Background: Colorectal cancer shows a significant increase in South Korea due to westernization of diet, lack of dietary fiber, drinking and smoking, irregular defecation. There are surgery, chemotherapy, radiation therapy in treatment of colorectal cancer. There may be a medication errors in the process of chemotherapy because of its high toxicity, narrow therapeutic index and the health status of cancer patients. Consequently medication errors can cause increasing the risk of death, prolonging hospital stay and increasing the cost. Among medication errors on medication use process, prescribing errors are of particular concern due to higher risk of serious consequences. It is important for pharmacist to prevent the prescribing errors before reaching patient. Therefore we analyzed the prescriptions of colorectal cancer, classified prescribing errors, suggested guideline to reduce prescribing errors and verified the importance of pharmacist's role in prevention of medication errors activity. Methods: We collected the numbers of prescriptions of colorectal cancer(n=2,373) through anti cancer management program and EMR and analyzed the errors of prescriptions by categories from Oct 1st 2011 to Sep 30th 2012 at Chungbuk National University Hospital. We reviewed the prescriptions as follows - patients' characteristics, the result of test, previous prescriptions, characteristics of antineoplastic agents and patients' allergy, drug sensitivity, adverse events. Prescriptions are classified into inpatient and outpatient and analyzed the errors of prescriptions by categories (dosage form, dose, input, diluents, regimen, product). Results: Total prescription number of inpatient and outpatient of colorectal cancer was 1,193 and 1,180 and that of errors was 107(9%) and 22(1.9%), respectively. In case of errors of categories, the number of errors of dosage form is 69 and 8, errors of dose is 15 and 5, errors of input is 9 and 9 in inpatient and outpatient prescriptions, respectively. Errors of diluents is 8, errors of regimen is 3, errors of product is 3 in only inpatient prescriptions. In case of errors of categories by inpatient department, the number of errors of dosage form is 34 and 35, errors of dose is 7 and 8, errors of input is 6 and 3, errors of diluents is 4 and 4, errors of regimen is 2 and 1, errors of product is 2 and 1 in SG and HO, respectively. In case of outpatient department, the number of errors of dosage form is 8 in HO, errors of dose is 5 in HO, errors of input is 5 and 4 in SG and HO, respectively. Conclusions: The rate of errors of inpatient is higher than that of outpatient. Junior doctors are engaged in prescriptions of inpatient and pharmacist need to pay attention to review all prescriptions. If prescribing errors are discovered, pharmacist should contact the prescriber and correct the errors without delay. The guideline to reduce prescribing errors might be upgrading software of anti cancer management program, education for physicians as well as pharmacists and calling prescriber's attention to preventing recurrence of errors.

Develop a sustainable wet shotcrete for tunnel lining using industrial waste: a field experiment and simulation approach

  • Jinkun Sun;Rita Yi Man Li;Lindong Li;Chenxi Deng;Shuangshi Ma;Liyun Zeng
    • Advances in concrete construction
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    • v.15 no.5
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    • pp.333-348
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    • 2023
  • Fast infrastructure development boosts the demand for shotcrete. Despite sand and stone being the most common coarse and fine aggregates for shotcrete, excessive exploration of these materials challenges the ecological environment. This study utilized an industrial solid waste, high-titanium heavy slag, blended with steel fibers to form Wet Shotcrete of Steel Fiber-reinforced High-Titanium Heavy Slag (WSSFHTHS). It investigated its workability, shotcrete performance and mechanical properties under different water-to-cement ratios, fly ash content, superplasticizer dosage, and steel fiber content. The tunnel excavation and support were investigated by conducting finite element numerical simulation analysis and was used in 3 tunnel lining pipes in Zhonggouwan tailing pond. The major findings are as follows: (1) The water-to-cement ratio (w/c ratio) significantly impacted the compressive strength of WSSFHTHS. The highest 28-day compressive strength of 60 MPa was achieved when the w/c ratio was 0.38; (2) Adding fly ash improved the workability and shotcrete performance and strength development of WSSFHTHS. The best anti-permeability performance was achieved when the fly ash constituted 15%, with the lowest permeability coefficient of 4.596 × 10-11 cm/s; (3) The optimum superplasticizer dosage for WSSFHTHS is 0.8%. It provided the best workability and shotcrete performance. Excessive dosage resulted in water bleeding and poor aggregate encapsulation, while insufficient dosage decreased flowability and adversely affected shotcrete performance; (4) The dosage of steel fibers significantly impacted the flexural and tensile strength of WSSFHTHS. When the steel fiber dosage was 45 kg/m3, the 28-day flexural and tensile strengths were 8.95 MPa and 6.15 MPa, respectively; (5) By integrating existing shotcrete techniques, the optimal lining thickness was 80 mm for WSSFHTHS per simulation. The results revealed that after using WSSFHTHS, the displacement of the tunnel surrounding the rock significantly improved, with no cracks or hollows, similar to the simulation results.

Effect of Liposome Encapsulation on Intestinal Absorption of Rhodamine 123 (리포솜 봉입이 로다민 123의 소장 흡수에 미치는 영향)

  • Hong, Soon-Sun;Lee, Hae-Ree;Li, Hong;Chung, Suk-Jae;Kim, Dae-Duk;Shim, Chang-Koo
    • YAKHAK HOEJI
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    • v.49 no.2
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    • pp.185-191
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    • 2005
  • The absorption of a P-gp substrate, rhodamine 123, from a liposomal dosage form was investigated across Caco-2 cell monolayers, rat intestines and rat intestinal Peyer's patches in Ussing chamber, Rhodamine 123 was incorporated into liposomes according to the standard evaporation method, which led to a production of liposomes with a mean diameter of 71.3 nm. The permeability (Papp of rhodamine 123 from a water solution across the monolayer was $2.45{\times}10^{-6}$ cm/s for $A{\leftrightarrow}B$ (apical to basal) and $14.0{\times}10^{-6}$ cm/s for $B{\leftrightarrow}A$ (basal to apical) directions, consistent with the fact that rhodamine 123 is one of the P-gp substrates. The transport of rhodamine 123 from the liposomal dosage form was much lower for both directions compared to the solution of rhodamine 123. The transport of rhodamine 123 across the rat intestine was also significantly decreased for both directions, I.e., influx and efflux, by the liposomal incorporation of the compound. The transport of rhodamine 123 across the Peyer's patch was substantially reduced by liposomal incorporation. No difference was found in the transport between the Peyer's patch and non-Peyer's patch. These observations suggest that the contribution of transport via Peyer's patches in the uptake of liposomes may be minimal, especially for rapidly absorbed compounds like rhodamine 123. Therefore, the increased absorption of P-gp substrates does not appear to be feasible by incorporating the compounds in liposomes, due to negligible involvement of Peyer's patches in the uptake of particulate dosage forms like liposomes. Liposomes may rather represent a sustained release dosage form of incorporated compounds.

Formulation of Omeprazole Preparations using Omeprazole-Ethylendiamine Complex (오메프라졸-에칠렌디아민 복합체를 이용한 제제설계)

  • Oh, Sea-Jong;Park, Seong-Bae;Park, Sun-Hee;Hwang, Sung-Joo;Rhee, Gye-Ju
    • Journal of Pharmaceutical Investigation
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    • v.25 no.1
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    • pp.19-29
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    • 1995
  • The study was carried out to develop useful formulation for omeprazole(OMP) through OMP-ethylendiamine complex(OMPED), and the pharmaceutical properties of formula were tested to find out the difference in vivo behaviors of formulations between the free and complexed OMP. Oral and suppository dosage forms were also formulated and the dissolution profiles and pharmacokinetic parameters were measured to observe the difference in bioavailability between the free and complex form, and the correlation between dissolution rate and bioavailability was evaluated. The results are summarized as follows; In the case of formulation for oral administration, the release of OMP from enteric OMPED pellets was found satisfactory to the requirement standard and no decomposition of OMP in the pellets was found in acidic solution. Therefore the enteric OMPED pellets are anticipated to be a stable formulation. The release of OMP from OMPED tablet with chitosan as excipient and coated with cellulose acetate phthalate was found to be significantly retarded. The results of bioavailability test for OMP and OMPED tablets with lactose-excipient showed that the AUC value of OMP tablet was $116.89\;{\mu}g\;{\cdot}\;min/ml$, that of OMPED tablet was $161.10\;{\mu}g\;{\cdot}\;min/ml$, respectively. The reason why was thought that OMP decomposes more readily in body than OMPED, and the AUC of the tablet with chitosan-excipient and coated with cellulose acetate phthalate was most enhanced. In the case of bioavailability for suppositories with OMP, $OMP-{\beta}\;-cyclodextrin$ complex and OMPED, the AUC of OMPED suppository was most increased. From the above results, it is thought that the more stable and bioavailable oral or rectal dosage forms could be developed by using the OMPED as a potential OMP complex.

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Effect of Curing and Compression Process on the Drug Release of Coated Ion-Exchange Resin Complexes

  • Jeong, Seong-Hoon;Wang, Hun-Sik;Koo, Ja-Seong;Choi, Eun-Joo;Park, Ki-Nam
    • Journal of Pharmaceutical Investigation
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    • v.41 no.2
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    • pp.67-73
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    • 2011
  • Ion exchange resins can be one of the good carriers for sustained drug release. However, the sustained release may not be enough only with themselves and hence film coating with rate controlling polymers can be applied to have a further effect on the drug release. Due to the environmental and economic issues of organic solvent for the polymer coating, aqueous polymeric systems were selected to develop dosage forms. Among the many aqueous polymeric dispersions for the film coating, EC (ethylcellulose) based polymers such as Aquacoat$^{(R)}$ ECD and Surelease$^{(R)}$ were evaluated.A fluid-bed coating was applied as a processing method. The drug release rate was quite dependent on the coating level so the release rate could be modified easily by changing different levels of the coating. The drug release rate in the Aquacoat$^{(R)}$ coated resin particles was strongly dependent on curing, which is a thermal treatment to make homogeneous films and circumvent drug release changes during storage. After dissolution test using the compressed tablets in which the coated resin particles are contained, inhomogeneous coating and even pores could be observed showing that the mechanical properties of EC were not resistant to granulation and compaction process. However, when tablets were prepared in different batches, the release profiles were almost identical showing the feasibility of the coated resin particle as incorporated into the tablet formulation.

Preparation and Characterization of Pamidronate-loaded PLGA Wafer for the Treatment of Bone Resorption (골 재흡수 치료를 위한 파미드로네이트를 함유한 이식형 생분해성 PLGA 웨이퍼의 제조와 특성결정)

  • 유제영;김상욱;강길선;성하수;정제교
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.680-690
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    • 2002
  • Implantable biodegradable wafers were prepared with pamidronate -loaded poly (L-lactide-co-glycolide) (PLGA, 75 : 25 mole ratio by lactide to glycolide, molecular weight : 20000 and 90000 g/mole) by direct compression method for the sustained release of pamidronate to investigate the possibility for the treatment of bone resorption. Pamidronate-loaded PLGA powders were prepared by means of physical mixing and spray drying with the control of formulation factors and characterized by scanning electron microscope and X-ray diffractometer. The pamidronate-loaded PLGA powders fabricated into wafers by direct compression under the constant pressure and time at room temperature. These wafers were also observed for their structural characteristic, release pattern, and degradation pattern. The release rate of pamidronate increased with increasing their initial loading ratio as well as increasing wafer thickness. The molecular weight of PLGA affects the release pattern : the higher molecular weight of PLGA, the faster release rate. It can be explained that the higher viscosity of high molecular PLGA solution at same concentration tends to aggregate PLGA and pamidronate resulting in unstable pharmaceutical dosage form. This system had advantages in terms of simplicity in design and obviousness of drug release rate and nay be useful as an implantable dosage form for the treatment of aural cholesteatoma.

Stability and Dissolution Enhancement of Omeprazole by Pharmacentical Formulation (오메프라졸의 제제화 및 평가)

  • Jee, Ung-Kil;Lee, Gye-Won;Jeon, Un-Jong
    • Journal of Pharmaceutical Investigation
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    • v.22 no.4
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    • pp.281-287
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    • 1992
  • Omeprazole (OMZ) is very unstable in acidic solution, which selectively inhibit the release of the gastric juice in the gastric mucosa, In order to stabilize (OMZ) in oral solid dosage form, the enteric-coated microcapsules and compression-coated OMZ tablets containing lysine or arginine as stabilizer were prepared and their dissolution and stability test were performed. The haif life of OMZ microcapsules containing arginine was 194 days at $30^{\circ}C$ and OMZ was completely released in 60 min. The half-lives of enteric coated and non-coated compression-coated OMZ tablets with lysine were 292 and 95 days at $30^{\circ}C$, respectively. The half-lives of enteric coated and non-coated compression-coated tablets with arginine were 1752 and 293 days at $30^{\circ}C$, respectively, and OMZ were released completely in 20 min in the 2nd fluid of K.P.VI. Consequently, the enteric-coated compression-coated OMZ tablets with arginine as stabilizer provided a good formulation for oral solid dosage form.

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Herbal Drugs through Chosun Maiyak Corporation 《朝鮮賣藥株式會社》in Japanese Colonial period (조선매약주식회사를 통해 본 일제강점기 한약의 모습)

  • Baek, Kyu-Hwan;Park, Gyu-Ri;Lee, Sang-Jae
    • Herbal Formula Science
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    • v.23 no.1
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    • pp.15-24
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    • 2015
  • Objectives l: This study is to investigate the emergence of herbal medicine during Japanese colonial period by reviewing newspaper advertisements and brochures about patient medicine of Chosun Maiyak Corporation. Methods : 69 kinds of patent medications and 584 newspaper advertisements are throughly reviewed to investigate dosage form, drug effect, sales unit and method, price, and advertisement pattern. Results : Lyungsinwhan represented more than half of the total advertisements, followed by Yungmihwan, Sahyangsohabwon, Yeollyeonggobondan, and Chiljehyangbuhwan. Lyungsinwhan was advertised mostly in spring and summer whereas Yungmihwan and Yeollyeonggobondan were advertised in spring and fall. Dosage form included pill(丸), mixture(膏), powder(散), and liquid(水, 液), while pill and mixture prevailed over other forms. Drug effect included dermatological, pediatric, digestive, and gynecological effects in the increasing order of drug numbers. Sales unit and price were found to vary significantly. Sales method included nationwide network distribution of medicine through postcards and stores. Conclusion : Herbal medicine during the colonial period was distributed in various kinds of forms with different effects and advertisement patterns through diverse sales unit and price.