• Title/Summary/Keyword: Controlled release formulation

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Design and Optimization of Solid Dispersed Osmotic Pump Tablets of Aceclofenac, A Better Approach to Treat Arthritis

  • Edavalath, Sudeesh;Rao, B. Prakash
    • Journal of Pharmaceutical Investigation
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    • v.41 no.4
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    • pp.217-225
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    • 2011
  • The aim of this work was to prepare porous osmotic pump tablets for controlled delivery of Aceclofenac. Aceclofenac solid dispersion was prepared to improve the solubility by using the drug - carrier (Mannitol) ratio of 1:1. The osmotic pump tablets were prepared using the solid dispersed product of Aceclofenac. The formulation contains potassium chloride as osmotic agent, cellulose acetate as semipermeable membrane, poly ethylene glycol (PEG 4000) as pore former and sodium lauryl sulphate (SLS) as solubility enhancer. The formulations were designed by the general factors such as osmotic agent and pore former. All formulations were evaluated for various physical parameters and, the in vitro release studies were conducted as per USP. The drug release kinetic studies such as zero order, first order, and Higuchi and Korsmeyer peppas were determined and compared. All the formulations gave more controlled release compared to the marketed tablet studied. Numerical optimization techniques were applied to found out the best formulation by considering the parameter of in vitro drug release kinetics and dissolution profile standards. It was concluded that the porous osmotic pump tablets (F7) composed of Aceclofenac solid dispersion/Potassium chloride/Lactose/Sodium lauryl sulphate/Magnesium Stearate (400/40/95/10/5, mg/tab) and coating composition with Cellulose acetate/ PEG 4000 (60/40 %w/w) is the most satisfactory formulation. The porous osmotic pump tablets provide prolonged, controlled, and gastrointestinal environment-independent drug release.

Release Profile of 14C-Butachlor from Controlled Release Formulation Prepared with Alginate-Kaoline Matrix (Alginate와 Kaoline을 이용(利用)한 방출조절제(放出調節劑)의 14C-Butachlor 용출특성(溶出特性))

  • Oh, Byung-Youl
    • Korean Journal of Weed Science
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    • v.10 no.2
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    • pp.122-129
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    • 1990
  • The herbicide $^{14}C$-butachlot[N-(butoxymethyl)-2-chloro-2', 6'-diethylacetanilide] labelled uniformly in benzene ring was incorporated in alginate-based granules to get controlled release properties. The influence of kaoline addition on the formulation characteristics and release profiles were evaluated under a closed dark and an opened sunlight condition. Incorporation efficiency of $^{14}C$-butachlor in alginate-kaoline matrices was over 91.8%. Formulation yield was decreased with increase of kaoline concentration. The release rate from all the granules prepared with alginate was slower than that from the commercial granule impregnated in zeolite. The release rate from the granule containing kaoline was decreased as the kaoline content was increased under both conditions. Losses of butachlor from the leacheate solution of the alginate-kaoline matrices under an opened sunlight condition was diminished by increasing the kaoline content.

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Controlled Release of Tamsulosin from Nanopore-Forming Granules (미세 다공성 과립을 이용한 탐스로신의 방출제어)

  • Seo, Seong-Mi;Lee, Hyun-Suk;Lee, Jae-Hwi;Lee, Ha-Young;Lee, Bong;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.36 no.1
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    • pp.39-44
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    • 2006
  • Tamsulosin or a salt thereof such as its hydrochloride salt has been known to have an adrenaline ${\alpha}$ receptor blocking action for urethra and prostate areas. It has been widely used as a drug which lowers the prostate pressure and improves urinary disturbance accompanied by prostate-grand enlargement, thus for the treatment of prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is essentially required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin granules and assess their formulation variables. We designed entric coated sustained-release tamsulosin granules for this purpose. Nano-pores in the outer controlled release membrane were needed in order to obtain initial tamsulosin release even in an acidic environment such as gastric region. In our sustained release osmotic granule system, hydroxypropylmethylcellulose in a drug-containing layer was used as a rate controller. The drug-containing granules were coated with hydroxypropylmethylcellulose phthalate (HPMCP) and Eudragit, along with glycerol triacetate as an aqueous nano-pore former. The release of tamsulosin depended heavily on the type of Eudragit such as RS, RL, NE 30D, used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the Korean Food and Drug Administration.

A Study on the Properties of Hollow Silica Microspheres for Controlled-release Pesticide Formulation (농약 방출 조절제 소재로서 실리카 중공 미세구의 물성연구)

  • Jung, Byoung-Soo;Park, Yong-Sung
    • The Korean Journal of Pesticide Science
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    • v.8 no.4
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    • pp.319-324
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    • 2004
  • Pesticide formulations for controlled release were pepared with hollow silica microspheres. The hollow microsphere, which was obtained through calcination for the core removed after silica coating, showed maximum impregnation of benfuracarb up to 2.7 times of its mass in comparison with those obtained through the other core removal method. The release test of the pesticide formulation, when used with ESO(Epoxidized Soybean Oil) as a binder, showed ideal release pattern with steady release rate from the day 10 to 30 retaining the benfuracarb concentration in the water around 1.65 ppm.

Formulation and Evaluation of Controlled Release Patch Containing Naproxen (나프록센 함유 방출제어형 패취의 제제설계 및 평가)

  • Rhee, Gye-Ju;Hong, Seok-Cheon;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.29 no.4
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    • pp.343-348
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    • 1999
  • The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

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Effects of Solvent Selection and Fabrication Method on the Characteristics of Biodegradable Poly(lactide-co-glycolide) Microspheres Containing Ovalbumin

  • Cho, Seong-Wan;Song, Seh-Hyon;Shoi, Young-Wook
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.385-390
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    • 2000
  • To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20% were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.

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A Ternary Polymeric Matrix System for Controlled Drug Delivery of Highly Soluble Drug with High Drug Loading : Diltiazem Hydrochloride (염산 딜티아젬의 방출을 제어하기 위한 삼중 폴리머 매트릭스 시스템)

  • Kim, Hyun-Jo;Fassihi, Reza
    • Journal of Pharmaceutical Investigation
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    • v.31 no.1
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    • pp.19-25
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    • 2001
  • The purpose of this study was to use a ternary polymeric matrix system for high drug loading of a highly soluble drug for controlled release delivery. The controlled drug delivery of diltiazem HCl (solubility > 50% in water at $25^{\circ}C$) with high loading dose (the final loading dose of drug was 34%) from a ternary polymeric matrix (gelatin, pectin, HPMC) was successfully accomplished. This simple monolithic system with 240 mg drug loading provided near zero-order release over a 24 hour-period by which time the system was completely dissolved. The release kinetics of diltiazem HCl tablet with high loading dose from the designed ternary polymeric system was dependent on the ratios of HPMC : pectin binary mixture. The release rate increased as pectin : HPMC ratio were increased. Swelling behavior of the ternary system and the ionic interaction of formulation components with cationic diltiazem molecule appear to control drug diffusion and the release kinetics. Comparable release profiles between commercial product and the designed system were obtained. The binding study between gelatin with diltiazem HCl showed the presence of two binding sites for drug interaction with subsequent controlled diffusion upon swelling. This designed delivery system is easy to manufacture and drug release behavior is highly reproducible and offers advantages over the existing commercial product.

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Trend of Ceramic Materials Technology for Beauty-care (뷰티케어용 세라믹소재기술 동향)

  • Chang, Jeong Ho
    • Ceramist
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    • v.21 no.3
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    • pp.302-308
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    • 2018
  • This work reported the trends of bioceramic materials for beauty-care applications with the several represent examples - tone-up, sun-care and anti-pollution cosmetics. The development of cosmetic techniques was discussed and reviewed with various ceramic hybrid materials. Moreover, we also reported the preparation and application of functional cosmetics with silicified liposome particles as a good make-up material for controlled release with natural compounds. The homogeneous loading and highly controlled-release formulation with porous and silicified ceramic liposome ceramic materials were discussed.

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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Insecticidal effects of Chitosan-formulated etofenprox and α-cypermethrin against Myzus persicae and Aphis gossypii (Homoptera: Aphididae) (키토산 캐리어 나노제형의 α-cypermethrin과 etofenprox의 목화진딧물과 복숭아혹진딧물에 대한 살충효과)

  • Seo, Mi-Ja;Kang, Min-Ah;Kwon, Hye-Ri;Yoon, Kyu-Sik;Kang, Eun-Jin;Yu, Yong-Man;Youn, Young-Nam;Youn, Young-Nam
    • Korean journal of applied entomology
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    • v.49 no.4
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    • pp.333-342
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    • 2010
  • The possibility of commercializing the controlled release of chitosan carrier nano formulation was examined with mortalities and population increase rates of Aphis gossypii and Myzus persicae after treatment of 2 ${\alpha}$-cypermethrin nano type formulations of different chitosan carrier molecular weight (M.W. 3,000 and 30,000) and 2 etofenprox nano types of chitosan content (70% and 80%). After 14 days of treatment, ${\alpha}$-cypermethrin nano formulation showed over 40% mortality against A. gossypii. Therefore, it was confirmed that the insecticide release was controlled through chitosan carrier. Results of the investigation of insecticidal activity of ${\alpha}$-cypermethrin nano formulation showed there were no differences between nano types at 4 days after treatment. However, after 14 days, the population increase rate treated with chitosan M.W. 30,000 formulation was -0.037, much lower than that of M.W. 3,000 formulation with 0.231. The result exhibits that chitosan M.W. 30,000 formulation would be a suitable controlled release formulation. On the other hand, etofenprox formulations didn't show any significant insecticidal effect or persistency difference against both aphid species.