• 한국임상약학회지
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• 제1권1호
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• pp.23-30
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• 1991

The sustained-release beads containing terbutaline sulfate (TBS) were prepared by rotogranulation method. The drug was dusted on the non-pareil seeds in a CF-granulator. The sustained-release beads were obtained by coating the active beads with ethylcellulose or $Eudragits^{(R)}$, using in any case the same granulator employed for active beads preparation. The release characteristics of sustained-release beads were examined in vitro by rotating basket method applied to $Bricanyl^{(R)}$ durules which is a sustained-release TBS matrix tablet. The release of terbutaline from the beads in vitro was first-order, and the release rate was dependent on both the coat weight ratio and membrane hydrophilicity. Both surfaces of the beads before and after dissolution were smooth. The drug release pattern from the beads could be thought the diffusion through the polymer membrane. The release rate and the surface of the beads stored for 3 years at room temperature were the same with those of the initial beads.

• 약학회지
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• 제41권1호
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• pp.48-59
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• 1997

Sustained release matrix tablets, pellets, and coated pellets for the delivery of sulindac were prepared using cellulose derivatives at various ratios, and evaluated for the dis solution pattern. The release of sulindac, from matrix tablets prepared with low viscosity HPMC was relatively fast, and especially the tablets made of Metolose SM released all of sulindac within 1 hr. The release of drug from tablets made of other HPMC derivatives were retarded in the order of the following: Pharmacoat 645>Pharmacoat 606>Pharrnacoat 606+HPC-L>HPC-L. The most sustained release pattern was observed with the preparation of high viscous polymer. Metolose 90 SH. While release of sulindac, from matrix type pellet containing 10mg/cap of Metolose 90 SH or 60 SH was completed within 1 hr, a prolonged release formulation (30% in 1 hr) was obtained by the inclusion of EC. Pellets coated with HPMC showed a fast release pattern (${\geq}$ 80% within 2 hrs), whereas pellets coated with HPMC and EC (molar ratio 1 : 1) showed a sustained release pattern (${\geq}$ 80% in 12 hrs), vath the release from EC pellets being the most sustained. Fast (naked) and slow release pellets coated with EC, Metolose 60SH 50cps and propylene glycol. and enteric pellets coated with HPMCP 55 and Myvacet$^{\circledR}$ were prepared, and combined at various ratios for the assessment of dissolution pattern. The result indicates the possibility that the development of 24 hr sustained release delivery systems containing sulindac for oral administration could be achieved by means of combining sustained and fast release pellets at a proper portion.

• Journal of Pharmaceutical Investigation
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• 제34권6호
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• pp.471-475
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• 2004

Tamsulosin has been frequently used for the treatment of benign prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is 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 matrix tablets and assess their formulation variables. We designed enteric coated sustained-release tamsulosin matrices to fulfill above statement. Aqueous microchannels in the enteric film need to be formed in order to obtain tamsulosin release even in an acidic environment such as gastric region. In the sustained-release tamsulosin matrix, low viscosity hydroxypropylmethylcellulose was used as a rate controller. Povidone K30 was also added to the matrices to facilitate water uptake so that a decrease in the release rate of tamsulosin as time elapses was prevented, possibly leading to pseudo zero-order release of the drug. The matrices were enteric-coated with hydroxypropylmethylcellulose phthalate (HPMCP), along with povidone K30 as an aqueous microchannel former. With the aqueous microchannels formed within the enteric film, tamsulosin could be released in an acidic condition. The release of tamsulosin decreased with increasing thickness of HPMCP membrane while the release rates of tamsulosin from those having different HPMCP thickness in pH 7.2 aqueous media were not considerably different, indicating that the enteric film was promptly dissolved at pH 7.2. These results clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the KFDA.

• 대한수의학회지
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• 제51권1호
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• pp.1-6
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• 2011

Sixteen steers were used to investigate the efficacy of the sustained-release implant of bovine somatotropin (bST) in improving growth and feed:gain ratio during 12 weeks. Administration of the 400 mg bST implant resulted in a 16.1% increase in growth rate, and this increase was significant (p<.05). The use of the sustained-release implant did not alter (p>.05) feed intake and feed:gain ratio. Thirty-four cows were used to investigate the efficacy of the sustained-release implant of bST in milk production during 4 weeks. Administration of the 200 mg bST implant resulted in an 8.7% increase in milk production, and this increase was significant (p<.05). Twenty-four barrows were used to investigate the efficacy of the sustained-release implant of porcine somatotropin (pST) in improving growth, feed:gain ratio and backfat thickness during 6 weeks. Administration of the 120 mg pST implant resulted in a 11.4% increase in feed:gain ratio and a 60% decrease in backfat thickness, and these results were significant (p<.05). But the use of the sustained-release implant did not alter (p>.05) growth rate and feed intake.

• Journal of Pharmaceutical Investigation
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• 제31권1호
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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.

• 대한수의학회지
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• 제48권1호
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• pp.27-32
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• 2008

The present study was carried out to develop a sustained release implantable formula of bovine somatotropin (SRIF-BST) and to examine its sustained release effect. The SRIF-BST was produced by coating a solid pellet, which was comprised of BST and an excipient, made of a biodegradable polymer and poloxamer, which are capable of regulating the rate of BST release. The coated membrane of SRIFBST was observed with a field emission scanning electron microscope. The thickness of the coated membrane was approximately $1{\mu}m$, and the pore sizes of the coated membrane surface were below $10{\mu}m$. In dissolution test, the release duration of the SRIF-BST maintained for 10 days, whereas the release duration of the control BST formula maintained for 3 days. In weight gain assay and tibia test of hypophysectomized rats, the release duration of the SRIF-BST treated group was 12 days and the net weight gain was 53.16 g, also the tibia length and strength of the SRIF-BST treated group was increased 10.5% and 23.1% compared with those of the control group, respectively.

• Journal of Pharmaceutical Investigation
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• 제36권1호
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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.

• Journal of Pharmaceutical Investigation
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• 제27권3호
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• pp.213-217
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• 1997

The present sustained-release terfenadine-pseudoephedrine HCl dosage form was the core tablet composed of outer (fast-release) layer containing 60 mg of terfenadine and l0mg of pseudoephedrine HCl, and inner (sustained-release) layer containing 110 mg of pseudoephedrine HCl. The purpose of this study was to investigate the possibility of formulating the terfenadine-pseudoephedrine HCl double-layered tablet which was bioequivalent to the core tablet. Its sustained-release and fast-release layer were formulated with disintegrating agents and polymers, respectively, varying with their kinds and amounts. The comparative dissolution test of double-layered and core tablet was carried out at pH 1.2, 4.0 and 6.8, leading to select composite of double-layered tablet whose dissolution pattern was similar to that of core tablet. It was composed of fast-release layer containing 60mg of terfenadine. 10 mg of pseudoephedrine HCl, sodium bicarbonate, microcrystalline cellulose and sodium starch glycolate, and sustained-release layer containing 110 mg of pseudoephedrine HCl and ethylcellulose/hydroxypropyl methylcellulose) (110/30 mg/tablet).

• Journal of Pharmaceutical Investigation
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• 제23권4호
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• pp.213-216
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• 1993

${\kappa}-Carrageenan$, an anionic polysaccharide, was employed in tablet formulations and its function as a drug release sustaining agent was investigated. Tablets composed of ${\kappa}-carrageenan$ and hydroxypropyl methylcellulose were fabricated by using direct compression method. Lactose and sodium alginate were utilized as controls for ${\kappa}-carrageenan$. Drug release experiments performed at pHs 1.2 and 7.4 revealed that ${\kappa}-carrageenan$ retains pH-dependent sustained release effects due to its anionic characteristics. Also, the ionic interaction between ${\kappa}-carrageenan$ and drugs exerted significant affects on drug release kinetics. ${\kappa}-Carrageenan$ was found out to be a useful additive for sustained release tablet formulations.

• 약학회지
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• 제60권1호
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• pp.46-50
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• 2016

The purpose of this study was the development of sustained-release lyogel of chlorhexidine in the treatment of periodontal diseases. A sustained-release chlorhexidine lyogel (CHX-G) was formulated, based on Eudragit$^{(R)}$ (1~3%), polyvinyl pyrrolidone (PVP) (0~10%), triacetin (20~40%), hydroxy ethyl cellulose (HEC) (1%) and glycerin. In vitro studies were performed to determine the release rate of chlorhexidine from CHX-Gs using dialysis tube. Our results suggest that the release rate of chlorhexidine from lyogel could be controlled by changing the lyogel compositions.