• Journal of Pharmaceutical Investigation
• /
• v.41 no.2
• /
• pp.103-109
• /
• 2011

The objective of the study was to prepare self-microeulsifying drug delivery system (SMEDDS) incorporating atorvastatin calcium and evaluate its properties and oral bioavailability. Solubility of atorvastatin in various vehicles was determined. Pseudo-ternary phase diagrams were constructed to identify the good self-emulsification region. The droplet size distributions of the resultant emulsions were determined by dynamic light scattering measurement. The mean droplet size of chosen formulation (20% ethyl oleate, 40% tween-80, 40% Carbitol$^{(R)}$) was $23.4{\pm}1.3$ nm. The SMEDDS incorporating atorvastatin calcium appeared to be associated with better performance in dissolution and pharmacokinetic studies, compared with raw atorvastatin calcium. In dissolution test, the release percentage of atorvastatin from SMEDDS mixture could rapidly reach more than 95% within 3 min. Oral $AUC_{0{\rightarrow}8hr}$ values in SD rats was $1994{\pm}335\;ng{\cdot}hr/mL$, which significantly increased (P<0.05) compared with raw atorvastatin calcium. The SMEDDS formulation was relatively stable when stored at $4^{\circ}C$ during 3 months. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin, by the oral route.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.3
• /
• pp.157-163
• /
• 2005

The pellets with multiple drug release system (MDRS) of Diltiazem. HCl which consist of immediate drug release layer, drug reservoir layer and controlled release rate membrane, were prepared by using CF-Coater. As main factors for more effective MDRS of Diltiazem. HCl, ethylcellulose was used for the controlling drug release rate, and diethylphthalate was used for plasticizer, respectively. In vitro evaluation study was performed by comparative dissolution test between our test MDRS and reference Diltiazem. HCl preparation. The physical tests were performed using FT-IR and SEM. In vivo evaluation was also performed by observing the behavior of a plasma drug concentration after oral administration. The bioavailability was determined by analyzing the blood sample after oral administration to healthy, male volunteers once a day. As a result, there were no significant differences in bioequivalence parameters $(AUC_{\infty},\;C_{max},\;t_{1/2})$ between two systems. It might be concluded that our MDRS of Diltiazem. HCl could be an alternative delivery system to reference drug preparation.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
• /
• v.34 no.1
• /
• pp.49-58
• /
• 2008

Objective: The Purpose of the study was to investigate the bone morphogenic protein expression of rhBMP-2(recombinant human bone morphogenic protein-2) as singnaling molecule and ${\beta}-TCP$(Tricalcium phosphate) as a bone substitute and carrier medium of rhBMP-2. Materials and Methods: 16 rabbits divided into 2 group of each 8 rabbit. Two standardized bone defect, round bilateral defect was made in the cranium of the 8 rabbit of first group, and was grafted with $150{\sim}500{\mu}m$ diameter ${\beta}-TCP$ 0.25g in one side, which was soaked with rhBMP-2, and autogenous bone was grafted on another side as a positive control. Second group of 8 rabbit, only ${\beta}-TCP$ was grafted with same size and same manner. After 2, 4, 8, and 12 weeks, specimen was taken for microscopic immunohiostochemical and histomorphometric analysis. Result: Grafting ${\beta}-TCP$ with rhBMP show the early formation of the bone regenerative factor (BMP-4) and more quantity of new bone formation than only use of ${\beta}-TCP$ (8,12 week), even show less new bone formation than autogenous bone. Conclusion : The experimental study result that ${\beta}-TCP$ graft combination with rhBMP-2 as a delivery system is an effective with osteoinductive capacity and biodegradable properties, so that provide clinical availibility of composite use in reconstruction of bony defect.

• KSBB Journal
• /
• v.18 no.2
• /
• pp.161-164
• /
• 2003

Oral drug delivery system using pectin gel was developed for colon-targeting of peptide drug. BSA(bovine serum albumin)-loaded pectin and pectin-alginate beads were prepared for drug release properties in vitro. Morphological studies by electron microscopy indicated that pectin and pectin-alginate beads were spherical in shape and approximately 1.0 mm. In order to find the suitable beads, effects of cross-linking agents (calcium chloride or zinc acetate) and drying temperature of beads were investigated. Drug release decreased with concentration of cross-linking agents and drying temperature. For colonic drug delivery from pectin and pectin-alginate beads, pectin degradable enzymes were added at 5 hrs from the beginning of drug release. After addition of enzymes, drug release was suddenly increased against free enzymes. Therefore, pectin and pectin-alginate beads can be promised as useful drug release carriers for colon-targeted delivery.

• Maxillofacial Plastic and Reconstructive Surgery
• /
• v.35 no.6
• /
• pp.381-389
• /
• 2013

Two patients with partial edentulous maxilla were scheduled to undergo installation of implant fixtures using a tooth-supported surgical template based on computer assisted treatment planning. After 3-dimensional (3D) computed tomographic scanning was transferred to the OnDemand3D (Cybermed Co., Seoul, Korea) software program for virtual planning, fixtures of MK III Groovy RP implant of the Br${\aa}$nemark System (Nobel Biocare AB Co., G$\ddot{o}$teborg, Sweden) was installed using the In2Guide (CyberMed Co., Seoul, Korea) tooth-supported surgical template with a Quick Guide Kit (Osstem Implant Co., Seoul, Korea) system in the posterior maxilla of each patient. Sinus floor elevation with a xenogenic bone graft procedure was also performed simultaneously in one patient. Fixture installations were completed successfully without complications, such as sinus mucosa perforation, bony bleedings, fenestrations, or others. During the last two-year follow-up period after prosthetics delivery, each implant was found to be fine with no other minor complications. The entire procedures are reported and the literatures on use of tooth-supported surgical template was reviewed.

• Journal of Pharmaceutical Investigation
• /
• v.32 no.1
• /
• pp.27-33
• /
• 2002

A self-microemulsifying drug delivery system(SMEDDS) composed of Cremophor $EL^{\circledR},\;Labrasol^{circledR}$, and Lauroglycol $FCC^{circledR}$ was prepared for the enhancement of solubility, dissolution rate and bioavailability of ibuprofen(IBP), which is water-insoluble but soluble in oils and surfactants. Phase diagram with various regions including microemulsion area was depicted. The SMEDDS was encapsulated in soft gelatin capsules and their dissolution characteristics in various media were observed in comparison to the generic products commercially available in the market. Soft capsules of SMEDDS formulation showed better dissolution profiles, especially in acidic condition, than the others. For the period of 1 hr dissolution in pH 1.2 medium, it reached over 70% dissolution from soft capsules, compared to less than 40% dissolution from commercial reference tablets. On the other hand, in vivo pharmacokinetic parameters were obtained after oral administrations of different IBP preparations to Sprague Dawley rats. SMEDDS formulation showed higher $C_{max}$ and greater $AUC_{0-5hr}$ than the suspension of reference tablet or IBP powder. Therefore, it is possible to conclude that a newly developed soft capsules employing SMEDDS provides an alternative preparation to improve oral bioavailability of IBP.

• Journal of Pharmaceutical Investigation
• /
• v.34 no.6
• /
• pp.471-475
• /
• 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.

• Journal of Preventive Medicine and Public Health
• /
• v.14 no.1
• /
• pp.3-12
• /
• 1981

To identify the changes in professional care patterns after the introduction of medical insurance in Korea, professional care in hospitals and clinics of two succeeding years were compared. The hospitals and clinics selected for this study were those which located in Seoul city. Hospitals were classified into 3 categories: university hospital, general hospital and hospital. The diseases selected for this study were acute appendicitis and normal delivery. They were selected because their disease courses are considered to be fairly stable. The variables used for this study were length of stay, total hospital costs, costs of each components of cares. The information used for this study was obtained from the official forms requested by the medical facilities to the Korea Medical Insurance Corporation. The two periods studied were 3 months of each year from March 1st to May 31st in 1979 and 1980, The total number of normal delivery studied was 289 in 1979, 301 in 1980 respectively and the acute appendicitis was 92 and 111 respectively. In order to compare the quantity of medical care between 2 study periods the insurance price scores of 1979 were converted to prices of 1980. For statistical test of difference between 2 periods T-test and Welch's test were used. The result of the study were briefly summarized in below. 1. No significant difference was observed in the average length of stay of both disease between two study periods in all types of hospitals. 2. No significant difference was observed in the average total hospital costs of both diseases in all types of hospital, but in the private clinic the average clinic costs was rather decreased significantly in 1980. 3. More cost decrease were seen than cost increase in 1980 in all types of facilities, More cost changes by items were seen in acute appendicitis than in normal delivery between two study periods. The total hospital costs can be devided into 2 portions: charges for drug and material and for physician. In normal delivery, costs for physician's charges was significantly decreased in almost all the hospitals and costs for drug and material were not changed significantly in all the hospitals in 1980. In the university hospitals, however, the costs for drug and material were increased significantly in 1980. The cost decrease for physician's charge were mainly due to the decrease in the costs of laboratory test, treatment and physical therapy. The increase in the costs for the drug and material in the university hospitals was mainly due to the increase in the cost for drugs for oral administration and injection. 4. The proportion of components of medical care in the hospital has not been changed significantly, however, the cost for injection in normal delivery was characteristically increased in 1980 in all hospitals studied. In general the proportion of the costs for drug and material was tended to increase and the costs for physician was tended to decrease in 1980. The increase in the costs for drug and material were considered to be due to increase in the cost for drugs for oral administration and injection. The decrease in the costs for physician were due to decrease in the costs of laboratory test, treatment and physical therapy. Above mentioned changes in hospital and clinic care patterns are considered to be mostly influenced by the review criteria set by the K.I.C. for the assessment of the fee request made by clinics and hospitals.

• Journal of Ginseng Research
• /
• v.48 no.4
• /
• pp.417-424
• /
• 2024

Background: This research main objective was to evaluate a proliposomes (PLs) formulation for the enhancement of oral bioavailability of ginsenosides, using ginsenoside Rg3 (Rg3) as a marker. Methods: A novel PLs formulation was prepared using a modified evaporation-on-matrix method. Soy phosphatidylcholine, Rg3-enriched extract, poloxamer 188 (Lutrol® F 68) and sorbitol were mixed and dissolved using a aqueous ethanolic solution, followed by the removal of ethanol and lyophilization. The characterization of Rg3-PLs formulations was performed by powder X-ray diffractometry (PXRD), transmission electron microscopy (TEM) and in vitro release. The enhancement of oral bioavailability was investigated and analyzed by noncompartmental parameters after oral administration of the formulations. Results: PXRD of Rg3-PLs indicated that Rg3 was transformed from crystalline into its amorphous form during the preparation process. The Rg3-encapsulated liposomes with vesicular-shaped morphology were generated after the reconstitution by gentle hand-shaking in water; they had a mean diameter of approximately 350 nm, a negative zeta potential (- 28.6 mV) and a high entrapment efficiency (97.3%). The results of the in vitro release study exhibited that significantly more amount of Rg3 was released from the PLs formulation in comparison with that from the suspension of Rg3-enriched extract (control group). The pharmacokinetic parameters after oral administration of PLs formulation in rats showed an approximately 11.8-fold increase in the bioavailability of Rg3, compared to that of the control group. Conclusion: The developed PLs formulation could be a favorable delivery system to improve the oral bioavailability of ginsenosides, including Rg3.

• Applied Chemistry for Engineering
• /
• v.10 no.2
• /
• pp.201-205
• /
• 1999

Hydroxypropylmethylcelluloses (HPMC) are cellulose ethers which may be used as the basis for hydrophilic matrices for controlled release oral delivery and offer the advantages of being non-toxic and relatively inexpensive. In this work, we designed new drug release system using HPMC as matrix, manufactured by direct compression technology and have investigated the effects of the controlling factors on drug release from a swellable hydrophillic delivery system. It was found that the release rate of the drug decreased with increasing the polymer molecular weight and the polymer content in tablets, and was independent of compaction pressure and pH of dissolution fluids. Especially, the ability of the anionic surfactant, sodium laurylsulfate, to retard the release of pseudoephedrine hydrochloride from HPMC was characterised. With increasing the concentration of the sodium laurylsulfate within the matrix, drug release rate decreased. It is believed that, provided the pseudoephedrine hydrochloride and the sodium laurylsulfate are oppositely charged, they will bind together in situ within the HPMC matrix, leading to reduced drug release rates.