• The Korean Journal of Physiology and Pharmacology
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• v.28 no.3
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• pp.275-284
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• 2024

Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181-0.72) and (-13.4 to -6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.

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

• Polymer(Korea)
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• v.38 no.4
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• pp.434-440
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• 2014

We prepared nanoparticles containing insoluble celecoxib by the method of solid dispersions using a spray dryer to improve solubility of celecoxib. We used PVP K30 and Eudragit EPO as water-soluble carriers for the solid dispersion, and poloxamer 407 as a surfactant. Characterization of celecoxib solid dispersion was performed by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). The results of SEM, DSC and XRD demonstrated that celecoxib is amorphous in solid dispersion. The dissolution rate measured in intestinal juice showed that the method of solid dispersion improved celecoxib solubility as compared with a conventional drug (Celebres$^{(R)}$). In conclusion, solid dispersion formulation prepared by a spray dryer would improve the solubility of celecoxib in oral administration.

• Korean Journal of Pharmacognosy
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• v.36 no.2 s.141
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• pp.109-115
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• 2005

The herb of Allium victorialis var. platyphyllum (Liliaceae) has been used as an edible wild herb and to treat heart failure and gastritis. We have already reported antihyperlipidemic anti-tumor effects of this plant. To enlarge the commercial availability of this food, it was investigated whether the extracts of A. victorialis var. platyphyllum reduce hyperlipidemia and obesity or not. The plants tested in this experiment were collected from two eco-types of Is. Ullung and Mt. Odae cultivated at Pyongchang. Extracts were prepared by extracting the fresh leaves and those dried at $36^{\circ}C$ and $90^{\circ}C$, respectively. Pretreatment with the ethanolic extracts for two weeks(p.o.) reduced serum triglyceride-, total cholesterol- and LDL-cholesterol contents in rats induced by Triton WR-1339, respectively. Furthermore, oral administration of the extracts also inhibited the hyperlipidemia induced with oral diet of 30% corn oil. In the other attempt to find to alleviate the obesity, the model rats with obesity were induced by the high fat-diet for six weeks. Post-treatment with the extracts for two weeks significantly reduced the hyperlipidemia. Retroperitoneal-, epidymal- and total abdominal fat pad weights were considerably reduced at 100 mg/kg oral administration of the extracts. Increased feces lipid contents were also found in the rat treated with the extracts. The extract may lead to the higher activity in treatment of hyperlipidemia and obesity than of the dried one.

• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.167-172
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• 2000

The purpose of this study is to develop a transurethral liquid suppository containing prostaglandin $E_1\;(PGE_1)-loaded$ microemulsion, which undergoes a phase transition to gels at body temperature. The effects of oils, ethanol as solvent and HCl as pH-controlling agent on the physicochemical properties of liquid suppositories composed of poloxamer P 407, P 188 and carbopol was investigated. The stability of $PGE_1$ and release of $PGE_1$ from liquid suppository were evaluated. Oils such as Neobee and soybean oil significantly decreased the gelation temperature but increased the gel strength of liquid suppository due to their strongly binding with the components of liquid suppository base. However, ethanol slightly did the opposite. The pH of liquid suppositories hardly affected the gelation temperature and gel strength due to addition of very small HCl (0.005-0.01%). A liquid suppository [$PGE_1/P$ 407/P 188/carbopol/Neobee/ethanol/HCl (0.2/14/14/0.4/7/2/0.005%)], which had the gelation temperature $(34.2{\pm}0.6^{\circ}C)$ and gel strength $(31.35{\pm}4.37\;sec)$ suitable for liquid suppository system, was easily administered and not leak out from the body. About 60% of $PGE_1$ was released out within 2 h from this formulation. It was shown that the release of $PGE_1$ was proportional to the square root of time, indicating that $PGE_1$ might be released from the suppository by Fickian diffusion. It was stable at $4^{\circ}C$ for at least 2 months. The results suggest that transurethral liquid suppository containing prostaglandin $E_1-loaded$ microemulsion is thought to be a convenient, safe and effective dosage form for $PGE_1$. However, it should be further developed as a more convenient and stable dosage form for $PGE_1$.

• Polymer(Korea)
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• v.33 no.6
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• pp.596-601
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• 2009

We prepared nanoparticles containing insoluble aceclofenac by the method of solid dispersions using spray dryer to improve solubility of aceclofenac. We used PVP-K30 as a water soluble carrier for the solid dispersion and poloxamer as a surfactant. Characterization of aceclofenac solid dispersion was performed by SEM, DSC, XRD and FT-IR. The results of SEM, DSC and XRD demonstrated that aceclofenac is amorphous in solid dispersion. The formation of salt by hydrogen bond between aceclofenac and PVP K-30 was confirmed by FT-IR. The dissolution rate measured in intestinal juice showed the method of solid dispersion improved aceclofenac solubility as compared with a conventional drug($Airtal^{(R)}$). In conclusion, the method of solid dispersion using spray dryer would improve solubility of aceclofenac in oral administration.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.6
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• pp.708-713
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• 2008

The effects of administration alone or mixed of Angelica keiskei and turmeric extract on blood lipids were evaluated in hypercholesterolemic diet or P-407-induced hyperlipidemic rats. In the study 1, female Sprague-Dawley rats weighing 160-180 g were divided into each groups and fed high cholesterol diets for 8 weeks. Experimental groups were administered with following diets: basal diet (Normal), high cholesterol diets (1% cholesterol). We did the oral administration for evaluation in experimental groups: C (vehicle), A (angelica extract), T (turmeric extract), AT (angelica extract, turmeric extract/ 1:1 complex). The concentrations of serum total cholesterol, and LDL-cholesterol were decreased by 6.8%, 9.8% in A group, by 22.1%, 28.8% in C group and by 28.2%, 35.6% in AT group, compared to the C group, respectively. HDL-cholesterol levels were not different among the experimental groups. In the study 2, we induced the hypertriglyceridemia in rats by intraperitoneal injection of P-407 (0.5 g/kg) once per three days. From the next day after P-407 injection beginning, we did the oral administration as the study 1. Angelica keiskei extract, turmeric extract and complex extract decreased serum triglyceride by 17.2%, 19.7% and 48.3%, respectively. These results suggested that Angelica keiskei and turmeric extract complex might have synergistic effect in lowering total cholesterol, LDL-cholesterol and triglyceride in hyperlipidemic rats.