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1.
The purpose of the study was to develop a multiunit sustained release dosage form of diltiazem hydrochloride using a natural
polymer, sodium carboxymethyl xanthan gum and polyethyleneimine (PEI) from a completely aqueous environment. PEI treated diltiazem
resin complex loaded beads were characterized by morphology, drug entrapment efficiency, in vitro and in vivo release behaviour. 40% and 80% drug was released in 2 hour in pH 1.2 and in 5 to 6 h in pH 6.8 respectively depending on
the formulation variables. The prolonged release was attributed to decreased swelling of the beads due to PEI treatment. Maintaining
the shape throughout the dissolution process, PEI treated diltiazem resin complex beads released the drug following non-Fickian
transport phenomena. In vivo pharmacokinetic evaluation in rabbits shows slow and prolonged drug release when compared with diltiazem solution. The designed
beads are suitable for prolonged release of a water soluble drug under a complete aqueous environment using natural gum. 相似文献
2.
Paris polyphylla Smith var. yunnanensis extracts, Rhizoma Paridis saponins (RPS) have been found to show strong antitumor activity. However, few studies have yet
investigated pulmonary metastasis treatment with this herb. To detail the effective components in RPS and discuss the preliminary
mechanism of antitumor effects in vivo and in vitro, a mixture isolated from RPS was investigated. The main constituents were identified as polyphyllin D, formosanin C, dioscin,
Paris H, Paris VII and pennogennin 3-O-α-L-rhamnopyranosyl (1→4)-[β-L-rhamnopyranosyl (1→2)]-β-D-glucopyranoside. In our experiments,
LA795 cells were exposed to the mixed compounds. Migration inhibition was evaluated by wound healing assay and migration assay
in non-cytotoxic dose which was determined by MTT assay. The results demonstrated that the constituent in varying degrees
inhibited the migration of the tumor cells in vitro. The mixture also showed antitumor effects on carcinoma in vivo. In conclusion, the mixture is a potent anticancer agent that elicits programmed cell death and inhibits the migration in
murine lung adenocarcinoma, both in vitro and in vivo. 相似文献
3.
The pharmaceutical equivalence of Zantac (reference drug) and 10 domestic and foreign generics of ranitidine hydrochloride
as 150-mg coated tablets has been studied using the pharmacopoeic (USP 29) dissolution test. Analyses showed insignificant
differences in the excipients entering into the compositions of ranitidine generic tablets registered in Russia. It is established
that Zantac and generics of two manufacturers are rapidly soluble (according to the WHO classification). Analysis of the similarity
coefficients determined for the dissolution profiles measured in media with different pH values showed the biological nonequivalence
of some generics and the reference drug. It is demonstrated that the in vitro dissolution test recommended by WHO can be used for determining the bioequivalence of ranitidine generics. 相似文献
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6.
Yingqi Hua Zhiyu Zhang Jianxin Li Quan Li Shuo Hu Jian Li Mengxiong Sun Zhengdong Cai 《Investigational new drugs》2011,29(2):258-265
This study was undertaken to investigate the inhibitory effects of triterpenoid compound oleanolic acid and its synthetic
derivatives on osteosarcoma cells in order to identify new therapeutic candidates for the treatment of this disease. We used
the 3-(4,5-dimethyl-2 thiazolyl)-2,5-diphenyl tetrazolium bromide assay to assess the effect of oleanolic acid compounds on
the proliferation of osteosarcoma cells. The effect of dextrose-oleanolic acid (the most potent oleanolic acid derivative)
on apoptosis of osteosarcoma cells was evaluated using the Annexin-V method. The cell cycle of dextrose-oleanolic acid-treated
cells was examined by flow cytometry, and the in vivo effects of dextrose-oleanolic acid were evaluated in a mouse osteosarcoma model. Oleanolic acid compounds had an overall
inhibitory effect on the proliferation of osteosarcoma cells. Our in vitro data showed that the dextrose-oleanolic acid derivative brought about maximal inhibition of proliferation of osteosarcoma
cells while inducing apoptosis. It could also inhibit the growth of osteosarcoma and decreased the rate of lung metastasis
in vivo. Of the oleanolic acid derivatives, dextrose-oleanolic acid exhibited the most potent anti-osteosarcoma activity; it may
represent a new frontier in the treatment of osteosarcoma. 相似文献
7.
The anti-oxidant activities of tectochrysin, a major compound of propolis, were investigated. Tectochrysin exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl4-intoxication in rats. Tectochrysin tested exhibited a lipid peroxidation causing a significant decrease in MDA production in TBA-reactant assay. Tectochrysin was strong in the increase in the anti-oxidant enzymes such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase activities in CCl4-intoxicated rats. These results suggest that tectochrysin possess not only the anti-oxidant, but also the activities in CCl4-intoxicated rats. Especially, tectochrysin was found to cause significant increases in the rat liver cytosolic SOD, catalase, GSH-px activities as well as a significant decrease in the MDA production. 相似文献
8.
Sun-A. Im Young-Ran Lee Young-Hee Lee Myung-Koo Lee Young In Park Sungwon Lee Kyungjae Kim Chong-Kil Lee 《Archives of pharmacal research》2010,33(3):451-456
The gels of Aloe species contain immunomodulatory components such as aloctin A and acemannan. Most studies on these gels were performed in
in vitro cell culture systems. Although several studies examined their immunomodulatory activity in vivo, the route of administration was intraperitoneal or intramuscular. Here, we evaluated the in vivo immunomodulatory activity of processed Aloe vera gel (PAG) in mice. Oral administration of PAG significantly reduced the growth of C. albicans in the spleen and kidney following intravenous injection of C. albicans in normal mice. PAG administration also reduced the growth of C. albicans in streptozotocin-induced diabetic mice. PAG administration did not increase ovalbumin (OVA)-specific cytotoxic T lymphocyte
(CTL) generation in normal mice, but did increase it in high-fat-diet induced diabetic mice. These findings provide the first
clear evidence for the immunomodulatory activity of orally administered Aloe vera gel. 相似文献
9.
In the present study, an extended release pellet dosage form of ketoprofen was prepared using powder layering technique. A
combination of ethyl cellulose (45 cps) and shellac polymers was used as a binder (12% w/w polymer) during drug layering and
an extended release coating (1:3 ratio at 2%, 4% and 7% w/w polymer) within the same apparatus. The coated pellets were characterized
for sphericity, Hardness-Friability Index, and drug content, and also underwent scanning electron microscopy. In vitro dissolution was performed in 900 mL of phosphate buffer (pH 6.8) using paddle apparatus at 100 rpm. Ethyl cellulose and shellac
when used as binders during drug loading did not extend ketoprofen release beyond 3 h. However, coating of the drug loaded
pellets using ethyl cellulose and shellac resulted in an extended release profile of about 10 h. Using Higuchi’s model and
the Korsmeyer equation, the drug release mechanism from the pellets was found to be an anomalous type involving diffusion
and erosion. Scanning electron microscopy was used to visualize the pellet morphology and drug release mechanism during dissolution
testing. In vivo evaluations of the extended release pellets in rats indicated a significant increase in the time to reach maximum concentration
(tmax) and extent of absorption (AUC0-∞) compared to the ketoprofen immediate release tablet blend dispersed and dosed. In conclusion, extended release pellets of
ketoprofen could perform therapeutically better than conventional dosage forms, leading to improved efficacy for a prolonged
period. 相似文献
10.
Chun-Woong Park Yun-Seok Rhee Sung-Hoon Park Son Dao Danh Sung-Hoon Ahn Sang-Cheol Chi Eun-Seok Park 《Archives of pharmacal research》2010,33(3):427-432
Using the nano-composite deposition system (NCDS) as a microfabrication technique, implantable scaffolds were prepared with
poly(DL-lactide-co-glycolide)(85:15) [PLGA(85:15)] as a biodegradable polymer. 5-Fluorouracil (5-FU) was used as a model drug,
and hydroxyapatite (HA) was incorporated as a release modifier. In vitro drug release was evaluated and we confirmed that HA could control the release of drug from the prepared scaffolds, especially
in the initial phase of the release. Furthermore, in vivo tests demonstrated that the microfabricated scaffold with pores was useful in reducing immune response and maintained its
original shape, indicating that the drug delivery system was highly biocompatible. 相似文献
11.
Summary
Purpose: DDB (dimethyl-4,4′-dimethoxy-5,6,5′6′-dimethylene dioxybiphenyl-2,2′-dicarboxylate) is a synthetic hepatoprotectant which
has been widely used to treat chronic viral hepatitis B patients in China for more than 20 years. In this study, we evaluated
DDB as a multidrug resistance (MDR) chemosensitizing agent.
Methods: A panel of sensitive and resistant cancer cell lines were treated with various concentration of DDB, and the effect on chemosensitivity
and accumulation of anticancer drugs; promotion of apoptosis and P-glycoprotein (P-gp) expression were determined by MTT (Dimethyl
thiazolyl-2,5-diphenyltetrazolium bromide) assay, fluorospectrometry and flow cytometry respectively. Drug resistance reversal
activity of DDB was also examined in BALB/c nude mice bearing both acquired MDR human nasopharyngeal carcinoma KBv200 and
parental KB xenografts. The effect of DDB on the pharmacokinetics of Dox and hematological toxicity induced by Dox was measured
in ICR and C57/BL mice, respectively.
Results: DDB at nontoxic concentrations of 12.5, 25 and 50 μM partly reversed the resistance to vincristine, doxorubicin, paclitaxel
in acquired MDR breast carcinoma MCF-7/Adr cells, KBv200 and intrinsic MDR human hepatocarcinoma Bel7402 cells, whereas no chemosensitizing effect of DDB was observed in sensitive KB and MCF-7 cells. DDB increased the intracellular
accumulation of doxorubicin and inhibited surface P-gp expression in MCF-7/Adr cells. Furthermore, it was found that DDB promoted
doxorubicin-induced apoptosis of Bel7402 cells through enhanced caspase-3 activation. Co-administration of DDB at 300 and 500 mg/kg orally to nude mice increased
the antitumor activity of vincristine to KBv200 xenografts without a significant increase in toxicity. In contrast, Co-administration
of DDB did not inhibit the growth of KB xenografts. DDB also markedly reduced the decrease of leukocytes in doxorubicin-treated
C57/BL mice. Co-administration of DDB increased Dox concentration in ICR mice bearing S180 sarcoma, but no pharmacokinetical
interaction with Dox was observed.
Conclusion: These results indicate that DDB has MDR reversal activity by inhibiting P-gp and when used in combination with anti-cancer
drugs, it could potentially be used as a clinical treatment for P-gp-mediated MDR cancers. 相似文献
12.
M. R. Bhalekar K. P. Patil S. J. Kshirsagar S. Mohapatra 《Pharmaceutical Chemistry Journal》2011,45(8):503-508
Mucoadhesive microspheres of the novel polymer, xyloglucan, have been formulated and their performance characteristics have
been systematically evaluated in vitro and in vivo. The mucoadhesive microspheres were obtained by incorporating glipizide as model drug in xyloglucan as a mucoadhesive polymer
and sodium alginate as a gel-forming polymer by the orifice-ionic gelation method. A32 factorial design was employed to study the effect of independent variables, xyloglucan concentration (X
1
) and calcium chloride (CaCl2) concentration (X
2
), on the dependent variables including drug entrapment efficiency, release time (t
80), and percentage mucoadhesion in 1h. The best batch exhibited high drug entrapment efficiency (92.98%) and percentage mucoadhesion
(78% after 1h). The drug release was also controlled for more than 8 hours. In vivo testing of the mucoadhesive microspheres revealed significant hypoglycemic effect of glipizide. 相似文献
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14.
Three new ent-abietanoids, named xerophilusins XIV–XVI, and four known analogues, as well as four known chemical constituents were isolated
from the leaves of Isodon xerophilus. Their structures were elucidated by extensive spectroscopic studies, and comparison with literature data. In addition, the
cytotoxic activity of the ent-abietanoids against chronic myelogenous leukemia (K562), stomach adenocarcinoma (MKN45), and hepatocellular carcinoma (HepG2)
human cell lines was investigated and no activities were observed. 相似文献
15.
Haruka Asahina Junichi Shinozaki Kazuo Masuda Yasujiro Morimitsu Motoyoshi Satake 《Journal of natural medicines》2010,64(2):133-138
Species identification of five Dendrobium plants was conducted using phylogenetic analysis and the validity of the method was verified. Some Dendrobium plants (Orchidaceae) have been used as herbal medicines but the difficulty in identifying their botanical origin by traditional
methods prevented their full modern utilization. Based on the emerging field of molecular systematics as a powerful classification
tool, a phylogenetic analysis was conducted using sequences of two plastid genes, the maturase-coding gene (matK) and the large subunit of ribulose 1,5-bisphosphate carboxylase-coding gene (rbcL), as DNA barcodes for species identification of Dendrobium plants. We investigated five medicinal Dendrobium species, Dendrobium fimbriatum, D. moniliforme, D. nobile, D. pulchellum, and D. tosaense. The phylogenetic trees constructed from matK data successfully distinguished each species from each other. On the other hand, rbcL, as a single-locus barcode, offered less species discriminating power than matK, possibly due to its being present with little variation. When results using matK sequences of D. officinale that was deposited in the DNA database were combined, D. officinale and D. tosaense showed a close genetic relationship, which brought us closer to resolving the question of their taxonomic identity. Identification
of the plant source as well as the uniformity of the chemical components is critical for the quality control of herbal medicines
and it is important that the processed materials be validated. The methods presented here could be applied to the analysis
of processed Dendrobium plants and be a promising tool for the identification of botanical origins of crude drugs. 相似文献
16.
The aim of the current work was to design and develop matrix pellets of hydroxy propyl methyl cellulose K200M and microcrystalline
cellulose in an admixture for a mucoadhesive gastroretentive drug delivery system. Pellets containing metformin hydrochloride
(500 mg) were prepared by the pelletization technique using an extruder-spheronizer. Pellets were characterized by differential
scanning calorimetry (DSC), x-ray diffraction (XRD), scanning electron microscopy (SEM), circularity, roundness, percent drug
content, percent production yield, in vitro swelling, ex vivo mucoadhesion, in vitro drug release and in vivo x-ray imaging studies. Optimized pellets were sufficiently porous spheroids, free flowing, had smooth surfaces, had yields
up to 75.45 ± 0.52% and had drug content up to 96.45 ± 0.19%. The average particle size of formulations MF2 and MF6 were 1.13
± 0.41 mm and 1.22 ± 0.18 mm, respectively. Formulation MF6 exhibited strong adhesion, about 94.67%, to goat mucosal tissue,
and the desired in vitro swelling, with a sustained drug release profile for 12 h and with retention in the upper small intestine of rabbits for 10
h. We conclude that hydroxy propyl methyl cellulose K200M and microcrystalline cellulose at a 2.80:1.00 w/w ratio could be
an effective carrier for multiple unit controlled delivery of metformin hydrochloride. 相似文献
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18.
Bioassay-guided fractionation of the MeOH extract of Suaeda glauca yielded four phenolic compounds, methyl 3,5-di-O-caffeoyl quinate (1) and 3,5-di-O-caffeoyl quinic acid (2), isorhamnetin 3-O-beta-D-galactoside (3), and quercetin 3-O-beta-D-galactoside (4). Compounds 1 and 2 were hepatoprotective against tacrine-induced cytotoxicity in human liver-derived Hep G2 cells with the EC(50) values of 72.7+/-6.2 and 117.2+/-10.5 microM, respectively. Silybin as a positive control showed an EC(50) value of 82.4+/-4.1 microM. 相似文献
19.
Tanaka H Hattori H Tanaka T Sakai E Tanaka N Kulkarni A Etoh H 《Journal of natural medicines》2008,62(2):228-231
A new Erythrina alkaloid, 10-hydroxy-11-oxoerysotrine (1), has been isolated from the flowers of Erythrina herbacea together with five known compounds: erytharbine (2), 10,11-dioxoerysotrine (3), erythrartine (4), erysotramidine (5) and erysotrine-N-oxide (6). The structure of the new compound was elucidated on the basis of its spectral data, including 2-D NMR and mass (MS) spectra.
The new compound is a rare C-10 oxygenated Erythrina alkaloid. The antioxidant activities of the isolated compounds 1–6 were evaluated by scavenging with peroxynitrite. 相似文献
20.
Rezvan Yazdian-Robati Mohammad Ramezani Seyed Hamid Jalalian Khalil Abnous Seyed Mohammad Taghdisi 《Pharmaceutical research》2016,33(9):2289-2297