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1.
Heliyon ; 10(6): e28066, 2024 Mar 30.
Article in English | MEDLINE | ID: mdl-38524612

ABSTRACT

Luteolin is a potent anti-colorectal cancer chemical. However, its effectiveness is hindered by its poor solubility in water and fat, and it is easy to degrade by gastrointestinal enzymes. In this study, a nano-composite carrier, NH2-MIL-101(Fe)@GO (MG), based on aminated MIL-101(Fe) and graphene oxide (GO) was developed and evaluated. This carrier co-delivered luteolin and matrine, while marine was used to balance the pH for the nano-preparation. The loading capacities for luteolin and matrine were approximately 9.8% and 14.1%, respectively. Luteolin's release at pH = 5 was significantly higher than at pH = 7.4, indicating it had an acidic pH response release characteristic. Compared to MOF and GO alone, MG and NH2-MIL-101(Fe)@GO@Drugs (MGD) enhanced anti-cancer activity by inhibiting tumor cell migration, increasing ROS generation, and upregulating the expression of Caspase-3 and Caspase-9. In conclusion, this study contributes new ideas and methods to the treatment strategy of multi-component anti-colorectal cancer therapy. It also advances drug delivery systems and supports the development of more effective and targeted treatment approaches for colorectal cancer.

2.
Membranes (Basel) ; 12(3)2022 Mar 01.
Article in English | MEDLINE | ID: mdl-35323760

ABSTRACT

This study examined the behavior and penetration mechanisms of typical phenolic (benzoic) acids, which determine their observed penetration rates during membrane separation, focusing on the influence of electrostatic and hydrophobic solute/membrane interactions. To understand the effects of hydrophobicity and electrostatic interaction on membrane filtration, the observed penetration of five structurally similar phenolic acids was compared with regenerated cellulose (RC) and polyamide (PA) membranes at different solute concentrations and solution pHs. Variation partitioning analysis (VPA) was performed to calculate the relative contributions of electrostatic and hydrophobic effects. The penetration of phenolic acids was mainly influenced by the electrostatic interaction, with salicylic acid having the highest penetration. Penetration of phenolic acids through the PA membrane decreased from 98% at pH 3.0 to 30-50% at pH 7.4, indicating the dominance of the electrostatic interaction. Moreover, based on its hydrophobicity and greater surface charge, the PA membrane could separate binary mixtures of protocatechuic/salicylic acid and 4-hydroxybenzoic/salicylic acid at pH 9.0, with separation factors of 1.81 and 1.78, respectively. These results provide a greater understanding of solute/membrane interactions and their effect on the penetration of phenolic acids through polymeric ultrafiltration membranes.

3.
Zhongguo Zhong Yao Za Zhi ; 45(1): 106-112, 2020 Jan.
Article in Chinese | MEDLINE | ID: mdl-32237418

ABSTRACT

To explore the permeation mechanism of micro-molecule medicinal ingredients of water extract of tradition Chinese medicine(TCM) in membrane separation process. With phenolic acid components as the model solute, five phenolic acids with similar molecular weight and structure, namely gallic acid, protocatechuate acid, 4-hydroxybenzoic acid, 3-hydroxybenzoic acid and salicylic acid, were selected in the PES membrane separation experiments. With the relative flux and the transmission rate as indexes, the scanning electron microscopy(SEM) and the electrochemical impedance spectroscopy(EIS) were used to analyze the permeation mechanism of different phenolic acid components. The results showed phenolic acids with similar molecular weight had different permeation behaviors, with decreased relative flux and increased solute permeation with the increase of solute concentration. According to the permeation behavior analyzed by the molecular structure of solute, the transmission rate of phenolic acids increased with the increase of the number of hydroxyl, and the order of substituent positions of phenolic acids based on the permeation rate as follows: para-substituted > meta-substitution > ortho-substitution. Electrochemical impedance spectroscopy reflected the role of charge repulsion in the membrane process; that is to say, the greater the resistance is, the less the solute permeation is. Therefore, the permeation phenomenon of the phenolic acid components in the PES membrane is not only the result of simple sieving mechanisms, but also has the effects of steric hindrance and charge repulsion during the membrane process.


Subject(s)
Drugs, Chinese Herbal/analysis , Hydroxybenzoates/isolation & purification , Membranes, Artificial , Medicine, Chinese Traditional , Molecular Structure , Molecular Weight
4.
Zhongguo Zhong Yao Za Zhi ; 43(8): 1642-1648, 2018 Apr.
Article in Chinese | MEDLINE | ID: mdl-29751711

ABSTRACT

To investigate the feasibility of vapor permeation membrane technology in separating essential oil from oil-water extract by taking the Forsythia suspensa as an example. The polydimethylsiloxane/polyvinylidene fluoride (PDMS/PVDF) composite flat membrane and a polyvinylidene fluoride (PVDF) flat membrane was collected as the membrane material respectively. Two kinds of membrane osmotic liquids were collected by self-made vapor permeation device. The yield of essential oil separated and enriched from two kinds of membrane materials was calculated, and the microscopic changes of membrane materials were analyzed and compared. Meanwhile, gas chromatography-mass spectrometry (GC-MS) was used to compare and analyze the differences in chemical compositions of essential oil between traditional steam distillation, PVDF membrane enriched method and PDMS/PVDF membrane enriched method. The results showed that the yield of essential oil enriched by PVDF membrane was significantly higher than that of PDMS/PVDF membrane, and the GC-MS spectrum showed that the content of main compositions was higher than that of PDMS/PVDF membrane; The GC-MS spectra showed that the components of essential oil enriched by PVDF membrane were basically the same as those obtained by traditional steam distillation. The above results showed that vapor permeation membrane separation technology shall be feasible for the separation of Forsythia essential oil-bearing water body, and PVDF membrane was more suitable for separation and enrichment of Forsythia essential oil than PDMS/PVDF membrane.


Subject(s)
Forsythia , Oils, Volatile , Distillation , Steam , Water
5.
J Pharm Biomed Anal ; 151: 75-83, 2018 Mar 20.
Article in English | MEDLINE | ID: mdl-29310050

ABSTRACT

Alzheimer's disease (AD) is a progressive neurodegenerative disease with neither definitive pathogenesis nor effective treatment method so far. Huang-Lian-Jie-Du-Tang (HLJDT) is a classic formula of traditional Chinese medicine (TCM) proven to have ameliorative effects on learning and memory deficits of dementia. Morris water maze (MWM) test and pathology analysis have demonstrated that HLJDT could ameliorate learning and memory deficits in AD mouse model, which may act via its anti-neuroinflammation properties. According to our previous studies, an UPLC-QTOF/MS-based metabolomics approach was performed to explore the potential mechanisms of HLJDT on preventing AD. As a result, a total of 23 potential metabolites (VIP >1, |Pcorr| >0.58, CUFjk excludes 0, P < 0.05) contributing to AD progress were identified. The metabolic pathway analysis with MetPA revealed that glycerophospholipid metabolism, sphingolipid metabolism, arachidonic acid metabolism, linoleic acid metabolism and tryptophan metabolism were disturbed in mouse model of AD. After HLJDT treatment, 14 metabolites were restored back to the control-like levels.


Subject(s)
Alzheimer Disease/blood , Drugs, Chinese Herbal/metabolism , Metabolomics/methods , Tandem Mass Spectrometry/methods , Alzheimer Disease/drug therapy , Alzheimer Disease/genetics , Animals , Chromatography, High Pressure Liquid/methods , Drugs, Chinese Herbal/pharmacology , Drugs, Chinese Herbal/therapeutic use , Male , Maze Learning/drug effects , Maze Learning/physiology , Medicine, Chinese Traditional/methods , Mice , Mice, Transgenic , Random Allocation , Treatment Outcome
6.
Drug Deliv Transl Res ; 8(1): 83-96, 2018 02.
Article in English | MEDLINE | ID: mdl-29134552

ABSTRACT

Alpha-asarone is a bioactive component of Acorus tatarincuii Schott with low bioavailability, which is often used for treatments of various brain diseases in clinical setting. This study was to formulate biodegradable methoxy polyethylene glycol-polylactic acid (mPEG-PLA) nanoparticles (NPs) surface-modified by lactoferrin (Lf), for delivering α-asarone into the brain following intranasal administration. Alpha-asarone NPs were prepared by premix membrane emulsification. The relative parameters were optimized by a Box-Behnken experimental design. The particle size, zeta potential, and dispersibility index of NPs and Lf-NPs were characterized. Their ex vivo permeation, pharmacokinetics, distribution in the brain and other tissue, brain targeting, and toxicity were investigated. Following intranasal administration, Lf-NPs had a better permeability and no significant poor bioavailability compared to NPs; the area under curve from 0 to 12 h of α-asarone in Lf-NPs of the olfactory bulb, hippocampus, olfactory bundles, and thalamus were 2.14-, 4.17-, 3.62-, and 1.96-fold of those in NP group, respectively. Lactoferrin could enhance the efficacy of brain targeting with NPs and reduce its liver accumulation. Toxicity of NPs on nasal mucosal cilia and epithelial cells was also decreased by Lf. To summarize, these results demonstrate that Lf-NPs of α-asarone have potential as a carrier for nose-to-brain delivery of α-asarone for brain diseases.


Subject(s)
Anisoles/administration & dosage , Brain/metabolism , Drug Delivery Systems , Lactoferrin/administration & dosage , Nanoparticles/administration & dosage , Polyesters/administration & dosage , Polyethylene Glycols/administration & dosage , Administration, Intranasal , Allylbenzene Derivatives , Animals , Anisoles/pharmacokinetics , Cilia/drug effects , Emulsions , Female , Lactoferrin/pharmacokinetics , Lactoferrin/toxicity , Male , Microscopy, Electron, Scanning , Nanoparticles/toxicity , Nasal Mucosa/drug effects , Nasal Mucosa/metabolism , Nasal Mucosa/pathology , Nasal Mucosa/ultrastructure , Polyesters/pharmacokinetics , Polyesters/toxicity , Polyethylene Glycols/pharmacokinetics , Polyethylene Glycols/toxicity , Rabbits , Rats, Sprague-Dawley , Tissue Distribution
7.
Zhongguo Zhong Yao Za Zhi ; 40(6): 1091-6, 2015 Mar.
Article in Chinese | MEDLINE | ID: mdl-26226751

ABSTRACT

Tetradrine-tashionone II(A)-PLGA composite microspheres were prepared by the SPG membrane emulsification method, and the characterization of tetradrine-tashionone II(A) -PLGA composite microspheres were studied in this experiment. The results of IR, DSC and XRD showed that teradrine and tashionone II(A) in composite microspheres were highly dispersed in the PLGA with amorphous form. The results of tetradrine-tashionone II(A) -PLGA composite microspheres in vitro release experiment showed that the cumulative release amounts of tetradrine and tashionone II(A) were 6.44% and 3.60% in 24 h, and the cumulative release amounts of tetradrine and tashionone II(A) were 89.02% and 21.24% in 17 d. The process of drug in vitro release accorded with the model of Riger-Peppas. Tetradrine-tashionone II(A) -PLGA composite microspheres had slow-release effect, and it could significantly reduce the burst release, prolong the therapeutic time, decrease the dosage of drugs and provide a new idea and method to prepare traditional Chinese medicine compound.


Subject(s)
Benzofurans/chemistry , Benzylisoquinolines/chemistry , Drug Carriers/chemistry , Drug Compounding/methods , Drugs, Chinese Herbal/chemistry , Lactic Acid/chemistry , Polyglycolic Acid/chemistry , Drug Compounding/instrumentation , Kinetics , Microspheres , Particle Size , Polylactic Acid-Polyglycolic Acid Copolymer
8.
Zhongguo Zhong Yao Za Zhi ; 40(24): 4847-52, 2015 Dec.
Article in Chinese | MEDLINE | ID: mdl-27245033

ABSTRACT

Taking α-asarone as model drug, mono methoxy polyethylene glycol-polylactic acid copolymer (mPEG-PLA) as the drug carrier material to prepare drug-loading nanoparticles by premix membrane emulsification for nasal administration. The prepared nanoparticles were spherical with smooth surface and average particle size of 360 nm. Polydispersity index (PDI) was 0. 030, average drug loading of (11.5 ± 0.045) % (n = 3), and the encapsulation efficiency of (86.34 ± 0.11) % (n = 3). X-ray diffraction and differential scanning calorimetry results showed that, α-asarone existed in mPEG-PLA carrier in amorphous or molecular state, different from simple physical mixture. In the in vitro release test in simulated human nasal cavity, α-asarone apis can be released quickly at close to 94% at 102 h, in line with the first-order kinetics (R² = 0.981 9). mPEG-PLA drug-loading nanoparticles release only 54%, with slow release effect, in line with Riger-Peppas model (R² = 0.967 9, n = 0.630 2), for non-fick diffusion, released by the spread of drugs and skeleton dissolution dual control. This provided the foundation for nasal drug delivery in vivo pharmacokinetic study.


Subject(s)
Anisoles/chemistry , Nanoparticles/chemistry , Polyesters/chemistry , Polyethylene Glycols/chemistry , Administration, Intranasal , Allylbenzene Derivatives , Calorimetry, Differential Scanning , Solubility , X-Ray Diffraction
9.
Zhongguo Zhong Yao Za Zhi ; 39(9): 1728-32, 2014 May.
Article in Chinese | MEDLINE | ID: mdl-25095393

ABSTRACT

Resource of traditional Chinese medicine residue is an inevitable choice to form new industries characterized of modem, environmental protection and intensive in the Chinese medicine industry. Based on the analysis of source and the main chemical composition of the herb residue, and for the advantages of membrane science and technology used in the pharmaceutical industry, especially membrane separation technology used in improvement technical reserves of traditional extraction and separation process in the pharmaceutical industry, it is proposed that membrane science and technology is one of the most important choices in technological design of traditional Chinese medicine resource industrialization. Traditional Chinese medicine residue is a very complex material system in composition and character, and scientific and effective "separation" process is the key areas of technology to re-use it. Integrated process can improve the productivity of the target product, enhance the purity of the product in the separation process, and solve many tasks which conventional separation is difficult to achieve. As integrated separation technology has the advantages of simplified process and reduced consumption, which are in line with the trend of the modern pharmaceutical industry, the membrane separation technology can provide a broad platform for integrated process, and membrane separation technology with its integrated technology have broad application prospects in achieving resource and industrialization process of traditional Chinese medicine residue. We discuss the principles, methods and applications practice of effective component resources in herb residue using membrane separation and integrated technology, describe the extraction, separation, concentration and purification application of membrane technology in traditional Chinese medicine residue, and systematically discourse suitability and feasibility of membrane technology in the process of traditional Chinese medicine resource industrialization in this paper.


Subject(s)
Drugs, Chinese Herbal/isolation & purification , Medicine, Chinese Traditional/methods , Membranes, Artificial , Technology, Pharmaceutical/methods , Biomedical Research/instrumentation , Biomedical Research/methods , Biomedical Research/trends , China , Drugs, Chinese Herbal/therapeutic use , Humans , Medicine, Chinese Traditional/instrumentation , Medicine, Chinese Traditional/trends , Phytotherapy/instrumentation , Phytotherapy/methods , Phytotherapy/trends , Technology, Pharmaceutical/instrumentation , Technology, Pharmaceutical/trends
10.
Eur J Pharm Sci ; 63: 63-70, 2014 Oct 15.
Article in English | MEDLINE | ID: mdl-25008114

ABSTRACT

The goal of the present paper is to compare the distributions of α-asarone administered to rats through three different routes: oral, intravenous and intranasal. The concentrations of α-asarone in seven distinct brain regions, the olfactory bulb, cerebellum, hypothalamus, frontal cortex, striatum, hippocampus and medulla/pons as well as in plasma and cerebrospinal fluid (CSF), were determined by HPLC. The quantities of α-asarone accumulated in liver were measured to determine whether α-asarone could generate hepatotoxicity when administered via the three different routes. The results indicated that α-asarone could be absorbed via two different routes into the brain, after intranasal administration of dry powders. In the systemic route, α-asarone immediately entered the brain through the blood-brain barrier (BBB) after uptake into the circulatory system. In the olfactory bulb route, α-asarone traveled from the olfactory epithelium in the nasal cavity straight into brain tissue via the olfactory bulb. Furthermore, intranasal administration of α-asarone as a dry powder can ensure quick absorption and avoid excessive concentrations in the blood and liver, while achieving concentrations in the brain comparable to those attained by intravenous and oral administration routes.


Subject(s)
Anisoles/administration & dosage , Anisoles/pharmacokinetics , Brain/metabolism , Administration, Intranasal , Administration, Intravenous , Administration, Oral , Allylbenzene Derivatives , Animals , Anisoles/chemistry , Chromatography, High Pressure Liquid , Male , Rats , Rats, Sprague-Dawley , Tissue Distribution
11.
Am J Chin Med ; 42(2): 393-407, 2014.
Article in English | MEDLINE | ID: mdl-24707870

ABSTRACT

Huanglian-Zhizi couplet medicine comes from classical prescription Huang-Lian-Jie-Du-Tang (HLJDT), which has been proven by previous researches to be an effective compound for cerebral ischemia. This paper explores the integrated pharmacokinetics of gardenia acid and geniposide-time-antioxidant efficacy after the oral administration of Huanglian-Zhizi couplet medicine from HLJDT in rats with middle cerebral artery occlusion (MCAO). To investigate the differences in pharmacokinetics and antioxidant effect of Huanglian-Zhizi and HLJDT in MCAO rats, which have been scarcely reported, an oral dose, 24 crud drug g/kg, of Huanglian-Zhizi and 40 crud drug/kg of HLJDT were administered in two groups of normal rats and two groups of Sprague-Dawley (SD) MCAO rats, respectively. At different time points, concentrations of gardenia acid and geniposide were determined by high performance liquid chromatography (HPLC), and levels of superoxide dismutase (SOD) were calculated by ELIASA. Pharmacokinetic parameters including AUC, MRT, t1/2, T max , C max were estimated by statistical moment analysis using a data analysis system (DAS) 2.0. An AUC based on weighting approach was used for integrating gardenia acid and geniposide. Finally, the concentration-time efficacy profiles were obtained. The integrated pharmacokinetics profiles of index components could reveal the pharmacokinetics behavior of Huanglian-Zhizi and HLJDT, corresponding to the antioxidant efficacy.


Subject(s)
Antioxidants , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/pharmacology , Infarction, Middle Cerebral Artery/drug therapy , Infarction, Middle Cerebral Artery/metabolism , Iridoids/pharmacokinetics , Phytotherapy , Administration, Oral , Animals , Chromatography, High Pressure Liquid , Disease Models, Animal , Dose-Response Relationship, Drug , Drugs, Chinese Herbal/pharmacokinetics , Enzyme-Linked Immunosorbent Assay , Iridoids/pharmacology , Rats, Sprague-Dawley , Superoxide Dismutase/metabolism , Time Factors
12.
Yao Xue Xue Bao ; 49(11): 1607-13, 2014 Nov.
Article in Chinese | MEDLINE | ID: mdl-25757290

ABSTRACT

For effective inhalable dry-powder drug delivery, tetrandrine-PLGA (polylactic-co-glycolic acid) nanocomposite particles have been developed to overcome the disadvantages of nanoparticles and microparticles. The primary nanoparticles were prepared by using premix membrane emulsification method. To prepare second particles, they were spray dried. The final particles were characterized by scanning electron microscopy (SEM), dry laser particle size analysis, high performance liquid chromatography (HPLC), X-ray diffraction (XRD), differential scanning calorimetry (DSC), infrared analysis (IR) and confocal laser scanning microscope (CLSM). The average size of the primary particles was (337.5 ± 6.2) nm, while that second particles was (3.675 ± 0.16) µm which can be decomposed into primary nanoparticles in water. And the second particles were solid sphere-like with the drug dispersed as armorphous form in them. It is a reference for components delivery to lung in a new form.


Subject(s)
Benzylisoquinolines/chemistry , Lactic Acid/chemistry , Nanocomposites/chemistry , Polyglycolic Acid/chemistry , Administration, Inhalation , Calorimetry, Differential Scanning , Drug Delivery Systems , Dry Powder Inhalers , Microscopy, Electron, Scanning , Nanoparticles/chemistry , Particle Size , Pharmaceutical Preparations , Polylactic Acid-Polyglycolic Acid Copolymer , X-Ray Diffraction
13.
Zhongguo Zhong Yao Za Zhi ; 39(23): 4583-9, 2014 Dec.
Article in Chinese | MEDLINE | ID: mdl-25911806

ABSTRACT

Relatively uniform-sized nanoparticles made of poly (lactic-co-glycolic acid) (PLGA) were prepared by premix membrane emulsification method. After the drug loading property was completed, the dynamic tissue distribution of nanoparticles was recorded. With the average particle size and span as indexes, membrane pore size, number of passing membrane times, membrane pressure, volume ratio of oil-water phase and the concentration of poly(vinyl alcohol) (PVA) in external water phase were investigated by single factor test, the optimum preparation technology of blank PLGA nanlparticles was as following: pore size of SPG membrane was 1 µm, membrane pressure was 1. 15 MPa, the number of passing membrane time was 3, the mass fraction of PVA of 2%, volume ratio of oil-water phase of 1 : 5. Prepared nanoparticles were round with smooth surface, the mean diameter was 332.6 nm, span was 0.010, the confocal laser scanning microscope (CLSM) concluded that fluorescent substance is uniform composizion in PLGA nanoparticle, and the in vivo imaging technology in mice include that the nanoparticles show good liver and spleen targeting property.


Subject(s)
Drug Delivery Systems/instrumentation , Fluorescent Dyes/chemistry , Lactic Acid/chemistry , Nanoparticles/chemistry , Polyglycolic Acid/chemistry , Animals , Drug Carriers/chemistry , Emulsions/chemistry , Mice , Mice, Nude , Particle Size , Polylactic Acid-Polyglycolic Acid Copolymer
14.
Article in English | MEDLINE | ID: mdl-24367386

ABSTRACT

Huang-Lian-Jie-Du-Tang (HLJDT), a classical Chinese prescription, has been clinically employed to treat cerebral ischemia for thousands of years. Geniposide is the major active ingredient in HLJDT. The aim is to investigate the comparative evaluations on pharmacokinetics of geniposide in MCAO rats in pure geniposide, geniposide : berberine, and geniposide : berberine : baicalin. Obviously, the proportions of geniposide : berberine, geniposide : baicalin, and geniposide : berberine : baicalin were determined according to HLJDT. In our study, the cerebral ischemia model was reproduced by suture method in rats. The MCAO rats were randomly assigned to four therapy groups and orally administered with different prescription proportions of pure geniposide, geniposide : berberine, geniposide : baicalin, and geniposide : berberine : baicalin, respectively. The concentrations of geniposide in rat serum were determined using HPLC, and main pharmacokinetic parameters were investigated. The results indicated that the pharmacokinetics of geniposide in rat serum was nonlinear and there were significant differences between different groups. Berberine might hardly affect the absorption of geniposide, and baicalin could increase the absorption ability of geniposide. Meanwhile, berberine could decrease the absorption increase of baicalin on geniposide.

15.
Zhongguo Zhong Yao Za Zhi ; 38(12): 2033-8, 2013 Jun.
Article in Chinese | MEDLINE | ID: mdl-24066607

ABSTRACT

In the principle of "correspondence of prescription and syndrome", this article focuses on key technical issues of traditional Chinese medicine (TCM) biopharmaceutis by using the integrated pharmacokinetic and pharmacodynamic model: (1) As the prescription formulation and compatibility of TCM compounds could be influential to the in vivo pharmacokinetics of chemical components of TCMs, and closely related to therapeutic and adverse effects, how to describe these actions in a biopharmaceutics model? (2) As there are differences between pharmacokinetic processes in the normal and pathological states, how to express characteristic "syndromes" in an animal model? (3) As prescriptions work to reduce and transform syndromes, how o confirm the type and amount of effective substances in case of physiological and pathological indicators and drug distribution in a dynamic corresponding state. In response to the above key issues, we proposed the TCM biopharmaceutic study model based on PK/PD. (1) The integrity of TCMs was better expressed with the effect at the core, supplemented with the component pharmacokinetics; (2) An integrated pharmacokinetic and pharmacodynamic system was established on the basis of pharmacokinetics and pharmacodynamics of many major effective components; (3) AK/PD mathematical function with the three-phase synchronous characterization of "time-concentration-effect" was established by using the data mining techniques, to explore the biopharmaceutic principle of "correspondence of prescriptions and syndromes", in which prescriptions are only required for syndromes, whereas no prescription is required in case of no syndrome.


Subject(s)
Medicine, Chinese Traditional , Models, Biological , Pharmacokinetics , Humans , Syndrome
16.
Phytomedicine ; 20(10): 767-74, 2013 Jul 15.
Article in English | MEDLINE | ID: mdl-23628154

ABSTRACT

Our previous studies showed that after oral administration of an Huang-Lian-Jie-Du-Tang (HLJDT) decoction, there is a higher concentration of the pure components, berberine, baicalin and gardenoside in the plasma of Middle cerebral artery occlusion (MCAO) rats than in sham-operated rats, The aim of the present study was to determine whether these components could be reliably measured in MCAO rat tissues. First, the plasma concentration-time profiles of berberine, palmatine, baicalin, baicalein and gardenoside were characterised in MCAO rats after oral administration of the aqueous extract of HLJDT. Subsequently, liver, lung and kidney tissues were obtained from sudden death MCAO rats in the absorption phase (0.25 h), the distribution phase (1.0 h) and the elimination phase (8.0 h) after administration of the HLJDT aqueous extract. An HPLC method was developed and validated for the determination of the distribution characteristics of berberine, palmatine, baicalin, baicalein and gardenoside simultaneously from the above-mentioned rat tissues. The results indicated that berberine, palmatine, baicalin and baicalein distributed rapidly and accumulated at high levels in the lung, while gardenoside distributed widely in the lung and the kidney. To the best of our knowledge, this is the first report to describe the distribution of the active ingredients derived from HLJDT in MCAO rat tissues. The tissue distribution results provide a biopharmaceutical basis for the design of the clinic application of HLJDT in cerebrovascular disease.


Subject(s)
Drugs, Chinese Herbal/pharmacokinetics , Infarction, Middle Cerebral Artery/drug therapy , Animals , Berberine/pharmacokinetics , Berberine/therapeutic use , Berberine Alkaloids/pharmacokinetics , Berberine Alkaloids/therapeutic use , Drugs, Chinese Herbal/therapeutic use , Flavanones/pharmacokinetics , Flavanones/therapeutic use , Flavonoids/pharmacokinetics , Flavonoids/therapeutic use , Iridoids/pharmacokinetics , Iridoids/therapeutic use , Male , Rats , Rats, Sprague-Dawley , Tissue Distribution
17.
Fitoterapia ; 88: 50-75, 2013 Jul.
Article in English | MEDLINE | ID: mdl-23602902

ABSTRACT

Recent studies have focused more on Chinese medicine used for the treatment of cerebrovascular disease. The current review covers researches on the pharmacokinetics of Chinese medicine, providing a convenient reference for researchers to increase efficiency of drug discovery, by compiling and discussing the pharmacokinetics of four classical Chinese medicines for therapy of cerebrovascular disease containing: Panax notoginseng, Salvia miltiorrhiza, Ligusticum Chuanxiong and Gardenia. It also helps to eliminate side effect as far as possible from inappropriate Chinese medicine usage. Current integrative and comprehensive review of Chinese medicine for cerebrovascular disease including 1) the absorption of some constituents is limited such as ginsenosides Rg1 and Rb1. It may be affected by gastric juice, first-pass effect, etc. 2) The interactions between Chinese medicine and prescription can occur. Borneol and carbomer would enhance the absorption of R1 and Rg1 in vivo by increasing adjacent cell transport ability. 3) The distribution of active constituents in brain is important for cerebrovascular disease. BBB protects brain from xenobiotic. Intranasal, intra-tympanic administration is a promising alternative to conventional administration to reach brain for ligustrazine. 4) Renal excretion is the uppermost route of these Chinese medicines. But biliary, fecal and urinary excretion are the other major routes. Theoretical and practical aspects are described with pharmacokinetic examples. In the end, this paper also discusses recent development of bio-analysis of Chinese medicine.


Subject(s)
Cerebrovascular Disorders/drug therapy , Drugs, Chinese Herbal/pharmacokinetics , Gardenia/chemistry , Ligusticum/chemistry , Panax notoginseng/chemistry , Phytotherapy , Salvia miltiorrhiza/chemistry , Blood-Brain Barrier , Drugs, Chinese Herbal/therapeutic use , Humans , Intestinal Absorption
18.
J Sep Sci ; 36(2): 383-90, 2013 Jan.
Article in English | MEDLINE | ID: mdl-23255314

ABSTRACT

The volatile oil parts of frankincense (Boswellia carterii Birdw.) were extracted with supercritical carbon dioxide under constant pressure (15, 20, or 25 MPa) and fixed temperature (40, 50, or 60°C), given time (60, 90, or 120 min) aiming at the acquisition of enriched fractions containing octyl acetate, compounds of pharmaceutical interest. A mathematical model was created by Box-Behnken design, a popular template for response surface methodology, for the extraction process. The response value was characterized by synthetical score, which comprised yields accounting for 20% and content of octyl acetate for 80%. The content of octyl acetate was determined by GC. The supercritical fluid extraction showed higher selectivity than conventional steam distillation. Supercritical fluid-CO(2) for extracting frankincense under optimum condition was of great validity, which was also successfully verified by the pharmacological experiments.


Subject(s)
Boswellia/chemistry , Chromatography, Supercritical Fluid/methods , Oils, Volatile/isolation & purification , Plant Oils/isolation & purification , Animals , Anti-Inflammatory Agents/analysis , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Carbon Dioxide , Chromatography, Gas , Chromatography, Supercritical Fluid/instrumentation , Female , Humans , Inflammation/drug therapy , Male , Mice , Mice, Inbred ICR , Oils, Volatile/analysis , Oils, Volatile/pharmacology , Plant Oils/analysis , Plant Oils/pharmacology
19.
J Ethnopharmacol ; 141(1): 158-69, 2012 May 07.
Article in English | MEDLINE | ID: mdl-22387241

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Huang-Lian-Jie-Du-Tang (HLJDT, or Oren-gedoku-to in Japanese), an important multi-herb remedy in China and other Asia countries, has been used clinically to treat cerebral ischemia for decades. MATERIALS AND METHODS: According to the previous studies we have reported, an HPLC method was developed and validated for determination of berberine, palmatine, baicalin, baicalein and geniposide simultaneously in MCAO rat plasma after administration of HLJDT aqueous extract. A classified integral pharmacokinetic method was put forward after having compared the integrated concentration-time profile with that of single component. An AUC based weighting approach was used for integrated principle. RESULTS: The results indicated the classified integral pharmacokinetic profile of index components from HLJDT could reveal the pharmacokinetic behavior of original components, and was corresponding to the holistic pharmacological effects of anti-ischemia with HLJDT. CONCLUSIONS: This study was aimed to explore an approach that could be applied to integrate the pharmacokinetic behavior of different components derived from HLJDT. The integrated pharmacokinetic results also provided more information for further understanding of the clinical cerebrovascular disease in use of HLJDT.


Subject(s)
Cardiovascular Agents/administration & dosage , Cardiovascular Agents/pharmacokinetics , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/pharmacokinetics , Infarction, Middle Cerebral Artery/drug therapy , Models, Biological , Administration, Oral , Animals , Area Under Curve , Biotransformation , Cardiovascular Agents/blood , Chromatography, High Pressure Liquid , Disease Models, Animal , Drug Stability , Infarction, Middle Cerebral Artery/blood , Male , Phytotherapy , Plants, Medicinal , Rats , Rats, Sprague-Dawley
20.
Molecules ; 17(2): 1319-34, 2012 Feb 01.
Article in English | MEDLINE | ID: mdl-22298116

ABSTRACT

Membrane separation is an alternative separation technology to the conventional method of filtration. Hence, it has attracted use in the purification and concentration of Chinese Herbal Medicine Extracts (CHMEs). The purpose of this work was to study the process of microfiltration of Tongbi liquor (TBL), a popular Chinese herbal drink, using ceramic membranes. Zirconium oxide and aluminum oxide membranes with pore mean sizes of 0.2 µm and 0.05 µm, respectively, are used for comparisons in terms of flux, transmittance of the ingredients, physical-chemical parameters, removal of macromolecular materials and fouling resistance. The results show that 0.2 µm zirconium oxide membrane is more suitable. The stable permeate flux reaches 135 L·h(-1)·m(-2), the cumulative transmittance of the indicator is 65.53%. Macromolecular materials, such as starch, protein, tannin, pectin and total solids were largely eliminated in retentate after filtration using 0.2 µm ZrO2 ceramic membrane, resulting in clearer TBL. Moreover, this work also reveals that continuous ultrasound could strengthen membrane process that the permeate flux increases significantly. This work demonstrates that the purification of CHME with ceramic membranes is possible and yielded excellent results.


Subject(s)
Filtration/methods , Medicine, Chinese Traditional , Membranes, Artificial , Aluminum Oxide/chemistry , Ultrasonics , Zirconium/chemistry
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