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Strigolactones(SLs) are a class of sesquiterpenoids derived from the carotenoid biosynthesis pathway with the core carbon skeleton consisting of tricyclic lactone(ABC tricyclic ring) and α,β-unsaturated furan ring(D ring). SLs are widely distributed in higher plants and are symbiotic signals between plants and Arbuscular mycorrhiza(AM), which play key roles in the evolution of plant colonizing terrestrial habitats. As a new type of plant hormone, SLs possess such important biological functions as inhibiting shoot branching(tillers), regulating root architecture, promoting secondary growth, and improving plant stress resistance. Therefore, SLs have attracted wide attention. The biological functions of SLs are not only closely related to the formation of "excellent shape and quality" of Chinese medicinal materials but also have important practical significance for the production of high-quality medicinal materials. However, SLs have been currently widely studied in model plants and crops such as Oryza sativa and Arabidopsis thaliana, and few related studies have been reported on SLs in medicinal plants, which need to be strengthened. This review focused on the latest research progress in the isolation and identification, biological and artificial synthesis pathways, biosynthesis sites and transport modes, signal transduction pathways and mechanisms, and biological functions of SLs, and prospected the research on the regulation mechanism of SLs in the growth and development of medicinal plants and their related application on targeted regulation of Chinese herbal medicine production, which is expected to provide some references for the in-depth research on SLs in the field of Chinese medicinal resources.
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Arabidopsis , Lactonas , Plantas MedicinalesRESUMEN
Based on the metabolomics, this paper systematically analyzed the metabolic substance basis of Zuogui Pills and Yougui Pills in syndrome differentiation and treatment of diminished ovarian reserve(DOR), so as to provide a scientific basis for the traditional Chinese medicine(TCM) syndrome differentiation and treatment of DOR. Patients with DOR of kidney-Yin deficiency syndrome were collected from outpatient department of hospitals and treated with Zuogui Pills for 12 weeks. And kidney-Yang deficiency syndrome were treated with Yougui Pills for 12 weeks. Based on the non-targeted metabolomic research techniques, the potential biomarkers of Zuogui Pills and Yougui Pills in the treatment of DOR with kidney-Yin deficiency and kidney-Yang deficiency, respectively, were screened out, and metabolic pathways of biomarkers were analyzed. The pregnancy rate, basic serum hormone levels [basal follicle-stimulating hormone(bFSH), basal-luteinizing hormone(bLH), basal-estradiol(bE_2), and anti-Müllerian hormone(AMH)], TCM syndrome type score, and Kupperman score were recorded and statistically analyzed after treatment. The results showed that 23 patients with DOR of kidney-Yin deficiency syndrome and 25 patients of kidney-Yang deficiency syndrome were collected. Twenty-six differential metabolites, including L-carnitine, acetyl-CoA, coenzyme A, and coenzyme Q_(10)(CoQ10), were mapped to 12 metabolic pathways in patients with kidney-Yin deficiency treated with Zuogui Pills. Twenty-two differential metabolites, such as adipoyl-CoA, L-lysine, lysine arginine, and α-tocopherol, were mapped to 11 metabolic pathways in patients with kidney-Yang deficiency. After treatment, bFSH and bLH of patients with DOR were significantly lower than those before treatment(P<0.05). Although the comparison of bE_2 and AMH had no significant differences, there was a improvement trend. The TCM syndrome type score and Kupperman score of patients with DOR after TCM treatment were significantly lower than those before treatment(P<0.05).
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The purpose of the study is to analyze the outcomes of randomized controlled trial(RCT) of Chinese herbal medicine formula(CHMF) in the treatment of gastrointestinal dysfunction in sepsis in recent two years. We systematically searched four Chinese databases, three English databases, and two clinical trial registries to analyze the reports of outcome indicators of clinical trials, and evaluated the risk of bias by using the ROB tool of Cochrane Collaboration. After screening, 55 clinical RCTs were included. The results showed that the current clinical studies of gastrointestinal dysfunction in sepsis reported the efficacy and safety indicators. The efficacy indicators included APACHE Ⅱ scores, gastrointestinal dysfunction scores, bowel sound scores, and inflammatory indicator such as C-reactive protein and procalcitonin. The safety indicators mainly include gastrointestinal reactions, skin reactions, and other adverse events and adverse reactions. However, there was no distinction between primary and secondary outcomes. The relevant indicators of health economics were not reported, and the quality of research methodology was poor. Therefore, we suggest that future researchers should be well prepared in the top-level design stage and actively construct the core outcome set, so as to improve the quality of clinical trials.
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Humanos , Medicamentos Herbarios Chinos/uso terapéutico , Enfermedades Gastrointestinales/tratamiento farmacológico , Medicina Tradicional China , Ensayos Clínicos Controlados Aleatorios como Asunto , Proyectos de Investigación , Sepsis/tratamiento farmacológicoRESUMEN
In recent years, with the rapid development of traditional Chinese medicine industry in China, the efficacy of Chinese medicinals in treating disease and maintaining health has been increasingly recognized. Tripterygium wilfordii, a Chinese medicinal for expelling wind, dredging collaterals, removing dampness, and relieving pain, is commonly used for treating acute and chronic glomerulonephritis, rheumatoid arthritis, and other diseases. However, the frequent occurrence of adverse reactions has limited its wide application in clinical practice. The existing studies have gradually confirmed that T. wilfordii and its active ingredients exert the bidirectional effects on kidney function. This paper reviewed the related clinical applications and articles published in the past decades and summarized the material basis for its bidirectional effects and the specific action mechanisms in renal protection and renal damage. It was found that the main active ingredients in T. wilfordii were tripterygium glycosides and triptolide, which exerted the protective or toxic and side effects on kidney by regulating immunity, influencing mitogen-activated protein kinases (MAPK) pathway, and changing the expression and function of renal transporters. Besides, the roles of administration time, dosage, and body status in the exertion of protective or toxic and side effects by T. wilfordii were also discussed. The review aimed to provide new ideas for the research on the treatment of kidney diseases with T. wilfordii and its safety application.
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OBJECTIVE@#To explore the therapeutic effect and partial mechanism of electroacupuncture (EA) for patients with insulin resistance (IR) polycystic ovary syndrome (PCOS).@*METHODS@#Seventy patients with IR-PCOS were randomly divided into an EA group (36 cases, 5 cases dropped off) and a medication group (34 cases, 4 cases dropped off). The patients in the medication group were treated with oral administration of metformin hydrochloride, 500 mg each time, twice a day. The patients in the EA group were treated with EA (continuous wave, 2 Hz of frequency) at Zusanli (ST 36), Zhongwan (CV 12), Qihai (CV 6), Yishu (EX-B 3), Shenshu (BL 23), Pishu (BL 20), Ciliao (BL 32) for 30 min, three times a week. One menstrual cycle or 4 weeks were taken as a course of treatment, and 3 continuous courses were given. The follow-up was 3 months. The lipid metabolism indexes of triacylglycerol (TG), total cholesterol (TC), high-density lipoprotein (HDL) and low-density lipoprotein (LDL), homeostasis model assessment-insulin resistance index (HOMA-IR) and testosterone (T) in serum were compared before and after treatment, and the clinical effects of the two groups were evaluated during the follow-up.@*RESULTS@#The total effective rate was 67.7% (21/31) in the EA group and 60.0% (18/30) in the medication group, with no significant difference between the two groups (>0.05). After treatment, the levels of serum T, HOMA-IR, LDL, TG and TC were decreased significantly in the two groups (<0.01, <0.05), and HDL was increased significantly (<0.01); the levels of TC in the EA group after treatment was lower than that in the medication group (<0.05).@*CONCLUSION@#EA may adjust some dyslipidemia in patients to correct IR and improve endocrine disorder of PCOS, which had superior/similar effects to metformin.
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Femenino , Humanos , Puntos de Acupuntura , Electroacupuntura , Resistencia a la Insulina , Síndrome del Ovario Poliquístico , TerapéuticaRESUMEN
Data of clinical trial projects involved by clinical trial institutions certified by the State Food and Drug Administration from 2002 to November 2012 were collected to summarize adverse reactions in project summary/statistical reports, analyze the rate of adverse reactions of clinical trials of new traditional Chinese medicines and relevant influencing factors, and increase the awareness of the safety of new traditional Chinese medicines. A total of 73 050 cases in 209 projects of 14 specialties were collected, including 49 689 cases in the new traditional Chinese medicine group and 271 adverse reaction cases, with an incidence rate of adverse reactions at 0.55%. The adverse reaction rate in 3 months < middle long course ≤ 6 months was the highest (1.04%), whereas that in short course ≤ half a month was the lowest (0.48%). The adverse reaction was closely related with the route of administration, 1.28% for topical > 0.63% for injection > 0.50% for oral. In the administration of only the test drug, the adverse reaction rate of patches was the highest (2.68%), whereas that of aerosols and suppositories was lowest (0). In the combined administration of the test drug and the simulation agent, the adverse reaction rate of external test patch + capsule was the highest (3.38%), whereas that of capsule + oral liquid, pills + granules, tablets + oral liquid, tablets + pills, tablet + capsule was the lowest (0). In the administration of only the test drug, the adverse reaction rate was 0.47%; In the combined administration with simulation agent (drug volume increase), the adverse reaction rate was 0.74%. Different doses caused adverse reaction different rates; The adverse reaction rate of drugs with whole-course dose between 1 100-1 200 g was the highest (3.36%), that for whole-course doses of 500-600, 900-1 000, 1 400-1 500, 1 600-1 700, 1 800-1 900 g was the lowest (0). In conclusion, the adverse reaction rate of new traditional Chinese medicines was still up to 0.55%, with the adverse reaction rate between 0.47% and 0.72% over the 11 years, without significant difference in each year. The adverse reaction rate was closely related to course of treatment, approach of administration, dosage form and medication dosage, with no significant correlation with medication dosage during the course of treatment. The adverse reaction rate increased with the rise in trial duration and drug volume. In the administration of only the test drug, the adverse reaction rates of external formulations and injections were higher than that of oral dosage forms. It is suggested to give more attention to the adverse reactions of drugs with long course of treatment and large volumes, injections and external patches in clinical trials of new traditional Chinese medicines.
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Humanos , Ensayos Clínicos como Asunto , Medicamentos Herbarios Chinos , Medicina Tradicional ChinaRESUMEN
<p><b>OBJECTIVE</b>To study the efficacy and mechanism of Weiyangning pills against experimental gastric ulcer.</p><p><b>METHOD</b>The gastric ulcer model were established by acetic acid, water-immersion stress, aspirin induction, pyloric ligation in rats, in order to observe the effect of Weiyangning pills against experimental gastric ulcer and study its effect on the content of nitric oxide (NO) and epidermal growth factor (EGF), gastric mucosal blood flow, the content of PGE2, gastric secretion, gastric acid content and the activity of pepsin.</p><p><b>RESULT</b>Weiyangning pills markedly reduced index of gastric ulcers of various types, increased the content of NO, EGF, PGE2 and gastric mucosal blood flow, inhibited gastric secretion and gastric acid content, and decreased the activity of pepsin.</p><p><b>CONCLUSION</b>Weiyangning pills has a significant effect against experimental gastric ulcer, which is related to the reduction of gastric mucosa damage factors (gastric acid and pepsin) and the increase in gastric mucosa's function as a barrier and its recovery effects, such as NO, EGF, PGE2 and gastric mucosal blood flow.</p>
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Animales , Femenino , Masculino , Ratas , Ácido Acético , Aspirina , Dinoprostona , Metabolismo , Medicamentos Herbarios Chinos , Farmacología , Usos Terapéuticos , Factor de Crecimiento Epidérmico , Metabolismo , Ácido Gástrico , Metabolismo , Secreciones Corporales , Ligadura , Óxido Nítrico , Metabolismo , Ratas Sprague-Dawley , Flujo Sanguíneo Regional , Úlcera Gástrica , Quimioterapia , MetabolismoRESUMEN
<p><b>OBJECTIVE</b>To study the intestinal absorption mechanism of traditional Chinese medicine monomer syringopicroside in rats.</p><p><b>METHOD</b>The in situ rat single-pass intestinal perfusion model was established to detect the concentration of syringopicroside by HPLC. The absorption at different intestine segments in rat and the influence of concentration, pH and P-glycoprotein inhibitors of the drug solution on the absorption of syringopicroside were also observed.</p><p><b>RESULT</b>The absorption rate constant (K,) of syringopicroside at duodenum, jejunum, ileum, and colon were 0.00255, 0.00630, 0.00900, 0.00799 min- , respectively; Ka from intestine at syringopicroside concentration of 0.090, 0.180, 0.360 g x L(-1) were 0.00370, 0.00708, 0.00694 min(-1), respectively; and Ka at pH of 7.4, 6.8 and 5.0 were 0.00733, 0.00747, 0.00362 min(-1), respectively. P-glycoprotein inhibitor on the intestinal absorption of syringopicroside showed significant influence (P < 0.05).</p><p><b>CONCLUSION</b>Syringopicroside is well absorbed at the lower small intestine. When the drug concentration is low, the absorption rate constant is low, where as Ka increases at medium and high concentrations; the Ka is low at pH 5.0 and increases at pH 6.8 and pH 7.4. Syringopicroside is proved to be a substrate of P-glycoprotein.</p>
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Animales , Masculino , Ratas , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP , Fisiología , Glicósidos , Farmacocinética , Concentración de Iones de Hidrógeno , Absorción Intestinal , Ratas Sprague-DawleyRESUMEN
Professor DONG Gui-rong's theoretical principle and manipulation points for peripheral facial paralysis were introduced in details from the angels of syndrome differentiation, timing, acupoint prescription and needling methods. For the syndrome differentiation and timing, the professor emphasized to check the treatment timing and follow the symptoms, which should be treated by stages, besides, it was necessary to find and distinguish the reason and nature of diseases to have a combined treatment of tendons and muscles. For the acupoint prescription and needling methods, he has proposed that the acupoints selection should be compatible of distal and lacal, and made a best of Baihui (GV 20) to regulate the whole yang qi, also he has paid much attention to the needling methods and staging treatment. Under the consideration of late stage of peripheral facial paralysis, based on syndrome differentiation Back-shu points have been selected to regulate zang-fu function, should achieve much better therapeutic effect.
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Adulto , Humanos , Masculino , Terapia por Acupuntura , Parálisis Facial , TerapéuticaRESUMEN
OBJECTIVES: The purpose of the study was to evaluate digestion of pectin/Kollicoat SR30D free films for colonic delivery in vitro and in vivo. METHODS: Free films containing different ratios of pectin to Kollicoat SR30D were prepared by casting/solvent evaporation method. An in-vitro comparison of swelling, degradation and permeability of the free films was carried out in simulated colon fluids containing caecal contents from normal rats with colitis induced by 2,4,6-trinitrobenzene sulfonic acid (TNBS) or oxazolone. A comparative in-vivo evaluation of degradation was also conducted in normal and colitis-induced model rats. KEY FINDINGS: The pectin within the mixed films was susceptible to rat colonic bacterial enzymes. The extent of digestion correlated with the amount of pectin present within the film. In vitro, the swelling index, drug permeability and extent of film digestion in simulated colon fluids with caecal contents obtained from normal rats were higher than from TNBS- or oxazolone-induced model rats, whereas in-vivo degradation was similar in the three groups of rats. The pectin/Kollicoat SR30D free films were completely degraded in the colitis-induced rats. CONCLUSIONS: Pectic/Kollicoat SR30D films may be useful as coatings to target delivery of drugs to the colon.
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Colitis/fisiopatología , Colon/efectos de los fármacos , Colon/microbiología , Sistemas de Liberación de Medicamentos/métodos , Pectinas/química , Polivinilos/química , Animales , Ciego/efectos de los fármacos , Ciego/microbiología , Ciego/fisiopatología , Colitis/inducido químicamente , Colon/enzimología , Modelos Animales de Enfermedad , Fluorouracilo/normas , Fluorouracilo/toxicidad , Vidrio/química , Oxazolona/toxicidad , Pectinas/farmacología , Permeabilidad , Polivinilos/farmacología , Ratas , Vapor , Temperatura , Ácido Trinitrobencenosulfónico/toxicidadRESUMEN
<p><b>OBJECTIVE</b>To observe effects of intervention time of local acupuncture at the affected side on the facial nerve injury and the therapeutic effect at acute stage of peripheral facial paralysis.</p><p><b>METHODS</b>Two hundred and seventy-nine cases within 3 days of attack were randomly divided into 4 groups, group A (n=74), group B (n=70), group C (n=74) and control group (n=61). The 4 groups were treated with Prednisone on the third day after attack, and acupuncture was added in the group A, B and C, with Fengchi (GB 20), Yangbai (GB 14), Taiyang (EX-HN 5), Sibai (ST 2), Yingxiang (LI 20), etc. on the affected side and bilateral Hegu (LI 4) selected, and with superficial insertion method used for acupoints on the ear-face parts without manipulating the needles, and electroacupuncture was added from the fifth session of the treatment, and uniform reinforcing-reducing method was used for the distal acupoints selected. The needles were retained for 20 min and the treatment was given for 25 sessions, once other day. The therapeutic effects, the mean therapeutic courses for the cured patients and changes of electroneurography (ENoG) were compared among the groups.</p><p><b>RESULTS</b>The clinical total effective rate was 98.6%, 95.7%, 94.6% and 72.1% in the group A, B, C and the control group, respectively, with a significant difference (P < 0.05), and the therapeutic course for the cured patients increased in the order of the group A, B, C and the control group; and there was no significant difference among the 4 groups in changes of ENoG at the third day and the fourteenth day (both P > 0.05).</p><p><b>CONCLUSION</b>Acute stage is the best opportunity for acupuncture treatment of peripheral facial paralysis, and the earlier the intervention time, the better the therapeutic effect and the shorter the therapeutic course.</p>
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Adolescente , Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad , Adulto Joven , Puntos de Acupuntura , Terapia por Acupuntura , Métodos , Terapia Combinada , Electroacupuntura , Parálisis Facial , Terapéutica , Factores de Tiempo , Resultado del TratamientoRESUMEN
The aim of the present study was to define in-vitro and in-vivo characteristics of pectin/ethylcellulose-film-coated pellets of 5-fluorouracil (5-FU) for colonic targeting. The pellet cores were coated to different film thicknesses with three different pectin/ethylcellulose formulations using a fluidized bed coater. The gastrointestinal (GI) transit of coated pellets was determined by counting the percentage of coated pellets in the GI lumen by celiotomy at certain times after oral administration. 5FU was administered to rats at a dose of 15 mg kg(-1). The toxicity of 5-FU in the GI tract was evaluated using histological examination. The 1:2 ratio pectin:ethylcellulose-coated pellets with 30% total weight gain (TWG-30%) produced more satisfactory drug-release profiles in the simulated gastric, intestinal and colonic fluids. Most of the coated pellets were eliminated from the stomach in 2 h, moved into the small intestine after 2-4 h, and reached the large intestine after 4 h. After oral administration of coated pellets, 5-FU started appearing in the plasma at 7 h, and reached peak plasma concentration (Cmax) of 3.21+/-2.01 microg mL(-1) at 16 h (Tmax); the Cmax for uncoated pellets was 22.21+/-2.60 microg mL(-1) at Tmax 0.75 h. The TWG-30% formulation showed delayed Tmax, decreased Cmax and prolonged mean residence time compared with uncoated pellets. Marked pathological features in the colon were seen in rats given coated pellets, but no injuries were observed in the upper GI tract. The formulation of TWG-30% could deliver 5-FU to the colon for local action.
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Celulosa/análogos & derivados , Colon/metabolismo , Implantes de Medicamentos/farmacocinética , Fluorouracilo/farmacocinética , Pectinas/química , Administración Oral , Animales , Área Bajo la Curva , Celulosa/química , Cromatografía Líquida de Alta Presión , Materiales Biocompatibles Revestidos/química , Implantes de Medicamentos/administración & dosificación , Implantes de Medicamentos/química , Fluorouracilo/administración & dosificación , Fluorouracilo/química , Fármacos Gastrointestinales/administración & dosificación , Fármacos Gastrointestinales/química , Fármacos Gastrointestinales/farmacocinética , Tránsito Gastrointestinal/efectos de los fármacos , Semivida , Técnicas In Vitro , Microscopía Electrónica de Rastreo , Distribución Aleatoria , Ratas , Ratas Wistar , Tecnología Farmacéutica/métodosRESUMEN
<p><b>OBJECTIVE</b>To investigate the effect of prim-O-glucosylcimifugin and 4'-O-p-D-glucosyl-5-O-methylvisa-mminol con on the proliferation of smooth muscle cell stimulated by TNF-alpha.</p><p><b>METHOD</b>The primary cell culture method of smooth muscle cell (SMC) was established by attachment-block. The SMC was identificated by immunochemistry method, and the growth curve was drawn by cytometry. The third generation of SMC was adopted in the experiment. The effect of prim-O-glucosylcimif-ugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol con on the proliferation and cell cycle of SMC was investigated by MTT and flow cytometry respectively.</p><p><b>RESULT</b>TNF-alpha of 5 micro g x L(-1) can stimulate the proliferation of SMC and increase the proportion of G2 phase and S phase in cell cycle which has great significant difference (P < 0.01) compared with control. The three dose groups of prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisammin-ol con can inhibit the proliferation of SMC and increase the proportion of G0/G1 phase, which has great significant difference (P < 0.01) compared with model group.</p><p><b>CONCLUSION</b>Prim-O-glucosylcimifugin and 4'-O-beta-D-glucosyl-5-O-methylvisamminol con can inhibit the proliferation of SMC stimulated by TNF-alpha.</p>
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Animales , Femenino , Masculino , Ratas , Proliferación Celular , Células Cultivadas , Medicamentos Herbarios Chinos , Farmacología , Monosacáridos , Farmacología , Miocitos del Músculo Liso , Biología Celular , Ratas Wistar , Factor de Necrosis Tumoral alfa , Farmacología , Xantenos , FarmacologíaRESUMEN
<p><b>OBJECTIVE</b>To research the expectorant components in volatile oil from the root and rhizome of Aster tataricus.</p><p><b>METHOD</b>GC-MS was applied to isolate and identify the compounds. In addition, TLC was used to isolate compound, and its structure was elucidated on the basis of spectral data analysis. At the same time, its expectorant effect was observed by method of the excretion quantity of phenol red in trachea of mice.</p><p><b>RESULT</b>Seven compounds were isolated and identified by GC-MS, they were (R)(-)-p-menth-1-en-4-ol (1), 2-undecanone (2), n-decanoic acid (3), (-)-spathulenol (4), hexahydrofamrnesyl acetone (5), hexadecanoic acid (6), and cis-9, cis-12-octaecadienoic acid (7). A known compound 1-acetoxy-2-ene(E)-4,6- decandiyne was isolated from the root and rhizome of A. tataricus, and it was shown to have expectorant effect.</p><p><b>CONCLUSION</b>1-Acetoxy-2-ene(E) -4,6- decandiyne, a main compound in volatile oil, had been found to have expectorant effect.</p>
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Animales , Masculino , Ratones , Aster , Química , Medicamentos Herbarios Chinos , Química , Farmacología , Expectorantes , Química , Farmacología , Cromatografía de Gases y Espectrometría de Masas , Espectroscopía de Resonancia Magnética , Aceites Volátiles , Química , Raíces de Plantas , Química , Rizoma , QuímicaRESUMEN
The aim of the present study is to develop colon-targeted drug delivery systems for 5-fluorouracil using pectin combined with ethylcellulose as a film coat with fluidized bed coater. Pellets (0.8-1.0 mm in diameter) containing 40% 5-fluorouracil and 60% microcrystalline cellulose were prepared by extrusion and spheronization. Film-coated pellets of 5-fluorouracil containing various proportions (1:0, 0:1, 1:1, 1:2, w/w) of pectin and ethylcellulose (Surelease) were prepared and subjected to in vitro drug release. The amount of 5-fluorouracil released from pellets at different time intervals was estimated by high-performance liquid chromatography. Drug release was assessed using flow testing in the presence and absence of rat caecal contents. The film thickness is expressed as the theoretical percentage of the weight gained (TWG-%) used relative to the weight of the coated pellets. Coated pellets with pectin alone and TWG-20% released 100% of the 5-fluorouracil in the simulated gastric and small intestinal conditions and failed to control the drug release in the first 5 h of the dissolution study in the simulated gastric and small intestinal conditions; while coated pellets with ethylcellulose alone and TWG-20% released 11.7 +/- 0.9% of the 5-fluorourail at the end of 24 h. When the ratio of pectin to Surelease was 1:1 (w/w) and film coat TWG-20%, the release was rapid and was accompanied by splitting of the coat. When the ratio of pectin to Surelease was 1:2 (w/w) and film coat TWG-13% and TWG-20%, the formulations released 9.8 +/- 0.7% and 4.1 +/- 0.4%, respectively, of 5-fluorouracil in the first 5 h of the dissolution study in the simulated gastric and small intestinal conditions. When the dissolution study was continued in simulated colonic fluids (4% w/v rat caecal content medium) for another 19 h, the film coat with the formulations of TWG-13% and TWG-20% released 96 +/- 1.3% and 85.0 +/- 0.3%, respectively, of 5-fluorourail in simulated colonic fluids at the end of 24 h of the dissolution study, whereas in the control study the formulations released 51.4 +/- 1.0% and 34 +/- 0.5%, respectively, of 5-fluorouracil in absence of rat caecal contents at the end of 24 h. The results of the study show that the formulation of TWG-20% (pectin to Surelease 1:2, w/w) is most likely to provide targeting of 5-fluorouracil for local action in the colon, as it released only 4.1 +/- 0.4% of the drug in the simulated gastric and small intestinal conditions, and it released 85.0 +/- 0.3% of 5-fluorourail in simulated colonic fluids at the end of 24 h. The 5-fluorouracil-coated pellets showed no change in physical appearance, drug content, or dissolution pattern after storage at 40 degrees C/75% relative humidity for 6 months. Differential scanning calorimetric study indicated no possibility of interaction between 5-fluorouracil and pectin or other excipients used in the coated pellets.
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Antimetabolitos Antineoplásicos/química , Celulosa/análogos & derivados , Colon/metabolismo , Sistemas de Liberación de Medicamentos , Excipientes/química , Fluorouracilo/química , Pectinas/química , Animales , Antimetabolitos Antineoplásicos/administración & dosificación , Antimetabolitos Antineoplásicos/metabolismo , Rastreo Diferencial de Calorimetría , Celulosa/química , Química Farmacéutica , Composición de Medicamentos , Estabilidad de Medicamentos , Heces/química , Fluorouracilo/administración & dosificación , Fluorouracilo/metabolismo , Concentración de Iones de Hidrógeno , Técnicas In Vitro , Absorción Intestinal , Ratas , Ratas Wistar , Solubilidad , Comprimidos Recubiertos , Tecnología Farmacéutica/métodos , Factores de TiempoRESUMEN
Despite the availability of six classes of antihypertensive agents, control of blood pressure and improving patients' quality of life remain far from ideal. There is a wide variability in terms of the hypotensive effect and side effect profile for the same antihypertensive agent used in different patients. How to select the right agent to provide the most beneficial results in terms of efficacy and improvement of quality of life as well as to decrease clinical symptoms and minimize adverse reactions is an important therapeutic challenge. It has been suggested that clinical usage of pattern (Zheng) diagnosis of traditional Chinese medicine may improve the accuracy in selecting the right antihypertensive agents with improved efficacy and deceased adverse effects. Limited research in this area suggested the calcium channel blocker may work better in treating phlegmatic damp excess pattern and blood stasis pattern while beta-blockers may be more beneficial in the liver yang rising pattern. On the other hand, angiotensin converting enzyme inhibitors may be more suitable in a yin deficiency and yang hyperactivity pattern as well as combined liver and kidney yin deficiency pattern. More research studies using this innovative approach in improving the selection of antihypertensive agents including mechanistic studies are urgently needed.
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<p><b>OBJECTIVE</b>To study the hepatotoxicity effects in rats with different extract of Fructus Gardeniae.</p><p><b>METHOD</b>Observe the change of appearance, behavior and weight of rats through oral gavage daily for 3 d. Weigh the liver and calculate the liver index. Detect the ALT, AST and TBIL. Observe the liver tissue by optical microscope.</p><p><b>RESULT</b>The weight and index of liver were increased by 3.08 g x kg(-1) aqueous extract, 1.62 g x kg(-1) alcoholic extract and 0.28 g x kg(-1) geniposide, compared to those of the blank group (P < 0.005, P < 0.001) and the activities of ALT, AST and the content of TBIL were also increased, compared to those of the blank group (P < 0.05, P < 0.001). The liver cells were obviously swell, necrotic and changed with inflammatory infiltrate.</p><p><b>CONCLUSION</b>Aqueous extract, alcoholic extract and geniposide displayed hepatotoxicity, and the geniposide which was the main substance of the Fructus Gardeniae might be mainly responsible for the hepatotoxicity.</p>