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This study aims to explore the mechanism of Qingkailing(QKL) Oral Preparation's heat-clearing, detoxifying, mind-tranquilizing effects based on "component-target-efficacy" network. To be specific, the potential targets of the 23 major components in QKL Oral Preparation were predicted by the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP) and SwissTargetPrediction. The target genes were obtained based on UniProt. OmicsBean and STRING 10 were used for Gene Ontology(GO) term enrichment and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment of the targets. Cytoscape 3.8.2 was employed for visualization and construction of "component-target-pathway-pharmacological effect-efficacy" network, followed by molecular docking between the 23 main active components and 15 key targets. Finally, the lipopolysaccharide(LPS)-induced RAW264.7 cells were adopted to verify the anti-inflammatory effect of six monomer components in QKL Oral Preparation. It was found that the 23 compounds affected 33 key signaling pathways through 236 related targets, such as arachidonic acid metabolism, tumor necrosis factor α(TNF-α) signaling pathway, inflammatory mediator regulation of TRP channels, cAMP signaling pathway, cGMP-PKG signaling pathway, Th17 cell differentiation, interleukin-17(IL-17) signaling pathway, neuroactive ligand-receptor intera-ction, calcium signaling pathway, and GABAergic synapse. They were involved in the anti-inflammation, immune regulation, antipyretic effect, and anti-convulsion of the prescription. The "component-target-pathway-pharmacological effect-efficacy" network of QKL Oral Preparation was constructed. Molecular docking showed that the main active components had high binding affinity to the key targets. In vitro cell experiment indicated that the six components in the prescription(hyodeoxycholic acid, baicalin, chlorogenic acid, isochlorogenic acid C, epigoitrin, geniposide) can reduce the expression of nitric oxide(NO), TNF-α, and interleukin-6(IL-6) in cell supernatant(P<0.05). Thus, the above six components may be the key pharmacodynamic substances of QKL Oral Preparation. The major components in QKL Oral Prescription, including hyodeoxycholic acid, baicalin, chlorogenic acid, isochlorogenic acid C, epigoitrin, geniposide, cholic acid, isochlorogenic acid A, and γ-aminobutyric acid, may interfere with multiple biological processes related to inflammation, immune regulation, fever, and convulsion by acting on the key protein targets such as IL-6, TNF, prostaglandin-endoperoxide synthase 2(PTGS2), arachidonate 5-lipoxygenase(ALOX5), vascular cell adhesion molecule 1(VCAM1), nitric oxide synthase 2(NOS2), prostaglandin E2 receptor EP2 subtype(PTGER2), gamma-aminobutyric acid receptor subunit alpha(GABRA), gamma-aminobutyric acid type B receptor subunit 1(GABBR1), and 4-aminobutyrate aminotransferase(ABAT). This study reveals the effective components and mechanism of QKL Oral Prescription.
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Medicamentos de Ervas Chinesas , Fator de Necrose Tumoral alfa , Ácido Clorogênico , Medicamentos de Ervas Chinesas/farmacologia , Ácido gama-Aminobutírico , Interleucina-6 , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular , Fator de Necrose Tumoral alfa/genética , Animais , Camundongos , Células RAW 264.7RESUMO
This study aims to explore the mechanism of Qingkailing(QKL) Oral Preparation's heat-clearing, detoxifying, mind-tranquilizing effects based on "component-target-efficacy" network. To be specific, the potential targets of the 23 major components in QKL Oral Preparation were predicted by the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP) and SwissTargetPrediction. The target genes were obtained based on UniProt. OmicsBean and STRING 10 were used for Gene Ontology(GO) term enrichment and Kyoto Encyclopedia of Genes and Genomes(KEGG) pathway enrichment of the targets. Cytoscape 3.8.2 was employed for visualization and construction of "component-target-pathway-pharmacological effect-efficacy" network, followed by molecular docking between the 23 main active components and 15 key targets. Finally, the lipopolysaccharide(LPS)-induced RAW264.7 cells were adopted to verify the anti-inflammatory effect of six monomer components in QKL Oral Preparation. It was found that the 23 compounds affected 33 key signaling pathways through 236 related targets, such as arachidonic acid metabolism, tumor necrosis factor α(TNF-α) signaling pathway, inflammatory mediator regulation of TRP channels, cAMP signaling pathway, cGMP-PKG signaling pathway, Th17 cell differentiation, interleukin-17(IL-17) signaling pathway, neuroactive ligand-receptor intera-ction, calcium signaling pathway, and GABAergic synapse. They were involved in the anti-inflammation, immune regulation, antipyretic effect, and anti-convulsion of the prescription. The "component-target-pathway-pharmacological effect-efficacy" network of QKL Oral Preparation was constructed. Molecular docking showed that the main active components had high binding affinity to the key targets. In vitro cell experiment indicated that the six components in the prescription(hyodeoxycholic acid, baicalin, chlorogenic acid, isochlorogenic acid C, epigoitrin, geniposide) can reduce the expression of nitric oxide(NO), TNF-α, and interleukin-6(IL-6) in cell supernatant(P<0.05). Thus, the above six components may be the key pharmacodynamic substances of QKL Oral Preparation. The major components in QKL Oral Prescription, including hyodeoxycholic acid, baicalin, chlorogenic acid, isochlorogenic acid C, epigoitrin, geniposide, cholic acid, isochlorogenic acid A, and γ-aminobutyric acid, may interfere with multiple biological processes related to inflammation, immune regulation, fever, and convulsion by acting on the key protein targets such as IL-6, TNF, prostaglandin-endoperoxide synthase 2(PTGS2), arachidonate 5-lipoxygenase(ALOX5), vascular cell adhesion molecule 1(VCAM1), nitric oxide synthase 2(NOS2), prostaglandin E2 receptor EP2 subtype(PTGER2), gamma-aminobutyric acid receptor subunit alpha(GABRA), gamma-aminobutyric acid type B receptor subunit 1(GABBR1), and 4-aminobutyrate aminotransferase(ABAT). This study reveals the effective components and mechanism of QKL Oral Prescription.
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Animais , Camundongos , Ácido Clorogênico , Medicamentos de Ervas Chinesas/farmacologia , Ácido gama-Aminobutírico , Interleucina-6 , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular , Fator de Necrose Tumoral alfa/genéticaRESUMO
This study primarily concentrated on scientific problems of poor taste caused by unclear critical quality attributes of oral preparations manufactured by Chinese materia medica, successfully established an identification method for taste critical quality attribute and a taste improvement method combining electronic tongue with human senses, and determined the optimal taste formula, to improve patients' oral medication compliance. The study received ethical approval from the Review Committee of the Beijing University of Chinese Medicine. The results showed that the proportion of bitterness of Xiaoer Qingrening Granule was 61.8%, and its bitterness grade was 3.70, it was determined that bitterness is the critical quality attribute that caused the poor taste of Xiaoer Qingrening Granule. Additionally, the optimal taste formula per milliliter of Xiaoer Qingrening sugar-free intermediate was determined with allowable daily intake, solubility, and sweetness as the limiting conditions, which was 40 mg hydroxypropyl β-cyclodextrin, 180 mg trehalose, and 1.5 mg acesulfame potassium. Compared with the Xiaoer Qingrening Granule, the sensory evaluation score of the optimal taste formula was increased by 37.5 points. In conclusion, this study achieved the taste improvement of Xiaoer Qingrening Granule and formed a set of taste improvement strategies including the identification of taste critical quality attribute, the selection of the type and dosage of corrigent, and the optimization of taste formula, which provided a thought reference for the taste improvement of other oral preparations and a new perspective for quality control of intelligent manufacturing of traditional Chinese medicines.
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In light of the liver injury risk associated with the oral administration of Xianlin Gubao oral preparation, this study compared the differences in liver injury induced by two different extraction processes in rats and explored the correlation between hepatotoxicity and extraction process from the perspective of the differences in the content of the relevant components. Thirty male Sprague-Dawley(SD) rats were randomly divided into a normal group, tablet extract groups of different doses, and capsule extract groups of different doses, with 6 rats in each group. Each group received continuous oral administration for 4 weeks. The assessment of liver injury caused by different extracts was conducted by examining rat body weight, liver function blood biochemical indicators, liver coefficient, and liver pathological changes. In addition, a high-performance liquid chromatography(HPLC) method was established to simultaneously determine the content of icariin, baohuoside I, and bakuchiol in the extracts to compare the differences in the content of these three components under the two extraction processes. The results showed that both extracts caused liver injury in rats. Compared with the normal group, the tablet extract groups, at the studied dose, led to slow growth in body weight, a significant increase in triglyceride levels(P<0.05), a significant decrease in liver-to-brain ratio(P<0.05), and the appearance of hepatic steatosis. The capsule extract groups, at the studied dose, resulted in slow growth in body weight, a significant increase in aspartate aminotransferase levels(P<0.05), a significant decrease in body weight, liver weight, and liver-to-brain ratio(P<0.05), and the presence of hepatic steatosis and inflammatory cell infiltration. In comparison, the capsule extraction process had a higher risk of liver injury. Furthermore, based on the completion of the liquid chromatography method, the content of icariin and baohuoside Ⅰ in the capsule extract groups was 0.83 and 0.81 times that in the tablet extract groups, respectively, while the bakuchiol content in the capsule extract group was 29.80 times that in the tablet extract groups, suggesting that the higher risk of liver injury associated with the capsule extraction process may be due to its higher bakuchiol content. In summary, the differences in rat liver injury caused by the two extracts are closely related to the extraction process. This should be taken into consideration in the formulation production and clinical application.
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Ratos , Masculino , Animais , Ratos Sprague-Dawley , Fígado/patologia , Doença Hepática Induzida por Substâncias e Drogas/patologia , Fígado Gorduroso , Comprimidos , Peso Corporal , Extratos Vegetais , FenóisRESUMO
In light of the liver injury risk associated with the oral administration of Xianlin Gubao oral preparation, this study compared the differences in liver injury induced by two different extraction processes in rats and explored the correlation between hepatotoxicity and extraction process from the perspective of the differences in the content of the relevant components. Thirty male Sprague-Dawley(SD) rats were randomly divided into a normal group, tablet extract groups of different doses, and capsule extract groups of different doses, with 6 rats in each group. Each group received continuous oral administration for 4 weeks. The assessment of liver injury caused by different extracts was conducted by examining rat body weight, liver function blood biochemical indicators, liver coefficient, and liver pathological changes. In addition, a high-performance liquid chromatography(HPLC) method was established to simultaneously determine the content of icariin, baohuoside I, and bakuchiol in the extracts to compare the differences in the content of these three components under the two extraction processes. The results showed that both extracts caused liver injury in rats. Compared with the normal group, the tablet extract groups, at the studied dose, led to slow growth in body weight, a significant increase in triglyceride levels(P<0.05), a significant decrease in liver-to-brain ratio(P<0.05), and the appearance of hepatic steatosis. The capsule extract groups, at the studied dose, resulted in slow growth in body weight, a significant increase in aspartate aminotransferase levels(P<0.05), a significant decrease in body weight, liver weight, and liver-to-brain ratio(P<0.05), and the presence of hepatic steatosis and inflammatory cell infiltration. In comparison, the capsule extraction process had a higher risk of liver injury. Furthermore, based on the completion of the liquid chromatography method, the content of icariin and baohuoside â in the capsule extract groups was 0.83 and 0.81 times that in the tablet extract groups, respectively, while the bakuchiol content in the capsule extract group was 29.80 times that in the tablet extract groups, suggesting that the higher risk of liver injury associated with the capsule extraction process may be due to its higher bakuchiol content. In summary, the differences in rat liver injury caused by the two extracts are closely related to the extraction process. This should be taken into consideration in the formulation production and clinical application.
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Doença Hepática Induzida por Substâncias e Drogas , Fígado Gorduroso , Fenóis , Ratos , Masculino , Animais , Ratos Sprague-Dawley , Fígado/patologia , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/patologia , Comprimidos , Peso Corporal , Extratos VegetaisRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cerebral infarction is the second leading cause of death and the third most common cause of disability. The use of anti-platelet aggregation drugs is prone to bleeding, liver and kidney damage, gastrointestinal reactions, and is not suitable for patients to take for a long time. Xuesaitong oral preparations (XSTOP), a traditional Chinese medicine formula, has shown therapeutic effect on treating cerebral infarction based on the clinical practice and pharmacological mechanism. AIM OF THE STUDY: The study aims to evaluate the effectiveness and safety of XSTOP combined with conventional treatment (CT) in treatment of acute cerebral infarction (ACI), and to provide the reliable evidence for clinical application. MATERIALS AND METHODS: We performed a literature search in Chinese National Knowledge Infrastructure (CNKI), Wanfang Database, VIP Database, PubMed, EMBASE, Cochrane Library and Web of Science from their inceptions to August 2021. Systematic searches for randomized controlled trials (RCTs) of XSTOP in treatment of ACI. Odds ratio (OR) or mean difference (MD) with their 95% confidence interval was calculated between with and without XSTOP therapy. Cochrane risk of bias tool was used to evaluate the methodological quality of the included trials. RESULTS: Eight RCTs involving 827 patients were included in this meta-analysis. By comparing XSTOP plus conventional treatment with conventional treatment alone, the meta-analysis gave the following results: (1) Total effective rate (OR = 4.53, 95% CI[2.85, 7.19], P < 0.0001); (2) National Institutes of Health Stroke Scale (NIHSS) score (MD = -3.22, 95% CI[-4.52, -1.92], Pï¼0.00001); (3) Plasma viscosity (PV) (MD = -0.74, 95%CI [-0.96, -0.51], Pï¼0.00001), hole blood high-cut viscosity (HBV) (MD = -0.63, 95%CI [-0.73, -0.53], P = 0.84), whole blood low-cut viscosity (LBV) (MD = -0.37, 95%CI [-0.56, -0.19], P = 0.96), fibrinogen (FIB) (MD = -23.78, 95%CI [-28.57, -18.99], P = 1.00), hematocrit (Hct) (MD = -2.76, 95%CI [-3.16, -2.36], P = 0.96); (4) China Stroke Scale (CSS) score (MD = -6.53, 95% CI[-9.07, -3.99], Pï¼0.00001); (5) No significant adverse reactions were reported; (6) The evidence was downgraded to "very low" quality, according to GRADE system. CONCLUSION: XSTOP plus CT is conditional recommended to improve the total effective rate, NIHSS score, PV, CSS score, and no serious adverse reactions were noted. The GRADE assessment indicates that the overall certainty quality of evidence is very low. Further large-scale, well-designed and high-quality RCTs are needed to confirm the positive results. As all studies included were conducted in China. It is unclear if the findings of this meta-analysis could be generalized to other populations.
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Infarto Cerebral/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Saponinas/uso terapêutico , Administração Oral , Animais , Medicamentos de Ervas Chinesas/química , Humanos , Estrutura Molecular , Saponinas/químicaRESUMO
Objective: To systematically evaluate the clinical efficacy of Compound Yuxingcao Oral Preparation in the treatment of respiratory diseases in children, and provide basis for its clinical application. Methods: The clinical controlled trial literatures of Compound Yuxingcao Oral Preparation in the treatment of respiratory diseases in children were searched from database to evaluate the effectiveness of Compound Yuxingcao Oral Preparation by evaluating the quality of literatures based on Meta-analysis. Results: A total of 17 literatures were included, of which 15 were RCT literatures. The average score of literatures was 4. A total of 1766 patients were included in the included literatures. The total effective rate and safety of Compound Yuxingcao Oral Preparation were higher than that of the control group, and the difference was statistically significant. Conclusion: Compound Yuxingcao Oral Preparation has good efficacy and safety in the treatment of children with respiratory tract infection.
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In commonly used oral solid preparations, poor mouthfeel results in poor patient compliance with the drug, which in turn reduces the market competitiveness of the drug. The problem of taste masking of pharmaceutical preparations has always been one of the important problems faced by pharmaceutics. With the increasing demand for the taste of drugs, the methods of masking bad taste of drugs have gradually increased in recent years. By summarizing the relevant literature covering the bad taste of drugs, the commonly used taste masking techniques include the addition of taste masking agents, inclusion techniques, microsphere/microcapsule technology, solid dispersion technology, ion exchange technology and the like. However, in addition to the above taste masking techniques, in the manufacturing process of the solid preparation, the granulation technique also can achieve the shielding of the bad taste of the medicine, and the granulation technique is simple, and can well achieve the effect of masking the bad taste of the medicine. This paper systematically introduces the research progress of granulation technology in drug taste masking, in order to provide reference for the selection of drug taste masking technology. With the increasing demand for drug taste, drug masking technology has been paid more and more attention by the majority of preparation workers, however, there are still some problems, such as imperfect taste evaluation system and low specificity of methods. This series of problems need to be further studied and solved by relevant pharmaceutical researchers.
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OBJECTIVE: To optimize the preparation technology of Oridonin A oral liposomes (ORI-LIP) by using supercritical fluidsolution-enhanced dispersion (SEDS) technology, and to investigate its advantage with routine liposome preparation technologies. METHODS: Using particle size as evaluation index, orthogonal design was employed to investigate the influence of pressure, temperature and flow rate on the preparation technology of ORI-LIP by SEDS. At the same time, thin film dispersion and reverse evaporation method were used to prepare ORI liposomes. The particle size, encapsulation efficiency, drug loading amount and stability (accelerated test for 6 months) were compared among 3 methods. Moreover, the difference in dissolution behavior in vitro of ORI crude drug and 3 kinds of liposomes was evaluated. RESULTS: The optimized preparation condition of ORI liposomes by SEDS included temperature of 50 ℃, pressure of 18 MPa, flow rate of 1 mL/min. Compared with thin film dispersion and reverse evaporation method, the liposomes prepared by the SEDS method exhibited smaller particle size [(147.4±4.8)nm], better encapsulation efficiency (67.8%), drug-loading amount (7.8%) and stability (particle size increased slightly, encapsulation efficiency decreased only by 4.4%). Results of in vitro dissolution test showed that compared with crude drug, release rate of each liposome was slow and persistent, and the cumulative release rate was higher. The accumulative release rate of ORI-LIP prepared by SEDS could achieve to 67.2%, and reached to dissolution equilibrium at 24 h. CONCLUSIONS: ORI-LIP prepared by SEDS has smaller particle size, higher encapsulation efficiency, drug loading amount and stability, which can improve the in vitro release of ORI. Compared with conventional methods, SEDS technology has certain advantages.
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BACKGROUND & RATIONALE: Medicare's 2011 prospective payment system (PPS) was introduced to curb overuse of separately billable injectable drugs. After epoietin, intravenous (IV) vitamin D analogues are the biggest drug cost drivers in hemodialysis (HD) patients, but the association between PPS introduction and vitamin D therapy has been scarcely investigated. STUDY DESIGN: Interrupted time-series analyses. SETTING & PARTICIPANTS: Adult US HD patients represented in the US Renal Data System between 2008 and 2013. EXPOSURES: PPS implementation. OUTCOMES: The cumulative dose of IV vitamin D analogues (paricalcitol equivalents) per patient per calendar quarter in prevalent HD patients. The average starting dose of IV vitamin D analogues and quarterly rates of new vitamin D use (initiations/100 person-months) in incident HD patients within 90 days of beginning HD therapy. ANALYTICAL APPROACH: Segmented linear regression models of the immediate change and slope change over time of vitamin D use after PPS implementation. RESULTS: Among 359,600 prevalent HD patients, IV vitamin D analogues accounted for 99% of the total use, and this trend was unchanged over time. PPS resulted in an immediate 7% decline in the average dose of IV vitamin D analogues (average baseline dose = 186.5 µg per quarter; immediate change = -13.5 µg [P < 0.001]; slope change = 0.43 per quarter [P = 0.3]) and in the starting dose of IV vitamin D analogues in incident HD patients (average baseline starting dose = 5.22 µg; immediate change = -0.40 µg [P < 0.001]; slope change = -0.03 per quarter [P = 0.03]). The baseline rate of vitamin D therapy initiation among 99,970 incident HD patients was 44.9/100 person-months and decreased over time, even before PPS implementation (pre-PPS ß = -0.46/100 person-months [P < 0.001]; slope change = -0.19/100 person-months [P = 0.2]). PPS implementation was associated with an immediate change in initiation levels (by -4.5/100 person-months; P < 0.001). LIMITATIONS: Incident HD patients were restricted to those 65 years or older. CONCLUSION: PPS implementation was associated with a 7% reduction in the average dose and starting dose of IV vitamin D analogues and a 10% reduction in the rate of vitamin D therapy initiation.
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Análise de Séries Temporais Interrompida/métodos , Falência Renal Crônica/economia , Medicare/economia , Sistema de Pagamento Prospectivo/economia , Diálise Renal/economia , Vitamina D/economia , Idoso , Estudos de Coortes , Esquema de Medicação , Feminino , Humanos , Infusões Intravenosas , Falência Renal Crônica/epidemiologia , Falência Renal Crônica/terapia , Masculino , Pessoa de Meia-Idade , Sistema de Pagamento Prospectivo/tendências , Diálise Renal/métodos , Estados Unidos/epidemiologia , Vitamina D/administração & dosagemRESUMO
BACKGROUND: As society has developed and living standards have improved, diabetes has become a severe public health issue. Insulin plays a crucial role in managing hyperglycemia caused by type I diabetes and particular type II diabetes. Many researchers are seeking alternative, more acceptable methods of insulin delivery, such as oral insulin. An oral formulation has become a new goal for insulin delivery in recent years. METHODS: The PubMed and CNKI databases were searched for "oral insulin, " "drug delivery systems, " and "pharmacokinetics, " and 85 relevant articles were selected from the results as material for this review. These papers were authoritative and had a higher number of citations. RESULTS: Oral insulin would be highly advantageous but is poorly absorbed. The main reason for low absorptivity is the hydrolysis of insulin by enzymes in the gastrointestinal tract. Lack of active transport vectors that pass through the intestinal epithelium is also a non-negligible problem. Additional issues need to be considered to facilitate appropriate research, such as long-term efficacy and safety, clinical data, and toxicological characteristics. CONCLUSION: This review summarized recent advances in oral insulin and the pharmacokinetic profile of the suitable delivery system, providing valuable reference material for future research.
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Hipoglicemiantes/administração & dosagem , Insulina/administração & dosagem , Administração Oral , Animais , Sistemas de Liberação de Medicamentos , Humanos , Hipoglicemiantes/farmacocinética , Insulina/farmacocinética , Absorção Intestinal , Inibidores de Proteases/administração & dosagem , Inibidores de Proteases/farmacocinéticaRESUMO
As a new generation of anti-tumor drugs, taxanes has a good clinical efficacy in the treatment of ovarian cancer, breast cancer, non-small cell lung cancer, head and neck cancer. However, low bioavailability of oral administration from low water solubility and low permeability significantly limited the development of their oral applications. Currently, the marketed preparations were non-oral drug preparations, and the injection contained a large number of surfactants (cremophor EL or Tween 80) and organic solvents (ethanol), which could result in fluid retention, hypersensitivity and other side effects, as well as poor compliance. Oral preparation will be an ideal form for development of taxanes medicines. According to the research by our and other groups in recent years, we investigate the technical strategies enhancing the water solubility and absorptive permeability to improve their oral bioavailability. Among them, we emphasize the application prospects of crystallography technology, and provide a theoretical basis to guide future research in the development of oral preparations for taxanes.
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To optimize the extraction technology for Lonicerae Flos and Gardeniae Fructus in Reduning Oral Preparation by information entropy theory. With the contents of chlorogenic acid, gardenoside, luteoloside, and the yield of extract as comprehensive evaluation indexes, the extraction time, dosage of water, and extraction times were selected as factors, the weight of them was determined by information entropy theory, and the extraction technology was optimized by orthogonal test. Optimum extraction technology was: Reflux extraction for 3 times with 12 folds water, 1 h each time. The information entropy theory could be used in optimizing the extraction technology for Reduning Oral Preparation.
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Capsaicinoids show several pharmacological effects including weight loss. However, their pungency limits the long-term use through the gastrointestinal tract. In that sense, the goal of this study was to prepare capsaicinoids-loaded poly(ε-caprolactone) microparticles as an oral carrier in order to improve their gastric tolerability and to make feasible the long-term treatment of obesity. Formulations containing 3, 5 and 10% capsaicinoids were successfully obtained by simple emulsion/solvent evaporation method. Values of encapsulation efficiency above 90% were achieved. Microparticles showed spherical shape and smooth surface. The particle size was suitable for oral use in order to provide an extended release through the gastrointestinal tract. No chemical bond was observed between drug and polymer. Microencapsulation led to drug amorphization. Formulations prolonged the release of capsaicinoids without changing the release kinetic (biexponential model). Microencapsulation increased the gastric tolerability of capsaicinoids because it prevented inflammatory processes in the stomach of rats. Microparticles containing 5% capsaicinoids demonstrated a statistically significant reduction of Lee index, mesenteric and retroperitoneal fat pads of rats with obesity induced by hypothalamic lesion using monosodium l-glutamate. In summary, capsaicinoids-loaded poly(ε-caprolactone) microparticles are low-irritative oral controlled-release carriers for a long-term use in obesity.
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Capsaicina/farmacologia , Portadores de Fármacos/química , Microesferas , Poliésteres/química , Estômago/efeitos dos fármacos , Administração Oral , Animais , Capsaicina/administração & dosagem , Capsaicina/química , Obesidade/tratamento farmacológico , Tamanho da Partícula , Ratos , Ratos Wistar , Estômago/patologia , TemperaturaRESUMO
OBJECTIVE:To optimize the extraction technics of liver-strengthening cholagogue oral preparation.METHODS:The effects of the four factors-the quantity of the added water,the decoction time,the decoction times and the alcohol precipitation concentration on the extraction results were determined with content of total flavonoids taken as index.RESULTS:The best extracting condition was the following,the amount of the added water was 10 times that of the medicinal materials,the decoction duration was 60min,the alcohol precipitation concentration was 50%and the decoction was carried out twice.CONCLUSION:The preparation under this technics is of high clarity and stable contents.
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OBJECTIVE:To analyze the renal lesions induced by oral preparations of traditional Chinese medicines so as to provide theoretic basis for clinical rational drug use.METHODS:The CNKI full-text database between January 1991 and December 2008 were retrieved for clinical reports of renal lesions induced by oral preparations of traditional Chinese medicines.And the pertinent literature was sorted,analyzed and compared.RESULTS:176 reports(totaled 619 cases)were collected.Repeated long-term medication and overdosing etc were the major factors accountable for the renal lesion.CONCLUSION:Importance should be attached to the nephrotoxicity of oral preparations of traditional Chinese medicines,and which should be used rationally in the clinic and periodic examination of patients' renal function should be performed in taking oral preparations of traditional Chinese medicines.