A Randomized, Double-Blind, Placebo-Controlled Study of a Blend of Herbal Extracts Taken Once Per Day for Weight Loss in Healthy Volunteers

Aims: We previously demonstrated that a blend of herbal extracts (Weighlevel®; a mixture of extracts from the leaves of Alchemilla vulgaris, Olea europaea, Mentha longifolia and from the seeds of Cuminum cyminum) taken 3 times per day produces weight loss in preclinical and clinical studies. The aim of the present study was to test the efficacy of a new slow-release formulation (Weighlevel® One) taken once per day on change in body weight and related measures. Study Design: Randomized, double-blind, placebo-controlled study. Place and Duration of Study: Health Clinics in Copenhagen, Denmark between 7 January 2016 and 5 March 2016. Methodology: Thirty-six adult subjects were randomized to consume the herbal blend (n = 20) or placebo (n = 16) once per day for 8 weeks. Weight and waist circumference were assessed weekly. The primary endpoint was the change from baseline in body weight for the herbal blend group compared with placebo. Secondary assessments included waist circumference, appetite, craving, bowel health, and safety and tolerability. Results: After 8 weeks, the herbal blend group lost an average of 3.7 kg (95% CI of 3.0 to 4.5 kg); whereas the placebo group lost 0.1 kg (95% CI of -0.7 to 1.0 kg). This difference in mean weight loss between the herbal blend and placebo groups was statistically significant (P <.001). A statistically significant reduction in waist circumference was also observed for the herbal blend compared with placebo (P <.001). The herbal blend was well tolerated; no adverse events were reported. Conclusion: Daily administration of this blend of herbal extracts, administered once daily, may produce weight loss.

Persistence and efficacy of a new formulation based on dog allomonal repellents against Rhipicephalus sanguineus sensu lato tick / Persistência e eficácia de uma nova formulação baseada em repelentes alomônios de cães contra o carrapato Rhipicephalus sanguineus sensu lato

Abstract Beagles are less susceptible to Rhipicephalus sanguineus sensu lato tick due to the production of the allomones benzaldehyde and 2-hexanone. Our previous published work showed that these compounds can reduce tick burden on susceptible dogs. Here we tested the hypothesis that an increase in repellent dose and release rate could increase repellent efficacy and persistence. Slow-release formulations of these compounds, with higher doses and release rates, were tested on artificially-infested dogs. Ten dogs were randomly assigned to two groups with five dogs each. The treated group received collars with slow-release formulations of the compounds attached, while the control group received collars with clean formulations attached. Five environmental infestations were performed, with the number of ticks (at all stages) on the dogs being counted once a day for 40 days. No significant increase in repellent efficacy was observed with the higher doses and release rates, whereas a greater persistence in repellent activity was observed. Treatment with the formulations resulted in a two-to-three-fold reduction in the number of immature stage ticks for up to three weeks. However, the number of adults was similar in both groups. Loss of repellent activity after the third week of testing coincided with a marked change in the relative release rates for the two compounds. It is hypothesized that relative amounts, rather than absolute amounts, of repellent release from slow-release formulations are important for repellent activity. We also hypothesize that the avoidance of less-preferred hosts by ticks relies on olfactory-mediated perception of specific blends of volatile cues from less preferred hosts.

Resumo Beagles são menos suscetíveis ao carrapato Rhipicephalus sanguineus sensu lato devido à produção de benzaldeído e 2-hexanona. Nosso trabalho anterior já publicado mostrou que esses compostos podem reduzir a carga de carrapatos em cães suscetíveis. Aqui testamos a hipótese de que um aumento na dose destes repelentes e na taxa de liberação poderia aumentar a eficácia e a persistência do efeito repelente. As formulações de liberação lenta destes compostos, com doses e taxas de liberação mais elevadas foram testadas em cães infestados artificialmente. Dez cães foram distribuídos aleatoriamente em dois grupos com cinco cães cada. O grupo tratado recebeu colares contendo formulações de liberação lenta dos compostos, enquanto o grupo controle recebeu colares com formulações limpas. Cinco infestações ambientais foram realizadas, com o número de carrapatos (em todas as fases) nos cães sendo contados, uma vez ao dia, por 40 dias. Não se observou aumento significativo na eficácia do repelente com doses e taxas de liberação mais elevadas e, enquanto observou-se maior persistência na atividade repelente. O tratamento com as formulações resultou em uma redução de duas a três vezes no número de carrapatos dos estágios imaturos, por até três semanas. No entanto, o número de adultos foi semelhante em ambos os grupos. A perda de atividade repelente após a terceira semana de teste coincidiu com uma mudança nas taxas de liberação relativa para os dois compostos. A hipótese é que as quantidades relativas, ao invés das quantidades absolutas de liberação lenta, são importantes para a atividade repelente. Então, a hipótese é de que a repelência apresentada por hospedeiros menos susceptíveis aos carrapatos depende da percepção pelos carrapatos de misturas específicas de voláteis liberados por estes hospedeiros.

The effect of enteral nutrition liquid containing slow release starch on clinical efficacy in elderly patients with diabetes under mechanical ventilation / 中国中西医结合急救杂志

Objective To observe the clinical therapeutic effect of enteral nutrition (EN) liquid containing slow release starch for treatment of elderly patients with diabetes under mechanical ventilation (MV). Methods Fifty-six senile patients with diabetes treated with MV were admitted to Hangzhou Geriatric Hospital from January 2015 to December 2016, they were divided into an observation group (29 cases) treated with continuous instillation of EN liquid containing slow-release starch (Fresubin diabetes) and a control group (27 cases) treated with instillation of standard EN liquid (TPF) by nasointestinal tubes. After treatment for 14 days, the clinical efficacy was evaluated in the two groups. The levels of fasting blood glucose (FBG), 2-hour postprandial blood glucose (2 h PBG), glycosylated hemoglobin (HbA1c), serum albumin (ALB), pre-albumin (PA), arterial partial pressure of oxygen (PaO2), arterial partial pressure of carbon dioxide (PaCO2), and 14-day and 28-day survival rates were observed after treatment in the two groups. Results The blood glucose fluctuation in the observation group was small, while the blood glucose in the control group was significantly elevated necessary to add insulin for treatment. After treatment for 7 days and 14 days, the FBG, 2 h PBG and PaCO2in the observation group were significantly lower than those in the control group [7 days after treatment: FBG (mmol/L) was 8.18±1.91 vs. 8.83±2.08, 2 h PBG (mmol/L) was 9.54±1.86 vs. 9.94±3.01, PaCO2(mmHg, 1 mmHg =0.133 kPa) was 39.0±4.3 vs. 43.0±4.5; 14 days after treatment: FBG (mmol/L) was 7.11±1.01 vs. 9.01±1.22, 2 h PBG (mmol/L) was 8.15±2.35 vs. 10.28±2.77, PaCO2(mmHg): 37.0±3.9 vs. 41.0±4.1], PaO2were significantly higher than those of the control group (mmHg: 7 days after treatment was 81.8±10.1 vs. 76.6±10.7, 14 days after treatment was 92.2±10.0 vs. 77.7±11.2), and the differences were all statistically significant (all P < 0.05). After treatment, the HbA1c in the observation group was lower than that before treatment, and serum ALB and PA were higher than those before treatment, however, there were no statistical significant differences between the two groups (all P > 0.05). The 14-day and 28-day survival rates of the observation group were significantly higher than those of the control group [14 days: 93.1% (27/29) vs. 88.8% (24/27), 28 days: 89.7% (26/29) vs. 85.2% (23/27), all P < 0.05]. Conclusion Using EN preparation containing sustained-release starch for treatment of elderly diabetic patients under MV, their blood glucose levels are stable, the ventilation function and gas exchange of lung are improved, and their survival rates are obviously elevated.

Preparation and characterization of baicalin PEG-PLGA nanomicelles and tissue distribution in rats with acute myocardial ischemia / 中草药

Objective To prepare baicalin-polyethylene glycol-poly (lactic-co-glycolic acid) copolymer (PEG-PLGA)-loaded nanomicelles, and study its in vitro drug release properties and tissue distributed in rats with acute myocardial ischemia. Methods The preparation process of baicalin PEG-PLGA nanomicelles was optimized by orthogonal test. The optimized baicalin PEG-PLGA nanomicelles were characterized by particle size, Zeta potential, and TEM electron microscopy. The in vitro release assay and tissue distribution of the acute myocardial ischemia rat model were used to evaluate this drug delivery system. Results The preferred preparation conditions for baicalin PEG-PLGA nanomicelles were a mass ratio of baicalin to PEG-PLGA at 1:10 with a rotary evaporator rotation rate of 80 r/min and a hydration temperature of 40 ℃. The optimized baicalin PEG-PLGA nanomicelle particle size was (18.5 ± 0.5) nm, the zeta potential was (-10.9 ± 0.7) mV, the drug loading was (7.9 ± 0.3)%, and the encapsulation efficiency was (86.2 ± 2.5)%. The critical micelle concentration of PEG-PLGA nanomicelles was 3.8 μg/mL by oxime assay. TEM showed that baicalin PEG-PLGA nanomicelles presented a spherical shape with uniform particle size, In vitro release test showed that baicalin PEG-PLGA nanomicelles had obvious sustained release characteristics; Tissue distribution test showed that the order of distribution of baicalin PEG-PLGA nanomicelles in normal rat organs was liver > spleen > heart > kidney > lung > brain, while the distribution of baicalin PEG-PLGA nanomicelles in acute myocardial ischemia model was liver > heart > spleen > kidney > brain. Compared with normal rats, the drug concentration in the heart of rats with acute myocardial ischemia showed a significant increase trend in all time periods, and the highest drug concentration at 120 min could reach (2 897 ± 135) ng/mL, the highest drug concentration of the heart in the normal rats was (2 411 ± 89) ng/mL, which indicated that the baicalin PEG-PLGA nanomicelles had good targeting in the acute myocardial ischemia zone. Conclusion Baicalin PEG-PLGA nanomicelles have good drug-loading properties, slow release in vitro, and can accumulate drugs in the ischemic myocardium, which has good cardiac targeting.

Preparation and in vitro release evaluation of slow releasing intrauterine silicone rubber bar made of Panax notoginseng and Rubia cordifolia / 中国中药杂志

To prepare the intrauterine slow release silicone rubber bar made of Panax notoginseng and Rubia cordifolia, and finish its preliminary evaluation of in vitro releasing properties. The open mill method was used for plasticating of silicone rubber. The process parameters of the silicone rubber and drugs mixing were optimized by orthogonal test. The parameters of silicone rubber vulcanization was optimized by single factor test. The preliminary evaluation of in vitro release performance of the silicone rubber bar was conducted with ginsenoside Rg₁, ginsenoside Rb₁, notoginsenoside R₁, purpurin and rubimaillin as the indexes. The results showed that optimum technologic parameters for silicone rubber and drugs mixing：the roller spacing 2 mm; speed ratio 1∶1.2; front roller temperature 55-60 ℃; rear roll temperature 50-55 ℃; and mixing time 20 min. The optimum parameters for silicone rubber vulcanization：temperature 90 ℃, and time 60 min. The studies on release process in vitro revealed that the release process of silicone rubber bar was in line with the Higuchi equations. After 90 days, the cumulative release of ginsenoside Rg₁, ginsenoside Rb₁ and notoginsenoside R₁ was 46.7%, and the cumulative release of purpurin and rubimaillin was 51.9%. The preparation method can be applied to the preparation of silicone rubber bar, with slow release characteristics.

Study on low concentration of nicotine sustained release particles collagen membrane system in promoting the hard palate mucosa wound healing in rats / 医学研究生学报

Objective Studies have shown that low concentrations of nicotine can promote neovascularization and promote wound healing.This article aimed to investigate the influence of low concentration collagen membrane slow-release system on the hard palate trauma of rats.Methods Using poly(lactic acid-co-glycolic acid) (PLGA) copolymer as carrier materials, low concentration nicotine sustained-release particles were prepared by emulsion evaporation method (w/o/w), using collagen membrane as the brace and establish a low concentration collagen membrane system.48 Wistar rats were divided into experimental group and blank group, 3 mm diameter circular wound was made in the forepart palate.Low concentration of nicotine collagen membrane sustained-release particle system and blank collagen membrane (control) were sutured on the wound with 6-0 absorbable thread.Then, observed the wound healing of 0, 3, 7, 10 days and compared the healing differences between each groups.Results Under the electron microscope, the nicotine sustained-release particles were circular, similar size with rough surface, the average diameter were 3.0±0.2μm, the encapsulation efficiency and drug loading rate was 50.2% and 4.12% respectively.In vitro, nicotine sustained-release particles released much more nicotine on the first day, less on the second day, tends to stable and fluctuate within a certain range from the third day on, and declined sharply after about 10 days, nicotine concentration from 3rd to 10th day was fluctuate within 10-5-10-4mol/L.Postoperative wound healing, no significant difference in 3 days(P>0.05), after 7 days, the wound healing of experimental group significantly greater compared with the control (P=0.015).The wound was healed in 10 days after operative, there was no significant difference between two groups(P>0.05).The epithelial proliferation in the experimental group was significantly greater than that in the blank group, there were many fibroblasts, inflammatory cells and new capillaries, the epithelial process is short, the submucosa is loose, and a large number of collagen fibers are produced.The lamina propria is closely connected with the periosteum, and the wound is healed Conclusion Low concentration of nicotine sustained-release particles collagen membrane system may promote wound healing in the hard palate mucosa of rats.

Preparation of compound TF-PLGA microcapsule and its drug release characteristics in vitro / 吉林大学学报(医学版)

Objective:To use polylactic-co-glycolic acid(PLGA) as vector material to prepare the compound total flavonoids of Rhizoma Drynariae(TFRD) and total flavonoids of Chrysanthemum(TFC) sustained release microcapsule TF-PLGA microcapsules,and to investigate the the best preparation technique of TF-PLGA microcapsules and their sustained release characteristics in vitro.Methods:The TF-PLGA microcapsules were prepared with TFRD,TFC,and PLGA by emulsifying-solvent evaporation technique under certain conditions.With the encapsulation efficiency(EE) as the evaluation indicator,the optimal formulation was verified by single factor experiment and orthogonal design;the general morphology,the particle size and distribution of the microcapsules were observed by light microscope(LM) and scanning electron microscope(SEM);the cumulative drug release rate of TF-PLGA microcapsules was detected by constant temperature commotion method in vitro and the release curves of the TF-PLGA were drawn.Results:The optimal prescription was as follows:the concentration of PLGA was 140 g·L-1,oil phase volume was 1.4 mL,emulsifying speed was 900 r·min-1,emulsifying time was 5 min,the average EE was(83.89±2.30)%,and the average drug loading rate(DL) was(5.90±0.07)%.The LM and SEM resluts showed that the TF-PLGA microcapsules presented as round ball,the average particle size was(44.34±14.68)μm,and the distribution was relatively narrow.The drug release in vitro results showed that the initial drug release rate(24 h)was about 40%,and the cumulative drug release rate was over 90% after 50 d.Conclusion:The TF-PLGA sustained release microcapslue has better drug-loaded and sustained-release effects with simple preparation technique and better repeatability.

Fertilizers with coated urea in upland rice production and nitrogen apparent recovery / Doses de fertilizantes com ureia revestida na produção de arroz de terras altas e recuperação aparente de nitrogênio

Urea is the most used N fertilizer for upland rice, however, a great percentage of N loss can occur with the use of this fertilizer. The use of products that provide reduction of N loss for urea fertilizers can contribute to increase N use efficiency. The objective of this study was to determine the effect of N rates applied in the form of coated urea in the content and accumulation of N in dry biomass, apparent recovery of nitrogen and grain yield of upland rice. The experimental design was a randomized complete blocks arranged in a 4 x 3 + 1 factorial scheme. The treatments consisted of four sources of N fertilizer [1. Common urea; 2. Polymer-coated urea for slow release of N (PCU); 3. urea with the urease inhibitor N-(n-Butyl) thiophosphoric triamide (NBPT); and 4. urea coated with copper sulfate and boric acid as urease inhibitors (UCCB)], with three fertilization rates (30, 60 and 90 kg ha-1 of N). In addition, we included a control treatment without N application. Coated urea did not provide increases in rice grain yield in relation to common urea. The increasing amount of N resulted in significant increases in rice grain yield (from 3217 to 5548 kg ha-1, 2010/11, and from 3392 to 4560 kg ha-1, 2011/12). The apparent nitrogen recovery rate decreased with the increase in N applied doses.

A ureia é o fertilizante nitrogenado mais utilizado para o arroz de terras altas, no entanto, esse fertilizante tem grande percentual de perda de N. O uso de produtos que proporcionam redução da perda de N em fertilizantes com ureia pode contribuir para aumentar a eficiência de uso do nitrogênio. O objetivo deste estudo foi determinar o efeito de doses de N aplicadas na forma de ureia encapsulada no teor e acúmulo de N na biomassa seca, recuperação aparente de nitrogênio e produtividade de grãos de arroz de terras altas. O delineamento experimental foi em blocos ao acaso no esquema fatorial 4 x 3 + 1. Os tratamentos consistiram de quatro fontes de N fertilizante [1. ureia tradicional; 2. Polímero de ureia revestida para liberação lenta de N (PCU); 3. ureia com o inibidor de urease N- (n-butil) triamida tiofosfórico (NBPT); e 4. ureia revestida com sulfato de cobre e ácido bórico como inibidores de urease (UCCB)], com três doses de fertilizante (30, 60 e 90 kg ha-1 de N). Além disso, incluímos uma testemunha sem aplicação de N. Ureia revestida não forneceu aumentos no rendimento de grãos de arroz em relação à ureia comum. O aumento da quantidade de N resultou em aumentos significativos no rendimento de grãos de arroz (de 3217 para 5548 kg ha-1, 2010/11, e de 3392 para 4560 kg ha-1, 2011/12). A taxa de recuperação aparente de nitrogênio diminuiu com o aumento das doses aplicadas de N.

Study the release kinetics of curcumin released from PVA/curcumin composites and its evaluation towards hepatocarcinoma.

The polymer composites based on Polyvinyl alcohol loaded with different concentrations of commercial curcumin were prepared to be applied forcontrolled release drug delivery system to overcome the growth promotion of tumor cells. The prepared composites were subjected to drug release in aqueous media at room temperature. It was found that the amount of the released curcumin changed according to different pH media and the concentration of the loaded drug onto the polymer carrier. The diffusion coefficient of the released curcumin from the prepared composites was found to be 2.739X10-2, 1.638X10-2, and 5.777X10-4 in basic, acidic and neutral solution respectively according to Higuch's equation. The results of the in/vitro cytotoxic activity of the released curcumin showed sustained antiproliferative potency up to 30 % growth inhibition against the human liver cancer cell line (HEPG2) which extended to 25 days, to overcome hepatocarcinoma.

Clinical effect of endoscopic implantation of accurate and slow-release particles for advanced esophageal carcinoma / 中国内镜杂志

Objective To observe the clinical effects by endoscopic implantation of accurate and slow-release particles for advanced esophageal carcinoma. Methods Under endoscopy, we dividing the whole focus into several layers by each 1.0 cm and implanting one slow-release particles (about 10 mg) in each point whose interval is 1.0 cm. One course of treatment includes three-time implantation and each treatment needs four weeks, by the way the details depend on the state of illness. In this research, all of patients complete the treatment smoothly. By comparing the patients’ situation before treatment, three-month treatment and six-month treatment, which include the remission of clinical symptom, the changing of focus area, the improvement of swallow function, untoward effect and life quality, et al. Results The results show several test indexes changed a lot. When treated for 3 months and 6 months, the levels of focus area and swallow difficulty classification were decreased significantly (P 0.05), by the way there isn’t individual difference appearing because of a little short of testing time and a few of samples. In addition, the WBC had a significant statistical difference between before treatment and three-month treatment (P < 0.05), and the ratio of complication didn’t have a significant change. Conclusions Endoscopic implantation of 5-Fu slow-release particles for the treatment of advanced esophageal carcinoma is a safety, high efficacy, low toxic and good tolerant palliative treatment.

Ghost pill: knowledge and awareness of this phenomenon among health care professionals.

Background: Slow release (SR) drug formulations associated with the passage of intact tablet like object in faeces sometimes known as the “ghost pill” have been in the market for many years. Anecdotal evidence suggests that few health care professionals are aware of this phenomenon. Our study aims were to find out what proportion of health care professionals was aware of the ghost pill phenomena and what drug formulations and specific drugs were associated with it. Methods: A survey was conducted among health care professionals at three hospital sights in the West Midlands, UK. The subjects included doctors, nursing staff, pharmacists, and other allied professionals involved in patient care. Results: A total of 321 health care professionals were included in the final analysis. Very few, 12.8% (41) have heard of the ghost pill phenomenon and a further 14 (4.4%) have come across of a patient who has experienced it. Only 13 (4%) correctly associated the phenomenon with SR drug formulations. Conclusion: Our survey has shown that the ghost pill phenomenon, a normal outcome of a novel way of delivering orally taken SR drugs, is not well-known among health care professionals. Lack of awareness of it has implications to trainers, medical and nonmedical prescribers and nursing staff working with patients who are taking these medications. Lack of awareness among health care staff, may result in relevant information not being shared with patients at the time of prescribing or when patients enquires of it.

Dual-drug sustained-release carrier:Preparation and performance / 中国组织工程研究

BACKGROUND: During conventional treatment for bone tuberculosis, there is a low effective concentration of anti-tuberculosis drugs, and the therapeutic effect is poor. OBJECTIVE:To develop a new biomaterial as a slow-release artificial carrier that can be directly implanted into the surrounding tissue of bone tuberculosis, maintain a certain anti-tuberculosis drug concentration for a long time, thereby playing an effective therapeutic action. METHODS:Rifampicin/polylactic acid/glycolic acid microspheres and isoniazid/polylactic acid/glycolic acid microspheres were prepared using the emulsion-solvent evaporation method. Usingα-cyanoacrylate, a biological adhesive, two kinds of microspheres were processed into a long-term slow-release bicomponent drug carrier. Then, in vitro release characteristics of the dual-drug sustained-release carrier were observed. After that, the dual-drug sustained-release carrier was implanted into rabbit intertrochanteric femur bone defects for observing drug release concentrations, histocompatibility and bone defect healing at different time points after drug delivery carrier implantation. RESULTS AND CONCLUSION:For rifampicin/polylactic acid/glycolic acid microspheres, the mean particle size was (240±13)μm, and the drug loading load rate was (26±1.5)%. For isoniazid/polylactic acid/glycolic acid microspheres, the mean particle size was (250±10)μm, and drug loading rate was (28±1.8)%. The in vitro cumulative release rate could reach 80%for rifampicin and 90%for isoniazid at day 90. The in vivo released concentration of rifampicin and isoniazid within 90 days was (0.5±0.4) and (0.6±0.3)μg/g, respectively. There were a smal amount of infiltrated neutrophils between the fascia and muscle fibers after the drug delivery carrier was implanted, and the amount of neutrophils in the muscle were reduced significantly at day 59. X-ray plain film showed that bone defects decreased obviously in size. These findings indicate that this dual-drug sustained-release carrier can maintain a certain anti-tuberculosis drug concentration in the surrounding tissues of bone tuberculosis, which is expected to provide a new type of dual-drug delivery carrier in the surgical treatment of bone tuberculosis.

Disponibilidade de fósforo em solos com diferentes texturas após aplicação de doses crescentes de fosfato monoamônico de liberação lenta / Phosphorus availability in soils with different textures after application of growing doses of slow release monoammonium phosphate

A disponibilidade de P no solo é dependente do seu teor de argila, quanto maior o seu teor e o tempo de permanência do P no solo, maior sua adsorção e menor sua disponibilidade. O uso de fontes de liberação lenta podem aumentar esta disponibilidade, uma vez que o revestimento impede o contado do fertilizante com os óxidos, diminuindo sua adsorção. O experimento foi conduzido no Laboratório de análises de fertilidade do solo CeFert, localizado no Campus do Centro Universitário de Patos Minas, em Minas Gerais. Objetivou-se quantificar os teores de P disponível, após incubação de solos com diferentes texturas. Os tratamentos foram testemunha (sem aplicação de P) e doses crescentes de P2O5 (50; 100; 200 e 400 mg dm-3), utilizando o fosfatado monoamônico de liberação controlada, em solo argiloso, médio e arenoso. Avaliou-se o P disponível aos 30, 60 e 90 dias da incubação do fertilizante com o solo. Os resultados demonstraram que o solo argiloso apresentou maior disponibilidade do nutriente quanto maior a dose aplicada.

The availability of P in soil is dependent on its clay content, the higher degree and permanence of soil P, the greater its absorption and lower availability. The use of slow-release sources may increase this availability, since the coating prevents the counting of the fertilizer with the oxides, thus reducing their adsorption. The experiment was conducted in the laboratory of analysis of soil fertility CeFert, located on the campus of the Centro Universitário de Patos Minas, in Minas Gerais. The objective was to quantify the levels of available P after incubation of soils with different textures. The treatments were control (no P application) and increasing doses of P2O5 (50, 100, 200 and 400 mg dm-3), monoammonium phosphate using controlled release, in clay soil, sandy medium. We assessed P available 30, 60 and 90 days incubation of the fertilizer with soil. The results showed that the clay soil had a higher nutrient availability as the doses applied.

Preparation and in vitro transdermal diffusion characteristics of ephedrine chitosan-modified liposomes gels / 中草药

Objective To prepare the ephedrine chitosan-modified liposomes gels, detect the particle diameter and the entrapment efficiency, and investigate the transdermal diffusion characteristics in vitro. Methods Ephedrine liposomes suspensions were prepared using thin film evaporation and slowly dropped by 0.35% chitosan solution with pH values 5-6 in order to prepare the chitosan-modified liposomes gels. The particle diameter of the modified liposomes was detected by Laser Scattering Particle Size Distribution Analyzer. The entrapment efficiency was determined by reverse dialysis method with HPLC. Using Franz Diffusion Cell to investigate transdermal diffusion characteristics of the modified liposomes gels in vitro. Results The mean particle diameter of the modified liposome prepared was from 1 400 to 1 900 nm. The average entrapment efficiency of the modified liposomes was up to (41 ± 0.94)%. Ephedrine in the modified liposomes could penetrate rat skin. The results of the transdermal diffusion test showed the cumulative penetration amount of the ephedrine chitosan-modified liposomes gels was lower than that in the ephedrine solutions with time variation. Conclusion This preparatiom is prepared with simple technology and stable character. The entrapment efficiency of the ephedrine is higher and the assay method is simple and accurate. The penetrating rate of ephedrine is slow and the drug releasing is stable.

Preparation of folate-targeted Ergosta-4,6,8(14),22-tetraen-3-one liposomes and its evaluation in vitro and pharmacokinetic studies / 中国药学杂志

OBJECTIVE: To prepare folate-conjugated ergosta-4,6,8,22-tetraen-3-one liposomes(FLE). Then to study the release feature of FLE in vitro and the eytotoxieity and targeting ability of it via folate receptor-mediated endocytosis on tumor cells in vitro. Pharmacokinetic characterization was also studied in rats. METHODS The characteristics were measured by transmission electron microscope(TEM), laser light scattering granularity equipment and HPLC. Dialytic method was used to determine ergone release rate of FLE in vitro. The cytotoxicity and targeting ability of FLE on HeLa in vitro was measured by MTT assay. The concentrations of ergone in plasma of rats and their pharmacokinetic behaviors after oral administration were studied by HPLC. The pharmacokinetic parameters were computed by software DAS2.0. RESULTS: The prepared FLE was round and uniform, and the mean particle size was 112 nm. The encapsulating efficiency of it reached 73%. The experiment of drug release in vitro follows Higuchi releasing process and showed significant sustained-release feature. The IC50 of ergone, LE and FLE was 10, 14, 5 μg · mL-1, respectively. Compared with ergone solution, AUC in FLE had increased significantly. And the residence time of ergone was prolonged. CONCLUSION: The FLE were characterized by sustained-release performance, target recognition, and low toxic and side effect and did improve the bioavailability of ergone significantly. It can also be expected to be used for tumor by targeting therapy.

Preparation of captopril pulsed pellets and its pharmacokinetics in rats / 中国药学杂志

OBJECTIVE: Compared with the compound captopril tablets (compound Cap), to study the pharmacokinetics characteristics and bioavailability in twelve wista rats after oral administration of Cap pulsed pellets and compound CAP tablets by HPLC. METHODS: To prepare captopril pulsed pellets (Cap pulsed pellets). The pharmacokinetic parameters were computed by software program DAS2.1. RESULTS: In vivo the lag time for 4.75 h, compared with ordinary tablet, it has an obviously lag time, tmax was 9.67 h and the relative bioavailability was(117.29 ± 46.87)%. CONCLUSION: The release of CAP from CAP pulsed sustained-release pellets was shown to be sustained-release after an conspicuous lag time in vitro and in vivo. So the drug can be taken by the patient before sleeping and can achieve the purpose in the morning. Copyright 2012 by the Chinese Pharmaceutical Association.

Experimental study of acute toxicity of slow-release PLGA-gemcitabine microsphere / 肿瘤研究与临床

Objective To study the acute toxicity of slow-release (poly lactic-co-glycolic acid) PLGA-gemcitabine microsphere and gemcitabine on mice.Methods Up and down procedure (UDP) was used to determine the median lethal dose (LD50) of PLGA-gemcitabine microsphere and gemcitabine on mice respectively.Results The LD50 of PLGA-gemcitabine microsphere on mice was 256.30 mg/kg,gemcitabine was 8.91 mg/kg.The difference was 28.8 times.Conclusion PLGA-gemcitabine microsphere can markedly reduce the acute toxicity of gemcitabine.

Organic matrix based slow release fertilizer enhances plant growth, nitrate assimilation and seed yield of Indian mustard (Brassica juncea L.).

Field experiments were conducted to study the effect of organic matrix based slow release fertilizers (SRFs) on plant growth, nitrate assimilation and seed yield of Brassica juncea L. cv. pusa bold. The agro-waste materials like cow dung, clay soil, neem leaves and rice bran were mixed together in 2:2:1:1 ratio and used as organic matrix for the immobilization of chemical fertilizer nutrients with commercial grade saresh (Acacia gum, 15% solution) as binder. Different fertilizer treatments were organic matrix based slow release fertilizers, SRF-I (542.0 kg ha-1); SRF-II (736.5 kg ha-1) and chemical fertilizer combinations, boron (3 kg ha-1)+sulphur (15 kg ha-1)+nitrogen (80 kg ha-1) and boron (3 kg ha-1) + sulphur (15 kg ha-1)+nitrogen (80 kg ha-1)+phosphorus (15 kg ha-1)+potassium (100 kg ha-1). Organic matrix based SRF-II released ammonium up to 50-d in wet soil under laboratory conditions which showed maximum retention of the nutrients. A very significant increase in plant growth, nitrate assimilation and seed yield was recorded in organic matrix based SRF-II applied plants. The maximum percent increase in biomass production was observed with organic matrix based SRF-II (increase of 65.8% in root fresh weight, 38.0% in root dry weight, 45.9% in leaf fresh weight plant-1 and 27.5 % in leaf dry weight plant-1 in 60-d old plants). It also increased the acquisition and assimilation of nitrate from the plant’s rhizosphere which was evident by 45.6% increase in nitrate, 27.5% in nitrite and 11.7% in nitrate reductase activity (NRA) in leaves of 45-d old plants over control. The organic matrix based SRF-II significantly increased the seed yield by 28% in Indian mustard. Cost analysis revealed that this formulation is cost effective as it is based on agro waste materials.

Adubação antecipada na cultura da soja com superfosfato triplo e cloreto de potássio revestidos por polímeros / Antecipated fertilization on soybean with triple superphosphate and potassium chloride coated with polymers

Neste trabalho, objetivou-se comparar épocas e doses de aplicação do superfosfato triplo (SFT) cloreto de potássio (KCl) com e sem revestimento por polímero no desempenho produtivo da soja em condições edafoclimáticas de cerrado. O experimento foi realizado em Rio Verde, GO, em um Latossolo Vermelho distroférrico. Os tratamentos foram dispostos em delineamento de blocos ao acaso, em esquema fatorial 2x2x2+1. O primeiro fator foi constituído pelos fertilizantes SFT e KCl revestidos ou não por polímeros, o segundo por duas doses de fósforo e potássio (40 + 40 e 80 + 80 kg ha-1 P2O5 e K2O), e o terceiro, por duas épocas de aplicação dos fertilizantes (15 dias antes da semeadura e na semeadura). Inclui-se ainda, um tratamento testemunha sem adubação. Foi avaliada a produção de biomassa, a produtividade de grãos e componentes de produtividade. Houve resposta à aplicação da adubação com P e K na produção de massa fresca e produtividade, sendo a ausência de adubação prejudicial ao desenvolvimento da cultura da soja. A aplicação a lanço de superfosfato triplo e cloreto de potássio, revestidos por polímeros 15 dias antes da semeadura, proporcionou maior produção de massa seca, número de vagens por planta e produtividade de grãos de soja em relação aos fertilizantes convencionais. Quando aplicados na semeadura, os fertilizantes convencionais e fertilizantes revestidos por polímeros conferiram a mesma produção de massa seca e produtividade de grãos de soja.

The objetive of this work was to compare times and application rates of triple superphosphate (TSF) and potassium chloride (KCl) with and without polymer coating on soybean yield performance in the cerrado environmental conditions. The experiment was conducted in Rio Verde, GO, in an Oxisol. Treatments were arranged in a randomized block design, in factorial 2x2x2+1. The first factor consisted by fertilizer TSF and KCl coated or not by polymer, the second by two doses of phosphorus and potassium (40 + 40 and 80 + 80 kg ha-1 P2O5 and K2O, respectively), and the third by two times of application fertilizer (15 days before sowing and at sowing). It also includes a treatment control without fertilization. Biomass yield, grain yield and yield components were evaluated. There was a response to the application of fertilizer P and K in fresh mass production and productivity, with the absence of fertilizer detrimental to the development of soybean. The broadcast application of superphosphate and potassium chloride coated polymer 15 days before sowing promoted dry matter yield, number of pods per plant and grain yield of soybeans compared to conventional fertilizer. When applied at sowing, the conventional fertilizer and slow release fertilizers promoted the same dry matter yield and grain yield of soybeans.

Endoscopic implantation of 5-FU slow-release particles for advanced gastroenteric tumor / 中国综合临床

Objective To investigate the feasibility, safety and short-term efficacy of endoscopic implantation of 5-FU Slow-release Particles for advanced gastroenteric tumor. Methods During the endoscopy procedure,slow-releasing 5-FU agents were implanted densely into the tumors and infiltrated area. Forty-five to sixty pieces of agents ( each piece equivalent to 1.67 mg 5-FU)were injected, which containing an average dose of 100 mg 5-FU. Results A total of 13 advanced gastric cancer patients were enrolled into this study. Significant effects were observed in 3 patients and good effects in 8 patients, but 2 cases with no effects. The total effective rate was 84.62%. The endoscopy examination showed that the size of tumors reduced in various degree at 1 - 2months after the implantation. No hemorrhage or perforation was observed. Parameters of hepatorenal function and routine blood test were stable after implantation. Conclusion Endoscopic implantation of 5-FU Slow-release Particles can relieve the symptoms of patients and limit tumor growth in advanced gastroenteric tumor with no marrow and hepatorenal functional impair.