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Objective To investigate and analyze the efficacy of CT guided percutaneous cisplatin cisplatin implantation in the treatment of non-small cell lung cancer.Methods 80 cases of non small cell lung cancer patients in our hospital from January 2015 to March 2016 were randomly divided into the control group and the experimental group, each group of 40 patients.The control group was treated with cisplatin and cisplatin, and the patients in the experimental group were treated with CT guided percutaneous cisplatin sustained-release implantation.The clinical standards of the experimental group and the control group were compared and analyzed.Results After treatment, the number of invalid cases in the experimental group was 8 cases, the effective number was 32 cases, the effective rate was 80%.The number of invalid cases in the control group was 32 cases, and the effective number was 8 cases.The effective rate of the patients in the experimental group was significantly higher than that in the control group (P<0.05).The 1-year survival rate of the experimental group was 77.5%, significantly higher than that of the control group, and the survival rate was 60%, with statistical difference (P<0.05).The incidence of adverse reactions in the experimental group (37.5%) was significantly lower than that in the control group (17.5%), with statistical difference (P<0.05).Conclusion CT guided percutaneous treatment of percutaneous intratumoral implantation of slow-release cisplatin in treatment of non-small cell lung cancer can improve the treatment efficiency in a certain degree, high security, with the further promotion and application significance.
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Objective To optimize the formulation of controlled-onset extended-release tablets of nicorandilby central composite design-response surface method. Methods The tablets containing nicorandil were prepared bydry-compression coating technique.The influence factors included the amount of HPMC, the amount of EC, and the ratio of lactose/MCC in coating film. The evaluation parameter was Q4 h and Q5 h . The possibly optimal formulation was predicted by response surface method. Results The OD was simulated using second-order polynomial equation and the r2was 0.970 1.Optimal prescription was as follows:HPMC 89.96 mg, EC 46.21 mg, Lactose/MCC 1.87.Bias between the observed and predicted values of the OD was within 0.43%. Conclusion The controlled-onset extended-release tablets of nicorandil can release drug quickly in vitro at the predetermined time.Central composite design-response surface method can be used to optimize the formulation and the model developed in this study was proved highly predictable.
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The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
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The present study was an attempt to formulate and evaluate enteric coated tablets for Ilaprazole to reduce the gastrointestinal tract side effects. Four formulations of core tablets were prepared and one who shows rapid disintegration (near around three minutes) was selected for enteric coating. Ilaprazole which have an irritant effect on the stomach can be coated with a substance that will only dissolve in the small intestine. Enteric coat was optimized using two different polymers such as HPMCP 50 and Eudragit L 100 in different concentrations. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics and in-vitro release study. 2.5% seal coating on core tablets was optimized and 9% enteric coating on seal coated tablets was performed using HPMC P 50 (60%), triethyl citrate (10%) and IPA:DCM (60:40) which gives the highest dissolution release profile and f2 value.
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Background Proliferative vitreoretinopathy(PVR) is a tissue repair prevention and treatment of PVR in clinic.Natural delayed release microballoons are therefore becoming a hot spot for its easy manipulation,large lading dose and long acting duration.Objective This study was to evaluate the effect of 5-fluorouracil natural delayed release microballoons on the prevention of PVR.Methods The lymphocytes were collected from clean pigment rabbit to prepare the 8×107/ml cell suspension with complete culture fluid.PVR models were established in 45 healthy pigment rabbits by intravitreal injection of lymphocyte suspension.The animals were randomly divided into 3 groups and 15 rabbits for each.0.1ml normal saline,10g/L or 20g/L 5-fluorouracil natural delayed release microballoons were injected into vitreous cavity respectively.PVR was graded on Fastenberg's method under the slit lamp in 1,2,4,8 weeks.The animals were sacrificed and retinas were obtained for the histopathological and ultrastructural examination in the eighth week after administration of drug.Results The numbers of eyes with different grades of PVR were significantly different among 3 groups in 1 week,2,4,8 weeks(P＜0.05).The eye numbers with PVR was significant less in 20g/L Fu group than those of 10g/L Fu group and normal saline group(P＜0.05).There was statistical difference in PVR ranking among these 3 groups in 8 weeks after injection of drug(H=46.795,P＜0.05).The morphology and ultrastructure of retinas under the light microscope and transmission electron microscope were near normal in all of the three groups.Conclusion Implantation of 5-fluorouracil natural delayed release microballoons into vitreous cavity is effective and safe in preventing PVR in experimental model,and the therapeutic effect of microballoons with 20g/L 5-Fu is better.
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No presente trabalho, foram elaboradas microesferas de acetobutirato de celulose (ABC) contendo cetoprofeno com o objetivo de prolongar a liberação do fármaco. Utilizou-se a técnica de emulsão e evaporação do solvente, variando-se os seguintes parâmetros: massa molar do ABC e a adição ou não de poli(3-hidroxibutirato) (PHB), segundo um planejamento fatorial 22. Maiores eficiências de encapsulação do cetoprofeno foram obtidas quando utilizado ABC com maior massa molar e a adição do PHB levou a uma diminuição do percentual de fármaco encapsulado. Todas as formulações originaram partículas esféricas, com cristais de fármacos aderidos à superfície externa e matriz polimérica porosa quando adicionado o PHB. Os perfis de liberação in vitro indicaram que o aumento da massa molar do ABC levou a uma diminuição do percentual de fármaco inicialmente liberado e a um prolongamento de sua liberação. Por outro lado, a adição do PHB acelerou a liberação do cetoprofeno a partir das microesferas.
In the present study, cellulose acetate butyrate (CAB) microspheres containing ketoprofen were produced, with the objective of prolonging its release. The emulsion/solvent evaporation technique was used to make the spheres, varying the parameters (1) CAB molecular weight and (2) addition or not of poly(3-hydroxybutyrate) [PHB], to optimize drug encapsulation, following a 2² factorial design. Higher ketoprofen encapsulation efficiency was obtained when higher molecular weight CAB was used, while the addition of PHB caused a decrease in the percentage of encapsulated drug. All the preparations produced spherical particles, with drug crystals adhering to the external surface, and a porous polymer matrix when PHB was used. The in vitro release profiles indicated that lowering the CAB molecular weight led to a decrease in the drug initially released and a prolonged release. On the other hand, the addition of PHB accelerated the release of the ketoprofen from the microspheres.
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Preparaciones de Acción Retardada , Cetoprofeno , MicroesferasRESUMEN
@#Objective To observe the pharmacokinetics and concentration of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) in brain tissue after BCNU-polylactic acid (PLA) delayed release wafer embedded in brain tissues of dogs.Methods 10% BCNU-PLA delayed release wafer were prepared and embedded in brains of 12 dogs. Peripheral blood of dogs was taken and the animals were executed for brain tissue after surgery in different times. BCNU concentrations in blood and brain tissue were quantified by high-performance liquid chromatography.Results BCNU was able to be detected at 22nd hour, and the Cmax (average 243.64 ng/ml) appears at 35th hour after surgery. The average BCNU concentration in brain tissue was 26.60 μg/g at 5th day after surgery.Conclusion BCNU-PLA delayed release wafer is a useful type for treatment of malignant gliocoma.
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Objective To prepare Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and study its pharmacokinetics and pharmacodynamics in dogs in vivo. Methods Borneol and the extracts of Cortex Moutan, Rhizoma Chuanxiong, and Rhizoma Cyperi prepared by CO2 supercritical fluid extraction method were solidified or included with ?-cyclodextrin. Pellets were prepared by means of powder layering with the solidified extracts and borneol. The pH-dependent delayed-release pellet system was prepared by coating with HPMC, Eudragit L-30D-55, and Eudragit L100-S100 (1∶5) combinations, respectively. Tongshuan Jiuxin pH-Dependent Delayed-release Capsula was prepared by mixing the three kind of pellets at the ratio of 1∶1∶1. The concentration of paeonol in plasma was determined by HPLC and the pharmacodynamic parameters were evaluated by serum pharmacology method. Results The results from the paeonal concentration in plasma showed that the mean residence time (MRT) in vivo were 8.04 h for Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and 2.89 h for Tongshuan Jiuxin Tablet, and the relative bioavailability was 126.3%. Meanwhile, the results from the pharmcodynamic parameters evaluated by serum pharmacology method showed that the MRT were 11.27 h for Tongshuan Jiuxin pH-Dependent Delayed-release Capsula and 5.94 h for Tongshuan Jiuxin Tablet, and the relative bioavailability was 129.1%. Conclusion Tongshuan Jiuxin Tablet has the characteristics of rapid absorption, qucik elimination, and shorter action-maintaining time. Whereas Tongshuan Jiuxin pH-Dependent Delayed-release Capsula has the characteristics of rapid absorption, prolonged and relaxed effective action compared with Tongshuan Jiuxin Tablet.