ABSTRACT
Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）. Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: tmax:（3.2±0.4）and（0.9±0.1）h, Cmax:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ± 30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）.
ABSTRACT
Objective@#To compare the clinical effect of metoprolol combined with valsartan and nifedipine controlled release tablets in the treatment of primary hypertension complicated with coronary heart disease(CHD).@*Methods@#200 primary hypertension patients with CHD were selected, and they were randomly divided into observation group and control group according to the digital table, 100 cases in each group.The observation group was treated with metoprolol combined with valsartan, the control group was treated with nifedipine controlled release tablets.The clinical effect of the two groups was compared.@*Results@#Before treatment, the diastolic and systolic blood pressure of the control group were (106.8±12.3)mmHg and (173.4±22.8)mmHg, respectively, which of the observation group were (104.3±11.4)mmHg, (177.6±24.2)mmHg, respectively, the differences were not statistically significant between the two groups(t=1.265, 0.337, all P>0.05). The diastolic and systolic blood pressure after treatmentin of the observation group were (131.6±17.4)mmHg, (85.3±7.1)mmHg, respectively, and the total effective rate of the observation group was 93.0%(93/100), the improvement rate of angina symptoms of the observation group was 86.0%(86/100), which were significantly better than those of the control group[(131.6±17.4)mmHg, (85.3±7.1) mmHg, 68.0%(68/100), 63.0%(63/100)], the differences were statistically significant (t=5.229, 6.122, χ2=9.148, 7.224, all P<0.05).@*Conclusion@#The combination of metoprolol and valsartan has better effect in the treatment of primary hypertension complicated with CHD compared with nifedipine controlled release tablets.
ABSTRACT
Objective To investigate the clinical efficacy and safety of oxycodone hydrochloride controlled-release tablets in treatment of advanced cancer pain.Methods 130 patients with advanced cancer pain were selected and randomly divided into two groups,65 patients received oxycodone hydrochloride controlled-release tablets as observation group,65 patients received morphine sulfate controlled-release tablets as control group.Quality of life score was evaluated, clinical efficacy and safety were compared between two groups.Results After treatment, cancer pain of patients in two groups were relieved than pre-treatment (P<0.05), and patients in observation group were better than control group (P<0.05).After treatment, the quality of life in two groups were all improved ( P <0.05 ) , and patients in observation group was more obvious than control group ( P <0.05 ) .During the treatment, adverse reactions occurred in different degrees, and the incidence of adverse reactions in the observation group was lower than control group (P<0.05).Conclusion Oxycodone hydrochloride controlled-release tablets are effective drug in treatment of advanced cancer pain,which can significantly relieve pain and improve quality of life.
ABSTRACT
OBJECTIVE:To evaluate the clinical efficacy and safety of triple therapy in the treatment of type 2 diabetes melli-tus(T2DM),and to open up more effective way to treat T2DM. METHODS:76 patients with T2DM were randomly divided into control group and observation group with 38 cases in each group. The control group received conventional therapy,i.e. oral hypo-glycemic agents Glipizide controlled-release tablet 5 mg,qd+Metformin tablets 5 mg,tid. The observation group was treated with triple therapy,i.e. berberine hydrochloride 0.5 g,tid,for 3 months,on the basis of control group. The biochemical index were compared between 2 groups Before and after treatment,including fasting blood glucose (FBG),postprandial 2 h blood glucose (2 h FPG),glycosylated hemoglobin(HbA1c),insulin(FINS),total cholesterol(TC)and triglyceride(TG),high/low density li-poprotein cholesterol (HDL-C/LDL-C),etc.,to evaluate its safety. RESULTS:After treatment,FBG,2 h FPG,HbA1c,FINS, TC and LDL-C of 2 groups and TG of observation group were all decreased significantly,while the level of HDL-C was increased significantly,with statistical significance(P<0.05);FBG,2h FPG,HbA1c,FINS,TC and LDL-C of observation group were im-proved more significantly than control group,the difference was statistically significant(P<0.05). ADR was found in 4 patients of observation group,and the symptoms were relieved after symptomatic treatment. CONCLUSIONS:In the treatment of T2DM,tri-ple therapy can down-regulate blood lipid and blood sugar stably,have definite therapeutic efficacy and little side effect.
ABSTRACT
Objective To study the antihypertensive effects and treatment compliance of extended release nifedipine tablets and nifedipine controlled release tablets .Methods 120 cases of patients with hypertension from April 2012 to April 2013,with informed consent of patients and in accordance with the medical ethics standard ,were divided into the group I and group II of 60 cases in each group according to the random number table method , the group I was given extended release nifedipine tablets for treatment while the group II was given nifedipine controlled release tablets for therapy ,antihypertensive effect ,treatment compliance and adverse reaction of two groups were com-pared.Results The total efficiency of group II was 93.3%,which was higher than 80.0%of the group I,there was statistically significant differences between the two groups (χ2 =12.019,P=0.019);The adverse reaction rate of group II was 8.3%,which was significantly lower than 18.3%of the group I,there was statistically significant differ-ences between the two groups (χ2 =11.271,P=0.021);The treatment compliance of group II was 96.7%,which of the group I was 95.0%,there was no significant differences between the two groups (χ2 =5.419,P =0.067). Conclusion Nifedipine controlled release tablets has a better antihypertensive effect ,with less adverse reaction when compared with nifedipine controlled release tablets .
ABSTRACT
Objective To observe the therapeutic effect of methylphenidate hydrochloride controlled-release tablets (OROS-MPH) on attention-deficit hyperactivity disorder (ADHD). Methods Seventy-two cases of children with ADHD were randomly divided into treatment group (40) and control group (32). Cases of treatment group were given 0.8-1.0 mg??kg-1 of OROS-MPH for three months. Cases of control group were given 1.2-1.4 mg??kg-1 of atomoxetine hydrochloride for three months. After 12 weeks treatment, children were evaluated by Wechsler intelligence test, Integrated visual and auditory continuous performance test (IVA-CPT), the SNAP-Ⅳ effect assessment scale and TESS scale. Results The treatment efficiency was similar in both groups. Attention deficit and hyperactivity in both groups were improved obviously. Wechsler intelligence score was significantly elevated ( P<0. 05), SNAP-Ⅳ score was significantly decreased ( P<0. 05), and IVA-CPT score was increased significantly after treatment ( P<0.05) . The changes of scores on hyperactivity, auditory attention and visual attention were more in OROS-MPH group than those in atomoxetine group(P<0.05). There was loss of appetite in 10 children of OROS-MPH group and in 14 children of atomoxetine group. There was drowsiness in 1 child of OROS-MPH group and in 5 children of atomoxetine group, as well as difficulty to fall asleep in 6 children of OROS-MPH group and 1 child of atomoxetine group (P<0.05). One child developed a transient spasm after 4-month treatment. Conclusion Both of OROS-MPH and atomoxetine hydrochloride can improve learning ability and the symptom of attention deficit and hyperactivity, and they are similarly effective and safe in children with ADHD, but OROS-MPH can work faster.
ABSTRACT
Objective To observe clinical efficacy and safety on the treatment of moderate-severe cancer pain by Fluvoxamine combined with Oxycodone. Methods 120 cancer patients with moderate pain and 120 cases with severe pain were selected, randomly divided into experimental group and control group. The control group were given oxycodone alone , and experimental group given fluvoxamine combined with oxycodone , till the pain relieved, then the degree of pain relief, oxycodone dosage, life quality and side effects were evaluated. Results The degree of pain relief in experimental group were much better than control group (P < 0.05). Oxycodone consumption were lower in experimental group than control group , and the difference was no significant difference in controlling moderate pain (P = 0.065), while statistically significant in controlling severe pain (P = 0.035). The general status, daily activity, mood, and sleep affected by cancer pain were released after treatment, especially in experimental group (P < 0.05). The most common side effects were approximative, and the incidence of constipation, nausea/vomiting, lethargy were lower in experimental group than control group (P =0.026). Conclusion Fluvoxamine combined with Oxycodone can effectively control moderate-severe cancer pain, and reduce the oxycodone dosage and some side effects, and therefore, improve the quality of life.
ABSTRACT
The objective of the current study was to formulate mucoadhesive controlled release matrix tablets of flurbiprofen and to optimize its drug release profile and bioadhesion using response surface methodology. Tablets were prepared via a direct compression technique and evaluated for in vitro dissolution parameters and bioadhesive strength. A central composite design for two factors at five levels each was employed for the study. Carbopol 934 and sodium carboxymethylcellulose were taken as independent variables. Fourier transform infrared (FTIR) spectroscopy studies were performed to observe the stability of the drug during direct compression and to check for a drug-polymer interaction. Various kinetic models were applied to evaluate drug release from the polymers. Contour and response surface plots were also drawn to portray the relationship between the independent and response variables. Mucoadhesive tablets of flurbiprofen exhibited non-Fickian drug release kinetics extending towards zero-order, with some formulations (F3, F8, and F9) reaching super case II transport, as the value of the release rate exponent (n) varied between 0.584 and 1.104. Polynomial mathematical models, generated for various response variables, were found to be statistically significant (P<0.05). The study also helped to find the drug's optimum formulation with excellent bioadhesive strength. Suitable combinations of two polymers provided adequate release profile, while carbopol 934 produced more bioadhesion.
O objetivo do presente estudo foi formular comprimidos mucoadesivos de flurbiprofeno, de liberação controlada, e otimizar o perfil da liberação do fármaco e a bioadesão, utilizando a metodologia de superfície de resposta. Prepararam-se os comprimidos via técnica de compressão direta, que foram avaliados in vitro quanto aos parâmetros de dissolução e da força bioadesiva. Planejamento com componente central para dois fatores em cinco níveis cada foi empregado para esse estudo. Carbopol 934 e carboximetilcelulose sódica foram tomados como variáveis independentes. Efetuaram-se estudos de espectroscopia por transformada de Fourier (FTIR) para observar a estabilidade do fármaco durante a compressão direta e para avaliar a interação a fármaco-polímero. Aplicaram-se vários métodos cinéticos para avaliar a liberação do fármaco dos polímeros. Gráficos de superfície de contorno e de resposta foram efetuados para retratar a relação entre as variáveis dependentes e a resposta. Os comprimidos mucoadesivos de flurbiprofeno apresentaram cinética de liberação não-fickiana, estendendo para ordem zero, para algumas formulações (F3, F8 e F9), alcançando transporte super caso II, à medida que o valor do expoente (n) de taxa de liberação variou entre 0,584 e 1,104. Modelos matemáticos polinomiais, gerados por diversas variáveis de resposta, foram estatisticamente, significativos (P<0,05). O estudo também auxiliou a encontrar a formulação ótima do fármaco, com excelente força de bioadesão. Combinações adequadas dos dois polímeros resultaram em perfis de liberação adequado, sendo que o Carbopol 934 produziu mais adesão.
Subject(s)
Tablets/analysis , In Vitro Techniques/methods , Flurbiprofen/analysis , Drug Liberation , Methods , Chemistry, Pharmaceutical/classificationABSTRACT
Objective To evaluate the effect of irbesartan and nifedipine controlled-release tablets on morning blood pressure surge in patients with essential hypertension. Methods Ninety patients with essential hypertension were randomly divided into irbesartan group ( group A, n = 45) and nifedipine group (group B, n =45). Irbesartan tablets 150 mg/d and nifedipine controlled-release tablets 30 mg/d were respectively given in group A and group B for 4 weeks. The levels of diastolic blood pressure (DBP), systolic blood pressure (SBP), mean arterial pressure ( MAP ) and morning blood pressure surge ( MBPS ) before and after treatment were measured by ambulatory blood pressure monitoring. Results The DBP, SBP, MAP and MBPS levels of two groups after treatment for 4 weeks were all decreased (P < 0.01). All the indexes of group B decreased more significant compared to group A (P < 0.05 ). Conclusion To control blood pressure and prevent morning blood pressure surge, nifedipine controlled-release tablets are better than irbesartan.
ABSTRACT
Possible interaction between carbamazepine and different HPMC grades was done using DSC thermal analysis. The results indicated that the drug was compatible with these grades. Seven preparations of carbamazepine 200 mg controlled release tablets were prepared by wet granulation method and one preparation was prepared by direct compression method where different HPMC grades with different ratios were used. Concerning uniformity of weight, hardness and assay; all tablets conformed to pharmacopeal limits. Dissolution of the prepared tablets was done using basket method for 24 hours and paddle method for 4 hours. Tablets prepared by 30.0, 35.0 and 40.0% w/w HPMC K 100, 25.0% HPMC K 100 in combination with 5.0% HPMC K 4M and 15.0% w/w HPMC K 4M were conforming to USP limits, while tablets prepared by 15% K4M are not conforming to these limits. Tablets prepared by 12.5% HPMC K 15M by direct compression technique showed similar dissolution values to the innovator in five different media: distilled water, distilled water containing 1.0% SLS, buffer pH 1.2, acetate buffer pH 4.5 and phosphate buffer pH 6.8. The difference and similarity factors were found very acceptable. Scaling up of carbamazepine 200 mg controlled release tablets formulation from lab scale (500 tablets) to full production scale (500,000 tablets) was done. All the results of the scaling up were conforming to specifications and indicated that scaling up process has been done successfully and drug release kinetics indicated that the drug dissolution was zero order.
ABSTRACT
Objective To investigate the efficacy and safety of oxycodone hydrochloride controlled-release tablets combined with gabapentin in the treatment of painful diabetic neuropathy.Methods Eighty patients with painful diabetic neuropathy were divided into group A and group B with 40 cases each by random digits table.Patients of group A received simple oxycodone hydrochloride controlled-release tablets,while patients of group B received oxycodone combined with gabapentin.The intensity of pain, oxycodone dosage, quality of life and adverse effect in two groups was observed and compared.Results The pain was obviously relieved in two groups, and the effective analgesic rate at 21-28 d after treatment in group B was superior to group A[95.0% (38/40) vs.62.5% (25/40)], there was significant difference between two groups (P＜0.05).Numerical rating scale NRS score at 28 d after treatment in group B and group A was 1.2 ± 0.3 and 2.8 ± 0.5 respectively,and there was significant difference between two groups (P＜ 0.01 );the oxycodone dosage at 28 d after treatment in group B was lower than that in group A[(32.2 ± 4.3 )mg vs.(40.3±5.5 ) mg], and there was significant difference between two groups (P ＜ 0.05 ); the quality of life in group B was superior to group A, and there was significant difference between two groups (P ＜ 0.05 or ＜ 0.01 );the incidence of dizzy at 7, 14 d after treatment in group B was higher than that in group A[35.0% (14/40) vs.15.0% (6/40) and 30.0% (12/40) vs.10.0% (4/40)],and there was significant difference between two groups (P ＜ 0.05 ).Conclusion Oxycodon hydrochloride controlled-release tablets combined with gabapentin is effective and safe for the management of painful diabetic neuropathy.
ABSTRACT
Objective: To observe the analgesic effect and adverse effects of Controlled-Release Oxyco-done tablets(oxycontin) on moderate and severe chronic cancer pain, and the improvement of quality of life(QOL) in the cancer patients after the treatment. Methods: A total of 72 patients with moderate and se-vere chronic cancer pain were selected .The analgesic effects,adverse effects and quality of life (QOL) were observed and evaluated. Controlled-Release Oxycodone tablets were administered at an initial dose of 5 mg or 10 mg every 12 hours according to the degree of pain. The next analgesic dose should be adjust-ed if breakthrough pain occurs more than twice in 24 hours. If the initial dose is 5 mg, it may be increased to greater than or equal to 10 mg. If the initial dose is greater than or equal to 10 mg, the dosage may increased by 25%～50%. Short-acting morphine tablets are used to control the breakthrough pain. Results: The doses ranged between 10～100mg/d .Among the 72 patients with moderate and severe chronic cancer pain, 12 (16.7%)achieved complete remission ,52(72.2%)achieved partial remission,6(8.3%) achieved minor remis-sion.The overall rate of pain relief 88.9%. The mainly adverse reactions were including, nausea and vomiting, dizziness, drowsiness and dysuria. Followed the reduced of the pain intensity ,the QOL of most cancer pa-tients was improved. The KPS of 12 patients had been obviously improved, 20 patients had mildly improved, and 40 patients were stabilized. Conclusion: Oxycodone hydrochloride controlled-release tablets are effective and safe for the management of chronic cancer patients with moderate and severe pain, with less adverse reactions, and the QOL of cancer patients were significantly improved.
ABSTRACT
0.05),but the rectal administration showed a quicker response in pain-relieving than the oral administration of Morphine Sulfate Controlled-release tablets(P
ABSTRACT
OBJECTIVE: To optimize the formula and preparation technology of gliclazide controlled-release tablets. METHODS: Gliclazide controlled-release tablets were prepared in different formulations and the release rates of the prepared tablets were determined to obtain the optimum formula and preparation technology. RESULTS: The optimized formula of gliclazide controlled-release tablets were determined as follow: with HPMC(K4M)=17g and HPMC(E50)=35g as matrix materials; Calcium hydrogen phosphate=91g as the bulking agent and magnesium stearate as lubricant. Gliclazide controlled-release tablets showed a similar release rate as the reference samples. CONCLUSION: The releasing rate of gliclazide controlled-release tablets prepared in the optimized formula is in line with the standards stated in China Pharmacopeia.
ABSTRACT
OBJECTIVE: To study the pharmacokinetics and bioavailability of pulse controlled-release tablets of ketoprofen(KRT) in dogs.METHODS: A total of 6 dogs were randomly assigned to receive KRT(trial group,n=3) or KP enteric-coated capsules(control group,n=3) 150 mg,then a crossover trial was conducted 1 week later.Plasma samples were taken at different time points and the plasma concentration of ketoprofen in dogs was determined by HPLC.The pharmacokinetic parameters of the two KP preparations were computed and the correlation between absorption percentage in vivo and release rate in vitro was compared.RESULTS: The pharmacokinetic parameters of KRT versus those of its control preparation were as follows: tmax:(5.00?0.41) vs.(3.75?0.00) h;Cmax:(15.40?1.94) vs.(20.73?1.72) ?g?mL-1;AUC0～t(101.33?17.49) vs.(93.21?25.03) ?g?h?mL-1.The relative bioavailability of the trial preparation was 108.71%.The test preparation showed a good correlation(r=0.987) between absorption percentage in vivo and release rate in vitro.CONCLUSIONS: The KRT and KP enteric-coated capsules were bioequivalent.
ABSTRACT
Objective To prepare osmotic pump-controlled release tablets of total flavones in Lysimachia clethroides.Methods Two components of the extract from L.clethroides,rutin and naringenin-7-O-glucoside were used to evaluate the release behavior of osmotic pump controlled release tablets.Single factor investigation was carried out on the membrane compositions and orifice variables,and uniform design was used to optimize the formulation of coating mambrane.Results The membrane weight,PEG400 content,and dibutyl phthalote(DBP) content were the main factors influencing the drug release,and based on 45% and 8.5% of cellulose acetate,respectively,to prepare osmotic pump-controlled release tablets could achieve the desired zero-order release profile.Conclusion The formulation and technology are simple and easy to be carried out.Osmotic pump-controlled release tablets have a stable drug release bahavior and a good reproducibility.
ABSTRACT
AIM: To prepare controlled release tablets of colchicine and establish the relationship among formula factors of membrane and drug release rate. METHODS: Uniform design was used to achieve the quantitative relationship among the release rate of colchicine,acetyl cellulose and PEG 6000.Optimized prescriptions were calculated from the regression equation. RESULTS: A significant correlation and a fine precision were obtained.(Osmotically) controlled release tablets of colchicine were prepared based on the calculations,and the drug release pattern was in accordance with zero-order kinetics(r=0.990 2). CONCLUSION: Uniform design is a convenient and efficient approach to the formulation optimization of elementary osmotic-pump tablets.
ABSTRACT
AIM: To investigate the influence of three dimentional printing processes(3DP) on the release of controlled-release helicid tablet. METHODS: Parameters of 3DP,such as skeleton polymer,binder,thickness of powder layering,number of spray painting,subregion ser up and diameter of aperture,were selected in the preparation of donut-shape multilayer controlled-release helicid tablet.Dissolution tests in vitro were carried out to analyse the effect of technological parameters on the release of helicid. RESULTS: Under the condition of fixed subregion and diameter of aperture,the selections of binders and thickness of spray painting were key factors concerning the release period of helicid. CONCLUSION: 3DP processes shows high flexibility and efficacy in the preparation of controlled-release tablets.