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Objective To observe the clinical efficacy of Huajian-Badu membrane in the treatment of moderate and severe cancer pain. Methods The 80 malignant tumor patients with moderate to severe cancer pain from January 2016 to June 2017 in Tianjin University of Traditional Chinese Medicine First Teaching Hospital were recruited and randomly divided into the observation group and the control group, each of 40 cases. The control group were treated with Oxycodone Hydrochloride Prolonged-release Tablets, while the treatment group were treated with Huajian-Badu membrane on the basis of the treatment in control group. The pain relief, pain frequency, morphine consumption and quality of life (Karnofsky score), adverse reaction were evaluated between two groups before and after treatment. Results Compared with the control group, the total efficiency in the observation group was significantly higher (95.0％ vs. 80.0％, χ2=4.114, P=0.043). The frequency of breakthrough pain of two groups increased on the seventh and fourteenth treatment days(0.3 ± 0.6 times vs. 0.8 ± 0.7 times, t=-3.430 and 0.4 ± 0.6 times vs. 0.9 ± 0.8 times, t=-3.162), but the number of outbreaks of pain in the observation group significantly less than the control group (P<0.05 or P<0.01). The morphine injection dosage increased on the seventh and fourteenth treatment days (3.01 ± 4.28 g vs. 5.62 ± 6.37 g, t=-2.151 and 3.21 ± 4.32 g vs. 7.84 ± 7.76 g, t=-3.297), but the amount of the observtation group was significantly lower than that of control group (P<0.05 or P<0.01). The KPS score in the observation group increased significantly, and significantly higher than the control group on the seventh and fourteenth treatment days (73.0 ± 15.0 vs. 66.0 ± 12.0, t=2.305 and 77.0 ± 13.0 vs. 70.0 ± 15.0, t=2.230, P<0.05). The adverse reaction rate of the control group was 25％, while the the observation group was 20％. The difference between two groups was significant (χ2=0.287, P=0.592). Conclusions The Huajian-Badu membrane combined Oxycodone Hydrochloride Prolonged-release Tablets can improve the total effective rate of pain relief, reduce the number of outbreaks, reduce morphine consumption, improve patient KPS score of the patients with cancer pain.
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Objective@#To observe the efficacy and adverse effect of oxycodone hydrochloride prolonged-release tablets rectal administration in the treatment of cancer pain.@*Methods@#From July 2016 to July 2017, eighty patients with cancer pain in the Second People's Hospital of Jiandewere selected in the research.The patients were randomly divided into control group and observation group according to the digital table, with 40 cases in each group.The two groups were treated with oxycodone hydrochloride prolonged-release tablets, the control group was treated by oral administration, while the observation group was treated by rectal administration.At different time points after administration, the degree of pain(NRS) score, pain remission rate, quality of life before and after treatment, the incidence of adverse reactions were compared between the two groups.@*Results@#After the administration of 1 h, 3 h, the NRS scores of the observation group were (4.49±1.25)points, (3.80±1.13)points, which were lower than those of the control group[(5.56±1.42)points, (5.04±1.10)points], the differences were statistically significant(t=3.58, 4.97, all P<0.05). After administration of 1 d, 1 week and 2 weeks, the NRS scores between the two groups showed no statistically significant difference(P>0.05). The pain relief rate of the observation group was 92.50%, which was significantly higher than 75.00% of the control group, the difference was statistically significant(χ2=4.50, P<0.05). The indicators of quality of life in the observation group were significantly better than those in the control group, the differences were statistically significant(t=2.09, 2.20, 3.16, 3.28, all P<0.05). The incidence rate of adverse reaction of the observation group was 12.50%, which of the control group was 10.00%, there was no statistically significant difference between the two groups(P>0.05).@*Conclusion@#The analgesia effect of oxycodone hydrochloride prolonged-release tablets by rectal administration is similar with oral administration for cancer pain patients, and has less adverse reaction, high safety, and it is worthy of popularization and application.
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Abstract An innovative technology (Physiomimic Technology) has been applied to amino acids (AAs) formulated for patients with phenylketonuria, with the objective of masking AA taste and odor and prolonging AA release in the gut, allowing a physiological absorption. This technology entails that the AAs are processed with functional additives that are able to modify their release and their organoleptic features. Two prototypes, obtained using sodium alginate + ethylcellulose (engP-1) or sodium alginate + ethylcellulose + glyceryl dibehenate (engP-2), have been tested for AA prolonged release versus the same AAs (n-engP) without the application of the Physiomimic Technology. In vitro tests indicated that the technology is able to prolong the release of the engineered AAs versus the free compounds. A crossover in vivo kinetic study in pigs showed reduced peak concentrations (Cmax) and, as expected, similar areas under the concentration/time curve (up to 5 hours) for the engineered products versus the free AAs. Significantly lower Cmax values (P < .01) were attained for essential AAs, large neutral AAs, and branched-chain AAs, indicating that the technology is able to reduce the typical absorption peak of free AAs. Taste and odor masking has been obtained as a consequence of the AA coating. The Physiomimic Technology, applied to free AAs, provided AA mixes with improved organoleptic features and with modified AA kinetics sustaining a more physiological AA absorption.
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Objective:Tacrolimus prolonged-release(PR) formulation is a new once-daily formulation of the calcineurin inhibitor tacrolimus,which is currently used in adult liver or kidney transplant patients,and is also gradually widely used in children with nephrotic syndrome.The present study was undertaken to preliminarily investigate the pharmacokinetic characteristics of tacrolimus PR in pediatric nephrotic syndrome recipients.Methods:This single-center open-label prospective study was performed in pediatric nephrotic syndrome recipients.Pharmacokinetic samples were collected from eight pediatric subjects with nephrotic syndrome from Department of Pediatric Nephrology in Peking University First Hospital between June and August 2011.They followed administration of single oral doses of tacrolimus PR formulation at 0.02 mg/kg (n =2),0.05 mg/kg (n =2) and 0.10 mg/kg (n =4).Blood samples were taken before the dose and 1,2,4,6,8,10,12 and 24 h after drug intake.No other medicines or interacting food or drinks were taken during the study period.Blood concentrations were measured using an enzyme multiplied immunoassay technique.Pharmacokinetic analysis was performed using WinNolin Phoenix software Version 6.0 (Pharsight,Cary,NC,USA).Results:The pharmacokinetic data were best described by a non-compartment model.Pharmacokinetic parameters of tacrolimus PR formulation in the 3 ascending doses groups (0.02 mg/kg,0.05 mg/kg and 0.10 mg/kg) were as follows:the maxi mum drug concentrations (Cm=/D) were (1.7 ± 1.0) μg/L,(3.1 ± 1.9) μg/L,(8.0 ± 3.5) μg/L,respectively;Areas under the drug concentration-time curve (AUCo-∞/D) were (47.2 ± 47.1) h · μg/ L,(84.0 ± 13.1) h · μg/L,(175.6 ± 107.1) h · μg/L,respectively;Oral clearance rates were (0.8±0.9) L/(h·kg),(0.4±0.1) L/(h · kg),(1.9 ±1.3) L/(h · kg),respectively;Body weight normalized distribution volumes were (7.0 ± 3.4) L/kg,(12.4 ± 8.4) L/kg and (73.6 ± 68.6) L/kg,respectively.Both mean Cmax normalized level for the administered dose (Cmax/D) and mean AUC0-∞ normalized level for the administered dose (AUC0-∞/D) were higher in the 0.05 mg/kg dosage group than in the 0.02 and 0.10 mg/kg dosage group.There were two peaks in the drug concentrations in every dose group;a primary peak appeared at the end of about 2 h followed by a small secondary peak at h 12,which was more noticeable in the 0.10 mg/kg dose group than in the two lower dosages.Conclusion:The pharmacokinetic characteristics of tacrolimus PR formulation were initially explored in pediatric patients with nephritic syndrome.The data presented form a basis for subsequent larger scale studies on pharmacokinetics of tacrolimus PR formulation in nephritic syndrome children.
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Objective To discuss the pharmaceutical care protocol and methods for clinical pharmacists taking part in cancer pain management. Methods A patient developed delirium and drowsiness after using oxycodone hydrochloride prolonged-release tablet ( OXYCONTIN) and morphine hydrochloride tablet for pain titration treatment. The clinical pharmacist analyzed the reasons of delirium and drowsiness,and suggested a dose reduction of OXYCONTIN or converting OXYCONTIN to another opioid analgesic. Results The suggestion of the clinical pharmacist was partly accepted. After adjusting the treatment, the delirium and drowsiness disappeared gradually, and the pain was well controlled. Conclusion In clinical practice, especially when faced with a rare adverse drug reaction, clinical pharmacists are helpful for ensuring the safety and effectiveness in pain management, as well as improving the level of the treatment, by the implementation of individualized drug therapy.
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Objective To explore the influence of Methylphenidate Hydrochloride prolonged-release tablets on the cognitive processing of children with attention deficit hyperactivity disorder (ADHD).Methods Thirty ADHD children and 30 healthy controls were enrolled in this study,and the ADHD subjects were treated with Methylphenidate Hydrochloride prolonged-release tablets for (28 ± 3) days.Pre-test and post-test by the Das-Naglieri:Cognitive Assessment System(DN:CAS) were done to evaluate the cognitive function of all individuals.The differences of cognitive processing in pre-treatment and post-treatment of ADHD group with healthy control group were compared.The difference between before and after treatment of ADHD was also compared.Results Compared with healthy control group,there were lower of planning score [(21.86 ± 4.61) scores vs.(29.33 ± 5.06) scores],attention score [(25.00 ± 4.57) scores vs.(29.83 ± 3.79) scores],and the total scores [(111.93 ± 13.95) scores vs.(127.26 ±15.53) scores] in ADHD group,and there were significant differences (t =-5.976,-4.455,-4.023,all P ＜0.05).The matching number,planned codes,planned connections,expressive attention,number detection and receptive attention scores were also lower in ADHD group,and there were significant differences (t =-4.787,-3.703,-4.991,-2.216,-2.488,-3.219,all P ＜ 0.05).Compared with healthy control group,there were lower of planning score with significant difference [(25.53 ± 4.98) scores vs.(29.33 ± 5.06) scores,t =-2.931,P ＜ 0.05] in ADHD group after treatment,matching number and planned codes were lower with significant difference (t =-2.654,-2.044,all P ＜ 0.05) in ADHD group after treatment.In ADHD group,the scores of planning [(25.53 ± 4.98)scores vs.(21.86 ± 4.61) scores],simultaneous processing [(36.10 ± 7.10) scores vs.(34.13 ± 6.04) scores],attention [(27.90 ± 5.69) scores vs.(25.00 ± 4.57) scores] and the total score [(121.50 ± 16.55) scores vs.(111.93 ± 13.95) scores] were significantly higher after treatment than that before treatment and there were significant differences (t =-5.679,-2.949,-3.869,-5.963,all P ＜ 0.05);matching number,planned codes,planned connections,nonverbal matrices,number detection,receptive attention and word series were significantly higher after treatment than that before treatment,and there were significant differences (t =-2.528,-3.209,-3.890,-2.276,-4.489,-2.208,-2.373,all P ＜ 0.05).Conclusion The Methylphenidate Hydrochloride prolonged-release tablets can improve the function of cognitive processing in children with ADHD,especially in attention.
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Objective To explore the influence of Methylphenidate Hydrochloride prolonged-release tablets on the cognitive processing of children with attention deficit hyperactivity disorder (ADHD).Methods Thirty ADHD children and 30 healthy controls were enrolled in this study,and the ADHD subjects were treated with Methylphenidate Hydrochloride prolonged-release tablets for (28 ± 3) days.Pre-test and post-test by the Das-Naglieri:Cognitive Assessment System(DN:CAS) were done to evaluate the cognitive function of all individuals.The differences of cognitive processing in pre-treatment and post-treatment of ADHD group with healthy control group were compared.The difference between before and after treatment of ADHD was also compared.Results Compared with healthy control group,there were lower of planning score [(21.86 ± 4.61) scores vs.(29.33 ± 5.06) scores],attention score [(25.00 ± 4.57) scores vs.(29.83 ± 3.79) scores],and the total scores [(111.93 ± 13.95) scores vs.(127.26 ±15.53) scores] in ADHD group,and there were significant differences (t =-5.976,-4.455,-4.023,all P ＜0.05).The matching number,planned codes,planned connections,expressive attention,number detection and receptive attention scores were also lower in ADHD group,and there were significant differences (t =-4.787,-3.703,-4.991,-2.216,-2.488,-3.219,all P ＜ 0.05).Compared with healthy control group,there were lower of planning score with significant difference [(25.53 ± 4.98) scores vs.(29.33 ± 5.06) scores,t =-2.931,P ＜ 0.05] in ADHD group after treatment,matching number and planned codes were lower with significant difference (t =-2.654,-2.044,all P ＜ 0.05) in ADHD group after treatment.In ADHD group,the scores of planning [(25.53 ± 4.98)scores vs.(21.86 ± 4.61) scores],simultaneous processing [(36.10 ± 7.10) scores vs.(34.13 ± 6.04) scores],attention [(27.90 ± 5.69) scores vs.(25.00 ± 4.57) scores] and the total score [(121.50 ± 16.55) scores vs.(111.93 ± 13.95) scores] were significantly higher after treatment than that before treatment and there were significant differences (t =-5.679,-2.949,-3.869,-5.963,all P ＜ 0.05);matching number,planned codes,planned connections,nonverbal matrices,number detection,receptive attention and word series were significantly higher after treatment than that before treatment,and there were significant differences (t =-2.528,-3.209,-3.890,-2.276,-4.489,-2.208,-2.373,all P ＜ 0.05).Conclusion The Methylphenidate Hydrochloride prolonged-release tablets can improve the function of cognitive processing in children with ADHD,especially in attention.
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ABSTRACT Drug delivery to treat ocular disorders locally is a challenging endeavor. Traditional ocular dosage form - eye drops - exhibits poor availability, consequently inefficient therapeutic response. The objective of the study was to formulate and characterize a ketorolac tromethamine ocular system with a prolonged release pattern based on liposomes as a vesicular carrier and to design once daily liquid preparation realizing the thermal in situ gelation principle. Liposomes were prepared by film hydration method. The influence of cholesterol concentration, pH and volume of hydration medium, and type and concentration of charging imparting agents were studied. Liposomes were characterized via, morphological examination, vesicular size, and encapsulation efficiency, and in vitro release performance, moreover its stability was assessed. The results obtained highlighted that liposomes showed a closed vesicular multi-lamellar structure. Ketorolac was successfully encapsulated within the liposomal structure in a cholesterol and charge inducing agent concentration-dependent behaviour. The dispersion of liposomes within thermosensitive Poloxamer in situ gel was able to retard the release of the drug by diffusion providing a controlled prolonged delivery. The liposomal formulations were physically stable for six months. Ketorolac tromethamine in situ liposomal gel representing an efficient alternative in terms of ocular retention and patient compliance when compared with conventional eye drops.
Subject(s)
Ketorolac Tromethamine/pharmacokinetics , Reactivity-Stability , Drug Compounding/classification , Liposomes/antagonists & inhibitors , Tromethamine/antagonists & inhibitors , Eye Abnormalities/complications , Skin Diseases, Vesiculobullous , Administration, OphthalmicABSTRACT
Objective: To investigate the efficacy and safety of oxycodone hydrochloride prolonged-release tablets and tramadol hydrochloride sustained-release tablets in the treatment of moderate cancer pain. Methods:Totally 290 cases of the patients with mod-erate pain were divided into the observation group with 148 cases and the control group with 142 cases. The observation group received oxycodone hydrochloride prolonged-release tablets, while the control group was given tramadol hydrochloride sustained-release tablets. The treatment course was 2 weeks, and the total efficiency and the incidence of adverse drug reactions( ADR) in the two groups were calculated and compared. Results:The total efficiency in the observation group and the control group was 92. 6% and 81. 7%, respec-tively, and the difference was statistically significant (P0.05). Conclusion: The effect of oxycodone hydrochloride prolonged-release tablets in the treatment of moderate cancer pain is better than that of tramadol hydrochloride sustained-release tablets.
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Neste trabalho, avaliou-se a utilização da quitosana como matriz hidrofílica no desenvolvimento de comprimidos de liberação prolongada de captopril. Os comprimidos foram obtidos por compressão direta utilizando-a em diferentes proporções (10, 15, 20 e 25%). As formulações contendo quitosana foram comparadas com uma formulação de liberação imediata contendo croscarmelose. Os resultados obtidos nos ensaios de peso médio, friabilidade, dureza, uniformidade de conteúdo e doseamento indicaram que todos os comprimidos apresentavam características de qualidade condizentes com os limites especificados na Farmacopeia Brasileira. Os ensaios de dissolução evidenciaram um aumento do tempo de liberação do captopril com o aumento da proporção de quitosana na matriz, indicando que essas formulações apresentaram perfis de liberação prolongada do fármaco, especialmente a formulação contendo 25% de quitosana. Os valores dos coeficientes de correlação indicaram que os modelos cinéticos que melhor se ajustam ao perfil de dissolução das formulações avaliadas foram o modelo proposto por Higuchi (pH 1,2) e o de primeira ordem (pH 6,8).
In this study, chitosan was used as a hydrophilic matrix in the development of prolonged-release tablets of captopril. The tablets were obtained by direct compression, with the chitosan in various proportions (10, 15, 20 and 25%). The formulations were compared with an immediate-release formulation containing croscarmellose. In assessments of weight variation, friability, hardness, content uniformity and drug assay, all the tablets complied with the standards of quality set by the Brazilian Pharmacopoeia. Dissolution tests showed that the release time of captopril increased with the content of chitosan in the matrix, indicating that these formulations showed prolonged-release profiles of the drug, especially the one containing 25% chitosan. The kinetic models that fitted the dissolution profiles of the formulations best (with the highest correlation coefficients) were the Higuchi (at pH 1.2) and first-order (at pH 6.8) models.