Establishment of the quality research method for diclofenac potassium cataplasms and the preparation evaluation / 国际药学研究杂志

Objective: To prepare the new diclofenac potassium cataplasms, establish a quality research method and evaluate the preparation quality by the established method. Methods: A high performance liquid chromatography(HPLC)was performed on an ODS column(the column temperature 35℃)using the methanol-4% glacial acetic acid solution(80: 20, V/V)as mobile phase, and the detection wavelength was set at 276 nm. Diclofenac potassium was extracted with methanol, and the adhesion, content and uniformity of potassium diclofenac were measured. The release of diclofenac potassium from the cataplasms was determined in accordance with the fourth method of the XD release methods in the Appendix of the Chinese Pharmacopoeia. Results: The average maximum number of steel ball stuck in the cataplasms in the initial adhesion test was No. 6. Under the HPLC conditions, potassium diclofenac showed good linearity within the concentration range of 400-800 μg/ml, with the average sample recovery rate 1.33 % and RSD< 1.93%(n=6). The methodological studies for the drug release test for the diclofenac potassium cataplasms showed that the diclofenac potassium showed a good linearity within the range of 1-50 μg/ml in the drug release test, and the precision and recovery well satisfied the requirements of Pharmacopoeia. The content uniformity of the cataplasms was in accordance with the Pharmacopoeia. The release amounts of the cataplasms in 2, 5 and 8 hours were 20%-45%, 40%-80% and more than 70% of the labeled amount, respectively, and the release curve followed the first-order release equation. Conclusion: The established HPLC method is sensitive, accurate, easily operable and reproducible, which could be used for the quality control of diclofenac potassium cataplasms. The prepared diclofenac potassium cataplasms were of uniform content and showed characteristics of the sustained release, which is expected to be developed to a new preparation of diclofenac potassium.

Uso indiscriminado de diclofenaco de potássio pela população idosa na cidade de Anápolis, no estado de Goiás, Brasil em 2014 / Indiscriminate use of diclofenac potassium for elderly population in Anápolis city, state of Goiás, Brazil in 2014

O presente estudo teve como finalidade evidenciar o uso indiscriminado de diclofenaco de potássio e o desconhecimento dos efeitos colaterais deste medicamento contidos na bula pelos idosos do Município de Anápolis, Goiás em 2014. Trata-se de uma pesquisa analítica em loco que teve como amostra 2500 indivíduos idosos de 58-77 anos. Os dados foram compilados através de questionários e revelaram que a droga foi extensivamente utilizada pelos entrevistados sem receituário médico. Dentre os motivos que os levaram a adquirir o diclofenaco de potássio, ressaltam-se: o preço acessível e à eficácia da droga sobre sintomas como dores no corpo, principalmente nas pernas e costas. Foi detectado um estimulo a automedicação resultante do sistema de vendas praticado nas drogarias, nas quais atendentes sem conhecimento farmacológico pertinente realizam indicações de fármacos sem conhecimento técnico. Os resultados da pesquisa reforçam a necessidade de maiores orientações sobre o uso racional desse medicamento, uma vez que o consumo inadequado pode ocasionar distúrbios gástricos, renais e circulatórios.

This work intended to evaluate the drug abuse and the knowledge of side effects presented in the guidelines of potassium diclophenac used by elderly people from Anapolis-Brazil. In this study, 2500 people, ranging between 58 and 77 years old, were interviewed in 2014. The data collected by a questionnaire revealed the excessive use of this drug without medical prescription. The main reasons raised by the respondents, when asked about why they use this drug, were the affordable price and the efficiency of potassium diclophenac in the common symptoms at this age, especially back and joint pain. The market, with unprepared sellers, stimulates self-medication and input a risk at the health of Brazilian population. The results presented the need of further guidance on the rational use of this drug, since inadequate intake may cause stomach, kidney and circulatory disorders.

Utilizando Espectroscopia de EnergiaDispersiva (EDS) para Comparação deMedicamentos Genéricos e Similarcom o seu Referência / The Use of Energy Dispersive Spectroscopy (EDS) For Comparison of Generic and Similar Drugs with Their Reference Drugs

Os medicamentos genéricos devem apresentar mesmoprincípio ativo que o seu referência, na mesma concentração, dose eforma farmacêutica. Normalmente o seu valor é inferior, assim,muitas pessoas questionam: sua composição, eficiência e tempo deresposta. O Microscópio Eletrônico de Varredura (MEV) produz imagensde alta ampliação e resolução através da interação de elétrons comos átomos da amostra. Nele também é possível realizar uma análisemultielementar através de um sistema de Espectroscopia por EnergiaDispersiva (EDS). Objetivo: Visto a característica do MEV/EDS e oquestionamento levantado pelo uso de genéricos, realizou-se umaanálise qualitativa do medicamento referência, genéricos e similar doDiclofenaco de Potássio 50 mg a fim de verificar suas composiçõese compará-las. Material e Métodos: Utilizou-se medicamentos genéricosde 3 indústrias farmacêuticas distintas, o similar e o seu referência.As amostras foram irradiadas durante 300s no MEV/EDS TM-3000Hitachi, com 3 medidas em pontos distintos de cada comprimido. Asmedidas também foram feitas com os medicamentos sem osrevestimentos. Resultados: A técnica conseguiu verificar tanto oselementos presentes nos excipientes quanto no princípio ativo domedicamento. Foi visto que alguns se distinguiam quando irradiadocom o revestimento, mas ao retirar o mesmo, todos os genéricosapresentaram-se bem semelhantes qualitativamente quandocomparados ao medicamento de referência. Conclusões: A técnicamostrou-se eficiente e adequada para as amostras, pois através dosespectros dos fármacos genéricos e similar foi possível identificarnão somente o princípio ativo, mas também seus excipientes ecompará-los ao fármaco referência...

Generic drugs should have the same active ingredientthan their reference drugs, at the same concentration, dose anddosage form. As the costs of generics are lower, many people haveraised questions about their composition, efficiency and responsetime. A Scanning Electron Microscope (SEM) produces highmagnification and resolution images through the interaction of electronswith the sample atoms. This equipment may also be used to performa multielement analysis using an Energy Dispersive Spectroscopy(EDS) system. Objective: Given the SEM/EDS features and thequestions raised on the use of generics, we carried out a qualitativeanalysis of the reference, generic and similar drugs of PotassiumDiclofenac (50 mg), in order to verify their compositions and comparethem. Materials and Methods: Three different brands of each drug(reference, generic and similar) were tested. The samples were irradiatedfor 300 seconds using a SEM/EDS Hitachi TM-3000 microscope, withthree measurements at different points in each tablet. Themeasurements were also made with the drug without the coating.Results: The technique was able to detect the constituents present inboth the excipients and the active ingredient of the drug. Somedifferences were found when the samples were irradiated with theircoating. On the other hand, all generic drugs were found to bequalitatively similar to their reference drugs when the coating wasremoved. Conclusions: The technique was proven efficient and suitablefor the samples, because through the spectra of the generic andsimilar drugs it was possible to identify not only the active principlebut also the excipients, and compare them to the reference drug...

Avaliação dos óleos essenciais de plantas nativas da Mata Atlântica como promotores de permeação cutânea / Evaluation of essential oils of plants native to the Atlantic Forest as skin permeation enhancers

Os óleos essenciais da Pimenta pseudocaryophyllus (Gomes) Landrum de planta de populações naturais de três ecossistemas, localizados na Ilha de Cananéia, região de restinga, no Morro da Cataia, cidade de Cajati, região de encosta, ambas em área de Mata Atlântica, e na Reserva Natural Morro Grande, cidade de Caldas, região de campos montanos, foram avaliados como promotores de permeação cutânea do diclofenaco de potássio. Os óleos essenciais foram extraídos de partes aéreas das plantas e o rendimento do processo foi entre 0,90% (p/p) e 2,7% (p/p). A análise da composição química mostrou diferenças, indicando tratar-se de três quimiotipos diferentes. A interação dos óleos essenciais e dos componentes majoritários com membrana biológica natural foi avaliada por FT-Raman e ATR- FTIR, indicando a interação com as porções lipídicas do tecido. Foram desenvolvidas seis membranas biológicas artificiais, compostas por ceramidas, ácidos graxos e colesterol em proporções equimolares, que foram caracterizadas por espectroscopia Raman confocal e foram consideradas semelhantes. As membranas foram utilizadas no desenvolvimento do sistema PAMPA (Parallel Artificial Membrane Permeability Assay) para avaliar a segurança e eficácia dos óleos essenciais e componentes majoritário como promotores de permeação do diclofenaco de potássio. Os resultados dos ensaios com o sistema PAMPA foram estatisticamente avaliados. A segurança foi avaliada com o critério de permeação mínima dos óleos através das membranas do sistema PAMPA, verificada pela absorbância mínima do eugenol na solução aceptora. Os óleos essenciais e componentes majoritários foram utilizados no pré-tratamento das membranas, nas concentrações de 0,125%, 0,25%, 0,50% e 2,00% (v/v) em etano!. Ensaios de permeação do diclofenaco de potássio no sistema PAMPA indicaram efeito de promoção da permeação para todos os compostos avaliados. O método de doseamento do fármaco por UV foi validado e utilizado para os ensaios de permeação de formulações de gel em base aquosa contendo o diclofenaco de potássio (1,0% p/p). As amostras de gel foram preparadas com o óleo procedente de Morro Grande, selecionado na etapa de avaliação de segurança, a 0,125% (p/v). Adicionalmente, foram preparadas formulações com citronelol e etanol, na mesma concentração. O óleo essencial da Reserva Natural Morro Grande teve efeito de promoção da permeação superior ao do citronelol e etanol, que foram equivalentes

The essential oils of the species Pimenta pseudocaryophyllus (Gomes) Landrum collected from natural populations of three existing ecosystems in the Cananéia Island, located at sea level, Cajati city, located in hillside region, both in the Atlantic Forest areas, as well as species collected in the Morro Grande Natural Reserve, region of montane fields, were evaluated as skin permeation enhancers of potassium diclofenac. Essential oils were extracted from the aerial parts of the plants and the process yield was between of 0.90% (w/w) and 2.7% (w/w). The chemical composition analysis showed differences between the plants of three origins, indicating that they are different chemotypes. The interaction of the essential oils and their major components with natural biological membrane was evaluated by FT- Raman and ATR-FTIR, indicating interaction with the Iipid portions of the natural membrane. Six artificial biological membranes have been developed, consisting of ceramides, cholesterol and fatty acids in equimolar proportions, which were characterized by confocal Raman spectroscopy and found to be similar. The membranes were used in developing the PAMPA (Parallel Artificial Membrane Permeability Assay) system to evaluate the safety of the potential permeation enhancers. The test results with PAMPA system were statistically evaluated. Safety was evaluated with the criterion of minimum permeation of the essential oil through the membranes, checked by the minimum absorbance of eugenol in the acceptor solution. The essential oils and the major components were used in the pretreatment of the membranes, at concentrations of 0.125%, 0.25%, 0.50% and 2.00% (v/v) in ethanol. Results indicated permeation enhancement effect for ali compounds evaluated. The analytical method for the quantification of potassium diclofenac was validated and used for the evaluation of the permeation of aqueous based gel formulations containing potassium diclofenac (1.0% w/w). The gel samples were prepared with the oil from Morro Grande Natural Reserve, selected in the safety evaluation step, at 0.125% (w/v). In addition, formulations were prepared with citronellol and ethanol at the same concentration. The essential Gil of Morro Grande Natural Reserve was more efficient as permeation enhancer than citronellol and ethanol under the test conditions

Development and validation of a dissolution method using HPLC for diclofenac potassium in oral suspension

The present study describes the development and validation of an in vitro dissolution method for evaluation to release diclofenac potassium in oral suspension. The dissolution test was developed and validated according to international guidelines. Parameters like linearity, specificity, precision and accuracy were evaluated, as well as the influence of rotation speed and surfactant concentration on the medium. After selecting the best conditions, the method was validated using apparatus 2 (paddle), 50-rpm rotation speed, 900 mL of water with 0.3% sodium lauryl sulfate (SLS) as dissolution medium at 37.0 ± 0.5°C. Samples were analyzed using the HPLC-UV (PDA) method. The results obtained were satisfactory for the parameters evaluated. The method developed may be useful in routine quality control for pharmaceutical industries that produce oral suspensions containing diclofenac potassium.

O presente estudo descreve o desenvolvimento e validação de um método de dissolução in vitro para avaliação da liberação de diclofenaco potássico suspensão oral. O teste de dissolução foi desenvolvido e validado de acordo com as diretrizes internacionais. Parâmetros como linearidade, especificidade, precisão e exatidão foram avaliados, bem como a influência da velocidade de rotação e a concentração de tensoativono meio. Depois de selecionar as melhores condições, o método foi validado usando o aparato 2 (pás), velocidade de rotação de 50 rpm, 900 mL de água com 0,3% de lauril sulfato de sódio (LSS) como meio de dissolução a 37,0 ± 0,5 ºC. As amostras foram analisadas pelo método de CLAE-UV (PDA). Os resultados obtidos foram satisfatórios para os parâmetros avaliados. O método desenvolvido pode ser útil na rotina de controle de qualidade para as indústrias farmacêuticas que produzem suspensões orais contendo diclofenaco potássico.

Formulation, in vitro and in vivo Characterisation of Diclofenac Potassium Sustained Release Tablets Based on Solidified Reverse Micellar Solution (SRMS).

Aims: To formulate sustained release diclofenac potassium tablets based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties of the tablets. Study Design: Formulation, in vitro and in vivo evaluation of sustained release diclofenac potassium. Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka and Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Nigeria. Methodology: SRMS, consisting of mixtures of phospholipid and triglyceride were prepared in the ratios of 1:1, 2:1 and 1:2 (Phospholipon® 90H: Softisan® 154) respectively. SRMS-based tablets containing 100 mg of diclofenac potassium each were prepared using validated plastic mould. The physicochemical properties of the tablet formulations were studied and compared with the market brands of the drug for sustained release properties. In vitro release was carried out in simulated intestinal fluid (SIF, pH 7.5) using the USP paddle method. Anti-inflammatory, analgesic/anti-nociceptive and ulcerogenic properties of the formulated tablets were studied using adult Wistar rats. Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix (LM) used (p < 0.05). The hardness of the tablets ranged from 4.55 ± 0.50 to 5.10 ± 0.39 kgf for tablets formulated with LM 1:2 and 1:1 (M3 and M1) respectively. Friability results indicated that all the SRMs tablets exhibited friability values less than 1 %. The erosion time ranged from 35.8 ± 1.10 to 120.3 ± 0.32 min. The release profile of the tablets showed maximum release between 8 – 11 h for all the batches. Diclofenac potassium tablets based on SRMS had good anti-inflammatory and analgesic properties and also inhibited the ulcerogenicity of the NSAID by up to 85 %. Conclusion: Diclofenac potassium tablets based on SRMS could be used for once daily administration.

A simple method for the quantification of diclofenac potassium in oral suspension by high-performance liquid chromatography with UV-detection

A rapid, simple and low cost method was developed to determine diclofenac potassium (DP) in oral suspension, using a reverse-phase column (C8, 150 mm x 4.6 mm, 5 µm), mobile phase containing methanol/buffer phosphate (70:30 v/v, pH 2.5), at a flow rate of 1.0 mL/min, isocratic method, and ultraviolet detection at 275 nm. A linear response (r = 1.0000) was observed in the range of 10.0-50.0 µg/mL. Validation parameters such as linearity, specificity, precision, accuracy and robustness were evaluated. The method presented precision (repeatability: relative standard deviation = 1.21% and intermediate precision: between-analyst = 0.85%). The specificity of the assay was evaluated by exposure of diclofenac potassium under conditions of stress such as hydrolysis, photolysis, oxidation and high temperature. The method presented accuracy values between 98.28% and 101.95%. The results demonstrate the validity of the proposed method that allows determination of diclofenac potassium in oral suspension and may be used as an alternative method for routine analysis of this product in quality control.

Desenvolveu-se método simples, de baixo custo para determinar o diclofenaco potássico (DP) em suspensão oral, usando coluna de fase reversa (C8, 150 mm x 4,6 mm, 5 µm), fase móvel contendo metanol/tampão fosfato (70:30 v/v, pH 2,5), com fluxo de 1,0 mL/min, método isocrático e detecção no ultravioleta a 275 nm. Observou-se resposta linear (r = 1,0000) na faixa de 10,0-50,0 µg/mL. Avaliaram-se parâmetros de validação, como linearidade, especificidade, precisão, exatidão e robustez. O método apresentou precisão (repetibilidade: desvio padrão relativo = 1,21% e precisão intermediária: entre analista = 0,85%). A especificidade do ensaio foi avaliada pela exposição do diclofenaco potássico a condições de estresse, tais como hidrólise, fotólise, oxidação e alta temperatura. O método apresentou valores de exatidão entre 98,28% e 101,95%. Os resultados mostram a validade do método proposto, que permite a determinação de diclofenaco potássico em suspensão oral e pode ser utilizado como alternativa para análise de rotina desse produto no controle de qualidade.

Effect of a cholesterol rich diet, recurrent infection and possible treatment modalities on the pulmonary vascular system: an experimental study / Efecto de la dieta rica en colesterol, la infección recurrente, y las posibles modalidades de tratamiento sobre el sistema vascular pulmonar: un estudio experimental

OBJECTIVE: Infection may lead to inflammation, atherosclerosis and thrombotic vascular events. The atherosclerotic effect of hypercholesterolaemia on the vascular system is well-known. However, limited studies were done on the therapeutic and preventative agents. The aim of this study was to investigate the effects of infection and cholesterol rich diet combined with an antibiotic, anti-inflammatory agent and red wine on the pulmonary vascular system. METHODS: Fifty-nine rats were evaluated. Six groups were created: Control-Group I (n = 10); infection - Group II (n = 9), infection-cholesterol rich diet - Group III (n = 12), infection-cholesterol rich dietcefepime - Group IV (n = 11); infection-cholesterol rich diet-diclofenac potassium - Group V (n = 9); infection-cholesterol rich diet and red wine - Group VI (n = 8). Blood samples of rats were collected for cholesterol analysis every month. Sections of central pulmonary arteries were examined for thickness of the intima and medial wall by computerised image analysis. RESULTS: There was a statistically significant difference in serum cholesterol levels and in thickness of the intima between the groups (p = 0.000). The rest of the groups had more intimal thickening than Group I (p = 0.000). Group III had thicker intima than Groups IV and V (p = 0.009, p = 0.011 respectively). There was no significant difference between the groups in thickness of media (p = 0.432). CONCLUSION: Infection and cholesterol rich diet have a synergistic effect on atherosclerosis in pulmonary arteries. However, antibiotics and anti-inflammatory agents could be useful in prevention.

OBJETIVO: La infección puede conducir a inflamación, ateroesclerosis y eventos vasculares trombóticos. El efecto aterosclerótico de la hipercolesterolemia en el sistema vascular es bien conocido. Sin embargo, se hicieron estudios limitados sobre los agentes preventivos y terapéuticos. El objetivo de este estudio fue investigar los efectos de la infección y la dieta rica en colesterol, combinados con agentes antibióticos, anti-inflamatorios, y vino tinto, sobre el sistema vascular pulmonar. MÉTODOS: Cincuenta y nueve ratas fueron evaluadas. Se hicieron seis grupos: grupo-control I (n = 10), grupo-infección II (n = 9), grupo infección-dieta rica en colesterol III (n = 12), grupo-infección-dieta rica en colesterol-cefepima IV (n = 11), grupo-infección-dieta rica en colesterol-diclofenaco potásico V (n = 9), grupo-infección-dieta rica en -vino tinto VI (n = 8). Se tomaron muestras de sangre de ratas para analizar el colesterol cada mes. Se examinaron secciones de las arterias pulmonares centrales para determinar el grosor de la pared íntima y media mediante análisis computarizado de imágenes. RESULTADOS: Hubo una diferencia estadísticamente significativa en los niveles de colesterol en suero y el grosor de la íntima entre los grupos (p = 0.000). El resto de los grupos tenía más engrosamiento de la íntima que el grupo I (p = 0.000). El grupo III tenía una íntima más gruesa que los grupos IV y V (p = 0,009, p = 0.011 respectivamente). No hubo ninguna diferencia significativa entre los grupos en cuanto al espesor de la media (p = 0.432). CONCLUSIÓN: La infección y la dieta rica en colesterol tienen un efecto sinérgico sobre la aterosclerosis en las arterias pulmonares. Sin embargo, los antibióticos y los agentes antiinflamatorios podrían ser útiles para la prevención.

Preparation and in vitro evaluation of diclofenac potassium delayed-sustained release pellets / 中国药科大学学报

Diclofenac potassium delayed-sustained release pellets were prepared by double-layer coating method with ethylcellulose aqueous dispersion.The effects of release condition and pellet compositions on the in vitro drug release were evaluated.The formulation was optimized by the central composite design-response surface methodology.It was shown that the pH of the media greatly affected the in vitro drug release of the pellets while the viscosity of the media had little influence.Drug release from the pellets was related to the proportion of the inner coat to the outer coat and the amount of pore forming agent in the outer coat.The optimization of the formulation could be achieved by the central composite design-response surface methodology.

Comparison of bioavailability and pharmacokinetics of diclofenac sodium and diclofenac potassium in normal and dehydrated rabbits / 药学学报

Two different salts of diclofenac, diclofenac sodium and dielofenae potassium, in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study. Biochemical and physiological parameters were also measured in both normal and dehydrated states. Diclofenac levels in plasma were determined using a validated reversed phase HPLC method. Primary kinetic parameters i.e. AUC0-∞, Cmax, Tmax and other disposition kinetics were obtained with non-compartmental procedure. Biochemical parameters i.e. packed cell volume, plasma glucose and total lipid concentration in dehydrated rabbits increased significantly. Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits. In comparison, diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.

Study on the Bioequiavailability of Diclofenac Potassium Capsule in Human Body / 中国药房

OBJECTIVE:To study the bioequiavailability of2kinds of diclofenac potassium capsules in human body.METHODS:The blood concentrations of the20healthy male volunteers were determined by HPLC-MS;the pharmacokinetics and the bioequiavailability in whom were calculated after orally taking by randomized crossover way single dose of trial capsule and reference capsule.RESULT:The concentration-time curves of the trial capsules and the reference capsules were in conformity with one-compartment model.The experiment data showed that the AUC 0～8 of the2kind of capsules were(2.27?0.66)、(2.16?0.58)(?g?h)/ml,respectively;their C max were(1.27?0.40)and(1.38?0.58)?g/ml,respectively;their t max were(0.9?0.7)、(1.0?0.7)h,respectively.The relative bioavailability of the trial capsules was(104.9?12.8)%.CONCLUSION:The2kinds of diclofenac potassium capsules are bioequivalent.

Effect of Different Penetration Enhancers on the Transdermal Permeation of Diclofenac Potassium Gel in Vitro / 中国药房

OBJECTIVE: To study the effects of Azone,propylene glycol(PG),oleic acid(OA) alone or in combination of two or three as penetration enhancers on the in vitro transdermal efficacy of diclofenac potassium(DP) gels.METHODS: Thirteen formulations of DP gels containing the following different penetration enhancers at different concentrations were prepared: blank,3% Azone, 5% OA,12% PG,6% PG+2.5% OA,12% PG+5% OA,1.5% Azone+2.5% OA,1.5% Azone+6% PG+5% OA,1.5 % Azone+12% PG,3% Azone+5% OA,3% Azone+6% PG,3% Azone+6% PG+5% OA,and 3% Azone+12% PG.The in vitro permeation test was performed on a modified Franz-type diffusion cell with human skin as transdermal barrier taking transdermal velocity(J) as index to determine and compute the transdermal properties of the DP gels after treated respectively by the above 13 penetration enhancers.RESULTS: Compared with the blank control group,all the penetration enhancer-treated formulations showed significant higher J value,with the formulation treated by 3% Az-one+12% PG enhancer showing the highest J value of 10.253 0 ?g?cm-2?h-1.CONCLUSION: All the three penetration enhancers could promote the transdermal permeation DP gels,much as in the combination of Azone and propylene.

Study on the Bioequivalence of Diclofenac Potassium Granule and Diclofenac Potassium Tablet in Man / 中国药房

0.05).The relative bioavailablity of diclofenac potassium granule was(99.47?9.79)%.CONCLUSION:The diclofenac potassium granule and diclofenac potassium tablet are bioequivalent.

In Vitro Dissolubility of Diclofenac Potassium Double-layer Tablet and the Factors Affecting Its Dissolubility / 中国药房

OBJECTIVE:To investigate the characteristics of drug release and the factors affecting the in vitro dissolubility of diclofenac potassium double-layer tablets(DPD).METHODS:UV-spectrophotometry and rotating basket method in the pha-rmacopeia of China 2000 edition were used to determine the in vitro dissolubility of DPD and Higuchi equation was adopeted to simulate the in vitro drug release.The main parameters of dissolution were stastistically analysed.RESULTS:Dissolution parameters of DPD were as follows:T0.3=0.10h,Td=3.30h,T0.9=9.19h.Hardness of tablets did not affect the dissolution rate significantly;pH of dissolution media significantly influenced on the rate.Rotation speed had a significant effect on dissolution action only at the beginning of test.CONCLUSION:DPD has good properties of fast and sustained release.Proper media is the key of in vitro drug release test,however,the ultimate results should be based on in vivo trial.