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1.
Article in English | IMSEAR | ID: sea-163524

ABSTRACT

The present investigation targets to develop a simple, specific, sensitive and accurate reverse phase high performance liquid chromatographic (RP-HPLC) method in human plasma for the estimation of metformin HCl and propranolol HCl from bulk drug and also from the marketed products. Human plasma samples were subjected to correct procedure for protein precipitation by methanol and protein free plasma samples were directly injected into HPLC C18 column. Chromatographic determination was performed on a reversed phase C18 column (3.9 mm X 300 mm, particle size 5 μm) using a mixture of acetonitrile and 0.1M pH 4.5 potassium dihydrogenortho phosphate buffer (mL) (40:60) at a flow rate of 0.8 mL/min and maintained at a pressure of 140 to 150 Kg/cm2. The retention time for metformin HCl and propranolol HCl was found to be 9.084 min and 6.132 min respectively at 232 nm without any interference of endogenous compounds in the plasma. The method was linear in the range between 50-2000 ng/mL. The peak areas were reproducible as indicated by low coefficient of variation. It was found that the excipients in the tablet dosage form do not interfere in the quantification of active drug by proposed method.

2.
Braz. j. pharm. sci ; 50(2): 431-439, Apr-Jun/2014. tab, graf
Article in English | LILACS | ID: lil-722176

ABSTRACT

The aim of the present research is to formulate and evaluate the gastroretentive floating drug delivery system of antihypertensive drug, propranolol HCl. Gastroretentive floating tablets (GRFT) were prepared by using a synthetic hydrophilic polymer polyethylene oxide of different grades such as PEO WSR N-12 K and PEO 18 NF as release retarding polymers and calcium carbonate as gas generating agent. The GRFT were compressed by direct compression strategy and the tablets were evaluated for physico-chemical properties, in vitro buoyancy, swelling studies, in vitro dissolution studies and release mechanism studies. From the dissolution and buoyancy studies, F 9 was selected as an optimized formulation. The optimized formulation followed zero order rate kinetics with non-Fickian diffusion mechanism. The optimized formulation was characterised with FTIR studies and observed no interaction between the drug and the polymers.


O objetivo da presente pesquisa é o de formular e avaliar o sistema de liberação de fármaco gastrorretentivo flutuante, contendo o anti-hipertensivo, cloridrato de propranolol. Comprimidos gastrorretentivo flutuantes (GRFT) foram preparados utilizando um polímero hidrofílico sintético, o óxido de polietileno, de diferentes graus, tais como GE WSR N-12 K e GE 18 NF, como polímeros de retardamento de liberação, e carbonato de cálcio, como agente gerador de gases. Os GRFT foram comprimidos por compressão direta e avaliados para determinação das propriedades físico-químicas, flutuabilidade in vitro, estudos de inchamento, de dissolução in vitro e de mecanismo de liberação. Dos testes de dissolução e de flutuabilidade, selecionou-se F 9 como formulação otimizada. A formulação otimizada seguiu cinética de ordem zero, com mecanismo de difusão não-Fickiano. Essa formulação foi caracterizada por estudos de FTIR, não se observando interação entre o fármaco e os polímeros.


Subject(s)
Hydrophobic and Hydrophilic Interactions , Drug Liberation , Tablets/chemistry , Chemistry, Pharmaceutical/classification
3.
Invest. clín ; 54(4): 347-359, dic. 2013. ilus, tab
Article in English | LILACS | ID: lil-740352

ABSTRACT

The aim of the present research was to prepare and evaluate a gastroretentive drug delivery system for metformin HCl, using synthetic and semi-synthetic polymers. The floating approach was applied for preparing gastroretentive tablets (GRT) and these tablets were manufactured by the direct compression method. The drug delivery system comprises of synthetic and semi-synthetic polymers such as polyethylene oxide and Carboxymethyl ethyl cellulose (CMEC) as release-retarding polymers. GRT were evaluated for physico-chemical properties like weight variation, hardness, assay friability, in vitro floating behaviour, swelling studies, in vitro dissolution studies and rate order kinetics. Based upon the drug release and floating properties, two formulations (MP04 & MC03) were selected as optimized formulations. The optimized formulations MP04 and MC03 followed zero order rate kinetics, with non-Fickian diffusion and first order rate kinetics with erosion mechanism, respectively. The optimized formulation was characterised with FTIR studies and it was observed that there was no interaction between the drug and polymers.


El objetivo del presente trabajo consistió en preparar y evaluar un sistema de administración gastro-retentivo de metformina HCl, utilizando polímeros sintéticos y semisintéticos. Se aplicó el método de flotación para la elaboración de los comprimidos de retención gástrica (CRG) y éstos se prepararon mediante el método de compresión directa. El sistema de suministro del fármaco estaba constituido por polímeros sintéticos y semisintéticos, tales como el óxido de polietileno y la carboximetil etil celulosa, como agentes retardadores de la liberación del fármaco. Se evaluaron las propiedades físico-químicas de los CRG, tales como: variación de peso, dureza, friabilidad, comportamiento flotante in vitro, capacidad de inflación, estudios de disolución in vitro y su tasa de orden cinético. Se seleccionaron dos fórmulas (MP04 y MC03), sobre la base de la liberación del fármaco y las propiedades de flotabilidad, como fórmulas óptimas. Estas fórmulas MP04 y MC03 optimizadas siguieron cinéticas de velocidad de orden cero, con difusión no-Fickian y tasa cinética de primer orden con mecanismo de erosión, respectivamente. Las fórmulas óptimas se caracterizaron con estudios FTIR y se observó que no hubo interacción entre el fármaco y los polímeros.


Subject(s)
Drug Delivery Systems , Metformin/administration & dosage , Chemistry, Pharmaceutical/methods , Drug Delivery Systems/methods , Polymers , Stomach , Tablets
4.
Jordan Journal of Pharmaceutical Sciences. 2013; 6 (1): 9-22
in English | IMEMR | ID: emr-147456

ABSTRACT

The aim of the present investigation is to obtain a programmed drug delivery from a novel system containing a fast release and prolonged release tablet [PRT] placed into a capsule to achieve the biphasic release pattern of lornoxicam. Fast release tablets [FRT] with 3.25 mg were prepared with different diluents and varying concentrations of disintegrant and binders. Hydrogenated castor oil and hydrogenated vegetable oil are used to modulate drug release for the development of PRT with a 12.25 mg dose calculated as a zero-order principle. The compressed tablets were evaluated for various physicochemical parameters like hardness, friability, drug content uniformity, weight variation and in-vitro drug release studies. The optimized FRT and PRT tablets were placed in the size 2 capsule to attain biphasic release in which the immediate rapid release was obtained by the FRT followed by slow release from the PRT for 24 hours. The optimized 'tablet in capsule' [TCHV] [containing 3%w/w of HVO] followed first-order release with a Non-Fickian diffusion mechanism. FT-IR studies revealed no interaction between the drug and polymers. There were no marketed dosage forms of lornoxicam with biphasic release; hence, the present study indicated the applicability of the 'tablets in capsule' technique in the design of biphasic release systems of lornoxicam

5.
Invest. clín ; 53(3): 223-236, sep. 2012. ilus, tab
Article in English | LILACS | ID: lil-676474

ABSTRACT

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50°C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.


El propósito de la presente investigación fue la elaboración de tabletas flotantes de HCL propanolol térmicamente sinterizadas y estudiar los efectos de las condiciones de sinterización sobre la liberación de la droga, así como sobre sus propiedades de flotabilidad in vitro. Se seleccionó un polímero hidrofílico, el óxido de polietileno, como polímero sinterizado, para retardar la liberación de la droga. Las fórmulas se prepararon mediante un método de compresión directa y se evaluaron mediante estudios de disolución in vitro. Los resultados demostraron que la temperatura de sinterización y el tiempo de exposición tuvieron una gran influencia sobre las propiedades de flotabilidad y de disolución. Se encontró que el intervalo de retardo en la flotación disminuyó, el tiempo total de flotación aumentó y se retardó la liberación de la droga, a medida que aumentaron la temperatura de sinterización y el tiempo de exposición. Se seleccionó una fórmula óptima de sinterización (temperatura de sinterización de 50°C y tiempo de exposición de 4 h), basados en las propiedades retardativas sobre la droga. La fórmula sinterizada se caracterizó mediante estudios FITR y DSC y no se encontró ninguna interacción entre la droga y el polímero utilizado.


Subject(s)
Chemistry, Pharmaceutical/methods , Propranolol , Tablets , Drug Delivery Systems , Hot Temperature , Physical Phenomena , Stomach
6.
Braz. j. pharm. sci ; 48(4): 609-619, Oct.-Dec. 2012. ilus, tab
Article in English | LILACS | ID: lil-665857

ABSTRACT

The objective of the present investigation was to develop bilayered tablets of lornoxicam to achieve biphasic release pattern. A bilayered tablet, consisting of an immediate and controlled release layer, was prepared by direct compression technique. The controlled release effect was achieved by using various hydrophilic natural, semi synthetic and synthetic controlled release polymers such as xanthan gum, hydroxypropyl methylcellulose (HPMC) and polyethylene oxide (PEO) to modulate the release of the drug. The in vitro drug release profiles showed the biphasic release behavior in which the immediate release (IR) layer containing the lornoxicam was released within 15 minutes, whereas the controlled release (CR) layer controlled the drug release for up to 24 h. All the bilayered tablets formulated have followed the zero order release with non-Fickian diffusion controlled release mechanism after the initial burst release. FTIR studies revealed that there was no interaction between the drug and polymers used in the study. Statistical analysis (ANOVA) showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 24 h from optimized formulations was observed. Based on the release kinetic parameters obtained, it can be concluded that xanthan gum polymer was suitable for providing a biphasic release of lornoxicam.


O objetivo do presente trabalho foi desenvolver comprimidos bicamada de lornoxicam para atingir padrão de liberação bifásica. Preparou-se, por compressão direta, comprimido bicamada, consistindo de uma camada de liberação imediata e uma de liberação controlada. A liberação controlada foi obtida pelo uso de vários polímeros naturais hidrofílicos, semi-sintéticos e sintéticos, tais como goma xantana, hidroxipropilmetil celulose (HPMC) e óxido de polietileno (PEO) para modular a liberação do fármaco. Os perfis de liberação in vitro mostraram comportamento bifásico em que a camada de liberação imediata (IR) contendo lornoxicam foi liberada em 15 minutos, enquanto a camada de liberação controlada (CR) liberou o fármaco em mais de 24 horas, Todos os comprimidos bicamada formulados seguiram a liberação de ordem zero com mecanismo de liberação controlada por difusão não fickiana após a liberação inicial por erupção. Os estudos de FTIR revelaram que não há interação entre o fármaco e os polímeros utilizados no estudo. A análise estatística (ANOVA) não mostrou diferença significativa na quantidade acumulada de fármaco após 15 minutos de liberação, mas observou-se diferença significativa (p<0,05) na quantidade de fármaco liberado após 24 h nas formulações otimizadas. Com base nos parâmetros de cinética de liberação obtidos, pode-se concluir que a goma xantana foi adequada para se atingir liberação bifásica de lornoxicam.


Subject(s)
Tablets/pharmacokinetics , Bentonite/antagonists & inhibitors , Polymers/pharmacokinetics , Drug Liberation
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