The Design And Development Of Carvedilol Gastroretentive Floating Drug Delivery Systems Using Hydrophilic Polymers And In Vitro Characterization

Objective: The primary aim of the present examination was to create carvedilol phosphate floating tablets using factorial designs and for retention in the upper portion of the gastrointestinal (GI) tract to sustain the dissolution where the solubility of carvedilol phosphate is more in an acidic medium. Methods: The floating tablets of carvedilol phosphate were ready to employ different concentrations and a combination of these polymers of Na-alginate, Carbopol 934P, and sodium carboxymethyl cellulose (NaCMC) with lubricants magnesium stearate by direct compression technique. In the present experiment, involved sodium bicarbonate and citric acid as a gas-producing agent. Fifteen formulations structured and judged for pre-compression components like the angle of repose, bulk and tapped density, Hausner’s ratio, compressibility index, and post-compression factors are weight uniformity, hardness, drug content, friability, in vitro buoyancy, dissolution studies, and Fourier transforms infrared spectroscopy (FTIR). Results: The drug released 90.02% in 12 h by combining NaCMC (7.5 mg) and Na-alginate (7.5 mg) in the formulation F14 towards the achievement of sustained release. Batch F14 selected as optimized, as provided desired zero-order release profile as well as floating lag time 20 s and total floating time>12 h, and the mechanism of drug release observed (n = 1.098, super case-II transport). Conclusion: From the results fulfilled that all the preparation found to be within the pharmacopeia limits and was the best dosage form to treat moderate heart failure and hypertension. The in vitro dissolution profiles of all formulations placed into various kinetic models, the statistical parameters like slope, regression coefficient and intercept determined. The gastro-retentive dosage form to maintain the sustain drug delivery, which would improve the maximum therapeutic efficacy and patient compliance.

Preparation and in vitro-in vivo evaluation of ezetimibe tablets / 国际药学研究杂志

Objective: To prepare ezetimibe tablets by direct compression technology. Methods: By comparison with the reference standard, the formulation of self-made ezetimibe tablets was optimized using the disintegration time and the release profile similarity factor f2 as the main indexes by the single factor experiments. The pharmacokinetic parameters of ezetimibe tablets in Beagle dog were determined by LC-MS/MS. The pharmacodynamic effects of ezetimibe tablets were evaluated by measuring serum total cholesterol (TC), triglycerides(TG), high-density lipoprotein cholesterol(HDL-C)and low-density lipoprotein cholesterol(LDL-C)levels. Results: Three batches of self-made ezetimibe tablets with the optimal formulation had similar in vitro dissolution behaviors as the reference preparations(f2>70). There was no significant difference in pharmacokinetic parameters in Beagle between the self-made ezetimibe tablets and the reference standard tablets, and the effect on the high serum cholesterol level was similar. Conclusion: The preparation process of the ezetimibe tablet developed in this study is simple, and the self-made tablet has bioequivalence with the reference standard, which provides a reference for the development of the ezetimibe generic drug.

Formulation and pharmacopoeial quality evaluation of ketorolac tromethamine IR tablet and comparison with marketed product

This study describes the formulation of immediate release Ketorolac tromethamine (KT) 10-mg tablet by directcompression method; evaluation of their compliance to various Pharmacopoeial quality parameters, i.e., weightvariation, friability, hardness, thickness, moisture content, disintegration, assay, and dissolution; and their comparisonwith marketed brands for determination of pharmaceutical equivalency. Five formulations of KT were prepared(coded as FKT1, FKT2, FKT3, FKT4, and FKT5) by direct compression method using different superdisintegrants.Micrometric properties of the mixtures of the drug and the excipients prepared for formulation were evaluated. Qualityevaluation of the five different formulations and randomly selected four different brands of KT 10-mg tablets purchasedfrom the local market (coded as LKT1, MKT2, MKT3, and SKT4) were performed according to Pharmacopoeia. Theresults were obtained by UV-Vis spectrophotometer and all the dissolution profiles were characterized by the zeroorder kinetics. All the brands of KT and developed formulations met the official specification except SKT4 whichshowed excessive moisture content of 7.18%. None of the tested brands of KT were found to be pharmaceuticallyequivalent, whereas two developed formulation were pharmaceutically equivalent with the in house benchmark(MKT2) from which their interchangeability can be suggested.

Evaluation of Cissus populnea gum as a directly compressible matrix system for tramadol hydrochloride extended-release tablet

The aim of this study was to evaluate and compare the compactibility, mechanical and release properties of tramadoltablets prepared by direct compression using cissus gum, a naturally occurring plant polymer as directly compressibleexcipient in comparison with xanthan gum. Compactibility was measured by Heckle, mechanical properties by tensilestrength and friability, and release properties by dissolution profile. Student t-test with GraphPad Prism 5 was used toidentify differences between data at p < 0.05. The result showed that the Py of xanthan formulation was significantlylower than cissus formulations (p = 0.03). Onset of plastic deformation was directly dependent on the concentrationof the polymer and the properties of the active ingredient. The presence of the active ingredient retarded the onsetof plastic deformation. There was increase in crushing strength and tensile strength with decrease in friability as theconcentration of the polymer increased in all formulations. The mechanical properties of cissus gum and xanthan gumformulations were not significantly different (p > 0.05). Tramadol dissolution decreased as the concentration of thepolymers increased. Cissus gum has some properties that would make it suitable as direct compressible excipient inmatrix systems for extended-release.

A Review On Co-Processed Excipients: Current And Future Trend Of Excipient Technology

There is no single-component excipient fulfills all the requisite performance to allow an active pharmaceutical ingredient to be formulated into a specific dosage form. Co-processed excipient has received much more attention in the formulation development of various dosage forms, specially for tablet preparation by direct compression method. The objective of this review is to discuss the emergence of co-processed excipients as a current and future trend of excipient technology in pharmaceutical manufacturing. Co-processing is a novel concept of combining two or more excipients that possess specific advantages that cannot be achieved using a physical admixture of the same combination of excipients. This review article discusses the advantages of co-processing, the need of co-processed excipient, general steps in developing co-processed excipient, limitation of co-processed excipient, technologies used in developing co-processing excipients, co-processed excipients in the literature, marketed products and future trends. With advantages offered by the upcoming newer combination of excipients and newer methods of co-processing, co-processed excipients are for sure going to gain attraction both from academia and pharmaceutical industry. Furthermore, it opens the opportunity for development and use of single multifunctional excipient rather than multiple excipients in the formulation.

Influence of MCC on direct pressure properties of powder extracted from Shufeng Jiedu formula / 中草药

Objective: To study the influence of microcrystalline cellulose (MCC) on the direct pressure properties of powder extracted from Shufeng Jiedu formula (SFJDE), and discuss the correlation between the basic physical properties and its functional properties of the powder before compression. Methods: SFJDE and MCC was mixed in different proportions, the physical properties of the mixed powder and the compression parameters under different pressures were determined. The basic physical properties and functional parameters of the powder were processed and analyzed by linear regression and partial least squares (PLS). Results: The addition of MCC in SFJDE showed a good linear relationship with the moisture content (MC), bulk density (ρb), and porosity ratio (ε) of the powder (r2 ≥ 0.991 9), and showed a good positive correlation with Hausner ratio (HR) and Carr’s index (CI) of the powder flow index (r2 ≥ 0.834 2). The parameters of powder compressibility compaction ratio (CR) and yield pressure (Py) gradually decreased, Unit effective work (Esp) and paramter a gradually increased; The powder compaction parameter kA was gradually increased, and kB was gradually decreased. The basic physical properties of MC, ρb, tap density (ρt), true density (ρtrue), and particle size (D0.5) of the powder had the obvious impact on these parameters by PLS analysis, while size distribution (span), HR, CI had little effect on it. However, span, HR, and CI had the obvious influence on the parameters ab and f, which characterized powder breakage and rearrangement. Conclusion: The increase of MCC reduces the fluidity of SFJDE, improves the compressibility and compactibility of the powder, therefore, we should pay attention to the influence of fluidity and pressure sensitivity during the process of use.

Property evaluation of co-processed excipient of mannitol and polyplasdone and its application in orally disintegrating tablets / 中国药学杂志

OBJECTIVE: To evaluate the properties of co-processed excipient of mannitol and polyplasdone (Man-Cro) and apply it in direct compression of orally disintegrating tablets. METHODS: The physical and micromeritic properties of the co-processed excipient were compared with those of mannitol, polyplasdone, and physical mixture of the two compounds. The interaction between the two components was studied by using FT-IR, SEM, DSC and X-RD. The flowability and compressibility of the Man-Cro co-processed excipient were also compared with the two components by determining the angle of repose, bulk density, tap-density, Carl index and Kawakita's equation. The co-processed excipient was applied to prepare ibuprofen orally disintegrating tablets. The in vitro dissolution and bioavailability of the tablets were evaluated. RESULTS: The co-processed excipient of mannitol and polyplasdone formed novel aspheric particles after cocrystallization. The excipient showed good flowability, compressibility, filling ability and disintegrability. Compared with commercially available ibuprofen tablets, the ibuprofen orally disintegrating tablets prepared with the co-processed excipient had more rapid in vitro dissolution. And the homemade and commercially available preparations were bioequivalent in rats. CONCLUSION: The co-processed excipient is superior to physical mixture as drug carrier and suitable for preparation of orally disintegrating tablets by direct compression.

The Compaction, Mechanical and Disintegration Properties of Modified Pennisetum glaucum (Poaceae) Starch in Directly Compressed Chloroquine Tablet Formulations.

Pennisetum glaucum L (Millet) starch is a potential source of direct-compression excipient for use in tableting but has not been commercially explored. The aim of this study was to investigate the compaction properties of pregelatinized freeze (PFDMS) and oven-dried (PODMS) millet starch in directly compressed Chloroquine tablet formulation and compare with the native starch (NMS) and Avicel®. Tablets were directly compressed using the starch in drug-diluent ratios of 1:2, 1:4 and 1:9 and evaluated by compaction, mechanical and disintegration properties. The result showed that PFDMS and PODMS starch samples had higher flow properties in comparison to the native starch and PFDMS also gave the fastest onset of plastic deformation. Tablets formulated with PFDMS and PODMS showed acceptable mechanical and disintegration properties comparable with Avicel® in the order Avicel® > PFDMS > PODMS > NMS. The pregelatinized starch samples can be substituted for Avicel® for direct compression.

Effect of thermal and chemical modifications on the mechanical and release properties of paracetamol tablet formulations containing corn, cassava and sweet potato starches as filler-binders

Objective: To investigate the effects of acetylation and pregelatinization of cassava and sweet potato starches on the mechanical and release properties of directly compressed paracetamol tablet formulations in comparison with official corn starch. Methods: The native starches were modified by acetylation and pregelatinization. The tablets were assessed using friability (F

Characterisation of a novel, multifunctional, co-processed excipient and its effect on release profile of paracetamol from tablets prepared by direct compression

Objective: To characterise a novel multifunctional pharmaceutical excipient and investigate its effect on paracetamol release from tablets prepared by direct compression. Methods: The excipient was prepared by co-processing gelatinized maize starch with sodium carboxymethyl cellulose and microcrystalline cellulose in a ratio of 2:1:1, dried and pulverized into powder. The excipient formulated was characterized using Fourier transform infrared spectroscopy and differential scanning calorimetry. The excipient was used to prepare batches of tablets by direct compression with drug-excipient ratios of 1:1, 1:2, 1:3 and 1:4. Parameters evaluated on tablets include crushing strength, friability and in vitro dissolution studies. Results: Differential scanning calorimetry analysis revealed a crystalline excipient while Fourier transform infrared spectroscopy showed no interaction between the excipient and paracetamol. Tablets from all the batches gave average crushing strength values between 3.47 and 4.88 kp. The 1:1 and 1:2 tablet batches were comparable to each other while 1:3 and 1:4 were also comparable to one another in their dissolution profiles. The dissolution parameters of the 1:4 batch was faster with - m

Effect of thermal and chemical modiifcations on the mechanical and release properties of paracetamol tablet formulations containing corn, cassava and sweet potato starches as ifller-binders

Objective:To investigate the effects of acetylation and pregelatinization of cassava and sweet potato starches on the mechanical and release properties of directly compressed paracetamol tablet formulations in comparison with official corn starch. Methods: The native starches were modified by acetylation and pregelatinization. The tablets were assessed using friability (Fr), crushing strength (Cs), disintegration time (Dt) and dissolution parameters. Results: Starch acetylation produced paracetamol tablets that were stronger and had the best balance of mechanical and disintegration properties, while pregelatinization produced tablets that were more friable but had a better overall strength in relation to disintegration than formulations made from natural starches. Correlations mainly existed between Dt and the dissolution parameters t80, t2 and k1 in the formulations. Conclusions:Modification of the experimental starches improved the mechanical and release properties of directly compressed paracetamol tablet formulations. Thus, they can be developed for use as pharmaceutical excipients in specific formulations.

Characterisation of a novel, multifunctional, co-processed excipient and its effect on release profile of paracetamol from tablets prepared by direct compression

To characterise a novel multifunctional pharmaceutical excipient and investigate its effect on paracetamol release from tablets prepared by direct compression. Methods: The excipient was prepared by co-processing gelatinized maize starch with sodium carboxymethyl cellulose and microcrystalline cellulose in a ratio of 2:1:1, dried and pulverized into powder. The excipient formulated was characterized using Fourier transform infrared spectroscopy and differential scanning calorimetry. The excipient was used to prepare batches of tablets by direct compression with drug-excipient ratios of 1:1, 1:2, 1:3 and 1:4. Parameters evaluated on tablets include crushing strength, friability and in vitro dissolution studies. Results: Differential scanning calorimetry analysis revealed a crystalline excipient while Fourier transform infrared spectroscopy showed no interaction between the excipient and paracetamol. Tablets from all the batches gave average crushing strength values between 3.47 and 4.88 kp. The 1:1 and 1:2 tablet batches were comparable to each other while 1:3 and 1:4 were also comparable to one another in their dissolution profiles. The dissolution parameters of the 1:4 batch was faster with - m∞(90.5%), t50% (3.5 min), t70% (11.6 min) while that of ratio 1:1 was the least with - m∞ (48.6%), m5min (23.8%). Their release kinetics followed a Korsmeyer-Peppas model with a super case-II transport mechanism. Conclusions: The drug-excipient ratios of 1:3 and 1:4 gave pharmaceutically acceptable tablets that met the British Pharmacopoeia specifications. The t50% value of the 1:4 batch of tablets may find its usefulness in formulating drugs for which a fast onset of action is desired.

Preparation of a co-processed compound based on mainnitol and starch fordirect compression and properties evaluation / 中国药学杂志

OBJECTIVE: To prepare mannitol and starch co-processed compound for direct compression. METHODS: The compound was prepared with granulation technique, and the ratio of mannitol to starch was 20:1. Then the compound was compared to the physical blend to evaluate its properties. RESULTS: The compound exhibited good flowability, packing rate, compressibility, and shorter disintegration time. It also improved the content uniformity of low dosage formulations. CONCLUSION: The compound is superior to physical blend as drug carrier and suitable for direct compression.

Preparation optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test / 重庆医学

Objective To prepare optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test. Methods Palonosetron hydrochloride oral disintegrating tablets were prepared with direct compression process.The content of pal-onosetron hydrochloride was determined by HPLC.The formulation was optimized with disintegration time as evaluation indices. Results The optimal formulation(60 mg/tablet)was as follows:L-HPC 12%,mannitol∶SMCC= 2∶1,magnesium stearate 2%, stevia glycosides 3%.The oral disintegrating tablets showed dine appearance and tested better;the disintegration time was 12 sec-onds;the tablets featured a hardness of 3 kg;4 min dissolution rate was 99%.Conclusion The preparation method is simple and reasonable,and the tablets can disintegrate rapidly.

Fabrication and Optimization of Novel Lornoxicam Matrix Tablets Using 3-Factor 3-Level Box-Behnken Statistical Design: Invitro and Invivo Evaluation.

In the present study efforts have been made to prepare sustained release matrix tablets of Lornoxicam. Matrix tablets were prepared by direct compression method by using Hydroxypropyl methyl cellulose K15 (HPMC- K15), Ethyl cellulose (EC) and Sodium carboxy methyl cellulose (Na-CMC) as polymers in different concentrations. A 3-factor 3- level Box-Behnken statistical design was used as an optimization tool having total of 17 experimental runs with 5 central points. All three polymers were selected as independent variables while %age drug release at various time intervals and hardness were used as dependant variables. In vivo studies were conducted on human plasma using Tenoxicam as internal standered. All the detections were made on SYKNM HPLC. Foriour Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetery (DSC) studies were conducted and no chemical interaction was found between drug and polymers. The drug release mechanism was mainly governed by non-fickian (anomalous) diffusion and zero-order (case II) transport diffusion. Regression analysis was performed on dissolution data obtained with the selected response variables and polynomial models were constructed. Polynomial models were further validated using one way ANOVA and results indicated that all the polymers used have significant effect on selected response (p>0.05). Contour plots and three dimensional response surface curves were drawn. In- vivo studies were conducted on two tablet formulation indicating slow and sustained release of the drug from matrix. From Behnken design it is possible to successfully formulate and optimize Lornoxicam sustained release matrix tablets with three polymers (HPMC- K15, EC and Na-CMC) in combination.

Implementation of time release technology in formulation development and evaluation of sustained release tablet of Lornoxicam.

In present study, the attempts have been made to formulate sustained release tablets of lornoxicam by direct compression method. Based on viscosity grades different proportions of hydrophilic polymers (HPMC K4M, HPMC K15M, HPMC K100M) are used for preparation of lornoxicam sustained release matrix tablet. The drug excipient mixtures were subjected to preformulation studies comprising of micromeritic properties. The tablets were subjected to various studies like as physicochemical studies, in vitro drug release, kinetic studies, etc. FTIR studies shown there was no interaction between drug and polymers. The physicochemical properties of tablets were found within the limits. Lornoxicam is a first generation analgesic, inflammatory & antipyretic agent used in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. From developed formulations batch F1 have shown zero order drug release behavior and prolong drug release over a period of 12 h which was deemed as suitable and optimum formulation for sustained drug delivery. Results of the present study indicated the suitability of the low viscous polymer in the proportion of (drug:polymer) 1:1 in the preparation of sustained release formulation of lornoxicam.

Preparation and scale up of extended-release tablets of bromopride

Reproducibility of the tablet manufacturing process and control of its pharmaceutics properties depends on the optimization of formulation aspects and process parameters. Computer simulation such as Design of Experiments (DOE) can be used to scale up the production of this formulation, in particular for obtaining sustained-release tablets. Bromopride formulations are marketed in the form of extended-release pellets, which makes the product more expensive and difficult to manufacture. The aim of this study was to formulate new bromopride sustained release formulations as tablets, and to develop mathematical models to standardize the scale up of this formulation, controlling weight and hardness of the tablets during manufacture according to the USP 34th edition. DOE studies were conducted using Minitab(tm) software. Different excipient combinations were evaluated in order to produce bromopride sustained-release matrix tablets. In the scale-up study, data were collected and variations in tableting machine parameters were measured. Data were processed by Minitab(tm) software, generating mathematical equations used for prediction of powder compaction behavior, according to the settings of the tableting machine suitable for scale-up purposes. Bromopride matrix tablets with appropriate characteristics for sustained release were developed. The scale-up of the formulation with the most suitable sustained release profile was established by using mathematical models, indicating that the formulation can be a substitute for the pellets currently marketed.

A reprodutibilidade do processo de fabricação de comprimidos e o controle das suas propriedades farmacotécnicas depende da otimização dos aspectos de formulação e dos parâmetros de processo. O planejamento de experimentos como o Desenho de Experimentos (DOE) pode ser utilizado para acelerar a produção desta formulação, em particular, para a obtenção de comprimidos de liberação prolongada. Formulações de bromoprida são comercializadas sob a forma de péletes de liberação prolongada, o que torna o produto caro e de difícil fabricação. O objetivo deste estudo foi preparar novas formulações de bromoprida de liberação prolongada na forma de comprimidos e desenvolver modelos matemáticos visando ao escalonamento destas formulações, controlando o peso e a dureza dos comprimidos durante a fabricação, de acordo com a 34ª Edição da USP. Estudos de DOE foram realizados utilizando o software Minitab(tm). Diferentes combinações de excipientes foram avaliadas visando à obtenção dos comprimidos de liberação prolongada de bromoprida. No estudo de scale-up, coletaram-se e mediu-se a influência das variações nos parâmetros da máquina de compressão. Processaram-se os dados obtidos pelo software Minitab (tm), gerando equações matemáticas aptas para a previsão do comportamento de compactação do pó em escala industrial. Os comprimidos obtidos apresentavam características adequadas em termos de liberação sustentada, sendo a cinética de liberação estabelecida utilizando modelos matemáticos, indicando que esta formulação pode ser uma substituta aos péletes de bromoprida atualmente comercializados.

Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

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.

Formulation design and evaluation of Cefuroxime axetil 125 mg immediate release tablets using different concentration of sodium lauryl sulphate as solubility enhancer

Cefuroxime axetil immediate release tablets were formulated by direct compression method with different percentages of sodium lauryl sulphate (SLS) such as 0.5, 1.0, 1.5 and also without SLS. Resulting batches of tablets were evaluated by both pharmacopeial and non-pharmacopeial methods to ascertain the physico-mechanical properties. Dissolution test were carried out in different medium like 0.07 M HCl, distilled water, 0.1M HCl of pH 1.2 and phosphate buffers at pH 4.5 and 6.8 to observe the drug release against the respective concentration of SLS used. Later, test formulations were compared by f1 (dissimilarity) and f2 (similarity) factors using a reference brand of cefuroxime axetil. Significant differences (p<0.05) in dissolution rate were recorded with the change in concentration of SLS in different media. Test formulation T3 containing 1% SLS was found to be best optimized formulation based on assay, disintegration, dissolution and similarity and dissimilarity factors.

Formularam-se comprimidos de liberação imediata à base de cefuroxima axetil, pelo método de compressão direta, com diferentes percentagens de lauril sulfato de sódio (LSS), tais como 0,5, 1,0, 1,5, e também sem SLS. Os lotes resultantes dos comprimidos foram avaliados por ambos os métodos da farmacopeia e não farmacopeicos para determinar as propriedades físico-mecânicas. O teste de dissolução foi realizado em meios diferentes, como HCl 0,07 M, água destilada, HCl 0,1 M com pH 1,2 e os tampões fosfato (pH 4,5 e 6,8) para observar a liberação do fármaco contra a correspondente concentração de LSS utilizado. Em seguida, as formulações de teste foram comparadas por fatores f1 (dissimilaridade) e f2 (similaridade), utilizando uma marca de referência de cefuroxima axetil. Diferenças significativas (p<0,05) na taxa de dissolução foram registradas com a mudança na concentração de LSS em diferentes meios de dissolução. A formulação T3 contendo LSS a 1% foi considerada a melhor formulação otimizada com base nos ensaios de desintegração, dissolução e fatores de semelhança e dissimilaridade.

Design and evaluation of fast dissolving tablets containing diclofenac sodium using fenugreek gum as a natural superdisintegrant

Objective: To formulate diclofenac sodium as fast dissolving tablets (FDTs) using fenugreek gum as a natural superdisintegrant which also possess anti-inflammatory activity.Methods:physicochemical characterizations. The swelling index and viscosity of fenugreek gum was 221% and 293.4 mpa.s respectively. FDTs of diclofenac sodium was formulated by direct compression technique using different concentrations (1%-6%, w/w) of fenugreek gum as a natural superdisintegrant and compared with renowned synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium. The anti-inflammatory activity of a formulation was evaluated with carrageenan induced experimental rats.Results:An attempt was made to extract the fenugreek gum and evaluated it for various friability, hardness and results complied with the limits. The drug release from all the formulations ascertained first order kinetics. Among all the formulations F3 containing fenugreek gum with the concentration of 6% produced least disintegrating time 21 seconds resulting in higher drug release rate 93.74% at the end of 25 min. Hence, it was considered as optimized formulation. The present study revealed that the fenugreek gum as a natural superdisintegrant showed better disintegrating property than the most widely used synthetic superdisintegrants like sodium starch glycolate and croscarmellose sodium in the formulations of FDTs. The formulated tablets were evaluated for various physical tests like weight variation, Conclusions: The results suggested that the fenugreek gum act as a good super disintegrating agent and it showed promising additive anti-inflammatory activity with diclofenac sodium.