Formulation And Evaluation Of Famotidine Fast Dissolving Tablets Using Synthetic Superdisintegrants

Objective: The main aim of the present research work was to formulate fast dissolving tablets of famotidine by direct compression method and to evaluate the effect of synthetic super disintegrating agent on drug release pattern. Methods: The fast dissolving tablets were prepared by using crospovidone, croscarmellose sodium, sodium starch glycolate as superdisintegrants (2, 4 and 6 %w/w), mannitol 20 % and microcrystalline cellulose (44, 46 and 48 % w/w) as a directly compressible vehicle. All the prepared tablets were evaluated for hardness, friability, drug content uniformity, weight variation, disintegrating time, wetting time and in vitro drug release studies. Results: All the prepared fast dissolving tablets formulations were within the Pharmacopoeial standards limits. Based on in vitro drug release studies (>90 % within 30 min), the optimised formulations were optimised tested for the short term stability (at 40 ˚C/75% RH for 3 mo) and drug excipient interaction (fourier transform infrared spectroscopy). Conclusion: Hence, formulation prepared with 6 % w/w of crosspovidine and 44 % w/w of microcrystalline cellulose as emerged as the overall best formulation (>90 % within 30 min) compared to marketed product (>70 % within 30 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro drug release (p<0.05).

Formulation, in vitro Characterization and Stability Studies of Fast Dispersing Tablets of Diclofenac Sodium.

The present study was aimed to formulate, develop and evaluate the fast dissolving tablets of diclofenac sodium, used for the treatment of arthritis, inflammation, pain. Fast dissolving tablets of diclofenac sodium were prepared by direct compression method using crospovidone and sodium starch glycolate as superdisintegrants in concentrations of 5.3%, 6.6% and 8% w/w and in combination. In this work microcrystalline cellulose and mannitol are investigated as diluents. Prepared powder mixtures were evaluated for drug excipient compatibility with FTIR spectroscopy and DSC analysis. Prepared formulations are evaluated for In vitro dissolution, disintegration dispersion and wetting time. Formulation FCS6 prepared with combination of crospovidone and sodium starch glycolate at weight ratio of 6.6 and 2.3% showed better results compare with control. Post compression parameters like hardness (3.4 kg/cm2) and friability (0.31%) are at good acceptable levels in accordance with official compendia. FCS6 showed improved dissolution (99.8 %) and dispersion (75 seconds) profiles compared to control. The FTIR and DSC showed no interaction between the drug and excipients. The optimized formula FCS6 showed good drug release characteristics with acceptable mouth feel and fast dissolving properties.

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

<p><b>OBJECTIVE</b>To formulate diclofenac sodium as fast dissolving tablets (FDTs) using fenugreek gum as a natural superdisintegrant which also possess anti-inflammatory activity.</p><p><b>METHODS</b>An attempt was made to extract the fenugreek gum and evaluated it for various 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.</p><p><b>RESULTS</b>The formulated tablets were evaluated for various physical tests like weight variation, 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.</p><p><b>CONCLUSIONS</b>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.</p>

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.

Formulation & Evaluation of Fast Dissolving Tablets of Amlodipine Besylate by Using Co- Processed Superdisintegrants.

Aims: To formulate fast dissolving tablets of amlodipine besylate using co-processed superdisintigrant and evaluate the properties of fast dissolving tablets. Study Design: Formulation, evaluation of fast dissolving tablets of amlodipine besylate. Place and Duration of Study: Department of Quality Assurance S. N. D. College of Pharmacy Babhulgoan Yeola Dist Nashik 423401, between July 2012 to February 2013. Methodology: In the present study, novel co-processed superdisintegrants were developed by solvent evaporation method using crospovidone and sodium starch glycolate in different ratios (1:1, 1:2 1:3 2:1, 3:1) in the fast dissolving tablet formulations. Drug and the developed excipients were characterized for compatibility studies with FTIR and DSC. The co-processed superdisintigrant mixture was evaluated for angle of repose, Carr’s index and Hausner’s ratio in comparison with physical mixture of superdisintegrants. Fast dissolving tablets of Amlodipine Besylate were prepared using co-processed superdisintegrants and evaluated for pre-compression and postcompression parameters. Effect of co-processed superdisintegrants (crospovidone and sodium starch glycolate) on wetting time, disintegrating time, drug content, in-vitro release, and stability parameters have been studied. Results: The angle of repose of the developed excipients was found to be < 300 Compressibility (%) index in the range of 13.14 to 14.63 % and Hausner’s ratio in the range of 1.15-1.19. The prepared tablets were characterized by FTIR and DSC Studies there was no change in the result. Based on in-vitro dispersion time (approximately 40 sec), promising formulation CP5 was tested for in-vitro drug release pattern in phosphate buffer pH 6.8. Conclusion: Among the designed formulations, the formulation (CP5) containing coprocessed superdisintegrant (3:1 mixture of crospovidone and sodium starch glycolate) emerged as the overall best formulation based on drug release characteristics in phosphate buffer pH 6.8. From this study, it can be concluded that dissolution rate of amlodipine besylate could be enhanced by tablets containing co-processed superdisintegrant.

Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate

The demand for fast dissolving tablets has been growing during the last decade, especially for elderly and children who have swallowing difficulties. In the present work, fast dissolving tablets of metoprolol tartrate, were prepared using sodium starch glycolate, sodium croscarmellose and crospovidone as superdisintegrants, by the direct compression method. The tablets prepared were evaluated for various parameters including weight variation, hardness, friability, in vitro dispersion time, drug-polymer interaction, drug content water absorption ratio, wetting time, in vitro drug release, FTIR and DSC studies. The tablets prepared by the direct compression method had a weight variation in the range of 145 mg to 152 mg, which is below ± 7.5%, a hardness of 3.6 kg/cm² to 4.5 kg/cm², percentage friability of 0.46% to 0.73%, in vitro dispersion time of 18 s to 125 s, drug content uniformity of between 98.12% and 100.03%, a water absorption ratio of 67% to 87%, wetting time of 32 sec. to 64 sec., and an in vitro drug release of 53.92% - 98.82% within 15 min. The IR spectral analysis and DSC study showed no drug interaction with formulation additives of the tablet, and the formulations indicated no significant changes in hardness, friability, drug content or in vitro drug release. Fast dissolving tablets of metoprolol tartrate have enhanced dissolution and will lead to improved bioavailability and more effective therapy.

A exigência por comprimidos de dissolução rápida aumentou durante a última década, especialmente para idosos e crianças, com dificuldades de deglutição . No presente trabalho prepararam-se, pelo método de compressão direta, comprimidos de tartarato de metoprolol de rápida dissolução, utilizando glicolato sódico de amido, croscarmellose sódica e crospovidona como superdisintegrantes. Os comprimidos preparados foram avaliados em relação a diferentes parâmetros, como variação de peso, dureza, friabilidade, tempo de dispersão in vitro, interação fármaco-polímero, taxa de absorção de água pelo fármaco, tempo de umedecimento, liberação do fármaco in vitro,, FTIR e estudos de DSC. Os comprimidos preparados por compressão direta apresentaram variação de peso de 145 mg a 152 mg, abaixo de ±7,5%, dureza de 3,6 kg/cm² a 4,5 kg/cm² , porcentagem de friabilidade de 0,46% a 0,73%, tempo de dispersão in vitro de 18 s a 125 s, uniformidade de conteúdo de fármaco entre 98,12% e 100,03%, taxa de absorção de água de 67% a 87%, tempo de umidificaçãode 32 s a 64 s liberação do fármaco in vitro entre 53,92% e 98,82%, em 15 min. A análise no IV e de DSC mostrou que não houve interação de fármacos com os aditivos de formulação do comprimido e as formulações indicaram que não houve mudança significativa na dureza, friabilidade, s uniformidade de conteúdo de fármaco e na liberação do fármaco in vitro. Os comprimidos de liberação rápida apresentaram aumento na dissolução de tartarato metoprolol e conduzem à melhoria dabiodisponibilidade e à terapia eficaz.

Observation of the effect of Sodium Starch Glycolate in the treatment of children with recurrent respiratory tract infection and its influence on cellular and humoral immunologic function / 中国基层医药

Objective To explore the curative effect of Sodium Starch Glycolate on children with recurrent respiratory tract infection(RRI) and its influence on cellular and humoral immunologic function.Methods 50 RRI children were selected as treatment group and treated by Sodium Starch Glycolate orally for 12 weeks.The changes of cellular and humoral immunologic function before and after treatment,and the curative effect and adverse reaction were observed.Another 3 0 non RRI but ARI children who received outpatient medical treatment during the same period were selected as control group.Results Before treatment,the level of CD4+ and CD4+/CD8+ of treatment group were significantly lower than that of control group,but the level of CD8+ was the opposite(t =2.27,2.25,2.91,P ＜0.05 or P ＜0.01).After treatment for 12 weeks,the level of CD4+ and CD4+/CD8+ of treatment group increased significantly compared with before treatment,but the level of CD8+ reduced significantly (t =2.12,2.17,2.43,all P ＜ 0.05).The plasma levels of IgG,IgA and IgM of treatment group were significantly lower than those of the control group before treatment (t =2.45,2.91,2.44,P ＜ 0.05 or P ＜ 0.01).After treatment for 12 weeks,the levels of IgG,IgA and IgM of treatment group increased significantly(t =2.14,2.25,2.31,all P ＜ 0.05),and the total effective rate was up to 96.0％ (48/50).No obvious adverse reaction occurred during treatment.Conclusion Sodium Starch Glycolate in treating RRI children shows good effect and high safety,which maybe relate with regulating the imbalance of the T cell subsets and immune globulin and enhancing the cellular and humoral immunologic function.

Cápsulas gelatinosas duras de nimesulida: a influência do amido glicolato de sódio, e sua concentração, na dissolução do fármaco / Hard gelatin capsules of nimesulide: the influence of sodium starch glycolate, and its concentration, on the dissolution of the drug

This article reports a study of the influence of sodium starch glycolate (SSG) on the dissolution of nimesulide carried in hard gelatin capsules. Some physicochemical parameters of nimesulide were characterized and formulations containing three different contents of SSG were prepared, to compound the hard gelatin capsules of nimesulide. The capsules obtained, as well as the reference drug, were subjected to in vitro dissolution tests. During the maximum pharmacopoeial dissolution time, the amount of drug substance dissolved was determined and the dissolution profile was traced from the amount of drug dissolved in each time interval. The dissolution profiles were compared by the simple Model-Independent Method, by statistical assessment of the dissolution profile data for each time interval and by the dissolution efficiency (DE). The results show that SSG, used as a disintegrant, has a positive influence on the dissolution of nimesulide, facilitating the disintegration of the dosage form, increasing the contact surface of the drug with water and with it the dissolution rate. The N3 capsules, which had the highest content of SSG, 13% (w/w), complied with the pharmacopoeial specification for dissolution tests and the comparative tests of dissolution profiles showed that the N3 capsules exhibited rapid dissolution and an in vitro dissolution profile similar to that of the reference drug. Thus, the N3 capsules can be considered as a pharmaceutical alternative to the reference drug.

O presente trabalho avaliou a influência do Amido Glicolato de Sódio (AGS) na dissolução da nimesulida veiculada em cápsulas gelatinosas duras. Para tanto, foram caracterizados alguns parâmetros físico-químicos da nimesulida; e formulações, contendo diferentes concentrações de AGS, foram preparadas para compor as cápsulas gelatinosas duras de nimesulida. As cápsulas obtidas, bem como o medicamento referência, foram submetidos aos ensaios de dissolução in vitro. Determinou-se, para o tempo de dissolução máximo farmacopeico, a quantidade da substância ativa dissolvida, bem como traçou o perfil de dissolução a partir da quantidade de substância dissolvida em cada intervalo de tempo. A comparação dos perfis de dissolução foi realizada pelo Método Modelo Independente Simples, pela avaliação estatística dos dados dos perfis de dissolução para cada intervalo de tempo e pela Eficiência de Dissolução (ED). Os resultados mostram que o AGS, utilizado como desintegrante, tem características que interferem positivamente na dissolução da nimesulida, facilitando a desintegração da forma farmacêutica, aumentando a superfície de contato do ativo com a água e, com isso, a velocidade de dissolução. As cápsulas N3, que possuem 13% (p/p) de AGS, cumprem com as especificações farmacopeicas para os testes de dissolução, e ensaios comparativos de perfis de dissolução mostram que as cápsulas N3 apresentam dissolução rápida e perfil de dissolução in vitro semelhante ao medicamento referência. Logo, as cápsulas N3 podem ser consideradas como alternativas farmacêuticas aos comprimidos referência.

Formulation and Characterization of Fast Disintegrating tablets of Amlodipine using Super-disintegrants.

Amlodipine besylate is a long‐acting calcium channel blocker used to treat chronic stable angina, vasospastic angina and hypertension. Amlodipine is a sparingly soluble orally administered drug and the rate of absorption is often controlled by the rate of dissolution. The rate of dissolution will increase by incorporating the drug in a fast dissolving dosage form. An attempt will be made to develop rapidly disintegrating oral tablets of Amlodipine Besylate by direct compression method. In this study, Fast Dissolving Tablet (FDT) was prepared using direct compression method using Crospovidone and Sodium starch glycolate as the super disintegrants. Amongst all formulations, formulation F3 prepared by a combination of both Crospovidone and Sodium starch glycolate showed least disintegrating time, and faster dissolution of 87%. Combination of super disintegrants were found to be better to formulate fast dissolving tablets of Amlodipine besylate.

Effect of superdisintegrants on formulation of taste masked fast disintegrating Ciprofloxacin tablets.

The present investigation deals with the formulation of taste masked fast disintegrating tablets of Ciprofloxacin that disintegrate in the oral cavity upon contact with saliva and thereby improve therapeutic efficacy. Ciprofloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial that kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and protein. It may also be used to prevent or slow anthrax after exposure. The influence of superdisintegrants, crospovidone and sodium starch glycolate on disintegration time, wetting time and water absorp-tion ratio were studied. Tablets were evaluation for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disinte-gration tablets was found to be within 36 seconds. Tablets containing crospovidone (40%) exhibits quick disintegration time than tablets containing sodium starch glycolate. The fast disintegrating tablets of ciprofloxacin with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.

Effect of superdisintegrants on formulation of taste masked fast disintegrating Ciprofloxacin tablets.

The present investigation deals with the formulation of taste masked fast disintegrating tablets of Ciprofloxacin that disintegrate in the oral cavity upon contact with saliva and thereby improve therapeutic efficacy. Ciprofloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial that kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and protein. It may also be used to prevent or slow anthrax after exposure. The influence of superdisintegrants, crospovidone and sodium starch glycolate on disintegration time, wetting time and water absorp-tion ratio were studied. Tablets were evaluation for weight and thickness variation, disintegration time, drug content, in vitro dissolution, wetting time and water absorption ratio. The in vitro disintegration time of the best fast disinte-gration tablets was found to be within 36 seconds. Tablets containing crospovidone (40%) exhibits quick disintegration time than tablets containing sodium starch glycolate. The fast disintegrating tablets of ciprofloxacin with shorter disintegration time, acceptable taste and sufficient hardness could be prepared using crospovidone and other excipients at optimum concentration.

Formulation and Evaluation of Oral disintegrated tablets of Alfuzosin Hydrochloride using superdisintegrants.

In the present work, orodispersible tablets of Alfuzosin Hcl were prepared by direct compression and sublimation methods with a view to enhance patient compliance. In these methods, varying concentrations of crospovidone, sodium starch glycolate and croscarmellose sodium of 3.3, 6.6 and 10% w/w were used, along with camphor used as subliming agent in sublimation method. The prepared batches of tablets were evaluated for hardness, friability, drug content, wetting time, dispersion time, disintegration time and dissolution studies. Based on disintegration time (approximately 13-18 seconds) all the promising formulations (from each method) were tested for in-vitro drug release pattern (in pH 6.8 phosphate buffer), drug-excipient interaction (FTIR spectroscopy) and short term stability studies. Among the promising formulations, the formulation F4 and F14 containing 10% w/w Crospovidone emerged as the overall best formulation (t50%1.79 and 1.21 minutes) based on drug release characteristic (in pH 6.8 phosphate buffer) compared to controlled formulation F1 (t50% >10 minutes).

First step in the assessment of mechanical properties of pure API: production of tablet with minimum addition of excipient.

There are a number of challenges during tablet dosage form development like excipient selection, poor powder flow, poor tableting, lack of hardness, high friability, elevated disintegration time, low dissolution rate etc. Most of them are significantly influenced by the mechanical properties (like elasticity, plasticity, brittleness, powder compressibility, tensile strength, etc.) of the active pharmaceutical ingredient (API). Assessment of these properties of the pure actives is not always easy. Absence of lubrication may induce a lot of friction, causing capping, lamination or sticking or in many cases, combination of them, damaging the test tablet when taken out. Different approaches were studied to overcome this problem and a solution was found by compaction of a tablet of Sodium Starch Glycolate-Magnesium Stearate in a ratio of 2.75:1 before compressing each tablet of pure API.

Formulation and evaluation of fast dissolving tablets of granisetron hydrochloride.

Fast dissolving drug delivery systems offers a solution for those patients having difficulty in swallowing tablets/capsules etc. Granisetron hydrochloride was selected as the model drug. In the present study, an attempt had been made to prepare fast dissolving tablets of the drug using , plantago ovata mucilage and sodium starch glycolate as super disintegrants (2.5 to 10 % w/w) following by direct compression method. Formulations were evaluated for precompressional parameters such as angle of repose, carr’s compressibility index and hausner’s ratio. The tablets were evaluated for uniformity of weight, thickness, hardness, friability, drug content, wetting time, in-vitro dispersion time and in-vitro dissolution study. The prepared tablets were characterized by FTIR studies. No chemical interaction between drug and exciepients was confirmed by FTIR studies.

Superdisintegrant Selection for Tramadol Dispersible Tablets

The selection of a suitable superdisintegrant for a rapidly disintegrating dosage form is of the utmost importance, since disintegration time (DT) is a critical parameter. An experimental design was implemented, to find out the effects of superdisintegrants (sodium starch glycolate, crospovidone, croscarmellose sodium and methacrylic copolymer with divinyl benzene), at 2, 4, 6% w/w, on tablet hardness, with respect to DT. Methacrylic copolymer with divinyl benzene (at 4 wt%) was selected as the best superdisintegrant, adequate for the formulation of dispersible Tramadol tablets. With increasing hardness, there was a considerable increase in DT at all concentrations of superdisintegrants. A combination of crospovidone and methacrylic copolymer with divinyl benzene showed a remarkable drop in DT to 0.33 min. The stability of the batch with lowest DT was also tested under various conditions and the results suggested that there was no degradation over the test period.