Design and characterization of intra-oral fast dissolving tablets containing diacerein-solid dispersion

Diacerein (Diacetylrhein, DCN) is anthraquinone derivatives used in the curing of osteoarthritis, but its usage isrestricted due to its very poor solubility and wettability which result in bioavailability variation. The objective ofthis work was to design fast dissolving tablets (FDTs) of DCN solid dispersion. Solid dispersions (SDs) and physicalmixtures (PMs) were prepared with PEG4000, Polyvinylpyrolidone K25 (PVPK25), and Sorbitol. SD formationincreased the dissolution rate of DCN compared to PM; this demonstrates that the improvement of dissolution ratewith SD can be due to physical change in drug crystal which was confirmed by thermal analysis. SD with Sorbitol wasselected for the preparations of FDTs. Seven formulations were prepared by direct compression method using differentconcentrations of crospovidone (CP) as superdisintegrant and camphor as subliming agent. Pre- and post-compressionevaluation were carried for powder blend and the prepared FDTs, respectively. F7 (composed of 120 mg CP, 45 mgcamphor, 200 mg SD containing 50 mg DCN, 7.5 mg aspartame, 2.5 mg menthol, 2.5 mg Magnesium stearate, and22.5 mg lactose) showed the shortest disintegration time and the highest dissolution rate and it was selected for furtherinvestigation. Kinetic studies of the in vitro release results showed that F7 followed first-order kinetics. Stabilitystudies conducted for formula F7 showed good stability upon storage at 30oC/75% RH and 40oC/75% RH for 12 weeks.

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).

Development of fast dissolving tablets of flurbiprofen by sublimation method and its in vitro evaluation

Flurbiprofen belongs to Biopharmaceutical Classification System (BCS) class II drugs which are poorly soluble in water. The objective of present research work was to prepare fast dissolving tablets of Flurbiprofen using varying concentrations of three different sublimating agents to improve the dissolution rate. Seven formulations were prepared containing different concentrations of camphor, ammonium bicarbonate and thymol as sublimating agent along with primogel as a superdisintegrant. Tablets were manufactured by direct compression method. The prepared tablets were evaluated for pre-compression and post-compression parameters result, For all formulations result was within official limits. FTIR studies revealed that there were no interactions between the drug and the excipients used. From in vitro drug release studies it was concluded that the formulations F6 and F7 containing 10% and 15% of thymol showed fast drug release of 100.00% and 100.84% respectively in 30 minutes. Formulations containing camphor (F2 & F3) and ammonium bicarbonate (F4 & F5) as sublimating agents showed a drug release of less than 80%, while the control formulation F1 having no sublimating agent showed 49.14% of drug release in 30 minutes. Thus thymol can successfully be used to formulate fast dissolving tablets of flurbiprofen by sublimation method with much better dissolution profile

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.

Formulation and evaluation of fast dissolving tablets of metoclopramide hydrochloride using natural sweetening agent of stevia leaf powder.

Taste masking becomes a pre-requisite for bitter drugs to improve the patient compliance especially in the pediatric and geriatric population. Metoclopramide hydrochloride is recommended in dose of 10 to 15 mg four times a day for getting relief from nausea, vomiting, stomach pain and reflux oesophagitis. It finds application in all the categories of patients.In the present study an attempt has been made to prepare bitterless fast dissolving tablet of Metoclopramide Hydrochloride using stevia leaf powder as a taste masking agent. Direct compression was the technique used for preparing taste masked tablets.

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.

Design and development of levofloxacin hemihydrate fast dissolving tablets using fenugreek powder.

Levofloxacin hemihydrate is an antibiotic used for bacterial infections. It belongs to flouroquinolones class. Fast dissolving tablets gaining popularity over conventional tablets due to their convenience in administration and suitability for patients like geriatrics and pediatric patients because of their swallowing difficulties. The half-life of the drug is 6-8 hrs and it is rapidly and completely absorbed after oral use for that levofloxacin prepared as fast dissolving tablets. Tablets were prepared by direct compression technique by using MCC as binder. Super disintegrants used are SSG(2%,3%,4% and 5%),CCS(AC-DI-SOL) (2%,3%,4%and 5%), CP(2%,3%,4%and5%)and FGP(2%,3%,4%and 5%),.Among these 4 super disintegrants, Fenugreek powder (FGP) was show best results in the evaluation tests.

Solubility enhancement, physicochemical characterization and formulation of fast-dissolving tablet of nifedipine-betacyclodextrin complexes

The main objective of the study was to enhance the dissolution of nifedipine, a poorly water soluble drug by betacyclodextrin complexation and to study the effect of the preparation method on the in vitro dissolution profile. The stoichiometric ratio determined by phase solubility analysis for inclusion complexation of nifedipine with β-cyclodextrin was 1:1. Binary complex was prepared by different methods and was further characterized using XRD, DSC and FT-IR. A saturation solubility study was carried out to evaluate the increase in solubility of nifedipine. The optimized complex was formulated into fast-dissolving tablets by using the superdisintegrants Doshion P544, pregelatinized starch, crospovidone, sodium starch glycolate and croscarmellose sodium by direct compression. Tablets were evaluated for friability, hardness, weight variation, disintegration and in vitro dissolution. Tablets showed an enhanced dissolution rate compared to pure nifedipine.

Este estudo teve por objetivo principal incrementar a dissolução do nifedipino, fármaco pouco solúvel em água, por meio de sua complexação com β-ciclodextrina e estudar o efeito do método de preparação sobre o perfil de dissolução in vitro. A razão estequiométrica, determinada por ensaio de solubilidade de fase, para a complexação de nifedipino por inclusão em β-ciclodextrina foi 1:1. O complexo binário foi preparado por diferentes métodos, sendo caracterizado utilizando-se difratometria de raios X (XRD), calorimetria diferencial de varredura (DSC) e espectroscopia no infravermelho com transformada de Fourier (FT-IR). Realizou-se estudo de solubilidade de saturação para avaliar o incremento da solubilidade do nifedipino. O complexo otimizado foi formulado em comprimidos de dissolução rápida preparados por compressão direta, nos quais se utilizaram os superdesintegrantes Doshion P544, amido pré-gelatinizado, crospovidona, amidoglicolato de sódio e croscarmelose sódica. Os comprimidos, que foram avaliados quanto à friabilidade, dureza, variação de peso, desintegração e dissolução in vitro, apresentaram taxa de dissolução superior à do nifedipino pura.