Disintegrant In Tablet Formulations Research Articles

Isolation, Characterization of Banana Starch and its Evaluation as a Disintegrating Agent in Dispersible Lornoxicam Tablet

Objective: The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation. Methods: The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch. Results: Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia. Conclusion: From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.

Formulation Study of a Co-Processed, Rice Starch-Based, All-in-One Excipient for Direct Compression Using the SeDeM-ODT Expert System.

A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets.

Exploration of Elephant Foot Yam (Amorphophallus paeoniifolius) Starch: An Alternative Natural Disintegrant for Pharmaceutical Application

Abstract: Aim and Objectives: The aim of the current study is to isolate the starch from elephant foot yam (Amorphophallus paeonifolius) and investigate its potential as a disintegrant in tablet formulation as compare to standard corn starch. The objective of the study is to explore the applications of natural resources and develop an alternative to commercially available starches. Materials and Methods: Starch was isolated by a simple method, evaluated for phytochemical and physico-chemical properties. Tablets were prepared by wet granulation by varying concentrations of elephant foot yam or corn starch in the range of 2.5%, 5%, 7.5% and 10%. Further granules were evaluated for flow properties and tablets were evaluated for post-compression parameters. Results: It was found that the pH of the isolated starch sample was found to be neutral; it exhibited good swelling capacity and fair flow properties. P-XRD pattern showed a C-type diffraction pattern, SEM studies indicated that starch granules had a smooth surface. Granules possessed good flow properties and tablets complied with standard limits of weight variation. Hardness and friability were found in the range of 4.11-4.69 kg/cm2 and 0.11-0.50% respectively. The wetting time was found in the range of 7 to 35 sec for elephant foot yam starch and 16-49 sec for corn starch. Disintegration time for elephant foot yam starch was found to be 28 to 84 sec and for corn starch, it was 40 to 90 sec. Conclusion: Formulations containing elephant foot yam starch showed a similar dissolution profile as that of corn starch. Stability studies were performed on F4 batch and it was found stable for three months. Key words: Elephant foot yam, Corn starch, Disintegrant, Fast Disintegrating tablet, Disintegration time, Wetting time.

Effect of Extracted Microcrystalline Cellulose from Dracaenea arborea Stem on Aceclophenac Tablet Formulation

Micro crystalline cellulose (MCC) is a major derivative from the bio composite of natural materials such as D. arborea plant stem. It could be useful as a secondary binder and disintegrant in tablet formulation especially following direct compression technique anticipating it to provide high level of disintegration at low use level and utilizing dual mechanisms of wicking and swelling. Tablets of aceclofenac a BCS class II and non steroidal anti inflammatory drug (NSAID) which potently inhibits the cyclo oxygenase enzyme (COX-2) involved in prostaglandin synthesis was formulated by direct compression using MCC from D. arborea stem. Qualitative assessment of the plant extract was carried out and the presence of cellulose confirmed by the appearance of violet – blue coloration while the physicochemical and physicotechnical properties were comparatively evaluated with reference to avicel and corn starch. Three batches of aceclofenac tablets involving Batch A (D. arborea MCC), Batch B (Corn starch) and Batch C (Corn starch and D. arborea MCC in a 1:1 ratio), were implcated in the formulation. Physicochemical study of the MCC reveals a pH of 7.8, mean swelling index 1.14±0.05 ml and hydration capacity of 3.60±0.15 g while the pH of corn starch is 3.90 with swelling and hydration capacity at 5.09±0.03 ml and 8.26±0.01 g respectively. Quality control evaluation of resulting tablet was investigated and the wetting time of batch A tablets was 1.50, batch B 2.30 and batch C 1.80 with percentage moisture content (%) of 60.5, 56.56 and 57.8 and disintegration time (minutes) of 0.22±0.07, 0.35±0.051 and 1.60±0.286 respectively. The drug release profile of batch A, reveals an initial burst release within 10 minutes followed by gradual release while batch C had consistent drug release which was maintained although faster than that of batch A after 10 minutes but batch B had the least drug release rate.

Design, optimization and evaluation of telmisartan chronotherapeutics press coated tablets employing as novel synthetic disintegrate and as novel coated Chronotherapeutic polymers

Starch Glutarate prepared by reacting potato starch with Glutaric acid at elevated temperatures was found to be a white, crystalline powder. Starch glutarate prepared exhibited excellent flow characteristics it was insoluble in water and aqueous fluids of acidic and alkaline buffers. It also exhibited good swelling (70%) in water. It has no gelling property when heated at 100Co in water for 30 min. It is considered as a promising disintegrant in tablet formulations and was evaluated as disintegrant in tablet formulations. Tablets of Telmisartan were prepared by direct compression method employing starch glutarate at 0–10% as novel super disintegrate and were evaluated. In the present research work, 23 factorial design was used for optimization of level of independent variables (starch glutarate, sodium starch glycolate and croscarmellose sodium) on dependent variables (disintegration time, water absorption, wetting time and percent released in 5 minutes) in the formulations. The optimized formula was further press coated by synthetic controlled time released polymers such as starch acetate, starch succinate in varying ratios. The best formulation was selected based on post-compression parameters and dissolution data was subjected to accelerated stability studies for 3 month. Amongst 5 formulations prepared for coating tablets we are F2CC1 produced convincing results with a maximum cumulative drug release of 99.21%. in 8 hr. By virtue of its release pattern and delivering the drug at the right time, right place and in right amounts, the developed delivery system holds good promises of benefiting the patients suffering from hypertension.

In Vitro Evaluation of Native Taro Boloso‐I Starch as a Disintegrant in Tablet Formulations

Introduction. In drug delivery, solid dosage forms, of which tablet is the commonest, are still the leading preferences. An area of research focus in tablet drug delivery is the search for tablet excipients. This study was aimed at evaluating and optimizing native Taro Boloso‐I starch as a tablet disintegrant. Methods. The response surface method with central composite design (CCD‐RSM) was used for the analysis and optimization of the concentration of native Taro Boloso‐I starch and compression force. Wet granulation method was used for the preparation of paracetamol tablets. The response variables considered were tablet crushing strength, friability, and disintegration time. Results and Discussion. Both the native Taro Boloso‐I starch concentration and compression force had increasing effect on the tablet breaking force. The friability of the tablets was shown to decrease with increasing levels of the disintegrant concentration. On the other hand, compression force had a decreasing effect on friability in the investigated range. The disintegration time of the tablets was found to decrease with the concentration of the starch. The paracetamol tablets prepared with the optimized levels of native Taro Boloso‐I starch and compression force showed tablet breaking force of 116.24 N, friability of 0.153%, disintegration time of 1.36 min, disintegration efficiency ratio of 562.3 N/(%Min), and comparative disintegration efficiency ratio of 13.6 with respect to commercial potato starch. Conclusions. The tablets exhibited improved crushing strength, friability, in vitro disintegration time, and disintegration efficiency ratio which suggest the novel applicability of the native Taro Boloso‐I starch as an efficient pharmaceutical tablet disintegrant.

Evaluation of Microcrystalline Cellulose Derived from Saccharum officinarum L. (Sugarcane) Leaves as a Disintegrant in Tablet Formulations.

Purpose: Complete recycling of the crop residues of sugarcane in the Philippines remains to be achieved. This study purposed to derive microcrystalline cellulose (MCC) from sugarcane leaves and test its disintegrating properties in tablet formulation. Methods: Saccharum officinarum L. (sugarcane) leaves were used to prepare MCC powder. According to the conventional method, the preparation of cellulose powder requires heating the raw material with acid and alkali followed by washing, bleaching, and sieving. Hydrolysis of the bleached product was carried out using hydrochloric acid to obtain MCC powder, and the physicochemical properties of the produced MCC powder were studied including its organoleptic properties, pH value, %loss on drying, %water soluble substances and Fouriertransform infrared (FTIR) spectrum. Results: The resulting powder was evaluated for its disintegrating property in the preparation of blank tablets, which were compared to tablets prepared using commercially available MCC. MCC powder derived from sugarcane leaves had properties at par with commercially available MCC and was in conformance with National Formulary (NF) specifications. Conclusion: Disintegrating properties were also significantly better than the commercially available MCC.

Characterization Sodium Carboxymethyl Cellulose from Alpha Cellulose Betung Bamboo (Dendrocalamus asper)

Objective: Sodium carboxymethylcellulose (Na-CMC) is one of pharmaceutical excipients that can be used to increase viscosity in topical, oral and parenteral pharmaceutical formulation, beside that it can also be used as binder and disintegrant in tablet formulation. Betung bamboo is one of natural material that contains high concentration of holocellulose for about 83.80%. The purpose of this study was to characterize Na-CMC obtained through alkalization and carboxymethylation reaction. Methods: Alkalization was carried out using 25% sodium hydroxide and 1.7% sodium tetraborate. Carboxymethylation was done with sodium monochloroacetate to alpha cellulose ratio 1.3 : 1. Product was identified by FTIR and further characterized by XRD, SEM, DS value and pH. Result: The product was white colour powder which has similarities of its infrared spectrum to reference. Other characteristics that showed similarities to reference was degree of substitution 0.7073, pH 7.61, average of particle size distribution 71.54 μm, moisture content 5.88%, sulfated ash content 32.64% and loss on drying 9.85%. Conclusion: Based on the comparison of X-ray diffraction, there is similarity between reference and product (Na-CMC) from betung bamboo. However, there were differences in melting temperature, viscosity and morphological analysis with SEM to reference.

Investigation of α-Cellulose Content of Sugarcane Scrappings and Bagasse as Tablet Disintegrant

The aim of this study is to investigate the physicochemical and disintegrant properties of α – cellulose obtained from sugarcane scrapings and bagasse. The mechanical and release properties of paracetamol tablets containing the extracted celluloses and two standard disintegrants- corn starch B.P and microcrystalline cellulose – were determined using crushing strength, friability, disintegration time, the time taken for 50% (T50) and 90% (T90) drug dissolution as assessment parameter. α – cellulose obtained from sugarcane scrapings and bagasse possess better flow properties than cornstarch and microcrystalline cellulose and are capable of absorbing up to five times their own weight in water and swell considerably. α – cellulose obtained from sugarcane scrapings and bagasse have high moisture sorption capacity and they formed relatively softer tablets which became increasingly harder as their concentration increased. All the tablets formulated with cellulose derived from sugarcane scrapings and bagasse passed the official disintegration test for uncoated tablets. Cellulose obtained from sugarcane bagasse had superior disintegrant property to cornstarch and microcrystalline cellulose while cellulose obtained from sugarcane scrapings showed comparable disintegrant property to microcrystalline cellulose. Tablets containing 2.5% w/w cellulose derived from sugarcane scrapings and 5.0% w/w cellulose derived from sugarcane bagasse gave more optimum result as tablet disintegrant. Formulations containing cellulose derived from sugarcane scrapings and bagasse show faster drug release (lower T50 and T90) than tablets containing corn starch and microcrystalline cellulose. There was a linear correlation between T90 and disintegration time (r = 0.976, p< 0.05) for tablets formulated with cellulose derived from sugarcane scrapings. Results show that α – cellulose obtained from sugarcane bagasse and scrapings are potentially useful as disintegrants in tablet formulations.

Evaluation of Native and Pregelatinized Arrowroot (Maranta Arundinacea) Starches as Disintegrant in Tablet Formulation

The purpose of this study was to investigate the disintegrating properties of native arrowroot starch and pregelatinized arrowroot starch in comparison with corn starch and sodium starch glycolate (Explotab®). Tablets were prepared by direct compression. The tablet formulations contained dibasic calcium phosphate as filler and magnesium stearate as lubricant. Each starch at various concentrations between 2-10 % w/w was used in formulation as disintegrant. The swelling volume and weight of starches and disintegration time of tablets were evaluated. At 2% w/w concentration of starch, the pregelatinizaed starch provided disintegration time faster than the native starch (2.5 times). The disintegration time of 2% w/w pregelatinized arrowroot starch was comparable to Explotab and faster than that of native starch. The disintegration time of native starch at the concentration of 4, 6 and 10 %w/w was comparable to that of corn starch and Explotab®. Native arrowroot starch and pregelatinized arrowroot starch could be used as effective disintegrants in tablet formulation.

Microwave Assisted Synthesis and Evaluation of Cross-Linked Carboxymethylated Sago Starch as Superdisintegrant

The aim of this study was to modify the sago starch and evaluate its efficacy as tablet disintegrant. Cross-linked car-boxymethylated sago starch (CMSS) was synthesized using native sago starch (SS) and monochloroacetic acid (MCA) with sodium hydroxide in microwave radiation environment. FT-IR analysis of the sample confirmed the carboxy-methylation by showing absorption peak at 1607.2 cm-1. CMSS with degree of substitution (DS) of 0.31 was formed and, it was further evaluated as disintegrant in Ondasetron based tablets. The results revealed that CMSS could be used as disintegrant in tablet formulation in concentration dependant manner.

Evaluation and Optimization of Godare Starch as a Binder and Disintegrant in Tablet Formulations

The binding and disintegrating properties of Godare (Colcosia esculenta) starch in paracetamol tablet formulations were evaluated in comparison with potato starch. Tablet crushing strengths (Hs), friabilities Frs), disintegration times (DTs) and porosities were determined. The results showed that Godare starch has a better binding ability than potato starch giving tablets of higher H, lower Fr and porosity. Its disintegrating efficacy is comparable to that of potato starch. Optimum binder and disintegrant concentration of Godare starch was obtained by employing a 22 factorial design. Statistical analysis showed that as a binder, Godare starch provided paracetamol tablets with desired properties (88.1 N H, 2.69 min DT and 0.74% Fr) when used at 6.3% w/w concentration and compressed at 18.75 KN. As a disintegrant, Godare starch at 7% w/w concentration, provided tablets with a H of 109.1 N, DT of 3.22 min and 0.88% Fr, when the formulation contained povidone as a binder and AC-Di-Sol® as a disintegrant and compressed at 19 KN. Keywords: Godare starch, paracetamol, binders, disintegrants, experimental design Ethiopian Pharmaceutical Journal Vol. 24 (2) 2006: pp.98-105

Some physicochemical properties and application of A. Cellulose from Pennisetum purpureum as a disintegrant in tablet formulation

Some physicochemical properties and application of A. Cellulose from Pennisetum purpureum as a disintegrant in tablet formulation

A combination of vapor sorption and dynamic laser light scattering methods for the determination of the Flory parameter χ and the crosslink density of a powdered polymeric gel

Reliable techniques can be easily used to determine the crosslink density and the Flory interaction parameter of polymeric gels, on condition that monolithic matrices of the crosslinked polymer are available, but they cannot be profitably applied to powdered forms. In the present work we propose an experimental procedure which is particularly suitable to determine the above mentioned parameters in the case of polymeric gel particles. The technique is based on polymer swelling experiments performed in the presence of vapour and liquid external phases, and was applied to four different commercial types of sodium starch glycolate. Such a crosslinked polymer is normally supplied in a powdered form and commonly used in the pharmaceutical field as disintegrant in tablet formulation. For each polymer, the crosslink density ρ x and the Flory interaction parameter χ were calculated from the experimental swelling data by solving the relevant equilibrium equations deriving from the Flory theory for gel/liquid and gel/vapor equilibrium conditions. The crosslink density values were then used to estimate the mesh size of the polymeric networks. Such a parameter is of great interest in the pharmaceutical field since it can play an important role in the performance of drug release systems based on polymeric gel matrices or minimatrices.

Evaluation of sorghum starch as a tablet excipient

AbstractThe suitability of sorghum starch as a binder and disintegrant at various concentrations in diverse tablet formulations have been investigated. Sodium bicarbonate and calcium carbonate were used as soluble and insoluble inorganic medicinal substances in various tablet formulations.The effect of sorghum starch on the physical properties of the tablets were compared with those formulated with maize starch using the same concentrations of binder and disintegrant under the same experimental conditions.The observations show that sorghum starch can be used as binder and disintegrant in tablet formulations. The indication is that the starch exhibit about twice the disintegrant power and about the same binding efficacy compared to maize starch.

An evaluation of starch obtained from pearl millet - Pennisetum typhoides. As a binder and disintegrant for compressed tablets

AbstractThe binding and disintegrant properties of millet starch obtained from Pearl Millet - Pennisteum typhoides (Staph. Burn, and Hubb.) Fam. Gramineae have been evaluated using tablet formulations of four drugs.The results showed that Millet starch compared favourably with Maize starch with regards to most of the parameters used to evaluate the tablets. It can be safely concluded that millet starch is suitable for use as a binder and disintegrant in tablet formulations.

On the Similarity of Sodium Starch Glycolate from Different Sources

AbstractThe physico-pharmaceutical properties of different batches of two brands of sodium starch glycolate have been investigated as disintegrant in direct compression. Differences in disintegration efficiency were found to be related to the purity of the products. The differences, however, were too small to have practical significance. The currently available low-sodium chloride content sodium starch glycolates may consequently be considered as being pharmaceutically equivalent, when used as disintegrant in tablet formulations.