Natural Superdisintegrant Research Articles

Formulation and Evaluation of Fast Dissolving Tablets of Cefixime Trihydrate

Fast Dissolving Tablet instead of dissolving or disintegrating in water is expected to dissolve or disintegrate in oral cavity without drinking water. Super disintegrates are added to a drug formulation to facilitate the break-up or disintegration of tablet or capsule content into smaller particles that can dissolve more rapidly than in the absence of disintegrates In the present study, the effects of a natural superdisintegrants Plantago ovata, Hibiscus rosa sinensis and synthetic superdisintegrants like sodium starch glycolate (SSG), Crosspovidone and Croscarmellose sodium (Ac-di-sol) were compared in the formulations of fast dissolving tablets (FDT). FDTs of Cefixime were prepared by direct compression method and were evaluated for weight variation, hardness, thickness, disintegration time, wetting time, water absorption ratio, In vitro dispersion, friability and dissolution. Among all the super disintegrates, Plantago ovata showed the highest swelling index and natural super disintegrates like husk of Plantago ovata showed better disintegrating property than the most widely used synthetic super disintegrates like AC-di-Sol, C.P and SSG in the formulations.

In vitro‐in vivo performance evaluation of treated Plantago ovata husk based fast dissolving tablets of glipizide: Flashtab technology

Physicians suggest premeal administration of glipizide (30 min before a meal) because of longer disintegration time (approximately 15 min) of conventional tablet. Hence, the dosage form was developed, called as fast dissolving tablet (FDT), which disintegrates rapidly within a minute. FDTs by Flashtab technology is based on a swellable agent and a superdisintegrant. In the current study, treated Plantago ovata husk (TPOH), and microcrystalline cellulose were utilized as natural superdisintegrant and swellable agent, respectively. FDT formulations were prepared by direct compression and evaluated for in vitro tablet performance, such as disintegration time, wetting time, hardness, friability, swelling and percent drug release. On the basis of finding, formulation with 15% TPOH concentration (TPOH 7) was selected as optimized formulation. To evaluate the in vitro performance, the formulation TPOH 7 and the marketed tablets (glynase) were administered to rabbits. In the case of marketed tablet, the peak plasma‐concentration of glipizide was obtained in 2.83 h of administration whereas it was 2 h for TPOH 7 indicating immediate absorption and therefore faster onset of action of the prepared FDT formulation than the marketed one. Drug interaction studies, performed by using FTIR spectroscopy, X‐ray diffractometry and differential scanning calorimetric methods, indicate that the glipizide is compatible with the formulation components. The accelerated stability study (40°C ± 2°C/75% ±5% relative humidity) for the optimized formulation showed a negligible change over time for the in vitro parameters. The results suggest that TPOH has promising potential for faster disintegration and fulfills the requirement of FDTs. Key words: Direct compression, fast dissolving tablets, flashtab technology, glipizide, Plantago ovata husk, superdisintegrant

Formulation development and optimization of fast dissolving tablets of aceclofenac using natural superdisintegrant.

The current research work involves preparation of fast dissolving tablets of Aceclofenac by direct compression method using different concentrations of Lepidium sativum mucilage as natural superdisintegrant. A two-factor three-level (32) factorial design is being used to optimize the formulation. Nine formulation batches (D1–D9) were prepared accordingly. Two factors as independent variables (X 1-amount of β-cyclodextrin and X 2-amount of Lepidium sativum mucilage) were taken with three levels (+1, 0, −1). The levels of two factors were selected on the basis of preliminary experiments conducted and their effect on three dependent variables (disintegration time, wetting time, and in vitro drug release) was studied along with their % prediction error. All the active blends were evaluated for postcompression parameters (angle of repose, Carr's index, Hausner ratio, etc.) and the tablets were evaluated for postcompression parameters (weight variation, hardness, and friability, wetting time, disintegration time, water absorption ratio, and in vitro drug release studies). The optimum batch was further used for SEM and stability studies. Formulation D5 was selected by the Design-Expert software which exhibited DT (15.5 sec), WT (18.94 sec), and in vitro drug release (100%) within 15 minutes.

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

To formulate diclofenac sodium as fast dissolving tablets (FDTs) using fenugreek gum as a natural superdisintegrant which also possess anti-inflammatory activity. 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. 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. 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 and evaluation of orally disintegrating tablets of captopril using natural super disintegrants

Formulation and evaluation of orally disintegrating tablets of captopril using natural super disintegrants

Formulation and Evaluation of Orodispersible Tablets of Clonazepam using Natural Superdisintegrants

Present study is aimed at the development of oro-dispersible tablets of clonazepam using natural superdisintegrants. Mucilage of Hibiscus rosa sinensis leaf and seeds of Ocimum basilicum were extracted, evaluated for the organoleptic, physicochemical parameters. The dried mucilage was used as superdisintegrant for the preparation of orodispersible tablets by direct compression method. The blends were evaluated for the pre-compression parameters and all the formulations were found to possess good flow properties. Tablets were compressed by direct compression technique, evaluated for weight variation, hardness, thickness, friability, water absorption, disintegration time, dispersion time, drug content and dissolution studies. The drug release profiles of the two superdisintegrants were compared. The optimized formula F10 was subjected to wet granulation using PVP in IPA as the dry binder. The tablets containing 5%w/w dried mucilage of Ocimum basilicum as superdisintegrant prepared by direct compression technique was found to be the best which disintegrated in 22 sec. with 99.8%drug release. The tablets were found to be stable during the accelerated stability studies conducted for three months at 40±2 0 C/75±5% RH.

Preparation and evaluation of sublingual tablets of zolmitriptan

Aim:Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan.Materials and Methods:Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline.Results:The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline.Conclusion:The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action.

Development and Optimization of Fast Dissolving Tablets of Losartan Potassium Using Natural Gum Mucilage

Current research work involves preparation of fast dissolving tablets of Losartan Potassium by direct compression method using different concentrations of Plantago ovata and Lepidium sativum mucilage as natural superdisintegrants. A two factor three level (32) factorial design is being used to optimize the formulation. Nine formulation batches (A1-A9) were prepared by taking two factors as independent variables (X1- amount of Plantago ovata mucilage and X2- amount of Lepidium sativum mucilage) were taken with three levels (+1, 0, -1). All the active blends were evaluated for precompression parameters (angle of repose, bulk density, carr’s index, hausner’s ratio) and formulated tablets were evaluated for post compression parameters (hardness, friability, weight variation, wetting time, disintegration time, water absorption ratio). In vitro drug release studies were carried out using USP II dissolution apparatus for 30 min. The software Design Expert (8.0.7.1) was used for generating experimental design, modeling the response surface and calculating the statistical evaluation. Tablet parametric tests of formulation batches (A1-A9) of FDT were found within prescribed limits. DT was observed in the range from 12±2 to 58.7±2.52 sec and WT from 10.3±1.52 to 49.7±5.13 sec for formulation batches (A1-A9). More than 87% drug release was observed in all formulation batches (A1-A9) within 15 minutes. Polynomial mathematical models, generated for various response variables using multiple linear regression analysis, were found to be statistically significant (P < 0.05). Formulation A7 was selected by the design expert software which exhibited DT (22.15sec), WT (17.31sec) and in vitro drug release (100%) within 15 minutes.

COMPARATIVE EVALUATION OF NATURAL AND SYNTHETIC SUPERDISINTEGRANTS FOR FAST DISSOLVING TABLET

In the present study, fast dissolving tablets of Salbutamol sulphate were prepared by direct compression method for better patient compliance and immediate action in asthma. The tablets were prepared by using synthetic superdisintegrants (Croscarmellose sodium and Sodium starch glycolate) and natural superdisintegrant (mucilage of Plantago ovata and Plantago ovata husk powder) at different concentrations as 2, 4, 6, 8 and 10 %. The Plantago ovata mucilage was extracted from the seeds of Plantago ovata (Plantaginaceae).The tablets were characterized for weight variation, hardness, friability, disintegration time, wetting time, water absorption ratio, drug content and in vitro dissolution tests. The Drug excipients compatibility study was performed by DSC and IR spectroscopy and no incompatibility was found. The tablets were subjected for accelerated stability study at 40°C /75% RH and were found to be stable. The results clearly shows Natural superdisintegrants requires less disintegration time as compared to synthetic superdisintegrants. Hence present study reveals that the fast dissolving tablets prepared by using mucilage of Plantago ovata and husk powder of Plantago ovata as superdisintegrants having better appearance and rapid disintegration time. Key-words: Fast dissolving tablets, Superdisintegrants, Plantago ovata, Croscarmellose sodium and Sodium starch glycolate.

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF PERINDOPRIL ERBUMINE USING NATURAL SUPERDISINTEGRANT

Oral disintegrating tablets are emerging trend in Novel drug delivery system & received increasing demand & popularity due to ease of administration & better patient compliance .In recent years superdisintegrant have been employed to develop effectual mouth dissolving tablet & to overcome limitation of conventional tablets .In present study attempt was made to compare to disintegrating efficiency of natural superdisintegrats .Main aim of using oscimum basilicum as natural superdisintegrant was to achieve quick onset of action ,increases water uptake with short wetting time & decreasing disintegration time by cost effective direct compression method. 3 preliminary batches were prepared & these are evaluated for precompression parameter like angle of repose, carr`s index & post compression parameters like wetting time, water absorption ratio,in vitro disintegration. Hardness, friability of all formulations found within limit. Best formulation F2 batch had shown good hardness, friability, disintegration time, swelling time. Present study revealed that mucilage obtained from oscimum basilicum was effective for their disintegrating property.

EMERGENCE OF NATURAL SUPER-DISINTEGRNATS IN ORO-DISPERSIBLE TABLETS: AN OVERVIEW

Orally disintegrating tablets (ODTs) are an emerging trend in novel drug delivery system and have received ever - increasing deman d during the last few decades. ODTs are solid unit dosage forms, which disintegrates or dissolves rapidly in the mouth without chewing and water. This type of property in dosage form can be attain ed by addition of different excipients, in which disintegrants are the key adjuvant. In recent years, several newer agents have been developed known as super - disintegrants. Super - disintegrants are used to improve the efficacy of solid dosage form and influ ence the release rate of dosage for m. Diverse categories of super - d isintegrants are such as synthetic, semi - synthetic, natu ral and co - processed blends etc. These h ave been employed to develop effect ual ODTs and to overcome the limitations of con ventional t ablet dosage forms. The plant derived natural super disintegrants comply with many requirements of pharmaceutical excipients as they are non - toxic, stable, easily available, associated with less regulatory issues as compared to their synthetic counterpart and inexpensive; also these can be easily modified in to more polar form . This review discuss about the development of various kind of natural super - disintegrating agent s , along with their role in the tablet disintegration and as potent candidate to b e used in ODTs , w hich are being used in the formulation to provide the safer, effective drug delivery with patient compliance.

FORMULATION AND EVALUATION OF SOLUBILITY ENHANCED FAST DISINTEGRATING TABLETS OF TELMISARTAN USING NATURAL SUPERDISINTIGRANTS

Telmi sartan (TLM) is an angiotensin II receptor antagonist used in the treatment of hypertension. According to biopharmaceutical classification system , telmisartan belongs to class II drug. It is practically insoluble in water and it shows low dissolution profi le and poor absorption. In ord er to improve the solubility and dissolution rate of telmisartan, 6 inclusion complexes were prepared by both physical mixing and kneading methods in 1:1, 1:2 and 1:3 molar ratios of telmisartan and β - cyclodextrin. The complexes were tested for dug content and in - vitro drug release studies. Based on these parameters formulation KM3 was selected as best one for further studies as % drug content was 98.47% and in - vitro drug release was 76.991% in 45min. The tablets were formulated for the inclusion complex KM 3 using two natural super disintegrants gum karaya and soy polysaccharides in three concentrations and were evaluated for % weight variation, hardness and disintegration time and in - vitro drug release studies. The % weight variation range was found to be b etween 508±0.57 to 524±0.34, the hardness range was found to be between 3.4±0.29 to 4.2±0.18 kg/cm2, the disintegration time ranges between 5min 20sec to 7min 25sec, in - vitro drug release shows that as concentration of super disintegrant increases rate of drug release increases. Among all the formulations, F3 shows best result with a disintegration time of 5min 30sec and drug release up to 92.555% in 45min.

RAPID DISSOLVE ORAL DOSAGE FORMS- A DETAIL REVIEW

In the current scenario of novel drug delivery system, much emphasis has been given to effective dosage form in term of producing steady level concentration in plasma for controlled release drug delivery system and rapid release drug for quick effects. In case of allergy, chemotherapeutics side effect treatment, pain medicines and pediatric as well as geriatrics drug delivery prefers rapid response of drug. Numbers of drug from above categories have been formulated in rapid release tablet or film. With the use of natural polymers and superdisintegrants it is feasible to prepare these dosage forms to dissolve within 1min with minimum quantity of water. The aim of present review is to give complete detailed including all formulation aspects and evaluation parameters of rapid dissolve tablets and films. This review is first of its kind, as per our knowledge, which compiles complete information in one article. Rapid dissolve formulation have very high acceptance rate due to patient friendly formulation. Several technologies have been developed and patented. This review also covers patented technology.

Comparative Success of Natural Superdisintegrant over Synthetic Superdisintegrants in Fast Disintegrating Tablets

In the present study, fast disintegrating tablets of Amlodipine Besylate were prepared by direct compression methods for better patient compliance and immediate action in angina. The tablets were prepared by using synthetic superdisintegrants (Crospovidone and Croscarmellose sodium) and natural superdisintegrant (Plantago ovata) at different concentrations. The prepared tablets were evaluated for weight variation, hardness, Friability, disintegration time, wetting time, dispersion test, drug content and in vitro dissolution tests. The tablets were subjected for stability study at 25°C /60% RH and 40°C/ 75% RH. The results clearly shows Natural superdisintegrant (husk of Plantago ovata) requires less disintegration time as compared to synthetic superdisintegrants. Hence present study reveals that the fast disintegrating tablets prepared by using husk of Plantago ovata as superdisintegrants having better appearance and it having rapid disintegration time.

Taste Masked Microspheres of Ofloxacin: Formulation and Evaluation of Orodispersible Tablets

Ofloxacin is a synthetic chemotherapeutic antibiotic used for treatment of a variety of bacterial infections, but therapy suffers from low patients’ compliance due to its unpleasant taste. This study was aimed to develop taste masked microspheres of ofloxacin using Eudragit and to prepare orodispersible tablets of the formulated microspheres using natural superdisintegrant. Taste masking Eudragit E100 microspheres were prepared by solvent evaporation technique with an entrapment efficiency ranging from 69.54 ± 1.98 to 86.52 ± 2.25%. DSC revealed no interaction between the drug and polymer. Microspheres prepared at a drug/polymer ratio of 1:4 and 1:5 revealed sufficient flow properties and better taste masking as compared to other ratios. Drug loaded microspheres were formulated as orodispersible tablets using locust bean gum as a natural superdisintegrant offering the advatages of biocompatibility and biodegrad-ability. The wetting time, water absorption ratio and in-vitro disintegration time of the tablets were found to range between 19 ± 2 to 10 ± 3 seconds, 59.11 ± 0.65 to 85.76 ± 0.96 and 22 ± 2 to 10 ± 2 seconds, respectively. The in-vitro ofloxacin release was about 97.25% within 2h. The results obtained from the study suggested the use of eudragit polymer for preparing ofloxacin loaded microspheres with an aim to mask the bitter taste of the drug and furthermore orodispersible tablets could be formulated using locust bean gum as a natural superdisintegrant.

Lallemantia reylenne seeds as superdisintegrant: Formulation and evaluation of nimesulide orodispersible tablets

Aim:Orodispersible tablets also known as fast dissolving tablets disintegrate instantaneously within the mouth and thus can be consumed without water. The present study was aimed to formulate orodispersible tablets of nimesulide by using Lallemantia reylenne seeds as natural superdisintegrant.Materials and Methods:Powdered lallemantia seeds were characterized for powder flow properties (bulk density, tapped density, carr's consolidation index, hausner ratio, angle of repose), swelling index, viscosity, pH, and loss on drying. The prepared tablets were evaluated for different tablet parametric tests, wetting time, water absorption ratio, effective pore radius, porosity, packing fraction, in vitro and in vivo disintegration time, in vitro dissolution and stability studies.Results and Discussion:Increase in Lallementia reylenne concentration had an appreciable effect on tablet hardness and friability which clearly indicated binding potential of the seeds. Water absorption ratio increased with increase in Lallemantia reylenne concentration from batch A1 to A4. Water uptake coupled natural polymer swelling could be the most probable mechanism for concentration dependent reduction in disintegration time by the Lallemantia reylenne seeds. Porosity of the formulated tablets was found to increase from batch A1-A4. The in vitro disintegration results were in line with in vivo disintegration results.Conclusion:It could be concluded that Lallemantia reylenne seeds could be used as natural superdisintegrant in the formulation of orodispersible tablets.

Comparative study on effect of natural and synthetic superdisintegrants in the formulation of fast dissolving tablets

In the present study, the effects of a natural superdisintegrant vis-a-vis isolated mucilage of Plantago ovata and synthetic superdisintegrants like sodium starch glycolate (SSG) and croscarmellose sodium (Ac-di-sol) were compared in the formulations of fast dissolving tablets (FDT). FDTs of aceclofenac (model drug) were prepared by direct compression method using microcrystalline cellulose as direct compressible vehicle. Th ose tablets were evaluated for weight variation, hardness, disintegration time, drug content, friability and dissolution. Swelling index was also investigated with an aim to compare the swelling property of mucilage of Plantago ovata with SSG and Ac-di-sol. Among all the super disintegrants, Plantago ovata mucilage showed the highest swelling index. Hence, the present study revealed that this natural superdisintegrant (Plantago ovata mucilage) showed better disintegrating property than the most widely used synthetic super disintegrants like SSG and Ac-di-sol in the formulations of FDTs. Key words: Fast dissolving drug delivery, Plantago ovata mucilage, swelling index, sodium starch glycolate, croscarmellose sodium