Formulation Of Orodispersible Tablets Research Articles

Novel Patient-Friendly Orodispersible Formulation of Ivermectin is Associated With Enhanced Palatability, Controlled Absorption, and Less Variability: High Potential for Pediatric Use.

Ivermectin has been used since the 1980s as an anthelmintic and antiectoparasite agent worldwide. Currently, the only available oral formulation is tablets designed for adult patients. A patient-friendly orodispersible tablet formulation designed for pediatric use (CHILD-IVITAB) has been developed and is entering early phase clinical trials. To inform the pediatric program of CHILD-IVITAB, 16 healthy adults were enrolled in a phase I, single-center, open-label, randomized, 2-period, crossover, single-dose trial which aimed to compare palatability, tolerability, and bioavailability and pharmacokinetics of CHILD-IVITAB and their variability against the marketed ivermectin tablets (STROMECTOL) at a single dose of 12 mg in a fasting state. Palatability with CHILD-IVITAB was considerably enhanced as compared to STROMECTOL. Both ivermectin formulations were well tolerated and safe. Relative bioavailability of CHILD-IVITAB compared to STROMECTOL was estimated as the ratios of geometric means for Cmax, AUC 0-∞, and AUC0-last, which were 1.52 [90% CI: 1.13-2.04], 1.27 [0.99-1.62], and 1.29 [1.00-1.66], respectively. Maximum drug concentrations occurred earlier with the CHILD-IVITAB formulation, with a median Tmax at 3.0 h [range 2.0-4.0 h] versus 4.0 h [range 2.0-5.0 h] with STROMECTOL (P =.004). With CHILD-IVITAB, variability in exposure was cut in half (coefficient of variation: 37% vs 70%) compared to STROMECTOL. Consistent with a more controlled absorption process, CHILD-IVITAB was associated with reduced variability in drug exposure as compared to STROMECTOL. Together with a favorable palatability and tolerability profile, these findings motivate for further clinical studies to evaluate benefits of such a patient-friendly ODT formulation in pediatric patients with a parasitic disease, including infants and young children <15 kg.

Formulation, Development and Optimization of Silymarin Loaded Nanoparticle Orodispersible Tablets for its Anti-inflammatory Activity

The objective of this work was to enhance the anti-inflammatory properties of silymarin by developing and refining an orodispersible tablet formulation loaded with nanoparticles. Formulation development and optimization of silymarin-loaded nanoparticle orodispersible tablet for its anti-inflammatory activity is the focus of this research paper. Nanoparticle drug delivery systems can help to overcome these limitations by enhancing solubility and absorption. Disintegration and dissolution of Orodispersible tablets take place in the mouth rapidly without water, providing a faster onset of action. These nanoparticles were then incorporated into orodispersible tablets containing superdisintegrants and sweeteners using direct compression. A Box-Behnken design was utilized to systematically optimize the tablet formulation based on responses including disintegration time, wetting time, hardness and friability. After 15 minutes, SL-NP Formulation -3, which contains 5% crospovidone as a superdisintegrant, demonstrated maximal drug release, or 98.5%. Rats with paw edema caused by carrageenan were used to test the anti-inflammatory potential. Following three hours, the 400 mg/kg dose showed a strong 48% inhibition; the impact grew to 52% after three hours. Overall, the development of silymarin nanoparticle orodispersible tablets shows promise for improving the anti-inflammatory effects of silymarin through a synergistic combination of nanoencapsulation and rapid disintegrating tablet technologies.

Solubility enhancement of etoricoxib using inclusion complexation with cyclodextrins: formulation of oro dispersible tablets by QbD approach

Background: The work was intended to enhance etoricoxib's solubility and dissolution rate and then develop oro-dispersible tablets for faster onset of action. Methodology: Inclusion complexes (ICs) of the drug were obtained with β-cyclodextrin (β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) at ratios of 1:0.125, 1:0.25, 1:0.5, 1:1, and 1:2 (w/w). The selected cyclodextrin at appropriate drug carrier proportion was used to develop oro-dispersible tablets (ODTs) by direct compression, adding crospovidone as a super disintegrant. Phase solubility studies of etoricoxib were carried out by using multiple concentrations of β-cyclodextrin and hydroxypropyl β-cyclodextrin, i.e., 1 %, 2 %, 3 % w/v in distilled water at 37±2°C. Spectroscopic (FT-IR) and thermal analysis (DSC) techniques were employed to identify the drug-carrier interactions. Result: It showed that etoricoxib solubility improves with increasing hydrophilic carrier concentration. The Gibbs free energy values (ΔG˚tr) are consistently negative, showing the solubility of etoricoxib. Significant drug carrier interaction in spectroscopic or thermal analysis was not found. Discussion: The ICs of drugs with β-CD and HP β-CD have successfully addressed the challenges of solubility enhancement and taste masking for etoricoxib. Conclusions: It is observed that the inclusion complexes formed by the kneading method using β-cyclodextrin (β-CD) at a 1:1 ratio and hydroxypropyl β-cyclodextrin (HP β-CD) at a 1:2 ratio can be used to improve dissolution. Hence β-CD (at a 1:1 ratio) is selected for the formulation of oro-dispersible tablets. ODTs offer more patient compliance and an alternative to available conventional tablets.

Bioequivalence and Safety of Bilastine 20 mg Orodispersible Tablets and Conventional Tablets: A Randomized, Single-Dose, Two-Period Crossover Study in Healthy Volunteers Under Fasting Conditions.

Orodispersible tablets (ODT) rapidly dissolve in the oral cavity and can improve patient's convenience. This pharmacokinetic study assessed the bioequivalence of a novel 20 mg ODT formulation of bilastine compared with bilastine 20 mg tablets in healthy volunteers under fasting conditions. A phase I, single-center, open-label, two-period, two-sequence crossover randomized clinical trial was conducted. The study comprised two periods, in which participants were administered a single oral dose of bilastine 20 mg in the form of ODT as the test product, or conventional tablets as the reference product, and a washout of 7 days between each period. Blood samples were collected for up to 72 h. Bioequivalence was established if the 90% confidence intervals of the Cmax and AUC0-t were within the acceptance range (80-125%). Safety was evaluated at the follow-up visit (days 4-7 after the second dose) and throughout the study. A total of 42 healthy volunteers were randomized, and 41 completed the study. Pharmacokinetic parameters were comparable for both formulations after a single dose of 20 mg. Bilastine ODT and conventional tablets were bioequivalent as the 90% confidence intervals of the test over reference ratios were within the predefined range (80-125%). Both formulations were well tolerated and showed a similar safety profile. Bilastine ODT was bioequivalent to the reference treatment formulated as conventional tablets when administered as a single oral dose of 20 mg under fasting conditions. Both formulations showed a similar tolerability and safety profile, with no serious adverse events or significant analytical alterations reported. 2019-004071-39. Date of authorization: 10 December 2019.

Cariprazine Orodispersible Tablet: A New Formulation for Cariprazine.

Cariprazine is an atypical dopamine receptor partial agonist antipsychotic available in the form of capsules. Although capsules are one of the most desirable routes of administration, there are certain situations (e. g., in an acute psychiatric setting, or when swallowing difficulties, or liquid shortages are present) when they cannot be administered. Therefore, alternative solutions like orodispersible tablets are needed. This study aimed to investigate the bioequivalence of a newly developed orodispersible tablet to the commercially available hard gelatine capsule of cariprazine 1.5 mg. This was a phase I, open-label, randomized, single-dose bioequivalence study. It had a 2-period, 2-sequence, cross-over design, where each subject received one test and one reference product in a randomized sequence, separated by a wash-out period of 55 days. Blood sampling was performed over 72 h after dosing. Cariprazine concentrations were analyzed by a validated HPLC-MS/MS method. Standard bioequivalence statistics was applied to PK parameters calculated by non-compartmental analysis. Safety measures were analyzed descriptively. Pharmacokinetic data of 43 healthy volunteers and safety data of 54 subjects was analyzed. Cariprazine AUC0-72h and Cmax geometric mean ratios were 117.76% and 100.88%, respectively. The 90% confidence intervals were within the pre-defined bioequivalence acceptance limits of 80.00% - 125.00%. Safety data was in line with the Summary of Product Characteristics of Cariprazine. The result of this clinical trial proved the bioequivalence of the new orodispersible tablet formulation when compared to hard gelatine capsules, enabling an alternative option for treatment of those suffering from schizophrenia.

Formulation and bioavailability studies on orodispersible tablets containing standardized extracts of Glycyrrhiza glabra, Curcuma longa and Piper nigrum

BackgroundGlycyrrhizin, Curcumin and Piperine indicated good antiasthamatic properties owing to their ability to inhibit airways constriction and anti-inflammatory properties. Orodispersible tablets have advantage of faster drug release and has patient compliance in asthmatic patients. Hypothesis / PurposeTo develop an orodispersible polyherbal tablets using the standardized extracts of Glycyrrhiza glabra, Curcuma longa and Piper nigrum with respect to glycyrrhizin, curcumin and piperine respectively and evaluate bioavailability of the markers from the formulation. MethodsAlcoholic extracts of G. glabra, C. longa, and P. nigrum were standardized using HPTLC for glycyrrhizin, curcumin, and piperine content, respectively. The orodispersible tablet formulation was created and standardized for curcumin (50 mg), glycyrrhizin (75 mg), and piperine (2.5 mg) per tablet, using the HPTLC method. The absolute Bioavailability studies were conducted for glycyrrhetinic acid and curcumin in rats by administering pure marker compounds intravenously (2 mg/kg b.w) and orally (10 mg/kg b.w.), followed by determining relative bioavailability through oral administration of the orodispersible tablet formulations. ResultsOrodispersible tablets could be successfully developed using the standardized extracts. The HPTLC bioanalytical method was developed and validated as per M 10 guideline and results were in accordance to specifications. The bioavailability studies in rats indicated absolute bioavailability of Glycyrrhetinic acid and Curcumin to be 20.35 and 2.57% respectively and relative bioavailabilities of orodispersible formulation F1 were found to be 75 and 38.67%. ConclusionA standardized orodispersible formulation can be a better option for asthma patients. The low absolute bioavailability of curcumin was significantly (P<0.05) increased in both the formulations F1 and F2. This may be attributed to the extracts containing saponin glycosides like Glycyrrhizin aiding into greater dissolution of curcumin. Formulation with piperine (F1) showed significant increase in bioavailability is due to inhibition of human P-glycoprotein, cytochrome P450 3A4 (CYP3A4) and increase secretion of bile acids.

Comprehensive Review of Oro Dispersible Tablets and Co Processed Super disintegrants

Due to their ease of administration, self-administration, and improved patient compliance, solid dosage forms are most popular. The most normally utilized strong dose structures are tablets and capsules, which is challenging for pediatric and geriatric patients. Considering these prerequisites endeavors have been made to foster rapid dissolving Tablets. The solid dosage form of a medicine that dissolves in a matter of seconds when swallowed is known as orodispersible tablet. The utilization of Superdisintegrants improves the crumbling season of the tablet. Fast Dissolving Tablets are generally liked because of their convenience, higher bioavailability, quick disintegration and breaking down of the medication. The various technologies utilized in the formulation of Orodispersible tablets (ODT) and their evaluation are the primary focus of this review.

Optimization of Semha-Pinas Extract Orodispersible Tablets Using Response Surface Methodology

The original dosage form of the Semha-Pinas herbal formula, an expectorant in Thai traditional medicine, is in a pill form. However, it is inconvenient to use because it must be powdered and dissolved in hot water or juice of Citrus x aurantium L. before use. The development of a new dosage form presents a challenging prospect. This work aimed to develop Semha-Pinas extract orodispersible tablets based on the response surface methodology using the Box-Behnken design. Firstly, Semha-Pinas extract was tested for its safety in HepG2 cells. The safe extract was further developed as orodispersible tablets. Four levels of three factors — compressional force (500–2,000 psi), the quantity of microcrystalline cellulose (0–15%), and the quantity of croscarmellose sodium and sodium starch glycolate (0:8–6:2%) — were screened using the one factor at a time technique. The Box-Behnken design has three levels for each factor: 1,000–2,000 psi, 5–15%, and 2:6–6:2%, respectively. Tablet thickness, hardness, friability, and disintegration time were the four responses that were monitored. The results indicated the safety of the Semha-Pinas extract, even at a concentration of 5 mg/mL. The optimal orodispersible tablet formulation had a compressional force of 1,500 psi, microcrystalline cellulose of 10%, and croscarmellose sodium to sodium starch glycolate of 4:4%. In summary, this study successfully fabricated Semha-Pinas extract orodispersible tablets using response surface methodology, achieving the desired property of fast disintegration. Moreover, these findings can serve as a valuable reference for pilot scale and industrial scale production.

Sugar content and erosive potential of commonly prescribed Orodispersible tablets- An in vitro study.

Background:Dental caries is a major non-communicable disease of public health concern caused due to freely available dietary sugars. We aimed to compare the sugar content and erosive potential with duration of use and drug classes of orodispersible tablets (ODTs). Methods:We conducted an in vitroevaluation of the total sugar content (TSC), Potential of Hydrogen (pH), solubility, and Titratable Acidity (TA) of commonly prescribed 62 ODTs. TA was measured by titrating the samples with known amount of. 0.1N sodium hydroxide (NaOH) with phenolphthalein indicator and pH was determined by digital pH meter. TSC was evaluated by phenol sulphuric acid. Solubility was assessed by filtration. Results:Out of the 62 ODTs, majority were Antimicrobials (n=30). One-quarter of the ODTs (26%) had a mean pH below ≤5.5. No significant difference was seen in the mean pH with respect to different drug classes (p=0.082) and duration of use of ODTs. A significant difference was seen in the mean percentage solubility with respect to drug classes (p<0.001). Antimicrobials had the least percentage of solubility as compared to other drug classes. Antiemetics and proton pump inhibitors (24.33 ± 17.34) had significantly higher mean percentage sugar content than Antimicrobials (23.25 ± 17.16). No significant difference was seen in the mean TSC with respect to various drug classes (p=0.718) and between the duration of use of drugs (P=0.568) respectively.No significant difference was seen in the mean percentage TA with respect to drug class (p=0.123) and duration of use of drugs (p=0.424). Conclusion:Overall, we can conclude that one in four ODT formulations had a pH below 5.5 (critical pH). Only one ODT formulation did not have a sugar content. No difference was seen in the mean pH, sugar content, and TA with respect to duration of use of drugs and drug classes.

Sugar content and erosive potential of commonly prescribed Orodispersible tablets- An in vitro study.

Background:Dental caries is a major non-communicable disease of public health concern caused due to freely available dietary sugars. We aimed to compare the sugar content and erosive potential with duration of use and drug classes of orodispersible tablets (ODTs). Methods:We conducted an in vitroevaluation of the total sugar content (TSC), Potential of Hydrogen (pH), solubility, and Titratable Acidity (TA) of commonly prescribed 62 ODTs. TA was measured by titrating the samples with known amount of. 0.1N sodium hydroxide (NaOH) with phenolphthalein indicator and pH was determined by digital pH meter. TSC was evaluated by phenol sulphuric acid. Solubility was assessed by filtration. Results:Out of the 62 ODTs, majority were Antimicrobials (n=30). One-quarter of the ODTs (26%) had a mean pH below ≤5.5. No significant difference was seen in the mean pH with respect to different drug classes (p=0.082) and duration of use of ODTs. A significant difference was seen in the mean percentage solubility with respect to drug classes (p<0.001). Antimicrobials had the least percentage of solubility as compared to other drug classes. Antiemetics and proton pump inhibitors (24.33 ± 17.34) had significantly higher mean percentage sugar content than Antimicrobials (23.25 ± 17.16). No significant difference was seen in the mean TSC with respect to various drug classes (p=0.718) and between the duration of use of drugs (P=0.568) respectively.No significant difference was seen in the mean percentage TA with respect to drug class (p=0.123) and duration of use of drugs (p=0.424). Conclusion:Overall, we can conclude that one in four ODT formulations had a pH below 5.5 (critical pH). Only one ODT formulation did not have a sugar content. No difference was seen in the mean pH, sugar content, and TA with respect to duration of use of drugs and drug classes.

Efficacy and Safety of New Orodispersible Tablet Formulations of Praziquantel (Racemate and L-Praziquantel) in Schistosoma mansoni-Infected Preschool-Age Children and Infants: A Randomized Dose-Finding Phase 2 Study

IntroductionTwo novel formulations of praziquantel (PZQ) and Levo-(L-)PZQ (arpraziquantel) have been developed for the treatment of schistosomiasis in preschool-age children and infants.MethodsThis open-label, dose-finding Phase 2 study assessed the efficacy and safety of PZQ formulations in children and infants infected with Schisostoma mansoni in Côte d’Ivoire. In Part 1, 420 children aged 2.1–6.9 years (weight 10.0–29.9 kg) were enrolled and randomized to one of 7 treatment arms (n=60 per arm): commercially available racemate (rac)-PZQ at 3x20 mg/kg or 40 mg/kg (treatment arms 1 and 2); rac-PZQ orodispersible tablet (ODT) at 40 mg/kg or 60 mg/kg (treatment arms 3 and 4); or L-PZQ ODT at 30 mg/kg, 45 mg/kg, or 60 mg/kg (treatment arms 5, 6, and 7). The optimal formulation and dose identified (L-PZQ ODT 50 mg/kg) was used in Part 2, which enrolled 24 infants aged 6–24 months (weight 7.5–14.8 kg). Infants were treated in an age-staggered approach: age 13–24 months (treatment arm 8, n=20) and age 6–12 months (treatment arm 9, n=4). The primary endpoint was clinical cure rate (CR) demonstrated by the Kato–Katz method 14–21 days post-treatment. Secondary endpoints included CR by point-of-care circulating cathodic antigen, egg reduction rate (ERR), and adverse events (AEs).ResultsIn Part 1, CRs ≥70% were achieved in all treatment arms and were highest with L-PZQ ODT 60 mg/kg (89.7%), rac-PZQ 3x20 mg/kg (89.5%), and L-PZQ ODT 45 mg/kg (86.0%). In Part 2, CRs were &amp;gt;90%. All treatment arms had ERRs &amp;gt;95%. Treatment-related AEs were reported by 71 participants (16.0%) and were similar across treatment arms; most were mild and transient. The most common treatment-emergent AEs were laboratory abnormalities. No deaths or discontinuation due to treatment-emergent AEs were reported and no new safety concerns were identified.ConclusionNew rac-PZQ and L-PZQ ODT formulations used as single-dose therapy against S. mansoni demonstrated acceptable overall efficacy and safety in preschool-age children and infants, warranting further studies in this population.Clinical Trial RegistrationClinicalTrials.gov, identifier NCT02806232; Pan African Clinical Trials Registry, identifier PACTR201604001493593.

Investigation of Plantago ovata Husk as Pharmaceutical Excipient for Solid Dosage Form (Orodispersible Tablets).

The objective of the study was to investigate the suitability of the Plantago ovata (PO) husk as a pharmaceutical excipient. Various phytoconstituents of the husk were determined according to the standard test procedures. The Plantago ovata husk was evaluated for various pharmaceutical parameters related to flow, swelling index, and compressibility index. Orodispersible tablets (ODTs) were prepared, containing different concentrations (2.5, 3, 5, 7.5, 10, and 15% w/w) of the Plantago ovata husk. Before compression, all the formulations were evaluated for their flow. Compressed ODTs were evaluated for physical characteristics (physical appearance, weight and weight variation, thickness, and moisture content), mechanical strength (crushing strength, specific crushing strength, tensile strength, and friability), disintegration behavior (disintegration time and oral disintegration time), drug content, and in vitro drug release. Phytochemical evaluation of the Plantago ovata husk confirmed the presence of various phytoconstituents like alkaloids, tannins, glycosides, saponins, flavonoids, and phenols. SEM photograph of the Plantago ovata husk showed that it has a fibrous structure, with a porous and rough surface. The Plantago ovata husk had a high swelling index (380%) which decreased by pulverization (310%). Precompression evaluation of the powder blend for all the formulations of ODTs showed good flow properties, indicating that the Plantago ovata husk improved the rheological characteristics of the powder blend. Compressed ODTs had good mechanical strength, and their friability was within the official limits (<1%). Best disintegration was observed with formulation F-6 containing 10% w/w of the Plantago ovata husk. It is concluded that the Plantago ovata husk can be used as a disintegrant in the formulation of ODTs.

PRELIMINARY STUDIES ON THE PHYSICAL PARAMETERS OF ORODISPERSIBLE TABLETS USING SUPERDISINTEGRANTS

There are various routes of drug administration available such as oral, sublingual, inhalation, and rectal. Among all, the oral route of drug administration is most widely used. Tablet is the most popular dosage form among all existing dosage forms. The most conventional tablets are immediate release but these tablets are only suitable for drugs with high solubility and high permeability. In this study, five different Orodispersible tablet formulations were prepared. Various Natural and Synthetic super disintegrants were used in all formulations including Plantago Ovata (F1), Sodium Alginate (F2), Fenugreek (F3), Croscarmellose Sodium (F4) &amp; Crospovidone (F5). Various pre-formulation and post-formulation tests were performed for all five (05) formulations like Angle of repose, Bulk density, Tapped density and Compressibility index. Additionally, all of the prepared formulations were evaluated for weight variation, friability, hardness, drug content, and disintegration time and dissolution rate. Furthermore, stability testing of Risperidone Oro dispersible tablets was conducted. The results revealed that all the formulations F1, F2, F3, F4, and F5 complied with the official specification limits. Among all formulations, F1 showed the best results in terms of less disintegration and increased dissolution of drug as compared to other formulations, and the F1 formulation showed good stability results as well.

The insights on Oro-dispersible tablet

Orodispersible tablets (ODTs) were the conventional product that disintegrates or dissolves into the buccal mucosa in less than 1mins in the absence of water and without chewing. They were first acquainted with the market during the 1980s, and end up one of the quickest developing subdivisions of the oral medication conveyance industry and their items are creating at an extraordinary rate. New orodispersible tablet innovations address numerous pharmaceutical and need of patients, extending from upgraded life-cycle the executives for reasonable medicating for pediatric, aged, and mental patients with trouble in swallowing. These supposedly affect about 35% of the all-inclusive community and related to various ailments like Parkinsonism, mental incapacity, motion sickness, obviousness, water inaccessibility, and so on. Other individuals possibly will face difficulties by utilizing control release solid oral product comprise the psychologically ill, partially developed patients, and rare patients those are unco-operative, on taking place diminished fluid consumption and are nauseated. To defeat such troubles, orodispersible tablets have been formulated. In this dosage form, the property of ODTs can be reached by the expansion of various additives such are super- the disintegrating agent is the main excipient. This has been motivated by both industry and academia to develop advanced orally dispersible products and advanced methodologies in the market. The ODTs are the most extensively implemented marketable products than others. The main purpose of this review paper is to provide the complete information of ODTs formulation

Orodispersible Carbamazepine/Hydroxypropyl-β-Cyclodextrin Tablets Obtained by Direct Compression with Five-in-One Co-processed Excipients.

The development of orodispersible tablets (ODTs) for poorly soluble and poorly flowable drugs via direct compression is still a challenge. This work aimed to develop ODTs of poorly soluble drugs by combining cyclodextrins that form inclusion complexes to improve wetting and release properties, and directly compressible co-processed excipients able to promote rapid disintegration and solve the poor flowability typical of inclusion complexes. Carbamazepine (CBZ) and hydroxypropyl-β-cyclodextrin (HPβCD) were used, respectively, as a model of a poorly soluble drug with poor flowability and as a solubilizing agent. Specifically, CBZ-an antiepileptic and anticonvulsant drug-may benefit from the studied formulation approach, since some patients have swallowing difficulties or fear of choking and are non-cooperative. Prosolv® ODT G2 and F-Melt® type C were the studied five-in-one co-processed excipients. The complex was prepared by kneading. Flow properties of all materials and main properties of the tablets were characterized. The obtained results showed that ODTs containing CBZ/HPβCD complex can be prepared by direct compression through the addition of co-processed excipients. The simultaneous use of co-processing and cyclodextrin technologies rendered ODTs with an in vitro disintegration time in accordance with the European Pharmacopoeia requirement and with a fast and complete drug dissolution. In conclusion, the combination of five-in-one co-processed excipients and hydrophilic cyclodextrins may help addressing the ODT formulation of poorly soluble drugs with poor flowability, by direct compression and with desired release properties.

Evaluation of the disintegrant property of co-processed sorghum starch-silicon dioxide excipient in chlorpheniramine orodispersible tablets

Background: Fast dissolving or orodispersible tablets are highly desirablein groups such as children, uncooperative, nauseated, or those on reduced water intake to ease the difficulties associated with swallowing the conventional solid dosage forms. Objectives: The work aimed to evaluate the disintegrant property of sorghum starch-silicon dioxide co-processed mixture in the formulation of chlorpheniramine orodispersible tablets. Method: Different batches of orodispersible tablets of chlorpheniramine maleate (4 mg) were prepared by direct compression method using Avicel® as a bulking agent and four different types of disintegrants (sorghum starch, co-processed sorghum starch-colloidal silicon dioxide, sodium starch glycolate and croscarmellose sodium) at varying concentrations (5, 10 and 20 %). The formulated tablets were subjected to weight variation test, thickness, crushing strength, friability test, wetting time, water absorption ratio, disintegration test and in-vitro dissolution study. Results: For tablets above 250 mg, it is expected that not more than two tablets should deviate from the average weight by 5% and none should deviate by more than 10%, all the formulations yielded tablets within this specification. The disintegration time of tablets containing 10% of disintegrants was all less than 60 s except those containing sorghum starch (SS) which took a long time. Similarly, the time taken to release 50 % of the drug (t50%) for tablets containing 10% sorghum starch was 25 s, 5 s for tablets containing 10% sorghum starch-colloidal silicon dioxide excipient and 8 s for tablets containing 10% of either croscarmellose sodium or sodium starch glycolate. The differential scanning calorimetry study results suggested that the drug and the excipient are compatible. Conclusion: The results show that sorghum starch-silicon dioxide co-processed mixture can be used as an alternative to croscarmellose sodium and sodium starch glycolate in orodispersible tablet formulations.

Design and characterization of taste masked metronidazole microcapsules and its utilization in the formulation of orodispersible tablets

Orodispersible tablet (ODT) containing microcapsules is an advanced and convenient drug delivery system that offers advantages of easy administration, and increased bioavailability. Metronidazole is an antiprotozoal, with a bitter and metallic taste as its major drawback. A taste masking is required since the tablet will disintegrate in the oral cavity releasing the drug into close proximity to the taste buds. The purpose of the study is to design and evaluate metronidazole microcapsules for formulation of taste masked orally ODT metronidazole tablets. Taste masked metronidazole microcapsules were prepared by emulsion polymerization method with sodium alginate as polymer using different drug to polymer ratio. The microcapsules were evaluated for drug loading, entrapment efficiency, drug-polymer interaction by FTIR spectrometry, DTA, and flow properties. Batches B4 and B5 were formulated into orally disintegrating tablet by direct compression method. The results of FTIR spectrometry and DTA characterization of microcapsules revealed absence of drug-polymer interaction. Evaluation of the microcapsules showed fairly good flow properties and increase in entrapment efficiency as the polymer concentration increased. Evaluation of the directly compressed ODTs showed acceptable weight variation, and average disintegration time less than 60 sec. The average tablet crushing strength range from 18 to 19 N, and the drug release profiles showed greater than 80% release of metronidazole within 10 min. The successful microencapsulation of metronidazole, fast disintegration, rapid drug release profile, and evidence of compatibility between metronidazole and the process polymer demonstrates the suitability of the microcapsules for formulation of orally disintegrating tablet for convenient delivery of metronidazole.Keywords: Orally disintegrating tablets, microencapsulation, taste masking

FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS (ODTS) OF DICLOFENAC SODIUM BY USING SUPERDISINTEGRANT FROM NATURAL ORIGIN

Objective: In this study, a polysaccharide isolated from the seeds of Cajanus cajan (pigeon pea) was investigated as a super disintegrant in the orodispersible tablets of diclofenac sodium.&#x0D; Methods: Diclofenac sodium tablets were prepared separately using different concentrations (5%, 7.5%, 10%, and 15% w/w) of isolated Cajanus cajan seed polysaccharide (natural) and sodium starch glycolate (synthetic) as super disintegrant by the direct compression method. Evaluation of tablets was done for various pre-and post-compression parameters. The stability studies were performed on optimized formulation F5. The disintegration time and in vitro drug release of the formulation F5 was compared with pregelatinized starch and synthetic super disintegrant (sodium starch glycolate).&#x0D; Results: The drug-excipient interactions were characterized by Fourier transform infrared studies. The Optimized formulation F5 containing 15% polysaccharide showed wetting time of 118.7 seconds with 105.3 seconds of disintegration time and 95.61% dissolved in 3 min.&#x0D; Conclusion: The present work revealed that Cajanus cajan seed polysaccharide has a good disintegrating agent in the formulation of orodispersible tablets.

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

Now-a-days, Orodispersible drug delivery systems are extensively used to improve bioavailability and patient compliance. Over the past three decades, Orodispersible tablets (ODTs) have gained considerable attention as a preferred alternative to conventional tablets and capsules due to better patient compliance, improved solubility and stability profiles. ODTs are solid dosage forms containing medicinal substances which disintegrate rapidly, usually in a matter of seconds, when placed on the tongue. New ODT technologies address many pharmaceutical and patient needs, ranging from enhanced life-cycle management to convenient dosing for paediatric, geriatric, and psychiatric patients with dysphagia. The therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. Hence disintegration has major role for facilitating drug activity. In recent years, several newer agents have been developed known as superdisintegrants. The objective of the present article is to highlight the various kinds of superdisintegrants (Natural &amp; Synthetic) along with their role in tablet disintegration and drug release, which are being used in the formulation to provide the safer, effective drug delivery with patient compliance.&#x0D; Keywords: ODTs, Orodispersible tablets, Disintegrants, Superdisintegrants, Natural, and Synthetic.

EVALUATION OF MUSA ACUMINATA FRUIT AS A NATURAL SUPERDISINTEGRANT FOR TABLET FORMULATION

Objective: The objective of the present work was to develop and evaluate a new, low-cost effective superdisintegrant from Musa acuminata fruit for tablet formulation.Methods: The study involved collection of M. acuminata fruit powdered and evaluated for physicochemical properties. Propranolol Hcl was used as a model drug for tablet formulation. Different concentrations of M. acuminatea powder were used as superdisintegrant, and orodispersible tablet is prepared and evaluated. In the present study, sodium starch glycolate was used as synthetic superdisintegrant for comparative study.Result: The powder was dark brownish and did not change throughout the study. The percentage porosity of powder was found to be 42.88% and angle of repose of was found to be 33.69°. The solubility study shows that the powders are sparingly soluble in water and disperse into individual particles. Total ash and acid insoluble ash values of powder were found to be 2.61 and 2.11% w/w, respectively. The average weight of tablets was ranged from 101.42 to 103.52 mg and averaged hardness was found to be 3.4 kg/cm2. Moreover, the tablets exhibited acceptable friability. Disintegration time of all formulations was found to be in the range of 22–80 s and wetting time was found to be 07–18 s.Conclusion: From the study, it was concluded that M. acuminatea powder in the range of 2–12% can be used as superdisintegrant in orodispersible tablet formulation and shall be preferred as having nutritive value as well as cost profit in the development of orodispersible tablet than synthetic polymer.