AN EXPERIMENTAL DESIGN IN THE OPTIMIZATION OF VARIOUS TABLET EXCIPIENT FORMULATIONS = A CONCISE REVIEW

The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

PHYSICOCHEMICAL STANDARDISATION OF SIDDHA TABLET PREPARATION JATHIKAAI MATHIRAI

The aim of this study is to standardize the herbal Mathirai preparation Jathikaai Mathirai based on qualitative and quantitative methods as per the analytical specifications of Tablet/Mathirai prescribed by the Protocol testing of ASU drugs by Pharmacopoeial laboratory for Indian Medicines. The Tablet is prepared as described in the text Bala Vagadam. The medicine is subjected to Physicochemical standardisation as per the pharmacopoeial laboratory standards of Indian medicine. The tablet is in solid form which is brown in colour. It is rigid with strong characteristic odor. The aflatoxin assay and pesticide residue revealed that the tablet is free of aflatoxins and pesticide residue. The formulation is free of microbial contamination and shows positive for the presence of steroids, alkaloids, coumarins, tannins, carbohydrates, glycosides etc. The heavy metals are below detectable limit. The result of HPTLC finger printing of the drug at UV 366 nm shows that the peak at Rf 0.02 constitutes 100% of the total area of the separated peaks, which denotes the abundant existence of the drug at minimum peak level itself. It indicates drug as phytochemicals. The result of the present study ensures the safety profile of the Jathikaai Mathirai – Siddha herbal Tablet intended for paediatric usage and indicative of presence of active phytoconstituents that are responsible for its efficacy in treating the Valippu Noi (Seizure disorder) in children.

Isolation, Characterization, Chemical Modification and Application of Echinochloa Colona Starch as Tablet Disintegrant

Oral disintegrating tablets are solid dosage form containing medical substances which disintegrate rapidly, usually within few seconds when placed upon tongue requiring no additional water to facilitate swallowing. Solid dosage forms that can be disintegrated, dissolved, or suspended by saliva in the mouth resulting in easy swallowing can provide significant benefits to the pediatric and geriatric population, as well as other patients who prefer the convenience of easily swallowable dosage forms Superdisintegrants are currently approached and utilized in the formulation of the orally disintegrating tablets. The present work includes isolation of starch from Echinochloa Colona and further characterizing it for various physicochemical and phytochemical analysis. The isolated starch has been modified chemically and its disintegrating efficiency has been tested in tablet formulation; the present work also explores the optimization of concentration of starch in formulation of Ibuprofen tablets in comparison with synthetic and natural superdisintegrants. Phytochemical analysis confirmed the presence of starches and carbohydrates. Results indicated that the Echinochloa Colona starch samples could be potential superdisintegrants in orally disintegrating tablets of Ibuprofen. Tablet performance was found to influence by the way of addition of starch, its concentration and the method of tablet preparation. From these results it is possible to conclude that Echinochloa Colona starch could be used as a superdisintegrant.

Development and Characterization of Orally Dissolving Tablet of a Poorly Soluble Antiemetic Drug

The aim of present work is to prepare the orally dissolving tablets of poorly soluble Ondransetron Hydrochloride as its soluble form by adopting complexation method using different superdisintegrants alone and in combination. The growing importance of orally dissolving tablet was underlined recently when European Pharmacopoeia adopted the term “Oro dispersible tablet” as a tablet that to be placed in the mouth where it disperses rapidly before swallowing. Their characteristic advantages such as administration without water anywhere, anytime lead to their suitability to geriatric and paediatric patients. The complex prepared was showed better solubility in simulated salivary PH of 6.8. The pre compression characteristics of drug, drug with Beta cyclodextrin and final blend were evaluated with respect to standards. Results of the study showed that the optimized tablet with combination of superdisintegrants (2.5% crosspovidone, 3.5% sodium starch glycolate) showed hardness of 3.5Kg/Cm2, thickness 2.10mm, wetting time 18 sec, drug content 99.15%, disintegration time 20sec, in-vitro dispersion time 25sec, in-vitro drug release of 89.59% (in 3min) and percentage of drug permeation as 89.45% (in 5 min) and it is comparable with higher percentage of superdisintegrants used for tablet preparation. So this method was a promising approach for developing cost effective dosage form with high efficacy in treatment.

Development of Fourier transform infrared spectrophotometric method for identification and determination of marketed metamizole tablet preparation

Metamizole is a nonsteroidal antiinflammatory drug (NSAID) that functions as an analgesic, antipyretic, and antiinflammatory. Examination of active substance contents is a requirement that must be met to ensure the quality of drug preparations. The aims of this study were to develop and validate the Fourier Transform Infrared spectrophotometric method for the quantitation of metamizole content in marketed tablet preparation. Identification and determination of metamizole contents by Fourier Transform Infrared spectrophotometric method used methanol solvent in the wavenumber range 4000 cm–1 to 650 cm–1. The results showed that the specific wavenumbers of metamizole were 1649.3 cm–1; 1623.3 cm–1; and 1589.7 cm–1; and the contents metamizole in marketed tablet preparation ranged from (97.954 ± 0.121)% to (104.541 ± 0.257)%. From the validation method, the recovery result is 100.129%; the relative standard deviation is 0.057%; the limit of detection is 2.09526 mg/mL; the limit of quantitation is 6.34928 mg/mL; and the range 40 mg/mL to 60 mg/mL. The quantitation of metamizole contents can be carried out by Fourier Transform Infrared spectrophotometric method with accurate and precise quantitation results.

Diode Array Detection for UPLC Determination of Cinnarizine and Dimenhydrinate in their Combined Dosage Form

Background: Cinnarizine is used to treat nausea and vomiting accompanied by motion sickness. Dimenhydrinate is used in the treatment of nausea and vomiting and dizziness. The coformulation of the two drugs showed the lowest rate of adverse effects compared to single dimenhydrinate. Objective: A fully validated ultra-performance liquid chromatographic method has been conducted for the simultaneous estimation of cinnarizine (CIN) and dimenhydrinate (DIM). Materials and Methods: The UPLC method used Acquity Column as stationary phase and mobile phase methanol: buffer (pH = 3.5 ± 0.05) and acetonitrile in the ratio of 50: 25: 25 at a flow rate of 0.2 mL/min. Detection was performed by DAD at 260 nm. Results and Discussion: Retention time was 0.71 and 1.12 min for DIM and CIN, respectively. The linearity was found to be 1-40 μg/mL and 2-80 μg/mL for CIN and DIM; respectively. Conclusion: The method was appropriately used for the quantitation of both drugs in pure form, synthetic mixtures and tablet preparation.

Formulation, Development, and Evaluation of Herbal Effervescent Mouthwash Tablet Containing Azadirachta Indica (Neem) and Curcumin for the Maintenance of Oral Hygiene

Background: Dental caries originate due to the localized dissolution of the hard tissues of teeth, mainly caused by acids, developed by the presence of microorganisms in the biofilm (dental plaque) on the surface of teeth causing “cavities”. Commercially available liquid mouthwashes containing synthetic active ingredients possess limitations like teeth staining, higher alcoholic content, taste disturbances, xerostomia, and stability issues. Objective: To make the solid preparation for oral hygiene (US6428770B1) in the form of herbal effervescent mouthwash tablet (CN106619318A, US8728446B2) using Azadirachta indica and Curcumin having antimicrobial, antibacterial, antiplaque, and anti-inflammatory activity. Methods: The optimization study of effervescent granules was performed by 33 factorial design. A total of 27 preliminary experimental batches were prepared by the fusion method, varying the amount of citric acid, tartaric acid, and sodium bicarbonate. A complex of curcumin was prepared with hydroxyl propyl β-cyclodextrin and further examined by scanning electron microscopy. The prepared tablets were evaluated for pre and post-compression parameters. The in vitro antimicrobial study was performed by Agar well diffusion method against S. mutans. Results: All the experimental batches of effervescent granules were evaluated for pH, effervescent time, and CO2 content. Six batches were further selected for final tablet preparation. The results of the pre-compression parameters revealed excellent flow properties and post-compression parameters; the results were also significant. The antimicrobial study revealed the F3 as a final best formulation. Conclusion: The developed herbal formulation (F3) has a good potential to maintain oral hygiene as compared to alcoholic mouthwash and further studies may be necessary to confirm the efficacy of the formulation since only a single bacterial strain was assayed.

SeDeM-ODT Expert System: A Solution to Challenges in Characterization of Pharmaceutical Powders and Powdered Material

In the field of pharmaceutical sciences, material characterization has been a focus of research as properties of the powder ingredients govern characteristics of the finished dosage form. It has been a tedious and time-consuming job to develop a correlation between the characteristics of powder material and final dosage form. Extensive experimentation is carried out at different stages of formulation development to optimize the final blend and produce a product fulfilling official requirements. Various approaches have been applied for the purpose with varying degree of applications. SeDeM-ODT expert system is a novel pre-formulation technique developed for characterization of powder material of varying nature. Experimental and quantitative determination of various parameters provides a basis for SeDeM-ODT expert system. The system predicts suitability of powder material (APIs and excipients) for tablet preparation by direct compression technology and disintegration behavior of the resultant dosage form. It provides a basis for selection of excipients, both quantitatively and qualitatively. The present study covers area of powder characterization at pre-formulation level of pharmaceutical product development. SeDeM-ODT expert system reduces lead time for pre-formulation studies and provides formulations with minimum number of excipients. SeDeM-ODT expert system has been successfully applied for material characterization (APIs and excipients) before processing and after processing.

Co-Processed Excipients- A Review

Here is no single-component excipient satisfies all the essential execution to permit a active pharmaceutical component to be formulated into a selected dosage form. Co-processed excipient has received substantially more consideration in the definition improvement of different dosage form, uncommonly for tablet preparation by direct compression strategy. The main aim of this review is to talk about the rise of co-processed excipients as a present and future pattern of excipient innovation in pharmaceutical manufacturing. Co-processed excipients is a novel idea of consolidating at least two excipients designed to physical mixing without significant chemical change. These co-processed excipients have high functionalize compared to individual excipients such as better compressibility, flow property. All the developed excipients are enlisted for their beneficial and multifunctional characteristics. Further it gives opportunity for use of single multifunctional excipient rather than multiple excipients.