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.

Nanocellulose: Preparation, Characterization and Applications

The growth of nanocellulose has attracted outstanding interest in the last few decades due to its unique and potentially useful features. Novel nanocelluloses improve the strongly expanding field of sustainable materials and nanocomposites.CNCs and CNFs are two kind of nanocelluloses (NCs), and they own various superior properties, such as large specific surface area, high tensile strength and stiffness, low density, and low thermal expansion coefficient.Their application includesnanocellulose in transdermal drug delivery, Hydrogels, Aerogel Systems, Nanocellulose in Tablet Formulations and Nanocellulose in Microparticulate Drug Delivery (1). Different methods of nanocellulose like pretreatment method, mechanical process and chemical hydrolysis used for the synthesis of nanocellulose. Characterization of cellulose includes scanning electron microscopy, x-ray diffraction (XRD) analysis of samples and thermogravimetric analysis.

Review Article: The Effectiveness of Avocado Seed Starch (Persea Americana Mill) As An Excipients in Tablets Formulation

Avocado consists of pericarp (husk), mesocarp (flesh), and endocarp (seed). In avocado seeds there is a fairly high starch content, which is around 80.1% with amylose content of 43.3% and amylopectin of 36.8%. Starch is defined as a natural polymer consisting of a structure composed of amylopectin and another structure called amylose. Amylose content has properties that are easy to absorb water and amylose content can have excellent swelling power in the tablet crushing process. This allows avocado seeds as an alternative source of starch which can be an excipient in tablets. The research explored the effectiveness of avocado seed starch (Persea americana Mill) as an excipient in tablet formulations based on research that has been done. The method of the research is using secondary data obtained from literature studies, which were analyzed by bibliographic annotation by searching and analyzing data related to the effectiveness of avocado seed starch as an excipient. The data collection technique in this research is in the form of a review of published scientific journals, national and international journals. Analysis of the physical and chemical properties of avocado seed starch showed that avocado seed was able to become an excipient. Several studies also showed that avocado seed starch used as a disintegrant and binder in tablet formulations had an optimum concentration of 10%. In addition, avocado seed starch can also be used as an active substance in tablets.

The effectiveness of clove oil, its fractions, and clove oil-based fumigant tablet formulations, against Tribolium castaneum (Herbst)

Indonesia has seen an increase and widespread reports of resistance among stored-product insect pests to phosphine. The use of Syzigium aromaticum (clove oil) as an alternative fumigant may be a useful strategy to control infestation by phosphine-resistant varieties of stored-product insects. The objective of this study was to examine the effectiveness of whole (unfractionated) clove oil as well as its component fractions as a fumigant and repellent against the red flour beetle (Tribolium castaneum (Herbst)), and to develop a simple fumigant formulation for this purpose. The experimental design used to test the effectiveness of clove oil and its fractionation was a completely randomized design (CRD). Meanwhile, testing the effectiveness of tablet formulations was carried out by factorial CRD. Fumigation test results gave LD50 and LD95 values of 0.234 and 1.142 ml/l respectively, for crude clove oil used in a fumigation chamber against T. castaneum. An n-hexane fraction of clove oil tested under the same conditions was more lethal, causing 95% mortality of T. castaneum at the dose of 0.801 ml/l during fumigation. Finally, tablets containing a set proportion of clove oil and naphthalene (1:1) reached LD91 against T. castaneum after 7 days’ fumigation.

Tablet Formulation Studies on Recrystallized Active Pharmaceutical Ingredients of Valsartan and Olmesartan Medoxomil

Both the Valsartan (VAL) and Olmesartan medoxomil (OLM) are widely prescribed anti-hypertensive agents with angiotensin II type I receptor antagonistic activity. Both VAL and OLM are type of BCS class II drugs and having a low and variable oral bioavailability. Recrystallization of VAL and OLM from different organic solvents improved its aqueous solubility and thereby in vitro dissolution properties. In the present investigation, tablets containing Valsartan (VAL), Olmesartan medoxomil (OLM and) recrystallized products were prepared by direct compression method and evaluated for drug content, uniformity of weight, hardness, friability, disintegration time and dissolution properties. All the tablets fulfilled the compendial requirements with regarding to weight variation, friability and disintegration time etc for immediate release tablets. The DP15 (drug percent dissolved at 15 min) values for V-1 (tablets of VAL), V-4 (tablets of methanol recrystallized product with crospovidone as disintegrant) and DIOVAN™ 40mg tablet formulations are 45.97, 98.95 and 82.65 respectively and V-4 formulation showed higher dissolution rate when compared to other formulations. The DP15 values of O-1(tablets of OLM), O-4 (tablets of acetonitrile recrystallized product with crospovidone as disintegrant and OLMY™ (20mg) tablet formulations are 29.25, 99.93 and 84.82 respectively. O-4 tablet formulations showed higher dissolution rate when compared to other tablet formulations. Keywords: Valsartan, Olmesartan medoxomil, Recrystallization, Aqueous solubility

Utilization of Pectin from Okra as Binding Agent in Immediate Release Tablets

Polymeric materials from plants continue to be of interest to pharmaceutical scientists as potential binders in immediate release tablets due to availability, sustainability, and constant supply to feed local pharmaceutical industries. Paracetamol tablet formulations were utilized in investigating the potential binding characteristics of pectin harnessed from various okra genotypes (PC1-PC5) in Ghana. The pectin yields from the different genotypes ranged from 6.12 to 18.84%w/w. The pH of extracted pectin ranged from 6.39 to 6.92, and it had good swelling indices and a low moisture content. Pectin extracted from all genotypes were evaluated as binders (10, 15, and 20%w/v) and compared to tragacanth BP. All formulated tablets (F1-F18) passed the weight uniformity, drug content, hardness, and friability tests. Based on their crushing strength, tablets prepared with pectin from the various genotypes were relatively harder ( P ≤ 0.05 ) than tablets prepared with tragacanth BP. Tablets prepared with pectins as binders at 10%w/v and 15%w/v passed the disintegration and dissolution tests with the exception of PC4 at 15%w/v. Incorporation of pectin from all genotypes (excluding PC5) as a binder at concentrations above 15%w/v (F13, F16, F14, and F15) produced tablets which failed the disintegration test and showed poor dissolution profiles. Thus, pectin from these genotypes can be industrially commodified as binders in immediate release tablets using varying concentrations.

Simultaneous HPLC Method Development and Validation of Bilastine and Montelukast in Bulk and Formulation

A new, simple, rapid, selective, precise and accurate reverse phase high performance liquid chromatography assay has been developed for simultaneous estimation of Bilastine, and Montelukast in tablet formulations. The separation was achieved by using Phenomenax Kinetex XB C-18 column (150 x 4.6mm, 5 .) using mobile phase Methanol: 0.1% TFA water (80:20). Injection volume was 10µl. The flow rate was 1.0mL.min-1 and the separated drugs were detected using UV detector at the wavelength of 270nm. The retention time of Bilastine and Montelukast was noted to be 1.27, and 4.86 respectively, indicative of rather shorter analysis time. The method was validated as per ICH guidelines. The proposed method was found to be accurate, reproducible, and consistent. It was successfully applied for the analysis of these drugs in marketed formulations and could be effectively used for the routine analysis of formulations containing any one of the above drugs, or a combination, without any alteration in the chromatographic conditions.

Formulation and Evaluation of Tablets Containing Fenugreek Extract Using Sodium Starch Glycolate as Super Disintegrant

The present work is aimed to formulate the tablets containing fenugreek extract as drug by wet granulation method. Further the effect of Sodium Starch Glycolate as super disintegrant on disintegration and drug release was studied. Fenugreek extract contains mucilage which retards the disintegration of tablets and hence shows slower drug release. Hence in order to improve disintegration and thereby in vitro drug release, Sodium Starch Glycolate was used as super disintegrant. Tablet formulations were prepared without the SSG (Conventional-F1) and also with sodium starch glycolate (F2-F4) by wet granulation method. Assessment of flow properties of granules, physicochemical characterization of tablet formulations was carried out. Fenugreek is widely used for its antidiabetic activity which is attributed to mainly to the presence of an alkaloid Trigonelline. Hence in vitro release study of trigonelline was carried out which showed that the percentage release from F1 and F2 was found to be 58.12±4.49 and 99.08±0.01 respectively after 6 hrs. This study concludes that tablet formulation of fenugreek seed extracts with super disintegrants will be more desirable, advantageous and therapeutically more beneficial than incorporating the direct plant materials for the treatment of diabetes for faster onset of action.

Evaluation of the Disintegrant Properties of Silicified Oryza sativa Starch Co-Processed with Dioscorea dumentorum Starch in Directly Compressed Paracetamol Tablet Formulations

Starch is a readily available excipient which finds application in the pharmaceutical industry as binders, diluents and disintegrants. The use of starch is however limited by its poor flow characteristics. Co-processing exploits the desirable attributes of excipients, while masking the undesirable properties. Co-processed starch, thus presents great potential for use in formulation of directly compressed tablets which require materials with strong inherent cohesive and free flowing properties. In this study, Dioscorea dumentorum (Family: Dioscoreaceae) Starch (DdS) is co-processed with silicified rice starch (SRS) obtained from Oryza sativa; Family: Poaceae was incorporated as a disintegrant in directly compressed paracetamol tablet formulations in comparison with silicified rice starch and Avicel® as the official standard. Rice and DdS were extracted following standard procedures. The rice starch was silicified using colloidal silicon dioxide and co-processed with DdS in the ratio SRS:DdS (1:2). The DdS, SRS and SRS:DdS (1:2) were characterized using FTIR, particle size, angle of repose, bulk and tapped densities, Hausner ratio and Carr’s index. Paracetamol powder was directly compressed into tablets incorporating the co-processed excipient (SRS:DdS; 1:2) as disintegrants alongside Avicel®, SRS and DdS at varying concentrations (10% w/w, 15% w/w, 20% w/w, 25% w/w). The properties of the tablets were evaluated using friability, crushing strength and disintegration as the assessment parameters. Measurements were made in triplicates and the results were statistically analyzed. The yield of the starches was 41% w/w and 39% w/w for rice starch and DdS respectively. Silicifying the rice starch markedly improved the flow of the starch with a change of Carr’s index and Hausner ratio from 16.7 and 1.32 to 2.33 and 1.02 respectively. Tablets containing Avicel® had better crushing strength and friability values than those containing SRS: 2DdS at all disintegrant concentrations. The disintegration times for Avicel® and SRS: DdS compared favourably at all concentrations of disintegrant and at 15% w/w disintegrant, SRS: DdS showed better disintegrant properties than Avicel®.