Exploration of Neusilin® US2 as an Acceptable Filler in HPMC Matrix Systems—Comparison of Pharmacopoeial and Dynamic Biorelevant Dissolution Study

Modern pharmaceutical technology still seeks new excipients and investigates the further use in already known ones. An example is magnesium aluminometasilicate Neusilin® US2 (NEU), a commonly used inert filler with unique properties that are usable in various pharmaceutical fields of interest. We aimed to explore its application in hypromellose matrix systems (HPMC content 10–30%) compared to the traditionally used microcrystalline cellulose (MCC) PH 102. The properties of powder mixtures and directly compressed tablets containing individual fillers NEU or MCC, or their blend with ratios of 1.5:1, 1:1, and 0.5:1 were investigated. Besides the routine pharmaceutical testing, we have enriched the matrices’ evaluation with a biorelevant dynamic dissolution study and advanced statistical analysis. Under the USP apparatus 2 dissolution test, NEU, individually, did not provide advantages compared to MCC. The primary limitations were the burst effect increase followed by faster drug release at the 10–20% HPMC concentrations. However, the biorelevant dynamic dissolution study did not confirm these findings and showed similarities in dissolution profiles. It indicates the limitations of pharmacopoeial methods in matrix tablet development. Surprisingly, the NEU/MCC blend matrices at the same HPMC concentration showed technologically advantageous properties. Besides improved flowability, tablet hardness, and a positive impact on the in vitro drug dissolution profile toward zero-order kinetics, the USP 2 dissolution data of the samples N75M50 and N50M50 showed a similarity to those obtained from the dynamic biorelevant apparatus with multi-compartment structure. This finding demonstrates the more predictable in vivo behaviour of the developed matrix systems in human organisms.

FORMULASI TABLET HISAP EKSTRAK RIMPANG TEMULAWAK (Curcuma xanthorrhiza Roxb) DENGAN BAHAN PENGISI SORBITOL DAN LAKTOSA

Abstrak Temulawak adalah tanaman yang tumbuh berumpun, yang telah dimanfaatkan oleh sebagian masyarakat Indonesia, baik sebagai obat tradisional, sebagai pewarna maupun sebagai bahan pangan. Perlu dibuat sediaan tablet hisap agar dapat digunakan dengan nyaman dan praktis. Tujuan penelitian ini adalah untuk menguji pengaruh kombinasi bahan pengisi sorbitol dan laktosa terhadap karakteristik granul ekstrak rimpang temulawak dan terhadap mutu fifik tablet hisap ekstrak temulawak. Tablet hisap esktrak rimpang temulawak dibuat dengan campuran bahan pengisi sorbitol dan laktosa dengan konsentrasi berbeda yaitu F1 (sorbitol 5%: laktosa 95%), F2 (Sorbitol 10% dan laktosa 90%), F3 (Sorbitol 15%: Laktosa 85%), F4 (Sorbitol 20% : laktosa 80%), F5 (Sorbitol 25%: laktosa 75%). Tablet dibuat dengan granulasi basah. Penelitian ini menggunakan desain eksperimental laboratorium dengan melakukan pengamatan dan pencatatan hasil dari formulasi tablet hisap ekstrak rimpang temulawak (Curcuma xanthorrhiza Roxb) dengan bahan pengisi sorbitol dan laktosa. Data yang diperoleh dianalisis menggunakan SPSS versi 21 dengan metode ANOVA oneway dengan tingkat kepercayaan 95%. Hasil dari penelitian ini yaitu konsentrasi sorbitol dan laktosa terbaik untuk menghasilkan tablet hisap ekstrak temulawak adalah konsentrasi sorbitol (5%) dan laktosa (95%) dengan kecepatan alir 16,5±0,304 g/detik, persen kompresibilitas 6,57±0,069%, kadar lembab 1,47±0,06%, kekerasan 10,25±0,79 kP. Dari penelitian ini dapat disimpulkan bahwa penambahan konsentrasi sorbitol dapat menurunkan sifat tabletasi dan memperbaiki sifat fisik dari granul, makin tinggi konsentrasi sorbitol kekerasan tablet semakin menurun, dan meningkatkan kerapuhan dan waktu hancur tablet. Sedangkan semakin banyak konsentrasi laktosa meningkatkan sifat alir sudut diam, persen kompresibilitas dan menurunkan kadar lembab. Kata kunci : Temulawak, Tablet hisap, Sorbitol, Laktosa Abstrak Temulawak is a plant that grows in clumps, which has been used by some Indonesian people, both as traditional medicine, as a dye and as a food ingredient. It is necessary to make lozenges so that they can be used comfortably and practically. The purpose of this study was to examine the effect of the combination of sorbitol and lactose as fillers on the granule characteristics of the temulawak rhizome extract and on the physical quality of the lozenges of the temulawak extract. Temulawak rhizome extract lozenges were made with a mixture of sorbitol and lactose as fillers with different concentrations, namely F1 (sorbitol 5%: lactose 95%), F2 (Sorbitol 10% and lactose 90%), F3 (Sorbitol 15%: Lactose 85%), F4 (Sorbitol 20%: lactose 80%), F5 (Sorbitol 25%: lactose 75%). Tablets are prepared by wet granulation. This study used a laboratory experimental design by observing and recording the results of the formulation of lozenges of temulawak rhizome extract (Curcuma xanthorrhiza Roxb) with sorbitol and lactose as fillers. The data obtained were analyzed using SPSS version 21 with the one-way ANOVA method with a 95% confidence level. The results of this study are the best concentrations of sorbitol and lactose to produce lozenges of temulawak extract are concentrations of sorbitol (5%) and lactose (95%) with a flow rate of 16.5±0.304 g/second, percent compressibility 6.57±0.069%, moisture content 1.47±0.06%, hardness 10.25±0.79 kP. From this research, it can be concluded that the addition of sorbitol concentration can decrease the tableting properties and improve the physical properties of the granules, the higher the sorbitol concentration, the lower the tablet hardness, and increase the friability and disintegration time of the tablets. Meanwhile, the more lactose concentration increases the flow angle of repose, the percent compressibility and reduces the moisture content Keywords : Temulawak, Lozenges, Sorbitol, Lactose Keywords : Temulawak, Lozenges, Sorbitol, Lactose

Study of the technological properties of excipients in the development of the composition of orally dispersible tablets

Introduction. The article presents the results of studying the technological properties of individual excipients widely used in the compositions of existing orally dispersed tablets (ODT) for subsequent planning a multifactorial experiment. Samples of excipients were analyzed according to such pharmacopoeial indicators as description, flowability, bulk density, compressibility, fractional composition, solubility in water.Aim. The aim of the work is to create a list and study the technological properties of candidate substances for the role of auxiliary substances in the composition being developed by the ODT.Materials and methods. The technological properties of excipient samples were studied according to the methods of the State Pharmacopoeia of the XIV edition using the flowability tester GTL (ERWEKA, Germany), the bulk density tester SVM 221 (ERWEKA, Germany), the tablet press PGR-10 (LabTools, Russia) and the tablet hardness tester TBH 125 TDP (ERWEKA, Germany).Results and discussion. As a result of the study, experimental data on the technological properties of excipient samples were collected, and the selected samples were compared according to pharmaceutical and technological indicators.Conclusion. In the course of the study, a list of auxiliary substances for the development of the composition of ODT was formed and studies of their technological properties were carried out. The obtained experimental data will allow to develop an optimal matrix of a multifactorial experiment for the development of the composition of ODT and justify the choice of excipients.

Formulation and Evaluation of Immediate Release Tablets of Etizolam

In the present investigation, immediate release tablet formulation of etizolam was developed for management of insomnia and anxiety using different Superdisintegrants (Sodium Starch Glycolate, Croscarmellose, Crospovidone), Povidone K-30 and Magnesium stearate by wet granulation method. The drug-excipients interaction was investigated by UV spectrophotometer. The granules and tablets of Etizolam were evaluated for various pre and post compression parameters like angle of repose, compressibility index, hausners ratio, tablet hardness, friability and in vitro disintegration and dissolution studies and their results were found to be satisfactory. These results suggest that maximum in vitro dissolution profile of formulation F6 were found to have equivalent percentage of drug release and concluded that F6 is better and similar to innovator product.

Formulation Development and Evaluation of Fast Disintegrating Sustained Release Pellets Containing Verapamil Hydrochloride Tablets by Fluidized Bed Processor

This study aimed to developed novel fast disintegrating sustained release pellets containing tablet by using Fluidized Bed processor. Verapamil HCl used as a model drug for the formulation. Fluidized bed processor was used for coating of drug and polymer on the sugar spheres. To overcome the problem of swallowing for paediatric, geriatric, psychiatric, bedridden patients, uncooperative patients or for active patients who are busy and travelling and may not access to we aim to formulate the fast-disintegrating tablet. The superdisintigrant are commonly use like cross povidone, sodium starch glycolate which disintegrate tablet rapidly. It is assumed that, after the disintegration of tablets, pellets within tablets which are reside in GIT for several hours and gradually released a drug in controlled way. Eudragit RS 30D and ethyl cellulose were used as a sustained release polymer. Coating of spheres with sustained release film is achieved by bottom spray processor of FBP. Proper pellets coating film thickness, and concentration of polymers’, ensure obtaining desirable VH release profile for extended period of time, was defined. X composition of tablet with pellets were examined in order to obtained formulation, from which VH release would mostly appropriate pellets before compressing. Compression of pellets into tablet, being a modern technological process than enclosing them into hard gelatine capsule. The optimized batch evaluated by studied the effect of compression force, tablet hardness and friability and drug release from the pellets by sustained release manner.

Particle Engineering of Chitosan and Kaolin Composite as a Novel Tablet Excipient by Nanoparticles Formation and Co-Processing

Chitosan is not a common excipient for direct compression due to poor flowability and inadequate compressibility. Co-processing of chitosan and kaolin is a challenging method to overcome the limitations of the individual excipients. The purpose of the present study was to develop co-processed chitosan–kaolin by the spray drying technique (rotary atomizer spray dryer) and to characterize the excipient properties. The formation of chitosan nanoparticles was the major factor for desirable tablet hardness. The ratio of chitosan/tripolyphosphate of 10:1 and 20:1 had a significant effect on hardness. The successful development of co-processed chitosan–kaolin as a novel tablet excipient was obtained from a feed formulation composed of chitosan and kaolin at a ratio of 55:45 and the optimum chitosan/tripolyphosphate ratio of 20:1. Co-processing altered the physical properties of co-processed chitosan–kaolin in such a way that it enhanced the flowability and tableting performance compared to the physical mixture.

Analysis of Flow Characteristics and Paracetamol Tablet Hardness Using 2D Double Mixer of Design Drum Type with Rotation and Mixing Time Variations

One of the tablet manufacturing processes using the wet granulation method is the process of mixing the active ingredient granules, fillers, binders and pelicans. The parameters of the mixing process are important to study because they will affect the physical properties of the tablet. This study studied the effect of the variable duration and the size of the mixing cycle on the physical properties of paracetamol tablets using a 2D double mixer. The results of the analysis and testing showed that the variation of mixing time and the size of the rotation had a significant effect on the flow properties of the granules and the hardness of the tablets. In addition, the optimal parameter results to obtain optimal tablet hardness occurred at 15 minutes of mixing process and 50 rpm of rotation.

Review of Various Influential Factors in the Production of Robusta Coffee Effervescent Drink Tablets

Coffee is one of Indonesia's leading plantation commodities, which is ranked third in the world. Currently, coffee-based drinks have become a lifestyle in the millennial era. The high interest in coffee affects the economy of the community. Various efforts were made to further encourage the level of coffee consumption, especially in the form of beverages. On the other hand, it is necessary to diversify the product by highlighting the technology side, such as making effervescent which is easier, more practical, and can be enjoyed directly with cold water. Effervescent is known as a product that can cause gas bubbles as a result of the reaction of acids and bases when dissolved in water. The resulting gas bubbles are carbon dioxide which gives a sparkling effect (a taste sensation like sparkling water). The use of coffee as an effervescent raw material is related to its taste, bioactive compounds, and antioxidants. Coffee extract powder can be made from robusta and arabica coffee roasted at medium level with low-temperature crystallization, spray drying, freeze drying, and vacuum drying. Other materials that need to be added such as acid sources, bases, fillers, and binders can affect the effervescent characteristics such as tablet hardness, moisture content, hygroscopicity, and dissolution time. The recommended composition is citric acid, sodium bicarbonate, dextrin, and PVP (Polyvinilpyrrolydone).

OPTIMASI FORMULA TABLET BUKAL MUKOADHESIVE GLIBENKLAMID MENGGUNAKAN MATRIKS CMC NA SERTA ASAM OLEAT SEBAGAI ENHANCHER

Glibenclamide is a sulfonylurea class of antidiabetic drugs that works by stimulating insulin secretion in the pancreas so that it is effective only when the β-cells of the pancreas can still produce. The glibenclamide dosage form that is on the market is a conventional oral tablet which has various disadvantages in terms of pharmacokinetics. Based on this, it is necessary to develop a more effective drug delivery system for glibenclamide in order to avoid first-pass metabolism so as to increase the bioavailability of glibenclamide, namely by making mucoadhesive buccal tablets. This glibenclamide mucoadhesive buccal tablet is formulated using a variety of mucoadhesive polymers, namely CMC Na and oleic acid as enhancers. The manufacture of four mucoadhesive buccal tablet formulas used the direct compression method. The results of the weight uniformity test showed that they did not meet the NP requirements specified, all formulas had an NP of more than 15. The tablet hardness test also showed results that did not meet the test requirements. However, the results of the physical properties of the brittleness, pH and swelling index showed the results that met the test requirements. In this research, the optimum variation of CMC Na polymer and oleic acid as enhancers to physical properties (hardness, brittleness, pH, swelling ability) and the release of glibenclamide mucoadhesive tablets were CMC Na of 37.5 mg and oleic acid of 3.5. ml.