Inhibitory Effect of Oral Thin Films (OTFs) Containing Xylitol Against Streptococcus mutans

Dental Caries is a chronic disease affecting half of the global population, causing pain and discomfort due to progressive damage to the teeth. Whilst xylitol has been studied for its effect on dental caries prevention, current practices present few limitations for its successful oral delivery, including short residence time in the mouth and poor patient compliance. Recently, oral thin films (OTFs) emerged as an alternative to delivering xylitol in the oral cavity. This research aims to develop novel OTFs containing xylitol with extended-release properties (as determined by the disintegration time) and to investigate its effect on a cariogenic bacterial strain, Streptococcus mutans. The minimum inhibitory concentration (MIC) of xylitol was determined. Employing the microdilution broth method, the antibacterial activity of the oral thin films containing xylitol for oral S. mutans was performed with simulated salivary fluid, incubated at 1, 4, and 10 h. The MIC of xylitol was found at 10%. Meanwhile, there was no significant difference in the inhibition of S. mutans (p > 0.05) between the control, OTFs (10 h), and xylitol-OTF (1 h), with the latter, demonstrated only 16.58% inhibition. Interestingly, when compared to xylitol-OTF (1 h), xylitol-OTF showed significant inhibition (p < 0.05) to S. mutans after four h (+53.24 %) and almost a complete inhibition after ten h (-92.58 %). These results suggest that the OTFs demonstrated a gradual release of xylitol and inhibited oral biofilm formation by decreasing the growth of S. mutans in a time-dependent manner. Most importantly, the study indicated the successful development of a novel xylitol-OTF with potential as an oral health biotherapeutic agent.

DEVELOPMENT AND CHARACTERIZATION OF ORO-DISPERSIBLE TABLETS OF METFORMIN HYDROCHLORIDE USING CAJANUS CAJAN STARCH AS A NATURAL SUPERDISINTEGRANT

Objective: The aim of the research work was to explore the use of Cajanus cajan (Pigeon pea) polysaccharide as a superdisintegrant. The novel superdisintegrant has been evaluated for its action by incorporating it into orodispersible tablets of Metformin Hydrochloride. Methods: Cajanus cajan starch was extracted from its seeds and superdisintegrant was developed by microwave modification of the extract. Various characterization tests such as gelatinization temperature, water absorption index, pH, and viscosity were used to identify the microwave-modified polysaccharide. The orodispersible tablets were made using a direct compression process employing varying concentrations of modified Cajanus cajan starch. Prepared tablets were tested for several pre and post-compression parameters and compared with a well-established synthetic superdisintegrant, sodium starch glycolate. The stability studies were conducted on an optimized formulation. Results: Fourier transform infrared spectroscopy study showed that the drug had no interactions with the microwave-modified Cajanus cajan starch. SEM confirmed that Cajanus cajan starch granules exhibited intact granular structure in oval shapes and smooth surfaces. After microwave modification, the Cajanus cajan starch component lost its granular structure, which further led to the generation of surface pores and internal channels, causing overall swelling responsible for superdisintegrant activity. The optimized formulation (ODF5) containing 15 % modified Cajanus cajan starch performed better in terms of wetting time (22.21 s), disintegration time (53.3 s), and in vitro drug release (92%), as compared to formulation prepared by synthetic superdisintegrant (ODF1). Conclusion: The present investigation concluded that modified Cajanus cajan starch has good potential as a superdisintegrant for formulating oro-dispersible tablets. Furthermore, modified Cajanus cajan starch is inexpensive, non-toxic and compatible in comparison with available synthetic superdisintegrants.

DESIGN, DEVELOPMENT AND EVALUATION OF MOUTH DISSOLVING TABLETS OF TOFACITINIB CITRATE

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.

QUALITY CONTROL TESTING OF CONVENTIONAL CLOPIDOGREL BISULFATE TABLETS MARKETED IN IRAQ

Objective: This study was employed to evaluate the quality of marketed oral tablets containing clopidogrel bisulfate. Tablets produced by various companies and commercialized in the Iraq market were used in the study. Methods: Batches of clopidogrel bisulfate conventional tablets (containing 75 mg of drug) were exposed to the quality control tests. These tests involved friability, weight variation, hardness, drug content, disintegration time, and in vitro release study; these tests were conducted depending on USP pharmacopeia. Results: The data indicate that all batches of clopidogrel bisulfate complied with the limitations of USP pharmacopeia for variation of weight, results of the hardness of tablets were 7.2-9.6 Kg/cm2. Friability value (% loss) was less than one, which was within the required limits. The time of disintegration was less than 25 min in both artificial gastric fluid (AGF) and artificial intestinal fluid (AIF). Drug content was observed between 97.1 % and 99.8 %, indicating compliance with the limits of pharmacopeia (85-115 %). An in vitro release study of batches was greater than 80 % within 25 min. Conclusion: All batches of clopidogrel bisulfate were manufactured within the criteria of tablet manufacturing. The quality control tests of tablets showed acceptable pharmaceutical properties (effectiveness and safety) that lie within the limits of USP pharmacopeia.

FORMULATION AND EVALUATION OF THYROID HORMONE (T4) IMMEDIATE RELEASE TABLETS

The aim of this research work is to formulate and evaluate Levothroxine sodium immediate release tablets prepared by direct compression method . Five formulations were evaluated for different pre and post compression parameter and in vitro drug release studies.The results of pre compression parameters of formluation 1 to 5 were compared with prescribed limits. It showed that formulation 1 to 5 powder blend exhibit good flow property and compressibility property. The disintegration time of all formulation was found to be in the range 2mins 09 secsto 4mins 03 secs.Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablet Levothyroxine sodium was successfully done and F-5 showed almost 93% drug release at 45 mins in Alkaline borate buffer( pH 10). Keywords: Thyroid hormone (T4), Immediate release tablets, Direct compression, Dissolution.

Mucilage of Coccinia grandis as an Efficient Natural Polymer-Based Pharmaceutical Excipient

Natural eco-friendly materials are recently employed in products to replace synthetic materials due to their superior benefits in preserving the environment. The herb Coccinia grandis is widely distributed in continents like Asia and Africa and used traditionally to treat fever, leprosy, asthma, jaundice, and bronchitis. Mucilage of Coccinia grandis was accordingly extracted, isolated by a maceration technique, and precipitated. The mucilage was evaluated for its physicochemical, binding, and disintegrant properties in tablets using paracetamol as a model drug. The crucial physicochemical properties such as flow properties, solubility, swelling index, loss on drying, viscosity, pH, microbial load, cytotoxicity was evaluated and the compatibility was analyzed using sophisticated instrumental methods (TGA, DTA, DSC, and FTIR). The binding properties of the mucilage was used at three different concentrations and compared with starch and PVP as examples of standard binders. The disintegrant properties of mucilage were used at two different concentrations and compared with standard disintegrants MCCP, SSG, and CCS. The tablets were punched and evaluated for their hardness, friability, assay, disintegration time, in vitro dissolution profiles. In vitro cytotoxicity studies of the mucilage were performed in a human embryonic kidney (HEK) cell line. The outcome of the study indicated that the mucilage had good performance compared with starch and PVP. Further, the mucilage acts as a better disintegrant than MCCP, SSG and CCS for paracetamol tablets. Use of a concentration of 3% or less demonstrated the ability of the mucilage to act as a super disintegrating agent and showed faster disintegration and dissolution, which makes it as an attractive, promising disintegrant in formulating solid dosage forms to improve the therapeutic efficacy and patient compliance. Moreover, the in vitro cytotoxicity evaluation results demonstrated that the mucilage is non-cytotoxic to human cells and is safe.

Fused Deposition Modeling as a Possible Approach for the Preparation of Orodispersible Tablets

Additive manufacturing technologies are considered as a potential way to support individualized pharmacotherapy due to the possibility of the production of small batches of customized tablets characterized by complex structures. We designed five different shapes and analyzed the effect of the surface/mass ratio, the influence of excipients, and storage conditions on the disintegration time of tablets printed using the fused deposition modeling method. As model pharmaceutical active ingredients (APIs), we used paracetamol and domperidone, characterized by different thermal properties, classified into the various Biopharmaceutical Classification System groups. We found that the high surface/mass ratio of the designed tablet shapes together with the addition of mannitol and controlled humidity storage conditions turned out to be crucial for fast tablet’s disintegration. As a result, mean disintegration time was reduced from 5 min 46 s to 2 min 22 s, and from 11 min 43 s to 2 min 25 s for paracetamol- and domperidone-loaded tablets, respectively, fulfilling the European Pharmacopeia requirement for orodispersible tablets (ODTs). The tablet’s immediate release characteristics were confirmed during the dissolution study: over 80% of APIs were released from printlets within 15 min. Thus, this study proved the possibility of using fused deposition modeling for the preparation of ODTs.

A Novel Stability Study of Simvastatin Generic Tablet in Public Pharmacy Facilities of Purwakarta District, Indonesia

Drug stability is one of the most important criteria for producing safe, excellent and effective products. Some environmental factors that influence drug stability are light, temperature, and humidity. Simvastatin is a cholesterol-lowering drug that is known to be sensitive to high temperature and humidity. The purpose of this study is to analyze the effect of 6 months of real-time storage conditions on the stability of generic simvastatin tablets in public pharmacy facilities. This study used simulation method with 4 brands of simvastatin generic tablets with two different strengths (10 mg and 20 mg). In the process, the sample was conditioned in 6 different regions for 6 months. The results of temperature and humidity monitoring showed 2 locations at ≤ 25 ° C, 4 locations had a temperature of ≥ 25 °C and all locations had humidity > 65 %. The drug was evaluated for physical and chemical quality parameters at months 0, 3, and 6. After being stored for 6 months, the tablets showed a decrease in disintegration time and an increase in the friability, showing lack of durability. Similarly, there was a decrease in the content concentration in the tablets but fortunately the level was still within the accepted specification range (90 – 110 %). However, there was one tablet that did not meet the dissolution test requirements after the storage duration (Q ≤ 75 % at 30 minutes). The results of the stress test showed that simvastatin degraded in all conditions. This stress test confirmed the extreme instability of simvastatin. Poor storage conditions can reduce the quality of generic simvastatin tablets, thus a well-controlled environment is vital in pharmacy facilities.

FORMULATION AND EVALUATION OF THYROID HORMONE(T3) IMMEDIATE RELEASE TABLETS

The study was aimed to formulate and evaluate Thyroid hormone (T3) immediate release tablets of a model Reference Listed Drug (RLD). The objective was to develop a cost effective immediate release tablet formulation and to optimize the formula in product development same that of the reference product. The ingredients used were API (thyroid hormone), lactose monohydrate (diluent), acacia (binder), maize starch (disintegrant), sodium chloride (alkalinizing agent) and magnesium stearate (lubricant). The concentration of maize starch and magnesium stearate were altered to reach the objective. Totally five formulations (F1 - F5) were prepared by direct compression method. The plan of work involved involved in the study was1 Selection of drug and excipients, 2Physico–chemical characterization and drug identification, 3Preformulation parameters of the drug, 4Pre–compression parameters for the tablet blend, 5Formulation and development of the tablet dosage form, 6Post compression parameters of the tablet and 7Stability study. The stability studies were performed as per ICH guidelines. Among all the formulations F5 was found to be the best as it showed better results than the other formulations. In vitro disintegration time and percentage drug release results shown satisfactory results. Stability study results showed no significant changes in the formulation. Keywords: Thyroid hormone (T3), Immediate release tablets, Direct compression, Dissolution.

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