Formulation and Characterization of Ziprasidone Floating Pellets

The objective of this study is to design and evaluate Ziprasidone Floating pellets, which prolongs the release rate of the drug while extending the residence time of the drug within the body environment and without causing undeliterious effects to the subject. Ziprasidone and controlled matrix polymer granules were prepared by different granulation techniques in the ratio of 1:1, 1:1.5 and 1:2.Ziprasidone multi unit formulations comprising cellulose polymers were prepared by wet granulation technique, where as the Ziprasidone multi unit formulations comprising lipoidal / fatty polymers were prepared by melt granulation technique. Ziprasidone multi unit formulations with drug and polymer proportion as 1:1, F1 and F2 formulations consisting Cellulose polymers HPMC K4M and HPMC K100 respectively were prepared by wet granulation technique. Keywords: Ziprasidone, wet granulation, Floating pellets, melt granulation and polymer.

FORMULATION OF EFFERVESCENT GRANULES FROM RED GINGER (ZINGIBERIS OFFICINALE ROSCOE VAR. RUBRUM) EXTRACT AND ITS ANTIOXIDANT ACTIVITY

Objective: Ginger is one of the Indonesian plants that has been used as traditional medicine. The flavonoids and phenols compounds contained high antioxidant activity. This study aimed to formulate effervescent granules (EG) from red ginger (RG) extract and evaluate its antioxidant activity. Methods: The formulation of EG from RG extract was prepared by the wet granulation method using different concentrations of polyvinylpyrrolidone (PVP). Furthermore, the flowability of granules was evaluated, including flow rate, angle of repose, bulk density, tapped density, Carr's index, Hausner ratio, and effervescent time. The physical stability of granules such as organoleptic evaluation, effervescent time, and pH measurement was also evaluated after 28 d of storage, and the antioxidant activity of EG from RG extract was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Results: The result showed that the EG of RG extract was successfully prepared by wet granulation with a concentration of 15%. In addition, the flowability study showed that all formulas of EG from RG extract have good flow properties, and the granules showed excellent flow properties based on Carr′s index results. The effervescent time of granules remained within the acceptable range according to USP, and the physical stability did not change even after 28 d of storage. The IC50 of EG from RG extract was 283.28±3.6 ppm and has moderate in free radicals scavenging activity. Conclusion: EG from RG extract can be used as food supplements to protect the human body from free radicals and inhibit oxidases.

Assessment of Abrasion-Induced Visual Defects in Twin Screw Wet Granulation Using Wall Friction Measurements

Starting point of the presented study were abrasion effects occurring during a twin screw wet granulation (TSG) process of a new chemical entity (NCE) formulation, resulting in gray spots on the final tablets. Several actions and systematic changes of equipment and process parameter settings of TSG process were conducted which reduced the visual defect rate of the tablets, i.e., gray spots on the surface, below the specification limit. To understand the rationale and mechanism behind these improvements, correlations of defect rates and wall friction measurements using a Schulze ring shear tester were evaluated. To check the suitability of the method, a broad range of wall materials as well as powder formulations at various moisture levels were investigated with regard to their wall friction angle. As differences in wall friction angle could be detected, further experiments were conducted using wall material samples made out of different screw materials for TSG. Evaluation of these screw wall material samples gave first hints, which screw materials should be preferred in regard of friction for TSG process. In the finally presented case study, wall friction measurements were performed using the above mentioned NCE formulation with known abrasion issues at TSG processing. The results confirmed that changes which led to a reduced visual defect rate of tablets correlated with a decreased wall friction angle. The results suggest wall friction measurements as a potent tool for equipment selection and establishment of a suitable process window prior to conducting TSG experiments. Graphical abstract

Preparation of Tablet from Naagdon Plant by Wet Granulation Method for Treatment of Excessive Bleeding in Piles

The objective of present study was to formulate and evaluate the tablets for piles with different combination of herbal drugs. Material and Method: The tablet for piles containing lactose and mannitol as diluent and containing natural drugs like naagdon which was prepared by wet granulation method. The wet and compressed formulations were subject to several evaluation parameters like appearance, thickness, weight variation, hardness and friability. Results: The results of all evaluation parameters of piles tablet were within the acceptable limit. Pre-compression studies of piles tablet show satisfactory results. The thickness, hardness, weight variation, and friability of pilestablet were found to in acceptable range. The in-vitro drug release of eugenol from optimised for treatment piles formulation was found to be 90.23%. Significant results were obtained from present study. Discussion: The finding of current investigation clearly found that the health promotion of the body could be done by piles

Formulation and Evaluation of Nutraceutical Tablet Using Clove Drugs by Wet Granulation Method

The objective of present study was to formulate and evaluate the nutraceutical tablets with different combination of herbal drugs. Material and Method: The nutraceutical tablet containing lactose and mannitol as diluent and containing natural drugs like clove and cinnamon which was prepared by direct compression method. The compressed formulations were subject to several evaluation parameters like appearance, thickness, weight variation, hardness and friability. Results: The results of all evaluation parameters of nutraceutical tablet were within the acceptable limit. Pre-compression studies of nutraceutical tablet show satisfactory results. The thickness, hardness, weight variation, and friability of nutraceutical tablet were found to in acceptable range. The in-vitro drug release of eugenol from optimised nutraceutical formulation was found to be 90.23%. Significant results were obtained from present study. Discussion: The finding of current investigation clearly found that the health promotion of the body could be done by nutraceuticals. Keywords: Direct compression, Nutraceutical, Eugenol, In-vitro drug release

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

In Vitro Evaluation of Native Taro Boloso-I Starch as a Disintegrant in Tablet Formulations

Introduction. In drug delivery, solid dosage forms, of which tablet is the commonest, are still the leading preferences. An area of research focus in tablet drug delivery is the search for tablet excipients. This study was aimed at evaluating and optimizing native Taro Boloso-I starch as a tablet disintegrant. Methods. The response surface method with central composite design (CCD-RSM) was used for the analysis and optimization of the concentration of native Taro Boloso-I starch and compression force. Wet granulation method was used for the preparation of paracetamol tablets. The response variables considered were tablet crushing strength, friability, and disintegration time. Results and Discussion. Both the native Taro Boloso-I starch concentration and compression force had increasing effect on the tablet breaking force. The friability of the tablets was shown to decrease with increasing levels of the disintegrant concentration. On the other hand, compression force had a decreasing effect on friability in the investigated range. The disintegration time of the tablets was found to decrease with the concentration of the starch. The paracetamol tablets prepared with the optimized levels of native Taro Boloso-I starch and compression force showed tablet breaking force of 116.24 N, friability of 0.153%, disintegration time of 1.36 min, disintegration efficiency ratio of 562.3 N/(%Min), and comparative disintegration efficiency ratio of 13.6 with respect to commercial potato starch. Conclusions. The tablets exhibited improved crushing strength, friability, in vitro disintegration time, and disintegration efficiency ratio which suggest the novel applicability of the native Taro Boloso-I starch as an efficient pharmaceutical tablet disintegrant.

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.

Preparation and Evaluation of Diclofenac Sodium Effervescent Tablet

The oral dosage forms are the most popular way of taking medicine although having some disadvantages like deliberate absorption and thus onset of action is extend. This can be overcome by administrating the drug in a liquid form i.e. effervescent tablet. The research is a formulation of diclofenac sodium as a effervescent tablet by wet granulation method. The bitter taste of the drug are masked by added sweetening agent (lactose, glucose etc.) In the present work we are prepared effervescent tablet in that we are used active drug diclofenac sodium and other active ingredient acid like tartaric acid and base sodium bicarbonate in different concentrations. The formulation of tablet was done by using wet granulation, wet granulation is found to be acceptable method of effervescent tablet formulation. The various pre-formulation studies was performed hardness, weight variation, disintegration, dissolution etc.