scholarly journals Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 56
Author(s):  
Ryoma Tanaka ◽  
Supisara Osotprasit ◽  
Jomjai Peerapattana ◽  
Kazuhide Ashizawa ◽  
Yusuke Hattori ◽  
...  

The manufacturing of solid pharmaceutical dosage forms composed of cocrystals requires numerous processes during which there is risk of dissociation into parent molecules. Resonant acoustic wet granulation (RAG) was devised in an effort to complete theophylline–citric acid (THPCIT) cocrystal formation during the granulation process, thereby reducing the number of operations. In addition, the influence of granulation liquid was investigated. A mixture of anhydrous THP (drug), anhydrous CIT (coformer), and hydroxypropyl cellulose (granulating agent) was processed by RAG with water or ethanol as a granulation liquid. The purposes were to (i) form granules using RAG as a breakthrough method; (ii) accomplish the cocrystallization during the integrated unit operation; and (iii) characterize the final solid product (i.e., tablet). The RAG procedure achieved complete cocrystal formation (>99%) and adequately sized granules (d50: >250 μm). The granulation using water (GW) facilitated formation of cocrystal hydrate which were then transformed into anhydrous cocrystal after drying, while the granulation using ethanol (GE) resulted in the formation of anhydrous cocrystal before and after drying. The dissolution of the highly dense GW tablet, which was compressed from granules including fine powder due to the dehydration, was slower than that of the GE tablet.

2021 ◽  
Author(s):  
Zilhadia Zilhadia ◽  
Shoffiya Amaliya ◽  
Yuni Anggraeni ◽  
Vivi Anggia ◽  
Yahdiana Harahap

Abstract Halal gelatin extracted from goatskin could be used as a new excipient in pharmaceutical dosage forms. This study was to determine the potency of gelatin extracted from goatskin as a binder on paracetamol tablets using wet granulation process with 2, 3 and 4% concentration ranges. As a comparison, tablets were formulated using bovine gelatin at the same concentration level. The results showed that weight variation, thickness uniformity and hardness value have met the requirements. Here, the paracetamol tablets using goatskin gelatin as a binder had better friability value, faster disintegration time and easier dissolution than the comparison (p < 0.05). Comparative test result showed increasing the concentration of gelatine caused the hardness value to go up, the disintegration time to take longer, and the tablet friability value to decrease (p < 0.05). The best tablets were produced with the 3% concentration of goatskin gelatine with the following evaluation results: the hardness value of 15.07 ± 0.67 Kp, the disintegration time of 3.71 ± 1.00 minutes and the friability value of 0.62% ± 0.89 respectively. The concentration of paracetamol in the 30th-minute dissolution test was equal to 99.78 ± 0.94%. The goatskin gelatin was very promising as a good binder using the wet granulation process.


Author(s):  
Samer Housheh ◽  
Saleh Trefi ◽  
Haroun Mohammad ◽  
Fawaz Chehna M

Prasugrel is a novel ADP receptor inhibitor with antithrombotic properties. This paper proposes a new method for quantitative analysis of prasugrel in bulk and pharmaceutical dosage forms. The method used gas chromatography with electron-capture detection (GC–ECD). Chromatographic analysis was performed on an RTX-5 capillary column. Under the optimum conditions, good retention and peak response were achieved for prasugrel. The analytical method was fully validated by assessment of LOD and LOQ (0.24 µg/mL and 0.73 µg/mL), linearity (R = 0.997) over the range 0.5-2.5 µg/mL and extraction recovery (>98.7 %, with RSD below 1.0, for prasugrel spiked at 0.5, 1, 1.25, 2 and 2.5 µg/mL), the precision was 0.825% and the intermediate precision was 1.134%. The method required no clean-up of prasugrel before and after injection. It has been successfully used to determine prasugrel content in different commercial pharmaceutical dosage forms.  


Author(s):  
Dumpeti Janardhan ◽  
Joginapally Sreekanth ◽  
P.Theja Pavan Kumar ◽  
M.Vamshi Krishna

The purpose of this study was to evaluate the potential of polymers for masking the taste of bitter drugs when incorporated into orally disintegrating tablets. The tablets were produced by simple wet granulation technique with a model compound (baclofen) which is moderately bitter. The formulating procedure had two variables to obtain good taste masking with desirable characteristics. The optimal granulation process parameters were polymer selection and its concentration (w/w), suitable for pilot scale level. Dextrates, β- cyclodextrin, eudragit EPO and PVP K-30 were used in preparation of granules by using water and iso-propyl alcohol. Crospovidone was used intra and extra granularly as superdisintegrant.  Sodium bicarbonate and citric acid were used as effervescent for fast disintegration of tablets, which also optionally act as desensitizer of taste buds. Results from evaluation of tablets indicated a disintegration time (avg) of 30-35 sec and 100% drug release was achieved within 5 min. But taste masking was achieved by only with eudragit EPO. Results from an evaluation by a panel of six human volunteers demonstrated that the orally disintegrating tablets which are prepared by using polymer Eudragit EPO (5% and 7.5% w/w of tablet) and PVP (7.5% w/w of tablet) improved taste, significantly. On studying physical parameters, F9 formulation demonstrated acceptable level of hardness and friability with good taste masking and it was thus considered as an optimized formulation


Author(s):  
Sagar Suman Panda ◽  
Ravi Kumar B V V ◽  
D Patanaik

A simple, precise and accurate spectrophotometric method was developed for analysis of the osteoporesis drug alendronate sodium (ALS). The method is based on reaction of the drug with sodium-1,2-naphthoquinone-4-sulphonate (NQS) in presence of alkali to form a brown colored complex giving absorption maximum at 525 nm. The drug obeyed Beer’s law in the range of 5-70 µg/ml with a correlation coefficient of 0.999. The LOD and LOQ values are 1.7 µg/ml and 5.0 µg/ml, respectively. The average recoveries for recovery study were found to be in the range of 99.37%-100.46%. The R.S.D. values for intraday and inter-day precision were found to be 0.48 and 0.62, respectively. The optimized assay conditions were applied successfully for determination of ALS in pharmaceutical dosage forms. No interference was observed from the excipients present in the dosage form. The method is statistically validated as per the ICH requirements.  


2019 ◽  
Vol 15 (3) ◽  
pp. 207-218 ◽  
Author(s):  
Fatma Ağın

Background:Calcium Channel Blockers (CCBs) are widely used in the treatment of cardiovascular and ischemic heart diseases in recent years. They treat arrhythmias by reducing cardiac cycle contraction and also benefit ischemic heart diseases. Electroanalytical methods are very powerful analytical methods used in the pharmaceutical industry because of the determination of therapeutic agents and/or their metabolites in clinical samples at extremely low concentrations (10-50 ng/ml). The purpose of this review is to gather electroanalytical methods used for the determination of calcium channel blocker drugs in pharmaceutical dosage forms and biological media selected mainly from current articles.Methods:This review mainly includes recent determination studies of calcium channel blockers by electroanalytical methods from pharmaceutical dosage forms and biological samples. The studies of calcium channel blockers electroanalytical determination in the literature were reviewed and interpreted.Results:There are a lot of studies on amlodipine and nifedipine, but the number of studies on benidipine, cilnidipine, felodipine, isradipine, lercanidipine, lacidipine, levamlodipine, manidipine, nicardipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, diltiazem, and verapamil are limited in the literature. In these studies, DPV and SWV are the most used methods. The other methods were used less for the determination of calcium channel blocker drugs.Conclusion:Electroanalytical methods especially voltammetric methods supply reproducible and reliable results for the analysis of the analyte. These methods are simple, more sensitive, rapid and inexpensive compared to the usually used spectroscopic and chromatographic methods.


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