An Update on Impacts of Epigallocatechin Gallate Co-administration in Modulating Pharmacokinetics of Statins, Calcium Channel Blockers, and Beta-blockers.

Brewed green tea, green tea extract, and its primary active compound, epigallocatechin gallate, may interact with drugs and alter the drug's therapeutic effectiveness, ultimately leading to therapeutic failure or drug overdose. Several isolated reports have claimed that epigallocatechin gallate is the main active ingredient that causes these effects. While a few studies aimed to uncover evidence of epigallocatechin gallate-drug interactions, no study has thoroughly and collectively reviewed them. Epigallocatechin gallate is a potential cardioprotective agent used by many patients with cardiovascular diseases as a complementary medicine alongside conventional modern medications, either with or without the knowledge of their physicians. Therefore, this review focuses on the impact of concurrent epigallocatechin gallate supplementation on pharmacokinetics and pharmacodynamics of several commonly used cardiovascular drugs (statins, beta-blockers, and calcium channel blockers). The PubMed index was searched for key words related to this review, without year limit, and the results were analyzed for interactions of cardiovascular drugs with epigallocatechin gallate. This review concludes that epigallocatechin gallate increases systemic circulation of several statins (simvastatin, fluvastatin, rosuvastatin) and calcium channel blockers (verapamil), but decreases the bioavailability of beta-blockers (nadolol, atenolol, bisoprolol). Further studies on its clinical significance in affecting drug efficacy are required.

Comparison of Solvent Casting and Spray Casting Method on Compounding of an Orally Disintegrating Film Containing Amlodipine Besylate.

The amlodipine besylate tablet is one of the most highly prescribed medicines to manage hypertension in the geriatric population. However, the difficulty of swallowing tablets due to problems like dysphagia, fear of choking, and odynophagia has been identified as one of the contributing factors to non-compliance among geriatrics. Due to the swallowing factor among geriatrics, this study was conducted to compare two compounding methods of orally disintegrating films, namely solvent casting and spray casting, to produce an orally disintegrating film containing amlodipine besylate. Different polymers were used to develop the orally disintegrating films, and the formulations were subjected to validation tests such as thickness, folding endurance, tensile strength, percentage of elongation, Young's modulus, disintegration, and dissolution. Chemicals like hydroxypropyl methylcellulose, carboxymethyl cellulose, glycerin, mannitol, sodium lauryl sulfate, citric acid, peppermint oil, and a coloring agent were used to formulate the orally disintegrating films. In addition, orally disintegrating films were prepared using the solvent casting and the spraying method. An increase in the polymer's concentration resulted in the formation of a greater mechanical strength. After a comparison between the hydroxypropyl methylcellulose and the carboxymethyl cellulose as film-forming agents, it was discovered that hydroxypropyl methylcellulose had greater mechanical film properties than carboxymethyl cellulose, except for the folding endurance. Moreover, hydroxypropyl methylcellulose was shown to have a better disintegration time, which was in the range of 30 minutes to 90 minutes, with a drug release of 95% to 100%, while carboxymethyl cellulose disintegrated at 6 minutes to 15 minutes with a drug release of 60% to 75%. On the other hand, both the solvent casting and spraying methods produced an evenly matched orally disintegrating film quality. Orally disintegrating films containing amlodipine besylate were developed and characterized. It was concluded that these orally disintegrating films have a great potential in the market and a profound ability in the reduction of geriatric non-compliance to antihypertensive drugs.

Investigation of the Effects of Excipients in the Compounding of Amlodipine Besylate Orally Disintegrating Tablets.

Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.

Investigation of Filler Effects on the Compounding of Freeze-dried Orodispersible Tablets Containing Annona muricata Extract.

Orally disintegrating tablets are a solid dosage form that will disintegrate rapidly within 3 minutes upon contact with saliva. Fillers or diluents are excipients that are used to make up the volume of orally disintegrating tablets, and some might act as a disintegrant or binder that will affect the physical properties of orally disintegrating tablets. The objective of this study was to formulate and evaluate physical properties of orally disintegrating tablets containing Annona muricata leaves extract by a freeze-drying method using different fillers at different concentrations. In this study, fifteen formulations of orally disintegrating tablets were prepared by a freeze-drying method with different fillers such as starch, lactose, microcrystalline cellulose, StarLac, and CombiLac at 5%, 10%, and 15%. The orally disintegrating tablets were evaluated for hardness, thickness, weight variation, friability, and disintegration time test. The optimum formulation was chosen and incorporated with Annona muricata leaves extract. The results obtained in this work indicated that Formulation 3, with 15% starch, was the most optimum formulation due to the shortest disintegration time (21.08 seconds ± 4.24 seconds), and all the physical tests were within the acceptable range. The orally disintegrating tablets containing Annona muricata leaves extract possessed antioxidant activity and stable at least for 3 months under 60°C and 75% relative humidity.

Effect of processing methods on xylitol-starch base co-processed adjuvant for orally disintegrating tablet application.

Orally disintegrating tablet (ODT) is a friendly dosage form that requires no access to water and serves as a solution to non-compliance. There are many co-processed adjuvants available in the market. However, there is no single product possesses all the ideal characteristics such as good compressibility, fast disintegration and good palatability for ODT application. The aim of this research was to produce a xylitol-starch base co-processed adjuvant which is suitable for ODT application. Two processing methods namely wet granulation and freeze drying were used to compare the characteristics of co-processed adjuvant comprising of xylitol, starch and crospovidone XL-10 mixed at various ratios. The co-processed excipients were compressed into ODT and physically characterized for powder flow, particle size, hardness, thickness, weight, friability, in-vitro disintegration time and in-situ disintegration time, lubricant sensitivity, dilution potential, Fourier transform infrared spectroscopy, scanning electronic microscopy and x-ray diffraction analysis. Formulation F6 was selected as the optimum formulation due to the fastest in-vitro (135.33±11.52 s) and in-situ disintegration time (88.67±13.56s) among all the formulations (p<0.05). Increase in starch component decreases disintegration time of ODT. The powder flow fell under the category of fair flow. Generally, it was observed that freeze drying method produced smaller particle size granules compared to wet granulation method. ODT produced from freeze drying method had shorter disintegration time compared to ODT from wet granulation batch. In conclusion, a novel co-processed excipient comprised of xylitol, starch and crospovidone XL-10, produced using freeze drying method with fast disintegration time, good compressibility and palatability was developed and characterized. The co-processed excipient is suitable for ODT application.

Comparison of Disintegrant-addition Methods on the Compounding of Orodispersible Tablets.

Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.