Enhanced Bioavailability and Dissolution of Atorvastatin Calcium from Floating Microcapsules Using Minimum Additives

Khan, Furquan Nazimuddin

doi:10.3797/scipharm.1104-26

Cited by 19 publications

(12 citation statements)

References 9 publications

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“…However, it has low water solubility (0.142 mg/ml) [5]. Research shows that a tablet of AC on the market has a solubility and dissolution efficiency of 55 and 46%, respectively [6,7], therefore, these poor properties cause the drug's oral bioavailability to be only about 12% [5,8,9,10]. This phenomenon occurs because the oral bioavailability of AC is limited by its solubility and dissolution rates [5].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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Atorvastatin calcium (AC) is a statin drug used to lower cholesterol. Its crystalline form is usually found in the market with low solubility properties. The amorphization of crystalline AC is a technique used to increase its solubility however; the amorphous form has less thermodynamic stability. Therefore, to increase the solubility properties of its crystalline form, an AC coamorphous solid was prepared. This coamorphous solid was prepared using spray drying techniques, and coformers such as isonicotinamide (INA) and maleic acid (MA). Furthermore, characterization was carried out using powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy, and scanning electron microscopy, while the solubility properties test was conducted using the shake-flask and paddle method. The results showed that the spray-dried solids were coamorphous with single-phase homogeneous systems. Furthermore, the coamorphous solids, AC-INA and AC-MA were found to have a higher Tg than the melting points of other components, and formed intermolecular interactions between them. The higher Tg and presence of intermolecular interactions indicate that coamorphous solids are more stable than the amorphous form. Therefore, the results of the solubility and dissolution test showed that the coamorphous solid of AC-INA and AC-MA have better solubility properties compared to the AC crystalline form.

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Section: Introductionmentioning

confidence: 99%

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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“…In smaller monogastric herbivorous animals, such as rabbits, where gastric emptying is slower than dogs and can be greater than 24 hours 13 , gastric resident systems may be more amendable to prolonged resident times for drug release. Khan and Dehghan 22 looked at increased bioavailability of atorvastatin calcium when floating tablets were administered and drug released over a duration of 6 hours in rabbits. Thakar 23 reported floating retention times of 12 hours in rabbits and improved bioavailability of baclofen compared to the marketed sample.…”

Section: Introductionmentioning

confidence: 99%

Scalable Gastric Resident Systems for Veterinary Application

Bensel

Mazdiyasni

Rogner

et al. 2018

Sci Rep

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Gastric resident dosage forms have been used successfully in farm animals for the delivery of a variety of drugs helping address the challenge of extended dosing. Despite these advances, there remains a significant challenge across the range of species with large variation in body size. To address this, we investigate a scalable gastric resident platform capable of prolonged retention. We investigate prototypes in dimensions consistent with administration and retention in the stomachs of two species (rabbit and pig). We investigate sustained gastric retention of our scalable dosage form platform, and in pigs show the capacity to modulate drug release kinetics of a model drug in veterinary practice, meloxicam, with our dosage form. The ability to achieve gastric residence and thereby enable sustained drug levels across different species may have a significant impact in the welfare of animals in both research, agricultural, zoological, and clinical practice settings.

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“…The samples were analyzed spectrophotometrically at 246nm. [15][16] The release kinetics was fitted into various models using PCP dissolution v 2.08 software.…”

Section: Disintegration Testmentioning

confidence: 99%

Comparative assessment of different marketed brands of atorvastatin tablets in Asir region, Saudi Arabia

Rahamathulla

2018

MOJDDT

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IntroductionAtorvastatin (AVS) is lipid-lowering agent, which is selective, competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme. A reductase which catalyzes the conversion of HMG-CoA to mevalonate, which is a rate limiting step in cholesterol biosynthesis. AVS decreases the levels of low-density lipoprotein (bad cholesterol) and triglycerides in the blood, while enhancing the levels of highdensity lipoprotein (good cholesterol). 1-2 The empirical formula of AVS calcium is (C33H34FN2O5)2Ca2+·3H 2 O with a molecular weight of 1209.42, as shown in Figure 1. AVS is widely used to treat high cholesterol, to lower the risk of heart attack, myocardial infarction, angina, stroke, and other heart complications in people with type II diabetes and coronary heart disease. The dosage range of AVS is 10-80mg once a daily as a single dose with or without food at any time of the day. [3][4] The starting recommended dose of AVS is 10-20mg once daily, rapidly absorbed after oral administration. The half-life is approximately 12h, extensively metabolized to ortho-and para-hydroxylated derivatives and various beta-oxidation products (cytochrome P450 3A4) in the liver (hepatic metabolism) and a small amount of the drug metabolates from urine, elimination is mainly through bile. 5-7 Oral dosage forms are safest and commonest route of drug administration. The efficacy of the dosage systems can be assured when its quality is reliable. 8 The efficacy of pharmaceutical dosage systems usually depends on their formulation and manufacturing techniques, therefore the quality of dosage system may vary. [9][10][11] In this research to assess the quality/bioequivalence study of four different AVS marketed tablets (10mg) currently available in Asir region, kingdom of Saudi Arabia. They were chosen for the study to survey AVS tablets in terms of product quality and price difference in the various brands. This research was carried out for general organoleptic test, structural defects, and comparative evaluation of official and non-official quality control test such as thickness, diameter, friability, hardness, drug content uniformity, weight variation, in vitro dissolution studies, kinetic release of drug, and statistical analysis of AVS marketed/commercially available tablets, which is very useful for pharmacists and health care professionals in order to determine the interchangeability. Materials and methods MaterialsFour different marketed brands/samples of Atorvastatin calcium tablets (10mg) were purchased from community pharmacy (drug store) in Abha city, Asir region. The samples were properly checked for their drug dose, manufacturing license number, batch numbers, manufacturing and expiry dates. They were coded as A-D the details of all samples were shown in Table 1. The other solvents and chemical used in the study was analytical grade. MethodsThese are the following official and non-official quality control tests 12 are carried out during the study of different marketed brands of AVS. Uniformity of weightAccording to USP, Twenty (...

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Enhanced Bioavailability and Dissolution of Atorvastatin Calcium from Floating Microcapsules Using Minimum Additives

Cited by 19 publications

References 9 publications

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Scalable Gastric Resident Systems for Veterinary Application

Comparative assessment of different marketed brands of atorvastatin tablets in Asir region, Saudi Arabia

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