scholarly journals Application of the Solid Dispersion Method to Controlled Release of Medicine. II. Sustained Release Tablet Using Solid Dispersion Granule and the Medicine Release Mechanism.

1992 ◽  
Vol 40 (6) ◽  
pp. 1592-1596 ◽  
Author(s):  
Hiroshi YUASA ◽  
Tetsuya OZEKI ◽  
Yoshio KANAYA ◽  
Katsutoshi OISHI
Keyword(s):  
Controlled Release ◽  
Sustained Release ◽  
Solid Dispersion ◽  
Release Mechanism ◽  
Dispersion Method ◽  
Sustained Release Tablet ◽  
Release Tablet

scholarly journals Increased Bioavailability of β-Alanine by a Novel Controlled-Release Powder Blend Compared to a Slow-Release Tablet

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1517
Author(s):  
Lydia de Salazar ◽  
Ignacio Segarra ◽  
Francisco Javier López-Román ◽  
Antonio Torregrosa-García ◽  
Silvia Pérez-Piñero ◽  
...  
Keyword(s):  
Single Dose ◽  
Controlled Release ◽  
Side Effects ◽  
Sustained Release ◽  
Pharmacokinetic Analysis ◽  
Prediction Ability ◽  
Powder Blend ◽  
Sustained Release Tablet ◽  
Sensory Score ◽  
Release Tablet

Background: β-Alanine is a sport supplement with increasing popularity due to its consistent ability to improve physical performance, with the downside of requiring several weeks of supplementation as imposed to the maximum daily and single dose tolerated without side effects (i.e., paresthesia). To date, the only alternative to overcome this problem has been use of a sustained-release tablet, while powders are the most commonly used format to deliver several grams of amino acids in a single dose. In this study we assessed the bioavailability, pharmacokinetics and paresthesia effect of β-alanine after administration in a novel controlled-released powder blend (test) versus a sustained-release tablet (reference). Methods: Twelve subjects (25.6 ± 3.2 y, 50% female) participated in a randomized, single-blind, crossover study. Each participant was administered orally the test (β-alanine 8 g, l-histidine 300 mg, carnosine 100 mg) or the reference product (10 tablets to reach β-alanine 8 g, Zinc 20 mg) with a 1-week washout period. β-Alanine plasma concentrations (0–8 h) were determined by LC-MS/MS and model-independent pharmacokinetic analysis was carried out. Paresthesia intensity was evaluated using a Visual Analog Score (VAS) and the categorical Intensity Sensory Score (ISS). Results: The CMAX and AUC0→∞ increased 1.6- and 2.1-fold (both p < 0.001) in the test product, respectively, which yielded 2.1-fold higher bioavailability; Ka decreased in the test (0.0199 ± 0.0107 min−1) versus the reference (0.0299 ± 0.0121 min−1) product (p = 0.0834) as well as V/F and Cl/F (both p < 0.001); MRT0→last increased in the test (143 ± 19 min) versus reference (128 ± 16 min) formulation (p = 0.0449); t1/2 remained similar (test: 63.5 ± 8.7 min, reference: 68.9 ± 9.8 min). Paresthesia EMAX increased 1.7-fold using the VAS (p = 0.086) and the ISS (p = 0.009). AUEC increased 1.9-fold with the VAS (p = 0.107) and the ISS (p = 0.019) reflecting scale intrinsic differences. Pharmacokinetic-pharmacodynamic analysis showed a clockwise hysteresis loop without prediction ability between CMAX, AUC0→∞ and EMAX or AUEC. No side effects were reported (except paresthesia). Conclusions: The novel controlled-release powder blend shows 100% higher bioavailability of β-alanine, opening a new paradigm that shifts from chronic to short or mid-term supplementation strategies to increase carnosine stores in sports nutrition.

scholarly journals FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE TABLET USING MARDI GUM

2021 ◽  
pp. 52-55
Author(s):  
MANGESH M KUMARE ◽  
GIRIDHAR R SHENDARKAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Research Work ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Sustained Release Tablet ◽  
Weight Variation ◽  
Release Tablet

Objective: The present research work was to develop and evaluate alprazolam sustained release tablet using Mardi gum, a comparative study on binding properties of gum and hydroxypropyl methylcellulose (HPMC) was performed. Methods: Formulation of alprazolam tablets (f1–f6) was done by direct compression method using 15%, 30%, and 45% concentration of gum as a natural binder, and HPMC was used as synthetic matrix forming agent. Microcrystalline cellulose was used as diluents, talc, and magnesium stearate as a lubricant and PVP K30 as the binder. The formulated batches were evaluated for parameters such as tablet thickness, % friability, hardness, weight variation, and in vitro drug release characteristics. The release information was fitted into different dynamics models to decide the release mechanism of the drug. Results: The results showed that all the parameters of the developed tablets (f1–f6) were in fulfillment with pharmacopeia limits. In vitro, drug release studies showed that formulation f1 had most controlled and sustained manner releaser with maximum drug release of 97.89±0.52% in 18 h with comparison to f2–f4 and f6 drug release is 98.12±0.55%, 97.24±0.57%, 98.16±0.74%, and 97.26±0.35%, respectively, in 16 h and f5 giving 97.89±0.85% release in 14 h. Conclusion: On the basis of obtained result, it can be concluded that Mardi gum can be used to sustain the drug release as a natural polymer in tablet dosage form.

Sustained release tablet formulation of diethylcarbamazine. Part II

1985 ◽  
Vol 24 (2-3) ◽  
pp. 355-358 ◽  
Author(s):  
S.K. Baveja ◽  
K.V. Ranga Rao ◽  
Rajinder Kumar ◽  
K. Padmalatha Devi
Keyword(s):  
Sustained Release ◽  
Tablet Formulation ◽  
Sustained Release Tablet ◽  
Release Tablet

DESIGN DEVELOPMENT AND OPTIMIZATION OF A SUSTAINED RELEASE TABLET OF BOSENTAN MONOHYDRATE FOR PULMONARY ARTERIAL HYPERTENSION

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 61-67
Author(s):  
P. P Dighe ◽  
H. M Tank ◽  
Keyword(s):  
Pulmonary Arterial Hypertension ◽  
Sustained Release ◽  
Arterial Hypertension ◽  
In Vitro Release ◽  
Design Development ◽  
23 Factorial Design ◽  
Sustained Release Tablet ◽  
Pulmonary Arterial ◽  
Release Tablet

Pulmonary arterial hypertension (PAH) means high blood pressure in the lungs caused by obstruction in the small arteries of the lungs.The current study involves the fabrication of oral matrix sustained release tablet of bosentan monohydrate, a dual endothelin receptor antagonist, the optimisation of its in vitro release and characterisation. Methocel K4M PremiumDC2, a directly compressible HPMC grade, has been used as the sustained release polymer. Pregelatinised starch is used as a diluent and release modifier and sodium lauryl sulphate as a solubiliser. The influence of the above variables on drug release is measured using a 23 factorial design using design expert software. Surface response plots show significant interaction among the formulation variables, thus aiding in optimization of bilayer tablet.

scholarly journals Preparation and Evaluation of Nifedipine sustained release Tablet by using Natural Gums as release retardant

2014 ◽  
Vol 01 (03) ◽  
pp. 78-84 ◽  
Author(s):  
Gayatri D Medisetty ◽  
Girish B Botta ◽  
Uma maheshwari Yamana ◽  
Ashwini Avasarala
Keyword(s):  
Sustained Release ◽  
Sustained Release Tablet ◽  
Preparation And Evaluation ◽  
Release Tablet

Novel Chewable Sustained‐Release Tablet Containing Verapamil Hydrochloride

2004 ◽  
Vol 9 (2) ◽  
pp. 181-188 ◽  
Author(s):  
Omaima N. El‐Gazayerly ◽  
Vipaporn Rakkanka ◽  
James W. Ayres
Keyword(s):  
Sustained Release ◽  
Verapamil Hydrochloride ◽  
Sustained Release Tablet ◽  
Release Tablet
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