Formulation, Optimization and Evaluation of Bilayer Tablet of Antihypertensive Drug

Hypertension or high blood pressure occurs when the high cardiac output exerts pressure on the arterial wall as the blood flow increases. Bi-layer tablets are prepared with one layer of drug for immediate release while second layer designed to release drug later, either as second dose or in an extended release manner. Bi-layered tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances, and also for sustained release tablet in which one layer is immediate release as initial dose and second layer is maintenance dose. Bilayer tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances and also for sustained release tablet in which one Layer is immediate release as initial dose and second layer is maintenance dose. The preparation of tablets in the form of multi layers is used to provide systems for the administration of drugs. Keywords: Hypertension, Bi-layered tablet, Enalapril, Immediate release and Sustained release.

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Optimized chronomodulated dual release bilayer tablets of fexofenadine and montelukast: quality by design, development, and in vitro evaluation

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-019-0006-9 ◽

2019 ◽

Vol 5 (1) ◽

Cited By ~ 1

Author(s):

Bhupendra Singh ◽

Geetanjali Saini ◽

Manish Vyas ◽

Surajpal Verma ◽

Sourav Thakur

Keyword(s):

Drug Release ◽

Sustained Release ◽

Quality By Design ◽

Immediate Release ◽

Oral Dosage ◽

Nocturnal Asthma ◽

Sustained Release Tablet ◽

Bilayer Tablets ◽

Dual Release ◽

Release Tablet

Abstract Background The conventional oral dosage forms are not effective in dealing with chronopathological conditions, such as nocturnal asthma. Therefore, there is an unmet need to develop a delivery system that can deliver drug as per the chronopharmacology of the diseases. The purpose of the study is to use quality by design (QbD) technique and pulsatile principles for the development of Eudragit-coated dual release bilayer tablets. The dual layer consists of immediate release layer of fexofenadine HCl and sustained release layer of montelukast sodium. Results The quality target product profile of the formulation was developed, and the critical quality attributes were identified. Three-level, three-factor Box-Behnken design was used for the optimization of the bilayer tablets. Based on the design, a total of 13 formulation combinations (F1–F13 and M1–M13) were made having acceptable micromeritic properties. The developed immediate and sustained release layers were evaluated for physicochemical properties. Depending upon the value of the diffusion exponent, the Fickian diffusion mechanism is dominant among immediate and sustained release tablet layers. Response curve for immediate release layer showed that concentrations of sodium starch glycolate and sodium bicarbonate had a negative effect on disintegration time and a positive effect on drug release. For sustained release tablet layer, concentrations of HPMC E 5 LV and magnesium stearate had a significant effect on drug release. The ANOVA and diagnostic plots confirmed the significance and goodness of fit of the used model. Based on desirability plot values, optimized formulation was developed and coated with Eudragit coat. The coated bilayer tablet showed met the requirement of providing an immediate release during the first hour and a sustained release action for a period of more than 8 h after passing the gastric region. Conclusions The formulation can be fruitful in curbing the menace of nocturnal asthma and providing a high degree of patient compliance as the patient will not have to wake up at night to take the medication.

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Steady-state human pharmacokinetics and bioavailability of guaifenesin and pseudoephedrine in a sustained-release tablet relative to immediate-release liquids

International Journal of Pharmaceutics ◽

10.1016/0378-5173(94)00235-w ◽

1995 ◽

Vol 114 (2) ◽

pp. 171-176 ◽

Cited By ~ 4

Author(s):

Daniel L. Wagner ◽

Vikram S. Patel

Keyword(s):

Steady State ◽

Sustained Release ◽

Immediate Release ◽

Human Pharmacokinetics ◽

Sustained Release Tablet ◽

Release Tablet

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Bioanalytical method development and validation for estimation of formulated sustained release tablet of Nateglinide in Rabbit plasma.

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2019.11.01.040 ◽

2019 ◽

Vol 11 (1) ◽

Keyword(s):

Sustained Release ◽

Method Development ◽

Rabbit Plasma ◽

Bioanalytical Method ◽

Sustained Release Tablet ◽

Method Development And Validation ◽

Development And Validation ◽

Release Tablet

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Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽

10.3390/pharmaceutics11060260 ◽

2019 ◽

Vol 11 (6) ◽

pp. 260 ◽

Cited By ~ 4

Author(s):

Dongwei Wan ◽

Min Zhao ◽

Jingjing Zhang ◽

Libiao Luan

Keyword(s):

Citric Acid ◽

Drug Release ◽

Sustained Release ◽

Release Rate ◽

Diffusion Rate ◽

Immediate Release ◽

Pharmacokinetic Studies ◽

Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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Sustained release tablet formulation of diethylcarbamazine. Part II

International Journal of Pharmaceutics ◽

10.1016/0378-5173(85)90034-1 ◽

1985 ◽

Vol 24 (2-3) ◽

pp. 355-358 ◽

Cited By ~ 4

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

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

INDIAN DRUGS ◽

10.53879/id.56.03.11715 ◽

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.

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