Comparative release profile of sustained release matrix tablets of verapamil HCl

Aim: The term modified-release drug product is used to describe products that alter the timing and/or the rate of release of the drug substance.Objective: The objective of the present study was to formulate and evaluate the sustained release matrix tablet of venlafaxine hydrochloride.Methods: Venlafaxine hydrochloride is a structurally novel antidepressant for oral administration. It is widely prescribed for the treatment of depression, generalized anxiety disorder, and social anxiety disorder. Venlafaxine hydrochloride is currently available as immediate release tablet and as an extended release capsules under the brand names of Effexor (WYETH AYERST) and Effexor XR (WYETH AYERST). The biological half-life of venlafaxine very short (5 h) and the dose is to be taken 2–3 times a day and the recommended maximum daily dose is 75–450 mg/day. Venlafaxine hydrochloride is an antidepressant and so it is to be taken for quite a long period. Hence, to reduce the dosing frequency, simple, lower cost sustained release tablets of venlafaxine were preferred for the development.Conclusion: The venlafaxine hydrochloride sustained release matrix tablets shown controlled release profile as per the release profile ofthe innovator is EffexorTm_XR. The sustained release of this matrix tablet reduces the dosing frequency and reduces the side effects, bywhich in a long-term therapy, it may be useful as a product with patient compliance for the treatment of major depression disorder.

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Studies in Preparation and Evaluation of pH‐Independent Sustained‐Release Matrix Tablets of Verapamil HCl Using Directly Compressible Eudragits

Pharmaceutical Development and Technology ◽

10.1081/pdt-120024686 ◽

2003 ◽

Vol 8 (4) ◽

pp. 323-333 ◽

Cited By ~ 15

Author(s):

Mukesh C. Gohel ◽

Tejas P. Patel ◽

Shital H. Bariya

Keyword(s):

Sustained Release ◽

Matrix Tablets ◽

Verapamil Hcl ◽

Preparation And Evaluation

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Effects of release modifier on Carvedilol release from Kollidon SR based matrix

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i8.11095 ◽

2012 ◽

Vol 1 (8) ◽

pp. 186 ◽

Cited By ~ 1

Author(s):

Urmi Das ◽

Mohammad Salim Hossain

Keyword(s):

Drug Release ◽

Sustained Release ◽

Microcrystalline Cellulose ◽

Matrix Tablets ◽

Dissolution Time ◽

Release Mechanism ◽

Matrix Tablet ◽

Weight Variation ◽

The Matrix ◽

Tablet Formulations

Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a> International Current Pharmaceutical Journal 2012, 1(8): 186-192

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A Novel Design of Tri-Layer Membrane with Controlled Delivery of Paclitaxel and Anti-Biofilm Effect for Biliary Stent Applications

Nanomaterials ◽

10.3390/nano11020486 ◽

2021 ◽

Vol 11 (2) ◽

pp. 486

Author(s):

Abdelrahman I. Rezk ◽

Jeesoo Park ◽

Joon Yeon Moon ◽

Sunny Lee ◽

Chan Hee Park ◽

...

Keyword(s):

Sustained Release ◽

Antibacterial Effect ◽

Release Profile ◽

Biliary Stent ◽

Fickian Diffusion ◽

Release Mechanism ◽

Dual Function ◽

Electrospinning Technique ◽

Layer Membrane

Here, we developed a novel biliary stent coating material that is composed of tri-layer membrane with dual function of sustained release of paclitaxel (PTX) anticancer drug and antibacterial effect. The advantages of using electrospinning technique were considered for the even distribution of PTX and controlled release profile from the nanofiber mat. Furthermore, film cast method was utilized to fabricate AgNPs-immobilized PU film to direct the release towards the tumor site and suppress the biofilm formation. The in vitro antibacterial test conducted against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria species showed excellent antibacterial effect. The in vitro drug release study confirmed the sustained release of PTX from the tri-layer membrane and the release profile fitted first order with correlation coefficient of R2 = 0.98. Furthermore, the release mechanism was studied using Korsmeyer–Peppas model, revealing that the release mechanism follows Fickian diffusion. Based on the results, this novel tri-layer membrane shows curative potential in clinical development.

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Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial

Pharmaceutics ◽

10.3390/pharmaceutics13060804 ◽

2021 ◽

Vol 13 (6) ◽

pp. 804

Author(s):

Ewelina Juszczyk ◽

Kamil Kisło ◽

Paweł Żero ◽

Ewa Tratkiewicz ◽

Maciej Wieczorek ◽

...

Keyword(s):

Clinical Trial ◽

Sustained Release ◽

Development Strategy ◽

Matrix Tablets ◽

Matrix Tablet ◽

Mechanical Agitation ◽

Development Cycle ◽

Dissolution Tests ◽

Sustained Release Tablets ◽

Biopharmaceutical Properties

Sustained-release (SR) formulations may appear advantageous in first-in-human (FIH) study of innovative medicines. The newly developed SR matrix tablets require prolonged maintenance of API concentration in plasma and should be reliably assessed for the risk of uncontrolled release of the drug. In the present study, we describe the development of a robust SR matrix tablet with a novel G-protein-coupled receptor 40 (GPR40) agonist for first-in-human studies and introduce a general workflow for the successful development of SR formulations for innovative APIs. The hydrophilic matrix tablets containing the labeled API dose of 5, 30, or 120 mg were evaluated with several methods: standard USP II dissolution, bio-predictive dissolution tests, and the texture and matrix formation analysis. The standard dissolution tests allowed preselection of the prototypes with the targeted dissolution rate, while the subsequent studies in physiologically relevant conditions revealed unwanted and potentially harmful effects, such as dose dumping under an increased mechanical agitation. The developed formulations were exceptionally robust toward the mechanical and physicochemical conditions of the bio-predictive tests and assured a comparable drug delivery rate regardless of the prandial state and dose labeled. In conclusion, the introduced development strategy, when implemented into the development cycle of SR formulations with innovative APIs, may allow not only to reduce the risk of formulation-related failure of phase I clinical trial but also effectively and timely provide safe and reliable medicines for patients in the trial and their further therapy.

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Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502011000300012 ◽

2011 ◽

Vol 47 (3) ◽

pp. 545-553 ◽

Cited By ~ 2

Author(s):

Sathis Kumar Dinakaran ◽

Santhos Kumar ◽

David Banji ◽

Harani Avasarala ◽

Venkateshwar Rao

Keyword(s):

Sustained Release ◽

In Vitro Release ◽

Chemical Properties ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Floating Tablets ◽

Ir Studies ◽

Weight Variation ◽

The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

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