Formulation, in-vitro release and therapeutic effect of hydrogels based controlled release tablets of propranolol hydrochloride

AbstractThe aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids. The results suggest that both analogues, albeit more lipophilic than SQ109, and aminoethers (I) and (II), have the requisite in vitro release characteristics for oral administration. In conclusion, these formulations merit further assessment by conducting in vivo studies, at a later stage.

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Fabrication, in vitro and in vivo Characterization of Solid Dispersion - Microsphere Controlled Release System for Lornoxicam

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681210999200909112738 ◽

2020 ◽

Vol 10 ◽

Author(s):

Suraj Nupane ◽

Dipti Srivastava ◽

Mohini Chaurasia ◽

Himani Awasthi

Keyword(s):

Controlled Release ◽

Solid Dispersion ◽

In Vitro Release ◽

Immediate Release ◽

Effective Management ◽

Release Pattern ◽

Peg 4000 ◽

Vitro Release ◽

Release Form

Background: Lornoxicam is widely used for its anti-inflammatory, analgesic and antipyretic properties. However, it suffers from the limitations of possessing a relatively short elimination half-life ranging from 3 to 5 h, thereby; leading to repeated dosing which in turn may cause local irritation and ulceration. In addition, LXM also exhibits pHdependent solubility. Effective management of inflammation in diseases such as arthritis requires the formulation of delivery systems that may be able to provide immediate release of drug for instant relief which shall be maintained for a prolonged period. Objective: The present research work was aimed to modify the release pattern of poorly water-soluble drug Lornoxicam by designing a biphasic tablet comprising of solid dispersion (immediate release form) and microspheres (controlled release form) for the effective management of inflammation. Methods: The solid dispersion (SD) was prepared by melting method using PEG 4000 and tween 80 and formation was confirmed by Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (PXRD) studies. Polymeric microspheres loaded with Lornoxicam were prepared by ‘Emulsion Solvent-Evaporation’ method using Eudragit S-100 and Eudragit L-100. Microspheres (MS) were evaluated for drug entrapment efficiency, drug loading, drug content, particle size and in vitro release behaviour. Optimized microspheres (polymer concentration 0.5% w/v and drug concentration 0.1% w/v and solid dispersion (drug: PEG 4000: 4:6) were compressed in the ratio of 1:3 to produce biphasic tablet. The prepared tablets were evaluated for various pre-compression and post-compression parameters. Antiinflammatory activity of the F4, M6 and the combination of SD and Microspheres in a ratio of 1:3 was carried out by Carrageenan induced paw edema method in Wistar rats. Results: The solid dispersions prepared by melting technique showed an enhanced dissolution rate as compared to the pure drug. LXM microspheres exhibited a sustained drug release. In vitro release of lornoxicam from biphasic tablets showed that 20 % of the drug released at the end of first one hour, followed by 33% release at the end of 4th h and maximum release of 94.1 % at the end of 10 h. The prolonged effect continued till the end of 12 h. Results showed that the mixture of MS + SD exhibited 48 % inhibition in 30 min which is increased to 88.63% at the end of 4 h which can be explained by initial burst release from the soluble layer of SD (which gave initial required effective concentration of Lornoxicam) followed by sustained release from matrix of microspheres (which maintained required level of Lornoxicam in blood). Conclusion: A successful modification of the release pattern of LXM was achieved by designing a biphasic tablet comprising of solid dispersion for the effective management of inflammation.

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Controlled Release of Extract of Morus nigra from Eudragit L-100 Electrospun Fibers: Toxicity and in vitro Release Evaluation

Current Traditional Medicine ◽

10.2174/2215083803666170309123836 ◽

2017 ◽

Vol 3 (2) ◽

Author(s):

Juliana M. D. Soares ◽

Jackson R.G.S. Al`meida ◽

Helinando P. de Oliveira

Keyword(s):

Controlled Release ◽

In Vitro Release ◽

Electrospun Fibers ◽

Morus Nigra ◽

Vitro Release

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Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502014000400016 ◽

2014 ◽

Vol 50 (4) ◽

pp. 799-818 ◽

Cited By ~ 2

Author(s):

Tariq Ali ◽

Muhammad Harris Shoaib ◽

Rabia Ismail Yousuf ◽

Sabahat Jabeen ◽

Iyad Naeem Muhammad ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

In Vitro Release ◽

Angle Of Repose ◽

In Vitro Dissolution ◽

Physical Parameters ◽

Disintegration Time ◽

Weight Variation ◽

Vitro Release

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

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Controlled Release of Doxycycline by Magnetized Microporous MIL53(Fe); Focus on Magnetization and Drug Loading

Current Drug Delivery ◽

10.2174/1567201815666180926120525 ◽

2018 ◽

Vol 16 (1) ◽

pp. 42-50 ◽

Cited By ~ 2

Author(s):

Shakiba Naeimi ◽

Hossein Faghihian

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Drug Loading ◽

In Vitro Release ◽

Time Intervals ◽

Drug Content ◽

Releasing Process ◽

Phosphate Buffered Saline ◽

Vitro Release

Background: In this research, MIL-53(Fe) was magnetized and the performance of the magnetized material as a drug delivery system for doxycycline was studied. Objectives: The experiments were designed to load the magnetic delivery compounds with different amount of the drug. Methods: The in vitro release rate of doxycycline from magnetic MIL-53(Fe) with different drug content into saline buffered fluid (SBF, pH=7.4) and phosphate buffered saline (PBS, pH=3) was then studied. Results: The results showed that the releasing process of the drug in PBS media achieved the equilibration within 48h with 98% of releasing efficiency, while the releasing process in SBF media (pH=7.4) was slower and the equilibrium was established within 264 h with the releasing efficiency of 95%. The amount of the released doxycycline from the samples with different drug content was measured at various time intervals. Conclusion: It was concluded that in PBS media after 75 h, 85, 95 and 98% of loaded doxycycline released, respectively, from the sample containing 22, 32 and 35% of the drug. In SBF media, the release was slower and after 350 h, 82, 91 and 95% of loaded doxycycline released from the samples, respectively, containing 22, 32 and 35 % of the drug. The results of this study indicated that by use of drugreleasing profile and selecting appropriate carrier dose, the released amount of the drug into the patient body can be controlled.

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IMPACT OF HYDROXYPROPYL METHYLCELLULOSE (HPMC) TYPE AND CONCENTRATION ON THE SWELLING AND RELEASE PROPERTIES OF PROPRANOLOL HYDROCHLORIDE MATRIX TABLETS USNING A SIMPLEX CENTROID DESIGN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i2.31127 ◽

2019 ◽

pp. 143-151

Author(s):

PAKORN KRAISIT

Keyword(s):

Hydroxypropyl Methylcellulose ◽

In Vitro Release ◽

Matrix Tablets ◽

Direct Compression ◽

Propranolol Hydrochloride ◽

Buffer Solution ◽

Solution Ph ◽

Vitro Release

Objective: To prepare hydroxypropyl methylcellulose (HPMC) matrix tablets of propranolol hydrochloride (PNL) using a simplex centroid design. Methods: HPMC matrix tablets with different amounts and types of HPMC were prepared by direct compression. A simplex centroid design was used to evaluate tablet weight (Y1), thickness (Y2), hardness (Y3), axial swelling time at 0.5–12 h (Y4-Y9), radial swelling time at 0.5–12 h (Y10-Y15), and % released at 1–12 h (Y16-Y19). Results: The tablet weight, thickness, and hardness were 397.6–400.4 mg, 3.967–4.029 mm, and 106.9–139.0 N, respectively. The % swelling (axial) and % swelling (radial) at 0.5–12 h were-8.715 to 59.889 and-1.887 to 49.287, respectively. The negative % swelling could be attributed to erosion of the tablets. The in vitro release of PNL from the tablets in buffer solution pH 1.2 (1 h) and pH 7.5 (3–12 h) was 21.12–76.22%. Tables with a high proportion of K100M HPMC had high PNL release, and the mechanism of PNL release was diffusion-and erosion-controlled. Conclusion: The simplex centroid design is potentially advantageous for formulating PNL-HPMC matrix tablets.

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