Study and Evaluation of Release Kinetics of Tramadol HCl from Lipid Based Sustained Release Capsules by Melt Matrix

The aim of our study was to improve the dissolution of Tramadol hydrochloride (TH) via its semisolid filled lipid based capsules. Sustained release formulation is designed to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of single dose. Semisolid matrixes of TH were prepared by melt-matrix method and were filled in hard gelatin capsule shell (size 0). In this experiment, a mixture of Glycerol monostearate (GMS) and lipid materials like different lipophilic oils and surfactants were used to improve the matrix integrity and drug release. The effects of different oils like Arachis oil, Soyabean oil, castor oil, neobee oil and olive oil and different surfactants such as Span 80, Tween 80, PEG 400, Chremophore RH 40, Cremophor EL were analyzed by formulating at various ratios. The matrices were subjected to the paddle dissolution method using 900 ml of phosphate buffer (pH 6.8). The dissolution test was performed at 100 RPM and the temperature was set at 37 ± 0.50C. The amount of drug was measured from the absorbance with a UV spectrophotometer at 270 nm. The release of drug was plotted in zero order-, 1st order- and Higuchi-release patterns. The correlation coefficients values of the trend lines of the graphs revealed that the formulations best fit in Higuchian release pattern. So it can be said that the pharmaceutical quality of Tramadol HCl capsules can be improved by using a semisolid lipophilic matrix filled in hard gelatin capsules. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14572 Dhaka Univ. J. Pharm. Sci. 11(2): 137-145, 2012 (December)

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Formulation and evaluation of bilayer tablets: Glimepiride in floating drug delivery and Metformin in sustained release

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v10i3.1319 ◽

2019 ◽

Vol 10 (3) ◽

pp. 1602-1607

Author(s):

Harish Choodappa ◽

Subramanian Somaskandan

Keyword(s):

Drug Delivery ◽

Sustained Release ◽

Guar Gum ◽

Release Kinetics ◽

Dose Frequency ◽

Release Formulation ◽

Sustained Release Formulation ◽

Bilayer Tablets ◽

Weight Variation ◽

Floating Drug Delivery

In this study, we aimed to prepare bilayer tablets of Glimepiride in floating drug delivery and Metformin in sustained release formulation. Glimepiride is chosen in floating drug delivery to overcome the gastric irritation and gastric emptying time. Glimepiride was prepared by different polymers such as guar gum, xanthan gum, carbopol and sodium bicarbonate act as effervescent agent, and other excipients were mixed and compressed by direct compression as the first layer. Metformin was chosen in sustained release to reduce dose frequency using different polymer HPMC K100M, methylcellulose, PVP K30 in different ratio and other excipients were mixed and compressed as the second layer. The first layer and second layer are combined as a bilayer tablet. Tablets were evaluated for hardness, friability, thickness, weight variation; the In vitro studies were done for all formulation. Among all formulation, F2 was selected as best formulation and release kinetics studies were evaluated for formulation F2.

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Liqui-Mass Technology as a Novel Tool to Produce Sustained Release Liqui-Tablet Made from Liqui-Pellets

Pharmaceutics ◽

10.3390/pharmaceutics13071049 ◽

2021 ◽

Vol 13 (7) ◽

pp. 1049

Author(s):

Matthew Lam ◽

Nour Nashed ◽

Ali Nokhodchi

Keyword(s):

Drug Release ◽

Sustained Release ◽

Tween 80 ◽

Tween 20 ◽

Release Formulation ◽

Sustained Release Formulation ◽

Eudragit Rs ◽

Release Analysis ◽

Insoluble Drugs ◽

Eudragit Rs Po

The Liqui-Mass technology (also known as Liqui-Pellet technology) has shown promising results in terms of enhancing the drug release rate of water insoluble drugs in a simplistic approach. However, there is no current study on sustained-release formulation using the Liqui-Mass technology. In this study, an attempt was made to produce a sustained-release Liqui-Tablet for the first time using a matrix-based approach. The non-volatile co-solvent used in the investigation included Tween 80, Tween 20 and Kolliphor EL. The production of sustained-release propranolol hydrochloride Liqui-Tablet was successful, and data from the saturation solubility test and dissolution test did not show much difference among the mentioned non-volatile co-solvent. The best Liqui-Tablet formulation took 24 h for drug release to reach at around 100%. There seemed to be a synergistic retarding drug release effect when a non-volatile co-solvent and Eudragit RS PO were used together. The increase of Eudragit RS PO concentration increased the retardant effect. Kinetic drug release analysis suggests that the best formulation followed the Higuchi model. The flowability of pre-compressed Liqui-Tablet pellets had no issues and its size distribution was narrow. Liqui-Tablet was generally robust and most formulations passed the friability test. The study revealed that Liqui-Mass technology can be employed to sustain drug release.

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Preparation andin vitro/in vivocharacterisation of a melt pelletised paracetamol/stearic acid sustained release delivery system

Spectroscopy An International Journal ◽

10.1155/2004/989502 ◽

2004 ◽

Vol 18 (2) ◽

pp. 375-386 ◽

Cited By ~ 1

Author(s):

Mario Grassi ◽

Dario Voinovich ◽

Iztok Grabnar ◽

Erica Franceschinis ◽

Beatrice Perissutti ◽

...

Keyword(s):

Mathematical Model ◽

Sustained Release ◽

Stearic Acid ◽

Photoelectron Spectroscopy ◽

Release Kinetics ◽

Size Fraction ◽

Drug Dissolution ◽

Release Mechanism ◽

Release Formulation ◽

Sustained Release Formulation

The potential of a sustained release formulation for paracetamol produced by melt pelletisation was investigated. After the production of the pellets, based on the combination of stearic acid as a melting binder and anhydrous lactose as a filler, the 3000–2000μm size fraction was selected in the light of the promisingin vitrodissolution results for further characterisations, including scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), specific surface area and true density determination. Hence the release mechanism was analysed with the help of an appropriate mathematical model. The mathematical model was built on the hypotheses that drug diffusion and solid drug dissolution in the release environment are the key phenomena affecting drug release kinetics. Bioavailability of the developed formulation was evaluated in anin vivostudy in eight subjects.

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Formulation and Evaluation of Sustained Release Verapamil Hydrochloride Using Natural Polymers

International Journal of Applied Pharmaceutical Sciences and Research ◽

10.21477/ijapsr.v1i2.10179 ◽

2016 ◽

Vol 1 (02) ◽

pp. 76-87

Author(s):

B. Ramu ◽

S. Ullas Kumar ◽

G. Srikanth ◽

Bigala Rajkamal

Keyword(s):

Drug Release ◽

Sustained Release ◽

Guar Gum ◽

Release Kinetics ◽

Natural Polymers ◽

Release Formulation ◽

Verapamil Hydrochloride ◽

Sustained Release Formulation ◽

Release Pattern ◽

Zero Order Release

The aim of the present study was to develop sustained release formulation of Verapamil Hydrochloride to maintain constant therapeutic levels of the drug for over 12 hrs. Various grades of HPMC polymers, Guar gum, and Xanthum gum were employed as polymers. Verapamil Hydrochloride dose was fixed as 120 mg. Total weight of the tablet was considered as 400 mg. Polymers were used in the concentration of 60, 120 and 180 mg concentration. All the formulations were passed various physicochemical evaluation parameters and they were found to be within limits. Whereas from the dissolution studies it was evident that the formulation (F6) showed better and desired drug release pattern i.e.,96.10 % in 12 hours containing Guar gum polymer in the concentration of 180mg. It followed zero order release kinetics. For the optimized formulation alcohol effect has been studied by using various concentrations of alcohol in dissolution medium. As the concentration of alcohol increased the sustained action of polymer was decreased. Hence it was concluded that alcohol has significant effect on drug release pattern.

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Formulation of Isoniazide Sustained Release Formulation by Using Carbopol 934 P

International Journal of Applied Pharmaceutical Sciences and Research ◽

10.21477/ijapsr.v1i2.10177 ◽

2016 ◽

Vol 1 (02) ◽

pp. 60-69

Author(s):

Addanki Gopikrishna ◽

B. Ramu ◽

G. Srikanth ◽

Bigala Rajkamal

Keyword(s):

Sustained Release ◽

Guar Gum ◽

Release Kinetics ◽

Zero Order ◽

Release Formulation ◽

Sustained Release Formulation ◽

Dissolution Studies ◽

Zero Order Release ◽

Physicochemical Evaluation ◽

Evaluation Parameters

The aim of the present study was to develop sustained release formulation of Isoniazide to maintain constant therapeutic levels of the drug for over 12 hrs. Various polymers such as Guar gum, HPMCK100 M, PEG 6000 and Carbopol 934 p were employed as polymers. Isoniazide dose was fixed as 100 mg. Total weight of the tablet was considered as 400 mg. Polymers were used in the concentration of 100, 150 and 200 mg. All the formulations passed various physicochemical evaluation parameters and they were found to be within limits. Whereas from the dissolution studies it was evident that the formulation (F6) showed better and desired drug release pattern i.e.,96.10 % in 12 hours. It followed zero order release kinetics.

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Formulation Optimization of Sustained Release Resinate Microcapsules of Tramadol Hydrochloride by Using 3/2 Factorial Design

International Journal of Pharmaceutical and Phytopharmacological Research ◽

10.24896/eijppr.2016621 ◽

2017 ◽

Vol 6 (2) ◽

pp. 57

Author(s):

Kamble Ravindra K. ◽

Chauhan Chetan S. ◽

Kamble Priyadarshani R. ◽

Naruka Pushpendra S.

Keyword(s):

Drug Delivery ◽

Ion Exchange ◽

Sustained Release ◽

Factorial Design ◽

Linear Regression Analysis ◽

Extended Period ◽

Multiple Linear Regression Analysis ◽

Water Soluble ◽

Tramadol Hydrochloride ◽

Release Drug

The main aim of the present work was to develop the microcapsules of tramadol hydrochloride for the oral sustained release drug delivery. Tramadol hydrochloride a BCS class I drug a centrally acting synthetic analgesic was complexed with Indion 254 ion exchange resin. The microcapsules were prepared by encapsulating the prepared resinates by o/o solvent evaporation technique. In the investigation 32 full factorial design was used to investigate the joint influence of two formulation variable amount of eudragit RS 100 and plasticized PEG 400. The results of multiple linear regression analysis indicated that for obtaining a sustained release drug delivery the optimum concentrations of both the plasticizer and coating solution to be used. The factorial models were used to prepare optimized microcapsules and optimized formulations showed sustained release profiles for the extended period of more than 12 hrs. From the present investigations concluded that resinate microcapsules of highly water soluble drug can provide controlled release of drug for extended period.Key Words: Tramadol hydrochloride, ion exchange resinate, microcapsules, sustained release

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