Effects of Manufacturing Process Variables on In Vitro Dissolution Characteristics of Extended-Release Tablets Formulated with Hydroxypropyl Methylcellulose

2003 ◽  
Vol 29 (1) ◽  
pp. 79-88 ◽  
Author(s):  
Ye Huang ◽  
Kavita H. Khanvilkar ◽  
Angela D. Moore ◽  
Marquetta Hilliard-Lott
Author(s):  
Asfiya Fatima ◽  
Mamatha Tirunagari ◽  
Divya Theja Chilekampalli

The main objective of the present study was to prepare and evaluate the instant release oral thin films of Flunarizine, in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The instant release oral thin films of Flunarizine were prepared by solvent casting method using film forming polymer like Hydroxypropyl Methylcellulose E-15. The film was evaluated for various physicochemical parameters that include thickness, weight variation, folding endurance, tensile strength, drug content and in vitro drug release studies. No differences were observed in in vitro dissolution of drug from the formulated film F1-F9 as the film instantly gets wet by dissolution medium. The drug release for F5 formulations was about 98.1%. The accelerated stability studies for the optimized film formulations F5 were performed that indicates that the formulated instant release oral thin films were unaffected after initial and 3 months storage under accelerated conditions.


2021 ◽  
Vol 74 (9) ◽  
pp. 2315-2322
Author(s):  
Firas Aziz Rahi ◽  
Muath Sheet Mohammed Ameen ◽  
Mohammed Shamil Fayyadh

The aim: This work aimed to formulate gliclazide and linagliptin extended-release nanoparticles. Materials and methods: A HPLC method was developed and validated to determine gliclazide and linagliptin at the same time without interference. The nanoparticles were prepared by emulsion solvent evaporation using two polymers, namely hydroxypropyl methylcellulose (HPMC) 4000 cps and xanthan gum. Results: Nanoparticles prepared were characterized for drug contents, production yield and entrapment efficiency, zeta potential, particle size, morphology by transmission electronic microscopy (TEM) and in-vitro release rate. The formulae GLH1, GLX1 and GHX1 showed release of linagliptin more than 75% after 8 hrs. While the only formula among the three (GHX1) showed release of gliclazide more than 80% after 8 h. So, the formula GHX1 showed acceptable release of more than 80% of both gliclazide and linagliptin after 8 h. Conclusions: The formula GHX1 which containing (0.5:1 xanthan gum: drugs) was the best nanoparticles formula which released more than 80% of both drugs after 8 h and could achieve good extended release over 24 h.


Author(s):  
TEJASWINI MANE ◽  
MUKESH MOHITE

Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.


Author(s):  
Naveen Goyal ◽  
Anil Kumar

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).


Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 400 ◽  
Author(s):  
Galata ◽  
Farkas ◽  
Könyves ◽  
Mészáros ◽  
Szabó ◽  
...  

The pharmaceutical industry has never seen such a vast development in process analytical methods as in the last decade. The application of near-infrared (NIR) and Raman spectroscopy in monitoring production lines has also become widespread. This work aims to utilize the large amount of information collected by these methods by building an artificial neural network (ANN) model that can predict the dissolution profile of the scanned tablets. An extended release formulation containing drotaverine (DR) as a model drug was developed and tablets were produced with 37 different settings, with the variables being the DR content, the hydroxypropyl methylcellulose (HPMC) content and compression force. NIR and Raman spectra of the tablets were recorded in both the transmission and reflection method. The spectra were used to build a partial least squares prediction model for the DR and HPMC content. The ANN model used these predicted values, along with the measured compression force, as input data. It was found that models based on both NIR and Raman spectra were capable of predicting the dissolution profile of the test tablets within the acceptance limit of the f2 difference factor. The performance of these ANN models was compared to PLS models using the same data as input, and the prediction of the ANN models was found to be more accurate. The proposed method accomplishes the prediction of the dissolution profile of extended release tablets using either NIR or Raman spectra.


1998 ◽  
Vol 14 (5) ◽  
pp. 209-211 ◽  
Author(s):  
John Erramouspe ◽  
Eric J Jarvi

Objective: To compare the in vitro dissolution of methylphenidate hydrochloride from regular-release tablets to halves of extended-release tablets. Design: Regular-release 10-mg methylphenidate tablets and halves of 20-mg extended-release tablets from two manufacturers (MD Pharmaceuticals, Inc., and Ciba Pharmaceutical Company) were dissolved according to the USP method specified for regular-release methylphenidate tablets. Samples were collected at 0.25, 0.5, 0.75, 1, 2, 3, 3.5, 4, 5, 6, and 7 hours. Methylphenidate concentration was determined by HPLC. Results: Regular-release methylphenidate tablets had statistically greater cumulative dissolution at all sample collection times of 2 hours or less compared with halves of extended-release tablets. The most dramatic difference occurred in the first 30 minutes, at which time the difference in cumulative dissolution was 63% (generic) and 55% (Ritalin). At 3 hours and thereafter, there was no significant difference in cumulative dissolution. Conclusions: Despite being cut in half, extended-release methylphenidate still does not dissolve as fast as regular-release tablets. Halving methylphenidate extended-release tablets may be a clinically acceptable means of achieving a prolonged-acting 10-mg dose.


Author(s):  
Srinivasa Rao Baratam ◽  
Vijayaratna J

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.


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