Study of Different Chitosan/Sodium Carboxymethyl Cellulose Proportions in the Development of Polyelectrolyte Complexes for the Sustained Release of Clarithromycin from Matrix Tablets

This study investigated the combination of different proportions of cationic chitosan and anionic carboxymethyl cellulose (CMC) for the development of polyelectrolyte complexes to be used as a carrier in a sustained-release system. Analysis via scanning electron microscopy (SEM) Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) confirmed ionic interactions occur between the chitosan and carboxymethyl cellulose chains, which increases drug entrapment. The results of the dissolution study in acetate buffer (pH 4.2) showed significant increases in the kinetic profiles of clarithromycin for low proportions of chitosan/carboxymethyl cellulose tablets, while the tablets containing only chitosan had high relaxation of chitosan chains and disintegrated rapidly. The Korsmeyer–Peppas kinetic model for the different interpolymer complexes demonstrated that the clarithromycin transport mechanism was controlled by Fickian diffusion. These results suggest that the matrix tablets with different proportions of chitosan/carboxymethyl cellulose enhanced the ionic interaction and enabled the prolonged release of clarithromycin.

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DEVELOPMENT OF SUSTAINED RELEASE ALOGLIPTIN TABLETS USING A MULTIPARTICULATES SYSTEM MADE OF BENTONITE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i3.40664 ◽

2021 ◽

pp. 68-73

Author(s):

RASHAD M. KAOUD ◽

ALHAMZA HOSHI KHALAF ◽

JAMAL ALYOUSSEF ALKRAD

Keyword(s):

Sustained Release ◽

High Performance ◽

Hydroxypropyl Methylcellulose ◽

Hplc Method ◽

Fickian Diffusion ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Xrd Pattern ◽

Sustained Release Tablets ◽

Release Data

Objective: This study was designed to evaluate the use of bentonite in the formulation of sustained-release tablets containing alogliptin benzoate after granulation. Methods: Bentonite was used for preparing tablets after granulation. The prepared tablets were tested for their pharmacopeial requirements. Further, a high-performance liquid chromatography (HPLC) method was developed to assess the release pattern of alogliptin from the tablets. Besides, differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and powder X-ray diffraction (XRD) were used for evaluating the compatibility the drugs and bentonite. Finally, the release from the tablets was tested using the paddle apparatus. Results: The FTIR and DSC did not show any interaction between the drug and the excipient in contrast to the powder-XRD pattern, which showed a shift for montmorillonite crystal peak. This shift was interpreted by increasing in the spacing of the crystalline structure of montmorillonite. However, the results of pharmacopeial tests showed that the prepared tablets comply with the compendial requirements, In addition, the release profiles of these tablets with aid of hydroxypropyl methylcellulose (HPMC) as a binder revealed a sustained release of alogliptin. Furthermore, the fitting of release data showed that the release from these tablets followed Fickian diffusion that alogliptin released by diffusion from bentonite gel matrix. Conclusion: Bentonite was successfully used for producing sustained-release tablets of alogliptin. However, maintaining the crystal structure of montmorillonite was essential for building the gel structure of bentonite and releasing the drug in a controlled manner.

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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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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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DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

INDIAN DRUGS ◽

10.53879/id.55.11.10741 ◽

2018 ◽

Vol 55 (11) ◽

pp. 71-73

Author(s):

Ch. Taraka Ramarao ◽

◽

J Vijaya Ratna ◽

R. B. Srinivasa

Keyword(s):

Drug Release ◽

Dosage Forms ◽

Matrix Tablets ◽

Fickian Diffusion ◽

Release Mechanism ◽

Gastric Residence Time ◽

Drug Release Mechanism ◽

The Matrix ◽

Gastro Retentive

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

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In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v8i1.5333 ◽

1970 ◽

Vol 8 (1) ◽

pp. 31-38 ◽

Cited By ~ 1

Author(s):

Mohammad Nezab Uddin ◽

Ishtiaq Ahmed ◽

Monzurul Amin Roni ◽

Muhammad Rashedul Islam ◽

Mohammad Habibur Rahman ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Kinetics ◽

In Vitro Release ◽

High Viscosity ◽

Matrix Tablets ◽

Release Studies ◽

The Matrix ◽

Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

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FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

Journal of Pharmaceutical and Scientific Innovation ◽

10.7897/2277-4572.105218 ◽

2021 ◽

Vol 10 (5) ◽

pp. 131-136

Author(s):

Asim pasha ◽

C N Somashekhar

Keyword(s):

Drug Release ◽

Sustained Release ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Prolonged Release ◽

Matrix Tablet ◽

Direct Compression ◽

Dissolution Profile ◽

Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

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Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

Pharmaceutics ◽

10.3390/pharmaceutics12020174 ◽

2020 ◽

Vol 12 (2) ◽

pp. 174

Author(s):

Rebeca Simancas-Herbada ◽

Ana Fernández-Carballido ◽

Juan Aparicio-Blanco ◽

Karla Slowing ◽

Jorge Rubio-Retama ◽

...

Keyword(s):

Matrix Tablets ◽

Fickian Diffusion ◽

Metformin Hydrochloride ◽

Oral Toxicity ◽

Crosslinking Degree ◽

Polymer Swelling ◽

Hydrophilic Drugs ◽

Swelling Capacity ◽

The Matrix ◽

Model Drug

The potential of a new poly(magnesium acrylate) hydrogel (PAMgA) as a pharmaceutical excipient for the elaboration of matrix tablets for the extended release of highly hydrophilic drugs was evaluated. The polymer was synthetized with two different crosslinking degrees that were characterized by FTIR and DSC. Their acute oral toxicity was determined in a mouse model, showing no toxicity at doses up to 10 g/kg. Matrix tablets were prepared using metformin hydrochloride as a model drug and the mechanisms involved in drug release (swelling and/or erosion) were investigated using biorrelevant media. This new hydrogel effectively controlled the release of small and highly hydrophilic molecules as metformin, when formulated in matrix tablets for oral administration. The rate of metformin release from PAMgA matrices was mainly controlled by its diffusion through the gel layer (Fickian diffusion). The swelling capacity and the erosion of the matrix tablets influenced the metformin release rate, that was slower at pH 6.8, where polymer swelling is more intensive, than in gastric medium, where matrix erosion is slightly more rapid. The crosslinking degree of the polymer significantly influenced its swelling capacity in acid pH, where swelling is moderate, but not in intestinal fluid, where swelling is more intense.

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Erucamide-Nanoclay Systems Obtained by Intercalation Process

Materials Science Forum ◽

10.4028/www.scientific.net/msf.899.36 ◽

2017 ◽

Vol 899 ◽

pp. 36-41 ◽

Cited By ~ 2

Author(s):

Josiane R. Silvano ◽

J.M.M. Mello ◽

Lucinao Luiz Silva ◽

Humberto Gracher Riella ◽

Márcio Antônio Fiori

Keyword(s):

Differential Scanning Calorimetry ◽

Reaction Medium ◽

Film Surface ◽

Polymeric Materials ◽

Polymeric Films ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

X Ray ◽

Intercalation Process ◽

The Matrix

A major challenge in the manufacture of films for polymeric packaging is the definition and setting of the friction coefficient (FCO) for the film surfaces. The FCO values are established with the incorporation of additives during the processing of the polymeric films. But, the homogenization of these additives in the polymeric matrix is very difficult. The additives have different polarity that the matrix polymeric and not are mixable. So, these additives migrate for the surface of the polymeric films easily. Several molecules are used as sliding additives, but among the most efficient are the amides molecules, highlighting the erucamide. This molecule promotes the decrease of the FOC but due its quick migration for the polymeric film surface provides numerous problems for the manufacture of the polymeric packaging and during its application as the product. In this work a nanocomposite (MMT-ERU) was obtained by an intercalation process to improve the compatibility between the polymeric materials and the erucamide molecules. The results shown in this work refers to the studies about the intercalation processes of the erucamide molecules into nanoclays (montmorillonite) to obtain the nanocomposite MMT-ERU. The effect of the temperature and the percentage of the nanoclay in the intercalation processes were studied. The results of x-ray diffraction and differential scanning calorimetry shown that erucamide molecules were intercalated in the nanoclay structures and that intercalation efficiency depends positively of the temperature and percentage amount of the nanoclay in the reaction medium.

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Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL

International Journal of Research in Pharmaceutical Sciences and Technology ◽

10.33974/ijrpst.v1i4.206 ◽

2020 ◽

Vol 1 (4) ◽

pp. 138-145

Author(s):

B. Valli Manalan ◽

Nadendla Swathi ◽

Narra Nandini ◽

N. Hari Sree ◽

Nilla Tejaswi Sai Maha Lakshmi ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Matrix Tablets ◽

Physical Parameters ◽

Stability Studies ◽

Chemical Changes ◽

Accelerated Stability ◽

The Matrix ◽

Ft Ir

The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.

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Formulation and in-vitro evaluation of ciprofloxacin HCL floating matrix tablets

International Journal of Research in Pharmaceutical Sciences and Technology ◽

10.33974/ijrpst.v2i1.221 ◽

2020 ◽

Vol 2 (1) ◽

pp. 01-06

Author(s):

Dhulipalla Mounika ◽

I. Deepika Reddy ◽

K. Sai Chandralekha ◽

Kapu Harika ◽

Ramarao Nadendla ◽

...

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Drug Release ◽

Matrix Tablets ◽

Fickian Diffusion ◽

In Vitro Dissolution ◽

Oral Drug ◽

Prolonged Release ◽

Evaluation Parameters

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared.

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