scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE SUSTAINED RELEASE MATRIX TABLETS

Author(s):  
SAHIDUL ALAM ◽  
AMLAN BISHAL ◽  
BRATATI BANDYOPADHYAY

Objective: Now a days as very few antidiabetic drugs are coming out of research and development and some existing drugs are showing several side effects when administered orally, multiple times in a day, hence change in the operation is a suitable and optimized way to make some drug more effective by slight alteration in the drug delivery. Matrix type drug delivery systems of an antidiabetic drug like Metformin Hydrochloride, is an interesting and promising option when developing an oral sustained release system Methods: An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target sites. This research work is made in designing of sustained release dosage form of Metformin Hydrochloride by wet granulation method employing both Xanthan Gum and Hydroxy Propyl Methyl Cellulose (HPMC K4M) as a rate controlling polymer. Results: The development of oral sustained release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. From all the formulation trial batches, formulation F7 shows the best results. It has been observed that HPMC K4M alone cannot give satisfactory drug release profile but the blend of HPMC K4M and Xanthan gum together give the best drug release kinetics. Conclusion: The drug release mechanism from the matrix tablets follows Fickian diffusion with first order kinetics. Thus, sustained release matrix tablets of metformin hydrochloride can be expected to reduce the frequency of administration and decrease the dose dependent side effects

Author(s):  
A. Bhavani ◽  
B. Hemalatha ◽  
K. Padmalatha

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.


2010 ◽  
Vol 146-147 ◽  
pp. 589-598 ◽  
Author(s):  
Hong Lei Jian ◽  
Li Wei Zhu ◽  
Wei Ming Zhang ◽  
Xiang Qi ◽  
Jian Xin Jiang

The galactomannan from endosperm of G. sinensis seeds was used as sustained release material in the matrix tablets prepared at different concentration of 5, 10 and 15 % corresponding to formulations of G5, G10 and G15, for the release of theophylline. The drug release behaviors of the systems were investigated, including the swelling and morphological studies and texture analysis. The dissolution tests were conducted in 0.1 M hydrochloric acid and pH 6.8 phosphate buffered saline. The results of release studies demonstrated that G10 with 10 % galactomannan concentration showed a better control of the drug release profiles. The percents of cumulative drug released in 24 h were 98.8, 90.2 and 83.4 % for G5, G10 and G15, respectively. All the systems exhibited the typical morphological behavior of a swellable matrix. Results of texture analysis on the swollen tablets confirmed that diffusion drug release mechanism played the major role in G10 and G15 systems while the drug delivery kinetic towards an erosion/relaxation mechanism for G5 matrix tablets.


Author(s):  
Padmaja Bookya ◽  
Ramakrishna Raparla ◽  
Ramakrishna Raparla ◽  
Harikishan Prasad Sriramula ◽  
Ramakrishna Raparla ◽  
...  

 Objective: The aim of this investigation was to develop and optimize metformin hydrochloride matrix tablets for sustained release application. The sustained release matrix tablet of metformin hydrochloride was prepared by wet granulation technique using chitosan, xanthan gum, and hydroxypropyl methylcellulose at varying concentrations.Material and Methods: Extended release of metformin hydrochloride matrix tablets was prepared by wet granulation method. The influence of varying the polymer ratios was evaluated. The excipients used in this study did not alter physicochemical properties of the drug.Results: All the batches were evaluated for thickness, weight variation, hardness, and drug content uniformity. The in vitro drug dissolution study was carried out using USP apparatus Type II, paddle method, and the release mechanisms were explored. Mean dissolution time is used to characterize drug release rate from a dosage form and indicates the drug release is retarding efficiency of the polymer. This study revealed that as the concentration of matrix material increased, drug release from matrices decreased. This may be due to slower penetration of the dissolution medium into the matrices.Conclusion: Formulation with chitosan MS1 drug release was 86%, xanthan gum MS489%, and finally MS7 with hydroxypropyl methyl cellulose which exhibited the highest drug release retardation also had the lowest matrix concentration. Hence, lower concentration of polymers is suitable to prepare metformin hydrochloride tablets compared to higher concentrations.


2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain

<p>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.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>


Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa

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.


2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.


Author(s):  
S Shanmugam

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 


2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Amitava Roy ◽  
Kalpana Roy ◽  
Sarbani Roy ◽  
Jyotirmoy Deb ◽  
Amitava Ghosh ◽  
...  

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X60, X120, T50, T90, n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable.


Author(s):  
Dhulipalla Mounika ◽  
I. Deepika Reddy ◽  
K. Sai Chandralekha ◽  
Kapu Harika ◽  
Ramarao Nadendla ◽  
...  

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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