scholarly journals Response Surface Optimization of Sustained Release Metformin-Hydrochloride Matrix Tablets: Influence of Some Hydrophillic Polymers on the Release

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Amitava Roy ◽  
Kalpana Roy ◽  
Sarbani Roy ◽  
Jyotirmoy Deb ◽  
Amitava Ghosh ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Dissolution Kinetics ◽  
Matrix Tablets ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Response Surface Optimization

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.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals Formulation of Sustained-Release Matrix Tablet of Rotundin Sulfat

2019 ◽  
Vol 35 (1) ◽  
Author(s):  
Do Thi Ha ◽  
Nguyen Thanh Hai ◽  
Tran Thi Van Anh ◽  
Ha Thanh Hoa ◽  
Pham Thi Minh Hue
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Viet Nam ◽  
Pharmaceutical Sciences ◽  
Release Process ◽  
Tablet Hardness

Sustained-release matrix tablets containing rotundin sulfat are prepared by a wet granulation method. The influence of Metholose 100.000 RS,  4000 SR, Avicel PH101, lactose and tablet compression force on the ability to release rotundin from the tablets has been evaluated. Modde 8.0 software was used in the experiment. The influencing factors were evaluated by software FormRules v2.0 and the optimal formula predicted by the INForm v3.1 was optimized. The selected optimal formulation of rotundin sulfate tablets for a drug release process lasting 8 hours contained Metholose 100.000 RS 120 mg; Avicel PH101 24.0 mg; lactose 34.5 mg; and 8 kP tablet hardness. Keywords Rotundin sulfat, matrix tablet, sustained release, optimizing. References [1] Đỗ Tất Lợi, Những cây thuốc và vị thuốc Việt Nam, NXB Thời Đại (2011), 779. [2] Nguyễn Minh Chính và CS, Nghiên cứu tách chiết rotundin để sản xuất thuốc tiêm rotundin sulfat, Tạp chí Y Dược học Quân sự. 1 (1999) 55-56. [3] Nguyễn Thanh Hải, Bùi Thanh Tùng, Phạm Thị Minh Huệ (2017), Phỏng sinh học trong y dược học – Hướng nghiên cứu cần đẩy mạnh, Tạp chí khoa học ĐHQGHN, Khoa học Y Dược. 33(1) (2017) 1-4. [4] Bộ Y tế, Dược điển Việt Nam V, Nhà xuất bản Y học, 1 (2017), 842-844. [5] M. Levina, A.R. Rajabi-Siaboomi, The influence of excipients on drug release from hydroxypropyl methylcellulose matrices, Journal of Pharmaceutical Sciences. 93(11) (2004) 2746-2754. [6] Nguyễn Minh Chính, Nguyễn Thị Hồng Thắm, Nguyễn Văn Bạch, Tối ưu hóa công thức bào chế viên nén rotundin sulfat giải phóng kéo dài, Tạp chí Y Dược học Quân sự. số CĐ Dược (2016), 61-67. [7] N. Aruna, K.M. Babu, Formulation and evaluation of sustained release matrix tablets containing metformin HCl and Syzygium cumini, International Journal of Pharmaceutical and Biological Archive. 2(3) (2011), 900-905. [8] B.J. Lee, et al, Formulation and release charecteristics of hydroxypropyl methylcellulose matrix tablet containing melatonin, Drug Development and Industrial Pharmacy. 25 (1999) 493-501.[9] A. Nokhochi, J.L. Ford, P. Rowe, et al, The e ffects of compression rate and force on the compaction properties of different viscosity grades of hydroxypropyl methylcellulose 2208, International Journal of Pharmaceutics. 129 (1996), 21-31.  

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

2018 ◽  
Vol 11 (3) ◽  
pp. 342
Author(s):  
Padmaja Bookya ◽  
Ramakrishna Raparla ◽  
Ramakrishna Raparla ◽  
Harikishan Prasad Sriramula ◽  
Ramakrishna Raparla ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Matrix Material ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Matrix Tablet

 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.

Formulation and Evaluation of Sustained Release Bilayer Matrix Tablet of Glimepiride and Metformin Hydrochloride

2021 ◽  
pp. 273-279
Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane
Keyword(s):  
Sustained Release ◽  
Type Ii Diabetes ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Type Ii ◽  
Weight Variation

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.

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

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.

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Matrix Tablets of Venlafaxine

2017 ◽  
Vol II (I) ◽  
pp. 10-24
Author(s):  
Zubair Anwar ◽  
Tanveer Ahmed Khan ◽  
Muhammad Farhan Sohail ◽  
Maryam Anwar
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Sustained Effect ◽  
Release Data ◽  
Drug Studies

Sustained release matrix tablets of venlafaxine were formulated using synthetic polymers (ethylcellulose & hydroxypropyl methylcellulose). Six (06) different batches of matrix tablets of venlafaxine (dose 75 mg) were prepared by the wet granulation method. Polymers were used alone or in combination. The physical properties of compressed tablets were evaluated. In vitro release drug studies were performed in phosphate buffer at pH 6.8 over 24 hours. The drug release data fitted well to the First-order (R2 = 0.9725 � 0.9900). The n value obtained for most batches ranged from 0.523 to 0.946 indicates that the drug is released through an anomalous or non�Fickian transport. Results revealed that the combination of ethyl cellulose (EC) and hydroxypropyl methylcellulose produced a sustained effect compared to hydroxypropyl methylcellulose alone. Formulation F6 containing single polymer (EC) showed the highest control over initial burst release, and extended-release of the drug continued up to 16 hours.

scholarly journals DESIGN AND IN VITRO CHARACTERIZATION OF FLOATING TABLETS OF METRONIDAZOLE

2019 ◽  
pp. 539-544
Author(s):  
CHINNA ESWARAIAH M ◽  
JAYA S
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Matrix Tablet ◽  
N Value

Objective: The objective of the present study was to formulate the effervescent floating matrix tablet of metronidazole and to evaluate the effect of varying concentrations of hydrophilic polymers on drug release. Methods: Drug excipients interaction was studied by Fourier transform infrared spectrophotometer. The effervescent floating matrix tablets were prepared by direct compression technique using hydroxypropyl methylcellulose (HPMCK4) and xanthan gum alone and in combination as release retardants. Microcrystalline cellulose was used as diluent. Sodium bicarbonate was used as effervescent agent. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity, buoyancy time, and in vitro dissolution. Results: Micromeritic properties and post-compression parameters were evaluated and all the parameters were found within the acceptable limit. The drug release data were subjected to different models to evaluate release kinetics and mechanism of drug release. The matrix tablets prepared with xanthan gum and a mixture of xanthan gum and HPMCK4 were retarded the drug release up to 12 h. The release mechanism of metronidazole was evaluated on the basis of release exponent n value in Peppas model. The n value of the formulations ranged from 0.46 to 0.89 which indicated Case II transport and zero-order release. Conclusion: Floating matrix tablet is the simple, efficient, and economic method to sustain the release of metronidazole to eradicate Helicobacter pylori in peptic ulcer disease.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals FORMULATION AND EVALUATION OF SYNTHESIZED QUINAZOLINONE DERIVATIVE FOR COLON SPECIFIC DRUG DELIVERY

2017 ◽  
Vol 10 (3) ◽  
pp. 207
Author(s):  
Vidya Viswanad ◽  
Shammika P ◽  
Aneesh Tp
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Site Specific ◽  
The Matrix

ABSTRACTObjective: The current research deals with the formulation and evaluation of synthesized quinazolinone derivative for colon site specific delivery.Methods: The synthesized quinazolinone derivative was enteric coated 5% Eudragit L-100 with by wet granulation method using guar gum, pectin,and guar gum pectin combination as hydrophilic polymer. The prepared matrix tablet was characterized by differential scanning calorimetry andevaluated for different pre-compression and post-compression studies and drug release profiles.Results: All the matrix tablets were within the range of pharmacopeial limits with better flow properties. All the six formulations of matrix tablets haddisintegrated within 5-6 minutes. The optimized formulation selected was F6 formulation combination of guar gum and pectin with 95.79% of drugrelease than compared to the remaining formulation. The optimized matrix tablets followed zero order kinetics with Fickian diffusion.Conclusion: The results proposed that the combination of guar gum and pectin coated tablet with 5% Eudragit L-100 of synthesized quinazolinonederivative is a promising colon site specific delivery.Keywords: Quinazolinone derivative, In vitro drug release, Disintegration time, Guar gum, Pectin, 5% Eudragit L-100, Colon site-specific delivery, Wetgranulation, Compression.

scholarly journals Development and evaluation of gastroretentive norfloxacin floating tablets

2009 ◽  
Vol 59 (2) ◽  
pp. 211-221 ◽  
Author(s):  
Ramesh Bomma ◽  
Rongala Swamy Naidu ◽  
Madhusudan Yamsani ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

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