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Narayanaswamy, V. B.
- Formulation and Evaluation of Fast Dissolving Tablets of Doxazosin Mesylate
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
4 Department of Pharmacology, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Pharmaceutical Research, Vol 6, No 3 (2016), Pagination: 131-146Abstract
The objective of this research was to formulate fast dissolving tablets of Doxazosin mesylate that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Doxazosin mesylate is used for the treatment of the signs and symptoms of benign Prostatic Hyperplasia. Fast dissolving tablets of Doxazosin mesylate were prepared by direct compression method using superdisintegrant addition method, by using sublimation method and effervescent method. Thirty two formulations were prepared and evaluated for hardness, thickness, friability, weight variation, drug content, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio and in vitro dissolution studies.
FTIR and DSC studies revealed that there was no chemical interaction between the drug and the excipients. Formulation S8 was found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. The formulation S8 containing camphor (8%) as subliming agent was found to be the optimized combinations. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for formulation S8 for 60 days. The results of stability studies indicated no significant changes with respect to physicochemical properties, in vitro disintegration time, wetting time and in vitro drug release.
Keywords
Fast Dissolving Tablets, Doxazosinmesylate, Superdisintegrant, Directcompression, Sodium Starch Glycollate, Camphor, Citric Acid.- Formulation and Evaluation of Montelukast Sodium Fast Dissolving Tablets
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
4 Department of Pharmacology, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Pharmaceutical Research, Vol 6, No 3 (2016), Pagination: 159-169Abstract
Montelukast sodium is an anti-asthmatic, mainly prevents leukotriene mediated effect associated with asthma. Mouth dissolving tablets of montelukast sodium was prepared by direct compression method using superdisintegrants such as croscarmellose sodium, crospovidone and sodium starch glycolate.
Mouth dissolving tablets (MDTs) disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrants or maximizing pore structure in the formulation. The tablets were prepared using various diluents like MCC, Lactose and superdisintegrants namely Crosscarmellose sodium, Crosspovidone and Sodium starch glycollate in different concentrations. Pre-compression parameters such as angle of repose, bulk density, tapped density, compressibility index, Hausner's ratio were carried out to study the flow properties of powder to achieve uniformity of tablet weight and the values were within permissible limits.The prepared tablets were evaluated for hardness, thickness, weight variation, friability, % drug content, wetting time, water absorption ratio, in vitro disintegration time, in vitro dispersion time and in vitro drug release.The formulation M12 and L12 was found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for a period of 60 days for the selected formulations. The formulation M12 and L12 containing Crospovidone (8%) as superdisintegrant and microcrystalline cellulose and lactose as diluents was respectively found to be the optimized combination.
Keywords
Fast Dissolving Tablets, Superdisintegrants, Diluents, Mouth Dissolving Tablets, Montelukast Sodium, Asthama.- Formulation and Evaluation of Controlled Release Matrix Tablets of Labetalol HCl
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Pharmaceutical Research, Vol 6, No 2 (2016), Pagination: 107-120Abstract
Oral controlled drug delivery systems have received much attention of the researchers during the past two decades. The rationale for developing a controlled release formulation is to enhance its therapeutic benefits, reducing its side effects and improving the management of diseased condition.
Studies have been carried out for developing oral controlled release matrix tablet formulations of labetalol by using polymeric materials like polyox WSR 301, polyox WSR 303, polymethacrylates, ethyl cellulose, xanthan gum, guar gum, karaya gum and sodium alginate.
The prepared matrix tablets were evaluated for weight uniformity, hardness, friability and drug content. The matrix tablets were then evaluated for the influence of polymer concentration, polymer type and nature of diluents on the drug release from matrix by in vitro dissolution studies. FTIR Spectral studies shown that drug and excipients used were compatible with each other. Selected formulations of Labetalol were subjected to accelerated stability studies. The formulations were stored at 400C±2°C, 75±5%RH for 3 months. No significant changes were observed from the prepared tablets during the study period.
The results of present research work clearly indicated that the nature and level of poly (ethylene oxides) in the matrix tablets greatly influenced the drug release properties. Both the Polyox WSR 301 and Polyox WSR 303 were suitable for preparing the matrix tablets of labetalol. Among the two polymers used, high molecular weight polymer, POLYOX WSR 303 effectively extended the drug release for prolonged period of time than low molecular weight POLYOX WSR 301. Insoluble diluents like microcrystalline cellulose, dicalcium phosphate and slightly soluble diluent like starch 1500 can be used as release rate modifiers in the formulation of controlled release matrix tablets.
A combination of hydrophilic gums, hydrophobic eudragits and ethyl cellulose with high molecular weight poly (ethylene oxides) led to prolonged release of drug up to 22 hrs. Thus present research work fulfilled the objective of developing once a day formulations of Labetalol as matrix tablets employing poly (ethylene oxides).
Keywords
Labetalol, Controlled Release, Polymer, Ethyl Cellulose.- Formulation and Evaluation of Gastroretentive Floating Matrix Tablets of Atorvastatin Calcium
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Pharmacy and Technology, Vol 6, No 2 (2016), Pagination: 113-126Abstract
The present work focuses on the development of hydrodynamically balanced delivery system of Atorvastatin as a single-unit floating Tablet which, after oral administration should have the ability to prolong gastric residence time with the desired in vitro release profile for the localized action in the stomach. Fourier transform Infrared spectroscopy and DSC study confirmed the absence of any drug/polymers/excipients interactions. Floating effervescent tablets were formulated by various materials like. hydroxypropyl methylcellulose (HPMC) K4M, K15M, psyllium husk, swelling agent as crospovidone and micro crystalline cellulose and gas generating agent like sodium bicarbonate and citric acid and evaluated for floating properties, swelling characteristics and drug release studies. Floating non effervescent tablets were prepared by polypropylene foam powder and different matrix forming polymers like HPMC K4M, Carbopol 934P xanthan gum and sodium alginate. The Tablets were prepared by wet granulation method and the polymer in varying ratios. The prepared floating tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, buoyancy lag time, total floating time, water uptake (swelling index) and in-vitro dissolution studies Incorporation of gas- generating agent together with polymer improved drug release, besides optimal floating. The formulation was optimized on the basis of in vitro buoyancy and in vitro release in 0.1N HCl. By fitting the data into zero-order, first-order, and Higuchi models, we concluded that the mechanism of release of Atorvastatin from the floating tablet was anomalous diffusion transport and follows zero order kinetics, as the correlation coefficient (R value) was higher for zero-order release. Stability studies revealed that formulations were stable when stored at different temperatures and the values were within permissible limits.Keywords
Atorvastatin, Floating Drug Delivery System, Hydrocolloids, Gastric Residence Time, Buoyancy.- Design and Evaluation of Transdermal Patches Containing Risperidone
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
4 Department of Pharmacology, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Research in Pharmaceutical Sciences, Vol 6, No 4 (2016), Pagination: 208-222Abstract
Transdermal drug delivery systems are also known as patches, containing dispersed or dissolved drug with plasticizers, polymers, etc. are intended to deliver a therapeutically effective amount of drug across the skin. In the present work, Transdermal drug delivery of Risperidone were formulated in different concentration (10%, 20% and 30% ) of glycerine and polyethylene glycol 400 as plasticizer and a blend of two in different concentrations of polymers (PVPK30,HPMC,PVA and Eudragit RS 100) were formulated by solvent casting method. Drug polymer interaction study was carried out using FTIR and DSC studies. In this study the results indicates, as increase in the concentration of glycerine and Polyethylene glycol increases the diffusion rate of Risperidone patches. The physico-chemical parameters like weight variation, thickness, folding endurance. Percentage Flatness and Water vapour transmission of the Risperidone patches were evaluated. All the physico chemical parameters were found to be satisfactory. Risperidone patches formulated by using 30% glycerine 30% PEG400shows enhanced rate of diffusion than the patches prepared with 10% and 20% glycerine10% and 20% PEG400 respectively. Risperidone patches formulated with 20% glycerine 20% PEG400 had enhanced rate than the patches prepared with 10%glycerine/10% PEG400 respectively. Among polymers, combination of HPMC and Eudragit had enhanced diffusion rate than the combination of HPMC and PVPK30 in all formulations formulated by using glycerine as plasticizer. The polymers, combination of PVPK30 and Eudragit had enhanced diffusion rate than the combination of PVPK30 and PVA in all formulations formulated by using PEG400 as plasticizer. The Risperidone transdermal patches shows greater diffusion rate when formulated with higher concentration of plasticizer hence the30% of glycerine and PEG 400 had shown a values higher than 20 and 10 % glycerine and PEG 400. The kinetic study and mechanism for the diffusion of Risperidone transdermal patches obeys higuchi, peppas model. The correlation coefficient (R2) values were greater, indicating from the analysis of diffusion data as per above models. The T50 and T80 values for Risperidone patches formulated with glycerine andPEG400 are exhibited good results. The SEM films indicating uniform distribution of the drug with polymers and plasticizers.Keywords
Transdermal Drug Delivery, Diffusion Rate, Eudragit, Risperidone, Plasticizer, HPMC.- Formulation and Evaluation of Fast Dissolving Tablets of Flecainide Acetate
Authors
1 Karavali College of Pharmacy, Mangalore, IN
2 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore, IN
3 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore, IN
Source
Asian Journal of Research in Pharmaceutical Sciences, Vol 6, No 2 (2016), Pagination: 116-128Abstract
The objective of this research was to formulate fast dissolving tablets of Flecainide acetate that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Flecainide acetate is used for the treatment of cardiac arrhythmias and tachyarrhythmias. Fast dissolving tablets of Flecainide acetate were prepared by direct compression method using various superdisintegrants and by using sublimation method. Thirty two formulations were prepared by using different superdisintegrants and subliming agents and evaluated for hardness, thickness, friability, weight variation, drug content, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio and in vitro dissolution studies. FTIR and DSC studies revealed that there was no chemical interaction between the drug and the excipients. Formulation S4 were found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. The formulation S4 containing Crospovidone as superdisintegrant and camphor as subliming agent were found to be the optimized combinations. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for formulation S4 for 90 days. The results of stability studies indicated no significant changes with respect to physicochemical properties, in vitro disintegration time, wetting time and in vitro drug release.Keywords
Fast Dissolving Tablets, Flecainide Acetate, Superdisintegrant, Direct Compression, Sodium Starch Glycollate, Camphor, Crosspovidone.- Formulation and Evaluation of Controlled Release Matrix Tablets of Sotalol
Authors
1 Department of Pharmaceutics, Karavali College of Pharmacy, Mangalore-575028, Karnataka, IN
2 Department of Pharmacognosy, Karavali College of Pharmacy, Mangalore-575028, Karnataka, IN