Identification, Characterization and Drug-Excipient Compatibility of Diltiazem Hydrochloride by Physico-Chemical Techniques

 

Sandip Prasad Tiwari1,2*, Gali Vidyasagar3 

1Columbia Institute of Pharmacy, Tekari, Raipur (C.G.)-493111, India

2Bhagwant University,Sikar Road, Ajmer, (Rajasthan)-305004, India

3Veerayatan Institute of Pharmacy,Mandvi, Kutch, (Gujarat)-370435, India

Abstract

The enhancement of oral bioavailability of poorly water soluble drugs remains one of the most challenging aspects. Utilization of cyclodextrins attracted the attention of many researchers for the enhancement of the dissolution rate. The complexation of diltiazem hydrochloride with β- cyclodextrin (CD) was investigated by phase solubility. Phase solubility study was performed to determine stiochiometric proportion of Diltiazem HCl and complexing agent b-cyclodextrin. Solid inclusion complexes of diltiazem hydrochloride-βCD in 1:1 and 1:2 ratios were prepared by different methods, and the results were satisfactorily and complied with compendia. Mouth dissolving tablets were formulated employing Diltiazem hydrochloride alone and their βCD complexes with an objective of evaluating the feasibility of employing drug-βCD complexes in the design of immediate release tablet formulations for obtaining flow and complete drug release in 01 h. All the tablets prepared by optimizing the formula and were evaluated for pre compression, post compression, drug content, and drug release. The overall results indicate that formulation M3 was better and that it satisfies all the criteria as a fast mouth dissolving tablet.

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Optimization of Polymer Concentration for Designing of Oral Matrix Controlled Release Dosage Form

 

S. Budiasih1,2*, Jiyauddin K.1,2, Logavinod N.1,2, M. Kaleemullah2, Jawad A.1,2, Samer A. D.1,2, Fadli A.1, Eddy Y.1

1Unit of Research, School of Pharmacy, Management & Science University, 40100 Shah Alam, Selangor Darul Ehsan, Malaysia.

2Unit of Pharmaceutics, School of Pharmacy, Management & Science University, 40100 Shah Alam, Selangor Darul Ehsan, Malaysia.

Abstract

Patient’s compliance can be enhanced by using extended release drug delivery systems which allow decreasing the number of daily doses, and helping to maintain uniform drug levels and increase the safety margin for high-potency drugs. Hydroxypropyl methylcellulose (HPMC) is the most commonly used hydrophilic polymer for the preparation of oral controlled drug delivery systems. This research was conducted with the aim of  developing matrix based oral controlled release tablets for the drug diclofenac sodium using different viscosity grades of HPMC (K15M) and to compare the  drug release characteristics with those of a commercial product, Voltaren® SR 100. Similarity factor (f2), values in between test formulation and marketed preparation was calculated to choose the best formulation. The release kinetics from various matrices was also studied. Increasing in polymer content reduced the rate of drug release. At the same polymer content in the matrix, the drug release was most sustained with tablets prepared using HPMC (K15M). Out of all the formulations studies, matrix tablets containing 40% of HPMC (K15M) showed comparable dissolution profile to that of the marketed preparation as indicated by a similarity factor value of (f2) 88.30%. The release of drug from marketed preparation and matrix with HPMC (K15M) 40% was found to be a diffusion drug mechanism as per Higuchi equation.

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Improving the Bioavailability of Diltiazem Hydrochloride by Forming Complexes with β-Cyclodextrin

 

Sandip Prasad Tiwari1,2*, Gali Vidyasagar3

 1Columbia Institute of Pharmacy, Tekari, Raipur (C.G.)-493111, India

2Bhagwant University,Sikar Road, Ajmer, (Rajasthan)-305004, India

3Veerayatan Institute of Pharmacy,Mandvi, Kutch, (Gujarat)-370435, India

Abstract

The enhancement of oral bioavailability of poorly water soluble drugs remains one of the most challenging aspects. Utilization of cyclodextrins attracted the attention of many researchers for the enhancement of the dissolution rate. The complexation of diltiazem hydrochloride with β- cyclodextrin (CD) was investigated by phase solubility. Phase solubility study was performed to determine stiochiometric proportion of Diltiazem HCl and complexing agent β-cyclodextrin. Solid inclusion complexes of diltiazem hydrochloride-βCD in 1:1 and 1:2 ratios were prepared by different methods, and the results were satisfactorily and complied with compendia. Mouth dissolving tablets were formulated employing Diltiazem hydrochloride alone and their βCD complexes with an objective of evaluating the feasibility of employing drug-βCD complexes in the design of immediate release tablet formulations for obtaining flow and complete drug release in 01 h. All the tablets prepared by optimizing the formula and were evaluated for pre compression, post compression, drug content, and drug release. The overall results indicate that formulation M3 was better and that it satisfies all the criteria as a fast mouth dissolving tablet.

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Evaluation of Antidiabetic Activity of Isolated Compound from Ougeinia oojeinensis Bark Extract in Diabetic Rats

 

Manohar Lal Samyal1, Anil Ahuja1 Zabeer Ahmed2*

1Department of Pharmacy, Sunrise University, Alwar-301030, (Rajasthan), India
2IIIM Jammu, Canal Road, Jammu-180001, (J&K), India

Abstract

Ougeinia oojeinensis is used by tribal people for treatment of diabetes. The present aim of this study was to isolate different fractions from O. oojeinensis bark extracts, and evaluated the potency of antdiabetic activity of fractions. The nine different fractions were collected from ethanol extracts of O. oojeinensis bark. The fraction F4, F6, F7 and F8 were administered orally in Streptozotocin (STZ)-induced diabetic rats. After the administration of fractions, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. The effect of fractions on induced hyperlipidemia was analyzed where the fraction significantly lowered the elevated total cholesterol, triglycerides (TGL) and low density lipoprotein (LDL) level while increased the High density lipoprotein (HDL). Glibenclamide was used as a standard drug at a dose of 0.50 mg/kg body weight. Moreover, the fraction treated rats exhibited the significant rise in serum insulin level compared with streptozotocin- induced diabetic rats.The findings demonstrated that fraction isolated from ethanol extracts of O. oojeinensis bark has significant antidiabetic activity in streptozotocin-induced rats compared to standard drug.

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Estimation of Antihyperglycemic and Antihyperlipidemic Activity of Isolated Fractions from Ficus glomerata Bark Extract in Streptozotocin-Induced Diabetic Rats

 

Manohar Lal Samyal1,, Anil Ahuja1, Zabeer Ahmed2*

1Department of Pharmacy, Sunrise University, Alwar-301030, (Rajasthan), India

2IIIM Jammu, Canal Road, Jammu-180001, (J&K), India

Abstract

Ficus glomerata is commonly used for the treatment of diabetes. We planned to isolate compound from the ethanol extract of F. glomerata bark, and also evaluate the antidiabetic activity of isolated fractions in Streptozotocin (STZ)-induced diabetic rats.  Oral administration of ethanol extract of bark and root of F. glomerata at the doses of 200 and 400 mg/kg body weight was studied in STZ-induced diabetic rats.After administration of extract the fasting blood glucose levels were significantly decreased. The eight different fractions were collected from ethanol extract of F. glomerata bark and dried. The fraction F4, F5, F6, F7 and F9 were administered orally in Streptozotocin (STZ)-induced diabetic rats. After the administration of fractions, blood glucose levels were monitored at specific intervals and it was found that they were significant lowered. The effect of fractions on induced hyperlipidemia was analyzed where the fraction significantly lowered the elevated total cholesterol, triglycerides (TGL) and low density lipoprotein (LDL) level while increased the High density lipoprotein (HDL). Glibenclamide was used as a standard drug at a dose of 0.50 mg/kg body weight. Moreover, the fraction treated rats exhibited the significant rise in serum insulin level compared with streptozotocin- induced diabetic rats.The findings demonstrated that fraction isolated from ethanol extracts of F. glomerata bark has significant antidiabetic activity in streptozotocin-induced rats compared to standard drug.These results indicated that F. glomerata possesses significant antidiabetic and antihyperlipidemic effect due to presence of these fractions.

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Development and In Vitro/In Vivo Evaluation of Floating In Situ Gelling Oral Liquid Extended Release Formulation of Furosemide

 

Anas Tarik Nafei Alhamdany1*, Nidhal Khazaal Maraie1, Bahir Abdul Razzaq Msheimsh2

1Department of Pharmaceutics, College of Pharmacy, University of Al-Mustansiriya, Baghdad-Iraq

2Department of Pharmacology, College of Pharmacy, University of Al-Mustansiriya, Baghdad-Iraq

Abstract

Floating in situ gel as gastroretentive drug delivery system represents a revolution in oral controlled release dosage forms in comparison with conventional oral liquids, as it prolongs the residence time of the drugs that have narrow absorption windows in the absorptive sites like stomach or upper gastrointestinal tract by having a bulk density lower than gastric fluids and thus remains buoyant in the stomach without affecting the gastric emptying rate until the drug released slowly, continuously and completely. This study was undertaken to formulate furosemide oral solution, which undergoes gelation when it is in direct contact with gastric fluid by using primary polymer (sodium alginate) in addition to the secondary polymer (iota-carrageenan) at different concentrations. Different variables that affect drug release profile like cross linking agent, combination of polymer, gas generating agent and drug concentrations were studied to optimize the best formulation through measuring their effects on viscosity, gel strength, floating lag time and floating duration. The best formulation exhibited 94.9% release of the drug after 5 h with effective floating property. In vivo test was applied and demonstrated good indication to the gastroretentive property of the optimum formulation through its relation to the diuretic property of the drug, and it agreed with in vitro release and the proposed kinetic mathematical modeling.

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Chemically Modified Carbon Sensors Mixed or Single for the Determination of Cardiovascular Drug Nafronyl Oxalate in Bulk, Praxilene and Human Fluids  

 

Amal F. Khorshid

Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Nahda University, NUB, Beni-Sueff, Egypt

Abstract

Three novel modified carbon paste sensors (CMCPs) were proposed for the determination of nafronyl potentiometric in bulk, pharmaceutical dosage form; human plasma/urine. The sensors were based on an ion-pair associates of nafronyl silicotungstic acid (Nf-St) (sensor 1), nafronyl silicomolybdic acid (Nf-SM) (sensor 2), a mixture of [(Nf-St) + (Nf-SM)] (sensor 3). The modified sensors showed Nernstian slopes ranging from 58.5±0.5-60.7±0.5 mV over the concentration ranged from 1.0 x 10-7-1.0 x 10-2 M and pH 2.0-6.0 with a detection limit 0.1 nM. The sensors exhibited good selectivity for nafronyl with respect to inorganic /organic cations, sugars and amino acids. The calibration curve, standard addition and potentiometric titration methods were applied for the determination of nafronyl ion in its bulk powder, pharmaceutical dosage form, and human fluids plasma/urine taken from a healthy volunteer and for the monitoring Praxilene tablets in vitro dissolution rates. Sensor 3 was successfully used for the determination the solubility products of ion-pair associates. The results were excellent and satisfactory recovery comparable to those obtained with the British Pharmacopoeia.

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