Volume 6

January-March 2014

Research Articles

Development of mouth dissolving tablets containing tadalafil hydroxypropyl β-cyclodextrin inclusion complex

Hitendra S Mahajan, Swapnil R Bhagirath

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Abstract: 
The objective of the present study was to formulate mouth dissolving tablets of inclusion complex of tadalafil with improved aqueous solubility and dissolution rate. Tadalafil is a BCS class II drug having low aqueous solubility and therefore low oral bioavailability. In the present study, inclusion complex of tadalafil with hydroxypropyl-β-cyclodextrin were prepared by kneading method. Inclusion complex were characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and 1H NMR studies, and evaluated for in vitro dissolution, and phase solubility studies. DSC and XRD study demonstrated that there was a significant decrease in crystallinity of pure drug present in inclusion complex, which resulted in an increased dissolution rate of tadalafil and 1H NMR studies strongly, confirmed that the inclusion complex has formed. Inclusion complexation results in improvement in solubility and dissolution rate have been used in preparation of mouth dissolving tablets using super disintegrants by direct compression method. A total of nine formulations were developed and the tablets prepared were evaluated for weight variation, friability, hardness and wetting time. In vitro disintegration and dissolution studies were also performed. On the basis of these results, mouth dissolving tablets of tadalafil- HPβCD inclusion complex may be considered as a promising alternative to conventional tablets with improved patient compliance.

Keywords: Hydroxypropyl Beta Cyclodextrin, Tadalafil, Mouth Dissolving Tablets, Dissolution.

Almotriptan loaded sodium alginate microspheres for nasal delivery: Formulation optimization using factorial design, characterization and in vitro evaluation

Zaheer Abbas, Sachin Marihal, Akifuddin S K

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Abstract: 
Almotriptan malate, indicated for the treatment of migraine with or without aura in adults is not a drug candidate feasible to be administered via oral route during the attack due to its associated symptoms such as nausea and vomiting. This obviates an alternative dosage form. Nasal delivery of this drug is a good substitute to oral and parenteral administration, due to its numerous advantages. In the present study, sodium alginate microspheres of Almotriptan malate, for intranasal delivery, were prepared by water-in-oil (w/o) emulsification cross-linking technique. A 23 factorial design was employed with drug to polymer ratio, calcium chloride concentration and cross-linking time as independent variables while particle size and in vitro mucoadhesion of the microspheres were the dependent variables. Regression analysis was performed to identify the best formulation conditions. The microspheres were evaluated for characteristics like particle size, incorporation efficiency, swellability, zeta potential, in vitro mucoadhesion, thermal analysis, X-ray diffraction study and in vitro drug release. The shape and surface characteristics were determined by scanning electron microscopy which revealed spherical nature and nearly smooth surfaces of the microspheres. The drug encapsulation efficiency was found to be in the range of 69.62±1.15 – 89.11±0.95%. In vitro mucoadhesion was performed by adhesion number using sheep nasal mucosa and was observed in a range from 77.58±1.49 – 93.15±1.25%. Differential scanning calorimetry and X-ray diffraction results indicated a molecular level dispersion of drug in the microspheres. In vitro drug diffusion studies in phosphate buffer, pH 6.4 indicated non-Fickian or anomalous type of transport for the release of Almotriptan from the microspheres.

Keywords: Almotriptan Malate, Sodium Alginate, Mucoadhesive, Microspheres, Emulsification Cross-linking Technique, Factorial Design, Nasal Drug Delivery.

Determination of diclofenac in pharmaceutical preparations by UV- and first-order derivative spectrophotometry methods

Ulvihan Ciltas, Bilal Yilmaz

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Abstract: 
In this study, new, rapid UV spectrophotometry (UV) and first-order derivative spectrophotometry (1D) methods were developed for the determination of diclofenac in pure and tablets. The solvent system and wavelength of detection were optimized in order to maximize the sensitivity of the proposed methods. Parameters such as linearity, precision, accuracy, specificity, stability, limit of detection and limit of quantification were studied according to the International Conference on Harmonization Guidelines. Calibration curve was linear between the concentration range of 2-14 μg ml-1. Within- and between-day precision values for diclofenac were less than 4.27%, and accuracy (relative error) was better than 2.71%. The mean recovery value of diclofenac was 100.1% for pharmaceutical preparations. The developed method was successfully applied to tablet formulations and the results were compared statistically with each other.

Keywords: Diclofenac, UV Spectrophotometry, First-Order Derivative Spectrophotometry, Validation.

A novel magnetic pH-sensitive N-succinyl chitosan /alginate hydrogel bead for 5-fluorouracil delivery

Xiao-Qiang Li, Ping Li, Fa-Qin Wang, Yu-Min Li

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Abstract:
In this study, a novel magnetic pH-sensitive N-succinyl chitosan/alginate hydrogel bead was prepared by the single factors test design for controlled the delivery of 5- Fluorouracil (5-FU) and the bead was evaluated for pH sensitivity due to the drug release characteristics. The structure and surface morphology of the bead were characterized by FTIR, SEM, and VSM. The effects of six different factors influencing the swelling ability of the hydrogel bead were also investigated, such as the weight ratio of N-succinyl chitosan and alginate (X1), the weight ratio of drug to polymer (X2), CaCl2 concentration (X3) ,the volume ratio of N-succinyl chitosan/alginate to CaCl2 (X4), crosslinking time (X5), the weight ratio of Fe3O4 to polymer (X6). In addition, the delivery behavior of 5-FU from the hydrogel bead was studied. The amount of 5-FU released from the hydrogel bead at pH 1.5 was relatively low (47.93%), while this value approached 93.91% at pH 6.8. The results clearly suggested that the N-succinyl chitosan/alginate beads had pH-dependent swelling behaviors and a continuous release of 5-FU. From the magnetometer measurements data, the beads also had super paramagnetic property as well as fast magnetic response. So the magnetic pH-sensitive beads may be a potential polymeric carrier for drug delivery in the intestinal tract.

Keywords: 5- Fluorouracil, Magnetic/ pH-sensitivety, Hydrogel, N–succinyl chitosan, Release.

Formulation and in-vitro evaluation of vinyl ester type polymeric prodrugs of naproxen as drug delivery systems

Mirzaagha Babazadeh

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Abstract:
This present research work describes synthesis and in-vitro evaluation of a serious of vinyl ester type polymeric systems linked to naproxen as materials for drug delivery. First, naproxen reacted with vinyl acetate in the presence of catalyst to obtain vinyl ester derivative of naproxen. The resulted material was then copolymerized with 2-hydroxyethyl methacrylate and methyl methacrylate by utilizing azoisobutyronitrile as an initiator at the temperature range of 65-70°C to give drug-polymer conjugates. The obtained materials were characterized by FT-IR, 1H-NMR, 13C-NMR and elemental analysis techniques to confirm their structures. The hydrolysis of drug-polymer conjugates was carried out in cellophane membrane dialysis bags containing aqueous buffer solutions (pH 1, 7.4 and 10) at 37°C for 24 h. Detection of hydrolysis solution by UV spectroscopy at selected intervals showed that naproxen can be released by hydrolysis of the ester bond between the drug and polymer backbone. The release profiles indicated that the hydrolytic behavior of polymeric prodrugs is strongly based on the polymer hydrophilicity and the pH value of the hydrolysis solution. The obtained results suggested that these polymeric prodrugs could be useful for release of naproxen in controlled release systems after in-vivo examinations.

Keywords: Naproxen, Non-steroidal anti-inflammatory Drugs, Polymeric Prodrugs, Drug Delivery Systems, Polymerization.

Elemental analysis (ICP-OES), antibacterial and antioxidant activity of Maesa indica (Roxb.) A.DC

Rakesh K N, Dileep N, Syed Junaid, Prashith Kekuda T R, Ramesh Kumar K A, Vinayaka K S, Raghavendra H l

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Abstract:
Maesa indica (Roxb.) A.DC (Myrsinaceae) is a small tree or a large shrub. The present study aimed to estimate major and minor elements in powdered leaf and to determine antibacterial and radical scavenging activity of petroleum ether, chloroform, ethyl acetate and methanol extracts of leaf of M. indica. The elements in leaf powder were estimated using ICP-OES technique after microwave digestion. Antibacterial activity of solvent extracts was performed by Agar well diffusion assay. Radical scavenging effect of solvent extracts was determined by DPPH and ABTS radical scavenging assay. Total phenolic and flavonoid content of solvent extracts was estimated by Folin-Ciocalteau reagent and Aluminium chloride colorimetric estimation method respectively. Among major elements, the content calcium and sodium was highest and least respectively. In case of minor elements, the content of iron and chromium was highest and least respectively. The solvent extracts showed inhibitory potential against Gram positive and Gram negative bacteria but to a varied extent. All solvent extracts were found to scavenge both DPPH and ABTS radicals. Scavenging effect was superior in case of methanol extract followed by ethyl acetate, chloroform and petroleum ether extracts. The content of total phenolics as well as total flavonoids was higher in case of methanol extract than others. A direct correlation was observed between the phenolic and flavonoid content of extracts and the radical scavenging potential of extracts.

Keywords: Maesa indica, ICP-OES, Agar Well Diffusion, DPPH, ABTS, Total Phenolic, Flavonoids.

Evaluation of the effect of storage on the physicochemical properties of folic acid tablets formulated with sorgum starch

Mshelbwala K, Ofokansi K C, Kenechukwu F C, Bangudu A B, Onaolapo J O, Achuam J, Momoh M A, Ogbonna J D N

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Abstract:
Assessment of the stability of pharmaceutical formulations is always crutial in pharmaceutical product development. Stability could be viewed from the degradation of the active ingredients or a change in the physicochemical properties of the formulations. The objective of this study was to evaluate the effect of storage on the physicochemical characteristics of sorgum starch-based folic acid tablet formulations vis-a-vis tablets prepared with maize starch BP, a standard tablet binder. The folic acid tablets were prepared by wet granulation technique using sorgum and maize starches, and evaluated for physical properties, such as weight variation, thickness, hardness, friability, disintegration time, drug content and in vitro drug release study. The formulations were subjected to stability studies as per ICH guidelines at different temperatures and humidity conditions. Results indicated that the folic acid tablets did not show any appreciable changes with respect to hardness, disintegration time, drug content and dissolution profiles. In addition, results revealed that the stability of folic acid tablets formulated with the local sorgum starch as binder compared favourably with those formulated with imported maize starch B.P. when stored under various conditions of temperature and humidity over a period of one year. This study has shown that proper storage conditions are very necessary for folic acid tablets to have long shelf life, as high temperature and high humidity would negatively affect the stability of these tablets.

Keywords: Sorgum, Folic Acid Tablets, Physicochemical Properties, Maize, Stability, Starch.

Effect of diluents on immediate release tablet of hydrochlorothiazide

Ujjwala Y Kandekar, P D Chaudhari

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Abstract:
The current study is aimed to study the effect of diluents on the immediate release tablet of hydrochlorothiazide. The diluents used are Avicel PH 101 and starlac. Various flow properties are determined for the powder blend and optimised within the range with the help lubricants and glidants. Final bulk is maintained with the help of diluents mainly Avicel PH 101 and starlac. Final tablet are evaluated for various parameters like thickness and diameter, hardness, disintegration time, friability and dissolution rate etc. As the formulation contains diluents in major quantity the effect of these diluents drug release rate is examined. With increase in amount of disintegrating agent release rate is increased up to certain level and then decrease. Release rate of formulations containing Avicel PH 101 is faster as compared to starlac.

Keywords: Avicel PH 101, Starlac, Release Rate.

Comparative study of different solubility enhancement techniques and various excipients on solubility and dissolution rate of racecadotril

Vrushali Tambe, Priyanka Bagade, S K Shrivastava

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The present investigation envisages effect of various excipients and methods on solubility of Racecadotril which is used as an antidiarrhoeal. Solubility of antidiarrhoeal is paramount important for rapid onset of action. Complexation of drug with Beta-cyclodextrin and Hydroxypropyl Beta-cyclodextrin complexes was done by various methods like physical mixing, kneading, lyophylisation, microwave-irradiation, solvent evaporation and fusion. Mannitol and PEG6000 were used for solid dispersion. To ascertain stability of complexes at various pH, the phase solubility studies were carried out at different pH. Complexes were evaluated by DSC, XRD, SEM and IR. AL type profile was obtained with β-CD and HPβ –CD. The stability constants values are in the range of 100-1000 M-1. β-CD showed greater solubility enhancement as compared to all excipients. Enhancement of dissolution rates with increasing quantity of β-CD in the complex was observed. Complex formation is confirmed using various analytical techniques which primarily may be due to hydrogen bond formation.

Keywords: Racecadotril, Solubility, β-CD, Solvent Evaporation, Fusion.

Validation and stability indicating RP-HPLC method for the determination of strontium ranelate API in pharmaceutical formulations

B R C Sekhar Reddy, Nallagatla Vijaya Bhaskar Rao

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The present study describes the development and subsequent of a stability indicating RP-HPLC method for the analysis of Strontium Ranelate. The samples separated on an Inertsil C18 column by isocratic run using Methanol: Water: Acetonitrile 25:25:50(v/v/v) mobile phase with a flow rate of 1.1ml/min, and the determination wavelength was 239nm for analysis of Strontium Ranelate. The described method was linear within range of 10-70μg/ml (r2 = 0.999). The precision, ruggedness and robustness values were also within the prescribed limits (< 1% for system precision and < 2% for other parameters). Strontium Ranelate was exposed to acidic, basic, oxidative and thermal stress conditions and the stressed samples were analyzed by the proposed method. Chromatographic peak purity results indicated the absence of co eluting peaks with the main peak of Strontium Ranelate, which demonstrated the specificity of assay method for estimation of Strontium Ranelate in presence of degradation products. The proposed method can be used for routine analysis of Strontium Ranelate in quality control laboratories

Keywords: RP-HPLC, Strontium Ranelate, Validation, Stability Indicating Assay, Forced Degradation.

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