Volume 9, Issue 1, Jan-Mar 2017

Volume 9

January-March 2017

Fixed dose combination product: A review

Ige Pradum Pundlikrao

Abstract:
Fixed dose combination (FDC) are combinations of two or more active drugs in single dosage forms. It is the current hot topic of deliberation in the pharmaceutical industry, drug regulatory agency and pharmaceutical trade. It is not so among the doctor who prescribed the medicine or the patients who consume. Basically, it is increases the patients compliance but there are chances of consuming medicines, more than what is required. Reducing treatment complexity can be achieved through the use of single tablet fixed dose combinations of two active pharmaceutical ingredients. FDC’s improve patient compliance by reducing the number of pills. Clinical studies revealed that fixed dose combinations had many benefits compared to single entity and separate agents in terms of effects, convenience, compliance and cost. FDCs have become an important alternative to monotherapy in the treatment of diseases as hypertension, diabetes, cancer, tuberculosis, asthma and COPD by offering several advantages including patients compliance, simple dosage schedule, superior efficacy and tolerability, reduced risk of adverse events, cheaper shipment and packaging activities. In conclusion, FDCs had critical issues during evaluation such as safety efficacy, bioavailability and stability.

Keywords: Fixed Dose Combinations, Regulation of FDCs Products, India’s Regulatory Framework.

Study of Eudragit RS 100-indomethacin floating microballoons prepared by solvent evaporation technique

Dinesh M Morkhade, Vishwanath S Nande, S B Joshi

Abstract:
In this study, the floating microballoons of indomethacin were prepared by o/o solvent evaporation technique using Eudragit RS 100 as a wall polymer. Amongst different wall polymers, therapeutic agents and the anti-tacking agents, only, Eudragit RS 100: indomethacin: magnesium stearate system was able to float for a prolonged period of time. Thus, microballoons with this system were produced and evaluated for the impact of core: coat ratio, viscosity of liquid paraffin and stirring speed of external phase (EP). Increase in polymer concentration increased the particle size, drug loading, buoyancy, and decreased the porosity and drug release rate of microballoons. In contrast, increase in stirring speed and viscosity of EP decreased the particle size, buoyancy, drug loading, and increased the porosity and drug release rates of microballons. Microballoons particle sized ranged from 164 to 247 µm. Microballoons prepared with polymer: drug ratio of 2:1 released 28.31% drug at the end of 10 h. Drug release from most of the formulations followed Hixson-Crowell kinetic equation. Results revealed that Eudragit RS 100 can form floating microballoons with indomethacin conceivably by the formation of network between the quaternary ammonium groups of Eudragit RS 100 and Cl of indomethacin. Such microballoons, owing to their floating propensity, are promising candidates for sustained drug release.

Keywords: Eudragit RS 100, Indomethacin, Floating Microballoons, Solvent Evaporation, Magnesium Stearate, Hixon-Crowell Kinetics.

Development and evaluation of novel wound healing hydrogels based on PEGylated Mucuna flagellipes gum

Akpa P A, Kenechukwu F C, Okpe C, Momoh M A, Attama A A

Abstract:
This work was designed to evaluate the drug delivery and therapeutic (wound healing) potentials of PEGylated Mucuna flagellipes seed gum. The gum was extracted, PEGylated, dried, pulverized and sieved. The physicochemical properties of unPEGylated and PEGylated gum were determined. The wound healing activity of the PEGylated gum was evaluated using contraction of excision wounds on rat skin treated with varying gum-PEG ratios of 1:1, 1:2, 2:1, 1:3, 3:1, 1:1.5(2:3), 1:0 and 0:1, and their effects compared with standard antibiotic (cicatrin powder) and the untreated wounds by monitoring the wound healing process for three weeks. Results obtained from the characterization studies showed that there were enhanced physicochemical and biological properties in the PEGylated gum. The PEGylated gum showed significant increase in wound healing (p < 0.05) compared to the unPEGylated gum (negative control) and positive control (cicatrin powder). In all ratios, there was a progressive increase in rate of wound healing and this was due to the contributory action of the combined gum and PEG to wound healing. However, the 1:1.5 ratio PEGylated gum healed the wound faster than cicatrin powder; it healed the wound after 15 days, while cicatrin healed after 18 days. Thus, PEGylated Mucuna gum could be used as wound healing agent especially at optimal gum-PEG ratio (1:1.5). This study has shown that PEGylated mucuna gum has values in management of superficial skin wounds.

Keywords: Mucuna flagellipes Seed Gum, PEGylation, Characterization, Wound Healing.

Hepatoprotective activity of Ervatamia heyneana leaves extracts on carbon tetrachloride induced hepatotoxicity in rats

Nasreen Begum, Radhika B, Srisailam K

Abstract:
The present study was aimed at investigating hepatoprotective activity of different extracts of leaves of Ervatamia heyneana with a view to justify the use of the plant. The various extracts of leaves of Ervatamia heyneana were obtained by successive soxhlation with petroleum ether (60 – 80°C), chloroform, ethyl acetate, methanol and water for 6 hours. The dried extracts of leaves (Petroleum ether, methanol and aqueous) were used for hepatoprotective activity against carbon tetra chloride induced liver damage in albino rats. Various biochemical parameters were studied to evaluate the hepatoprotective activity of the extracts for total bilirubin (TBL), alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), total protein (TPL) and albumin levels (ALB). This study revealed that aqueous extract (500mg/kg) showed significant activity which was comparable to that of standard drug silymarin (100mg/kg). Aqueous extract (500mg/kg) was found to protect the rats from hepatotoxic action of carbon tetra chloride as evidenced by significant reduction in the elevated serum enzyme levels. Histopathological studies showed regeneration of hepatocytes of the extract treated liver samples which stipulate its hepatoprotective activity.

Keywords: Ervatamia heyneana, Carbontetrachloride, Hepatoprotective Activity.

RP-HPLC method development and validation for the determination of alfuzosin HCl in bulk and pharmaceutical dosage form

Umay Chen, Shadia Afrin, Antara Ghosh, Sujan Banik

Abstract:
The present study was undertaken to develop a simple, rapid, accurate and sensitive reverse phase HPLC method for determination of Alfuzosin HCl in bulk powder and pharmaceutical dosage form. The chromatographic separation was accomplished on Hypersill ODS (250×4.6mm, 5μm) column using a mobile phase methanol: water is 90:10 (v/v) at a column temperature of 25°C. The eluents were monitored at 244 nm and total run time was 5 min with a flow rate of 1 ml/min. The drug was well resolved on the stationary phase and the retention time was found as 1.3±0.89 min with injection volume of 20µl. The method was found to be linear at concentration ranges of 10-50μg/ml with correlation coefficient of 0.999. The method was validated for linearity, precision, robustness and accuracy as per ICH guidelines. The results of all the validation parameters were well within their acceptance values (%RSD <2.0 specified by the USP, ICH and FDA), which prove applicability of the proposed method for routine analyses and quality-control assay of Alfuzosin HCl in pharmaceutical preparations.

Keywords: Alfuzosin HCl, Bulk Powder, RP-HPLC, Tablets, Validation.

Formulation and evaluation of anti-emetic microspheres for nasal drug delivery system

Jaya Nigam, Preeti Pandey, Manoj K Mishra

Abstract:
The microsphere with natural biodegradable polymer creates immense potential for various pharmaceutical applications like mucoadhesive drug delivery via nasal route. Microspheres formulation helps in sustaining the release may be suitable for long term therapy is controlled alleviation of clinical manifestation. The purpose of this research work was to develop optimized and systematically evaluate performances of microspheres of antiemetic drug ondansetron. Alginate microspheres coated with polymer pectin, starch corn were prepared by ionotropic-gelation technique utilizing various cross linking agents. The microspheres obtained were discrete, spherical and free flowing. Alginate microsphere loaded with Ondansetron by using Ionic-gelation technique for control prolonged release of drug. Ondansetron microspheres were formulated by using drug with sodium alginate, pectin and starch in 9 formulations were F₁, F₂, F₃, F₄, F₅, F₆, F₇, F₈and F₉. All the formulation were investigation for various evaluation parameters like particle size (360 – 280nm), bulk density (0.55 – 0.46 gm/ml),flow behavior, entrapment efficiency (72 – 85%), percentage yield (55 -78 %), and invitro drug release. All the formulation showed good flow behavior. SEM study revealed that the microspheres were almost spherical in shape with smooth surface. In-vitro drug release study showed that by increasing the polymer concentration, decreased drug concentration among all formulations and the optimized formulation (F₃) was able to sustain the drug release for 12 h. So, it was concluded that alginate microspheres loaded with Ondansetron can be prepared by ionic-gelation technique and used for sustaining the drug release for prolong period of time.

Keywords: Ondansetron, Microspheres, Optimized Formulation, Mucoadhesive Drug Delivery.

Formulation and characterization of Eudragit RLPO based sustained release nanoparticles

Jayanthi, Shymala Bhaskaran, Arti Mohan

Abstract:
Osteoporosis is the most frequent metabolic disease that affects bone. Bisphosphonates, especially, alendronate sodium, are indicated as first line regimen for this disease. Alendronate is highly efficient but presents low absorption after oral administration, due to high water solubility burst release occurs. The aim of the present study was to reduce burst release and to sustain drug release from Alendronate sodium Nanoparticles containing the polymer Eudragit RLPO. The nanoparticles were prepared by Emulsion solvent evaporation technique and were characterized for mean particle size, surface charge, size distribution, drug entrapment efficiency, drug loading capacity and In vitro drug release. Drug excipients compatibility studies performed using DSC instrument indicated that there were no interactions. The results revealed that double emulsion solvent evaporation method is suitable for preparing nanoparticle formulation. The drug loading capacity of the particles varied depending on the drug polymer ratio. The mean particle size of the selected batch was 238 nm.

Keywords: Alendronate sodium, Nanoparticles, Eudragit RLPO, In vitro Release Kinetics.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500