Aims: A simple TLC Spectrodensitometric method was developed for analysis of Orphenadrine Citrate (OR), Caffeine (CAF) and Aspirin (ASP) either in pure form or in their pharmaceutical preparations.
Study Design: Validation study.
Methodology: In this method, The three drugs were separated on silica gel plate using ethyl acetate: acetone: methanol: triethylamine (6:3:1:0.2, by Volume) as mobile phase at room temperature. Many experimental parameters such as band size, slit width, different developing mobile phases and scanning wavelengths were examined and the optimum conditions were selected. The obtained bands were then scanned at 220 nm. The three drugs were adequately resolved with the Rf values of ASP (Rf = 0.08 ± 0.02), CAF (Rf = 0.55 ± 0.02) and OR (Rf = 0.35 ± 0.02). Validation parameters of the developed method were studied like linearity, accuracy, precision, and specificity.
Results: Linearity of the proposed method was found to be in the concentration ranges 0.4-2 μg/band for ASP, 0.4-2 μg/band for CAF and 0.3-3 μg/band for OR.
Conclusion: The suggested method was effectively used for analysis of ASP, CAF and OR in pure form and in their medicinal formulations. The method is proved to be specific, accurate and selective.
Purpose: To develop a highly selective, reproducible & precise rugged bio analytical method for estimation of Bortezomib (BTZ), “A Protease Inhibitor” in human plasma by validating the developed method in accordance to US-FDA guidelines.
Methodology Envisaged: BTZ D3 was used as an internal standard (ISTD) for the determination of BTZ in human plasma using a rapid & specific liquid chromatographic – Electron Spray Ionization –Mass spectrometric method. The analytical method was moduled with liquid-liquid phase extraction by using annular centrifugal contactor & the samples were analyzed by HPLC, on a column - ACE 5CN (150 x 4.6 mm 5 µm), using mobile phase consisting of ammonium formate buffer: ACN (25:75 v/v), delivered at 1.0 ml/min & 90% flow spitting. Applied Bio system MDS Sciex API 3000 Triple Quadruple MS equipped with Turbo Ion Spray (TIS) as LC/MS interface was used in for MS detection. TIS with multiple reaction monitoring (MRM) were acquired by ESI mass spectra, using the transitions m/z 362.95→310.21 & m/z 172.64→146.06 to quantify BTZ & BTZ D3 respectively.
Results: % variability was ≤ 5.52 & ≤ 6.15 [that was ≤ 15], indicating the specificity of the method, showing no matrix interferences across the elution system. Acceptance is ranging between -8.30 to 2.83 & -4.32 to 1.00% (< 5% CV) & accuracy in the range of 92.73 – 102.20 (< 10% difference) was observed over a linear range of 2.00 – 1000 ng/mL. The mean (n=3) correlation coefficient was 0.9991 & overall mean recovery was 85.62%. Retention time for drug & ISTD is found out to be 0.08 & 0.07; % CV of area ratio is 1.91% & area ratio ≤ 2.51%, which indicated system suitability.
Interpretation and Conclusion: The intended analyte is stable below 10ºC in all the performed stability experimentation & within the acceptance limits. It can be used for investigating drug concentration in routine quality control analysis in API & its pharmaceutical dosage forms.
The Phytochemical and antibacterial activities of Calotropis procera Leaf Organic Fractions were tested against vancomycin and methicliin resistant bacteria isolated from wound patients in Ondo State Specialist Hospital. The bacterial isolates are; Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus mirabilis and Streptococcus pyogenes. Agar well diffusion method was used to determine the antibacterial activities of the extracts on resistant bacterial isolates. Purification of the extracts was carried out using column chromatographic techniques, and the fractions obtained were spotted on the precoated TLC plates to obtain the active fractions by calculating the retention factor (Rf). The antibacterial potency of the active purified fractions was investigated against the resistant bacterial isolates. Ethanol extract had the highest zones of inhibition of 24.01 mm against Staphylococcus aureus while a lowest zone of inhibition of 10.19 was against Klebsiella pnuemoniae. Cold water extract highest zones of inhibition was against Escherichia coli at 15.00 mm and lowest inhibition against Pseudomonas aeruginosa at 7.20 mm. Phytochemical analysis of the extracts revealed the presence of alkaloids, flavonoids, tannin, saponin, terpenoids, cardic glycoside and phenols. The Fourier Transform Infrared (FT-IR) spectroscopic analysis of the active fractions showed five important functional groups namely; phenols, hydroxyl, carbon-hydrogen, carbonyl and aromatic. Findings from this research indicate that the leaf extracts of Calotropis procera posses antibacterial potency which will assist in the preliminary treatment of wound infections, most especially because of its high inhibitory effect against Staphylococcus aureus.
Objective: Lubricants are additives which reduce friction and so essential components of drug formulation. This piece of work was initiated to evaluate coconut oil as a co-processed lubricant in the formulation and compression of paracetamol tablets in comparison with magnesium stearate-talc as standard lubricant.
Methods: Various concentrations 0.5, 1.5, 2.0 and 2.5% w/w lubricant mixtures of magnesium stearate-talc (MT), coconut magnesium stearate-talc (CMT), magnesium stearate (M), coconut oil alone (C) respectively; and without lubricant (None) which served as control were thoroughly mixed with granules (200 mg) prepared from the basic formula for paracetamol tablets which contained 85% w/w, 5% w/w and 10% w/w of paracetamol powder, corn starch and lactose respectively. The mechanical properties of tablets produced were evaluated using crushing strength, friability and crushing strength -friability ratio while the release properties of tablets were evaluated using disintegration and dissolution tests.
Results: Granules lubricated with coconut oil co-processed with magnesium stearate had excellent flow. The crushing strength obtained for all the paracetamol tablets had acceptable values ranging from 4.82 to 6.85 kgf except for tablets lubricated with coconut oil alone. Generally, as the crushing strength values increased the friability decreased. Friability values for all the tablets generally decreased with increasing tablet lubricant concentrations of 2.0% w/w and 2.5% w/w though falling within range considered for conventional tablets. The disintegration time increased with increase in lubricant concentration as all the tablets had acceptable values. Tablets lubricated with coconut oil mixed with magnesium stearate-talc showed the highest CSFR/DT ratio. As the concentration of lubricant increased, there was a general decrease in the rate and extent of the drug release from the formulation.
Conclusion: Coconut oil is an effective lubricant which can be processed with magnesium stearate and talc for an effective lubrication of granules before compression into pharmaceutical tablets.
Seed oils of watermelon, unripe and ripe pawpaw were extracted and analyzed for their fatty acid composition using GC/EIMS, phenolic content and antioxidant potential using free radical scavenging effect on 2, 2-diphenyl-2-picrylhydrazyl (DPPH) radical. Watermelon seed oil has eight fatty acids ranging from C16– C21, unripe pawpaw seed oil has nine fatty acids also ranging from C16 – C21 and ripe pawpaw seed oil has twelve fatty acids ranging from C15-C27. The major chemical component identified in both watermelon seed oil (49.41%) and unripe pawpaw seed oils (39.07%) was 11-Octadecenoic acid methyl ester while 14-Octadecenoic acid methyl ester (40.25%) was the major component identified in ripe pawpaw seed oil. Only watermelon seed oil contained an essential fatty acid; linoleic acid (17.23%) in contrast to previous literatures values (60%). The fatty acids present in these oils are mixtures of saturated and unsaturated homologues. Ripe pawpaw seed oil showed more chemical compounds than the unripe pawpaw seed oil and this may be due to ripening. The phenolic contents of the oils ranged from 1.41-1.55 mg gallic acid equivalent per gram. The three oils showed significant DDPH free radical scavenging potential. The order of inhibition are; watermelon > ripe pawpaw > unripe pawpaw seed oil. The IC50 values of these oils were are, 36 mg/ml, 44 mg/ml and 56 mg/ml for watermelon, ripe pawpaw and unripe pawpaw seed oils respectively. This study however did not show a positive correlation between the phenolic contents and antioxidant activity. We recommend further studies into the use of these oils for treating various specific diseases.
Ocimum sanctum (L) is a well-known herbal plant used for the treatment of bronchitis, malaria, diarrhea, dysentery, skin disease, arthritis, eye diseases and insect bites. It is proposed to have anticancer, antidiabetic, antifungal, antimicrobial, cardio protective, analgesic and antispasmodic action. In our present study, we have tried to explore its antioxidant, free radical scavenging and its ability to prevent damage to protein from free radicals. The antioxidant and free radical scavenging activity of Ocimum sanctum leaves was determined using ferric thiocyanate, thiobarbituric Acid, 2, 2-diphenyl-1–picrylhydrazyl, hydrogen peroxide, hydroxyl radical and superoxide radical scavenging methods. Further, its protein protective property was evaluated using UV- VIS spectrophotometer methods. The results of ferric thiocyanate and 2, 2-diphenyl-1–picrylhydrazyl methods were determined that O. sanctum have strong antioxidant activity (92.12%) and free radicals scavenging property (50.74%) respectively. Further, hydrogen peroxide, hydroxyl radical and superoxide radical scavenging methods determined that extracts (100 µg/ml) have hydrogen peroxide (20.12%), hydroxyl radicals (12.68%) and superoxide radicals (21.68%) scavenging activity respectively. Hemoglobin is a standard protein which was damaged by hydrogen peroxide treatment and this damage was confirmed by UV-VIS spectrophotometer. The extract showed the significant pre and post protein protective action against hydrogen peroxide induced hemoglobin damage. Thus the study concluded that O. sanctum leaves have strong antioxidant, free radicals scavenging and pre and post proteins protective property.
Drug delivery to the posterior segment of the eye is a significantly challenging task due to the underlying physiological, anatomical and metabolic constraints. Delivery of drugs through ophthalmic route is significantly hindered by multiple physiological processes including potential static and dynamic barriers. Moreover, efflux pumps expressed on ocular tissues severely restrict the intra-ocular penetration of drugs, especially into the posterior ocular tissues. However, severe ocular complications which may be sight threatening, pose an urgency for the intervention/ treatment. Currently, invasive intravitreal injections are widely used to drugs/drug candidates to retina and vitreous body. Therefore, non-invasive drug delivery strategies that overcome the barriers encountered in the ocular milieu should be developed and explored. Various topical formulation approaches are being designed in order to address the safety and patient compliance issues associated with invasive routes. In this review, the targeted drug delivery to the ocular posterior segment via minimally invasive approaches is discussed.