Iranian Journal of Pharmaceutical Sciences

In India, the occurrence of diabetes mellitus is on increase and needs to be addressed properly. Herbal remedies are considered most suitable for the management of type 2 diabetes due to their traditional acceptability and availability, low costs, and fewer side effects. Traditionally Bauhinia tomentosa L. (Family- Fabaceae) is used in the treatment of diabetes in India. Aqueous extract and alcoholic extract (250 and 500 mg/kg) of stem were taken to evaluate the anti-diabetic activity in normal and streptozotocin (65 mg/kg) induced diabetic rats. After 21 days of oral administration of extracts resulted in the significance reduction in blood glucose level. Serum biochemistry showed that serum cholesterol, triglyceride, HDL, LDL levels were significantly decreased by both the extracts and standard drug glibenclamide (10 mcg/kg). HPLC and HPTLC analysis of alcoholic extract found to be rich in flavanoids and phenolic constituents whereas aqueous extract found to possess rich in flavanoids, phenolic constituents, tannins and glycosides. The antidiabetic activity of Bauhinia tomentosa L. may be attributed to its high phenolic and flavanoids constituents.

Determination of terazosin hydrochloride dihydrate (TRZ) in drug substance and tablets was studied by fluorimetric techniques. The fluorimetric methods are based on: (1) measurement of the native fluorescence of the drug in water at 750 nm after excitation at 330 nm. (2) sensitizing the native fluorescence by formation a binary complex of drug with aqueous uranyl acetate (0.1% w/v) at the same Ex / Em. under the described condition. the proposed methods were applicable over the concentration range of (10 -1000 and 0.5-12 ng mL-1) with good correlation ((r2=0.9982 and 0.9987), limit of detection of ( 3.47 and 0.198 ng/mL) and a lower limit of quantification of (10.5 and 0.6 ng mL-1) for method (1) and (2), respectively. The described methods were successfully applied for the determination of TRZ in its commercial tablets without interference from common excipients.

This study was undertaken to assess bioequivalence between test and reference formulations of escitalopram oxalate 20 mg in healthy Indian male subjects. This single-dose, randomized, open-label, 2-period crossover study was carried out in 12 Healthy Indian Male volunteers aged 18 to 55 years under fasting conditions with a wash out of 14 days. The subjects were randomly assigned to receive the test formulation followed by the reference formulation, and then vice versa. Blood samples were collected for up to 156 h postdose. Quantification was carried out using a validated LC-MS/MS method. Maximum plasma concentrations Cmax of 26.386 ± 5.54 ng/mL (test) and 24.430 ± 3.52 ng/mL (reference) were achieved. Areas under the plasma concentration-time curve AUC0-inf of 854.241 ± 91.22 ng. hr/mL (test) and 825.135 ± 1.37 ng. hr/mL (reference), AUC0-t of 848.766 ± 93.26 ng. hr/mL (test), 819.504 ± 1.91 ng. hr/mL (reference) were calculated. The median Tmax was 4.00 hr for test and reference formulation, respectively. Plasma elimination half-lives T1/2 of 19.26 ± 5.95 hr (test), 20.94 ± 2.88 hr (reference) were determined. Both formulations were well tolerated. The 90% confidence intervals obtained by analysis of variance were 94.49-120.68% for Cmax and 98.22-108.18% for AUC0-t which were within the predefined regulatory acceptance limit of 80.00-125.00%.

Potassium chloride (KCl) is a highly water soluble substance which is usually used to prevent hypokalemia. Oil in water disperse phase encapsulation method was used to prepare KCl loaded microcapsules using beeswax and carnauba wax as a hydrophobic matrix. The morphology and characteristics of KCl loaded microspheres were studied using scanning electron microscopy (SEM), photon correlation spectroscopy (PCS) and differential scanning calorimetery (DSC). The particle size distribution of resulting microspheres was narrow and DSC diagrams showed no interaction between waxes and drug. The effective variables were determined using Plackett-Burman design followed by Response Surface methodology for optimization of these variables. Based on this analysis, the most effective parameters on drug loading were found to be beeswax/carnauba wax ratio, drug/wax ratio and rate of emulsification. Using the response surface method, the optimum values of effective parameters were found to be beeswax/carnauba wax ratio = 6.245, drug/wax ratio = 0.668 and rate of emulsification = 679.8 rpm.

The methanol extracts of leaves of Bauhinia acuminata (MESF) and their different fractions obtained from modified Kupchan partitioning method i.e. methanol, pet ether, carbon tetrachloride, chloroform, and aqueous soluble fractions were subjected to biological screening such as total phenolic content and antioxidant activity screening.The amount of total phenolic content differed in different extractives and ranged from 15.90 mg of GAE/gm of extractives to 124.80 mg of GAE /gm of extractives of B. acuminate. Among all extractives of B. acuminate the highest phenolic content was found in AQSF (124.80 mg of GAE /gm of extractives) followed by CSF (103.78 mg of GAE /gm of extractives).Significant amount of phenolic compounds also present in CTCSF (75.59 mg of GAE /gm of extractives), MESF (66.20 mg of GAE /gm of extractives) and PETSF (15.90 mg of GAE /gm of extractives) were also found. The antioxidant activity of IC50 values in DPPH method differed in different extractives and ranged from 22.01 to 77.79. Among all extractives of B. acuminata the highest free radical scavenging activity was given by CTCSF (absorbance 22.01) followed by AQSF (absorbance 29.83).Significant free radical scavenging activity was also exhibited by CSF (absorbance 45.09), MESF (absorbance 43.78), PESF (absorbance 77.79).

The objective of the present study was to determine the antilipidperoxidation and in vitro α-amylase and lipase inhibitory activity of the Boswellia ovalifoliolata Bal Henry (BOB) extract. The polyphenolic compounds, flavonoids, and tannins content of the extracts were estimated by spectrophotometry. Antioxidant activity on goat liver lipid peroxidation and linoleic acid was determined.Moreover, α-amylase and lipase inhibitory activities were evaluated. All the extracts showed antioxidant, α-amylase, and lipase inhibitory properties. Among the other extracts of BOB, macerated methanol extract could extract the highest concentration of polyphenols, flavonoids, and tannins. Even macerated methanol extract showed antioxidant activity on goat liver lipid peroxidation and linoleic acid were 62.83±4.723 (p<0.01) and 56.67± 1.43 (p<0.01) respectively. Maximum α-amylase and lipase inhibitory activities were expressed as 56.34±2.1 (p<0.01) and 79.36± 1.58% (p<0.01) respectively for macerated methanol and ethanol extracts. The results indicated that all the extract exhibited low inhibition activity as compared to standard.

Promethazine hydrochloride, a 5-HT3 antagonist is a powerful antiemetic drug with an oral bioavailability of 25% due to extensive hepatic first pass metabolism and is extremely bitter in taste. To overcome the above draw backs, the present study was carried out to formulate and evaluate fast dissolving taste masked wafers of Promethazine hydrochloride for sublingual administration. Taste masking was achieved by inclusion
complexation with β-Cyclodextrin, confirmed by e-tongue evaluation. The wafers were prepared by lyophilization, using polymers such as Gelatin, Xanthan gum and Methyl cellulose in different ratios. The IR
spectral studies showed no interaction between drug and β-Cyclodextrin or with other additives. Satisfactory results were obtained when the wafers were subjected to tests such as uniformity of weight, thickness, surface
pH, uniformity of drug content, disintegration time, moisture uptake, moisture loss, moisture content, and in vitro drug release studies. Ex vivo drug permeation studies were carried out using porcine membrane model and a drug permeation of 33-99% was observed through porcine mucosa within 6 min. In vitro release studies indicated 98-100% release within 6 min. A higher percentage of drug release was observed from wafers
containing a combination of Gelatin and Xanthan gum. The stability studies conducted for a period of 12 weeks showed no appreciable change in drug content, surface pH, and in vitro drug release and ex vivo permeation for the first 8 weeks. Thus stable, porous, uniformly loaded fast disintegrating, taste masked Promethazine HCL lyophilized sublingual wafers with good compatibility and stability were achieved.

Non-Steroidal Anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase (COX)-2 inhibitors, have come to play an important role in the pharmacologic management of musculoskeletal disorders. Clinical trials have established the efficacy of etoricoxib in Osteoarthritis, Rheumatoid Arthritis, Acute Gouty Arthritis, Ankylosing Spondylitis, Low back pain, acute postoperative pain, and primary dysmenorrheal. The present research has been undertaken with the aim to develop a novel topical cream formulation of etoricoxib, which would attenuate the gastrointestinal relater toxicities associated with oral administration. Etoricoxib is a highly selective cyclooxygenase‐2 (cox‐2) inhibitor. In the present study, a fixed concentration of Etoricoxib cream (1%) was prepared by using a different combination of Active ingredient and Excipients. To access the efficacy of formulated cream, in vitro evaluation including stability studies, tube extrudes ability, spread ability, pH, viscosity and
rheological properties as well as drug diffusion studies were done. After in vitro evaluation of cream formulations, the formulation was evaluated for the anti‐inflammatory and skin irritation study. The results obtained were encouraging and formulation containing Etoricoxib (1%) exhibited the most satisfying results of all the parameters.