Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DDP-4 Inhibitor

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

New Drug Approvals Vol 24(2)

not available Bangladesh Pharmaceutical Journal 24(2): 195-197, 2021

Studies of Physico-chemical Properties and Cytotoxicity of Fruits of Syzygium jambos L. against HeLa and Vero Cell Lines

Syzygium jambos L. belonging to the family Myrtaceae has a long history of using as a dietary fruit and folklore medicine. Investigation of this fruit was carried out to evaluate the different chemical properties and biological activities. The moisture and ash content of the fruit sample were calculated as 86.88 ± 0.61% and 0.29±0.02%, respectively. Dried powder of the fruit was extracted successively with nhexane, dichloromethane (DCM) and methanol (MeOH). UV-Visible and FT-IR spectral analyses confirmed the presence of unsaturated carboxylic acid in n-hexane, unsaturated ester in DCM and a diketone in MeOH extracts. Cytotoxicity assay of different extracts was carried out against HeLa and Vero cell lines and no extract was found to be cytotoxic. Total phenolic contents of the n-hexane, DCM and MeOH extracts were 15.39 ± 0.24, 31.32 ± 0.25 and 42.19 ± 0.16 mg gallic acid equivalent per gram of dry extract, respectively and total flavonoid content of n-hexane, DCM and MeOH extracts were 6.52 ± 0.18, 15.55 ± 0.16 and 8.36 ± 0.16 mg quercetin equivalent per gram of dry extract, respectively. This study establishes that S. jambos fruit can be a potential source of natural antioxidants. Bangladesh Pharmaceutical Journal 24(2): 111-116, 2021

First-Time Generic Approvals Vol 24(2)

not available Bangladesh Pharmaceutical Journal 24(2): 198-199, 2021

Cytotoxicity and Sedative Activity of Steam Bark of Dillenia indica L.

The study aims to assess the cytotoxic activity of the methanolic extract (CME) and various fractions from the bark of Dillenia indica L (Family: Dilleniaceae) using brine shrimp lethality bioassay and sedative activities using hole cross, open field, and elevated-plus maze (EPM) test in Swiss albino mice. In brine shrimp assay, the LC50 for CME, pet-ether (PETF), chloroform (CHF) and aqueous (AQF) fraction were found to be 110, 24.55, 85 and 14.45 μg/ml, respectively, indicating significant cytotoxicity of PETF and AQF when compared to the standard vincristine sulfate (7.5 μg/ml). In open field test, the number of movements per min (after 120 min) was 40.90, 12.43, 5.45, 3.66, and 29.74 for control, standard diazepam, CME, CHF and AQF, respectively, indicating strong activity of the chloroform soluble fraction compared to the other test samples of D. indica. Similar data was observed in hole cross test where the number of movements per minute after 120 min were 3.60, 5.56, 4.77, and 7.99 for the standard, CME, CHF and AQF, respectively. In EPM test, the CME showed a significant decreased percentage of entries of mice into the open arms of EPM as well as the percentage of time spent in the open arms. The result indicates that the CHF significantly suppressed the locomotor activity than that of methanol and aqueous fractions. These findings will be helpful for bioassay-guided isolation of active principles responsible for cytotoxicity and sedative activities. Bangladesh Pharmaceutical Journal 24(2): 105-110, 2021

Phytochemical Screening and In vivo Analgesic Activity of Ampelocissus barbata (Wall.) Planch.

Ampelocissus barbata (Wall.) Planch. is a native medicinal herb in Bangladesh. The present study was aimed at exploring the phytochemical compositions and analgesic potential of the plant in vivo. The methanol extract of A. barbata along with its different fractions were subjected to phytochemical evaluation through established chemical tests for ascertaining the available pool of secondary metabolites within the plant. Eventually, the presence of at least eleven classes of phytoconstituents viz. alkaloids, flavonoids, phenolics, glycosides, saponins, starch, phytosterols, coumarins, tanins, resins and quinones were demonstrated. Among the four partitonates, ethyl acetate soluble fraction of A. barbata illustrated the maximum types of secondary metabolites qualitatively. The ability of the crude methanol extract (MEAB) and its ethyl acetate soluble fraction (EAAB) to suppress nociception both centrally and peripherally were investigated in Swiss albino mice by tail immersion method and acetic acid-induced writhing method, respectively. At the 90th minute of the tail immersion study, both MEAB and EAAB administered at the doses of 250 and 500 mg/kg body weight (MEAB1, MEAB2, EAAB1, EAAB2) exhibited 240.41%, 285.34%, 302.83% and 339.60% elongation of pain response, respectively, in comparison to the standard, pentazocine which effectuated 421.36% elongation at the same mark. Moreover, the test samples at the same doses as before exhibited reduction of pain sensation by 66.81%, 74.08%, 76.81%, and 83.52%, respectively, in the acetic acid-induced writhing response in mice. Both the central and peripheral analgesic potentials of EAAB were discernibly higher than those of MEAB at both doses. The findings of the study represents the pharmacological potential of this species in appropriate animal model for the first time and provides valid foundation to warrant future scientific endeavors into the plant. Bangladesh Pharmaceutical Journal 24(2): 117-124, 2021

Formulation and Evaluation of Fixed-Dose Combination Immediate Release Tablets of Ibuprofen and Famotidine through Quality by Design Approach

Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed by the physicians for the management of pain due to their anti-inflammatory and analgesic properties. Long term use of NSAIDs causes gastrointestinal (GI) toxicity and the common GI disorders are indigestion, ulcers or bleeding. Therefore, the production of local oral tablets containing NSAIDs and gastro-protectant is inevitable. In this experiment, combination of ibuprofen 600 mg and famotidine 20 mg tablets were prepared by direct compression technique, which is unique in Bangladesh. To pursue the study Design of Experiments (DoE) approach was implemented to create fifteen trial formulations where Polyvinylpyrrolidone (PVPK30) 1%-3%, Microcrystalline Cellulose (Avicel PH-102) 1%-7% and Starch-1500 1%-13% were considered as independent variables and the responses were depicted in friability and disintegration time which were found 0.21–0.45% and 1.8–20.5 minutes respectively. Out of fifteen formulation trials (F-1 to F-15), seven formulations (F-3, F-6, F-8, F-9, F-10, F-13 and F-14) had met the acceptable criteria and one formulation (F-9) with independent variables PVP-K30 2.00%, Avicel PH-102 4.75% and Starch-1500 6.5% was selected because of its better disintegration, dissolution and friability profile. Data obtained from in-vitro dissolution tests were fitted to different kinetic models such as zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas models. Also, a compatibility study was conducted using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA) and X-Ray Diffraction (XRD). Furthermore, Scanning Electron Microscopy (SEM) was performed to analyze surface morphology. Finally, the selected formulation was compared to FDA regulated QC parameters and proved its superiority over conventional market products. Bangladesh Pharmaceutical Journal 24(2): 133-148, 2021

New Indications & Dosage Forms for Existing Drugs Vol 24(2)

not available Bangladesh Pharmaceutical Journal 24(2): 200-201, 2021

Knowledge, Attitude, Perception of Biological Science and Healthcare Professional Students to Complementary and Alternative Medicine Health Belief and Practice in Southeastern Region of Bangladesh: A Comparative Study

The health professionals require scientific knowledge to advise their patients on complementary and alternative medicines (CAM). Previously, several studies were conducted regarding the CAM perception, attitude and use on health care professionals only; in contrast, our study encompasses both students of health care professionals and other disciplines. The aim of this study was to compare the attitudes and perception about CAM practices between students of biological sciences (Biochemistry and Molecular Biology, Microbiology and Botany) and health care professionals (Pharmacy and medical students) in public and private universities located in the southeastern region in Bangladesh. The questionnaire-based study conducted on 332 systematically sampled students (four private and one public universities) located in the southeastern region in Bangladesh. The cross-sectional study was conducted from March to July, 2018. All students showed a positive attitude towards CAM use. Herbal medicine, homeopathy, nutritional supplements followed by hypnosis, massage, spiritual healing, and meditation were the most commonly known and used CAM modalities. Most of the students (40.7%) believed that the integration of CAM and conventional medicine should be essential in health care setting. The major obstacles for CAM use are patient interest (48.2%) and lack of physician interest (43.4%). In addition, 36.7% students believed that CAM practices should be included in their school’s curriculum. Moreover, 39.5% students assumed that CAM knowledge is important to their daily life. Biological sciences and healthcare professional students of Bangladesh showed positive perception on CAM uses. Bangladesh Pharmaceutical Journal 24(2): 159-167, 2021

Free Radical Scavenging, Membrane Stabilizing and Thrombolytic Potentials of the Leaves of Quisqualis indica (L.)

Bangladesh is a land of thousands of plants which might provide a scope to obtain therapeutically important natural drugs. Systematic screening of plants is very vital to fulfill this goal. Quisqualis indica (L.) is a vine and it belongs to the Combretaceae family. It grows all over the Bangladesh. It has some local uses to treat headache, skin disease, diarrhea, fever, cough, etc. In order to assess its biological potential, the leaves of the plant were collected and subjected to methanol extraction followed by fractionating into petroleum ether, carbon tetrachloride, chloroform and aqueous soluble materials. Primary free radical scavenging power of the extractives was evaluated using the radicals generated by DPPH and H2O2. Methanol crude extract as well as aqueous and chloroform fractions showed noticeable radical scavenging potential. Besides, these extracts had higher level of phenolics. The membrane stabilizing potential of the extractives was estimated based on the prevention of hemolysis of RBC prompted by hypotonic solution as well as heat. The aqueous fraction showed the highest level of membrane stabilizing potential indicating its primary anti-inflammatory ability. The extractives were also subjected to thrombolytic study. Mild thrombolytic ability was displayed by them compared to the standard. Further studies are required to explore bioactive compounds. Bangladesh Pharmaceutical Journal 24(2): 99-104, 2021