OBJECTIVE: Ibuprofen, a nonsteroidal anti-inflammatory drug, is poorly soluble leading to its slow systemic absorption. This study aimed to optimize the formulation of an ibuprofen hydrogel-based matrix tablet to improve its dissolution for better oral bioavailability.

METHODS: Raw material of ibuprofen was subjected to quality control test and compatibility test with the excipients. Six trial formulations were performed, with polyethylene glycol (PEG) 6000 as the matrix for the first three trial formulations and carbopol for the remaining trial formulations. Finished product quality control (FPQC) tests were conducted to choose the best formulations to be compared against the marketed products using comparative dissolution and stability studies.

RESULTS: Among the trial formulations, Formulation 3 and Formulation 4 displayed highly satisfactory results from FPQC. The results of disintegration tests, comparative dissolution, and stability studies suggested carbopol as the better polymer over PEG 6000 which made Formulation 4 as the best.

CONCLUSION: Based on the percent drug release and similarity factor, it was concluded that the formulation optimized in this study was considered to be similar with the standard liquigel.

BACKGROUND AND OBJECTIVE: Pectin is a complex polysaccharide which is commonly used as a gelling agent for food preparations and pharmaceutical formulations. Currently, the Philippines imports 100% of its pectin requirement from other countries which adds to the cost of products that utilizes pectin. Hence, the aim of this study was to isolate and characterize pectin from ripe jackfruit peels.

MATERIALS AND METHODS: Peels of ripe jackfruit (Artocarpus heterophyllus Lam.) were subjected to digestion with water and sulfuric acid at 90°C then purified using alcohol and acetone. The isolated material from the peels was subjected to pectin identification tests using the methods from the US Pharmacopeia (USP). To further characterize the isolate, the methoxy and anhydrouronic acid contents, degree of esterification, functional groups (through FT-IR), ash content, and swelling index were determined.

RESULTS: Ripe jackfruit peels yielded 5.74% of brown-colored pectin which was verified using the US Pharmacopeia identification tests for pectin. The methoxy and anhydrouronic acid contents were found to be 4.05% and 1.77%, respectively, with results comparable with the standard pectin (p<0.05). The peel's pectin has a degree of esterification of 26.34, 1.77% ash content, and swelling index of 9.09. FT-IR analysis of isolated pectin revealed functional groups identical to that of the standard pectin.

CONCLUSION: Pectin from the ripe jackfruit peels is reported to be a potential source of pharmaceutical grade pectin. However, the AUA content and methoxy content of the isolated pectin did not meet the USP specification. Thus, the authors recommend that future investigators must optimize the isolation procedure to obtain pectin which meets the specification of USP.

Objective: To determine the antiangiogenic activity of Telescopium telescopium (Horn snail) extract using in ovo chorioallantoic membrane (CAM) assay. Methods Methanolic extract of Telescopium telescopium was subjected to modified Kupchan partitioning. Four treatment groups – negative control, positive control (quercetin), test samples, and blanks – were used for the in ovo chorioallantoic membrane (CAM) assay. ImageJ software was used to measure average vessel diameter (DV) and total length (LT) to determine the degree of vascularization, percent inhibition, and antiangiogenic activity. Biochemical screening was done for the crude extract and the fraction with the highest percent inhibition.
Chorioallantoic Membrane ; Gastropoda

Objective: The study determined the safety, efficacy and acceptability of a Philippine community preparation of Siling Labuyo liniment in the management of knee osteoarthritis. Methods: A 6-week randomized, double-blind, active-controlled clinical trial was conducted in three municipalities of Cavite from 2017-2018. The municipalities were randomly assigned to either the control or experimental group, using a commercially available Diclofenac 1% gel as the control agent. Knee Injury and Osteoarthritis Outcome Score (KOOS) and Pain Visual Analogue Scale (VAS) were used to measure the outcomes. Results: Forty-seven participants completed the study. Statistically significant improvement (p<0.05) in pain relief, reduction of symptoms and increase in knee functionality was reported by participants in both the experimental and control groups. Across the dimensions measured, at least 30% improvement in scores was reported by the experimental group, and at least 40% by the control group. The difference was statistically not significant (p>0.05). Itching (13%), burning sensation (11%) and reddening of the skin (15%) were experienced in both the experimental and the active control groups. Conclusion Use of the liniment led to a modest therapeutic effect and was well-tolerated by the participants.
Diclofenac ; Osteoarthritis, Knee ; Pain

OBJECTIVES

Carica papaya has been widely used commercially for skin care due to its therapeutic benefits. The potential of its flower to promote hair growth has been traditionally recognized in other countries but not in the Philippines. In this study, we explored the effect of various extracts of C. papaya flower in the biological activities associated with hair loss, including 5α-reductase inhibition and antioxidation, as well as identified the putative compounds present in the most potent extract.

The flowers of C. papaya were macerated separately with ethanol, ethyl acetate, and hexane to obtain their corresponding crude extracts. These extracts were subjected to antioxidant tests via 2,2′-diphenyl-1-picrylhydrazyl (DPPH), and ferric-reducing antioxidant power (FRAP) assays. The total phenolic and flavonoid contents (TPC and TFC) of the crude extracts were determined, as well as the ability of the extracts to inhibit 5α-reductase. The compounds present in the most potent extract were determined using ultraperformance liquid chromatography quadrupole time of flight mass spectrometer (UPLC/MS-QToF).

Ethyl acetate extract displayed significantly higher DPPH activity (0.001755 ± 0.00092 ascorbic acid equivalent antioxidant capacity) and 5α-reductase inhibitory activity (115.18 ± 11.61 mg dutasteride/g) compared to ethanol (DPPH: p=0.0121; 5α-reductase: p=0.0016) and hexane (DPPH: p=0.0038; 5α-reductase: p < 0.0001) extracts. Similarly, ethyl acetate extract gave the highest FRAP (0.4842 ± 0.0936 mg ascorbic acid/g) activity, TFC (0.0403 mg quercetin/g), and TPC (0.0463 mg gallic acid/g) among the extracts. Forty-nine compounds were annotated in the ethyl acetate extract, with seven (7) putatively identified as fatty acids (9-hydroxy-10,12-pentadecadienoic acid, 9,12,15-octadecatrienoic acid), hydroxyflavone (5-methylkaempferol), alkaloid (allomatrine), dipeptide derivative (aurantiamide acetate), bufotalinin, and 6β-acetoxy-5-epilimonin based on the Traditional Chinese Medicine Library.

These results suggest that local C. papaya flowers can be a source of hair growth-promoting agents via their antioxidant and 5α-reductase inhibitory potential.

Background: Pectin is a pharmaceutically relevant excipient that can be upcycled from selected Philippine fruit peel wastes. Method optimization of pectin extraction leads to maximizing yields from limited resources, while also reducing environmental wastes, and providing local alternative sources. Objectives: This study aimed to optimize the method of extracting pectin from selected Philippine fruit peel wastes using the Box-Behnken design, by varying the acid extraction solvent, treatment time, and working temperature. Methodology: The three-level (-1, 0, 1) Box-Behnken design (15 set-ups) was used to optimize the pectin extraction in each of the fruit peel samples (C. maxima; A. heterophyllus; ripe and unripe M. indica; D. zibethinus; and H. undatus). The three experimental factors were the type of 3N acid used as extracting solvent (HNO₃, H₂SO₄, and HCl); duration of treatment in minutes (60, 90, and 120); and temperature of treatment in C 60, 75, and 90). The %yield was computed in each set-up, and the projected yields were generated using multiple linear regression. The pectin samples obtained from the optimized conditions were subjected to the physicochemical characterization, with apple pectin as the standard. Degree of esterification (DE), equivalent weight (EW), methoxy content (MC), alkalinity of ash (AA), and anhydrouronic acid content (AUA) were performed. Results: Maximum yields were extracted from C. maxima (28.96%), A. heterophyllus (20.12%), ripe M. indica (26.23%), and unripe M. indica (25.89%), using 3N H₂SO₄, for a treatment duration of 60 minutes, at a working temperature of 90 C, and H. undatus (25.03%) at 60 C, for a treatment duration of 120 minutes. Conclusion Optimum conditions were identified to extract pectin in each of the fruit peel samples. The 3N H₂SO₄ produced the highest pectin yields in all of the set-ups, while the treatment time and working temperature vary per fruit peel sample. Pectin extract from C. maxima, A. heterophyllus, and M. indica was comparable to the standard.
Pectins

Objective: The study was conducted to determine the preservative activity of ethanolic extract of mangosteen (Garcinia mangostana L.) pericarp and its compatibility in an antacid suspension. Methods: The extract was subjected to phytochemical screening and was used as preservative in a formulated antacid suspension. Compatibility with the active pharmaceutical ingredient (API) and excipients were analyzed using fourier transform-infrared spectroscopy. Preservative activity of the formulation against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa was assessed using the United States Pharmacopoeia (USP) antimicrobial effectiveness test, with methylparaben as positive control and suspension without preservative as negative control. Results: The extract exhibited pharmaceutical compatibility with API and excipients. The formulation revealed comparable reduction in microbial count of E. coli, S. aureus, and P. aeruginosa with positive control at Day 14 (p=0.916, 0.624, 0.335). At Day 28, comparable activity with positive control was only observed against E. coli and S. aureus (p=0.999, 0.854). However, it displayed significant increase in activity against P. aeruginosa (p=0.010) at Day 28. These activities may be attributed to glycosides and reducing substances present in the extract. Conclusion The ethanolic extract from Garcinia mangostana L. pericarp acted as a preservative in the formulation of an antacid suspension. It conformed to the USP criteria for antimicrobial effectiveness test on bacteria.
Garcinia mangostana ; Suspensions

OBJECTIVE

The aim of this study was to investigate the protective effects of Lactobacillus brevis BIOTECH 1766 against oxidative damage in the brain, liver, and kidneys induced by aluminum (Al) poisoning in ICR mice.

Twenty mice were divided into four groups (n = 5): (I) control, (II) Al, (III) citric acid (CA), and (IV) L. brevis BIOTECH 1766 group. A 14-day treatment period was implemented, wherein groups I and II received sterile water, while groups III and IV received 10 mg/kg bw of CA and 1 x 109 cfu/kg bw of L. brevis BIOTECH 1766, respectively. On day 15, all except the control group received a single oral dose of 1438 mg/kg bw of AlCl3. 6H2O. After 24 h, mice were euthanized to collect the brain, liver, and kidneys for the oxidative stress marker analyses and histopathological examination.

Acute intoxication of Al led to a significant increase in tissue malondialdehyde (MDA) and a significant decrease in the tissue's reduced glutathione (GSH), catalase (CAT), and superoxide dismutase (SOD). Mice pretreated with CA or L. brevis BIOTECH 1766 have markedly reduced CAT activity in the liver, and SOD in all three organs. Extensive organ injuries were also prevented by CA and L. brevis BIOTECH 1766 pretreatment, with the latter providing better protection against liver damage.

The findings showed that L. brevis BIOTECH 1766 provides a protective effect against acute Al poisoning in mice by ameliorating oxidative damage in the brain, liver, and kidneys.

BACKGROUND: This study was conducted to characterize and compare the physicochemical and pharmacopoeial properties of starches isolated from the seeds of Artocarpus odoratissimus Blanco (marang), Nephelium lappaceum L. (rambutan), and unripe green Mangifera indica L. (mango) with corn starch, as possible sources of pharmaceutical grade starch.

METHODS: The starch from the seeds of these fruits was isolated and characterized through their physicochemical (organoleptic characteristics, percent yield, amylose-amylopectin ratio, bulk density, tapped density, compressibility index, Hausner ratio, angle of repose, solubility, swelling power, and viscosity) and pharmacopoeial properties (identification test, pH, loss on drying, and limit of iron). Morphology of the granules was also assessed.

RESULTS: The physicochemical properties showed that amylose content of the seed starches was significantly lower (p=0.001) and amylopectin content significantly higher (p=0.001) than the native high amylose corn starch. The lower values of bulk and tapped densities, and high values in compressibility index and Hausner ratio of the seed starches compared to corn starch may be due to their smaller particles. The results of the pharmacopoeial characterization showed compliance with the United States Pharmacopeia's (USP) acceptable limits, except for the pH of marang seeds.

CONCLUSION: The starches isolated from the fruit seeds have unique properties, but only rambutan seed starch has the most desirable physicochemical and pharmacopoeial properties that is comparable with corn starch. Rambutan seeds could be utilized as a source of starch for pharmaceutical applications.

BACKGROUND: Pectin is a heteropolysaccharide used in pharmaceutical formulations as a binding agent. Importation of pectin costs billions of Philippine pesos, but the local laboratory-scale production of this excipient from fruit peel wastes is estimated to be cheaper by 80%.

OBJECTIVE: To address economic and environment concerns associated with pectin production, this study aimed to optimize the isolation and purification of pharmaceutical grade pectin from pomelo (Citrus maxima Merr.) fruit peel as basis for commercial-scale production.

METHODS: Pectin was extracted from pomelo using different solvents: 6.2% w/w citric acid, 1N acetic acid, 3N hydrochloric acid, 3N nitric acid, and 3N sulfuric acid. Temperatures for extracting pectin were explored at 40°C, 60°C, and 90°C. Obtained pectin samples were characterized based on the following parameters: equivalent weight (EW), methoxyl content (MC), ash content (AC), anhydrouronic acid content (AUA), and degree of esterification (DE).

RESULTS: Highest pectin yield (9.25%) was obtained using 3N nitric acid and 3N sulfuric acid at 90°C.Based from the pharmacopeial standards (MC ? 6.7, AUA ? 74.0), all the samples did not pass the parameters, except the pectin extracted using 3N sulfuric acid at 90°C (MC = 6.76, AUA = 74.61).

CONCLUSION: Among the different solvents used for extraction, 3N sulfuric acid produced the highest percent yield of pharmaceutical grade pectin from pomelo fruit peel. Its optimum temperature for extraction was at 90°C. The sample passed the USP standards of MC values not less than 6.76 and AUA values not less than 74. Under the following conditions, pomelo fruit peel have the potential for commercial-scale production of pharmaceutical grade pectin.