African Journal of Pharmaceutical Research and Development

Quality assessment of furosemide tablet generics used in a teaching hospital in Nigeria

2025-02-01T22:08:49+00:00

The use of ineffective and poor-quality drugs endangers treatment leading to treatment failure. For the desired therapeutic effect, drugs should contain the appropriate amount of active pharmaceutical ingredients and the required physicochemical properties. This study aimed to evaluate the quality as well as the physicochemical properties of different generics of furosemide tablets used in a teaching hospital in Nigeria. Five different generics of furosemide tablets were purchased from different pharmacy units in the hospital. Their qualities were assessed via identification, assay, weight variation, friability, disintegration and dissolution tests using British Pharmacopoeia standards. All samples contain the stated active pharmaceutical ingredients, however, only two generics have furosemide within the 95 – 105% BP official limit. The weight variation test results indicated that two generics failed to comply with BP specification limits. The generics were found to be able to withstand the rigour of transportation as indicated by their friability values of less than 1 %. The generics were also found to be immediate release tablets as showed by their rapid disintegration time of less than 2 minutes. All the generics released more than 80 % furosemide within 60 minutes. Only two out of the five furosemide generics passed the quality assessment and are therefore expected to yield the desired therapeutic effect.

Effect of extract and fractions of stem bark of Morinda lucida Benth (Rubicaceae) on castor-oil induced diarrhea in mice

2025-02-01T22:31:40+00:00

Morinda lucida Benth is a common Nigerian medicinal plant generally used to cure
malaria parasite infection, though there is a lack of scientific reports on its capacity to
treat diarrhea. The current study evaluated the effect of extract and fractions of stem
bark of Morinda lucida Benth (Rubicaceae) on castor-oil-induced diarrhea in mice. The
ground (500 g) was macerated in 2500 mL of methanol for 72 h, thereafter filtered and
concentrated to obtain methanol extract. The extract (10 g) was subjected to gradient
elution to afford different fractions. The phytochemical screening method was used to
investigate the constituents of extract and fractions. The method of Lorke’s was
employed in the acute toxicity study. The evaluation of anti-diarrhea activity was carried
out by the castor-Oil-induced gastro-intestinal motility model. The secondary
metabolites present in the extract and fractions were alkaloids, flavonoids, saponins,
tannins, terpenoids, cardiac glycoside, anthraquinone glycoside, and steroids. The
Acute toxicity indicated no mortality or any adverse behavioral change even at 5000
mg/kg body weight. The extract at 200 mg/kg dose gave better antidiarrheal activity
than the 400 mg/kg dose indicating that the effect is not dose dependent. Among the
fractions ethyl acetate at 400 mg/kg showed better activity and indicated no significant
difference when compared to loperamide at 2 mg/kg dose. When compared, the
antidiarrheal activity of the extract and fractions differed significantly at (p<0.05) with
negative control. Morinda lucida's stem bark has an outstanding antidiarrheal effect as
a result of its copious bioactive constituents.

Druggability and molecular docking of essential secondary metabolites from Azadirachta indica leaf against angiotensin converting enzyme-2: Covid-19 in focus

2025-02-01T22:51:15+00:00

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly infectious and
virulent coronavirus that arose in late 2019 and poses great risk to public health and safety.
The SARS-CoV-2 utilizes peptidase, angiotensin-converting enzyme 2 (ACE2) for entrance
and invasion into host cells. Thus, this study explored the in-silico druggability and molecular
docking of essential secondary metabolites (ESMs) from Azadirachta indica leaf as potential
inhibitors of ACE-2, a main receptor for the SARS-CoV-2 virus causing the COVID-19
pandemic. Through a literature survey and database mining of known compounds from A.
indica in the National Center for Biotechnology Information (NCBI) database, 12 secondary
metabolites and 5 FDA COVID-19-approved drugs were identified. The in-silico druggability
and molecular docking experiments were performed using SwissADME and ADMETlab tools,
and Autodock vina and UCSF Chimera respectively. Discovery Studio was used for docking
visualization and analyses of ligand-target interactions. The results suggest potential
candidates for further consideration. Of the 12 secondary metabolites from A. indica and 5
FDA-approved drugs identified, azadirachtin A, azadirachtin D, azadirachtin H, azadirachtin F,
azadirachtin I and nimbolin, and ivermectin showed relatively poor druggability. Of the 5 FDAapproved medications for the treatment of COVID-19 under investigation, only paritaprevir was
able to dock (representing 20%); while 6 out of the 12 compounds from A. indica were able to
dock perfectly (representing 50%). The best docking results identified paritaprevir,
desacetylnimbin, azadiradione, nimbin, nimbolide, nimbinene, and azadirone as capable of
binding to ACE-2 with the lowest free energy (binding score) of -14.60, -11.88, -11.60, -12.33,
-12.78, -12.58, and -11.40 kcal/mol respectively. This study indicated that desacetylnimbin,
azadiradione, nimbin, nimbolide, nimbinene, and azadirone from A. indica leaf are potent
inhibitors of hACE2 with high druggability potentials. Hence, they are valuable natural bioactive
compounds capable of targeting ACE-2 as potential therapeutics against the SARS-CoV-2
virus causing COVID-19.

Toxicity and antioxidant assessment of ethanol leaf extract of Hibiscus surattensis in Wistar rats: hepatotoxicity evaluation

2025-02-01T23:03:45+00:00

Hibiscus surattensis is a medicinal plant with a vast beneficial use in the management and
cure of a variety of diseases, ranging from urethritis to inflammation and vertigo among others.
Notwithstanding the population's increasing use of it, particularly in rural regions, there is still
lack of adequate investigation into its toxicity profile. The aim of this study was to investigate
the ethanolic extract of Hibiscus surattensis leaf's potential for hepatotoxicity in Wistar rats.
The acute toxicity test was carried out in two phases (phases 1 and 2). Phase 1, used nine
mice which were randomized into three groups (n=3), receiving graded doses of the extract as
follows: 10, 100, and 1000 mg/kg, ip respectively. Phase 2 used three mice which were
randomized into three groups of one mouse each and administered the extract in graded doses
of 2000, 3500, and 5000 mg/kg, ip, respectively. They were monitored for behavioral
abnormalities, toxicity signs, and mortality for 24 hours following treatment. A subacute toxicity
experiment was then carried out, in which Wistar rats were given oral doses of H. surattensis
extract (141, 282, and 424 mg/kg) every day for eight (8) days. Behavioural changes,
haematological and liver function parameters, in-vivo oxidative stress markers and histological
changes were then evaluated. The LD50 of H. surattensis leaf extract was estimated to be
1414 mg/kg. Results revealed significant rise (p<0.01-0.001) in the levels of alanine
aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP),
conjugated bilirubin (C.B) and total bilirubin (T.B), as well as in white blood cell (WBC) and
platelet at high doses of the extract-treated rats compared to control. A significant reduction
was recorded in catalase among other antioxidant parameters while the histopathological
evaluations showed mild alterations. While caution is urged during long-term administration,
administration of H. surattensis ethanolic extract may be safe at the dosages studied in this
investigation.

Pharmacognostic evaluation of Lasimorpha senegalensis schott leaves (Araceae)

2025-02-01T23:18:14+00:00

The leaves of Lasimorpha senegalensis Schott (Araceae) have long been utilized in
conventional medicine to treat conditions like diabetes, inflammation, malaria, oxidative
stress, and fever. However, its properties have not been standardized to prevent
adulteration. The purpose of this research is to determine Lasimorpha senegalensis
Schott's numerous pharmacognostic, physicochemical, and phytochemical parameters.
Fresh leaf samples and dried leaf powder were examined macroscopically and
microscopically. The physicochemical and phytochemical parameters were determined
using the standard methods. Fresh leaves have a unique scent and are dark green in
colour, leathery texture, and acute apex. In addition to lacking trichomes, they have calcium
oxalate crystals, starch grains, xylem, phloem, epidermal cells, and collenchyma cells.
There was no mucilage, but lignin, starch, cellulose, oil globules, and calcium oxalate
crystals were found by chemomicroscopic examination. The physicochemical assessment
showed 9.2 % moisture content, 8.4 % total ash value, 0.9 % acid insoluble ash value, 2.6
% water soluble ash value, 16.5 % water soluble extractive value, and 41.5 % alcohol
soluble extractive value. The qualitative phytochemical test identified tannins, glycosides,
alkaloids, terpenoids, phenols, and flavonoids, as well as trace amounts of steroids,
saponins, and hydrogen cyanides. This study provided valuable insight into the
pharmacognostic standardization of L. senegalensis leaves and can be used to create a
monograph and prevent adulteration of this important leaf plant.