PHYTOCHEMICAL, PHARMACOLOGICAL AND FORMULATION STUDIES OF Andrographis paniculata Nee Acanthacae
PHYTOCHEMICAL, PHARMACOLOGICAL AND FORMULATION STUDIES OF Andrographis paniculata Nee Acanthacae
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Date
2010-07
Authors
KUBILI, MSHELBWALA
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Abstract
The leaves of Andrographis paniculata acanthaceae is used locally in Northern Nigerian for
the treatment of hypertension without quantification or dosage standardization. This work
was primarily set out to find justification for the local medicinal use of this plant and to
scientifically study the pharmacological activity of the plant and formulate it into a suitable
tablet dosage form, as a means of standardization of the dosage regimen.
Phytochemical, pharmacological and formulation studies of the leave, aqueous and
Methanolic extracts of the plant leaves were carried out using standard methods.
Phytochemical screening as described in official monograph was carried out to detect the
presence of secondary metabolites. Extracts were tested for antihypertensive activity in cats
by monitoring changes in blood pressure following administration of the extract. The
antihypertensive activity was compared with propranolol (standard drug). Toxicity study
was also carried out by determining the LD50 of the extract in rats.
In formulation studies, micrometric properties of the extracts and granules such as size
distribution, moisture content, angle of repose. Carr’s Index etc., were determined using
different binders (maize starch, polyvinyl pyrollidone (PVP) and gelatin). Disintegrants
(maize starch, pregelationised starch, microcrystalline cellulose, heavy magnesium
carbonate and dicalcium phosphate) and diluents (Lactose and heavy magnesium carbonate)
were also included in the formulations. Different methods of formulations were carried out,
but only the best three of the Methanolic extracts were used for this work. Properties of the
resulting tablets such as weight variation, crushing strength, disintegration properties,
friability and dissolution profiles were determined and analyzed. Effects of storage
condition (such as humidity and temperature) on the tablet properties were also determined.
Stability studies on the extract were carried out using TLC technique and Differential
Scanning Calorimetry (DSC).
Results of the Phytochemical test showed that the plant extract contained alkaloids tanning,
cardioglycosides, flavonoids and terpenes. The plant is relatively safe, with an LD50 of 1.90
x 104mg/kg body weight which is much higher than those of 0.81mg/kg body weight taken
by the local people. Pharmacological studies showed that the leave extract possesses
significant antihypertensive activity, comparable to Propranolol with methanol extract
exhibiting greater activity.Qualitative and pharmaceutically acceptable tablets could only be produced from
Methanolic extract using the wet granulation method. When excipients such as
pregelatinzed starch (disintegrants), heavy magnesium carbonate (diluents) and 2.5% w/v
gelatine binder was used. The thin layer chromatography and DSC studies showed that the
crude extract contain three distinct components. The stability studies showed that the
Methanolic extract tablets were stable under proper storage condition even after 4 years.
Description
A THESIS SUBMITTED TO THE POSTGRADUATE SCHOOL, AHMADU BELLO
UNIVERSITY ZARIA, IN FULFILMENT OF THE REQUIREMENT FOR THE
AWARD OF DEGREE OF DOCTOR OF PHILOSOPHY IN PHARMACEUTICS
DEPARTMENT OF PHARMACEUTICS AND PHARMACEUTICAL
MICROBIOLOGY, FACULTY OF PHARMACEUTICAL SCIENCES,
AHMADU BELLO UNIVERSITY, ZARIA
Keywords
PHYTOCHEMICAL,, FORMULATION,, STUDIES,, Andrographis, paniculata Nee Acanthacae