Pharmacokinetic Studies of Gastroretentive Mucoadhesive Matrices for Diltiazem Hydrochloride Using Some Natural Polysaccharides

Shende, M. A.; Marathe, Rajendra

doi:10.5958/0974-360x.2018.00087.2

Cited by 4 publications

(1 citation statement)

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“…Hence, this revealed that the pH of the mucilage was nearly neutral which in turn implied the biocompatibility of the mucilage. Thus, formulations prepared using this material would be biocompatible with minor or no irritation to the mucosal membrane of the GIT [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer

Embafrash Berhe,

Tesfay Mezgebo,

Abrha

et al. 2023

Advances in Pharmacological and Pharmaceutical Sciences

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Being biocompatible, less toxic, cheap, easily available, and environmentally friendly, there is an increased trust in natural polymers in the drug delivery system. Mucilages, among the natural polymers, are the primary metabolites of plants that have been widely utilized in pharmaceutical manufacturing for different purposes, and mucoadhesive is one among them. The present study was designed to investigate the use of LSM as a mucoadhesive polymer using ibuprofen as a model drug. The mucilage was extracted following an aqueous extraction method and its percentage yield was found to be 13.2% w/w. Besides, three microsphere formulations of ibuprofen were prepared using synthetic polymer hydroxyl propyl methyl cellulose (HPMC) K100M and the LSM in polymer to drug ratios of 1 : 1, 1 : 5, and 3 : 5 by applying ionotropic gelation followed by solvent evaporation methods. The microspheres were evaluated for various micromeritic properties and all the formulations exhibited free-flowing properties. Optical microscopic pictures of almost all the microspheres except F3 and F6 (which had more or less spherical shapes) were found to have irregular and discrete shapes. Besides, the surfaces of all the formulations were rough in texture. The drug entrapment efficiency of the microspheres was found to be between 52.08% ± 0.80 and 87.97% ± 0.72. The in-vitrowash-off test evidenced that almost 50 percent (especially F3) of the microspheres were able to adhere up to 18 h and showed remarkable bioadhesion properties. The in-vitro drug release profile indicated that all the formulations were able to prolong their drug release up to 12 h with a non-fickian release mechanism, except for F4, which followed a fickian release. Therefore, based on the findings of this study, LSM can be used as a potential alternative mucoadhesive excipient for sustained release formulations.

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Section: Resultsmentioning

confidence: 99%

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer

Embafrash Berhe,

Tesfay Mezgebo,

Abrha

et al. 2023

Advances in Pharmacological and Pharmaceutical Sciences

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Biologically active substances in the aboveground part of three Stellaria speciesx

Garnova

Filippova

Kasatkin

et al. 2022

RJPT

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The phytochemical screening of potentially efficient medicinal herbs is one of the current focus areas of modern pharmacochemistry. This work aims to analyze the phytochemical composition of the aboveground parts in three Stellaria species (S. bungeana, S. graminea, S. holostea). The study was conducted between May and July 2020 in the Moscow region of the Russian Federation. Yield values for raw herbal materials and density of stitchwort samples per 1 m2 (154 sites in total) were recorded, followed by a phytochemical analysis of the dry mass by chromatography. The maximum yield of S. bungeana was established to be 1.5 times higher than in two other species (p ≤ 0.05). In S. graminea, the maximum pectin concentration was 12 times higher than in S. holostea (p ≤ 0.001) and 0.5 times higher than in S. bungeana (p ≤ 0.05). The number of polysaccharides in S. bungeana was 14 times higher than in S. graminea (p ≤ 0.001) and two higher than in S. holostea (p ≤ 0.05). Hemicellulose content of S. bungeana extract was twice as high as that of other species (p ≤ 0.05). Tannins in S. graminea were found two times more often than in S. holostea (p ≤ 0.05) and eight times more often in S. bungeana (p ≤ 0.01). Vitamin C content in S. graminea was two times greater than in the other two stitchwort species (p ≤ 0.05). Stitchwort is a common, widespread plant that makes it easy to collect without harming plant communities. Biologically active substances (polysaccharides, vitamin C, tannins, and pectins) were found in the composition of all stitchwort species with a preventive and therapeutic effect on the human body. The concentration of tannins and vitamin C is maximal in S. graminea extract, amounting to 2.6% and 45.9%, accordingly. The extract from S. bungeana contains a lot of hemicellulose (13.2%) and polysaccharides (7.2%). No high concentration of these substances was recorded in S. holostea, which makes this species the least pharmaceutically valuable. S. graminea and S. bungeana plants can be recommended for pharmaceutical processing due to the high concentrations of vitamin C, pectins, tannins, polysaccharides, and hemicellulose.

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Effect of Capsaicin on Pharmacokinetics and Pharmacodynamics of Nateglinide in normal and diabetic rats

Kandukoori¹,

Yellu

2023

RJPT

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The Cytochrome P-450 (CYP) enzymes present in the human body are responsible for the metabolism of most antidiabetic drugs. These CYP enzymes may metabolize the drugs either to active metabolites or to inactive metabolites. Some phytoconstituents which are present in vegetables, fruits and ayurvedic products will alter the activity of CYP enzymes. In the present research, the alterations in pharmacokinetics and pharmacodynamics of Nateglinide in the presence of a phytochemical like Capsaicin were studied. The study was conducted both in normal and diabetic rats. Rats were divided into different groups. Drug was administered as alone in one group and administered in combination with Capsaicin to other groups. After 8 days of treatment, the blood samples were collected and analysed. The Pharmacokinetic parameters like Cmax, tmax, AUC, MRT, Vd and ClT were estimated for all groups and compared. The mean blood glucose levels before and after treatments were recorded and compared among the groups. From the results, it could be concluded that the Capsaicin has inhibited the activity of CYP 2C9 and CYP 3A4 enzymes, thereby decreased the metabolism of drug which ultimately resulted in the increase of Cmax and AUC. The Capsaicin could raise the antidiabetic effect of drug.

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Pharmacokinetic Studies of Gastroretentive Mucoadhesive Matrices for Diltiazem Hydrochloride Using Some Natural Polysaccharides

Cited by 4 publications

References 0 publications

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer

Extraction, Characterization, and Evaluation of Lepidium sativum Linn. Mucilage as a Mucoadhesive Polymer

Biologically active substances in the aboveground part of three Stellaria speciesx

Effect of Capsaicin on Pharmacokinetics and Pharmacodynamics of Nateglinide in normal and diabetic rats

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