Differently substituted flavanones were isolated from Leguminosae and their antibacterial activity was comparatively studied against methicillin-resistant Staphylococcus aureus (MRSA). The minimum inhibitory concentrations (MICs) of phytochemical flavanones to clinical isolates of MRSA were determined by a serial agar dilution method. The structure-activity relationship has indicated that 2',4'- or 2',6'-dihydroxylation of the B ring and 5,7-dihydroxylation of the A ring in the flavanone structure are important for significant anti-MRSA activity and that substitution with a certain aliphatic group at the 6- or 8-position also enhances the activity. Among the thirteen flavanones tested, tetrahydroxyflavanones with these structural characteristics isolated from Sophora exigua and Echinosophora koreensis showed intensive activity to inhibit the growth of all MRSA strains at 3.13-6.25 micrograms/ml. The present hydroxyflavanones would be useful in the phytotherapeutic strategy against MRSA infections.

Comparative Study on the Antibacterial Activity of Phytochemical Flavanones against Methicillin-resistant Staphylococcus aureus.

Fast dissolving Tablets are disintegrating and/or d issolve rapidly in the saliva without the need for water. Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds, and are true fast-dissolving tablets. Others contai n agents to enhance the rate of tablet disintegration in the oral cavity, and are more app ropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disinteg rate. Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. This tablet format is designed to allow administration of an or al solid dose form in the absence of water or fluid intake. Such tablets readily dissolve or disi ntegrate in the saliva generally within <60 seconds. Fast- or mouth dissolving tablets have bee n formulated for pediatric, geriatric, and bedridden patients and for active patients who are busy and traveling and may not have access to water. Such formulations provide an opportunity for product line extension in the Many elderly persons will have difficulties in taking convention al oral dosage forms (viz., solutions, suspensions, tablets, and capsules) because of hand tremors and dysphagia. Swallowing problems also are common in young individuals because of their underdeveloped muscular and nervous systems. Other groups that may experience problems using conventional oral dosage forms include the mentally ill, the developmentally disabled, and patients who are uncooperative, on reduced liquid-intake plans, or are nauseated. I n some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an una vailability of water, swallowing conventional tablets may be difficult.

Fast Dissolving Tablet: An Overview

Methods to improve patient’s compliance have always attracted scientists towards the development of fancy oral drug delivery systems. Among them, mouth dissolving drug delivery systems (MDDDS) have acquired an important position in the market by overcoming previously encountered administration problems and contributing to extension of patent life. MDDDS have the unique property of rapidly disintegrating and/or dissolving and releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. Therefore, these dosage forms have lured the market for a certain section of the patient population which include dysphagic, bed ridden, psychic, geriatric and paediatric patients. Several techniques have been developed in the recent past, to improve the disintegration quality of these delicate dosage forms without affecting their integrity. This article focuses on the technologies available and the advances made so far in the field of fabrication of mouth dissolving tablets. Apart from the conventional methods of fabrication, this review also provides the detailed concept of some unique patented technologies like Zydis, Lyoc, Quicksolv, Orasolv, Durasolv, Flashtab, Oraquick, Wowtab and Ziplet alongwith their advantages and limitations.

/pdf/mouth-dissolving-tablets-i-an-overview-of-formulation-nlolt83aot.pdf

Mouth Dissolving Tablets I: An Overview of Formulation Technology

Conventional dosage forms like tablets and capsules are now days facing the problems like dysphagia, resulting in the high incidence of non compliance and making the therapy ineffective. To obviate the problems associated with conventional dosage forms, mouth dissolving tablets have been developed having good hardness, dose uniformity, easy administration and serves as the first choice of dosage form for paediatrics, geriatrics and travelling patients. The MDTs were developed with an aim of having sufficient hardness, integrity and faster disintegration without water. Fast dissolving Tablets are disintegrating and/or dissolve rapidly in the saliva without the need for water. Some tablets are designed to dissolve in saliva remarkably fast, within a few seconds, and are true fast-dissolving tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity, and are more appropriately termed fast-disintegrating tablets, as they may take up to a minute to completely disintegrate. This tablet format is designed to allow administration of an oral solid dose form in the absence of water or fluid intake. Such tablets readily dissolve or disintegrate in the saliva generally within <60 seconds. Keywords: Mouth dissolving tablet, Disintegration, Patented technologies, Marketed MDTs

Mouth dissolving tablets: a review

Oral delivery is currently the gold standard in the pharmaceutical industry where it is regarded as the safest, most convenient and most economical method of drug delivery having the highest patient compliance. Formulation of a convenient dosage form for oral administration, by considering swallowing difficulty especially in case of geriatric and pediatric patient leads to poor patient compliance. To troubleshoot such problems a new dosage form known as orally disintegrating tablet (ODT), has been developed which rapidly disintegrate & dissolve in saliva and then easily swallowed without need of water which is a major benefit over conventional dosage form. In addition, patients suffering from dysphasia, motion sickness, repeated emesis and mental disorders prefer such preparation because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in such type of dosage form. The popularity and usefulness of the formulation resulted in development of several ODT technologies for preparation. The current article is focused on ideal characteristics, advantages and disadvantages, formulation aspects, formulation technologies, evaluation of products and future potential. Various marketed preparations along with numerous scientific advancements made so far in this avenue have also been discussed.

Orally disintegrating tablets : formulation, preparation techniques and evaluation.

The past decade has thrown open the doors for continuous technological advancements in the pharmaceutical sector. Mouth Dissolving Tablets are one of the fruitful results of these technological advancements. MD tablets play a major role in improving the patient's compliance. They rapidly disintegrate in the saliva hence obviating the need of the water. With the increasing incidences of non-compliance among the patients, Mouth dissolving tablets are the perfect answer to all these problems. A variety of drugs can be administered in the form of MD tablets as they give the advantage of the liquid medication in the solid preparation. These novel types of dosage forms have found acceptance among the geriatric, pediatric and dysphagic patients.

Mouth dissolving tablets- a novel drug delivery system

Background and Aim: Azadirachta indica has a long history of medicinal usage in skin ailments due to its antibacterial and anti-inflammatory properties. The present study was undertaken to explore the potential of the leaves and bark of Azadirachta indica in the treatment of acne. Materials and Methods: Monographic analysis of the plant was carried out, followed by the phytochemical screening of the sequential extracts of leaves and bark of Azadirachta indica. The results indicated presence of alkaloids, flavonoids, saponins, terpenes, and tannins. Gas chromatography-mass spectrometry (GC/MS) analysis of the test extracts indicated the presence of many phytoconstituents in dichloromethane and methanolic extracts namely stigmasterol, nimbiol, sugiol, 4-cymene, α-terpinene terpinen-4-ol, and vitamin E. The test extracts were evaluated against acne causing bacteria, namely Staphylococcus aureus (MTCC 96), Staphylococcus epidermidis (MTCC 2639), and Propionibacterium acnes (MTCC *1951), for their in vitro antimicrobial activity, using agar disc diffusion method. Results: Dichloromethane and methanolic extracts of Azadirachta indica showed very little activity against S. aureus and S. epidermidis, but did not show any antimicrobial activity against P. acnes. Conclusion: Despite possessing antibacterial properties, Azadirachta indica showed insignificant effect against acne causing bacteria.

Insignificant anti-acne activity of Azadirachta indica leaves and bark

Light petroleum, dichloromethane and methanolic extracts of Linum usitatissimum were investigated using GC/MS. The main components of three sequential extracts were methyl linolenate (11.9-33.9%) and methyl linoleate (3.4-9.1%). Components possessing antimicrobial activity against acne causing bacteria, namely alpha-linolenic acid (7.0 -7.1%), alpha-terpinene (1.7-3.1%), terpinen-4-ol (1.3-4.6%), 4-cymene (1.6-7.1%) and alpha-pinene (1.1%), were found in varying amounts. Antimicrobial screening indicated that the light petroleum extract was more active against aerobic and anaerobic test strains with a MIC value of 1.25 mg/mL and a MBC of 2.5 mg/mL against S. aureus and P. acnes. A MIC of 2.5 mg/mL was observed against S. epidermidis.

https://journals.sagepub.com/doi/pdf/10.1177/1934578X1100601133

Antimicrobial investigation of Linum usitatissimum for the treatment of acne.

Anti-acne herbal formulations are used for the treatment of acne vulgaris with the added advantage of not producing adverse effects unlike synthetic drugs. Phytoconstituents present in methanolic extracts of Camellia sinensis (CSME), Glycyrrhiza glabra (GGME) and Calendula officinalis (COME) have antibacterial and antioxidant properties. Validated HPTLC fingerprinting confirmed the presence of myricetin (CSME), glycyrrhizin (GGME) and kaempferol (COME) in these extracts. Extracts loaded with carbopol® 940 were used for the preparation of herbal (F1-F3) and polyherbal gel (PHF), followed by evaluation for pH, viscosity, spreadability and in vitro antibacterial potential against S. aureus , S. epidermidis and P.acnes . Polyherbal gel formulation indicated antibacterial potential and was further assessed for skin permeation by gamma scintigraphy using hydrophilic radiotracer 99m Tc-DTPA and lipophilic radiotracer 99m Tc-MIBI. Significant permeation (78.11%) was observed with hydrophilic radiotracer labeled 99m Tc-DTPA-PHF and this suggested that the formulation was capable of sustained drug delivery for the treatment of moderate to severe type of acne.

http://www.arjournals.org/index.php/ijdd/article/download/778/pdf

In vitro and in vivo assessment of polyherbal topical gel formulation for the treatment of acne vulgaris

In the present study, petroleum ether, dichloromethane and methanolic extracts of three medicinal plants namely Camellia sinensis, Glycyrrhiza glabra and Calendula officinalis were analyzed for their antibacterial and antioxidant activity in different test systems. Highest zone of inhibition (≥15) mm was observed with methanolic extract of Camellia sinensis using disc diffusion method. Phytochemical analysis indicated that amongst nine test extracts, methanolic extract of Camellia sinensis had the highest total phenolic content (104.93 ± 1.630 mg GAE /g). Flavonoid (115.503 ± 2.984 mg RuE /g dry extract) and flavonol content (574.446 ± 7.94mg RuE /g dry extract) of methanolic extract of Glycyrrhiza glabra was also found to be superior among all the extracts. Antioxidant assays revealed highest DPPH scavenging (IC50=44.03 ± 1.784 µg/ml) and metal chelating (IC50=234.64 ± 5.467 µg/ml) effect in methanolic extracts of Camellia sinensis. Similarly, methanolic extract of Glycyrrhiza glabra exhibited highest radical scavenging activity (IC50=21.37 ± 1.422 µg/ml) when reacted with the ABTS. +.

Pratibha Nand

Papers

Mouth dissolving tablets- a novel drug delivery system

Insignificant anti-acne activity of Azadirachta indica leaves and bark

Antimicrobial investigation of Linum usitatissimum for the treatment of acne.

In vitro and in vivo assessment of polyherbal topical gel formulation for the treatment of acne vulgaris

IN VITRO ANTIBACTERIAL AND ANTIOXIDANT POTENTIAL OF MEDICINAL PLANTS USED IN THE TREATMENT OF ACNE Research Article