The systemic delivery of drugs through novel methods of administration is one area in which significant changes and improvements have been made. Consequently, precise control of drug input into the body by a variety of routes is now possible.This study presents an idea of development of mucoadhesive buccal patch of Labetalol hydrochloride by using chitosan,PVP K 30,PVP K 90,HPMC,and polyethylene glycol(PEG)1000. The prepared patches were evaluated for their weight variation,thickness,folding endurance,swelling index,surface pH,drug content uniformity and in vitro release studies.
Pimozide is an anti-psychotic agent whose bioavailability is 40-50% because of first pass metabolism. The tmax of pimozide after oral administration is 4-12 hr, which is long and variable. Hence, Pimozide is a suitable drug for buccal drug delivery. log P of pimozide is 5.3432. Pimozide patches were prepared using HPMC (15 & 47 cps), carbopol 934, PVA, and PVP. FTIR and UV spectroscopic methods revealed no interaction between pimozide and polymers. The patches were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behaviour, tensile strength, and surface pH. Data of in vitro release from patches were fit to different equations and kinetic models to explain release kinetics. Kinetic models used were zero and first-order equations, Hixon-Crowell, Higuchi and Korsmeyer-Peppas models. Good correlation among in vitro release and in vivo absorption of pimozide was observed. Short-term stability study revealed that drug content decreased in various patches.
The objective of the study was to develop mucoadhesive buccal tablet of furosemide. Tablets of Furosemide were prepared by wet granulation method using mucoadhesive polymers like Carbopol 934P, Guar Gum, Chitosan and HEC in different ratios. Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, swelling index, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation, stability studies. The tablets were evaluated for in vitro release in pH 6.8 phosphate buffer for 12 hr in standard dissolution apparatus. Mucoadhesion strength was increased with increase in the concentration of carbopol. In order to determine the mode of release, the data was subjected to Zero order, first order, Higuchi and Peppas model. Short-term stability studies on the promising formulations indicated that there were no significant changes in drug content, ex-vivo mucoadhesive strength and in vitro dissolution characteristics. The prepared buccal tablets of furosemide could stay in the buccal for a longer period of time. Which indicate a potential use of this formulation.
Over the last few years, obesity is the major problem of humans regarding their helth. With this boom in obesity problem, here little effort was made to formulate the dosage form containing the anti-obesity drug-Rosuvastatin Calcium Buccal Tablet. Buccal drug delivery avoids the problem of extensive first pass metabolism regarding the Rosuvastatin Calcium which ultimately leads the enhancement in bioavaibility of drug. So, this book therefore provide the information regarding the buccal drug delivery of drug as a potential tool to bypass the extensive first pass metabolism & improve the biovaibility of drug. Analysis of this research work will help the research fellows, as a shed of light on the buccal drug delivery as a route of drug administration for drug candidate having low bioavaibility due to high first pass metabolism.
Venlafaxine Hydrochloride is an oral antidepressant agent of the Serotonin-Norepinephrine Reuptake Inhibitor class. Venlafaxine Hydrochloride has been studied for the treatment of panic disorder, post-traumatic stress disorder, and the treatment of hot flashes in patients who cannot or do not want to take hormone replacement therapy. The dose of Venlafaxine hydrochloride ranges from 75 to 225 mg three times a day and it undergoes extensive first pass metabolism hence it has only 45% bioavaibility. The short half life of the drug 5 hr indicates the need for modified release dosage form. Venlafaxine HCl was chosen as model drug with an aim to developed mucoadhesive buccal tablet that minimize dose related side effects and reducing the dosing frequency of drug and finally improve the bioavaibility.
Famotidine is histamine –H2 receptor antagonist. It has bioavailability of 40 to 45% and it has shorter plasma half life of 2.5 to 3.5 hrs. The effective treatment of erosive esophagitis and Zolinger-Elisons syndrome requires administration of 20 mg of Famotidine 4 times a day. A conventional dose of 20 mg can inhibit gastric acid secretion up to 5 hours but not up to 10 hours. An alternative dose of 40 mg leads to plasma fluctuations; thus a sustained release dosage form of famotidine is desirable. Direct access to the systemic circulation bypasses drugs from the hepatic first pass metabolism leading to high bioavailability. Moreover, the buccal route is easily accessible, has a good patient compliance and can be used in patients who can’t swallow. Bilayer buccal tablet was prepared by using mucoadhesive polymer combination of Sodium CMC and Carbopol934P, by direct compression with backing layer of Ethyl cellulose. The optimized formulation F1 had given release of 102.57% in 8hrs and it had optimum swelling, mucoadhesive property and permeation from buccal mucosa. It also had desired drug release kinetics and found to be stable for the period of 1 month.
In the present study, an attempt was made to formulate mucoadhesive buccal patches of flurbiprofen (FBN) in order to enhance solubility. Solubity enhancement was attempted by making solid dispersion of drug with ?-CD (cyclodextrin). Initially preformulation were carried out using reported methods. Buccal patches was prepared by solvent casting technique using polymers like Polyvinyl alcohol (PVA), Sodium carboxymethylcellulose (SCMC),and Hydroxypropyl methyl cellulose (HPMC). The prepared patches were evaluated for their weight variation, thickness, folding endurance, surface pH, swelling index, in-vitro residence time, in-vitro permeation studies, drug content uniformity and bioadhesion test.
Mucoadhesive drug delivery system is now-a-days a booming field for research interest. In the present study an anti-fungal and anti-inflammatory drug are formulated in combination to treat oral candidiasis. This research thus will open a new horizon for fellow researchers to explore buccal route for local targeting of drugs going apart from its conventional use of enhancing the bio availability of poorly absorbed drugs through G.I.Tract. The diverse conditions like Herpes infections, Oral lesions and many more local conditions can be treated efficiently by such formulations. Miconazole Nitrate molecule has been extensively studied and worked upon, which resulted into several formulations and had been brought into the market in various countries. The formulated combination thus is a step ahead treatment for the oral candidiasis, which will show its anti-fungal activity and will also take care of the local inflammation caused due to infection.
Bioadhesive polymers that bind to the gastric mucin or epithelial cell surface are useful in drug delivery for the purpose of (a) retaining a dosage form in the G.I tract and (b) increasing the intimacy and duration of contact of drug with the absorbing membrane. In this investigation, natural mucoadhesive materials were isolated from different edible fruits like Aegle marmelos (Linn.) Cor., Zizyphus mauritiana and Tamarindus indica by hot extraction method. Density and swelling property of natural materials were evaluated. Bioadhesive and mucoadhesive qualities of natural materials were evaluated individually by different in vitro testing methods and in vivo X-ray photograph method. It was observed that natural materials have good mucoadhesive property. Mucoadhesive tablets containing 7.5 mg of terbutaline sulphate tablets were prepared by wet granulation method. The sustained release pattern was evaluated by in vitro and in vivo studies. The drug release data were plotted using various kinetic equations (zero order, first order, Higuchi’s kinetics.Finally we confirmed our investigation by invitro-invivo correlation study.
Chemotherapy induced nausea and vomiting (CINV) is a serious distress for cancer patients, who have to receive chemotherapy for their treatment. Ondansetron HCl is an effective antiemetic drug which is used to prevent CINV. But this drug is commercially available in the form of tablet and injection, which causes its hepatic “first pass” metabolism or rapid clearance from the body, respectively. Hence, the need to formulate such a dosage form of this drug that will not only enhance its bioavailability but also provide adequate patient compliance. This book focuses on development and in vitro evaluation of a mucoadhesive buccal film of ondansetron HCl which will deliver the drug in a sustained manner via buccal mucosa and help to maintain effective blood level of the drug for a prolonged period.
Buspirone Hydrochloride is used in the treatment of anxiety. It has a short half life and low oral bioavailability of 5%. Therefore, the purpose of this research was to develop unidirectional Bucco- adhesive films of Buspirone Hydrochloride by solvent casting technique using full factorial designs. HPMC K15M and Eudragit RL-100 were used as polymers in different proportion. Polyethylene glycol 400 was used as plasticizer and Sodium lauryl sulphate was used as permeation enhancer in different concentration. The physicochemical compatibility of the drug and the polymers was studied by FT-IR spectroscopy. The results suggested no physicochemical incompatibility between the drug and the polymers. In full factorial designs, total amount of polymer (X1) and percentage of HPMC K15M (X2) was kept as a independent variables. After wards, statistically optimization process was carried out and two optimized formulation (OF1 and OF2) was developed. The results of optimization formulation showed greater degree of % similarity with predicted values. Stability studies of two optimized formulations were carried out at room temperature as per ICH Q1C guidelines.
For systemic delivery, the oral route has been the preferred route of administration for many systemic actively drugs. When administered by the oral route, however, many therapeutic agents have been reportedly subjected to extensive presystemic elimination by gastrointestinal degradation and/or hepatic metabolism. Results of low systemic bioavailability, short duration of therapeutic activity, and/or formation of toxic and inactive metabolite. The unique environment of the oral cavity offers its potential as a site for drug delivery. Because of rich blood supply and direct access to systemic circulation, the oral mucosal route is suitable for drugs, which are susceptible to acid hydrolysis in the stomach or which are extensively metabolized in the liver.
The work presented in this book is useful for preparation of Buccal tablets, in this three different grades of polymers were used and evaluated for in vitro dissolution, ex vivo permeation and bioadhesive properties. The present study concludes that buccal delivery of Glibenclamide tablets can be a good way to bypass the first pass metabolism and to prolong duration of action by reducing the frequency of dosing.
Mucoadhesive drug delivery system which utilize properties of bioadhesion of certain water-soluble polymers which become adhesive on hydration and hence can be used for targeting a drug to a particular region of the body for extended period of time. The mucosal layer lie a number of regions of the body including the GIT, the urogenital tract, the airways, the ear, nose, mouth and eye. The oral mucosal sites differ greatly from the one another in terms of anatomy, permeability to an applied drug and their ability to retain a delivery system for a desired length of time. The Buccal and sublingual mucosal is relatively, permeable, giving rapid absorption and acceptable bioavailability of drugs and is convenient, easily accessible and generally well accepted
One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in the GI tract is to control the gastric residence time (GRT) via gastroretentive drug delivery system which will provide us with new and important therapeutic options. Controlling the residence time of a drug delivery system in a particular region of GI tract can utilize several approaches which include floating drug delivery system, high density system and mucoadhesive system. Helicobacter pylori bacteria are the causative agents of gastric ulcers.Certain conventional dosage forms fail to eradicate the bacteria from the stomach so a novel drug delivery system is the need of the hour for proper elimination of these bacteria locally as well as systemically. The gastro retentive systems can be the remedy and the substitute for the conventional dosage forms, which will have more rationality with excellent efficacy towards the eradication of H.pylori infections. The focus of the research work in this book is to formulate,evaluate and optimize the newer gastro retentive dosage forms of various approaches.
For most of the industry’s existence, pharmaceuticals have preliminary consisted of simple, fast-acting chemical compounds that are dispensed orally or as injectables. During the last three decades, however, formulations that control the rate and target specific area of the body for treatment have become increasingly common. Nowadays, nanosuspension technology with mucoadhesive principle comes into front for achieving to increased uptake and accumulation of drug in affected region of targeted organ. In the present study, preparation of nanosuspension for famotidine and curcumin by solvent evaporation technique as well as media milling technique using stabilizers was initially adopted. Formulation and process variables were identified based on particle size analysis and in vitro drug release. Optimized nanosuspension was characterized by particle size analysis, zeta potential determination, scanning electron microscopy (SEM). In vivo and ex-vivo study of optimized mucoadhesive nanosuspension was performed using rat stomach and compared with marketed suspension for healing of peptic ulcer.
The focus of the pharmaceutical research is being steadily shifted from the development of new chemical entities to novel drug delivery systems of existing drug molecules to maximize their effectiveness in terms of therapeutic action and patent protection. This is made possible by the discovery of various compatible polymers (e.g. Carbopol polymers). Local delivery of the anesthetic agent(e.g.Lidocaine)leads to higher concentration of the drug at the intended site of action using a lower dose with an associated reduction in side effects relative to systemic administration.One of the most critical factors in enhancing the efficacy of a topical anesthetic is maintaining prolonged intraoral mucosal contact. Most topical agents come in gel form, which is difficult to localize to a particular site and easily diluted by saliva.To overcome these problems, bilayer buccal tablets were prepared with carbopol polymer.They seem to solve all these problems associated with the treatment of gingivitis and other periodontal diseases and adhere well to the gum and control the release of the drug for an extended period of time. Besides this,characteristics of carbopol polymers were also evaluated.
In this research work an attempt was made to prepare once a day formulation of gliclazide. The purpose was achieved by making mucoadhesive microcapsules of gliclazide. A combination of polymers, sodium alginate, sodium Carboxy Methyl Cellulose, hydoxy propyl methyl cellulose and carbopol 934P was utilized for this purpose. The formulation was prepared and optimized and evaluated for in-vitro and in-vivo performance. The results obtained were very satisfactory.
The work presented in this book is useful for both Academia and Industry. The work reflects the potential use of natural gums in the formulation of Buccal tablets. The gums used in the formulation are Xanthum gum and Locust bean gum, which were proved as bioadhesive gums. By successful usage of these gums buccal tablets of Losartan Potassium were prepared and evaluated for bioadhesive properties, ex vivo permeation, in vitro dissolution and mechanical properties.
Intradermal Drug Delivery System is a noval approach for the formulation of pharmaceutical dosage forms to increase the bioavailability of drug with sustained action. IDDS for Trazodone-Hcl is really advantageous to treat patients with depression and schizophrenia. IDDS as Patch formulation is inserted in intradermal space to exert its effect. Biodegradable polymer used in its formulation help its biodegradtion under skin itself without any side effects so removal is not a big issue.