AN EXPERIMENTAL DESIGN IN THE OPTIMIZATION OF VARIOUS TABLET EXCIPIENT FORMULATIONS = A CONCISE REVIEW

The use of an experimental design technique in the development of various pharmaceutical preparations, including tablet preparations, has become the latest trend. Because of their ease of use, tablet formulations are popular among both producers and patients. To increase the usage of tablets in diverse circles and settings, researchers are working to develop a variety of tablet excipients for various functions. Fast dissolving tablets (FDT), effervescent tablets, modified-release tablets, oral mucoadhesive tablets, gastroretentive tablets, and colon targeted tablets are some of the tablet formats that have been developed in addition to traditional tablets. This review will look at how formulation optimization in tablet preparations has been done during the previous ten years using specific literacies. The articles for this review were found using the keywords tablet, excipient, matrices, formulation, and QBD in specialized databases such as Elsevier, Pubmed, and Cambridge. Other options include Springer publications, material from the Internet, and articles published online by The Lancet Respiratory Medicine, Medscape, and Statpearls. The formulation design strategy is based on the experimental design approach carried out on the kind of tablet preparation, which has distinct important quality parameters.

Cyclodextrin as Functional Carrier in Development of Mucoadhesive Tablets Containing Polygoni cuspidati Extract with Potential for Dental Applications

Polygoni cuspidati root is a resveratrol-rich source with anti-inflammatory, angiogenic and neuroprotective effects. The raw material was standardized for the content of resveratrol, for which there is a special justification for administration within the oral mucosa. To improve the solubility of resveratrol and to assure its high content in plant material, an ultrasound-assisted extraction method was applied. The addition of cyclodextrin was found to increase the extraction efficiency of resveratrol (from 13 to 297 µg per 1 g of plant material in case of 50% ethanol extracts) and enhanced its antioxidant activity as compared to pure Polygoni cuspidati extract/resveratrol. Cyclodextrin plays the role of a functional extract regarding technological properties (increasing the extraction of resveratrol from the extract, improving mucoadhesive properties). Therefore, the aim of this study was to develop mucoadhesive tablets containing combinations of the Polygoni cuspidati extract with a cyclodextrin carrier for buccal delivery. The tests sequentially included extract preparation and characterization of its physical and biological properties and then formulation studies with a broad description of the prototype properties. The test results indicate that cyclodextrin increases the efficiency of resveratrol extraction from Polygoni cuspidati rhizome, which is a rich source of resveratrol, and its extract enclosed in a mucoadhesive tablet guarantees prolonged action at the site of administration.

Formulation and Evaluation of Vaginal Bioadhesive Drug Delivery System of Acyclovir

Acyclovir is an anti-viral, which has been used in the treatment of vaginal disorder. Acyclovir is almost completely absorbed after oral administration but has low bioavailability of about 10-15% because of first pass metabolism. As first pass metabolism removes approximately 85-90% of the drug, so for clinical efficacy of the drug it should be frequently administered. Hence an attempt has been made to produce sustained release dosage form of the acyclovir which can be specifically employed for the treatment of vaginal disordered by Herpes simplex virus. The Mucoadhesive tablets of acyclovir has been prepared by direct compression methods and evaluated for various parameter such as thickness, friability, hardness, drug content, weight variation, swelling index, surface pH, bioadhesive force, bioadhesive time, drug release etc. The kinetic data was applied to the optimized formulations. So formulation of acyclovir in a vaginal mucoadhesive tablet dosage form will decrease the frequency of administration, which can lead to an improvement in patient adherence and thereby improving its clinical efficacy.

Effect of various Polymers on Drug Release from Mucoadhesive Tablets of Cefixime Trihydrate

Cefixime trihydrate (CT) is a third-generation cephalosporin antibiotic and is used in the management of various infections caused by Gram +ve as well as Gram – ve bacteria. It has a plasma half-life of 3-4 h. It has poor oral bioavailability due to hepatic first pass metabolism. Hence, an attempt was made to develop CT mucoadhesive tablets for buccal delivery to avoid first-pass metabolism and improved oral delivery. CT mucoadhesive tablets developed using HPMC K4M, Na-CMC, guar gum and chitosan as rate controlling polymers and mucoadhesive agent, respectively and compressed by direct compression method. The prepared CT mucoadhesive tablets were evaluated for hardness, weight variation, thickness, friability, drug content uniformity, assay, mucoadhesive strength and in vitro release. From the results, all the evaluated parameters were within the pharmacopoeial limits. The in-vitro dissolution studies indicated that the CTmucoadhesive tablets formulation (F2) showed 99.7±1.4 % of drug release after 8 h and chose as the optimized formulation. The kinetic models suggest that the drug release follows Higuchi’s kinetics and tablets drug release was controlled by a diffusion mechanism.

OPTIMASI FORMULA TABLET BUKAL MUKOADHESIVE GLIBENKLAMID MENGGUNAKAN MATRIKS CMC NA SERTA ASAM OLEAT SEBAGAI ENHANCHER

Glibenclamide is a sulfonylurea class of antidiabetic drugs that works by stimulating insulin secretion in the pancreas so that it is effective only when the β-cells of the pancreas can still produce. The glibenclamide dosage form that is on the market is a conventional oral tablet which has various disadvantages in terms of pharmacokinetics. Based on this, it is necessary to develop a more effective drug delivery system for glibenclamide in order to avoid first-pass metabolism so as to increase the bioavailability of glibenclamide, namely by making mucoadhesive buccal tablets. This glibenclamide mucoadhesive buccal tablet is formulated using a variety of mucoadhesive polymers, namely CMC Na and oleic acid as enhancers. The manufacture of four mucoadhesive buccal tablet formulas used the direct compression method. The results of the weight uniformity test showed that they did not meet the NP requirements specified, all formulas had an NP of more than 15. The tablet hardness test also showed results that did not meet the test requirements. However, the results of the physical properties of the brittleness, pH and swelling index showed the results that met the test requirements. In this research, the optimum variation of CMC Na polymer and oleic acid as enhancers to physical properties (hardness, brittleness, pH, swelling ability) and the release of glibenclamide mucoadhesive tablets were CMC Na of 37.5 mg and oleic acid of 3.5. ml.

A Randomized, Double-Blind, Placebo-Controlled, Cross-Over Study to Evaluate the Efficacy of AqualiefTM Mucoadhesive Tablets in Head and Neck Cancer Patients Who Developed Radiation-Induced Xerostomia

Xerostomia, the subjective complaint of dry mouth, is caused by therapeutic interventions or diseases. Nowadays, radiotherapy (RT) in patients with head and neck cancer (HNC) stands out as one of the most important causes of xerostomia. Currently available therapies for the treatment of xerostomia are still less than optimal and xerostomia still represents an unmet clinical need. In this article, we present the results of a prospective clinical study with a new product, AqualiefTM, in patients treated with curative RT with or without chemotherapy for HNC. AqualiefTM is based on two main ingredients, carnosine and karkadé, which have acid buffering and antioxidant properties. The study was performed on 30 patients, with 4 of the patients being lost during the study period. Each patient received randomly one of the two treatments, AqualiefTM or placebo, for 8 days. After a 10-day wash-out period, each patient received the other treatment for a further 8 days. The results show that AqualiefTM stimulated salivation in these patients and reduced the pH drop that was observed in an equivalent placebo-treated population of patients. Moreover, no serious, treatment-related adverse events were observed. AqualiefTM has shown positive results, although with limitations due to unsuccessful trial accrual. Therefore, it may be further investigated as a tool for the treatment of RT-related xerostomia.

Synthesis and Characterization of Carboxymethylated Locust Bean Gum for Developing Compression Coated Mucoadhesive Tablets of Cinnarizine

Carboxymethylated locust bean gum (CLBG) was synthesized by carboxymethylation of locust bean gum (LBG) using monochloroacetic acid followed by characterization involving SEM, XRD and FTIR techniques. The CLBG exhibited changes in the surface morphology along with relative amorphous nature as indicated in SEM and XRD analysis, respectively. In SEM images, locust bean gum (LBG) exhibited irregular particle with smooth surface morphologies whereas CLBG depicted surface roughness with relatively irregular edges. XRD study indicated relative amorphous nature of CLBG. The modified gum was employed for developing compression coated tablets of cinnarizine. The core tablets coated with CLBG exhibited mucoadhesive detachment force of 11.44 ± 2.09 to 16.07 ± 1.88 N compared to 4.10 ± 0.95 to 5.52 ± 1.13 N of locust bean gum coated tablets. The CLBG depicted better sustained drug release behaviour when compared with the pure gum. In conclusion CLBG is a suitable polymer candidate for developing mucoadhesive drug delivery systems with controlled release property.