Sustained release matrix tablet of 100 mg losartan potassium: Formulation development and in vitro characterization

Abstract Sustained release matrix tablets of 100 mg losartan potassium HCl were fabricated with two release retarding polymers namely HPMC K100 M and affinisol by direct compression method. Nine trial formulations were prepared by varying content of these polymers, each from 50 mg to 100 mg; keeping the total weight of the tablet 310 mg. The best formulation was selected based on in vitro drug release profile for 12 hours conducted in Type II dissolution apparatus at 50 rpm and water as dissolution medium. Pre-compression parameters such as bulk density, tap density, Carr's index and Hausner ratio were evaluated for the selected tablet. The tablets were subjected to thickness, weight variation test, drug content, hardness and friability. Drug release kinetics, surface morphology and accelerated stability study were investigated for that selected formulation. Formulation F4 with the composition of 75 mg HPMC K100M and 100 mg affinisol was selected as the best formulation that extended the drug release up to 12 hours. Pre-compression parameters and other tableting properties were within the Pharmacopoeia limit. Release kinetics analysis proved non-fickian zero-order drug release and that was further confirmed by surface morphology of the tablets before and after dissolution study visualized by SEM. The developed formulation was found to be stable for one month stored at 60 ○C.

Stability and Sensory Evaluation of an Innovative Antiaging Formulation Based on Marine Ingredients

Abstract The high consumption of antiaging cosmetics represents an outstanding opportunity for the development of new processes and attractive products in the cosmetic industry. Stability studies and sensory analyses are critical steps in the development process and production chain. Here we present a potential antiaging cosmetic product with innovative sensory characteristics. Caviar extract antioxidant properties were firstly evaluated by the DPPH method since it is an important mechanism against skin aging. Ca-alginate beads containing 2% of caviar extract and 0.2% of black pigment were prepared to obtain spheres similar to caviar. The beads were incorporated in a gel phase (hydroxyethylcellulose 2.5%) containing 3% of dimethylaminoethanol. Stability was evaluated in different storage conditions (sunlight exposure, 5 ± 2 °C, 37 ± 2 °C and r.t.) through the parameters: appearance, color and odor, pH (6-7), density (0.98-1.14 g.mL-1), centrifugation and average size. After approval by the Committee for Ethics in Research (n° 3.503.061), 30 volunteers tested the new formulation and answered a questionnaire. At 2%, caviar extract was able to scavenge 10.9% ± 0.58 of DPPH radical. Formulations showed good stability after 90 days, even considering the average size (7.47 ± 0.41 - 8.4 ± 0.65 mm2). 90% of the sensory test participants reported that they would buy the new product. Therefore, the new product developed demonstrates a promising potential as an attractive cosmetic product.

Study of a tooth gel formulation for hygiene and oral sequelae management in irradiated patients

Cervical-facial radiotherapy causes innumerable sequelae, being systemic or restricted to the oral environment. Theoral mucosa of these patients is profoundly compromised by radiotherapeutic treatment with or without chemotherapy,presenting several complications. Dentifrices containing sodium lauryl sulfate cause damage, as they lead to drynessof the mucosa. The objective of this work was to develop a dentifrice capable of minimizing xerostomia related toa lower abrasive effect, which was intended for hygiene, prevention of caries, control of dental biofilm, and toothsensitivity in cancer patients. The qualitative composition and physicochemical characteristics of ten dentifrices wereanalyzed, which enabled the preparation of the proposed formulation (PF) that was analyzed periodically for 180days. The quantitative analysis of spreadability not only indicated favorable behavior of the PF in relation to thepackaging and storage conditions but also revealed the need to raise the propylene glycol concentration in the PF toavoid the occurrence of syneresis after 60 days. Furthermore, pH data showed that the PF is compatible with the pHof oral homeostasis thus avoiding the occurrence of dental demineralization. It is suggested that the PF has a singularcomposition and physicochemical quality to be used as a suitable dentifrice for patients undergoing anticancer therapy

Development of Oral Solid Formulation for Insoluble Drugs Based on PASD Technology / 中国药学杂志

The low aqueous solubility is the main reason that for most pharmacological active ingredients are challengeable to develop into oral solid formulation. Polymeric amorphous solid dispersion(PASD) can greatly improve the apparent solubility and dissolution rate of poorly soluble drugs, has become a common technology to improve the oral bioavailability of poorly soluble drugs. However, due to the amorphous form of the drug at a high surface free energy in PASD, crystallization would occur during storage and dissolution, thereby losing its formulation advantages. The review attempts to provide a structural development approach of PASD products from the aspects of formulation and technology, in order to guide the development of stable and commercially viable PASD formulations. And the trend analysis of marketed products and patents of PASD will be discussed to understand the prospects of PASD's application in improving the bioavailability of poorly soluble oral solid formulations.

Three-dimensional aspects of formulation excipients in drug discovery:a critical assessment on orphan excipients, matrix effects and drug interactions / 药物分析学报

Formulation/pharmaceutical excipients play a major role in formulating drug candidates, with the ob-jectives of ease of administration, targeted delivery and complete availability. Many excipients used in pharmaceutical formulations are orphanized in preclinical drug discovery. These orphan excipients could enhance formulatability of highly lipophilic compounds. Additionally, they are safe in preclinical species when used below the LD50 values. However, when the excipients are used in formulating compounds with diverse physico-chemical properties, they pose challenges by modulating study results through their bioanalytical matrix effects. Excipients invariably present in study samples and not in the cali-bration curve standards cause over-/under- estimation of exposures. Thus, the mechanism by which excipients cause matrix effects and strategies to nullify these effects needs to be revisited. Furthermore, formulation excipients cause drug interactions by moderating the pathways of drug metabolizing en-zymes and drug transport proteins. Although it is not possible to get rid of excipient driven interactions, it is always advised to be aware of these interactions and apply the knowledge to draw meaningful conclusions from study results. In this review, we will comprehensively discuss a) orphan excipients that have wider applications in preclinical formulations, b) bioanalytical matrix effects and possible ap-proaches to mitigating these effects, and c) excipient driven drug interactions and strategies to alleviate the impacts of drug interactions.

Research progresses and formulation development of natural anti-mildew agents based on Chinese herbal medicines / 中国中药杂志

Owing to the intrinsic factors and some extrinsic environmental conditions, many foods, agricultural products and Chinese materia medicas (CMMs), if not handled properly in the processes of growth, harvesting, processing and storage, can be easily contaminated by all kinds of molds to produce mycotoxins of serious toxicity, which will not only affect the quality, safety and effectiveness of CMMs, but also result in potential threatens to human and animal's health and life. Therefore, in recent decades, it has become the focus on how to prevent and control the foods, agricultural products and CMMs from being moldy and producing toxicity for scientific preservation. Many Chinese herbal medicines (CHMs) especially those with high content of volatile oils with strong antifungal activities have been applied for the scientific preservation of foods, agricultural products and CMMs. Based on these situations, natural anti-mildew agents have been further developed and made into some useful dosage forms, such as tablets, aerosol, liposomes and inclusion, which will not only greatly expand the application scope of CHMs to make the use of anti-mildew agents more convenient, but also achieve the sustained or controlled release of the antifungal effect for scientific preservation of foods, agricultural products and CMMs.

Enhancement of dissolution rate and formulation development of efavirenz tablets employing starch citrate-a new modified starch.

The objective of the study is to prepare, characterize and evaluate starch citrate, a new modified starch as a carrier in solid dispersions for enhancing the dissolution rate of efavirenz. The feasibility of formulating solid dispersions of efavirenz in starch citrate into compressed tablets with enhanced dissolution rate was also investigated. Starch citrate was prepared by reacting starch with citric acid at elevated temperatures. It was insoluble in water and has good swelling (1500%) property without pasting or gelling when heated in water. Solid dispersions of efavirenz in starch citrate were prepared by solvent evaporation method employing various weight ratios of drug: starch citrate such as 2:1(SD-1), 1:1(SD-2), 1:2(SD-3), 1:3(SD-4) and 1:9(SD-5) and were evaluated for dissolution rate and efficiency. All the solid dispersions prepared gave rapid and higher dissolution of efavirenz when compared to pure drug. A 12.94 and 40.41 fold increase in the dissolution rate (K1) of efavirenz was observed with solid dispersions SD-4 and SD-5 respectively. The DE30 was also increased from 10.66% in the case of efavirenz pure drug to 60.93% and 74.23% in the case of these solid dispersions. Efavirenz (50 mg) tablets were prepared employing efavirenz alone and its solid dispersions SD-3 and SD- 4 by wet granulation method and were evaluated. Efavirenz tablets formulated employing its solid dispersions in starch citrate gave rapid and higher dissolution rate and DE30 when compared to plain and commercial tablets. A 7.01 and 15.30 fold increase in the dissolution rate (K1) was observed with tablet formulations containing solid dispersions SD-3 and SD-4 respectively when compared to plain tablets.