Characterization of the critical quality attributes for hydroxypropyl methylcellulose with different sources and analysis of the release of sustained-release tablets in vitro / 药学学报

The quality difference of pharmaceutical excipients from different sources affects the molding properties of the powder, resulting in changes in the properties of the final product. In this study, the critical quality attributes of hydroxypropyl methylcellulose (HPMC) with different specifications from two manufacturers (manufacturer A and manufacturer B) were characterized including particle size, physical morphology, viscosity and powder physical quality attributes. Aminophylline, diclofenac sodium, and metformin hydrochloride were utilized as model drugs with different solubility to prepare sustained-release tablets, and the effect of HPMC from different sources on drug release of sustained-release tablets in vitro was investigated. The results showed that HPMC with the same viscosity specification from different sources had outstanding differences in the physicochemical properties (including particle size, physical morphology, viscosity, dimension, compressibility and powder flow), which could change the hardness and friability of the sustained-release tablets. The differences in the physicochemical properties of HPMC had different effects on the dissolution of different sustained-release tablets in vitro. It had no significant effect on the release of easily soluble aminophylline and metformin hydrochloride, but had a greater impact on the release of poorly soluble diclofenac sodium. Compared with manufacturer A, the sustained-release effect of matrix tablets prepared by HPMC from manufacturer B was more excellent. The results of this study will provide a theoretical reference on selecting the appropriate excipients for formulation design.

In vitro comparison test for chemical solid oral generic drugs administered by nasogastric tubes / 国际药学研究杂志

At present, the dosage and administration items in the marketing instructions of some oral solid brand drugs approved in China include related contents for administration via nasogastric tube. In order to achieve consistency with the original drugs in quality and efficacy, the generic drugs investigators should confirm whether the generic drugs and the original drugs have the same in vitro characteristics under the conditions of administration by nasogastric tube. The purpose is to eliminate the clinical risks brought by the way of administration. This article summarizes the experimental design and evaluation points for the in vitro comparative study of the solid oral generic drugs which can be administered by nasogastric tube, while referring to the individual drug guidelines issued by FDA and the related literature published, so as to provide a reference for the technical system construction for the consistency evaluation of oral solid dosage forms.

Evaluating the discriminatory power of a dissolution assay for rosuvastatin calcium capsules: Solid-state properties and dissolution media

We propose to evaluate the dissolution properties of rosuvastatin calcium (ROSC) capsules in different media to characterize the discriminatory power of the assay method. Dissolution assays were performed in media with different pH, and including the surfactant sodium dodecyl sulfate (SDS). Several immediate-release formulations were manufactured using the commercial raw material characterized as amorphous solid. The hydrophobic adjutant magnesium stearate was employed in some formulations due to its negative effect in the wettability and dissolution efficacy of solid dosages. These formulations showed the lower dissolution efficacy values in media without surfactant; however, when SDS was added to the medium, the dissolution efficacy increased, and the discriminatory power was lost. In spite of micellar solubilization does not increase the ROSC solubility, it modifies the discriminatory power of the assay method, increasing the wettability of the powder mixtures. The crystalline form M of ROSC was recrystallized in our laboratory, and it showed lower solubility in water than amorphous solid. However, its dissolution properties were not influenced by SDS. These results are important to develop dissolution assays for other hydrophilic drugs with increased water solubility, once that dissolution media with surfactants increase the wettability of the formulations, leading to an overrated dissolution rate.

Electrostatic Dry Powder Coating for Pharmaceutical Solid Dosage Forms / 中国药学杂志

Derived from industrial dry powder coatings, electrostatic dry powder coating for pharmaceutics gained numbers of attentions in recent years. In this technology, powdered coating materials are directly sprayed onto the surface of the solid dosage through an electrostatic gun without using any solvent or water, followed by a curing step to allow those deposited coating particles to coalesce together and form a coating film. The electrostatic dry powder technology has many advantages compared with solvent or aqueous coating such as higher coating efficiency with better coating film, less energy consumption and shorter processing time, which is a promising alternative of liquid coatings used in the present pharmaceutical industry.The objective of this review is to introduce the development background, fundamental principles, technological superiority of the electrostatic powder coating for solid dosage forms,and to summarize and discuss those reported results, giving prospects for the future industrial applications.

Engineering spray-dried rosemary extracts with improved physicomechanical properties: a design of experiments issue

ABSTRACT A 33 Box–Behnken design and Response Surface Methodology were performed to evaluate the influence of extract feed rate, drying air inlet temperature and spray nozzle airflow rate on the process yield, stability parameters (moisture content and water activity) and on several physicomechanical properties of spray-dried rosemary extracts. Powder yield ranged from 17.1 to 74.96%. The spray-dried rosemary extracts showed moisture content and water activity below 5% and 0.5%, respectively, which indicate their chemical and microbiological stabilities. Even without using drying aids, some sets of experimental conditions rendered dried products with suitable flowability and compressibility characteristics for direct preparation of solid dosage forms. Analysis of variance and Response Surface Methodology proved that studied factors significantly affected most of the spray-dried rosemary extract quality indicators at different levels. The main processing parameter affecting the spray-dried rosemary extract characteristics was inlet temperature. The best combination of parameters used to obtain a reasonable yield of stable dry rosemary extracts with adequate technological properties for pharmaceutical purpose involves an extract feed rate of 2 ml/min, 80 °C inlet temperature and 40 l/min SA. The design of experiments approach is an interesting strategy for engineering spray-dried rosemary extracts with improved characteristics for pharmaceutical industrial purpose.

Development of Fast Disintegration Tablets As Oral Drug Delivery System-A Review.

Fast disintegrating tablets (FDTs) have received increasing demand from the last few years and the field has become a rapidly growing field in the pharmaceutical industry. Fast disintegrating tablets (FDTs) are those solid doses form which when put on the tongue gets rapidly dissolved, releasing the drug within a few second without need of water. The development of FDTs have been formulated for paediatric, geriatric and bedridden patients and for active patients who are busy and travelling and may not have access to water. Such formulation provide an opportunity for product line extension in the many elderly persons will have difficulties in taking conventional oral doses forms (viz, solution suspensions tablet and capsules) because of hand tremors and dysphagia. This article focused on ideal requirements, need for development of FDTs, challenges in formulations, suitability of drug candidates superdisintegrants employed, various technologies developed for FDTs. Evaluation methods, and various marketed products.