Conventional forms of drug administration generally rely on pills, eye drops, ointments, and intravenous solutions. Recently, a number of novel drug delivery approaches have been developed. These approaches include drug modification by chemical means, drug entrapment in small vesicles that are injected into the bloodstream, and drug entrapment within pumps or polymeric materials that are placed in desired bodily compartments (for example, the eye or beneath the skin). These techniques have already led to delivery systems that improve human health, and continued research may revolutionize the way many drugs are delivered.

http://science.sciencemag.org/content/sci/249/4976/1527.full.pdf

New methods of drug delivery.

Biodegradation and biocompatibility of PLA and PLGA microspheres

Years of cumulative research can result in the development of a clinically useful drug, providing either a cure for a particular disease or symptomatic relief from a physiological disorder. A lead compound with a desired pharmacological activity may have associated with it undesirable side effects, characteristics that limit its bioavailability, or structural features which adversely influence its metabolism and excretion from the body. Bioisosterism represents one approach used by the medicinal chemist for the rational modification of lead compounds into safer and more clinically effective agents. The concept of bioisosterism is often considered to be qualitative and intuitive.1 The prevalence of the use of bioisosteric replacements in drug design need not be emphasized. This topic has been reviewed in previous years.2-5 The objective of this review is to provide an overview of bioisosteres that incorporates sufficient detail to enable the reader to understand the concepts being delineated. While a few popular examples of the successful use of bioisosteres have been included, the George Patani graduated with a B.Pharm. in 1992 from the College of Pharmaceutical Sciences, Mangalore University at Manipal, India. In 1996, he received his M.S. in Pharmaceutical Science at Rutgers University under the direction of Professor Edmond J. LaVoie. He is presently pursuing graduate studies in pharmaceutics. His current research interests are focused on drug design and controlled drug delivery.

https://www.mch.estranky.sk/file/228/1996chemrev96-3147-76_bioisosterism.pdf

Bioisosterism: A Rational Approach in Drug Design.

The manufacturing techniques of various drug loaded biodegradable poly(lactide-co-glycolide) (PLGA) devices.

This review covers recent developments in the area of particle engineering via spray drying. The last decade has seen a shift from empirical formulation efforts to an engineering approach based on a better understanding of particle formation in the spray drying process. Microparticles with nanoscale substructures can now be designed and their functionality has contributed significantly to stability and efficacy of the particulate dosage form. The review provides concepts and a theoretical framework for particle design calculations. It reviews experimental research into parameters that influence particle formation. A classification based on dimensionless numbers is presented that can be used to estimate how excipient properties in combination with process parameters influence the morphology of the engineered particles. A wide range of pharmaceutical application examples—low density particles, composite particles, microencapsulation, and glass stabilization—is discussed, with specific emphasis on the underlying particle formation mechanisms and design concepts.

/pdf/pharmaceutical-particle-engineering-via-spray-drying-1wv9pxpwlb.pdf

Pharmaceutical particle engineering via spray drying.

This invention relates to a process for preparing a cephamycin type antibiotic substance which comprises cultivating a microorganism belonging to the genus Streptomyces under aerobic conditions and a primary object of this invention is to provide a process for preparing the said product on a simple and industrial scale.

Process for preparing a cephamycin type antibiotic substance

A pharmaceutical composition, suitable for use in treating prostatomegaly, comprises an anti-androgenically active compound represented by the formula [1]:
 wherein the bond at the 10-position indicates a carbon-carbon single bond or a carbon-carbon double bond and A indicates a hydrogen atom or an ether or ester residue, and other appropriate components so that the preparation is in the form of an administration unit which is intended to be placed in the oral cavity of a patient to enable the anti-androgenically active compound of formula [I] to be absorbed through the oral mucous membrane. The administration unit has a disintegration time of 30 minutes or longer.

Anti-androgenic preparation for oral cavity administration

Novel antibiotics derivatives 7-(5-acylamido-5-carboxyvaleramido)-3-(α-methoxy-p-acyloxycinnamoyloxymethyl)-7-methoxy-3-cephem-4-carboxylic acids and the salts thereof which are useful as antibiotics and intermediates for the preparation of cephamycin derivatives, a process for preparing the same, and a process for recovering the cephamycin derivatives effectively and stably from the fermentation broth in the form of an N-acyl derivative.

Novel antibiotics derivatives and process for preparing the same

Preparation with sustained release

Microencapsulation techniques, phase separation and solvent evaporation, have been developed for preparation of drug-containing monolithic microcapsules for prolonged release using poly(lactide-co-gtycolide) and copoly(lactic/glycolic) acid. A new technique encapsulating highly water-soluble drugs has been established by modifying the solvent evaporation method using a w/o/w emulsion. The method can completely entrap the highly water-soluble drugs into the microcapsules and can easily prepare the microcapsules in a large scale. The drug releases in a pseudozero order kinetics for several weeks with degradation of the polymers after an initial burst release. Many prolonged release-microcapsules containing water-soluble peptides and proteins were prepared by this method. It is difficult to avoid the initial burst release from the microcapsules containing a water-soluble drug, and a technique to avoid the burst has not been found yet. But an insulin-microcapsule system without the initial burst release has just been presented in the DDS meeting in Japan in this summer. The initial burst problem will be solved in near future.

Yasuaki Ogawa

Papers

Process for preparing a cephamycin type antibiotic substance

Anti-androgenic preparation for oral cavity administration

Novel antibiotics derivatives and process for preparing the same

Preparation with sustained release

Microcapsules prepared with biodegradable polymer for prolonged release of drugs.