Neelam Sharma, MS, Lakshmi Lavanya Kundurthy, BE and Hemant N. Joshi, Ph.D., MBA* - Tara Innovations, LLC, www.tara-marketing.com, *[email protected]
The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in May 2023.
Composition Comprising Lactic Acid Bacteria Improved in Intestinal Adherence by Coating with Silk Fibroin;
B. Heo, Y. Kim, W. Kim, M. Seo, B. Kim, and I. Choi; CKD Bio Corp, Seoul, Korea; U.S. Patent # 11,642,318; May 9, 2023.
Lactic acid bacteria are a group of bacteria that produce lactic acid by using sugars as energy sources. Lactic acid bacteria are found in humans and are widely distributed in natural systems. Lactic acid bacteria are microorganisms that produce no harmful substances in human or animal intestines and have a beneficial function of preventing decay in the intestines. The present invention is to provide a composition containing lactic acid bacteria coated with silk fibroin and cellulose. Also, it provides a method for enhancing viability, storage stability, resistance against acid or bile, and intestinal epithelial cell adhesion of lactic acid bacteria. Conventional techniques construct only a physical protective barrier outside a lactic acid bacteria body by multi-stage coating and thus, retains the limitation of being unable to identify an effect on the coherence of lactic acid bacteria to intestinal epithelial cells upon the uptake of the lactic acid bacteria. In contrast, the present invention provides a method in which lactic acid bacteria is coated with silk fibroin extracted from cocoons, whereby the lactic acid bacteria are improved in stability under a storage and distribution condition as well as having remarkably increased stability and intestinal adherence particularly under an intestinal environment.
Solid Dispersion Forms of Rifaximin;
P. Golden and M.A. Kabir; Salix Pharmaceuticals, Inc., USA: U.S. Patent # 11,660,292; May 30, 2023.
The incidence of liver disease is on the rise and will continue to be a major health burden. Cirrhosis is a major cause of much of the chronic liver disease (CLD). The management of cirrhosis is based on disease severity. The use of rifaximin in preventing complications of cirrhosis is supported by multiple lines of clinical and experimental evidence. It has now been discovered that certain pharmaceutical compositions comprising solid dispersions of rifaximin effectively reduce the hospitalization time and prevent mortality associated with complications of liver disease. The present disclosure provides pharmaceutical compositions comprising solid dispersions of rifaximin as well as methods for their manufacture, and therapeutic uses associated with complications of liver disease. Present patent discloses solid dispersions comprising rifaximin and hydroxypropyl methylcellulose acetate succinate (HPMC-AS) wherein the HPMC-AS is present in an amount of from about 10 wt % to about 60 wt %.
Assays and Reagents for Antimicrobial Susceptibility Testing;
B. Spears and K. Flentie; Selux Diagnostics, Inc., USA; U.S. Patent # 11,649,477; May 16, 2023.
Antimicrobial resistance (AMR) has emerged as a major threat to public health globally. Phenotypic antimicrobial susceptibility testing (AST) of microorganisms is critical for informing physicians of appropriate therapeutic regimens. Using current methods, AST determination is time consuming. There is an urgent need for a more rapid and reliable test to improve infection diagnosis and support evidence-based antimicrobial prescribing. Present patent describes systems and methods for AST in which variances in anionic charge of microbes are taken into account. Cationic surfactants may be used to sensitize otherwise resistant microorganisms to polycationic antibiotics, such as polymyxins. Since microorganisms gain polycationic antibiotic resistance through mutations that decrease surface anionic charge, the susceptibility of a microorganism to a polycationic antibiotic may be indicative of its surface charge. In order to enable electrostatic interactions with the microorganism surface, a cationic surfactant may be applied to increase the anionic charge of the microorganism.
Pharmaceutical Compositions Containing Anti-Beta Amyloid Antibodies;
S.A. Lantz, K. Gupta, S. Sule, and A. Zunic; Biogen MA Inc., USA; U.S. Patent # 11,655,289; May 23, 2023.
Aβ is a peptide generated from the metabolism of amyloid precursor protein (APP). These have a tendency to aggregate into dimers and oligomers. Patients with higher amounts of anti-Aβ antibodies are likely to show reduced cognitive impairment. The patent describes a pharmaceutical composition comprising an anti-beta amyloid antibody, arginine, methionine, histidine, and a thiol-containing antioxidant. Antibody formulations degrade due to mechanical stress during manufacture. Polysorbate 80 seemed to protect the antibody from agitation-induced stress. Formulations containing arginine and methionine were found to be more effective.
Blend Compositions for Oral Administration as a Rapidly Dissolving Powder and/or Suspension;
A. Favara and M. Karetny; Marenda Pharmaceuticals, LLC, USA; U.S. Patent # 11,642,312; May 9, 2023.
Patient acceptance of medications, often referred to as patient adherence, has been reported to average 50% in developing countries around the world. For example, oral tablet formulations can sometimes cause nausea and vomiting in patients. Further, unpleasant taste may be a challenge in administering a medicine particularly for children. Formulations which can be administered both in dry powder form and in suspension by adding a minimum quantity of water to dissolve the dry powder are not available on the market. Powder, solution, and suspension dosage forms typically utilize a different set of excipients to achieve acceptable physical properties. Also, taste masking of active pharmaceutical ingredients (API) is typically dependent on type, concentration, and processing method of excipients. Accordingly, the inventors herein have succeeded in devising formulations that can be administered either as a dry powder or in a small quantity of water. The new formulations provide improved taste and mouthfeel to facilitate ease of administration and patient adherence. Disclosed is a dry powder oral formulation, a chewable, swallowable, and/or orally disintegrating tablet that includes an API, a lecithin powder, a galactomannan, one or more sweetening agents, one or more flavoring agents and an organic acid in a pharmaceutically acceptable preparation. Also disclosed is an excipient composition in the absence of an API and methods of making and using the formulations and compositions.
Nanocrystals, Compositions and Methods Th at Aid Particle Transport in Mucus;
A. Popov, E.M. Enlow, J. Bourassa, C.R. Gardner, H. Chen, L.M. Ensign, S.K Lai, T. Yu, J. Hanes and M.Yang; The Johns Hopkins University, USA; U.S. Patent # 11,642,317; May 9, 2023.
Mucus layers in various places in the body serves to protect tissues against pathogens, allergens and debris. Mucus tends to clear foreign substances by its turn-over. Polymer-based mucus penetrating particles (MPP) can encapsulate various therapeutic agents and enable their delivery. The current patent describes specially coated nanoparticles. The surface altering agents comprised a triblock copolymer comprising a hydrophilic block-hydrophobic block-hydrophilic block configuration. The method allows very high drug loading. The patent described various kinds of dosage forms delivering medicines to different parts of body.
Darunavir Combination Formulations;
U.A.C. Delaet, P.E.H. Heyns, E.M.J. Jans, R.J.M. Mertens, and G.V.D. Avoort; Janssen Sciences Ireland Ltd., IE and Gilead Sciences, USA; U.S. Patent # 11,654,150; May 23, 2023.
Darunavir is an antiretroviral medication used to treat HIV/AIDS. Tablets of Darunavir with a dose of 600 mg have a total weight of over one gram and they are hard to swallow. Direct compression leads to inferior formulations due to limited gliding and flowing capacity. The present invention describes granulation of darunavir, which allows high drug loading in the tablet. Hypromellose in water is sprayed on darunavir powder and the granules are dried. The granules are further mixed with MCC, silicone dioxide and a disintegrant before making tablets. The formulation also contains GS-9350, an inhibitor of cytochrome P450 3A isoform, a pharmacokinetic enhancer.
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