11 results about "Systemic absorption" patented technology

The present invention relates to oral films containing an active pharmaceutical ingredient (API) capable of providing seizure relief and one or more film-forming polymers, the use of such films, for example for the acute treatment of ongoing seizures, and methods for preparing such films. The film according to the invention is characterized by a rapid dissolution in the buccal cavity followed by a rapid and high systemic absorption.

The application belongs to the technical field of cosmetics and skin external preparation, and discloses a retinoid, a preparation method and application thereof. The compound is formed by covalently coupling a Schiff base or a kinin releasing enzyme cleavable peptide bond (L) and a free L-amino acid, a di- to hexapeptide or a C6-C22 fatty acid ester (P) of the retinol parent (R), and the structural general formula is R-L-P. The compound has a 12-week stability rate of ≥80% in a 25℃ aqueous preparation, is recognized by a keratin layer carboxylic acid esterase and a kinin releasing enzyme KLK-5 / KLK-7 after being applied to the skin, is subjected to enzymatic cutting in a skin acidic cuticle (pH 4.5-5.5) microenvironment, and releases free retinol at a fixed point. Compared with retinol palmitate, the in-situ release efficiency of the compound of the application is increased by 2.5-4.5 times, while the risk of systemic absorption is significantly reduced, and the incidence of sensitive skin irritation is ≤6.7%.

A transdermal patch for delivering lidocaine for pain relief comprises a backing layer, an adhesive layer, and a composition containing lidocaine in an amount ranging from about 1% to about 10% by weight and heparin as a non-anticoagulant permeation enhancer in an amount ranging from about 1% to about 50% by weight. The heparin enhances permeation of lidocaine through the skin without exerting systemic anticoagulant effects by temporarily disrupting lipid bilayers in the stratum corneum to create microchannels for increased diffusion of lidocaine molecules. The patch provides effective relief for multiple pain types including neuropathic pain, inflammatory pain, ischemic pain, post-surgical pain, nociplastic pain, mechanical pain, and compressive pain. The transdermal patch is configured to provide sustained release of lidocaine for periods ranging from about 8 hours to about 24 hours, reducing pain by at least 50% with minimal systemic absorption.

The invention described herein relates to pharmaceutical compositions that are capable of delivering active pharmaceutical ingredients, such as estrogens, to the vagina and vagina-associated tissues and related methods of making and using such compositions (e.g., in the treatment of disease). Compositions of the invention are capable of being absorbed by the vagina or vagina-associated tissues such that subjects receiving treatment with the compositions may resume ambulatory activity immediately after receiving the treatment, the frequency or amount of discharge associated with the composition is low or negligible, there is little or no systemic absorption associated with the administration of the active pharmaceutical composition, or results in a combination of any or all thereof.

This invention provides a topical finasteride formulation and its preparation method, belonging to the field of pharmaceutical formulation technology. The topical finasteride formulation provided by this invention is a topical dosage form, comprising finasteride and excipients; after scalp administration, the concentration in hair follicles and the epidermis is 999-5021 pg / mL, and the systemic blood concentration is 17.1-178.9 pg / mL; the systemic blood concentration is 1-10% of that of oral finasteride formulations. The method involves preparing finasteride and excipients, followed by steps of dissolving / preparing the matrix, fine filtration / homogenization, and filling to obtain finasteride topical formulations of different dosage forms. This invention effectively solves the shortcomings of existing finasteride formulations, such as high systemic absorption, high risk of adverse reactions, and difficulty in industrializing the process, making it suitable for large-scale clinical application in androgenetic alopecia, combining efficacy and safety.

The invention relates to formulation for oral delivery of peptides and / or drug molecules and a method of manufacturing the same. The oral formulation is useful for delivering peptides to the gastrointestinal tract, preferably at the ileo-caecal junction of colon.

The invention provides a soluble microneedle loaded with triptolide and salvianolic acid A as well as a preparation method and application of the soluble microneedle, and relates to the technical field of pharmaceutical preparations. According to the invention, the soluble microneedle is utilized to load the triptolide nanocrystal and the salvianolic acid A, and the medicine which can directly act on the diseased joint of a patient with rheumatoid arthritis through local transdermal administration is prepared. By using the soluble microneedle loaded with the triptolide and the salvianolic acid A, the skin delivery capacity can be improved, accumulation of diseased regions is increased, meanwhile, side effects caused by systemic drug absorption are reduced, the curative effect is improved by using the two drugs together, and the soluble microneedle loaded with the triptolide and the salvianolic acid A has a better treatment effect on rheumatoid arthritis.

The invention discloses a mesalazine colon-targeted drug delivery transfer system as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The transfer system comprises a mesalazine drug carrier skeleton, an enzyme sensitive component and a pH sensitive coating, the enzyme-sensitive component wraps the outer layer of the mesalazine drug carrier skeleton or is mixed with the mesalazine drug carrier skeleton; the pH-sensitive coating wraps the outer layer of the enzyme-sensitive component or the outer layer of the mixture of the enzyme-sensitive component and the mesalazine drug carrier skeleton. A unique enzyme-sensitive and pH-sensitive double-layer coating technology is adopted, so that enzymatic degradation of mesalazine in a gastric acid environment and the upper section of a small intestine is effectively protected, and early release and whole-body absorption of drugs are remarkably reduced; it is ensured that mesalazine is efficiently and intensively released in the colon environment; the bioavailability of mesalazine in a colon focus is improved, and the local treatment effect is enhanced; the systemic exposure of mesalazine is reduced, and potential systemic adverse reactions are reduced.

The invention discloses a hyoscyamine derivative and a preparation method thereof, relates to the field of drug synthesis, and aims to provide an effective and safe drug molecule for inhalation / local pulmonary administration. According to the invention, a linear polyethylene glycol chain containing seven ethylene glycol repeating units is introduced into a hydroxyl site of hyoscyamine, and quaternization is carried out on a nitrogen atom of the hyoscyamine, so that the hyoscyamine derivative is prepared. The derivative is specially designed for inhalation / local lung drug delivery, through structural modification, systemic absorption and central penetration of the compound are reduced, local exposure of the lung is improved, residence time in the lung is prolonged, and meanwhile good atomization performance is taken into account.

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and / or -8 mediated antiport of sodium and / or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and / or salt present in the GI tract.

This invention discloses a hyoscyamine derivative and its preparation method, relating to the field of drug synthesis, and aims to provide an effective and safe drug molecule for inhalation / local pulmonary administration. The invention prepares the hyoscyamine derivative by introducing a linear polyethylene glycol chain containing seven ethylene glycol repeating units at the hydroxyl position of hyoscyamine and quaternizing its nitrogen atom. This derivative is specifically designed for inhalation / local pulmonary administration. Through the above structural modification, it achieves reduced systemic absorption and central penetration of the compound, increased local lung exposure, and prolonged pulmonary retention time, while also maintaining good nebulization performance.