Hunt Valley, MD, United States
Hunt Valley, MD, United States

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PubMed | Kansas State University, Shanghai Institute of Planned Parenthood Research, CAS Shanghai Institute of Materia Medica and Pharmaceutics International Inc.
Type: Journal Article | Journal: European journal of drug metabolism and pharmacokinetics | Year: 2015

Nomegestrol acetate (NOMAC), a synthetic progestogen derived from 19-norprogesterone, is an orally active drug with a strong affinity for the progesterone receptor. NOMAC inhibits ovulation and is devoid of undesirable androgenic and estrogenic activities. The aim of this study was to evaluate the pharmacokinetics, tissue distribution, and excretion of NOMAC in female rats. Sprague-Dawleyfemale rats were orally administered a single dose of NOMAC (10, 20 or 40mg/kg) and drug plasma concentrations at different times were determined by RP-HPLC. Tissue distribution at 1, 2, and 4h and excretion of NOMAC into bile, urine, and feces after dosing were investigated. The results showed that NOMAC was rapidly absorbed after oral administration, with [Formula: see text] of 1-2h. The plasma concentration-time curves were fitted in a two-compartment model. The exposure to NOMAC ([Formula: see text] and [Formula: see text]) increased dose proportionally from 10 to 40mg/kg. The average CL and [Formula: see text] were 5.58L/(hkg) and 10.8h, respectively. The highest concentrations of NOMAC in ovary, liver, kidney, lung, heart, brain, spleen, muscle, and uterus were observed at 2h, whereas the highest concentrations in stomach, pituitary, and hypothalamus appeared at 1h. The total cumulative excretion of NOMAC in feces (0-72h), urine (0-72h), and bile (0-48h) was ~1.06, 0.03, and 0.08% of the oral administered dose, respectively. This study indicated that NOMAC had a widespread distribution in tissues, including ovary, pituitary, and hypothalamus, which are main target tissues where NOMAC inhibits ovulation. NOMAC was excreted via both feces and urine with few unchanged NOMAC excreted. Enterohepatic circulation was found in the drug elimination; however, it did not significantly affect [Formula: see text].


Hiremath P.S.,Pharmaceutics International Inc | Bhonsle S.A.,Pharmaceutics International Inc | Thumma S.,Pharmaceutics International Inc | Vemulapalli V.,Pharmaceutics International Inc
Recent Patents on Drug Delivery and Formulation | Year: 2011

Oral combination drug delivery systems have been proven to be highly beneficial and vital in the treatment ofseveral dreadful diseases such as cancer, HIV (AIDS) and tuberculosis. Further, pharmaceutical companies have oftenexplored the strategy of combination drug therapy for treating diseases such as diabetes (Type 2), cardiovascular diseases,central nervous system (CNS) disorders, and for treating several other microbial infections. Patenting combination drugdelivery systems and formulations has been proven to be very beneficial for the sustainment and growth of pharmaceuticalindustry. Several pharmaceutical companies have explored this opportunity in extending the life cycle of their blockbustermolecules, and providing additional sources of revenues when the new chemical entity (NCE) discovery is scarce. Thearticle reviews some recent combination formulation patents and patent publications, particularly the US patents andpatent applications, relevant to oral delivery of pharmaceuticals. Examples of some oral combination products on the USand worldwide market are presented. Patents and patent applications on combination oral formulations relevant toanalgesics (including anti-inflammatory and antipyretics), cardiovascular system (CVS) products, antibacterial andantiviral, and central nervous system (CNS) products are briefly discussed. © 2011 Bentham Science Publishers Ltd.


Patent
Pharmaceutics International Inc. | Date: 2010-11-24

The invention provides a formulation comprising (a) a drug that is poorly water-soluble, (b) at least one surfactant, and (c) at least one polar lipid, wherein the formulation is substantially free of a polar solvent, as well as methods of preparing the formulation and methods of increasing the bioavailability of a drug using the formulation.


Patent
Pharmaceutics International Inc. | Date: 2015-07-17

The invention provides a formulation comprising (a) a drug that is poorly water-soluble, (b) at least one surfactant, and (c) at least one polar lipid, wherein the formulation is substantially free of a polar solvent, as well as methods of preparing the formulation and methods of increasing the bioavailability of a drug using the formulation.


Patent
Pharmaceutics International Inc. | Date: 2012-05-25

The invention provides a method of preparing a pharmaceutical composition comprising: (a) combining progesterone particles with a liquid carrier to provide a mixture; (b) wet-milling the mixture to provide a wet-milled progesterone composition; and (c) processing the wet-milled progesterone composition to provide a pharmaceutical composition. Pharmaceutical compositions prepared by the method are also provided.


Patent
Pharmaceutics International Inc. | Date: 2014-02-07

This invention relates to macromolecular complexes useful in drug delivery systems, specifically tri-molecular complexes made between a water-soluble polymer and an acid-insoluble polymer in presence of a bridging molecule. In one aspect, the invention relates to a tri-molecular complex comprising gelatin, acrylic acid/methacrylic acid copolymers, and arginine for use in a soft capsule dosage form. In another aspect, the invention is directed to a tri-molecular complex a hydrophilic, film-forming, water-soluble polymer, a second water-soluble polymer, and a bridging molecule, wherein the second water-soluble polymer is less water-soluble than the hydrophilic, film-forming, water-soluble polymer.


Patent
Pharmaceutics International Inc. | Date: 2013-12-03

The invention provides a composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt, as well methods of producing such a solid naproxen concentrate.


Patent
Pharmaceutics International Inc. | Date: 2014-04-23

The invention provides a tri-molecular complex for use in enteric drug delivery systems comprising: (a) a hydrophilic, film-forming, water-soluble polymer; (b) an acid-insoluble polymer; and (c)an amino acid. The invention further provides a method or preparing such complexes.


Patent
Pharmaceutics International Inc. | Date: 2012-12-26

The invention provides a composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt, as well methods of producing such a solid naproxen concentrate.


Patent
Pharmaceutics International Inc. | Date: 2011-03-02

A pharmaceutical composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt.

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