Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol.

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Research Abstract Details 

Research Abstract Table of Contents

Jump to the:

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Abstract Text:

Koichi Yokogawa,Katsuhiro Toshima,Kayo Yamoto,Tatsuo Nishioka,Naoki Sakura,Ken-Ichi Miyamoto,

We examined the usefulness of intranasal (i.n.) administration of a novel osteotropic prodrug of estradiol, estradiol-17beta-succinate-(L-aspartate)(6) (E(2).17D(6)), for selective drug delivery to bone. E(2).17D(6) alone or with 5% 2,6-di-O-methyl-beta-cyclodextrin (DMbetaCD), 5% beta-cyclodextrin (betaCD), or 10% hydroxypropyl cellulose (HPC) as an absorption enhancer was administered to ovariectomized (OVX) mice via the i.n. route. The oral and nasal bioavailability after p.o. or i.n. administration of E(2).17D(6) (3.7 mumol/kg) in mice amounted to 9.9 and 23.0% of the dose, respectively. The values of nasal bioavailability of E(2).17D(6) administered with DMbetaCD, betaCD, and HPC were 74.9, 55.8, and 49.1%, respectively. The plasma concentration of E(2).17D(6) after i.n. administration of E(2).17D(6)-DMbetaCD decreased rapidly to the endogenous level by 6 h, but the concentration in the bone was about 200 times higher than that in plasma, and decreased slowly over a period of about a week. When E(2) (total dose 4.4 mumol/kg, i.n., every 3rd day) was administered to OVX mice for 35 d, bone mineral density (BMD), liver weight, and uterus weight increased, whereas E(2).17D(6)-DMbetaCD (total dose 0.44 to 8.8 mumol/kg, i.n., every 7th day) increased only BMD in a dose-dependent manner. In conclusion, intranasally administered E(2).17D(6)-DMbetaCD has a potent antiosteoporotic effect without side effects, and has potential to provide an improved quality of life for patients with osteoporosis.

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Publishing Authors By Initials

K Yokogawa,K Toshima,K Yamoto,T Nishioka,N Sakura,K Miyamoto,

For similar abstracts research abstracts see: abstracts research

PUBMED ID PMID:

MEDLINE DATE:

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Biological & pharmaceutical bulletin

VOLUME: 29

Page Numbers: 1229-33

Journal Abbreviation: Biol. Pharm. Bull.

ISSN: 0918-6158

DAY: 6

MONTH: Jun

YEAR: 2006

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9311984

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Keywords Mesh Terms:

KEYWORDS:

MESH TERMS:

Chemical & Substance for Abstract: Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol. Information

Substance Name:

Registry Number:

Grant and Affiliation Information for Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol.

AFFILIATION: Department of Clinical Pharmacy, Graduate School of Natural Science and Technology, Kanazawa University.

Country: Japan

AGENCY:

GRANT:

ACRONYM:

MEDLINETA: Biol Pharm Bull

REFSOURCE:

DATABASENAME:

ACCESSION NUMBER:

Number Hits: 0

Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol Related Publications

• A case of Pallister-Killian syndrome associated with West syndrome.
• A cone-beam volume CT using a 3D angiography system with a flat panel detector of direct conversion type: usefulness for superselective intra-arterial chemotherapy for head and neck tumors.
• A serum glycomics approach to breast cancer biomarkers.
• A word on protection afforded by profound hypothermic alpha-stat cardiopulmonary bypass for resuscitation.
• Analysis of lipid hydrolytic activity by esterase on blotting membrane followed by separation using non-denaturing two-dimensional gel electrophoresis.
• Apoptosis triggered by phagocytosis-related oxidative stress through FLIPS down-regulation and JNK activation.
• Bovine Endothelial Cells Interact with Fully-luteinized, but Not Luteinizing, Granulosa Cells in the mRNA Expression of Endothelin-1 System in Response to Prostaglandin F(2alpha).
• Calcium-dependent regulation of NEMO nuclear export in response to genotoxic stimuli.
• Circadian rhythm of cytochrome P4502E1 and its effect on disposition kinetics of chlorzoxazone in rats.
• Clinical Results of Carbon Ion Radiotherapy at NIRS.
• Concentration dependence of equivalent conductivity of polyelectrolyte.
• Development of a three-electrode-lens drift tube for time-of-flight mass spectrometry.
• Dosimetric factors used for thoracic X-ray radiotherapy are not predictive of the occurrence of radiation pneumonitis after carbon-ion radiotherapy.
• Incorporating experimental design and error into coalescent/mutation models of population history.
• Indoor Cultivation and Cultural Characteristics of Wolfiporia cocos Sclerotia Using Mushroom Culture Bottles.
• Influence of chronic hepatic failure on disposition kinetics of valproate excretion through a phase II reaction in rats treated with carbon tetrachloride.
• Inhibition of potential lethal damage repair and related gene expression after carbon-ion beam irradiation to human lung cancer grown in nude mice.
• Many faces of NF-kappaB signaling induced by genotoxic stress.
• Neural mechanisms involved in the comprehension of metaphoric and literal sentences: an fMRI study.
• Pharmacokinetic Advantage of an Intranasal Preparation of a Novel Anti-osteoporosis Drug, L-Asp-Hexapeptide-Conjugated Estradiol.
• Progesterone induces the expression of vascular endothelial growth factor (VEGF) 120 and Flk-1, its receptor, in bovine granulosa cells.
• Remodeling of the radial artery anastomosed to the internal thoracic artery as a composite straight graft.
• SUMO and NF-kappaB ties.
• Short communication: A positive relationship between the first ovulation postpartum and the increasing ratio of milk yield in the first part of lactation in dairy cows.
• The prognostic value of carcinoembryonic antigen in T1N1M0 and T2N1M0 non-small cell carcinoma of the lung.
• The relationship between post-prandial plasma glucose and post-challenge plasma glucose in Japanese population.
• The release of monovalent counterions by addition of divalent counterions in coulombic interaction system of polyions (II).
• Vasomotor effects of noradrenaline, acetylcholine, histamine, 5-hydroxytryptamine and bradykinin on snake (Trimeresurus flavoviridis) basilar arteries.
• [Hypophosphatemic rickets/osteomalacia. - Mainly on patients with PHEX mutations -]
• [The effect of non-steroidal anti-inflammatory drugs on upper gastrointestinal disorders in orthopaedic patients]