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Related Concept Videos

Intrauterine Drug Delivery Systems01:21

Intrauterine Drug Delivery Systems

Controlled-release systems for intravaginal and intrauterine drug delivery have been developed primarily for the administration of contraceptive steroid hormones. These delivery routes circumvent first-pass hepatic metabolism, thereby enhancing bioavailability and allowing for reduced systemic dosages compared to oral administration. Such approaches contribute to improved therapeutic efficacy and patient compliance, particularly in long-term contraceptive regimens.Intravaginal Drug Delivery...
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence01:22

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Generic intravenous (IV) drugs are considered bioequivalent to their branded counterparts due to their 100% bioavailability upon administration. However, variations in stability among different drug products can significantly influence their therapeutic performance, even if they are pharmaceutically equivalent.Cefuroxime, a prophylactic antimicrobial, is often used as a single-dose IV injection for patients undergoing coronary artery bypass grafting surgery. A 3 g dose typically provides...
Transdermal Drug Delivery Systems01:18

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Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

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Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
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Updated: Jun 16, 2026

Radiosynthesis of 1-(2-[18F]Fluoroethyl)-L-Tryptophan using a One-pot, Two-step Protocol
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Triptorelin embonate (6-month formulation).

Gillian M Keating1

  • 1Adis, a Wolters Kluwer Business, Auckland, New Zealand. demail@adis.co.nz

Drugs
|February 20, 2010
PubMed
Summary
This summary is machine-generated.

A new 6-month triptorelin embonate formulation effectively induces and maintains castrate testosterone levels in advanced prostate cancer patients. This long-acting treatment demonstrates good tolerability and rapid efficacy for managing advanced prostate cancer.

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Last Updated: Jun 16, 2026

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In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Area of Science:

  • Oncology
  • Endocrinology
  • Pharmacology

Background:

  • Advanced prostate cancer treatment often relies on androgen deprivation therapy.
  • Gonadotropin-releasing hormone (GnRH) agonists are a key component of androgen deprivation.
  • A sustained-release formulation of triptorelin embonate offers a potential improvement in treatment convenience and efficacy.

Purpose of the Study:

  • To evaluate the efficacy and safety of a 6-month formulation of triptorelin embonate (22.5 mg) for advanced prostate cancer.
  • To assess the time to achieve and maintain castrate serum testosterone levels.
  • To determine the tolerability and adverse event profile of the 6-month formulation.

Main Methods:

  • A pivotal, noncomparative, multicenter trial involving 120 patients with advanced prostate cancer.
  • Intramuscular administration of triptorelin embonate 22.5 mg on day 1 and at month 6.
  • Monitoring of serum testosterone levels throughout the 12-month study period.

Main Results:

  • Castrate serum testosterone levels (< or =1.735 nmol/L) were achieved in a geometric mean time of 18.8 days.
  • By day 29, 97.5% of patients achieved castrate levels.
  • From months 2 to 12, 93.0% of patients maintained castrate levels, with 98.3% achieving this prior to the second injection and at study completion.

Conclusions:

  • The 6-month formulation of triptorelin embonate 22.5 mg is effective in achieving and sustaining castrate serum testosterone levels in patients with advanced prostate cancer.
  • The formulation was generally well tolerated, with adverse events primarily of mild severity and consistent with triptorelin's known effects.
  • This long-acting formulation provides a convenient and effective treatment option for advanced prostate cancer management.