Hydroxy progesterone caproate oral preparation and its use

A technology of hydroxyprogesterone caproate and oral preparations, applied in the field of oral preparations of medicines, can solve problems such as slow absorption, induration, patient pain and the like

Inactive Publication Date: 2005-06-08
北京京卫燕康药物研究所有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As mentioned above, hydroxyprogesterone caproate is an oily preparation, which is slowly absorbed after injection and stored in local deposits. Long-term use will easily cause induration at the injection site, which will bring pain to the patient and affect the application.
Especially for patients with tumors, the treatment time is as long as several years, and it is inconvenient to use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0004] Embodiment 1: Measuring method Use high-performance liquid chromatography to measure hydroxyprogesterone caproate, Waters490 chromatograph C18 column, measuring wavelength 240nm, mobile phase: methanol: water=85: 15, flow rate 1ml / min, injection 20 μ l, specimen processing : Diethyl ether extracts hydroxyprogesterone caproate and internal standard medroxyprogesterone in plasma, the recovery rate is 85%, the linear range of the standard curve: 0.1, 0.2, 0.4, 0.8, 1.0 μg, and the correlation coefficient R=0.9998. The minimum detection amount is 0.02μg.

Embodiment 2

[0005] Embodiment 2: the bioavailability of hydroxyprogesterone caproate capsule after intragastric administration of mice Kunming species mice, body weight 25-30 grams, every 3 are blood points for a time, intraperitoneal injection and intragastric administration of 200mg / kg hexa For hydroxyprogesterone caproate, blood was taken at 0, 0.25, 0.5, 1, 2, 4, and 6 hours after administration to measure the concentration of hydroxyprogesterone caproate, and the area under the drug-time curve (AUC) and bioavailability were calculated. The bioavailability of hydroxyprogesterone caproate capsules after gavage in mice was 84.8%.

[0006] Table 1. Blood concentration of hydroxyprogesterone caproate in mice by intraperitoneal injection and intragastric administration

[0007] Post-drug time (h) and drug concentration (μg / ml)

[0008] Route of Administration AUC

[0009] 0.25 0.5 1 2 4 6 (μg / ml / h)

[0010] Intraperitoneal injection 1.23 1.16 0.87 0.56 0.42 0...

Embodiment 3

[0013] Example 3: Bioavailability of Hydroxyprogesterone Caproate Tablets in Dogs Oral Bioavailability Hydroxyprogesterone Caproate Tablets Prescription and Process: Hydroxyprogesterone Caproate 250g, Starch 120g, Microcrystalline Cellulose 120g, Magnesium Stearate 10g . Mix the first four kinds, pass through a 40-mesh sieve twice, make soft materials with 50% ethanol, pass through a 16-mesh sieve to make wet granules, and ventilate and dry at 60°C. Whole granules, granulated with magnesium stearate, mixed evenly, compressed into tablets. Beagle dog body weight 8-10kg, administration dose 100mg / kg, intravenous administration is slow injection 10 minutes, and oral administration is that medicine is put into 100ml broth, and dog eats in 2-3 minutes. Blood was collected at 0, 0.25, 0.5, 1, 2, 4, and 6 hours after administration to determine the concentration of hydroxyprogesterone caproate, and the area under the drug-time curve (AUC) and bioavailability were calculated. Hydrox...

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PUM

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Abstract

An orally taken medicine of hyproval-PA in the form of tablet, capsule, soft capsule, instant particles, etc for treating breast cancer and functional metrorrhagia is disclosed. its advantages are high biologic utilization rate and high curative effect.

Description

technical field [0001] The invention relates to an oral preparation and application of a medicine. Specifically, it is an oral formulation and use containing hydroxyprogesterone caproate. technical background [0002] Hydroxyprogesterone Caproates (Hydroxyprogesterone Caproates) is a standard drug collected in the Chinese Pharmacopoeia in 2000. Indications are the treatment of habitual abortion, irregular menstruation, endometriosis, dysfunctional uterine bleeding, etc. The dosage form is an oily injection, and the method of use is intramuscular injection, 1-2 times a week, 0.25-0.5g each time (250mg / support). After intramuscular injection, the drug is deposited and stored locally, slowly absorbed, and exerts long-acting effects. Oil preparations are suitable for the above indications. In addition to the above, other uses of hydroxyprogesterone caproate have been reported in the literature. In 1991, Cheng Zhaoming reported intramuscular injection fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/57A61P15/00A61P35/00
Inventor 张伟张佐云
Owner 北京京卫燕康药物研究所有限公司
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