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Progesterone formulations having a desirable pk profile

a technology of progesterone and formulation, applied in the field of progesterone formulation, can solve the problems of psychological side effects, inconsistent or irregular treatment of high levels of absorbed progesterone, and symptom and disorder, and achieve the effect of increasing the bioavailability of progesteron

Inactive Publication Date: 2015-07-16
THERAPEUTICSMD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text describes a new way to make progesterone that works better than traditional methods. This can be useful for improving the effectiveness of progesterone-based medications.

Problems solved by technology

But increased levels of estrogens, including estradiol, whether due to prescription or naturally-occurring increases, may lead to the symptoms and disorders previously mentioned.
Existing progesterone prophylactic methods and prescribed treatments inconsistently or irregularly achieve high levels of absorbed progesterone at low dosages of progesterone.
However, these compounds exert undesirable effects on the liver (notably on lipids) and often cause psychological side effects that can be severe enough to contraindicate their use.

Method used

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  • Progesterone formulations having a desirable pk profile
  • Progesterone formulations having a desirable pk profile
  • Progesterone formulations having a desirable pk profile

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Experimental program
Comparison scheme
Effect test

specific embodiments

[0254]Through extensive trial-and-error testing of various fatty acid esters of glycerol and other glycols, embodiments of the invention have been invented that have one or more favorable characteristics for development as a human drug product. Such favorable characteristics include those described above, e.g., improved PK properties and reduced inter- and intra-patient variability.

[0255]Such embodiments include an encapsulated liquid pharmaceutical formulation for orally administering progesterone to a mammal in need thereof, said formulation comprising: progesterone, as the sole active pharmaceutical ingredient, in ultra-micronized form suspended in a carrier that comprises a medium chain fatty acid-glycol ester or mixtures thereof and a non-ionic surfactant comprising a polyethylene glycol fatty acid ester.

[0256]In particular embodiments, the progesterone can be ultramicronized.

[0257]In certain embodiments, the progesterone is suspended or solubilized in one or more solubilizing ...

example 1

[0261]In an exemplary embodiment, a capsule is provided containing a fill material comprising a formulation set forth in one of Tables 2, 2A, or 2B

TABLE 2Ingredientmg / Capsule%FunctionUltra-micronized200.0030.77ActiveProgesteroneMedium ChainqsqsSolubilizing AgentTriglyceride(MIGLYOL 812 orequivalent)Lecithin Liquid1.630.25Lubricant / EmulsifierButylated0.130.02AntioxidantHydroxytoluene (alsoreferred to as “BHT”)

TABLE 2AIngredientmg / Capsule%FunctionProgesterone15033.3ActiveMedium Chain292.365.0Solubilizing AgentTriglyceride(MIGLYOL 812 orequivalent)Lauroyl polyoxyl-32-7.71.7Lubricant / Emulsifierglycerides (GELUCIRE44 / 14 or equivalent)

TABLE 2BIngredientmg / Capsule%FunctionProgesterone7533.3ActiveMedium Chain146.265.0Solubilizing AgentTriglyceride(MIGLYOL 812 orequivalent)Lauroyl polyoxyl-32-3.81.7Lubricant / Emulsifierglycerides (GELUCIRE44 / 14 or equivalent)

[0262]The formulation in Table 2 is prepared as follows: MIGLYOL is heated to about 45° C. GELUCIRE 44 / 14 is added and mixed until disso...

example 2

[0264]In an exemplary embodiment, a capsule is provided containing a fill material comprising:

TABLE 3Ingredient%mg / CapsuleFunctionUltra-micronized30.77200.00ActiveProgesteroneMedium Chain65.93428.55Solubilizing AgentTriglyceride(MIGLYOL 812 orequivalent)Lauroyl polyoxyl-32-3.0019.50Suspending Agentglycerides (GELUCIRE44 / 14 or equivalent)Butylated0.031.95AntioxidantHydroxytolueneTotal100650

[0265]In various embodiments, amounts of MIGLYOL may be present in a range from about 35-95% by weight; GELUCIRE 44 / 14 from about 0.5-30% by weight; and BHT from about 0.01-0.1% by weight.

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Abstract

This disclosure provides progesterone formulations, methods of using these formulations, and their related pharmacokinetic parameters. In particular embodiments, the formulations disclosed herein allow for a reduction in the amount of progesterone administered to a patient in need thereof, while still providing the benefits of a larger dosage amount.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. Provisional Application 61 / 972,068 filed 28 Mar., 2014 and is a continuation in part of U.S. Ser. No. 14 / 125,547 filed 11 Dec., 2013 which is a National Stage application under 35 U.S.C. §371 of International Application Serial No. PCT / US2013 / 046442, entitled “PROGESTERONE FORMULATIONS” which was filed on 18 Jun., 2013, and claims priority to the following U.S. patent applications: U.S. Provisional Application Ser. No. 61 / 661,302, entitled “ESTRADIOL FORMULATIONS,” which was filed on Jun. 18, 2012; U.S. Provisional Application Ser. No. 61 / 662,265, entitled “PROGESTERONE FORMULATIONS,” which was filed on Jun. 20, 2012; U.S. patent application Ser. No. 13 / 684,002, entitled “NATURAL COMBINATION HORMONE REPLACEMENT FORMULATIONS AND THERAPIES,” which was filed Nov. 21, 2012; U.S. Patent Application Serial No. PCT / US2013 / 023309, entitled “TRANSDERMAL HORMONE REPLACEMENT THERAPIES,” which was filed Jan. 2...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/14A61K9/48A61K31/57
CPCA61K47/14A61K9/4825A61K31/57A61K9/4858
Inventor CACASE, JANICEPERSICANER, PETERTHORSTEINNSON, THORSTEINNSANCILLIO, FREDERICKAMADIO, JULIABERNICK, BRIAN
Owner THERAPEUTICSMD INC