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Tranexamic acid formulations

a technology of tranexamic acid and formulation, which is applied in the direction of drug composition, extracellular fluid disorder, biocide, etc., can solve the problems of nausea, vomiting, diarrhea, nausea, and cramping, and achieve the effect of reducing the concentration of tranexamic acid, and reducing the undesirable gastrointestinal side effects

Inactive Publication Date: 2005-11-03
AMRING PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention is directed to a modified release oral dosage form of tranexamic acid which is suitable for administration on a two or three times a day basis. The modified release formulation minimizes or eliminates the undesirable gastrointestinal side effects associated with oral tranexamic acid therapy, such as nausea and diarrhea, while maintaining or improving its therapeutic effect. The modified release oral dosage form provides a controlled release of tranexamic acid that prevents a bolus of tranexamic acid from being introduced in the stomach, reducing the concentration of tranexamic acid in the stomach contents and improving patient compliance with therapy. The invention also provides a method of treating patients with heavy menstrual bleeding using the modified release oral dosage form."

Problems solved by technology

However, this treatment may cause adverse gastrointestinal reactions, including nausea, vomiting, diarrhea, and cramping, etc.
These gastrointestinal side effects are due to the quantity of tranexamic acid and / or rapid rate of release of tranexamic acid into the stomach with each dose, as well as the large quantity of excipients used in the tablet formulation that are introduced into the stomach.
Such side effects, in addition to the cramping, bloating, pain, and other symptoms that may accompany menses, are undesirable, and a formulation of tranexamic acid is needed which will reduce or eliminate these side effects.

Method used

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Examples

Experimental program
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Effect test

example 1

[0097] Modified release 650 mg tranexamic acid tablets were prepared having the ingredients listed in the Table 1 below:

TABLE 1QuantityQuantityper batchper tabletIngredient(kg)(mg)Active IngredientTranexamic Acid, EP84.50650.0Inactive IngredientsMicrocrystalline Cellulose NF (Avicel PH 101)5.75344.25Colloidal Silicon Dioxide NF0.09750.75Pregelatinized Corn Starch, NF6.43549.50Hypromellose, USP (Methocel K3 Premium LV)19.110147.00Povidone, USP (K value range 29-32)4.68036.00Stearic Acid, NF (powder)2.34018.00Magnesium Stearate, NF (powder)0.5854.50Purified Water USP*17.550135.00

*Purified water is removed during processing

The formulation of Example 1 was prepared as follows: [0098] 1. Weigh all ingredients and keep in moisture resistant containers until ready for use. [0099] 2. Measure water into a container. Mix povidone at medium speed until completely dissolved. [0100] 3. Add tranexamic acid, microcrystalline cellulose (MCC), pregelatinized corn starch, and colloidal silicon di...

example 2

[0110] In Example 2, immediate release 650 mg tranexamic acid tablets were prepared having the ingredients listed in Table 2 below:

TABLE 2Quantityper batchQuantity perIngredient(kg)tablet (mg)Active IngredientTranexamic Acid, EP (650 mg / tab)84.50650.0Inactive IngredientsMicrocrystalline Cellulose, NF5.75344.25(Avicel PH 101)Microcrystalline Cellulose, NF10.66082.00(Avicel PH 102)Colloidal Silicon Dioxide, NF0.09750.75Pregelatinized Corn Starch, NF6.43549.50Croscarmellose Sodium, NF19.5015.00Povidone, USP (K value range 29-32)4.68036.00Stearic Acid, NF (powder)2.34018.00Magnesium Stearate, NF (powder)0.5854.50Purified Water, USP*17.550135.00Film Coating (Inactive Ingredients)**Opadry White YS-1-70034.110—Purified Water, USP36.990—

*Purified water is removed during processing

**6 kg excess prepared to account for losses during transfer

The formulation of Example 2 was prepared as follows: [0111] 1. Weigh all ingredients and keep in moisture resistant containers until ready for use. ...

example 3

[0124] In Example 3, modified release 650 mg tranexamic acid tablets were prepared as in Example 1 and coated with a film coating similar to the immediate release tablets of Example 2. The ingredients are listed in Table 3 below:

TABLE 3QuantityQuantityper batchper tabletIngredient(kg)(mg)Active IngredientTranexamic Acid, EP84.50650.0Inactive IngredientsMicrocrystalline Cellulose NF (Avicel PH 101)5.75344.25Colloidal Silicon Dioxide NF0.09750.75Pregelatinized Corn Starch, NF6.43549.50Hypromellose, USP (Methocel K3 Premium LV)19.110147.00Povidone, USP (K value range 29-32)4.68036.00Stearic Acid, NF (powder)2.34018.00Magnesium Stearate, NF (powder)0.5854.50Purified Water USP*17.550135.00Film Coating (Inactive Ingredients)**Opadry White YS-1-70034.305—Purified Water, USP38.750—

*Purified water is removed during processing

**6 kg excess prepared to account for losses during transfer

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Abstract

Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith.

Description

[0001] This application claims priority from U.S. Provisional Application No. 60 / 550,113, filed Mar. 4, 2004, and U.S. Provisional Application No. 60 / 592,885, filed Jul. 30, 2004, the disclosures of which are both hereby incorporated by reference in their entireties.FIELD OF THE INVENTION [0002] The invention is directed to modified release oral tranexamic acid formulations that preferably minimize or eliminate undesirable side effects and methods of treatment with these formulations. BACKGROUND OF THE INVENTION [0003] Tranexamic acid (trans-4-(aminomethyl)cyclohexanecarboxylic acid, Cyklokapron® (Pfizer) is an antifibrinolytic agent. That is, it helps to prevent lysis or dissolution of a fibrin clot which forms in the normal physiologic process of hemostasis. Its mechanism of action is as a competitive inhibitor of plasminogen activation, and as a noncompetitive inhibitor of plasmin; both plasminogen and plasmin are activators of fibrinolysis and active clot-lysing agents. Tranexam...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K9/22A61K31/19
CPCA61K9/2027A61K9/2054A61K31/19A61K31/196A61K31/195A61K9/2009A61K9/2013A61K9/2059Y10S514/951A61P15/00A61P7/04
Inventor MOORE, KEITH A.HEASLEY, RALPH A.GREIWE, JEFFREY S.
Owner AMRING PHARM INC
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