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

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

US20050244495A1Inactive Publication Date: 2005-11-03AMRING PHARM INC +1
10 Cites 31 Cited by

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Tranexamic acid formulations
  • Tranexamic acid formulations
  • Tranexamic acid formulations

Examples

Experimental program
Comparison scheme
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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
weightaaaaaaaaaa
concentrationaaaaaaaaaa
mean transit timeaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
03 Nov 2005
Publication
US20050244495A1
IPC
A61K9/20; A61K9/22; A61K31/19
CPC
A61K9/2027; A61K9/2054; A61K31/19; A61K31/196; A61K31/195; A61K9/2009; A61K9/2013; A61K9/2059
Inventors
MOORE, KEITH A.; HEASLEY, RALPH A.