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Formulations of conjugated estrogens and bazedoxifene

A technology of bazedoxifene and estrogen, which is applied in the field of preparations of conjugated estrogens and bazedoxifene, and can solve problems such as unclear effects of non-antagonistic estrogens

Inactive Publication Date: 2008-08-27
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect of unopposed estrogens on breast tissue is less clear, but there is some concern

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0157] Preparation containing conjugated estrogen / bazedoxifene acetate

[0158] 0.45mg / 10mg tablet operation method

[0159] A. Preparation of 10% w / w hydroxypropyl methylcellulose, USP, 2910, 3cps stock solution.

[0160] 1. Place 900 g of purified water, USP, into a container fitted with a low shear (Lightnin type) mixer.

[0161] 2. Add 100 g of Hydroxypropyl Methylcellulose, USP, 2910, 3 cps. in small increments to the vortex created in the water by the moderate agitation of step 1.

[0162] 3. Continue stirring for a minimum of 1 hour or until all of the hydroxypropylmethylcellulose, USP, 2910, 3 cps. is dissolved.

[0163] 4. If necessary, add purified water USP to the total theoretical weight.

[0164] B1. Preparation of bazedoxifene acetate filler coating suspension:

[0165] 1. Place 428.30 g of purified water, USP, into a vessel equipped with a low shear (Lightnin type) and high shear (Silverson type) mixer.

[0166] 2. With the Lightnin type mixer turned on, he...

Embodiment 2

[0209] Process for preparing tablets containing conjugated estrogens / bazedoxifene acetate 0.45 mg / 20 mg

[0210] The method of operation is basically as described in Example 1, the difference is:

[0211] a) The color coating suspension contains:

[0212] 125.00g Opadry White YS-1-18202A;

[0213] 875.00g purified water, USP; and

[0214] b) The transparent coating suspension contains:

[0215] 50.00g Opadry Clear YS-2-19114A;

[0216] 950.00g Purified Water, USP; and

[0217] c) Use the following tablet coating procedure:

[0218] 1. Fill Premarin(R) 0.45 mg talc-free die-cast fill tablets into a perforated coating pan.

[0219] 2. Add enough bazedoxifene acetate filler coat suspension to achieve a total weight of 100 mg (± 2 mg) on ​​the inert tablet fill weight (approximately 489.8 mg bazedoxifene acetate filler coat mix per tablet). suspension). The tablets were coated with this suspension using the continuous sugar coating technique as described in Example 1.

[...

Embodiment 3

[0228] Process for preparing tablets containing conjugated estrogens / bazedoxifene acetate 0.45 mg / 40 mg

[0229] The method of operation is basically as described in Example 1, the difference is:

[0230] a) The color coating suspension contains:

[0231] 125.00g Opadry White YS-1-18202A;

[0232] 875.00g purified water, USP; and

[0233] b) The transparent coating suspension contains:

[0234] 50.00g Opadry Clear YS-2-19114A;

[0235] 950.00g Purified Water, USP; and

[0236] c) Use the following tablet coating procedure:

[0237] 1. Fill Premarin(R) 0.45 mg talc-free die-cast fill tablets into a perforated coating pan.

[0238] 2. Add enough bazedoxifene acetate filler coat suspension to achieve a total weight of 200 mg (± 2 mg) on ​​the inert tablet fill weight (approximately 979.6 mg bazedoxifene acetate filler coat mix per tablet). suspension). The tablets were coated with this suspension using the continuous sugar coating technique as described in Example 1.

[...

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PUM

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Abstract

The present invention relates to solid dosage formulations containing conjugated estrogens and bazedoxifene, or a salt thereof. In some embodiments, the compositions include a core comprising conjugated estrogens, and at least one coating that comprises bazedoxifene, or a salt thereof.

Description

[0001] This application claims priority to US Provisional Application Serial No. 60 / 694,889, filed June 29, 2005, the entire contents of which are incorporated herein by reference. technical field [0002] The present invention relates to a solid preparation containing conjugated estrogens and bazedoxifene or a salt thereof. In some embodiments, the composition comprises a core comprising a conjugated estrogen and a coating comprising bazedoxifene or a salt thereof. Background technique [0003] Hormone replacement therapy has been used well before to prevent bone loss in postmenopausal women. Standard protocols call for the use of estrone, estriol, ethinyl estradiol, or conjugated estrogens isolated from natural sources (ie, Premarin® from Wyeth-Ayerst). ((R) conjugated estrogens) for estrogen supplementation. In some patients, this treatment is not possible due to the proliferative effect of non-antagonistic estrogens (estrogens not used in combination with progesterone)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/565A61K31/55
CPCA61K31/565A61K9/209A61K31/55A61P15/12A61P19/10A61P5/30A61K9/20
Inventor R·S·查特拉巴利A·纳吉L·范佩尔特
Owner WYETH LLC
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