ACYCLOVIR FORMULATIONS
The present invention relates to acyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
1 . A solid pharmaceutical composition comprising:
(a) SNAC;
(b) acyclovir; and
(c) a disintegrant,
wherein the SNAC and acyclovir are at least substantially dissolved within an hour of contact with an aqueous medium.
2 . The pharmaceutical composition of claim 1 , wherein the SNAC and acyclovir are completely dissolved in the aqueous medium.
3 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is simulated gastric fluid, simulated intestinal fluid, or both.
4 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is simulated gastric fluid.
5 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is simulated intestinal fluid.
6 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is gastric fluid, intestinal fluid, or both.
7 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is gastric fluid.
8 . The pharmaceutical composition of claim 1 , wherein the aqueous medium is intestinal fluid.
9 . The pharmaceutical composition of claim 1 , wherein the weight ratio of SNAC to acyclovir is from about 0.75:1 to about 6:1.
10 . The pharmaceutical composition of claim 9 , wherein the weight ratio of SNAC to acyclovir is from about 0.9:1 to about 4:1.
11 . The pharmaceutical composition of claim 10 , wherein the weight ratio of SNAC to acyclovir is about 1:1.
12 . The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition comprises from about 200 to about 1500 mg of acyclovir.
13 . The pharmaceutical composition of claim 12 , wherein the pharmaceutical composition comprises from about 240 to about 500 mg of acyclovir.
14 . The pharmaceutical composition of claim 12 , wherein the pharmaceutical composition comprises from about 240 to about 1000 mg of SNAC.
15 . The pharmaceutical composition of claim 12 , wherein the pharmaceutical composition comprises from about 480 to about 1000 mg of acyclovir.
16 . The pharmaceutical composition of claim 15 , wherein the pharmaceutical composition comprises from about 480 to about 2000 mg of SNAC.
17 . The pharmaceutical composition of claim 1 , wherein the disintegrant is selected from cross-linked N-vinyl-2-pyrrolidone (“CLPVP”), sodium starch glycolate, polacrilin potassium, sodium alginate, microcystalline or microtine cellulose, methyl cellulose, hydroxypropylcellulose, carboxymethyl cellulose sodium, and croscarmellose sodium and a combination of any of the foregoing.
18 . The pharmaceutical composition of claim 17 , wherein the disintegrant is croscarmellose sodium.
19 . The pharmaceutical composition of claim 1 , further comprising (d) one or more wetting agents.
20 . The pharmaceutical composition of claim 19 , wherein the wetting agent is selected from polyethylene glycol, sodium lauryl sulfate, mixtures of glycerol and polyethylene glycol, esters of long-fatty acids, mixtures of monoglycerides and diglycerides of capyrilic and capric acid in glycerol, polypropylene glycol monocaprylate, soyabean oil, propylene glycol mono caprylate, caprylocaproyl polyoxylglycerides, and polysorbate 80 and any combination of any of the foregoing.
21 . The pharmaceutical composition of claim 1 , further comprising:
(e) a binder; and
(f) a lubricant.
22 . The pharmaceutical composition of claim 21 , wherein the binder is selected from methyl cellulose, microcrystalline or microtine cellulose, hydroxypropylcellulose, hydroxypropyl methylcellulose, carboxymethylcellulose, povidone, polyvinyl alcohol, gelatin, cassien, glycerine, sorbitol, mannitol, sucrose, lactose, fructose, starch, corn starch, pregelatinized starch, amylose, dextrose, amylodextrin, maltodextrin, cyclodextin, gums and any combination of any of the foregoing.
23 . The pharmaceutical composition of claim 22 , wherein the binder is povidone.
24 . The pharmaceutical composition of claim 22 , wherein the binder is gelatin.
25 . The pharmaceutical composition of claim 22 , wherein the binder is a combination of povidone and pregelatinized starch.
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