PH12014000359A1 - Cinzotect - Google Patents
Cinzotect Download PDFInfo
- Publication number
- PH12014000359A1 PH12014000359A1 PH12014000359A PH12014000359A PH12014000359A1 PH 12014000359 A1 PH12014000359 A1 PH 12014000359A1 PH 12014000359 A PH12014000359 A PH 12014000359A PH 12014000359 A PH12014000359 A PH 12014000359A PH 12014000359 A1 PH12014000359 A1 PH 12014000359A1
- Authority
- PH
- Philippines
- Prior art keywords
- mupirocin
- skin
- zinc oxide
- ointment
- preparation
- Prior art date
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- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 abstract description 40
- MINDHVHHQZYEEK-UHFFFAOYSA-N (E)-(2S,3R,4R,5S)-5-[(2S,3S,4S,5S)-2,3-epoxy-5-hydroxy-4-methylhexyl]tetrahydro-3,4-dihydroxy-(beta)-methyl-2H-pyran-2-crotonic acid ester with 9-hydroxynonanoic acid Natural products CC(O)C(C)C1OC1CC1C(O)C(O)C(CC(C)=CC(=O)OCCCCCCCCC(O)=O)OC1 MINDHVHHQZYEEK-UHFFFAOYSA-N 0.000 abstract description 26
- 229960003128 mupirocin Drugs 0.000 abstract description 20
- 229930187697 mupirocin Natural products 0.000 abstract description 20
- 239000011787 zinc oxide Substances 0.000 abstract description 20
- DDHVILIIHBIMQU-YJGQQKNPSA-L mupirocin calcium hydrate Chemical compound O.O.[Ca+2].C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC([O-])=O)OC1.C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC([O-])=O)OC1 DDHVILIIHBIMQU-YJGQQKNPSA-L 0.000 abstract description 18
- 230000000844 anti-bacterial effect Effects 0.000 abstract description 17
- 238000002360 preparation method Methods 0.000 abstract description 15
- 239000002674 ointment Substances 0.000 abstract description 7
- 238000001035 drying Methods 0.000 abstract description 6
- 230000000845 anti-microbial effect Effects 0.000 abstract description 5
- 206010040882 skin lesion Diseases 0.000 abstract description 5
- 231100000444 skin lesion Toxicity 0.000 abstract description 5
- 239000000126 substance Substances 0.000 abstract description 5
- 238000000855 fermentation Methods 0.000 abstract description 4
- 230000004151 fermentation Effects 0.000 abstract description 4
- 208000015181 infectious disease Diseases 0.000 abstract description 4
- 150000002484 inorganic compounds Chemical class 0.000 abstract description 4
- 229910010272 inorganic material Inorganic materials 0.000 abstract description 4
- 230000029663 wound healing Effects 0.000 abstract description 4
- 241000192125 Firmicutes Species 0.000 abstract description 3
- 239000000654 additive Substances 0.000 abstract description 3
- 230000000996 additive effect Effects 0.000 abstract description 3
- 238000012423 maintenance Methods 0.000 abstract description 3
- 230000002209 hydrophobic effect Effects 0.000 abstract description 2
- 230000001681 protective effect Effects 0.000 abstract description 2
- 101100243022 Mus musculus Pcnt gene Proteins 0.000 abstract 2
- 230000009545 invasion Effects 0.000 abstract 2
- 241000589516 Pseudomonas Species 0.000 abstract 1
- 230000008030 elimination Effects 0.000 abstract 1
- 238000003379 elimination reaction Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 244000005700 microbiome Species 0.000 abstract 1
- 210000000056 organ Anatomy 0.000 abstract 1
- 230000001717 pathogenic effect Effects 0.000 abstract 1
- 206010040872 skin infection Diseases 0.000 abstract 1
- 230000009885 systemic effect Effects 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 10
- MINDHVHHQZYEEK-HBBNESRFSA-N mupirocin Chemical compound C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC(O)=O)OC1 MINDHVHHQZYEEK-HBBNESRFSA-N 0.000 description 8
- 230000000699 topical effect Effects 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 239000000203 mixture Substances 0.000 description 5
- KKMHFUKZHJOMJL-ZDACLCLWSA-N (+)-Pseudomonic acid C Natural products O=C(OCCCCCCCCC(=O)O)/C=C(\C[C@H]1[C@@H](O)[C@H](O)[C@H](C/C=C/[C@H]([C@@H](O)C)C)CO1)/C KKMHFUKZHJOMJL-ZDACLCLWSA-N 0.000 description 4
- RJGJFSVDQPCELW-VCXQKUNESA-N (e)-9-[(e)-4-[(2s,3r,4r,5s)-3,4-dihydroxy-5-[[(2s,3s)-3-[(2s,3s)-3-hydroxybutan-2-yl]oxiran-2-yl]methyl]oxan-2-yl]-3-methylbut-2-enoyl]oxynon-4-enoic acid Chemical compound C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCC\C=C\CCC(O)=O)OC1 RJGJFSVDQPCELW-VCXQKUNESA-N 0.000 description 4
- JGKQAKOVZJHZTF-LHSFDMIQSA-N 9-[(e)-3-methyl-4-[(2s,3r,4s,5r)-3,4,5-trihydroxy-5-[[(2s,3s)-3-[(2s,3s)-3-hydroxybutan-2-yl]oxiran-2-yl]methyl]oxan-2-yl]but-2-enoyl]oxynonanoic acid Chemical compound C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@]1(O)[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC(O)=O)OC1 JGKQAKOVZJHZTF-LHSFDMIQSA-N 0.000 description 4
- KKMHFUKZHJOMJL-WZLBZGCNSA-N 9-[(e)-4-[(2s,3r,4r,5s)-3,4-dihydroxy-5-[(e,4r,5s)-5-hydroxy-4-methylhex-2-enyl]oxan-2-yl]-3-methylbut-2-enoyl]oxynonanoic acid Chemical compound C[C@H](O)[C@H](C)\C=C\C[C@H]1CO[C@@H](C\C(C)=C\C(=O)OCCCCCCCCC(O)=O)[C@H](O)[C@@H]1O KKMHFUKZHJOMJL-WZLBZGCNSA-N 0.000 description 4
- 201000004624 Dermatitis Diseases 0.000 description 4
- 208000035874 Excoriation Diseases 0.000 description 4
- RJGJFSVDQPCELW-IZCYIFJBSA-N Pseudomonic D Natural products O=C(OCCCC/C=C/CCC(=O)O)/C=C(\C[C@H]1[C@H](O)[C@H](O)[C@@H](C[C@H]2[C@@H]([C@H]([C@@H](O)C)C)O2)CO1)/C RJGJFSVDQPCELW-IZCYIFJBSA-N 0.000 description 4
- JGKQAKOVZJHZTF-LMLZBOKOSA-N Pseudomonic acid B Natural products O=C(OCCCCCCCCC(=O)O)/C=C(\C[C@H]1[C@H](O)[C@H](O)[C@@](O)(C[C@H]2[C@@H]([C@H]([C@@H](O)C)C)O2)CO1)/C JGKQAKOVZJHZTF-LMLZBOKOSA-N 0.000 description 4
- KKMHFUKZHJOMJL-UHFFFAOYSA-N Pseudomonic acid C Natural products CC(O)C(C)C=CCC1COC(CC(C)=CC(=O)OCCCCCCCCC(O)=O)C(O)C1O KKMHFUKZHJOMJL-UHFFFAOYSA-N 0.000 description 4
- 206010052428 Wound Diseases 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- RJGJFSVDQPCELW-UHFFFAOYSA-N pseudomonic acid D Natural products CC(O)C(C)C1OC1CC1C(O)C(O)C(CC(C)=CC(=O)OCCCCC=CCCC(O)=O)OC1 RJGJFSVDQPCELW-UHFFFAOYSA-N 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 241000589540 Pseudomonas fluorescens Species 0.000 description 3
- 241000191940 Staphylococcus Species 0.000 description 3
- 241000194017 Streptococcus Species 0.000 description 3
- 230000003385 bacteriostatic effect Effects 0.000 description 3
- 206010007247 Carbuncle Diseases 0.000 description 2
- 241000606161 Chlamydia Species 0.000 description 2
- 206010012444 Dermatitis diaper Diseases 0.000 description 2
- 208000003105 Diaper Rash Diseases 0.000 description 2
- 241000233866 Fungi Species 0.000 description 2
- 206010017553 Furuncle Diseases 0.000 description 2
- 101000599951 Homo sapiens Insulin-like growth factor I Proteins 0.000 description 2
- 206010021531 Impetigo Diseases 0.000 description 2
- 206010021639 Incontinence Diseases 0.000 description 2
- 208000006877 Insect Bites and Stings Diseases 0.000 description 2
- 102100037852 Insulin-like growth factor I Human genes 0.000 description 2
- 102000029793 Isoleucine-tRNA ligase Human genes 0.000 description 2
- 108700040464 Isoleucine-tRNA ligases Proteins 0.000 description 2
- 102000002274 Matrix Metalloproteinases Human genes 0.000 description 2
- 108010000684 Matrix Metalloproteinases Proteins 0.000 description 2
- 206010034133 Pathogen resistance Diseases 0.000 description 2
- 241000191967 Staphylococcus aureus Species 0.000 description 2
- 241000193996 Streptococcus pyogenes Species 0.000 description 2
- 208000002847 Surgical Wound Diseases 0.000 description 2
- 208000025865 Ulcer Diseases 0.000 description 2
- 208000027418 Wounds and injury Diseases 0.000 description 2
- UGUYQBMBIJFNRM-OQFOIZHKSA-N [(z)-but-2-en-2-yl]benzene Chemical compound C\C=C(\C)C1=CC=CC=C1 UGUYQBMBIJFNRM-OQFOIZHKSA-N 0.000 description 2
- 238000005299 abrasion Methods 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 239000004599 antimicrobial Substances 0.000 description 2
- 208000010668 atopic eczema Diseases 0.000 description 2
- 230000004888 barrier function Effects 0.000 description 2
- 229940000425 combination drug Drugs 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 210000002615 epidermis Anatomy 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 230000036737 immune function Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 230000000394 mitotic effect Effects 0.000 description 2
- 150000002924 oxiranes Chemical class 0.000 description 2
- 230000035790 physiological processes and functions Effects 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 238000001243 protein synthesis Methods 0.000 description 2
- 229930194369 pseudomonic acid Natural products 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- 230000014616 translation Effects 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- 241001148471 unidentified anaerobic bacterium Species 0.000 description 2
- 230000009471 action Effects 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000036039 immunity Effects 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The skin is the largest organ of the body is subjected to different conditions that threaten its integrity - pathogenic invasion and other circumstances. The elimination of these skin infections and the maintenance of skin integrity, thus, are paramount importance against the invasion of microorganism and setting in of more serious and systemic infections. Hence, we created a fixed dose ointment preparation that contains Mupirocin 2 pcnt and zinc oxide 10 pcnt . Mupirocin is a natural antibacterial produced from the fermentation of bacteria Pseudomonas flourescens that has an antimicrobial activity against gram positive bacteria. Zinc oxide is an inorganic compound appearing as a white powdery substance that is used as an additive to dermatological preparations for its drying and antibacterial properties. When Mupirocin and Zinc Oxide are combined together they exhibit enhanced bactericidal and protective effect. The combination of these two targets to eliminate susceptible infections and promote re-epitherlialization to hasten the wound healing process. The ointment was chosen as the vehicle for this dermatological preparation owning the hydrophobic characteristic of the two components. This will render greater miscibility between the two. The ointment is also desired since it adheres to both dry and wet surfaces and gives better occlusion, considering the nature of skin lesions for which the preparation is indicated.
Description
CINZOTECT a) A brief statement of its nature and purposes
Mupirocin is a naturally-occurring antibiotic obtained from fermentation of the bacteria
Pseudomonas fluorescens. It is both bacteriostatic and bactericidal at appropriate concentrations to susceptible organisms of the Staphylococcus and Streptococcus genera.
These organisms are found on the skin and commonly infect skin lesions. Mupirocin was approved for use as a topical preparation by the US FDA in 1987 and as an intranasal formulation in 1995. It is currently available in the local market under various trade names.
Zinc Oxide is an inorganic compound commonly added in dermatological preparations for its drying and anti-bacterial properties. More recent and comprehensive studies have shown that zinc oxide is an important cofactor for the activity of numerous enzymes needed for bodily functions such as immunity and wound healing.
The ointment was chosen as the vehicle for this dermatological preparation owing to the hydrophobic characteristic of the two components. This will render greater miscibility between the two. The ointment is also desired since it adheres to both dry and wet surfaces and gives better occlusion, considering the nature of skin lesions for which the preparation is indicated. b) Complete and detailed enabling description
MUPIROCIN
Mupirocin is a natural antibacterial produced from fermentation of the bacteria Pseudomonas fluorescens. Its chemical formula is C2sHa4Os and its IUPAC name is 9-[(E)-4-[(2S,3R,4R,5S)- 3,4-dihydroxy-5-[[(2S,3S)-3- [(2S,3S)-3-hydroxybutan-2-yljoxiran-2-yljmethyl] oxan-2-yl}-3- methylbut-2-enoylJoxynonanoic acid.
It is a mixture of several pseudomonic acids. At least 90% of this mixture is characterized as
Pseudomonic acid A (PA-A). The remaining acids are characterized as: Pseudomonic acid B (PA-B) with an additional hydroxyl group at C8; Pseudomonic acid C (PA-C) with a double bond between C10 and C11, instead of the epoxide of PA-A; and Pseudomonic acid D (PA-D) with a double bond at C4" and C5’ in the 9-hydroxy-nonanoic acid portion of mupirocin.
: ACTION
Topical Antibacterial
MECHANISM OF ACTION
Mupirocin is bacteriostatic at low concentrations and bactericidal at high concentrations.
However, it is possible to achieve these bactericidal concentrations with topical preparations.
Mupirocin is able to inhibit protein synthesis by binding to the isoleucyl t-RNA synthetase in Staphylococcus and Streptococcus bacteria. There is no in vitro cross-resistance with other antimicrobials and resistance is rare.
Its antimicrobial activity has been proven against the following Gram-positive bacteria:
Staphylococcus aureus, Streptococcus pyogenes (Group A beta-hemolytic), Staph. epidermidis and Staph. Saphrophyticus. It is also active against some Gram-negative bacteria but has no antimicrobial activity against anaerobic bacteria, Chlamydia and fungi.
INDICATIONS AND USAGE
Mupirocin is used to treat primarily and secondarily infected skin lesions by susceptible organisms such as impetigo, furuncles, carbuncles, open wounds, dermatoses, abrasions, insect bites, minor cuts, minor burns, ulcers and for the prevention of infection in suture wounds.
ZINC OXIDE
Zinc oxide is an inorganic compound appearing as a white powdery substance.
Zinc Oxide is used as an additive to dermatological preparations for its drying and antibacterial properties. It also becomes an effective barrier on the skin as it is not absorbed readily by the skin.
ACTIONS
Enhances re-epithelialization, drying, antibacterial
MECHANISM OF ACTION
Zinc Oxide has been shown to be an important cofactor in the activity of more than 300 enzymes in the body which, in tum, are necessary for maintaining and enhancing immune functions and other physiological processes as re-epithelization in wound healing. Specifically, zinc oxide has been shown to upregulate factors such as Insulin-like Growth Factor-1 and the activity of matrix metalloproteinase enzymes needed to induce the mitotic activity of cells in the basal layer of the epidermis.
: INDICATIONS AND USAGE
Zinc oxide in topical preparations may be applied to minor bums, cuts, incontinence- associated dermatitis (or diaper rash) or where protection of the skin and maintenance of skin integrity is desired in those with chafing, chapping, excoriations, eczema, ostomy sites and surgical wounds. d) Distinct and explicit claims we seek to be protected e Brand Name:
Cinzotect ¢ Fixed dose combination:
Per gram ointment contains:
Mupirocin : 20 mg (2%)
Zinc Oxide : 100 mg (10%) ¢ Therapeutic Claims:
This pharmaceutical preparation, Mupirocin and Zinc Oxide, falls under fixed dose combination, which is pharmaceutically and pharmacologically compatible. They exhibit enhanced bactericidal and protective effect when combined together.
Rcergy or rag,
CINZOTECT . = 1
A Fixed Dose Ointment Preparation Containing Mupirocin and Zin¢ Oxide 5 A - (Cinzotect) for Treatment of Skin Lesions ip:
I. Complete and detailed enabling description - )
Ft {
MUPIROCIN co] 1. Mupirocin is a natural antibacterial produced from fermentation of the bacteria Pseudomonas fluorescens. Its chemical formula is
CHO, and its IUPAC name is 9-[(E)-4-[(2S,3R,4R,55)-3,4- ~ ] dihydroxy-5-[[(25,35)-3- [(2S,35)-3-hydroxybutan-2-ylloxiran-2- = yllmethyl] oxan-2-yl]-3-methylbut-2-enoyl]Joxynonanoic acid. 2. It is a mixture of several pseudomonic acids. At least 90% of this mixture is characterized as Pseudomonic acid A (PA-A). The ! remaining acids are characterized as: Pseudomonic acid B (PA-B) with an additional hydroxyl group at C8; Pseudomonic acid C (PA-C) with a double bond between C10 and C11, instead of the epoxide of
PA-A; and Pseudomonic acid D (PA-D) with a double bond at C4" and C5" in the 9-hydroxy-nonanoic acid portion of mupirocin. 3. Mupirocin is bacteriostatic at low concentrations and bactericidal at high concentrations. However, it is possible to achieve these bactericidal concentrations with topical preparations. Mupirocin is able to inhibit protein synthesis by binding to the isoleucyl t-RNA synthetase in Staphylococcus and Streptococcus bacteria. There is ] no in vitro cross-resistance with other antimicrobials and resistance is rare. 4. Its antimicrobial activity has been proven against the following
Gram-positive bacteria: Staphylococcus aureus, Streptococcus pyogenes (Group A beta-hemolytic),Staph. epidermidis and Staph.
Saphrophyticus. It is also active against some Gram-negative ] bacteria but has no antimicrobial activity against anaerobic bacteria,
Chlamydia and fungi.
er 2 5. PURPOSE: It used to treat primarily and secondarily infected skin - "lesions by susceptible organisms such as impetigo, furuncles, carbuncles, open wounds, dermatoses, abrasions, insect bites, minor cuts, minor burns, ulcers and for the prevention of infection in © suture wounds. ie
ZINC OXIDE co 1. Zinc oxide is an inorganic compound appearing as a white powdery = substance. =
Li 1 2. Zinc Oxide is used as an additive to dermatological preparations for - its drying and antibacterial properties. It also becomes an effective barrier on the skin as it is not absorbed readily by the skin. 3. Enhances re-epithelialization, drying, antibacterial. 4. Zinc Oxide has been shown to be an important cofactor in the activity of more than 300 enzymes in the body which, in turn, are necessary for maintaining and enhancing immune functions and other physiological processes as re-epithelization in wound healing.
Specifically, zinc oxide has been shown to upregulate factors such as
Insulin-like Growth Factor-1 and the activity of matrix metalloproteinase enzymes needed to induce the mitotic activity of cells in the basal layer of the epidermis. 5. Zinc oxide in topical preparations may be applied to minor burns, cuts, incontinence-associated dermatitis (or diaper rash) or where protection of the skin and maintenance of skin integrity is desired in those with chafing, chapping, excoriations, eczema, ostomy sites and surgical wounds.
II. Distinct and explicit claims we seek to be protected 1. The unique combination of Mupirocin 20mg (2%) and Zinc Oxide 100 mg (10%).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PH12014000359A PH12014000359A1 (en) | 2014-12-01 | 2014-12-01 | Cinzotect |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PH12014000359A PH12014000359A1 (en) | 2014-12-01 | 2014-12-01 | Cinzotect |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PH12014000359A1 true PH12014000359A1 (en) | 2016-07-11 |
Family
ID=57908429
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12014000359A PH12014000359A1 (en) | 2014-12-01 | 2014-12-01 | Cinzotect |
Country Status (1)
| Country | Link |
|---|---|
| PH (1) | PH12014000359A1 (en) |
-
2014
- 2014-12-01 PH PH12014000359A patent/PH12014000359A1/en unknown
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